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Pharmacological Evaluation of Ayurvedic Plants for Aphrodisiac Activity in Experimental Animals
Abstract
Vajikaran Chikitsa is the branch of Ashtanga Ayurveda, which deals with all types of physical and psychological sexual problems like impotence, libido, poor erection, and early ejaculation in males. The WHO estimated that the usage of traditional medicine in developing countries is 80% and suggested a need for further exploration of the natural aphrodisiacs for the mechanism of action. Considering the prevalence of the sexual dysfunctioning in the society, side effects with the conventional aphrodisiac drugs, the study was planned to evaluate some Ayurvedic plants like Abutilon indicum and Withania somnifera for the aphrodisiac potential. An attempt was also made to elucidate the possible mechanism of action of these plants for their use in Vagikarana chikitsa. From the present study, it could be concluded that A. indicum and W. somnifera both possessed marked aphrodisiac activity complying many facets such as enhancement in libido, increase in the sexual performance, penile erection and anabolism, increased spermatogenesis as well as sperm validity. Study results pointed out the place of these drugs in the Vajikarana Chikitsa. A. indicum would be useful in management of erectile dysfunction as it had shown to relax penile cavernosal tissue probably by phosphodiesterase inhibition and cGMP accumulation.
... Ex Hiern (Rubiaceae) (Yakubu et al., 2005), Abutilon indicum Linn. SW (Malvaceae), Withania somnifera Dunal (Solanaceae) (Ganu et al., 2010), including the most commonly used spices (Tajuddin et al., 2003(Tajuddin et al., , 2005 have been demonstrated to show aphrodisiac activity that stimulate the mounting behavior, increases anxiety, and the mating performances. Some of these are empirically used as promising aphrodisiacs in traditional medicine practice in cases of sexual debility or depressed desire. ...
... Further, there was an increase observed in ESCs in treated (200 and 300 mg/kg) rats, which is a useful biochemical ''marker'' for testicular activity (Srivastav et al., 2010;Wang et al., 1999). The increased testicular function coincided with elevated weights of androgen-dependent accessory sex organs, sperm production/semen characteristics has shown to interfere with the normal testicular activity by enhancing the libido and sexual behavioral performance indicating testosterone-like effects in rats (Ganguly et al., 1992;Ganu et al., 2010;Thakur et al., 2009c). Interestingly, our results also showed an increase in the testicular activity as well as in androgen-dependent accessory sex organ weights (namely epididymis, prostate, and seminal vesicles) in AARR-treated rats at 200 and 300 mg/kg doses. ...
Context:
Asparagus adscendens Roxb (Liliaceae) has a promising role in modulation of various disorders such as leucorrhea, diarrhea, dysentery, diabetes, senile pruritus, asthma, fatigue antifilarial, antifungal, spermatorrhea, and sexual debility/seminal weakness.
Objective:
To investigate dose-dependent effects of Asparagus adscendens root (AARR) extract on anabolic, reproductive, and sexual behavioral activities with a view to emphasize the pharmacological basis.
Materials and methods:
Rats were divided into five groups: Group I (control), Groups II-IV (AARR treated, 100, 200, and 300 mg/kg body weight, respectively, orally for 30 d) and Group V (standard control treated with sildenafil citrate, 5 mg/kg body weight). On day 31, copulatory and potency tests were carried out and an autopsy was done to study the reproductive function, namely, organ weights, spermatogenesis, daily sperm production rate (DSP), and epididymal sperm counts (ESC).
Results:
AARR extract (200 and 300 mg/kg doses) caused a significant increase in body (p < 0.02 and p < 0.001) and testes (p < 0.01 and p < 0.001, control versus treated) weights. Reproductive activity showed significant a increase in testicular tubular diameter (p < 0.005-0.001), the number of round/elongated spermatids (p < 0.02-0.001), DSP, and ESC (p < 0.05-0.001). The sexual behavioral parameters including mounting/intromission frequency (13.0 ± 0.32/11.8 ± 0.37 and 18.2 ± 2.12/14.8 ± 1.15 versus 11.2 ± 0.66/8.2 ± 1.16), ejaculation latency (187.4 ± 1.91 and 191.4 ± 1.72 versus 180.0 ± 3.47), and penile erections (13.5 ± 0.3 and 14.5 ± 0.5 versus 8.5 ± 0.2) showed a significant increase at 200 and 300 mg/kg doses (ED50 300 mg/kg), but less than a standard control. In contrast, 100 mg/kg dose caused an increase (p < 0.005) in mounting latency only.
Conclusion:
These results indicate increased anabolic, reproductive, and sexual activities by AARR treatment. Thus, the data provide scientific rationale for its traditional use as an aphrodisiac or for sexual disorders.
