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Aphrodisiac properties of Tribulus Terrestris extract (Protodioscin) in normal and castrated rats
Abstract
Tribulus terrestris (TT) has long been used in the traditional Chinese and Indian systems of medicine for the treatment of various ailments and is popularly claimed to improve sexual functions in man. Sexual behaviour and intracavernous pressure (ICP) were studied in both normal and castrated rats to further understand the role of TT containing protodioscin (PTN) as an aphrodisiac. Adult Sprague-Dawley rats were divided into five groups of 8 each that included distilled water treated (normal and castrated), testosterone treated (normal and castrated, 10 mg/kg body weight, subcutaneously, bi-weekly) and TT treated (castrated, 5 mg/kg body weight, orally once daily). Decreases in body weight, prostate weight and ICP were observed among the castrated groups of rats compared to the intact group. There was an overall reduction in the sexual behaviour parameters in the castrated groups of rats as reflected by decrease in mount and intromission frequencies (MF and IF) and increase in mount, intromission, ejaculation latencies (ML, IL, EL) as well as post-ejaculatory interval (PEI). Compared to the castrated control, treatment of castrated rats (with either testosterone or TT extract) showed increase in prostate weight and ICP that were statistically significant. There was also a mild to moderate improvement of the sexual behaviour parameters as evidenced by increase in MF and IF; decrease in ML, IL and PEI. These results were statistically significant. It is concluded that TT extract appears to possess aphrodisiac activity probably due to androgen increasing property of TT (observed in our earlier study on primates).
... For example, alkaloids have ergogenic properties which induce vasodilation of the blood vessels, consequently resulting in erection" [23,24], and "saponin was reported to possess sexual enhancing properties by inducing the relaxation of smooth muscle Corpus cavernosum through the L-arginine/nitric oxide pathway" [25]. "Flavonoids, a constituent of the plant extract, with an antioxidant property have been reported to alter androgen levels in animals, thereby contributing to aphrodisiac effect" [26]. "It is a fact that an androgen, which may act both centrally and peripherally, induces sexual behaviour and erection" [27]. ...
... "It is a fact that an androgen, which may act both centrally and peripherally, induces sexual behaviour and erection" [27]. "The sexual behaviours of the male rats in this study may be due to the androgenic and gonadotropic activities of the extract, which could rationally be attributed to the flavonoid and saponin constituents of the plant, reported to alter androgen levels" [26]. "Furthermore, the steroidal nature of saponins may have facilitated its role as an intermediary in the steroidal pathway of androgen production" [28]. ...
... "It is, therefore, possible that through different mechanisms the extract might have crossed the blood-brain barrier of the animals to exert its aphrodisiac effect on the hypothalamicpituitary-testicular axis" [28]. Aphrodisiacs are substances which can stimulate sexual desire or libido [26] and can as well be used to revise impaired sexual functions [8]. In the male rats (active, sluggish, and impotent), the extract produced a clear modification in their sexual behaviours by causing a dose-dependent decrease in mount latency, intromission latency and post ejaculation latency and a dose-related increase in ejaculation latency, mount frequency, intromission frequency, and penile erection. ...
Aims: In this study, the methanol extract of Homalium letestui root was investigated with a view to ascertaining the scientific basis for its ethnobotanical use, and establishing, if any, the mechanisms of its effects, as an aphrodisiac. Methodology: The crushed root of Homalium letestui was soaked in methanol for 72h and filtered with Whatman paper No.4; the extract was stored at -4oC. Mature male rats were divided into three groups (active, sluggish, and impotent) and administered with various doses of the extract. The rats were, thereafter, observed for the following: mount latency, intromission latency, ejaculation latency, post ejaculation latency, mount frequency, intromission frequency, erection frequency, and penile erection latency. Results: The result showed that the Homalium letestui root extract (n-butanol, dichloromethane, ethyl acetate, petroleum ether and aqueous fractions) caused and maintained erection in the subjects, and their effects on the rats were dose-dependent and statistically significant (p<0.05-0.001). In addition, the aphrodisiac properties of the Homalium letestui root may in part be predicated on the properties of its phytochemical constituents which include alkaloids, saponins, flavonoids, tannins and cardiac glycosides. Conclusion: These findings, therefore, justify the Homalium letestui root’s folkloric use as a sexual performance enhancer and demonstrate that the plant possesses aphrodisiac properties.
... TT contains the steroidal saponins, mainly protodioscin, prototribestin and other important ingredients such as alkaloids, flavonoids, terpenoids, and phenol carboxylic acid. TT extracts have been found to improve sperm parameters, sex hormonal profile, and libido by some studies [11,[14][15][16][17][18], while others have reported its adverse effects [19][20][21]. Meanwhile, in some human clinical trials, TT showed no impact on the seminal parameters ( [22][23][24]. ...
... The shortlisted studies included five human clinical trials evaluating the therapeutic effect [10,25,27,33,34], of which two were randomized trials [25,27] and three were nonrandomized trials [10,33,34]. Five animal studies evaluated the preventive effect of TT against various fertility-compromising agents [35][36][37][38][39], ten evaluated the therapeutic effect of TT in model organisms [9,11,15,18,[40][41][42][43][44][45], and eighteen studies administered TT in normal animals to evaluate improvements in semen parameters, hormone levels, and its aphrodisiac effect [9,16,17,20,36,37,39,40,42,43,[45][46][47][48][49][50][51][52] (Table 2). ...
... Tribulus terrestris L. Improves the Mounting Frequency (MF). Pooled analysis including four datasets from two therapeutic studies [15,18] showed significant heterogeneity (Q = 39:418, I 2 = 92:389, p = 0:001), suggesting the use of the random effects model for inference. The pooled effect size estimate showed significant improvement in MF upon TT administration (Hedges' g = 7:355, 95% CI = 2:456 to 12.255, p = 0:003; Figure 9). ...
Tribulus terrestris L. (TT) is a traditional medicinal plant, which belongs to the Zygophyllaceae family. TT extracts have been widely used for diuretic, analeptic, aphrodisiac, and profertility properties. To quantitatively evaluate the profertility and aphrodisiac effects of Tribulus terrestris L., we undertook the present meta-analyses on published data. A thorough literature screening was performed to identify articles evaluating the effect of TT on spermatogenesis, male fertility, reproductive, and aphrodisiac parameters. We shortlisted 30 relevant studies conducted on humans and rodents. Meta-analyses were conducted to evaluate the quantitative impact of TT on various fertility parameters. In case of humans, the pooled analysis on 133 subjects showed significant improvements in sperm concentration (SDM = 0:624, 95% CI = 0:13 to 1.117, p = 0:013) and sperm motility (SDM = 0:742, 95% CI = 0:331 to 1.152, p = 0:001). TT resulted in nonsignificant increases in testosterone and LH and a nonsignificant decrease in FSH. Similar to the above, TT improved sperm count, sperm motility, and sperm viability in rodents with normal or compromised fertility. The effect on hormone levels was less credible with frequent variations across studies and animal models. The aphrodisiac activity was studied in castrated animal models or normal rodents, both of which showed significant improvements in mounting frequency and intromission frequency and significant declines in mounting latency and intromission latency. These meta-analyses suggested that TT possesses profertility and aphrodisiac activities.
... The increase caused by the extract could be attributed to the presence of saponins which help in improving testosterone levels and flavonoid which improves androgen levels. [16] Male fertility in mammals is regulated by the two adenohypophyseal gonadotropic hormones: Luteinizing hormone (LH) and Follicle stimulating hormone (FSH). Follicle stimulating hormone stimulates the production of spermatogonia to spermatocytes and also maintains the spermatogenic process. ...
... These findings agree with the studies on the fertility effects of other plant extract (Allium sativum) by other researchers [14] who reported that saponins, flavonoids, alkaloids and tannins present in plant extracts have the capability of increasing the body's natural Testosterone, LH and FSH levels. According to another group of researchers, [16] LH which is released by the pituitary gland helps to maintain testosterone levels. This therefore means that the increase in Luteinizing hormone level may be responsible for the increase in testosterone concentration which enhances male fertility. ...
... The reversal pattern in the serum concentrations of LH and Testosterone supports earlier reports that Luteinizing Hormone being released by the pituitary gland helps to maintain testosterone levels, such that as the serum concentration of LH increases, the serum concentration of Testosterone also increases and vice versa. [16] This result therefore suggests that to achieve the desired effect of the extract on male reproductive hormones, the extract has to be consumed in a reasonably large quantity. ...
The article is about the effect of the hydroethanolic leaf extract of Solanum aethiopicum on the concentration of reproductive hormones in male Wistar rats.
... Reducing in sperm quality can cause extinction or loss of populations. The literature reported that TT has been increased the number and motility of spermatozoa in human (Salgado et al., 2016;Khaleghi et al., 2017) and animals (rat, mice, mouse) (Gauthaman et al., 2002;Singh et al., 2012;Adaay and Mattar, 2012;Oliveira et al., 2015;Kumari and Singh, 2015;Kumar and Singh, 2015). Thus far, there is limited information about influences of TT supplementation on sperm motility. ...
... The positive roles of TT on various diseases and disorders have been emphasized in previous studies owing to its aphrodisiac and free-radicalscavenging properties (Singh et al., 2012;Hammoda et al., 2013;Keshtmand et al., 2014;Neychev and Mitev, 2016;Fernández-Lázaro et al., 2022). Even though there are no references on the use of TT as an agent for improving fish spermatozoa capacity during activation, the literature reported that TT has been increased the number and motility of spermatozoa in human and animals (rat, mice, mouse) (Gauthaman et al., 2002;Liu et al., 2004;Singh et al., 2012;Adaay and Mattar, 2012;Oliveira et al., 2015;Kumari and Singh, 2015;Kumar and Singh, 2015;Khaleghi et al., 2016;Salgado et al., 2016). The present results are going in line with previous studies in human and animals. ...
Tribulus terrestris (TT) is a famous traditional plant of family Zygophyllaceae and widely distributes around the world. TT has potential to elevate the testosterone, testosterone precursor and luteinizing hormone levels. In this study, trials were conducted to assessment the impact of Tribulus terrestris addition on sperm motility of rainbow trout (Oncorhynchus mykiss) for the first time. In the trial, we used to different concentrations [0 µg L-1 (Control), 200 µg L-1, 400 µg L-1, 600 µg L-1, 800 µg L-1 and 1000 µg L-1] of T. terrestris extract. Sperm motility characteristics and longevity were determined. In addition, protodioscin content of T. terrestris extract was assessed. The present study revealed that the presence of T. terrestris caused to increase in sperm motility. The increases in duration (49.00±3.61 s) and motility rate (91.67±2.89%) at 400 µg L-1 were statistically significant (p
... [31,32,33]. Phytochemicals found in P. guineense include saponin, alkaloids, steroids, glycosides, flavonoids, tannin and phenolic compounds [34].Saponins have been implicated as possible bioactive DOI: 10.9790/5736-1105010917 www.iosrjournals.org 14 |Page agent responsible for the aphrodisiac effects of many plants extract e.gTribulusterrestris, Massulariaacuminata [35,36,37,38]. It exerts it's effect due to its androgen increasing property [35]. ...
... Low density lipoproteins are the major arteriogenic lipoprotein and usually account for most of the coronary heart disease (CHD) associated with elevated plasma total cholesterol [58]. High density lipoprotein cholesterol protects against CHD, the risk of CHD from arteriosclerosis is inversely proportional to serum levels of HDL [59,60,57].The non-significant reduction (p> 0.05) in triglycerides and low density lipoprotein cholesterol by 50 and 100mg/kg body weight of P. guineense, and the significant decrease ( < 0.05) by the 150mg/kg of P. guineenseis an affirmation of its antihyperlipidemic effect of P. guineense [34]. In the same vein the significant increase ( < 0.05) by the 150mg/kg body weight of P. guineense on HDL speaks volume of its cardioprotective effect because increased HDL correlates inversely with CHD [61]. ...
The effect of graded doses (50, 100 and 150mg/kg body weight) of crude ethanol extract of the dry seeds of Piper guineenseSchumach&Thonn was investigated on the ovary, liver, hormonal and some biochemical parameters of female rats weighing between 150-190g. Twenty rats were randomly divided into four groups of five rats each per group, group A (control) were orally dosed once daily with 1ml of distilled water (vehicle) while the test groups i.e. B, C and D were orally dosed with 50, 100 and 150mg/kg body weight of the crude extract in 1ml of the vehicle. After twenty one (21) days of the extract dosing samples were collected for analysis. The results are expressed as the mean of five replicates ± standard deviation, means were analyzed using one way analysis of variance (ANOVA) followed by Posthoc Turkey. p < 0.05 was regarded as significant. All doses of the extract caused significant increase < 0.05 in a dose related manner on testosterone, luteinizing hormone, follicle stimulating hormone, progesterone and estradiol and at the same time reducing the prolactin level. AST, ALT and ALP were not significantly influenced > 0.05 except the 100 and 150mg/kg dose on ALP and only the 150mg/kg dose on the AST and ALT, all doses caused significant elevation (< 0.05) in cholesterol and HDL while the 150mg/kg caused significant reduction in triglyceride and low density lipoprotein cholesterol, microstructural integrity assessment of the liver (H&E× 40) of the 150mg/kg group in comparison with the control group showed microvesicular steatosis (fatty change), in the same vein the ovary of this group reveals enlarged cells with poor follicle development.
... The saponins are also known to boast fertility [64]. Saponins have been implicated as possible bioactive agent responsible for the aphrodisiac effects of many plants extract [65][66][67][68]. Many tannin molecules have been shown to reduce the mutagenic and carcinogenic activities of most mutagens and carcinogens and this is largely due their antioxidative properties which is important in protecting cellular oxidative damage and lipid peroxidation [64][65][66][67][68][69]. ...
... Saponins have been implicated as possible bioactive agent responsible for the aphrodisiac effects of many plants extract [65][66][67][68]. Many tannin molecules have been shown to reduce the mutagenic and carcinogenic activities of most mutagens and carcinogens and this is largely due their antioxidative properties which is important in protecting cellular oxidative damage and lipid peroxidation [64][65][66][67][68][69]. Tannin also has the capacity to accelerate blood clotting, reduce blood pressure, decrease serum lipid parameters and with strong antimicrobial properties [64,70]. ...