... Numerous articles mentioned in the references of the Danish report use extracts that have not been prepared according to the part of the plant used and the standards of extracts according to API (Volume-VIII): 1. Patel et al.: [9] The extract was prepared from the powdered root of W. somnifera first with ethanol as extractant and evaporation of the extractant, then with ethyl acetate: None of these components are mentioned in the W. somnifera monograph 2. Ilayperuma et al. [10] do not describe the preparation of the extract. According to the authors, the dose used was 15 times higher than the dose that humans take 3. Ganu et al. [11] do not describe how the extract is prepared. The DTU Food Institute report said that it had included the study by Ganu et al., but here, it must be noted that the study is inadequately described when it comes to extract preparation, experimental design, and results 4. Abdel-Magied et al. [12] do not comply with API standards for aqueous extracts and it is prepared with leaves instead of the root 5. Al-Qarawi et al. [13] investigated the effects of an aqueous extract of the leaves 6. Singh et al.: [14] The authors prepared an ethanol extract (50% ethanol) of the dried stem and do not comply with API standards and uses another part and not the root 7. Mali et al.: [15] Does not comply with API standards and used another part of the plant and not the root as it is a 50% ethanol extract of the fruit of W. somnifera 8. Ahmad et al., Mahdi et al., and Gupta et al.: [16][17][18] do not describe how the extract was prepared 9. Ambiye et al.: [19] It does not describe how the extract was prepared and what type it is 10. ...
Ashwagandha ( Withania somnifera [L.] Dunal) is one of the most renowned Ayurvedic medicinal plants, extensively used in traditional Indian medicine systems such as Ayurveda, Siddha, Unani, and Sowa Rigpa for millennia. Its medicinal uses of the root are documented in ancient texts such as the Charaka samhita , Sushruta samhita , and various Nighantus . Recognized globally, Ashwagandha is included in numerous pharmacopoeias, including the Ayurvedic Pharmacopoeia of India (API), British Pharmacopoeia, and United States Pharmacopoeia. Despite its extensive use and documented benefits, Ashwagandha faced scrutiny in Denmark. The Danish Veterinary and Food Administration banned Ashwagandha based on a 2020 report by the Technical University of Denmark (DTU). This report has been criticized for its technical, scientific, and ethical flaws, including reliance on unverified sources and omission of significant data from authoritative compendiums such as the API. Notably, the report’s references often included studies that did not adhere to established standards for Ashwagandha extracts. Furthermore, the alleged abortifacient properties cited in the Danish report are not supported by extensive reviews of traditional texts and modern scientific literature, which indicates the safety of Ashwagandha when used appropriately. This article aims to provide a comprehensive evaluation of the Danish report, emphasizing the necessity of adhering to rigorous scientific standards and accurately representing historical and contemporary data on Ashwagandha .
... The recurrent or repeated inability of the male to perform a satisfactory sexual function or any disorder that interferes with his full sexual response cycle is termed male sexual dysfunction [9]. Male sexual dysfunction is an important contributor of male infertility with about 30-50% of infertility cases attributed to problems with males alone [10] and there have been reports on the exclusive use of herbal remedies to be one of the most vital approaches accessible to man for the treatment and management of this menace [11][12][13][14]. Although, the acclaimed herbal remedies used in the treatment and management of sexual dysfunctions in humans are useful therapeutically, but the prolonged usage of these herbs without proper evaluation has brought about a number of health challenges affecting many couples all over the world in their quest seeking the fruit of the womb [15]. ...
... It has been acclaimed that aphrodisiacs with a healthy lifestyle can achieve a better sexual life. The sex is the most cherished, indispensable and an integral part of several people and can be a cradle of pleasure and satisfaction [3] . Globally, a happy and successful sex life is considered crucial to their quality of life, and physical and mental wellbeing. ...
Introduction: In general medicine, male sexual dysfunction is a major source of worry and consultation. Finding alternative substances like plants to regulate these disturbances is motivated by the side effects of standard aphrodisiac medicines. In the current investigation, male rats were used to test the aphrodisiac effects of an aqueous extract of Hibiscus asper leaves. Methodology: Aphrodisiac effect of the extract was evaluated following a single daily administration of Hibiscus asper at doses of 50, 100 and 200 mg/kg respectively. Sexual behavioural parameters such as mounting and intromission frequencies, mounting, intromission and ejaculatory latencies, sexual motivation were monitored on days 1, 4 and 8. At the end of the experiment, the grapping test was assessed, after which the animals were sacrificed and blood collected for the evaluation of cholesterol, fructose, proteins, acid phosphatase, testosterone, and other androgen-dependent enzymes. Some androgen-dependent organs, such as the testis, epididymis, seminal vesicle, prostate, and levator ani muscle, were also removed for biochemical and histological analysis. Results: The administration of the aqueous extract of H. asper leaves had a significant impact on sexual behaviour, increasing mounting frequency (MF), intromission frequency (IF), and ejaculatory latency (EL), and reducing mounting latency (ML), intromission latency (IL), and post-ejaculatory interval (PEI). There was also an enhancement in orientational activities, libido, arousal and potency. Cholesterol, acid phosphatase, vesicular fructose, proteins, nitric oxide and testosterone levels were all significantly increased in treated animals. Conclusion: These findings support the traditional use of H. asper leaves to enhance male sexual behavior by demonstrating the aphrodisiac potential of these plants.
... Indeed, sildenafil citrate, the reference molecule used in this study, is a non-androgenic aphrodisiac that acts directly on penile cavernous tissue. It inhibits the activity of phosphodiesterase-5, which prolongs the action of cGMP, the second messenger involved in the erection mechanism, and leads to muscle relaxation [31,32]. ...
Background: Sarcocephalus latifolius, a plant of the Rubiaceae family, is found exclusively in tropical Africa, more particularly in sub-Saharan West Africa, stretching from Senegal to Zaire, but is also found as far east as Sudan (Sudan-Guinean zone). The leaves of this plant are used in traditional African medicine to treat numerous pathologies such as infertility. Aims/Objective: The present study aims to evaluate the effects of the aqueous extract of Sarcocephalus latifolius leaves on sexual parameters in male rats. Methods: The sexual parameters (latency of the mating position, latency of intromission, latency of ejaculation and mean copulation interval) were assessed by the classical method by administering distilled water, sildenafil citrate (reference molecule) called Viagra at the dose of 5 mg/kg of body weight and the aqueous extract of Sarcocephalus latifolius leaves at the dose of 1000 mg/kg of body weight per day for eight days to three batches of male rats respectively. These parameters were determined over a period of thirty minutes. Results: The results obtained show that the aqueous extract of Sarcocephalus latifolius leaves at a dose of 1000 mg/kg of body weight significantly (P < .001) decreases the latency time of mating position and the latency time of intromission, whereas this extract significantly (P < .001) increases the latency time of ejaculation and the average copulation interval. Conclusion: Aqueous extract of Sarcocephalus latifolius leaves has aphrodisiac properties which are due to sterols, flavonoids and saponosides.
... (Kapikachchu) etc. modulate the level of pituitary hormones FSH and LH [21]. Mucuna pruriens L. & Asparagus racemosus (Shatavari) increase brain 5-HT & Melatonin. ...
Background: Vājīkarana - Aphrodisiacs / Virilification Therapy is one branch of Ashtanga Ayurveda. It deals with preservation and promotion of sexual potency of a healthy man, conception of healthy progeny, and management of sexual and reproductive ailments. Vājīkarana drugs have been selected for the present review due to high prevalence of reproductive disorders among young people below age 40 years, recorded neonatal death caused by congenital anomalies and the urgency of effective medicines in the community. Objectives: To identify Vājīkarana drugs mentioned in Bhaisajya Rathnavali and analyze the pharmacodynamics properties of commonly used Vājīkarana drugs. Methodology: The review was mainly based on Vājīkarana drugs mentioned in Bhaisajya Rathnavali by Acharya Govinda Das Sen and commonly used and mostly available drugs have been analyzed according to their pharmacodynamics properties. Collected pharmacodynamics properties from authentic texts and journal articles were tabulated and analysis was done by using SPSS. Results: Out of 67 Vājīkarana formulae, 208 single drugs were identified which included 83.65% of herbal origin drugs and 74.6% of drug formulae were used to increase the sexual power. 37.3% of the formulae were prepared as Churna (Powder) and most frequently used Anupana (Vehicle) was cow’s milk. Among frequently used & commonly available 10 drugs, Maricha - Piper nigrum has been used in majority of formulae (26.8%). Pharmacodynamics analysis revealed that 80% of drugs were Madhura rasa (sweet in taste), 70% were Guru guna (heavy in property), 70% were Shita virya (cold in potency) and 80% were Madhura vipaka (sweet in post digestive action). Based on modern science, 60% of the drugs had tonic action. Conclusion: Vājīkarana formulae mentioned in Bhaisajya Rathnavali were mainly used to increase the sexual power of man. Madhura rasa, Guru guna, Shita virya and Madhura vipaka were the pharmacodynamics properties of commonly used drugs in the formulae.
... Sexual ignorance is a social disease and can be solved via compulsory all-inclusive sex education, which can boost awareness and improve society [4]. However, aphrodisiac has been implicated in treating / managing these arrays of sexual disorders [6][7][8][9]. Most aphrodisiacs can amplify sensual experience facets such as light, touch, smell, taste, and hearing. ...
Energy drink is a type of drink containing sugar and stimulant compounds, usually caffeine or natural stimulants majorly from plant sources. This study evaluates the comparative aphrodisiac and toxicity effect of energy drinks consumption in male wistar rats. Determination of aphrodisiac potential following the oral administration of graded doses (0.5, 1.0, and 1.5 ml/kg) of red-bull, Orijin bitters, and monkey tail. Viagra (Sildenafil citrate) and distilled water served as positive and negative controls, respectively. Sexual behavioural parameters (mounting and intromission frequencies, mounting, intromission, and ejaculatory latencies) were observed. Serum testosterone and cholesterol concentrations were progressively monitored on days 1, 7, 14, and the acute toxicological evaluation of the various energy drinks based on any onset of mortality and behavioural changes. The results showed that red bull increased significantly mounting frequency. A significantly decreased in mounting and intromission latencies in dose-dependent manner, particularly on days 1 and 14. The Orijin bitters revealed a prolonged ejaculatory latency. Testosterone and cholesterol concentrations were also increased as the dose increased, particularly on days 1 and 7. The lowest dose of 0.5 ml/kg showed the best aphrodisiac effect for the Mockite energy drink. The toxicity studies showed that there were no acute behavioural changes with zero mortality. These findings, therefore, validated the claim of the local use of energy drinks as an aphrodisiac in males.