Three commonly used herbal plants (B. pinnatum, P. guineense, and Z. leprieurii) were assayed for some elemental, proximate and phytochemical compositions with a view of using these findings to validate their acclaimed ethnomedicinal usage. The elemental analysis was done using atomic absorption spectroscopy, while proximate composition and phytochemical analysis were done by methods of Association of Analytical Chemist (AOAC). The elemental compositions of these plant samples in mg/100g are Na: 0.04 ± 0.04, 0.02 ± 0.01, 0.36 ± 0.15, K: 0.05 ± 0.01, 0.11 ± .01, 0.74 ± 0.25, Mg: 0.12 ± 0.03, 0.12 ± 0.011, 0.03 ± 0.00; Ca: 0.34 ± 0.02, 1.20 ± 0.02, 2.10 ± 0.92; Fe: 1.88 ± 0.10, 0.07 ± 0.01, 0.00; Zn: 5.27 ± 0.28, 0.02 ± 0.00, 0.00 accordingly as above. The proximate composition of the plant samples in % are moisture: 93.57 ± 0.04, 8.50 ± 0.14, 6.20 ± 0.40; ash content: 1.33 ± 0.02, 4.43 ± 0.04, 3.91 ± 0.08; protein: 0.97 ± 0.03, 9.74 ± 0.10, 2.21 ± 0.05; carbohydrate: 0.71 ± 0.03, 50.60 ± 1.10, 27.89 ± 2.25; lipids: 0.23 ± 0.03, 14.64 ± 0.53, 6.31 ± 0.15 and fibre content as 3.68 ± 0.03, 12.32 ± 0.94, 52.63 ± 1.33; caloric values in Kcal/100g are 8.79, 1559.61 and 740.56 according to the order B. pinnatum, P. guineense, and Z. leprieurii. The phytochemicals assayed for in mg/100g indicated the following in the order of B. pinnatum, P. guineense, and Z. leprieurii as alkaloids: 1.57 ± 0.04, 2.15 ± 0.05, 1.87 ± 0.04; tannin: 0.60 ± 0.03, 3.01 ± 0.04, 0.96 ± 0.02; saponin: 1.87 ± 0.01, 2.83 ± 0.05, 3.02 ± 0.11; glycosides: 0.00, 1.64 ± 0.03, 1.53 ± 0.02; steroids: 2.94 ± 0.02, 2.98 ± 0.06, 2.73 ± 0.03;phenolics: 1.91 ± 0.03, 1.08 ± 0.01, 1.76 ± 0.10 and flavonoids as 1.83 ± 0.03, 0.75 ± 0.01, 1.66 ± 0.10. The presence of active pharmacological ingredients in B. pinnatum, P. guineense and Z. leprieurii thus justify their ethnomedical usage in the prevention, treatment and management of various biochemical, physiological, metabolical and microbial conditions, the low calorific value of 8.79 Kcal/100g of B. pinnatum may also help obese patient to come down on their body weight, while the high caloric values of P. guineense, and Z. leprieurii can serve as good energy source.
... The presence of steroidal saponins as possible cause of increase in testosterone levels in animals (Walid et al., 2007). Studies by Gauthaman et al. (2002), Gauthaman and Ganesan (2008) also reported increase in testosterone levels caused by steroids, specifically Protodioscin. Free amino acids and specifically arginine, which has been reported to have aphrodisiac effects as it is converted into nitric oxide which is an important vasodilator in the penile cavernosal tissue (Burnett, 2004). ...
The documentation of the medicinal uses of plants is becoming increasingly urgent because of the rapid loss of some plants' natural habitat due to anthropogenic activities. Traditional knowledge of medicinal plants is also at risk of extinction due to the dependency on oral transmission, and as such, there is an urgent need to document such knowledge. The study aimed to document medicinal plants used in the traditional treatment of erectile dysfunction in Akinyele Local Government Area, Oyo State, Nigeria, and was conducted from April to December 2019. A total of 160 respondents comprised of an equal number of Traditional Medical Practitioners (TMPs) or herbalists and hunters were selected from the study area. Medicinal information was collected using semi-structured questionnaires. The interview was conducted one-on-one using the local language (Yoruba). Data were analyzed with percentages, frequency of citation (FC) and relative frequency of citation (RFC). A total number of 25 plant species belonging to 20 families were reported to be used to treat erectile dysfunction in the study area. Fabaceae subfamily of Caesalpinioidea and Mimisoideae contributed the highest number of plant species. Of the plant identified during the survey, Epimedium grandiflorum had the highest frequency and relative frequency of citation (FC= 150, RFC = 0.94). Roots had the highest percentage of plant parts used. The major method of preparation of the recipes was by grinding while the route of administration of recipes was oral. Most medicinal plants are rare and collected from the wild (forest) while only a few are cultivated. The study showed that local people still have good knowledge of traditional treatment of erectile dysfunction. There is a need for domestication, adequate protection and conservation of these useful medicinal plants to prevent their extinction. Also, studies on the phytochemicals and pharmacological constituents of these medicinal plants to confirmed their bioactive ingredients relevant to the treatment of erectile dysfunction to be utilized for synthetic drugs.
... Tribulus terrestris contains the compound protodioscin (PTN), which was a steroid saponin. A study on 40 castrated mice showed that administration of Tribulus terrestris and testosterone could increase the sexual behaviour of mice in the test group compared to the control group (7) . The main compound that acts as an aphrodisiac in Panax ginseng was ginsenoside. ...
Tribulus terrestris and Panax ginseng are two therapeutic plants that might increase libido. The aim of the study was to see the effects of herbal medicine containing Tribulus terrestris and Panax ginseng on increasing male mice libido. This study used mice divided into two sets of 7 and 14 days. Each group was divided into four parts: control (solvent), comparator (Vitan), and test 1 (herbal medicine). Parameters measured were mice sexual behaviour (introduction, climbing, coitus), sperm concentration, sperm motility, and testicular weight. Except for coitus behaviour, there were no significant changes between groups in the 7 days of treatment. There were significant differences in introduction and climbing behaviour between the control group and test 2 after 14 days of treatment, but not in other parameters. There were no significant variations in any parameters of the mice’s libido between 7 and 14 days of treatment with 1x dose of herbal medicine; however, with 2x doses, only introduction behaviour showed a significant difference. Based on the research results, it can be concluded that administering two doses of herbal medicine can increase the frequency of treatment for 14 days.
... Saponins are known to increase sexual drive or libido. Hence, plants with these secondary metabolites or ingredients enhance sexual activity when consumed by humans [12]. It has been reported that alkaloids possess good aphrodisiac potentials by increasing sexual desire or libido in male rat [13]. ...
The root of Rauwolfia vomitoria (Afzel) is known for its anti-hypertensive, psychoactive properties and aphrodisiac potentials. This research work was aimed at studying the phytochemical constituents and aphrodisiac activities of the crude ethanol extract and its fractions. The root material was macerated for 72 h and the dried ethanol extract (EE) partitioned successively to obtain dichloromethane (DCM), ethyl acetate (EA), butanol (BuOH) and aqueous (AQ) fractions. The LD50 was determined using Miller and Tainter method. The aphrodisiac potential of the crude extract and these factions were evaluated using adult albino mature male rats. The crude ethanol extract was subjected to phytochemical screening. The median lethal dose (LD50) was determined to be 250±15.15mg/kg body weight. The result of phytochemical screening indicated the presence of alkaloids, saponins, cardiac glycosides, flavonoids, tannins and terpenoids. The extract and the fractions decreased mount latency, intromission latency, post ejaculation interval and increased ejaculation latency, mount frequency, erection frequency and penile erection. These effects were statistically significant (p<0.05, p<0.01, p<0.001) relative to control (normal saline). These findings authenticate the use of the root of Rauwolfia vomitoria as aphrodisiac agent.
... Sexual behaviour testing Protocol was carried out according to the method described by Gauthaman et al. (2002). A total of 25 sexually active male rats were housed individually in metabolic cages of dimensions 33.0 cm × 20.5 cm × 19.0 cm, with cleaning of the cages done once daily. ...
... It is a natural stimulant of Luteinizing hormone (LH) which signals the body to produce more of its own testosterone (Neychev et al. 2005). According to clinical studies, it improved reproductive functions, including increase concentration of hormones (Gauthaman 2002). With these valuable objectives, this study will help to create awareness about the pharmacological potent of T. terrestris along with its value-added utility, among the local people surroundings of Mahanadi River area in Cuttack district of Odisha. ...
Tribulus terrestris is an annual medicinal herb belonging to the Zygophyllaceae family, commonly known as 'Gokhura' or puncture-vine. It has been used for a long time in both the Indian and Chinese systems of medicine for the treatment of various kinds of health problems. Its different parts contain a variety of phytoconstituents that are medicinally important, such as flavonoids, tannins, saponins, alkaloids, and phenolic compounds, which show numerous pharmacological activities. It is a straggling, spreading herb found all over the Mahanadi River area in Cuttack, Odisha. Urbanisation is also impacting near-river areas, and slowly the population is going to vanish. Therefore, we are presenting this medicinal herb here to create awareness among the locals, students, and researchers.
... The mating behaviors were recorded using a night-vision camera (Hikvision network camera, Hikvision Digital Technology, Co., Ltd., Hangzhou, China) and the iVMS V3.9.0.5 software (Hikvision, IBCAM, Hangzhou, China). The mounting number, intromission number, mounting latency, intromission latency, and intromission ratio were the sexual behavioral parameters recorded [35,36]. ...
Oral phosphodiesterase inhibitors have emerged as a game changer for the treatment of erectile dysfunction (ED) since attaining FDA approval for its first member, sildenafil, in 1998. Topical penile therapy could be a viable replacement for oral medication that would transform the treatment of ED for many decades to come. This innovative idea could offer a safer topical alternative with less vision and cardiovascular side effects than the oral route. This work aims at developing proniosomal gels for three selected members (sildenafil, vardenafil, and tadalafil) and investigating the proniosomal gels on a rodent model. Niosomes derived from the parent proniosomal gels were characterized for entrapment efficiency (EE%), size, polydispersity index (PDI), zeta potential, and morphology. Proniosomal gels were evaluated for skin permeation, in vivo mating behaviors, and biochemical assays of nitric oxide (NO) and cyclic guanosine monophosphate (cGMP) post penile topical administrations. The optimized proniosomes loaded with tadalafil (F1-T) were compared with oral tablets (Cialis®). Proniosomal gels demonstrated significant enhancement of skin penetration by up to 5.5-fold, compared to control topical suspension. Tadalafil-loaded proniosomes showed superior skin permeability over sildenafil- and vardenafil-loaded proniosomes. In addition, significant improvement was noticed regarding intromission number, intromission ratio, NO, and cGMP for the proniosomal gel F1-T, compared to the untreated control. No statistically significant (p > 0.05) differences in sexual performance or biochemical parameters (NO and cGMP levels) were recorded among orally and topically (tadalafil proniosomal gel) administered groups. These findings support tadalafil topical penile therapy as a promising alternative to the oral route.
... Ginsenosides (Saponins) of Panax ginseng (Lee et al., 2005;Leung and Wong, 2010;Lee et al., 2017), Humic acid, fulvic acid and Dibenzo Alpha Pyrones of Shilajit (Rege et al., 2015;Sharma et al., 2003;Gallardo et al., 2012), sitoindosides VII-X and withaferin A of Withania somnifera (Bhattacharya et al., 1997;Kulkarni et al., 2008), Ptychopetalum olacoides (Antunes et al., 2001) and yohimbine of Pausinystalia yohimbe (Neha et al., 2017) reduced the lipid peroxidation by elevation of free radicals scavenging enzymes, superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPX) levels as reported in the rat, mice and rabbits in chronic disease conditions (Bhattacharya et al., 1997;Dhuley, 1998). Improvement in semen quality may be due to the improved androgen level in the body due to Tribulus terrestris's active component protodioscin as reported in the primates (Gauthaman et al., 2002;Gauthaman et al., 2003). Administration of Turnera diffusa having Apigenin as an active component, pinocembrin, and acacetin in combination significantly suppressed aromatase activity (Zhao el al., 2008;Kumar et al., 2006). ...
The present experiment was conducted to study the impact of herbal treatment on post thaw semen quality and fertility in subfertile buffalo bulls. Three Murrah subfertile buffalo bulls maintained at bull station, Guru Angad Dev Veterinary and Animal Sciences University (GADVASU), Ludhiana, India (Latitude/Longitude, 30.55°N, 75.54° E) with the history of poor semen quality (pre-freeze individual motility < 60%, post-thaw individual motility < 40%, Viability < 70% and Abnormality > 20%) were orally supplemented with herbal mixture (Panax ginseng roots, Shilajit, Withania somnifera roots, Tribulus terrestris fruits, Turnera diffusa leaves, Ptychopetalum olacoides bark of each 400 mg/100 kg body weight and 300 mg/100 kg body weight of Pausinystalia yohimbe bark) daily for 60 days of treatment phase. Two semen ejaculates per week per bull were collected during pre-treatment, treatment and post-treatment phases of 60 days each and extended with Tris egg yolk extender. The freezing of extended semen was carried out in a biofreezer (4°C to -15°C @-30°C/min, -15°C to -140°C @-50°C/min) followed by plunging into liquid nitrogen for storage. Post thaw semen quality was assessed in terms of individual motility, viability, total sperm abnormalities. Present study revealed that the oral treatment of subfertile buffalo bulls with Panax ginseng roots, Shilajit, Withania somnifera roots, Tribulus terrestris fruits, Turnera diffusa leaves; Ptychopetalum olacoides bark each @ 400 mg/100 kg body weight and Pausinystalia yohimbe bark @ 300 mg/100 kg body weight for 60 days improved post thaw semen quality and fertility.
... Testosterone is a male hormone with a significant impact on spermatogenesis (Amanatkar et al., 2014). Leydig cells of the testicles secrete testosterone, the adrenals, and ovaries, and is the most important androgen secreted into the blood (Mansoureh et al., 2016;Gauthaan et al., 2002). Testosterone, deficiency is presented with delayed puberty or regression of previously established male characteristics that depend on testosterone, such as hair distribution, potency, and libido. ...
Nanotechnology is a rapidly growing area of scientific interest due to its wide applications in catalysis, solar energy, waste management, and sensing technology. Nanomaterials are efficiently used in medicine for drug delivery, diagnosis, treatment of cardiovascular diseases, wound healing, and development of antimicrobial agents. The present study aimed to evaluate the effect of Costus afer-AgNPs extract on Testosterone, luteinizing hormone, and Follicle stimulating hormone in male rats. In this experimental study, 18 adult male rats were used. The rats were randomly divided into six groups. The first group (control) adequately consumed compressed food and water without any restrictions during the experiment. The second, third, fourth, fifth, and sixth experimental groups respectively consumed 200mg, 400mg, 600mg, 800mg, and 1000mg Costus afer-AgNPs extract per kilogram body weight in a daily manner. Blood samples were taken from all groups after four weeks through anesthesia. The serum was isolated. Serum concentrations of testosterone, LH, and FSH were measured. The collected data were analyzed using SPSS, ANOVA, and LSD tests. Serum levels of testosterone, LH, and FSH significantly increased in the experimental groups receiving 200mg, 400mg, 600mg, 800mg, and 1000mg Costus afer-AgNPs extract per kilogram body weight compared to the control group (P < 0.05). Costus afer-AgNPs maintained testosterone, luteinizing hormone, and follicle-stimulating hormone levels and could increase them.