... In this phase, female mice were introduced to the males after 30 min acclimatization in a glass made arena. The analysis of orientation towards female was carried out as indicated by female licking for the period of 1 h following the established method with minor modification (Ganu et al., 2010;Islam et al., 1991). Male mice were observed for 1 h for their orientation activity towards female mice and recorded with the video camera and then noted in the record book. ...
Ethnopharmacological relevance
Aglaonema hookerianum Schott is an ethnomedicinally important plant used to treat a variety of diseases, including sexual and depression-like disorders. However, the scientific basis underlying the aforesaid properties have not been well justified.
Aim of the study
The present investigation aimed to investigate the anxiolytic, antidepressant and aphrodisiac potentials of methanol leaves extract of A. hookerianum (MEAH) in Swiss albino mice.
Materials & methods
Swiss albino mice (20–30 g) were orally administrated with MEAH at the doses ranging from 100 to 400 mg/kg, b.w. The elevated plus maze (EPM) and hole board test (HBT) were performed to determine the anxiolytic activity and the forced swimming test (FST) and tail suspension test (TST) were performed to determine the antidepressant activity of MEAH. Besides, the aphrodisiac activity of MEAH was conducted through the mounting behaviour and orientation behaviour analysis. Diazepam (1 mg/kg, b.w., i.p.) for EPM and HBT; fluoxetine HCl (20 mg/kg, b.w., p.o.) for FST and TST, and sildenafil (5 mg/kg, b.w., p.o.) for the mounting behaviour analysis and orientation behaviour analysis were used as reference drugs.
Results
The administration of the MEAH produced a strong (p < 0.001) dose-dependent anxiolytic effects in both HBT and EPM tests. Likewise, the extract revealed a significant (p < 0.001) reduction in the immobility time in both FST and TST as compared to the control group. Besides, the MEAH also found to possess marked aphrodisiac activity complying several facets such as an increase in the sexual performance at the highest dose (400 mg/kg, p.o.) as well as the orientation toward female mice (p < 0.001) at all tested doses.
Conclusion
Taken together, MEAH can be recommended as a potent source of neuroprotective and a libido-boosting drug candidate for the management of neurological and sexual disorders.
... The extract at 200 and 400 mg/kg exhibited a significant increase in the frequency of penile erection episodes with penile erection index 229 and 332, respectively compared to 350 penile erection index of sildenafil. All the extract doses showed a significant increase in the number of female licking behavior and the mating performance of males in addition to significant increase in the sperm count [126]. ...
AbutilonMiller is a genus belonging to family Malvaceae comprises about 150 species. The plants of this genus are annual or perennial herbs, shrubs or even small trees. It is native to the tropical and subtropical countries of America, Africa, Asia and Australia. The genus has a significant importance, which is attributed to valuable insoluble fibers obtained from different species of the genus such as Abutilontheophrastii and also due to several species grown as garden ornamental plants such as A. ochsenii and A. vitifolium. Reviewing the available literature on genus Abutilonrevealed the presence of a diversity of secondary metabolites such as flavonoids, phenolic acids, sterols, triterpenes, quinones, coumarins, alkaloids, sphingolipids, megastigmanes, iridoids and others, which are responsible for its biological activities such as anti-inflammatory, analgesic, antipyretic, wound healing activities. This review showed that some species of genus Abutilon including A. pannosum, A. mauritianum, A. crispum, A. grandiflorum, A. bidentatum, A. figarianum, A. ochsenii and A. vitifolium need furter phytochemical and pharmacological investigation to develop new drugs from natural sources.
... In animal studies, WS is known to have gonadotropic function which increases gonadal weight by growthing follicles size in female and also increasing seminiferous tubular cell layers in male animals [27,28,31,33,35,37,41,[57][58][59]. WS is found to improve spermatogenic activity which is proposed to be due to supporting hypothalamic-hypophysial-gonadal hormonal axis and testosterone balance in testes [15,31,42]. ...
Introduction
Withania somnifera (WS) also known as ashwagandha is a well-known medicinal plant used in traditional medicine in many countries for infertility treatment. The present study was aimed at systemically reviewing therapeutic effects of WS on the reproductive system.
Methods
This systematic review study was designed in 2016. Required data were obtained from PubMed, Scopus, Google Scholar, Cochrane Library, Science Direct, Web of Knowledge, Web of Science, and manual search of articles, grey literature, reference checking, and expert contact.
Results
WS was found to improve reproductive system function by many ways. WS extract decreased infertility among male subjects, due to the enhancement in semen quality which is proposed due to the enhanced enzymatic activity in seminal plasma and decreasing oxidative stress. Also, WS extract improved luteinizing hormone and follicular stimulating hormone balance leading to folliculogenesis and increased gonadal weight, although some animal studies had concluded that WS had reversible spermicidal and infertilizing effects in male subjects.
Conclusion
WS was found to enhance spermatogenesis and sperm related indices in male and sexual behaviors in female. But, according to some available evidences for spermicidal features, further studies should focus on the extract preparation method and also dosage used in their study protocols.
... It has been acclaimed that aphrodisiacs with a healthy lifestyle can achieve a better sexual life [5]. Sexual feelings are an inevitable part of life. ...
Background
Aloe barbadensis (AB) is a short stemmed succulent medicinal herb that is being used by locals in Nigeria to enhance libido. Therefore this study evaluates the aphrodisiac potential and acute toxicological effect of A. barbadensis (AB) root in male Wistar rats.
Methods
Aphrodisiac potential was determined following the oral administration of graded doses (100, 200 and 400 mg/kg) of ethanol extract of A. barbadensis root. Sildenafil citrate (Viagra) and distilled water served as positive and negative controls respectively. Sexual behavioural parameters (mounting and intromission frequencies, mounting, intromission and ejaculatory latencies) were observed. Serum testosterone and cholesterol concentrations were also progressively monitored on days 1, 7 and 14. The acute toxicological evaluation of the plant were based on any onset behavioural changes and mortality respectively.
Results
The findings from the sexual behavioural study indicated that the ethanol extract of A. barbadensis significantly increased mounting frequency and intromission frequency but significantly decreased mount and intromission latencies in a dose dependent manner particularly on day 1 and 14. The ethanol extract also prolonged ejaculatory latency. The testosterone and cholesterol concentrations were also increased as the dose increased particularly on day 1 and 7. The lowest dose of 100 mg/kg showed the best aphrodisiac effect. The toxicity studies showed that there were no acute behavioural changes with zero mortality.
Conclusion
The increased blood testosterone and cholesterol concentrations by the ethanol extract of A. barbadensis can probably be said to be the possible mechanisms of action for its aphrodisiac property. The plant may also be used to treat hypotestosteronemia following its ability to increase testosterone. These findings therefore give backing to the acclaimed local use of A. barbadensis root as an aphrodisiac in males.
... The extract of S. hypoleuca caused a significant increase in testicular CREM gene expression and protein level in rat (Jasem et al., 2010). It has been shown that Abutilon indicum and Withania somnifera both possessed marked aphrodisiac activity complying many facets such as enhancement in libido, increase in the sexual performance, penile erection and anabolism, increased spermatogenesis as well as sperm validity and had shown to relax penile cavernosal tissue probably by phosphodiesterase inhibition and cGMP accumulation (Ganu et al., 2010). In castrated male rats, both testosterone and dihydrotestosterone (DHT) are very effective in restoring penile erections, but testosterone is most effective in restoring mating behaviour also as compared to DHT, which is totally ineffective (Gray et al., 1980). ...
This study was aimed to investigate the dose-dependent effects of Salvia haematodes Wall roots (SHW) extract on male reproductive function and copulatory behaviour in rats. Sexually mature males were assigned to four groups: control and treated (5, 50 and 300 mg kg(-1) day(-1) for 30 days). At the end of treatment regimes, the reproductive activity viz. body/organ weights, testicular spermatogenesis, daily sperm production rate (DSP) and epididymal sperm counts, and sexual behaviour including mounting latency (ML), mounting frequency (MF), intromission latency (IL), intromission frequency (IF), ejaculation latency (EL), post-ejaculatory interval (PEI) and penile reflexes (PE) were assessed. Results showed significant increase in body weight (at 300 mg kg(-1) ), testis/epididymis weights (at 50 and 300 mg kg(-1) ), testicular spermatids, DSP, tubular diameter and epididymal sperm counts (at 50 and 300 mg kg(-1) doses) in treated compared with control rats. It also produced dose-dependant changes in sexual behaviour. The 5 mg kg(-1) dose of extract increased MF and PE, whereas 50 and 300 kg(-1) doses caused significant increase in MF, IF, PE, EL (but less than sildenafil citrate treatment), hit rate and seminal plug weight. It is concluded that SHW extract enhances anabolic activity, testicular function and sexual behavioural performance in a dose-dependant manner.
Cnestis ferruginea, a plant of the connaraceace family, is well known to the West African population, including that of Côte d'Ivoire, through its common use in traditional medicine. The leaves of Cnestis ferruginea are used in traditional African medicine to treat numerous pathologies, including infertility. The present study aims to evaluate the effects of the aqueous extract of Cnestis ferruginea leaves on sexual parameters in male rats. The sexual parameters (latency of mating, latency of intromission, latency of ejaculation and mean copulation interval) were assessed by the classical method by administering distilled water, sildenafil citrate (reference molecule) called Viagra at the dose of 5 mg/kg and the aqueous extract of Cnestis ferruginea leaves at the dose of 100 mg/kg per day for eight days to three batches of male rats respectively. These parameters were determined over a period of thirty minutes. The results obtained show that the aqueous extract of Cnestis ferruginea leaves at a dose of 100 mg/kg of body weight significantly (p < 0.001) decreases the latency time of mating and the latency time of intromission, whereas this extract significantly (p < 0.001) increases the latency time of ejaculation and the average copulation interval. These results suggest that the aqueous extract of Cnestis ferruginea leaves has aphrodisiac potentialities which are due to the presence of sterols, flavonoids and saponosides in this extract.