... The TT extract increased the cytoplasmic, nuclear, and individual volume of Leydig cells in male Wistar rats (Neylanne et al., 2015). Several clinical examinations have shown that TT increases reproductive activity, including increased hormone levels such as estradiol, with testosterone being only slightly influenced and increasing reproductive activity, ovulation, and sexual desire (Gauthaman et al., 2002). In the testis, seminiferous tubules spermatogenesis is a multistep process highly regulated by hormones (Meri et al., 2013;Walker and Cheng, 2005). ...
... L'écorce de la tige possède également une fortes activité aphrodisiaques (Abioye et al., 2003). Les saponines retrouvés dans la plante renforcent les propriétés aphrodisiaques à cause de leur effet stimulant sur la production d'androgènes (Gauthaman et al., 2002). ...
Kigelia africana, or sausage tree, is a plant widely used in the management of human and animal diseases for a very long time. The objective of this study is to synthesize the knowledge on its biological and pharmacological properties. To achieve this, specific keywords were used to explore scientific databases such as PubMed, Google Scholar, Researchgate, Scorpus and Springer. The data obtained show that the different parts (barks, leaves, flowers, stems, fruits, roots) are used for the treatment of skin, fungal, cancerous, gynecological, malarial, diabetic, pneumonic, psoriasis, eczema, boils, leprosy, syphilis, constipation, tapeworm infestation, jaundice, ulcers and wounds. The pharmacological activities of the different extracts as well as the compounds isolated rom the plant are reported as analgesic, antipyretic, anti-inflammatory, hepatoprotective, antidiabetic, antibacterial, antifungal, nematicidal, antiamoebic, antiviral, antitrypanosomal, anticonvulsant, nutritive, antimalarial, antidiarrheal, anticancer, antioxidant, aphrodisiac, cosmetic and healing. Phytochemical analyses have revealed the presence of a wide range of secondary metabolites (flavonoid, quinones, phenolic compounds, coumarins, alkanes, unsaturated fatty acids). The different potentialities of this plant open the prospect of evaluating its effectiveness in the control of parasitic blood diseases of livestock, especially trypanosomiasis.
... B. alba is reported to increase testosterone production in adult male rat testes during in vitro studies (Moundipa et al. 1999(Moundipa et al. , 2005. T. terrestris has been used for boosting androgen production in human (Bucci, 2000) and rats (Gauthaman et al., 2002), treatment of impotency, premature ejaculation and spermatorrhoea (Umadevi and Rao, 2017). M. pruriens has also been reported to increase testosterone, LH, FSH and prolactin hormone levels, levator ani muscle weight, sperm count and motility in infertile obese mutant rat models (Kumar et al., 2011) and increase libido in men due to its dopamine inducing properties (Giuliano and Allard, 2001;Shukla et al., 2010). ...
Ethnopharmacological relevance:
Herbal plants such as Basella alba (Family: Basellaceae), Tribulus terrestris (Family: Zygophyllaceae), Asparagus racemosus (Family: Asparagaceae) and Mucuna pruriens (Family: Fabaceae) are mentioned in Indian traditional system of medicine Ayurveda to possess androgenic activity and increase male virility. The plants have been reported to improve testosterone level and sperm production in experimental male rodents as well.
Aim of the study:
Male Nile tilapias grow more quickly than females and hence are preferred for monosex Nile tilapia culture. Ethanol extracts of B. alba leaves (EB) and T. terrestris seeds (ET), and methanol extract of A. racemosus roots (MA) and M. pruriens seeds (MM) were found effective to induce masculinization in Nile tilapia. The present study intends to evaluate the anti-aromatase activity of EB, ET, MA and MM, to identify the androgenic bioactive compounds in the extracts, and to determine their pharmacokinetics. The study may validate the use of those plant extracts and their major bioactive phytoconstituents in the field of aquaculture and pharmaceuticals.
Materials and methods:
The four crude plant extracts were first fractioned through column and thin layer chromatography (TLC). Three days old Nile tilapia juveniles (mean weight 0.025 ± 0.009g; mean length 12.50 ± 0.12 mm; n = 50 fish/replicate, 3 replicates/treatment) were then fed diets fortified with the obtained fractions for 30 days. After 30 days, fish were sacrificed and gonad aromatase mRNA expression, and 11-ketotestosterone (11-KT) and estradiol (E2) levels were measured. Fractions yielding the highest male percentage for each plant were subject to gas chromatography-mass spectrometry (GC-MS) analysis. The in silico docking and SwissADME study were conducted with the components showing higher peak percentage in chromatogram.
Results:
After column chromatography and TLC analysis, EB, ET, MM and MA yielded 6 (EB1 - EB6), 8 (ET1- ET8), 14 (MM1-MM14) and 5 (MA1- MA5) fractions, respectively. Fish fed EB2, ET2, MA2 and MM13 fraction fortified diets showed significantly (p < 0.05) higher male percentage (92.32%-98.39%) compared to other treatment groups. EB2, ET2, MA2 and MM13 fed fish showed significantly (p < 0.05) higher 11-KT level compared to control male (+247.52 - +397.76%) and lower E2 level compared to control female (-95.92% to -90.65%). Aromatase mRNA expression was significantly (p < 0.05) down-regulated by all these four fractions (-1.32 to -5.65 fold) with respect to control female. GC-MS analysis revealed the presence of 1-Octadecene (OD) in EB2, Phenol, 2,4-bis(1,1-dimethylethyl) (PD) in ET2 and MA2, 9,12-Octadecadienoic acid (Z,Z)- (ODDA) in MM13. In silico molecular docking indicated that PD is more effective than ODDA and OD to inhibit aromatase. In addition, PD showed better pharmacokinetics and more drug-likeness compared to OD and ODDA in SwissADME analysis.
Conclusion:
The present results indicate that ET and MA are more potent to produce all-male tilapia by means of aromatase inhibition. PD can be an ideal compound to achieve masculinization in Nile tilapia through dietary administration, but further investigation is required.
... The sustained direction of different doses of PHF for 3 weeks increased testosterone and luteinizing hormone levels. An increase in testosterone level has been related with increasing of sexual desire, penile tumescence, and rigidity, as well as the accessory muscles which help to provide added sexual movement [20][21][22]. Study with the diverse animal and human models indicates that there is a strong connection between sexual behavior and brain neurotransmitters such as dopamine and 5-HT. The motor manage of ejaculation in animals is modulated by serotonin and its receptors. ...
Objective: The objective of the study was to study aphrodisiac activity of polyherbals on albino Wistar rats. Methods: Play Win and Ayurex are examples of the already marketed polyherbal formulations (PHFs), which are used in this study to determine their mating behavior and mating performance test activities in albino Wistar rats. Results: Both the test drugs Play Win and Ayurex created noteworthy increase in the mounting behavior of animals. It was also observed that mounting behavior activity (number of mounts) in Play Win, in the 1st h and the 3rd h, was greater than Ayurex. Administration of suspension of a single dose of Play Win, Ayurex, and sildenafil citrate concluded in the increase in the mating performance of the rats. The result of Play Win was found to be less than that of Ayurex and nearly the same as that of sildenafil citrate. Conclusion: From the research of the above-mentioned formulations with comparison to the standard drug (sildenafil), it is concluded that the PHFs are capable of producing aphrodisiac activity.
... These indices of libido, when taken together pointed to the fact that the extract may possess aphrodisiac properties; such increases in the frequencies of mount and intromission, suggest that libido, sexual vigour and sexual performance were enhanced. 40 This potential of the leaf extracts could be due to the abundance of flavonoids in the leaf extract; flavonoids are involved in penile erection onset and improve sexual performance. 41,42,43 ...
The effects of Eremomastax speciosa leaf extract on reproductive activities was evaluated; antioxidant activities and the phytochemistry of Eremomastax speciosa were assayed using standard methods. Thirty-five matured male Wistar rats were used for the experiment and they were divided into five groups of seven rats each; groups 1 and 2 were the positive and normal controls respectively and were given Manix capsule and distilled water respectively. Groups 3, 4 and 5 were administered the ethanol extract at the doses of 400 mg/kg, 200 mg/kg, and 100 mg/kg respectively. Twelve matured female rats were used for the aphrodisiac assessment. The phytochemical screening showed the presence of Alkaloids, Tannins, Saponins, Terpenes and Flavonoids and the leaves showed a significant free scavenging activity with an IC50 value of 90 μg/ml. The result showed a dose-dependent significant (P<0.05) increase in Testosterone levels and also an increase in Follicle Stimulating Hormone (FSH) and Luteinizing Hormone (LH) which was not significant when compared with the normal control. The result also showed a dose-dependent significant increase in the mount, intromission and ejaculatory frequencies while decreasing their latencies when compared with the normal control. In conclusion, the ethanol leaf extract of Eremomastax speciosa possesses aphrodisiac potentials and could boost testosterone level which could enhance reproductive indices.
... (Tribulus terestris L.) merupakan tanaman tahunan dari famili Zygophyllaceae yang berasal dari daerah Mediterania (Frohe 1999dalam Dinchev et al., 2008 termasuk golongan tanaman C4 (Yang and Yu, 1981) dengan daerah persebarannya yaitu di negara Eropa, Asia, Afrika dan Australia (Qureshi et al., 2014). Menurut Gauthaman et al., (2002) menyatakan bahwa 45% berat kering ekstra tribulus mengandung saponin steroid, dengan saponin steroid yang paling aktif yaitu protodioksin (PTN). Zat ini oleh tubuh manusia akan di ubah menjadi hormon dehidroepiandosteron atau DHEA, yang merupakan stimulan untuk memproduksi hormon testosteron dan estrogen. ...
Penelitian ini bertujuan untuk mendapatkan teknik sterilisasi yang tepat dalam budidaya tribulus secara in
vitro. Penelitian dilakukan di Laboratorium Kultur Jaringan Fakultas Pertanian Universitas Sebelas Maret
(UNS) Surakarta, mulai bulan Oktober sampai Desember 2017. Eksplan yang digunakan berupa kotiledon
dari kecambah tribulus dan media yang digunakan media Ms (murashige dan skoog). Penelitian
menggunakan rancangan acak lengkap (RAL) dengan 5 perlakuan: 1) kontrol, 2) perendaman fungisida 1%
1 jam dan bakterisida 1% 1 jam, 3) perendaman fungisida 1% 45 menit dan bakterisida 1% 45 menit +
dicelupkan etanol 70%, 4) perendaman fungisida 1% 45 menit dan bakterisida 1% 45 menit + perendaman
etanol 70% selama 2 menit dan, 5) perendaman fungisida 1% 1 jam dan bakterisida 1% 1 jam + dicelupkan
etanol 70%, setelah itu pada masing-masing perlakuan sterilisasi dilanjutkan dengan perendaman antibiotik
selama 30 menit, clorox 5% selama 15 menit, betadin 2 tetes/100 ml aquades selama 1 menit, dan terakhir
perendaman asam askorbat selama 30 menit, setelah sterilisasi dari bahan satu ke bahan yang lainnya
dilakukan pembilas 1x. Hasil penelitian menunjukkan bahwa perlakuan perendaman fungisida 1% 1 jam
dan bakterisida 1% 1 jam + dicelupkan pada etanol 70% memberikan hasil terbaik terhadap pertumbuhan
persentase eksplan tribulus dengan persentase eksplan yang hidup 62,5% dan persentase kontaminasi
terendah sebesar 37,5%. Sehingga teknik sterilisasi ini dapat digunakan untuk sterilisasi pada kultur jaringan
tribulus.
... In traditional Chinese and Indian medicine, the plants fruit is used in the treatment of infertility, impotence, erectile dysfunction and low libido (7). Tt is a completely natural non-hormonal herbal, product extracted from the herb has been shown to enhance sexual behavior in an animal model (8). Studies demonstrating that Tt contains steroids, saponins, flavonoids, alkaloids, unsaturated fatty acids, vitamins, tannins, resins, nitrate potassium, aspartic acid and glutamic acid (9). ...
A total of fifteen male rabbits of mixed breeds, aged between 4-5 months and weighed 1.5-1.7Kg were used in this experiment to determine the effect of oral administration of alcoholic extract of Tribulus terrestris (Tt) on male fertility parameters. The rabbits were randomly allocated into 3 groups, the 1st and 2nd experimental groups were treatment orally with alcoholic extract of Tt in a dose of 75mg/kg/day or 150mg/kg/day respectively, the 3rd groups considered as a control groups and administrated distal water daily. Feed and water were served ad libitum throughout the period of 40 experimental days. At the end of the experiment, the male rabbit's weight and blood samples were taken by heart puncture. Sera were separated, kept at-20°C until using to determine the testosterone value of bucks, then slaughtering male rabbits and the pairs of testes were carefully dissected and transported into normal saline. The weight of testis and epididymis were measured, and the caudal spermatozoa were evaluated. Result showed a significant (P< 0.05) effect of alcoholic extract at a dose of 75mg/kg/day and 150mg/kg/day on body weight, testicular weight, level of testosterone and sperm characteristics when compared with control group. This result showed that administration alcoholic extract (75mg/kg/day, 150mg/kg/day) increased fertility parameters in male rabbits, the dose of 150mg/kg/day gave best effect on fertility parameter in male rabbits. Introduction Infertility is one of the major health problems in couple's lives, approximately 30% of couples infertilities are due to male factors (1). Several conditions can interfere with spermatogenesis and reduce sperm quality and production. Many factors such as drug treatment, chemotherapy, toxins, air pollution, and inadequate vitamin intake may have damaging effects on sper-matogenesis and the normal production of sperm (2). Some studies have assessed the effect of Tribulus terrestris administration on male reproductive system and showed that the plant could positively influence on spermatogenesis (3).
... Hematoxylin and Eosin (H and E) results revealed increased thickness of germ cell layers, and increased population of spermatozoa in the low dose group (Plate 2). These observations have been previously documented to improve male sexual activity and male reproductive functions (Cao et al., 2012;Aversa and Fabbri, 2001;Gauthaman et al., 2002). The observed increased thickness of germ cell layers may be due to increased cell division sparked by the plant extract. ...