Increase in male sexual dysfunction, and its treatment with conventional aphrodisiac drugs with side effects lead to investigate the spermatogenesis and androgenesis augmentative efficacy of hydromethanolic (40 : 60) extract of root of Chlorophytum borivilianum (family - Liliaceae) against cyproterone acetate-induced subfertility in Wistar strain male albino rat. For this purpose, experimental rats were divided into three treatment groups: vehicle (received distilled water), cyproterone acetate (gastric intubation at 250 mg kg(-1) twice daily for 35 days) and cyproterone acetate plus root extract of C. borivilianum (gastric intubation at 250 mg kg(-1) plus 400 mg kg(-1) with an interval of 20 min twice daily for 35 days). After 35-day treatment, all rats were euthanised. Reproductive deviations towards negative side were investigated by screening the spermatogenic and steroidogenic biosensors. Oxidative stress profile in reproductive organs and sperm pellet was evaluated by biochemical assessment of antioxidative enzyme activities and level of end products of the lipid peroxidation. Apoptosis profile was evaluated by Western blot study, TUNEL assay and DNA fragmentation study of testicular tissues. Evaluation of toxicity profile was included for experimental investigation. After cyproterone acetate treatment, the pituitary-testicular axis was deviated towards the negative side and its tuning system was affected by oxidative stress and apoptosis-mediated process, which reduced the quality of semen and finally led to subfertility. Co-administration of C. borivilianum root extract enhanced male reproductive potentiality and prevented the negative deviations after the treatment with cyproterone acetate by means of increasing oxidative defence and maintaining homeostasis in testicular apoptosis process.
Starting from the hypothesis that drugs which specifically activate the hippocampal cholinergic nerve activity may ameliorate memory impairments, we carried out a series of evaluations for a novel cognitive enhancer using enhancement of penile erection as a sign of cholinergic activation, and found FR64822. The compound facilitated penile erection in naive rats, and it ameliorated scopolamine-induced amnesia of rats in passive avoidance tasks with bell-shaped dose-response curves, while it dose-dependently reduced body weight gain in Zucker fatty rats. Pretreatment with sulpiride (32 mg/kg, p.o.) hardly affected the former two activities, but significantly reduced the anorectic activity in Zucker rats. Further evaluation of FR64822 derivatives characterized a second compound, FR121196, which induces penile erection and memory enhancement, but not body weight reduction. Memory enhancing and erection stimulating activities of FR121196 were abolished in rats treated with either cysteamine (200 mg/kg, s.c.), a somatostatin depletor, or lesioning of the serotonergic raphe nuclei. Thus, classic whole animal studies based on a hypothesis proved to be efficient for reaching our objective, the discovery of a new drug. They also gave us insight into the common somatostatinergic and serotonergic mechanisms underlying penile erection and memory improvement.
We set out to establish a simple, reproducible, rat in vitro model of erectile function and to use this to demonstrate the functional importance of both neuronal- and endothelial-derived nitric oxide within this animal. Two corpora cavernosal smooth muscle strips were harvested from sexually mature male Wistar rats and mounted in an organ bath for measurement of isometric tension. Following contraction with noradrenaline the strips were relaxed by the addition of either acetylcholine or sodium nitroprusside. Electrical field stimulation was performed in the presence of atropine and guanethidine. Relaxation responses were repeated in the presence of methylene blue, L-arginine, L-NNA and haemoglobin +/- L-arginine. Methylene blue abolishes the relaxation to acetylcholine and EFS; L-NNA and haemoglobin cause a significant impairment in the relaxation response. L-arginine reverses the effect of haemoglobin. In conclusion, the inhibitory, relaxant stimulus of rat corpora cavernosa is due to both neuronal nitric oxide and endothelial-derived nitric oxide released in response to cholinergic stimulation.
JPM8 is a novel sildenafil-like PDE5 inhibitor. Its efficacy was tested in vivo by the oral administration of drugs to a rat model and recording penile activity changes. Effect on the relaxation of the rabbit cavernosa was tested in vitro using an organ bath were drugs are added to the tissue media and relaxation was recorded using a transducer connected to a chart recorder. The accumulation of cGMP and cAMP was measured by incubation of cavernosa strips and then extracting the produced cGMP and cAMP in the incubation mixture, then quantitating it using ELISA. JPM8 showed increased and promoted sexual and penile activity in rats in a similar but slightly higher trend than the positive control sildenafil. JPM8 was more efficient in relaxing the rabbit corpora cavernosa than sildenafil. The cGMP and cAMP accumulation showed a similar trend for both drugs. We concluded that JPM8 was very effective in promoting sexual activity in rats, relaxing the corpora cavernosa and promoting cGMP accumulation in rabbits.
Aphrodisiacs (sex stimulants) occupy a significant position in most of the ancient systems of medicine including ethnomedicine. They are associated with many myths. In Ayurveda and Unani systems of medicine these drugs have been recognised and given due importance. Ethnobotanical surveys have indicated use of a large number of plants and other items by tribals as aphrodisiacs. Though accepted reluctantly such activity has been confirmed pharmacologically. The paper reviews for the first time, the drugs reported to stimulate sexual functions, mentioned in the classical literature and ethnomedical surveys. Significance, composition and clinical reports of some of the composite herbal drugs available in the market and their aphrodisiac activity have also been reviewed.
The roots of Chlorophytum borivilianum (Liliaceae) Sant. & F. roots are used traditionally in Indian subcontinent as aphrodisiac and sexual stimulant. Ethanolic extract of roots as well as sapogenins isolated from the roots were studied for effect on sexual behavior and spermatogenesis in albino rats. Administration of 100 mg/Kg and 200 mg/Kg b.w. of the sapogenin and ethanolic extract respectively had pronounced anabolic and spermatogenic effect in treated animals as evidenced by weight gains in the body and reproductive organs and histological studies. The treatment also markedly affected sexual behavior of animals as reflected in reduction of mount latency, ejaculation latency, post ejaculatory latency, intromission latency and an increase of mount frequency and attractability towards female.
A 42-year-old male presented with acute onset of an inferior visual field defect OD after sildenafil citrate use. Examination revealed a right relative afferent pupillary defect and a swollen disc with a 0.1 cup-to-disc ratio and a prominent disc hemorrhage. Anterior ischemic optic neuropathy (AION) is associated with acute episodes of hypotension in patients with structurally crowded discs. Sildenafil citrate may cause episodes of hypotension and was temporally related to the onset of symptoms in this patient. Because patients are often reluctant to volunteer their history of sildenafil citrate use, the physician may need to ask specifically about use of this medication. Physicians should counsel patients with crowded optic discs and a history of nonarteritic anterior ischemic optic neuropathy in one eye that use of sildenafil citrate might increase their risk of ischemic optic neuropathy in the fellow eye.
Ayurveda holds a special position amongst the various traditional systems of medicine. Vajikaran is a speciality in Ayurvedic
system of medicine in India dealing with herbs possessing rejuvenative and revitalizing properties for improving sexual dynamics.
In the present study, the effect of five vajikaran herbs on pendiculatory activity and in-vitro sperm count was assessed.
The lyophilized aqueous extracts of Asparagus racemosus Willd., Chlorophytum borivilianum Sant. F., Curculigo orchioides Gaertn., Dactylorhiza hatagirea (D. Don)
Soo and Orchis latifolia
Linn.(200mg/Kg b.w.) were administered orally to wistar strain male albino rats. Following this the effect of all the five drugs
was evaluated for pendiculatory activity. The effect of extract on in-vitro sperm count was also assessed in a separate experiment
where the initial sperm count and count after 30min of incubation was determined. The results show that the herbs could significantly
(P<0.05) improve the pendiculatory activity in male rats after 14days of treatment. Similarly, the extract could also preserve
the in-vitro sperm count significantly when compared to control group after 30min. of incubation. Hence the present study
further supports the use of these plants as vajikaran or aphrodisiac in traditional Indian medicine.
The effect of an ethanolic extract of Salvia haematodes roots was studied on the sexual behaviour of male rats. In the initial experiments, male sexual responses were assessed by recording penile erection, licking and grooming of genitals and copulatory movement in absence of females. In the second set, copulatory behaviour was observed by caging males with a receptive female brought into estrus with s.c. injection of estradiol benzoate and progesterone. The frequencies of mounting and intromission and latency of the ejaculation were recorded. The results show that the extract (500 mg/kg, orally) produced a significant increase in episodes of penile erection. The drug was found to enhance the orientation of males towards the female by increased anogenital investigatory behaviour and enhanced licking and grooming of the genitals. The extract also increased the ejaculation latency. These findings support the folk use of this plant as aphrodisiac and for the treatment of premature ejaculation.
Penile erection is understood to be a neurally regulated physiologic event, although the underlying mechanisms have eluded characterization for more than a century. The classical autonomic parasympathetic and sympathetic nervous systems are involved, but the process of erection does not appear to require cholinergic or adrenergic mechanisms. As the search for the principal mediator of penile erection has continued over time, nitric oxide (NO), a gaseous messenger molecule, has been rapidly advanced to fulfill this elusive role. In the recent past, various biochemical and functional data have accumulated to support this understanding. These have shown that NO is an important mediator of corpus cavernosal smooth muscle relaxation and have revealed its potential sources and mechanisms of action in the penis. Additional work involving animal erection models has established that NO mediates physiologic penile erection. This minireview presents these data and includes results from recent clinical trials that have preliminarily evaluated the efficacy of NO-generating or -releasing compounds for the treatment of erectile dysfunction.
Administration of Trichopus zeylanicus leaf (ethanol extract) to male mice stimulated their sexual behaviour as evidenced by an increase in number of mounts and mating performance. This activity of the ethanol extract was concentration dependent and destroyed by heat treatment at 100 degrees C for 15 min. Although oral administration of a single dose (200 mg/kg) was effective, daily administration of the extract for 6 days was found to be more effective. The pups fathered by the drug treated mice were found to be normal with reference to foetal growth, litter size and sex ratio. The water as well as n-hexane extracts of the plant leaf were inactive. The present study reveals for the first time the aphrodisiac activity of Trichopus zeylanicus, an endemic herb of India.