... The rats were monitored with a digital video 1 hr in different transparent boxes (60 × 60 × 80 cm) to assess the erectile response of the rats. The sexual behavior parameters analyzed were: mounting latency (the time a female was introduced till the first pelvic thrust was achieved), mounting number (amount of mounts without intromission from the time a female was introduced to the male), intromission number (the number of intromissions from the time female rat was introduced till the experiment was concluded), intromission latency (the time a female was introduced till the first mount attempt with pelvic thrusting and vaginal penetration) (Gauthaman et al., 2002;Guohua et al., 2009). ...
Despite the antidepressant potency of paroxetine, its side effect of erectile dysfunction is burdensome. Grapefruit peels (GFPs) are underutilized cultivar wastes with wide range of therapeutic potentials which have been attributed to their antioxidant behavior and phenolic contents' abilities to effectively inhibit enzymatic activities and manage endothelial dysfunction in cardiovascular disorders. This study aims to investigate the erectogenic potentials of GFP extract in a rat model of paroxetine‐induced ED. Experimental rats were sectioned into five groups: [1: control; 2: paroxetine (10 mg/kg); 3: paroxetine + sildenafil (5 mg/kg); 4: paroxetine + GFP (50 mg/kg); 5: paroxetine + GFP (100 mg/kg)] and treated for 28 days. Sexual behavior of rats was assessed and effect of GFP on ecto‐5′ nucleotidases, phosphodiesterase‐5, and adenosine deaminase (ADA) activities was determined in rats' penile tissues. The levels of malondialdehyde, nitric oxide (NO) as well as superoxide dismutase (SOD) and catalase activities were also determined. HPLC‐DAD analysis showed the presence of naringin, rutin, caffeic acid, quercitrin, quercetin, and kaempferol glycoside. Oral administration of paroxetine reduced erectile response as revealed by their low intromission and mounting numbers as well as high intromission and mounting latencies. Paroxetine caused a significant elevation of ADA and phosphodiesterase‐5 activities and malondialdehyde levels with drastic reduction in levels of NO, SOD, and catalase activities in rats' penile tissues. However, GFP extract reversed PDE‐5, ADA, and antioxidant activities to normal levels, raised the concentration of NO. These results suggest the erectogenic effects and protective potentials of GFP extract against paroxetine‐induced erectile dysfunction.
Practical Application
Grapefruit peels are an environmental menace in many countries and this study showed that the peels can be used in the prevention / management of erectile dysfunction. The therapeutic potentials of the peels are due to the presence of bioactive compounds such as flavonoids and phenolic acids. Therefore, exploring the erectogenic potentials of the peels will translate to conversion of the wastes to therapeutic products.
... Link aqueous extract (500 mg/kg) is able to cure this condition [68]. Its assuaging effects may be due to the antioxidant [69] and androgenic properties of flavonoids [70], phenols [71], saponins [72,73] and phytosterols [74] present in it. Alloxan (120 mg kg −1 body weight) induced diabetic rat models have also shown impaired sperm parameters with testicular damages. ...
... 63 It is rich in proteins and minerals, phenols, terpenes, and steroids (saponins) present in its extracts. 64 This excellent phytochemical profile exhibited antioxidant, 65 anti-inflammatory, antimicrobial, 66 cardioprotective 67 aphrodisiac diuretic, 68 and iron-chelating 69 properties. ...
Background and Purpose: Irochel is a polyherbal formulation, comprises ethanolic extracts of Emblica officinalis, Cucurbita pepo L, Triticum aestivum, Fagonia cretica, Momordica charantia, and Tribulus terristris. It is prepared for the management of iron overload in transfusion-dependent thalassemia patients in which non-transfusion binds iron-produced reactive oxygen species ROS that causes severe damages to the organs leads to death. Research Study: In this study, phytochemical, antioxidant-DPPH assay, cytotoxicity, acute, and subacute toxicity in Wistar rats according to OECD guidelines 423 and 407, respectively, was carried out. The pharmaceutical analysis was conducted following standard protocols. Results: The results exhibited that each herb has a rich amount of phytochemical constituents. The DPPH assay showed IC 50 values for Irochel and Gallic Acid 106.6 ± 4.28 [uM] and 21.8 ± 1.03 [uM], respectively. The LC 50 124.327 μg/ml was obtained in cytotoxicity. In acute toxicity (14 days) and subacute toxicity (28 days) studies, the results revealed no treatment-related toxic manifestations, or mortality. Therefore, LD 50 was found > 5000 mg/kg. However, there was some hematological and biochemical variations observed at 3 different doses of 2000, 300, and 50 mg/kg bw. Conclusion: Thus, Irochel has significant antioxidant activity and it is a safe drug for human use.
... Phaleria macrocarpa, usually used for the treatment of cancer, diabetes, hypercholesterolemia, hypertension, heart disease, allergy etc. (Winarto and Mahkota 2002). The fruits of the plant contain alkaloid, saponin, flavoid, and polyphenol which can enhance the testicular function of male mouse (Gauthaman et al. 2002;. Parhizkar et al. (2014) reported that Phaleria macrocarpa enhance the number of spermatogonia cells and thickness of seminiferous tubules as well as improved rat's fertility when it administered @ 240 mg/kg of aqueous extract for 7 weeks. ...
Fertility of male animals is influenced by various factors such as neurohormonal imbalances, reproductive organ tissue changes, seminal attributes, libido and sexual behavior. The global decline in male reproductive health is a big worry, and modern therapeutic options to prevent male infertility are costly, less accessible, require long-term treatment, and have a variety of adverse effects. Herbal remedies, on the other hand, are better suited to providing more comprehensive approaches to improve the male reproductive health. There is a particular set of herbs known as vajikarana or aphrodisiacs in Ayurvedic pharmacology that nourishes and stimulates the sexual tissues. This review focuses on the Ayurvedic approach to improving male reproductive health, referring to some of the most important scientifically tested herbs that have been found to boost male fertility by having stimulating or nourishing effects on the male reproductive organs.
... Red tilapia has a high popularity worldwide due to its characteristics (high growth rates, attractive skin color, tolerance to high salinity, and relatively high price) (Thodesen et al., 2013). T. terrestris, also called gokshura, is a medicinal plant used in many countries to treat sexual deficiencies (Bucci, 2000;Gauthaman et al., 2002). The inclusion of T. terrestris extract in the diets of African catfish resulted in the production of high male populations . ...
... Although hibiscus is a native to tropical Africa, it can also be found in other Southeast Asia countries.Nowadays, different extracts and molecules isolated from various plants are usually utilized in treatment of various causes of infertility in male. Such extracts include Trichopuszeylanicusethanolic extract [9], Vanda tessellata flowers ethanolic extract [10], Lepidiummeyeniilipidic extract [11], Turneradiffuse and Pfaffiapaniculata extracts [12], Tribulusterrestris extract [13], Panaxginseng roots [14] Eurycomalongifolia extract [15] Terminalacatappa seeds extract [16], Rutachalepensisagueous extract [17], Polysaccharides of Lyciumbarbarum fruit extract [18], Shengjingpill; a Chinese formula of plant extracts [19], Hibiscusmacranthus and Basellaalba aqueous extracts [20], Crotonzambesicusethanolic extract [21], and Astragalusmembranaceus and Acanthopanacissenticosiaqueous extracts [22]. However, the antifertility activity is hibiscus flower has not been extensively examined. ...
Medical plants are characterized by physiological active principles that have been utilized in traditional medicine years ago in treatment of different diseases. Previous studies indicated that Hibiscus sabdariffa has ethno-medical and ethno-veterinary characteristics; however, the relationship between and male reproductive hormones levels has not been clearly demonstrated. The objective of the current work was to examine the impact of 30% concentration H. sabdariffa extract on reproductive hormones and histological effects of the testis of adult male rabbits.Crude extract of blooms of Hibiscus rosasinensis has been demonstrated that there was definite antifertility effect of this extract in causing degenerative changes in the germinal epithelium of male rabbits. Effect of H. sabdariffa on basal levels of testosterone, follicle stimulating hormone (FSH) and luteinizing hormone (LH) was studied using post pubertal healthy male rabbits. Calyx extract of H. sabdariffa at a dose of 300 mg/kg reduced reproductive hormones in experimental rabbits. In conclusion, calyx extract of H. sabdariffa can have negative impact on male reproductive hormones in rabbits and the histological formation of the testicle.
... protodioscin [8]. Steroidal saponins in the aerial parts : Protodioscin, neoprotodioscin and prototribestin [9]. ...
... The seeds of T. terrestris contain alkaloids, steroidal saponins, tannins, flavonoids, and flavonol glycosides, as bioactive compounds (Chhatre, Nesari, Somani, Kanchan, & Sathaye, 2014;Ghosal et al., 2015). The androgenic activity of T. terrestris is linked to the presence of protodioscin, a steroidal saponin (Dinchev et al., 2008;Ganzera, Bedir, & Khan, 2001), which induces production of testosterone phyto-dehydroepiandrosterone, dihydrotestosterone, and dehydroepiandros-teronesulfate in men (Adimoelja, Sartono, & Soedjono, 2005), rabbits and rats (Gauthaman, Adaikan, & Prasad, 2002;Gauthaman & Ganesan, 2008). Therefore, puncture vine extracts are used to treat sexual infertility, improve libido and spermatogenesis in humans (Adaikan, Gauthaman, Ng, & Prasad, 2000;Adaikan, Gauthaman, & Prasad, 2001;Adimoelja, 2000;Adimoelja & Adaikan, 1997;Bucci, 2000;Neychev & Mitev, 2005). ...
Control of prolific reproduction is vital for a profitable tilapia aquaculture enterprise. All‐male tilapia culture is a popular method used to control prolific breeding, because the male individuals grow faster than female and mixed‐sex populations. Presently, most farmers use 17α‐methyl testosterone (MT) to produce all‐male tilapia individuals, although synthetic hormones are linked to human health and environmental risks. Recently, considerable attention has focused on plant‐based products as alternatives to MT, because they are affordable, safe, and eco‐friendly. Despite the growing interest in using plant extracts to prevent frequent spawning in tilapia production, the available information is not collated to standardize application guidelines. Accordingly, this review article consolidates existing knowledge on the use of plant extracts to control prolific breeding in tilapia culture systems. In addition, limitations to commercial application of the extracts are identified. To date, seed, root, and leaf extracts of 20 plant species, most notably, Tribulus terrestris, Mucuna pruriens, and Carica papaya, exhibit potential for controlling unwanted breeding in tilapia production systems. The extracts are mainly administered orally, incorporated in fish feeds. Saponins and flavanoids are the main bioactive compounds in the phytoextracts, which induce sex inversion and fertility impairment in tilapia. The commercialization of plant extracts is, however, hampered by lack of standardized information on extract preparation, optimal dosages, and mechanism of action. Thus, future studies should address these technical limitations and highlight economic incentives for commercial use of plant extracts in tilapia aquaculture.
... Thereafter, these oestrous female rats were paired with treated (Gauthaman et al., 2002). The measure of penile erection was denoted as the number of penile lickings during the observation period. ...
We measured the effect of varieties of Fig leaves, Ficus exasperata Vahl. (FE) and Ficus asperifolia Miq (FA), commonly found in Sub‐sahara Africa for managing hypertension on sexual performance in hypertensive rats, which is unknown. Hypertensive rats experienced erectogenic damage after exposure to 40 mg kg−1 bw−1, N(G)‐nitro‐l‐arginine‐methyl‐ester (L‐NAME). Experimental rats were grouped into eight groups (n = 6) namely: control rats, hypertensive rats, hypertensive treatment groups with atenolol (10 mg kg−1 day−1) and sildenafil (5.0 mg/kg), rats treated with FE‐ and FA‐formulated biscuits at proportions of 2.5 g and 5.0 g respectively. Furthermore, we measured the level of sexual performance (Intromission number, latency, Mounting number, and latency), hormonal levels, phosphodiesterase‐5 enzyme (PDE‐5) activity and genes expressed using real‐time quantitative polymerase chain reaction (RT‐qPCR) in hypertensive rats. The result deduced revealed that treated hypertensive rats showed significantly reduced follicle‐stimulating hormone, luteinising hormone levels, PDE‐5 enzyme activity, tumour necrosis factor‐alpha (TNF‐α) expression while having a marked increase in testosterone level, sexual performance and endothelial nitric oxide synthase (eNOS) expression. Therefore, this study revealed the comparative dietary enhancing effect of FE‐ and FA‐formulated biscuit on sexual behaviour activity, hormonal levels and the level of eNOS and TNF‐α genes expressed in hypertensive rats.
... First, the rats were accommodated for 10 min before testing. Then, sexual behavior was recorded for 30 min after introducing female rats in the estrous phase [35,37,[57][58][59][60]. Behavioral parameters including courtship, mount latency (ML), intromission latency (IL), mount frequency (MF), intromission frequency (IF), and copulatory efficiency (CE) were recorded throughout the whole period by video. ...
Moringa oleifera Lam. (M. oleifera) has been called the “miracle tree” due to its attributes for therapy in various diseases. However, M. oleifera studies on the male reproductive system have been limited. The aim of this study was a phytochemical screening and investigation of the effects of M. oleifera leaf tea on sexual behavior, reproductive function and antioxidant activities. Male rats were fed with M. oleifera leaf tea extract at doses of 0.55, 1.10 and 2.20 mg/kg or distilled water for 30 days. The result showed that M. oleifera leaf tea contained rich total phenols and flavonoids. The courtship behavior, seminiferous tubule diameter, epithelium height, epithelium area, type A spermatogonia, and spermatogonia efficiency were significantly increased in all treatment groups. The groups treated with 1.10 and 2.20 mg/kg increased the number of Sertoli cells. The total of spermatogenic cells increased in the group treated with 0.55 mg/kg. M. oleifera leaf tea scavenged DPPH radical, ABTS radical and H2O2, and inhibited LPO and AGEs formation. Due to M. oleifera leaf tea containing rich total phenols, flavonoids, and antioxidants, it could enhance sexual function and the male reproductive system.
... Moreover, this increase in overtime could also be explained by the fact that the animals would have acquired a sexual experience. This improvement in libido could be the consequence in a possible elevation in the concentration of testosterone, since saponins could improve androgen production [32] , mainly testosterone which is hormone involved in the improvement of sexual desire, motivation and sexual performance in this study ...
Alchornea cordifolia, a shrub found in tropical Africa, is used to treat several physiological disorders, including male infertility and impotency. The main objective of this study was to determine the effect of the methanolic extract of Alchornea cordifolia leaves on the sexual behavior of senescent and sexually inexperienced rats. In order to evaluate aphrodisiac properties and reproductive performance, rats were divided into groups: group I receiving distilled water, group II receiving testosterone, group III receiving sildenafil citrate, group IV and V receiving the methanolic extract of Alchornea cordifolia leaves at 200 mg / kg and 400 mg / kg, respectively. The treatment was done by gavage for groups I, III, IV and V and subcutaneous injection of testosterone every three days for group II for 14 days. On days 1, 7 and 14, the rats were mated to the receptive females. At the end of this last treatment, the rats were mated with gonad-intact females. 14 days after of treatment, the extract leads to an increase in libido and sexual performance parameters (mounts, intromissions and ejaculations frequency) and an increase in sexual desire (decrease of mount and intromission latency). The extract also prolonged the duration of coitus by increasing the ejaculation latency and the average interval of copulation. An increase in the percentage of female’s rats impregnated as well as the numbers of implantations were recorded in females’ rats mated with the males treated with our extract. These results reveal the potential of the methanolic extract of Alchornea cordifolia leaves to improve male reproductive performance justifying its use in traditional medicine
... Its mainly affected constituent is terrestrosin, which is primarily composed to steroid saponins [22,23,24]. Modern pharmacological research has demonstrated the effects of steroid saponins against tumours, cardiovascular and cerebrovascular diseases, senescence, and inflammation [25,26,27]. The significant anti-inflammatory effects of steroid saponins originate from the N-trans-q-caffeoyl tyramine structure [28]. ...
Atrazine is considered moderately toxic to aquatic animals. In the present study protective effect of Tribulus terrestris on hepatotoxicity in fresh water fish Oreochromis mossambicus, at sub lethal concentration of atrazine (16.5mg/l) exposure fish for 120h was studied. After completing the exposure time experiment were carried out to find the level of lipid peroxidation, reduced glutathione, superoxide dismutase, catalase and glutathione peroxides (LPO, GSH, GPx, SOD, and CAT) activities in liver tissues. The results showed increases LPO and decreased level of GSH, GPx, SOD, and CAT when compared to normal. During the recovery period Tribulus terrestris (1.2g/l) plant exposure drastically restored to the normal level when compared to atrazine treatment. Present investigation concluded that the Tribulus terrestris significantly alters the metabolic activity in liver tissues of atrazine exposed fishes.
... Embora inúmeros efeitos da TT em animais (Arcasoy et al., 1998;Gauthaman et al., 2002;Gauthaman e Ganesan, 2008;) e humanos (Brown et al., 2000;Antonio et al., 2000;Kohut et al., 2003;Samani et al. 2016;GamalEl Din et al. 2020) tenham sido avaliados e muitos compostos ativos a partir de extrato de TT tenham sido estabelecidos, o modo de sua ação e eficácia ainda são incertos e controversos. Devido à escassez de trabalhos que correlacione os efeitos da TT sobre os níveis de testosterona e suas consequências na morfologia cardíaca, o presente estudo teve como objetivo avaliar o efeito do TT sobre o ganho de peso, o consumo de ração, a histomorfologia ventricular esquerda e fisiologia testicular em ratos wistar. ...
O Tribulus terrestris (TT) é uma planta originária da Índia, conhecida como Abrolo ou “Videira-de-punctura”. São muitas as incertezas relacionadas aos efeitos do TT na potência física de atleta, nos níveis de testosterona e como afrodisíaco. Há poucos relatos do efeito do TT no sistema cardiovascular, contudo citam que pode existir uma correlação negativa entre consumo do TT e atividade da enzima conversora de angiotensina. Neste estudo avaliamos o efeito do TT no ganho de peso, na concentração sérica da testosterona e na morfometria cardíaca de ratos. Trinca ratos foram divididos aleatoriamente dividido em 2 grupos experimentais (n=15): Grupo CT, tratados com solução fisiológica 0,9%; grupo TT, tratados com extrato de Tribulus terrestris. Após 60 dias de tratamento, os animais que receberam TT ganharam menos peso corporal e não apresentaram diferenças nos níveis séricos de testosterona e morfometria cardíaca quando comparados aos ratos do grupo CT. Nossos resultados sugerem que o TT preveniu ganho de peso sem alterar o equilíbrio energético da dieta, sem influenciar a secreção da testosterona e sem alterar a morfometria cardíaca. Portanto, o TT pode ter um futuro promissor em preservar o peso corporal, tornando a prevenção do ganho de peso mais fácil de alcançar do que perder peso e manter essa perda.
For ages plants have been used for various purposes, one of which is its use for treatment of varieties of illness/diseases such reproductive dysfunctions. One of such medicinal gifted plant of nature is Calotropis procera (Rooster Tree). In this research, the effect of Calotropis procera aqueous stem extract on some fertility hormones and biochemical parameters were assessed in male albino rats. A total of 25 male albino rats, were used for this study. The rats were grouped into five (5) with five (5) rats in each group. The fertility improving capability and its effects on some biochemical markers were determined using standard procedures, the effect of the continuous administration on liver and kidney function markers were also investigated following standard protocol after the oral administration of graded doses (100, 200 and 300 mg/kg) of C. procera stem aqueous extract and distilled water and sidnafil serving as negative and positive controls respectively, The result of the fertility markers showed significant (p<0.05) dose-dependent increase in FSH and LH concentrations. Results on the liver function marker showed a non-significant (p<0.05) increase in ALT, AST and ALP and the results of the kidney function parameters were observed to be significantly lower in the treated groups when compared group not administered with extract. The significant increase in the concentrations of Luteinizing hormones, follicle stimulating hormones and testosterone with the administrated of aqueous extract of C. procera may be responsible for the aphrodisiac activity of the extract. The results of this research may validate the folkloric use of C. procera stem in management of reproductive dysfunction in males.
İnfertilite, üreme çağında olan çiftlerin bir yıl süre ile düzenli korunmasız cinsel ilişkide bulunmalarına rağmen çocuk sahibi olamamaları ile sonuçlanan biyopsikososyal bir olgudur. Bu süreçte çiftler; benlik saygısında azalma, cinsel işlev bozuklukları, rol performansında etkisizlik, kontrol kaybı, anksiyete, depresyon, sosyal izolasyon, suçluluk, toplumsal baskı ve damgalanma gibi birçok sorun yaşamaktadır. Dolayısıyla yaşam kalitelerini olumsuz etkileyen adeta kriz olarak algıladıkları bu dönem ile baş etmede, tıbbi tedavinin yanı sıra gebe kalma şansını artırmayı amaçlayan, etkili, güvenli ve daha ekonomik olduğunu düşündükleri biyolojik temelli geleneksel ve tamamlayıcı tıp uygulamalarına başvurabilmektedirler. Derleme niteliğindeki bu makalede; infertil çiftlerin sıklıkla başvurduğu yaşam tarzı değişiklikleri, vitamin ve mineral takviyesi, bitkisel ürün tüketimi gibi biyolojik temelli geleneksel ve tamamlayıcı tıp uygulamalarına ilişkin çalışmaların kanıt düzeyi incelenmiştir. Elde edilen sonuçlar doğrultusunda; infertil çiftlerin güvenilir ve etkili geleneksel ve tamamlayıcı tıp uygulamalarını tercih etmeleri ve bu alanda çalışan hemşireler başta olmak üzere ilgili tüm sağlık profesyonellerinin farkındalıkla hasta yararına eğitim/danışmanlık hizmeti verebilmeleri hedeflenmektedir. Bu sayede infertil çiflerin kanıt düzeyi yüksek geleneksel ve tamamlayıcı tıp uygulamalarını tercih etme oranlarının artırılarak fertilitenin korunması ve iyileştirilmesine yönelik toplumsal katkı sağlanabileceği düşünülmektedir.
The medicinal properties and therapeutic efficacy of medicinal plants is because of the bioactive molecules or secondary metabolites present in them. There is a direct correlation between plant secondary metabolites and antioxidant activity which in turn is correlated with their biological or pharmacological activity. Hence it is of utmost importance to extract the phytoconstituents by the use of appropriate extraction technique, since there is no single universal method of extraction. In the present work, various phytoconstituents of leaf and stem of Terminalia crenulata Roth. were extracted using both conventional and modern methods. The conventional method used was decoction extraction method while in modern methods, microwave assisted extraction method and ultrasonic extraction method was used. Both qualitative and quantitative estimation of various phytoconstituents was attempted. In quantitative phytochemical analysis, phenolic content, phenolic acid content, flavonoid content, flavonol content and proanthocyanidin content was estimated. The results suggest that almost all the phytoconstituents were more in leaf than in stem. The modern method UAE was the best method for extracting phytoconstituents in this plant. The qualitative analysis revealed the plant to possess flavonoids, tannins and cardiac glycosides and quantitative analysis revealed presence of phenolics and flavonoids. Hence it is concluded that the plant can be successively used as a natural source of antioxidant and both leaf and stem extracts can be used in drug formulation but leaf should be given more preference.
Keywords: Terminalia crenulata, Conventional extraction methods, Green extraction methods, microwave assisted extraction, ultrasonic assisted extraction, Phytoconstituents, leaf, stem.
Meloxicam is a Non-Steroidal Anti-Inflammatory Drug (NSAID) given to humans and animals to treat inflammation that is most widely prescribed. The use of meloxicam that is not in accordance with the dose and in the long term will cause a toxic effect of meloxicam. Meloxicam can trigger oxidative stress and has a mechanism of inhibition of prostaglandin synthesis that can affect hormonal regulation and male reproduction. The purpose of this study was to analyze potential of (Moringa oleifera) leaf ethanol extract on sperm quality and testosterone hormone of male white rats (Rattus norvegicus) induced meloxicam. The design used was a (CRD) Completely Randomized Design consisting of three treatments and two controls with six replications. The treatment was given for 35 days. Meloxicam was given at a dose of 8,4 mg/kg body weight and moringa extract at a dose of 200 mg/kg body weight/day (P1), 400 mg/kg body weight/day (P2), and 600 mg/kg body weight/day (P3). The results showed that moringa extract dose of 400 mg/kgBW and 600 mg/kgBW has the potential to increase reproductive organ weight, motility, spermatozoa viability, spermatozoa count, and increase testosterone levels significantly (P<0,05).
Massularia acuminata stem is often used in folkloric medicine in the management of erectile dysfunction (ED), without full scientific basis for its action. Thus, the effects of aqueous extract of M. acuminata stem (MAS) on sexual activity, hormonal action, enzymatic activity and levels of molecules associated with erectile function were assessed. ED was induced by single intraperitoneal injection of 50 mg/kg body weight of streptozotocin in rats and treated with sildenafil citrate or MAS (50 or 100 mg/kg) orally for 2 weeks. The results revealed that there was significant (p < 0.05) reduction in mounting and intromission frequencies, testosterone, luteinizing hormone, and nitric oxide levels, as well as elevation in mounting and intromission latencies, phosphodiesterase 5, arginase, acetylcholinesterase, adenosine triphosphatidase, and adenosine deaminase activities, nitric oxide, thiobarbituric acid reactive species, and glycated haemoglobin levels were observed in ED rats in comparison with the control rats. Treatment with MAS or sildenafil citrate significantly (p < 0.05) modulated the sexual behaviour, biochemical parameters and histological architecture, with 100 mg/kg of MAS having the best erectogenic effects. Furthermore, phenolic characterization revealed that catechin and kaempferol as the main phenolic compounds present in MAS, that can act in synergistically or additively with other phytochemicals to confer erectogenic effect.
Atherosclerosis is a chronic inflammatory disease of the artery wall associated with lipid metabolism imbalance and maladaptive immune response, which mediates most cardiovascular events. First-line drugs such as statins and antiplatelet drug aspirin have shown good effects against atherosclerosis but may lead to certain side effects. Thus, the development of new, safer, and less toxic agents for atherosclerosis is urgently needed. Diosgenin and its analogs have gained importance for their efficacy against life-threatening diseases, including cardiovascular, endocrine, nervous system diseases, and cancer. Diosgenin and its analogs are widely found in the rhizomes of Dioscore, Solanum, and other species and share similar chemical structures and pharmacological effects. Recent data suggested diosgenin plays an anti-atherosclerosis role through its anti-inflammatory, antioxidant, plasma cholesterol-lowering, anti-proliferation, and anti-thrombotic effects. However, a review of the effects of diosgenin and its natural structure analogs on AS is still lacking. This review summarizes the effects of diosgenin and its analogs on vascular endothelial dysfunction, vascular smooth muscle cell (VSMC) proliferation, migration and calcification, lipid metabolism, and inflammation, and provides a new overview of its anti-atherosclerosis mechanism. Besides, the structures, sources, safety, pharmacokinetic characteristics, and biological availability are introduced to reveal the limitations and challenges of current studies, hoping to provide a theoretical basis for the clinical application of diosgenin and its analogs and provide a new idea for developing new agents for atherosclerosis.
In recent years, the incidence of erectile dysfunction (ED) has continued to rise worldwide. Since pharmacotherapy is still the most common and effective method for the treatment of ED at present, many methods and drugs have been designed or developed for the treatment of ED. Oral phosphodiesterase-5 inhibitors and androgen supplement therapy are currently the common therapeutics for ED; however, some patients have poor response to these drugs because of the multiple pathogenic mechanisms of ED. Researchers are trying to find other treatment ways. On the one hand, many new strategies and concepts such as targeted therapy are also integrated into clinical or preclinical research; on the other hand, some combined therapies which have synergistic effects with reduced dose of single drug and less adverse effects are also developed. This review article summarized the efficacy of the latest first-line, second-line drugs and adjuvant therapies for the treatment of ED, as well as the application of comprehensive treatments, which will help doctors to not only deeply understand the mechanism of ED but select the suitable therapeutics for those patients.
Infertility is a significant cause of anxiety, depression, and social stigma among couples and families. In such cases, male reproductive factors contribute widely to the extent of 20-70%. Male infertility is a multifactorial disease with several complications contributing to its diagnosis. Although its management encompasses both modern and traditional medicine arenas, the first line of treatment, adopted by most males, focuses on the reasonably successful medicinal plant-based conventional therapies. Phyto-therapeutics, which relies on active ingredients from traditionally known herbs, influences sexual behavior and male fertility factors. The potency of these phyto-actives depends on their preparation methods and forms of consumption, including decoctions, extracts, semi-purified compounds, etc., as inferred from in vitro and in vivo (laboratory animal models and human) studies. The mechanisms of action therein involve the testosterone pathway for stimulation of spermatogenesis, reduction of oxidative stress, inhibition of inflammation, activation of signaling pathways in the testes [extracellular-regulated kinase (ERK)/protein kinase B(PKB)/transformation of growth factor-beta 1(TGF-β1)/nuclear factor kappa-light-chain-enhancer of activated B cells NF-kB signaling pathways] and mediation of sexual behavior. This review critically focuses on the medicinal plants and their potent actives, along with the biochemical and molecular mechanisms that modulate vital pathways associated with the successful management of male infertility. Such intrinsic knowledge will significantly further studies on medicinal plants that improve male reproductive health.