The relaxant effects of electrical field stimulation (EFS) and exogenously applied acetylcholine (ACh) or acidified NaNO2 (a-NaNO2) were investigated in the isolated mouse corpus cavernosum precontracted with phenylephrine hydrochloride (PE). Tetrodotoxin (TTX) blocked the relaxant effects of EFS completely, whereas it had no effect on the responses to ACh or a-NaNO2. Guanethidine and indomethacin failed to affect the electrically or ACh-induced relaxations. Atropine completely blocked the effect of ACh; however, it caused a slight reduction in the relaxation evoked by EFS.N
G- Nitro-l-arginine (l-NOARG) reduced the effects of EFS and ACh significantly, but it was ineffective on the relaxations induced by a-NaNO2. The inhibitory action ofl-NOARG was partly restored byl-arginine, but not byd-arginine. Methylene blue (MB) and hydroxocobalamin (HC) exhibited significant inhibition on the relaxations evoked by EFS, ACh and a-NaNO2. Hydroquinone (HQ) reduced relaxation due to a-NaNO2, but did not affect that of EFS and ACh. Our findings suggest that EFS-induced relaxations of mouse cavernosal tissue are mediated by a transmitter which probably resembles an organic nitrate.
In human corpus cavernosum, release of nitric oxide from the non-adrenergic, non-cholinergic nerves and/or the endothelium activates guanylyl cyclase and increases intracellular cGMP levels. The increase in intracellular cGMP modulates intracellular calcium and in turn regulates smooth muscle contractility and erectile function. Phosphodiesterases play an important physiological role by regulating the intracellular levels of cyclic nucleotides. In this study, we investigated the kinetic parameters of inhibition of phosphodiesterase (PDE) type 5 (E.C. 3.1.4.35 3',5'-cyclic GMP phosphodiesterase) by a novel, high affinity, selective PDE type 5 inhibitor, sildenafil, in soluble extracts of human corpus cavernosum smooth muscle cells. Sildenafil inhibited PDE type 5 cGMP-hydrolytic activity, in the crude extract (Ki=4-6 nM) and in partially purified preparations (Ki=2 nM) in a competitive manner, as determined by Dixon plots. Sildenafil (Ki=2-4 nM) was a more effective PDE type 5 inhibitor than zaprinast (Ki=250 nM). Stimulation of intracellular cGMP synthesis by the nitric oxide donor, sodium nitroprusside, resulted in less than a 5% increase in cGMP levels in the absence of sildenafil and a 35% increase in cGMP levels in the presence of sildenafil, in intact cells at physiological temperatures. These results are in accord with the clinical observations that sildenafil, taken orally, promotes penile erection through increased intracellular cGMP in response to sexual stimulation, potentiating smooth muscle relaxation.
Sildenafil is a phosphodiesterase-type-5 inhibitor indicated for the treatment of erectile dysfunction in men. We report a case of NAION identified from a cohort of 8,893 patients (from a Prescription-Event Monitoring study) prescribed sildenafil by their primary care physician in England between April and June 1999. This 61-year-old patient had risk factors for NAION independent of drug therapy. It was not possible to be confident about a causal association between sildenafil and NAION, though the possibility could not be ruled out. Epidemiological data suggest that one case of NAION might be expected in a cohort of 8,893 subjects. Thus it remains important for clinicians to consider the range of risk factors for NAION; while equally, the processes of pharmacovigilance need to continue as for any recently launched drug preparation.
In the present study, the aphrodisiac activity of Butea frondonsa Koen. ex Roxb (Papillionaceae) bark extract was investigated. The extract (400 mg/kg body wt./day) was administered orally by gavage for 28 days. Mount latency (ML), intromission latency (IL), ejaculation latency (EL), mounting frequency (MF), intromission frequency (IF), ejaculation frequency (EF) and post-ejaculatory interval (PEI) were the parameters observed before and during the sexual behavior study at day 0, 7, 10, 14, 21, and 28. The extract reduced significantly ML, IL, EL and PEI (p < 0.05). The extract also increased significantly MF, IF and EF (p < 0.05). These effects were observed in sexually active and inactive male rats.
Seven patients, aged between 50 and 69 years, had typical features of nonarteritic anterior ischemic optic neuropathy (NAION) within 36 hours after ingestion of sildenafil citrate (Viagra) for erectile dysfunction. Six patients had vision loss within 24 hours after use of the agent. Final visual acuity in the affected eye ranged from 20/20 to light perception. Both eyes were affected in one individual. All affected individuals had pre-existing hypertension, diabetes, elevated cholesterol, or hyperlipidemia. Seven similar cases have been previously reported. Sildenafil may provoke NAION in individuals with an arteriosclerotic risk profile.
We report on a case of combined nonarteritic anterior ischemic optic neuropathy (NAAION) and cilioretinal artery occlusion resulting from misuse of sildenafil citrate (Viagra Pfizer Pharmaceuticals, New York, NY).
This is an observational case report.
A 54-year-old white man developed blindness in his left eye after an overdose of Viagra. He was examined and fully evaluated.
Ocular examinations revealed a left relative afferent pupillary defect and a left combined NAAION and obstruction of the ipsilateral cilioretinal artery.
Although ocular side-effects of Viagra are rare, they are potentially blinding. Patients should be warned about the side-effects and against misuse of this agent.