Medicinal plants are used all over the world and have rapidly gained economic importance. The study was conducted to investigate the effects of the aqueous extract of C. arabica leaves on the sexual behavior of Wistar rats. C. arabica is a medicinal plant with a foul odor, toxic, and has hallucinogenic effects. The experimental study was carried out on white rats (male and female) of the Wistar strain from the Pasteur Institute of Algiers (Kouba, Algeria) weighing between 150 and 200g sexually naive. The animals are raised in polyethylene cages, the rats were divided into 4 groups (n=10 rats/group) which received a saline solution (male and female control group), 0.17 µg/ml of the aqueous extract of C. arabica leaves for 7 days orally (male and female treated group). The sexual behavior test was carried out according to four crosses types. The results of the treated groups showed a significant decrease in the mating frequency compared to the control group. Overall, the results showed that C. arabica significantly altered the sexual behavioral parameters (mounts frequency, mating time, licking time, first contact time, contacts number, intromission, latency time, and frequency). The aqueous extract of the plant caused an inconsistent decrease in the parameters of sexual behavior and orientation activity that were recorded in the treated animals. The C. arabica leaves aqueous extract caused an inconsistent decrease in the sexual behavioral parameters and orientation activity that were recorded in the treated animals.
Background
Available evidence suggests that cimetidine is a reproductive toxicant that induces sexual and testicular dysfunction. Ocimum gratissimum (OG) is globally consumed for medicinal and nutritional purposes. To determine the modulating role of aqueous leaf extract of Ocimum gratissimum on cimetidine-induced gonado-toxicity, sexually mature male rats were randomized into four groups of six (n = 6) rats each. Group A: control given 2 ml distilled water. Group B received 500 mg/kg body weight (bwt) of OG extract, Group C received 50 mg/kg bwt cimetidine, and group D received 50 mg/kg bwt of cimetidine + 500 mg/kg bwt OG extract once daily for 8 weeks via gastric gavage. Parameters tested include sperm parameters, testosterone (TT), luteinizing hormone (LH), follicle stimulating hormone (FSH) and prolactin, testicular alkaline phosphatase (ALP), acid phosphatase (ACP), lactate dehydrogenase (LDH), protein, cholesterol, glycogen, sexual behavioural parameters, and testicular histology.
Results
There were depletions in the seminiferous epithelium, decreased sperm quality, TT, LH, and FSH, testicular enzymes, protein, cholesterol, glycogen, and sexual behaviour increase in animals treated with cimetidine only compared to control. OG restored and improved sexual behaviour and libido as evident from increased frequencies of mount, intromission, ejaculation, and ejaculatory latency. Mount latencies, intromission, post-ejaculation, and prolactin were significantly decreased. The significantly decreased testicular activities of ALP, ACP, LDH and protein, cholesterol, glycogen concentrations, TT, LH and FSH were increased by OG administration.
Conclusion
Ocimum gratissimum attenuated the deleterious effects of cimetidine on the testis, protected the seminiferous epithelium, restored, and boosted sexual competence, and promoted spermatogenesis.
Ethnomedicinal survey have shown that the different parts of Hunteria umbellata plant are used in Western and Southern parts of Nigeria in managing various human diseases such as sexually transmitted infections and to induce or augment labor. This is however, without information on its effect on reproductive functions. This study was therefore designed to ascertain if there is any health benefit or risk in the ingestion of Hunteria umbellata on reproductive functions. In this study, qualitative phytochemistry, acute toxicity test and the sub-chronic toxicity effects of 250, 500, and 1000 mg/kg/day of Hunteria umbellata (HU) methanol seed extract on reproductive functions in male and female Wistar rats were investigated for 90 days. To achieve this, effect of repeated doses of methanolic extracts of Hunteria umbellata seed were investigated on selected reproductive parameters of the test animals. Eighty (80) (40 male and 40 female) Wister rats, were randomly divided into 4 groups of 10 rats each. The first group received 10 ml/kg/day of distilled water and served as the control, while the second, third and fourth groups received 250, 500 and 1000 mg/kg/day of the extract for 90 days respectively. Blood samples were collected by retro-orbital puncture and delivered into plain tubes for hormonal assay, using ELISA hormone test kits (Biotec Laboratories Ltd, UK). After 90 days, the rats were anesthetized using chloroform. The histology of the testes and ovaries were also carried out. Result revealed that the prolonged treatment with methanol seed extracts of Hunteria umbellata for 90 days, caused minimal decreases (p>0.05) in testosterone, estrogen, progesterone level in all the extract treated groups as compared with the control group. Also, no significant distortions were observed in the histology of testes and ovaries. The results suggests that the prolonged oral treatment with 250-1000 mg/kg/day of the methanol extract of the seed of Hunteria umbellata did not have any effect on the reproductive functions as well as the reproductive organs in males and females’ rats treated, and could be safe following repeated use.
Sex differences and steroid hormones are known to influence the vascular system as shown by the different incidence of atherosclerosis in men and premenopausal women, or by the increased risk of cardiovascular diseases in women taking birth control pills or men taking estrogens. However, the mechanisms for these effects in vascular tissues are not known. Since steroid actions in target tissues are mediated by receptors, we have looked for cytoplasmic steroid receptor proteins in vascular tissues of dogs. We find specific saturable receptors, sedimenting at 8S on sucrose density gradients for estrogens (measured with [3H]estradiol +/- unlabeled diethylstilbestrol), androgens (measured with [3H]R1881 +/- unlabeled R1881 and triamcinolone acetonide), and glucocorticoids (measured with [3H]dexamethasone +/- unlabeled dexamethasone); they are absent for progesterone (measured with [3H]R5020 +/- unlabeled R5020 and dihydrotestosterone). Progesterone receptors can, however, be induced by 1-wk treatment of dogs with physiological estradiol concentrations (100 pg/ml serum estrogen), indicating a functional estrogen receptor. Receptor levels range from 20 to 2,000 fmol/mg DNA. They are specific for each hormone; unrelated steroids fail to complete for binding. Low dissociation constants, measured by Scatchard analyses, show that binding is of high affinity. Steroid binding sites are in the media and/or adventitia since they persist when the intima is removed. Compared with the arteries, receptor levels are reduced 80% in inferior venae cavae of females, and are absent in the venae cavae of males. We hypothesize that steroid hormones can have direct effects on vascular tissues medicated by specific receptors present in arterial blood vessel walls.
Since decreased serum levels of testosterone (T) do not necessarily predict good outcome of testosterone treatment for erectile disorder, the purpose, of this study was to determine which men with erectile disorder and decreased serum levels might benefit from treatment. From a sample of 31 men(
[`(x)]{\bar x}
age = 39 years), 15 (48%) with erectile disorder and decreased serum levels of T responded well after 8 weeks of testosterone treatment (100 mg of testosterone propionate in the sustained-release form given im once a week). Good treatment outcome was associated with several variables, but only high levels of luteinizing hormone (LH) and low values of the T/LH (testosterone/LH) ratio consistently emerged as significant correlates and/or predictors of effective treatment. Levels of LH above 7.5 IU/L or the values of the T/LH ratio equal to or below 0.87 nmol/IU in patients with erectile disorder and decreased serum levels of T suggest that testosterone treatment may be effective.
The copulatory behavior of 20 male rats was studied in a series of experiments using doses of tetrabenazine from 1.0 mg/kg to 16.0 mg/kg. Most of the animals attained ejaculation at all dose levels. Doses of 1.0, 2.0 and 3.0 mg/kg of tetrabenazine produced little alteration of copulatory behavior. Administration of tetrabenazine, 4.0 mg/kg, produced a reduction in the number of mounts without intromission and in the number of intromissions required to attain ejaculation. Similar effects were obtained with tetrabenazine, 5.0 mg/kg, in addition to increases in mean inter-intromission intervals and post-ejaculatory intervals. An interpretation is offered according to which tetrabenazine, like reserpine, produces two independent effects on copulatory behavior. Its specific effect at intermediate doses is to reduce intromission frequency and mount frequency. At higher doses, these effects become mixed with increases in latency measures. The animals appear to be in cataleptic-like state and much behavior is inhibited. These data are consistent with the hypothesis that moderate decreases in brain monoamine levels facilitate copulatory behavior in male rats.
Previous studies have shown that withdrawal and administration of testosterone propionate (TP) has a quantitative influence on sexual reflexes which parallels changes in copulatory activity following castration and administration of TP. The present study involving castrated spinal male rats explored further this parallel, focusing on the effects on sexual reflexes of the administration of dihydrotestosterone propionate (DHTP) and estradiol benzoate (EB), both of which can activate sexual behavior in spinally intact castrated male rats, but only if given in very large doses for a prolonged period of time. A parallel effect on reflexes and behavior was not found inasmuch as DHTP activated sexual reflexes at a dose (200 microgram daily) considerably below that needed to activate behavior, and EB did not appreciably activate reflexes, even after prolonged treatment at levels (100-200 microgram) higher than necessary to activate behavior. The results, with EB in particular, point out that the display of intromissive and ejaculatory patterns in rats may not involve spinal neural mechanisms that are customarily associated with these behavioral patterns.
This report communicates our attempt to design a small animal model for the evaluation of penile erection, based on the pharmacological responses of cavernous tissues in the rat that resemble those of human subjects. Male adult Sprague-Dawley rats anesthetized with pentobarbital sodium were used in conjunction with papaverine and prostaglandin E1, two vasoactive drugs most commonly used in clinical management of impotence. Intracavernous administration of papaverine (0.05, 0.1, 0.02, 0.4 or 0.8 mg.) induced a progressive increase in intracavernous pressure that peaked at 0.4 mg. This effect was associated with visible penile erection that became conspicuous when accompanied by additional bursts of transient intracavernous pressure fluctuations. The duration of papaverine-induced increase in intracavernous pressure was significantly shortened by clonidine (15 micrograms, intracavernous). Injection of prostaglandin E1 (1, 2 or 4 micrograms) into the corpus cavernosum also elicited an elevation in intracavernous pressure, but the responses exhibited acute tachyphylaxis. By manifesting a response to papaverine and prostaglandin E1 that is similar to that in human, we conclude that the intracavernous pressure in the rat may represent a suitable index for the evaluation of penile erection in small laboratory animals.
Previous research has shown that the frequency and duration of penile erection is diminished after castration and that replacement with testosterone will restore the process. Using rats, the present study was designed to confirm that erection is androgen-dependent and to determine whether castration and androgen replacement affect the penile vascular smooth muscle responsiveness to vasoactive drugs. Blood pressure in the corpus cavernosum was measured directly during erections induced by electrical stimulation of the autonomic innervation of the penis. Maximal cavernosal pressure was markedly reduced after castration but was returned to normal levels if the castrated animals were treated with testosterone. Infusion of nitroglycerin (vasodilator) or phenylephrine (vasoconstrictor) resulted in a decline in cavernosal pressure in androgen-treated animals but not in castrated animals, even though the mean arterial blood pressure was strongly affected in all treatment groups by these drugs. When an inhibitor of nitric oxide synthesis was infused, cavernosal pressure was decreased in all groups, indicating that this substance is involved in penile erection. Taken together, these results show that androgens maintain the erectile process and may act specifically to support the responsiveness of the vascular smooth muscle to vasoactive drugs.
Growth of the penis at sexual maturation is under the control of androgens, but growth ceases as the organ reaches adult size despite continued high levels of circulating androgen. Previous studies have shown that the cessation of penile growth is associated with a decrease in the quantity of androgen receptor, as detected by ligand binding and immunological methods. In the current studies we demonstrate that the decreased androgen receptor levels correlate with a decrease in androgen receptor mRNA content in the penile corpus and os, but not in the glans penis. These findings suggest that modulation of androgen receptor mRNA levels in the body of the penis may be important to the control of androgen-dependent growth in the tissue, and that the control of androgen receptor mRNA levels differs among the different cell types that comprise the penis. To explore the mechanisms controlling androgen receptor expression, we examined the transcription initiation site of the rat androgen receptor gene in ventral prostate and in three compartments of the penis: the corpus, the urethra, and the glans penis. The same promoter is employed in all preparations, suggesting that the different patterns of androgen receptor mRNA expression in these tissues with age are controlled by factors that modulate the activity of the same promoter.
The penile erection ability (PEA) was assessed in 27 dogs with intact orchids (Group I), seven dogs with bilateral orchidectomy for one month (Group II) and four dogs with bilateral orchidectomy for three months (Group III). PEA was indicated by the increase of the intracorporeal pressure (ICP) upon electrical stimulation of the cavernous nerves. PEA was significantly decreased in both orchidectomized groups. However, when reduction in the blood pressure was considered, the difference in PEA between Group I and the orchidectomized group was no longer significant. Before the orchidectomy, plasma testosterone level of 22 adult male dogs varied widely from 105 to 6302 pg./ml. At one or three months after the orchidectomy in 11 dogs, it decreased to a level below 100 pg./ml. There was no significant change in the body weight in the post orchidectomy period. These findings indicate that the castration and/or the resulting low plasma testosterone level does not directly affect PEA through the peripheral neural and cavernosal mechanism.
Coronary heart disease (CHD) was treated with saponin of Tribulus terrestris. According to 406 cases of clinical observation and a cross test (67 cases treated with Yufen Ningxin Pian as control), the results showed that the total efficacious rate of remission angina pectoris was 82.3%. It was higher than the control group with a total effective rate of 67.2% (P less than 0.05). The total effective rate of ECG improvement (52.7%) was even higher than that of the control group (35.8%). It is shown that saponin of Tribulus terrestris has the action of dilating coronary artery and improving coronary circulation, and thus has better effects on improving ECG of myocardial ischemia. If taken for a long time, it has no adverse reaction on blood system and hepatic and renal functions. Neither does it have side effects. It is one of the ideal medicines to treat angina pectoris.
Introduction STEROID hormones are familiar clinically and physiologically as regulators of physiological processes. Five groups of steroid hormones are generally recognized according to their physiological behavior: mineralocorticoids, which instruct the renal tubules to retain sodium; glucocorticoids, which are named for their carbohydratemobilizing properties but have many other effects as well; estrogens, which induce female secondary sexual characteristics; progestins, which are essential for reproduction; and androgens, which induce male secondary sexual characteristics. These classes of steroid hormones are structurally similar and arise from a common series of pathways. They are distinguished by their actions on one or more specific steroid hormone receptors. The hormone/receptor complexes function as tissue-specific transcriptional regulators of distinct domains of genes and, consequently, exert their broad array of physiological effects. (For reviews, see Refs. 1 and 2.) The pathways by which the...
Castrated male rats with complete midthoracic spinal transections were maintained on exogenous testosterone; they showed intermittent clusters of genital responses consisting of erections, quick flips, and long flips of the penis when gentle pressure was con stantly applied to its base. The number of these genital responses per 30-minute test was markedly influenced by withdrawal or administration of testosterone.
The display of penile reflexes and copulatory behavior appears to reflect the activity of two different underlying neuronal system, both of which are modulated by systemic testosterone (T) concentration. To indirectly compare the two systems, the responsiveness to T of penile reflexes and copulatory behavior was examined. In the first experiment castrated spinal male rats were given penile reflex tests while receiving replacement T through Silastic capsule implants filled with T (50 mm T). After capsule removal the number of penile erections and flips declined within 24 hr and gradually decreased for 12 days. Subjects were then reimplanted with new 50-mm T capsules. The number of penile flips and erections increased within 6 and 12 hr. respectively. This is a much more rapid response rate to T than has been established for copulatory behavior. In the second experiment castrated spinal male rats were tested for penile reflexes with a 50-mm T capsule, which was then replaced with a 10-, 5-, or 2-mm T or an empty capsule. The number of penile reflexes declined in a dose-response fashion. In the third experiment, castrated sexually experienced male rats were tested for copulatory behavior with two 25-mm T capsules which were then replaced with a 10 or 2-mm T or an empty capsule. Only males with empty capsules had decrements in copulatory behavior, revealing that a low level of T can maintain virtually normal sexual behavior despite a marked decline in penile reflex activity. The neuronal system underlying penile reflexes (spinal neurons) is apparently much more responsive to changes in T concentrations than the neuronal system underlying motivational and appetitive aspects of copulatory behavior (brain neurons).
Androgens are essential for the expression of normal libido in the male, but their role in the maintenance of the erectile response in humans is controversial. It has been shown previously in the rat that castration induces 1) loss of penile reflexes; and 2) considerable reduction in the erectile response to electric field stimulation (EFS) of the cavernosal nerve. Both of these effects can be reversed by testosterone replacement. The current study was performed to determine whether these testosterone effects are mediated via its conversion to dihydrotestosterone (DHT), and to what extent the synthesis of the mediator of penile erection, nitric oxide, is affected by castration and androgen replacement. Five-month-old rats were either castrated or left intact. The orchiectomized rats were implanted with SILASTIC brand silicon tubing (Dow Corning) containing testosterone or DHT with or without daily injections of the 5 alpha-reductase inhibitor finasteride. After 7 days, rats were submitted to EFS and the intracavernosal pressure was recorded. Castration reduced the EFS-induced erectile response by 50% in comparison with intact rats and testosterone restored this decrease to normal. When finasteride was given to these testosterone-treated castrate rats, erectile response was not restored. DHT was as effective as testosterone in restoring response to EFS in castrates and this effect was not decreased by finasteride. Nitric oxide synthase activity in the penile cytosol was measured by the arginine-citrulline conversion and was found to correlate with the EFS determinations. These results show that DHT is the active androgen in the prevention of erectile failure seen in castrated rats, and suggest that this effect may be mediated, at least partially, by changes in nitric oxide synthase levels in the penis.
To determine if nitric oxide synthase activity within the male reproductive tract is regulated by androgen.
Nitric oxide synthase activity was measured in the reproductive organs of three groups of mature rats: unoperated controls, 1-week castrates, and 1-week castrates given T capsules at the time of surgery. The presence of nitric oxide synthase activity was confirmed by using the nitric oxide synthase-specific inhibitor N-nitro-L-arginine methyl ester (L-NAME).
After castration, nitric oxide synthase activity was significantly reduced by 88%, 73%, and 54% in the caput, corpus, and cauda epididymidis, respectively. In the penis, nitric oxide synthase activity decreased 45% and nitric oxide synthase protein decreased 57% after castration. In the seminal vesicle and lateral prostate, nitric oxide synthase activity increased significantly after castration from nondetectable levels in controls. Nitric oxide synthase activity in the coagulating gland and ventral and dorsal prostate did not change after castration. The changes in nitric oxide synthase activity in all organs after castration were prevented by T replacement. Additionally, the activity measured in every organ in all three treatment groups was > 90% inhibited by L-NAME.
These data demonstrate that androgen differentially affects nitric oxide synthase activity in the male reproductive tract. To the best of our knowledge this is the first time that nitric oxide synthase activity has been shown to be influenced by androgen in any tissue.
An ethanolic extract of the fruits of T. terrestris showed significant dose dependent protection against uroliths induced by glass bead implantation in albino rats. On subsequent fractionation of the ethanol extract, maximum activity was localised in the 10% aqueous methanol fraction. It provided significant protection against deposition of calculogenic material around the glass bead. It also protected leucocytosis and elevation in serum urea levels. Further, fractionation lead to decreased activity. This could be either due to loss of active compounds during fractionation, or the antiurolithiatic activity of T. terrestris being a combined effect of several constituents present in the methanolic fraction.
It has been reported that there is no relationship between serum testosterone level and erectile function and that testosterone mainly acts on the brain and not on the penis. However, we have found that erectile dysfunction in some patients with low serum testosterone improved after androgen replacement therapy. We therefore studied the effects of testosterone on the contraction and relaxation of the corpus cavernosum penis.
Four groups of rabbits were studied over a similar time span. The testosterone group were non-operated and received testosterone propionate 10mg/day for 14 days before sacrifice. Two groups (castration+testosterone group and castration group) were castrated 28 days before sacrifice. The castration group received sesami oil for 14 days, and the castration+testosterone group received testosterone 10mg/day for 14 days. Entire penises were removed immediately after death by desanguination and dissected to obtain corpus cavernosum strips. These strips were suspended under 1g tension in a 20ml organbath containing Tyrode's solution. After equilibration for 2 hours, the addition of drugs was started. Changes in tension were monitored with an isometric transducer and recorded.
The vasoactive drugs used were norepinephrine bitartrate, 1-phenylephrine hydrochloride, clonidine hydrochloride, acetylcholine chloride and vasoactive in testinal polypeptide.
The contractility of the corpus cavernosum strips increased significantly in the testosterone group and the castration+testosterone group, but decreased significantly in the castration group as compared with the control after adding norepinephrine, phenylephrine and clonidine. Relaxation of the corpus cavenosum strips increased significantly in the testosterone group and the castration+testosterone group, but decreased significantly in the castration group as compared with the control after by adding acetylcholine and vasoactive intestinal polypeptide.
These results suggest that testosterone plays an important role in erectile function by a direct action on the corpus cavernosum penis.
We report the use of a modified rat model for the study of the mechanisms of penile erection. In 92 Sprague-Dawley rats, the cavernous nerve was stimulated with different pulse intensities and frequencies, and the intracavernous pressure, time to maximal pressure and total duration of tumescence were measured. A maximal response was elicited at 20 pulses per second (pps) and 1.5 mA. Using this as 100%, we determined the relative pressure responses obtained with other frequencies: 5 pps, 57.3% (p = 0.007), 10 pps, 84.9% (p = 0.043); 30 pps, 99.5% (p = 0.832); 40 pps, 97.8% (p = 0.168); 50 pps, 90.9% (p = 0.021); 100 pps, 76.1% (p < 0.001). The time to maximal pressure varied with different frequencies, but was in all cases significantly different from the 20-pps response. Erection time during continuous cavernous nerve stimulation was significantly longer with frequencies below 20 pps (10 and 5 pps). In 30 rats, the physiologic response to intracavernous injection (0.03 ml) of acetylcholine, atropine, guanethidine, norepinephrine, phenylephrine, papaverine, terbutaline (intravenous also) and phentolamine was measured. Papaverine caused a dose-dependent rise in pressure; acetylcholine, atropine (a parasympathetic blocking agent) and guanethidine all had minimal effects. Phentolamine and norepinephrine increased systemic blood pressure, whereas phenylephrine decreased the intracavernous pressure in response to electrostimulation significantly.(ABSTRACT TRUNCATED AT 250 WORDS)
The dependence of erectile behavior on androgen functioning is well established. Castration produces loss of both libido and potency in man and animals. The present study, using an animal model for potency, demonstrates the dependence of centrally induced erectile behavior on an intact androgen milieu. Castrated rats failed to produce an erection in response to apomorphine, an agent shown to produce erection in nearly all normal rats. Administration of exogenous testosterone propionate in dosages exceeding 60 micrograms./kg. produced a significant increase in erectile behavior. Yawning, an essentially parallel phenomenon to the stimulation of the erectile response, was also decreased following castration and responded similarly to increasing amounts of exogenous testosterone, demonstrating the influence of androgen functioning on the central nervous system. It was concluded that testosterone is a necessary prerequisite for the maintenance of a centrally induced erectile and yawning response. In an animal model of penile erection, testosterone increases the number of erections in a dose-dependent manner in castrated rats. The dependence of the erectile response on testosterone is, at least in part, centrally mediated.
Classically, androgens were thought to be linked to sexual activity in man through their action on increased libido. Recently, the sex hormone dependent nature of nitric oxide synthase (NOS), the enzyme system producing the neurotransmitter of erection (nitric oxide) has been reported. Our study evaluated how changes in testosterone levels alter erectile function. In forty-seven rats the erectile response to cavernous nerve electrostimulation was recorded 1, 5, 10, 20 and 30 d post-bilateral orchiectomy, and compared to controls. Penile tissue was subsequently stained for the presence of NOS, using an NADPH diaphorase technique. Forty eight rats were used in part two. After orchiectomy exogenous testosterone was administered and the erectile function as well as density of NOS positive nerve fibers was assessed. All castrated animals showed a rapid decrease in serum free testosterone levels within 24 h. In contrast, a gradual decrease in intracavernous pressure was recorded with cavernous nerve stimulation, proportional to the time post orchiectomy. NADPH diaphorase staining showed a decreased density of nonadrenergic noncholinergic (NANC) nerve fibers innervating the cavernosal tissue proportional to the time post orchiectomy. With reconstitution of the androgen mileu the erectile response returned to near normal values and recovery of NADPH-positive nerve fibers was observed. Based on presented data we conclude that testosterone or a metabolite plays a direct role in erection acting through an effect on nitric oxide synthase within the corpora cavernosa.
While it is generally accepted that the erectile response in mammals is regulated by androgens, the extent of in- volvement and the precise role of these steroids remains to be established. A number of neurotransmitters have been identified that may mediate erectile function, and several research groups are actively investigating how an- drogens may affect the synthesis and action of these agents. This article reviews what is known about the role of androgens in erectile function, the effects of these ste- roid hormones on the activity of some of the neurotrans- mitters that are thought to be involved, and it cites dif- ferent experimental designs and animal models used in the study of erectile physiology. Also discussed is the question of why castration in men is not always followed by the immediate and rapid loss of erectile capacity.
Neurons of the rat major pelvic ganglia provide innervation to the pelvic organs and external genitalia. In these ganglia, a subpopulation of neurons containing either nitric oxide synthase or vasoactive intestinal peptide or both molecules, is involved in penile erection. The androgen dependence of penile erection is a well established fact. After castration, decreased testosterone levels have been documented to produce erectile dysfunction possibly resulting from functional alterations in major pelvic ganglion neurons. It was therefore of interest to investigate the presence of androgen receptor within these ganglionic neurons. By using immunohistochemistry and a retrograde labeling technique we have demonstrated that the androgen receptor is present in about 40% of neurons of the major pelvic ganglion innervating the corpora cavernosa of the rat penis. In the major pelvic ganglion, 87% and 81% of the neurons labeled with the fluorescent dye Fast Blue from the penis contained nitric oxide synthase-like immunoreactivity and vasoactive intestinal peptide-like immunoreactivity, respectively. Androgen receptor was present in 20% of neurons containing vasoactive intestinal peptide-like immunoreactivity and about 40% of those containing nitric oxide synthase-like immunoreactivity. These results suggest that androgens, which are known to modulate penile erection, may regulate nitric oxide synthase and vasoactive intestinal peptide within the major pelvic ganglion via a direct interaction with ganglionic neurons.
A review of the current literature is conducted to explore the developmental aspects, animal and human experiences and the effects of pharmacological manipulation to explain the role androgens play in sexual function with special emphasis on erectile function and the erectile tissue. This review reveals that androgens are necessary for the normal development of the penis and their deficiency results in significant structural abnormalities. Although androgen receptors in the penis decrease after puberty, they usually do not disappear completely. Animal data show that androgens support erectile function through a direct effect on the erectile tissue. Experimental castration results in impaired erectile response to central and peripheral stimulation and decrease in penile tissue concentration of nitric oxide synthase-containing nerves. Testosterone replacement reverses these abnormalities. In the rat penis, apoptosis is induced by castration and new DNA synthesis is induced by testosterone replenishment. Human data are less clear than animal data. Castration results in loss of libido and in erectile dysfunction. However, these effects are not universal. Testosterone enhances libido, frequency of sexual acts and sleep-related erections. Its effects on erotic erections are not clear.
This double-blind placebo controlled, cross-over study was carried out to assess the effect of testosterone administration on sexual behavior mood, and psychological symptoms in healthy men with erectile dysfunction. Biweekly injections of 200 mg of testosterone enanthate were given over a period of 6 weeks separated by a washout period of 4 weeks. Blood samples for hormonal assessment, behavioral and psychological ratings were obtained prior to each injection. Luteinizing hormone remained significantly depressed but circulating testosterone had returned to baseline levels by 2 weeks following each hormonal injection. The ejaculatory frequency during the testosterone phase was statistically higher than during the placebo phase. There were marked, although statistically nonsignificant, increases in median frequency of reported sexual desire, masturbation, sexual experiences with partner, and sleep erections during the testosterone period. Testosterone did not have demonstrable effects on ratings of penile rigidity and sexual satisfaction. Mood variables and psychological symptoms did not change following hormonal administration. Results suggest that androgen administration to eugonadal men with erectile dysfunction may activate their sexual behavior without enhancing erectile capacity and without effects on mood and psychological symptoms.
To investigate the effects of castration and testosterone on the constricting effect of phenylephrine and endothelium-dependent and -independent relaxing effects of different agonists in the corpus cavernosum of male rabbits.
Twenty rabbits were castrated and 10 received testosterone replacement for 1 month after castration; 10 further rabbits underwent a sham operation and acted as controls. One month after operation the rabbits were killed and their penises excised. Strips of corpus cavernosum were used for isometric tension measurements in organ chambers; concentration-response relationships for phenylephrine, carbachol, adenosine and sodium nitroprusside were obtained by adding the reagent cumulatively to the bath.
The phenylephrine-induced contractions were markedly lower, with no change in the pD2 values (i.e. the negative logarithm of the concentration for half-maximal response), in cavernosal strips obtained from castrated rabbits than in those from controls. Endothelium-dependent relaxation elicited by carbachol increased in the castrated group but the relaxation induced by sodium nitroprusside did not change and those elicited by adenosine were strongly depressed when compared with controls. There were no significant changes in the pD2 values of agonist-induced relaxation responses in all groups. The relaxation elicited by electrical-field stimulation at lower frequencies increased in strips from castrated rabbits but at higher frequencies were unchanged when compared with controls. Castration-induced changes in the relaxation response of cavernosal strips were significantly restored by in vivo testosterone replacement but those induced by phenylephrine were not.
The lack of testosterone has an effect on the reactivity of the corpus cavernosum, indicating that testosterone has an important role in erectile function by a pre- or post-synaptic action on the corpus cavernosum.
Recent rat studies suggest that early exposure to exogenous testosterone accelerates the loss of androgen receptors and compromises eventual penile length. In humans we hypothesize that down regulation of the androgen receptor is not the mechanism that stops penile growth. To test this hypothesis we investigated the effects of androgen deprivation and supplementation on the developing human penis.
A total of 15 normal human fetal penises at 7 to 19 weeks of gestation (mean plus or minus standard deviation 12 +/- 4.5) was divided in half sagittally. Specimens were grafted beneath the renal capsule of male athymic nude mice or nude rats. Three groups of host animals were prepared, including 10 with no testosterone that were castrated at grafting, 15 with testosterone and 5 with super testosterone in which 50 mg. testosterone propionate pellets were implanted subcutaneously at grafting. Each fetal penile specimen was its own control, since half was implanted into an intact animal and the other into a castrated or super testosterone host. Six weeks after grafting the specimens were analyzed for gross size (length), histology and expression of androgen receptors.
All human fetal penile specimens grew from the nadir size and appeared as white exophytic growths on the surface of the host kidneys. Normal grafts were larger than castrate specimens (mean 6.9 +/- 2.1 versus 3.9 +/- 2.1 mm., p = 0.014). Mean length of the super testosterone specimens (7.3 +/- 2.3 mm.) was not significantly greater than that of normal specimens (p = 0.797). Histological analysis revealed that all specimens were composed of viable penile tissue. Cellular density of the castrate penises was approximately 2 times greater than that of the normal and super testosterone specimens (40.6 +/- 5.9 versus 25.1 +/- 2.8 cells per cm.2, p > 0.001), as calculated on enlarged micrographs. Supraphysiological doses of testosterone did not change the histology compared to controls. Immunohistochemical localization revealed androgen receptors expressed throughout the corporeal bodies, surrounding stroma and penile skin with intracellular localization to nucleus. The mean proportion of cells expressing androgen receptors was higher in the castrate (29.4 +/- 5.2 cells per cm.2) than in the normal (24.0 +/- 3.7) and super testosterone (24.7 +/- 4.5) grafts (p = 0.005). However, in regard to growth there was no change in the proportion of androgen receptor positive cells among the groups.
Testosterone influences penile growth, possibly as a result of extracellular stromal expansion. The number of androgen receptor positive cells in the human fetal penis did not change among the castrate, normal and super testosterone hosts. These experiments support the hypothesis that penile growth cessation is mediated by mechanisms other than down regulation of the androgen receptor. Furthermore, these data support the hypothesis that early administration of androgen to prepubertal male individuals does not result in a shorter phallus in adulthood.
Testosterone treatment of rats produces prostatic hypertrophy and detrusor overactivity. Whether or not the detrusor overactivity can be related to an increase in the responsiveness of lower urinary tract smooth muscles is not known.
Male Sprague-Dawley rats were given daily injections of testosterone propionate for 2 weeks. Effects on cystometric parameters and on the responsiveness of isolated detrusor, urethral, and prostate smooth muscle preparations to drugs and electrical field stimulation were investigated.
Testosterone treatment increased prostatic weight twofold (controls, 768 mg; testosterone-treated, 1,478 mg), but not bladder weight (103 mg vs. 116 mg). Micturition pressure (77%), bladder capacity (75%), residual volume (56%), and micturition volume (83%) increased significantly in treated animals, and bladder overactivity developed. No effect of intraarterial doxazosin on these changes was observed. The differences in urodynamic parameters between control and testosterone-treated rats could not be correlated with changes in bladder, urethral, or prostate excitatory innervation, as revealed by responses to electrical field stimulation, or by smooth muscle responses to different contractant drugs.
Some of the urodynamic effects seen after testosterone treatment seem to be caused by the mechanical obstruction of the enlarged prostate. Since there were no changes in smooth muscle responsiveness, it is suggested that the bladder overactivity observed can partly be related to testosterone-induced changes of the micturition reflex at the lower urinary tract, spinal, and/or supraspinal levels.
This study was designed to evaluate the safety and effectiveness of testosterone therapy for clinical symptoms of hypogonadism (low libido, low mood, low energy, loss of appetite/weight) in human immunodeficiency virus-positive men with CD4 cell counts less than 400 cells/mm3 and deficient or low normal serum testosterone levels. The trial consisted of 8 weeks of open treatment with 400 mg of intramuscular testosterone cypionate biweekly. Responders were maintained at this dosage for another 4 weeks and then were randomized in a double-blind, placebo-controlled, 6-week discontinuation trial. Of the 112 men who completed at least 8 weeks of treatment, 102 (91%) were rated as responders on a global assessment of sexual desire/function. Of the 34 study completers with major depressive disorder and/or dysthymia, 79% reported significant improvement in mood at week 8. Average weight change was a gain of 3.7 pounds, with 45% gaining more than 5 pounds. Eighty-four men entered and 77 completed the double-blind phase; of these, 78% of completers randomized to testosterone and 13% randomized to placebo maintained their response. No significant medical or immunologic adverse effects were identified. Testosterone therapy was well tolerated and effective in ameliorating symptoms of clinical hypogonadism, and equally so for men with and without testosterone deficiency. For patients with major depression and/or dysthymia, improvement was equal to that achieved with standard antidepressants.
In 1994, the Massachusetts Male Aging Study presented an inverse correlation of the serum levels of dehydroepiandrosterone (DHEA) and the incidence of erectile dysfunction (ED). We evaluated the efficacy of DHEA replacement in the treatment of ED in a prospective, double-blind, randomized, placebo-controlled study.
The inclusion criteria included ED, normal physical and neurologic examinations, serum levels of testosterone, dihydrotestosterone, prolactin, and prostate-specific antigen (PSA) within the normal range, and a serum DHEA sulfate level below 1.5 micromol/L. Also all patients had a full erection after a pharmacologic erection test with 10O microg prostaglandin E1; pharmacocavernosography showed no visualization in corporeal venous structures. Forty patients from our impotence clinic were recruited and randomly divided into two groups of 20 patients each. Group 1 was treated with an oral dose of 50 mg DHEA and group 2 with a placebo one time a day for 6 months. The International Index of Erectile Function (IIEF), a 15-item questionnaire, was used to rate the success of this therapy.
Therapy response was defined as the ability to achieve or maintain an erection sufficient for satisfactory sexual performance according to the National Institutes of Health Consensus Development Panel on Impotence. DHEA treatment was associated with higher mean scores for all five domains of the IIEF. There was no impact of DHEA treatment on the mean serum levels of PSA, prolactin, testosterone, the mean prostate volume, and the mean postvoid residual urine volume.
Our results suggest that oral DHEA treatment may be of benefit in the treatment of ED. Although our patient data base is too small to do relevant statistical analysis, we believe that our data show a biologically obvious trend that justifies further extended studies.
We investigated, in a rabbit model, the effects of castration and testosterone replacement on: 1) the hemodynamics of the corpus cavernosum; 2) alpha-1 adrenergic receptor protein expression; 3) neural NO synthase protein expression and activity; 4) phosphodiesterase type 5 activity; and 5) trabecular smooth muscle/connective tissue balance. One week after bilateral orchiectomy, animals were treated for 7 days with vehicle alone, testosterone, or estradiol. Intact control animals received vehicle only. Systemic arterial blood and intracavernosal pressures (ICP) were measured in each animal before and after electrical stimulation of the cavernosal nerve. Alpha1-adrenergic receptor protein expression was determined by ligand binding studies. NO synthase expression and activity were determined by Western blot analyses and conversion of L-arginine to citrulline, respectively. Phosphodiesterase type 5 activity was determined by hydrolysis of guanosine 3',5'-cyclic monophosphate (cGMP) in tissue extracts in the absence or presence of 100 nM sildenafil. Smooth muscle content was assessed by Masson's trichrome staining and computer-assisted histomorphometry. Castration significantly reduced ICP, but it did not alter systemic arterial blood pressure during stimulation of the cavernosal nerve. Testosterone, but not estradiol, treatment prevented the effects of castration and restored ICP to values similar to those obtained in intact animals. Castration reduced expression of alpha1-adrenergic receptor, and this reduction was prevented or reversed by testosterone replacement. Neural NO synthase protein expression and total activity were not altered significantly by castration or after testosterone replacement. However, phosphodiesterase type 5 activity increased in castrated animals treated with testosterone. Castration significantly reduced trabecular smooth muscle content, and this reduction was restored by testosterone (but not estradiol) treatment. The results of this study demonstrate that androgen deprivation alters the functional responses and structure of erectile tissue.
The objective of the present study was to investigate the effect of oral treatment of Tribulus terrestris (TT) extract on the isolated corpus cavernosal tissue of New Zealand white (NZW) rabbits and to determine the mechanism by which protodioscin (PTN), a constituent of the TT, exerts its pharmacological effects.
Twenty-four NZW rabbits were randomly assigned to 4 experimental groups of 6 each. Group I served as control. Groups II to IV were treated with the extract at different dose levels, i.e. 2.5 mg/kg, 5 mg/kg and 10 mg/kg body weight, respectively. The TT extract was administered orally, once daily, for a period of 8 weeks. The rabbits were then sacrificed and their penile tissue isolated to evaluate the responses to both contracting and relaxing pharmacological agents and electrical field stimulation (EFS).
PTN on its own had no effect on the isolated corpus cavernosal strips. The relaxant responses to EFS, acetylcholine and nitroglycerin in noradrenaline precontracted tissues from treated groups showed an increase in relaxation of a concentration dependent nature compared to that of the tissues from control group. However, the contractile, anti-erectile response of corpus cavernosal tissue to noradrenaline and histamine showed no significant change between the treatment and the control groups.
The relaxant responses to acetylcholine, nitroglycerin and EFS by more than 10%, 24% and 10% respectively compared to their control values and the lack of such effect on the contractile response to noradrenaline and histamine indicate that PTN has a proerectile activity. The enhanced relaxant effect observed is probably due to increase in the release of nitric oxide from the endothelium and nitrergic nerve endings, which may account for its claims as an aphrodisiac. However, further study is needed to clarify the precise mechanism of its action.
The clinical diagnosis of hypogonadism in the adult is difficult to establish on the basis of a history and physical examination and universally requires biochemical investigations. A serum testosterone determination is justified in men complaining of erectile dysfunction with or without alterations in sexual desire. Among the causes of erectile dysfunction, hypotestosteronemia rates are low. The prevalence of erectile dysfunction particularly is common at a period in life when alterations occur in male hormonal environment. The treatment of hypogonadal erectile dysfunction, regardless of age, is readily available, safe, and effective. The positive impact of treatment on the overall quality of life can be significant. The presence of erectile dysfunction in an aging man (> 55 years) does not imply the presence of hypogonadism, and, even if the two conditions are present, the indications for treatment require good clinical judgment. Persistent low testosterone levels may have significant detrimental effects in other organ systems; therefore, a timely diagnosis of androgen deficiency and appropriate treatment may have significant effects outside the narrow field of sexual performance.
Changes in hormonal parameters secondary to intravenous administration of Tribulus terrestris extract in primates
- Gauthaman
Gauthaman K, Adaikan PG, Prasad RNV, Goh VHH, Ng SC. Changes in hormonal parameters secondary to intravenous administration of Tribulus terrestris extract in primates. International Journal of Impotence Research 2000;12(Supplement 2):6 (Abstract).
Effect of hypercholestrolemia and some antihypertensive drugs on erectile physiology
- B Srilatha
Srilatha B. Effect of hypercholestrolemia and some antihypertensive drugs on erectile physiology. M. Sc., Thesis. National University of Singapore. 1998; 1 – 173.
Dehydroepiandrosterone (DHEA) and Ageing
- Md Majewska
- Neuronal
- Fl
- Ra Daynes
- Pj Hornsby
- Dh Lavrin
- Nestler
Majewska MD. Neuronal actions dehydroepiandrosterone. In: Bellino FL, Daynes RA, Hornsby PJ, Lavrin DH, Nestler JE, editors. Dehydroepiandrosterone (DHEA) and Ageing. The New York Academy of Sciences, vol. 774. 1995. p. 111 – 20. K. Gauthaman et al. / Life Sciences 71 (2002) 1385–1396 1396
Mount latencies recorded in different groups of rats (n = 8) The results are compared between a) the intact control and rest of the groups, b) the castrated control and rest of the castrated groups. The values are expressed as mean F SEM
- N Vehicle
- C Castrated
- Testosterone
- Tt
N = Normal rat; V = Vehicle; C = Castrated rat; T = Testosterone; TT = Tribulus terrestris extract. Mount latencies recorded in different groups of rats (n = 8). The results are compared between a) the intact control and rest of the groups, b) the castrated control and rest of the castrated groups. The values are expressed as mean F SEM. y and * indicates significant differences (p < 0.05) from control for a and b respectively. References
Selected medicinal plants of India (A Monograph of Identity, Safety and Clinical Usage) Compiled by Bharatiya Vidya Bhavan's Swamy Prakashananda Ayurveda Research Centre for CHEMEXCIL
- Chemexcil Tribulus
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CHEMEXCIL. Tribulus terrestris Linn. (N.O.-Zygophyllaceae). Selected medicinal plants of India (A Monograph of Identity, Safety and Clinical Usage). Compiled by Bharatiya Vidya Bhavan's Swamy Prakashananda Ayurveda Research Centre for CHEMEXCIL. Bombay: Tata Press; 1992. p. 323 – 6 (Ch 100).
Neuronal actions dehydroepiandrosterone
- Md Majewska
- Daynes Ra Bellino Fl
- Hornsby Pj
- Lavrin Dh
- Nestler
- Je
Majewska MD. Neuronal actions dehydroepiandrosterone. In: Bellino FL, Daynes RA, Hornsby PJ, Lavrin DH, Nestler JE, editors. Dehydroepiandrosterone (DHEA) and Ageing. The New York Academy of Sciences, vol. 774. 1995. p. 111 – 20.
Neuronal actions dehydroepiandrosterone
- Majewska