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Pro-sexual and Androgen Enhancing Effects of Tribulus terrestris L.: Fact or Fiction
... Puncture vine (Tribulus terrestris L.) is a popular medicinal plant, which is considered as a traditional stimulator of masculine sexual desire. The available reviews concerning this plant do not reflect the recent information (Ukani et al. 1997, Chhatre et al. 2014, Shahid et al. 2016, Zhu et al. 2017, or they are focused on puncture vine's influence and use in man's reproduction (Neychev and Mitev, 2016, GamalEl Din, 2018, Sanagoo et al. 2019, Santos et al. 2019, Abarikwu et al. 2020. Current reviews concerning Tribulus terrestris effect on female reproduction, as well as on non-reproductive physiological and therapeutical actions of puncture vine, are practically absent in the available literature. ...
... Analysis of phytochemical and pharmacological studies on animals and humans revealed an important role of Tribulus in treating erectile dysfunction and sexual desire problems (Neychev and Mitev, 2016) and fertility (Kumari et al. 2018). On the other hand, the performed clinical studies provided controversial and inconclusive results concerning the applicability of this plant for treatment of male infertility. ...
... It suggests that these signaling substances could be intracellular mediators of puncture vine on libido or androgen release. Furthermore, there is emerging compelling evidence from experimental studies in animals for possible endothelium and nitric oxide-dependent mechanisms underlying tribulus terrestris aphrodisiac and pro-erectile activities (Neychev and Mitev, 2016). It is still to be examined whether intracellular signaling mechanisms mediate puncture vine action on human male reproductive processes. ...
Tribulus terrestris, L. (puncture vine) have been used as a folk medicine for five thousands of years, but its targets, effects, their mechanisms and application requires further studies. This paper reviews the provenance, constituents and properties of Tribulus terrestris, L., its general physiological and health effects, as well as the currently available knowledge concerning its influence on male and female reproductive processes and their dysfunctions. Analysis of the available publications demonstrated the influence of Tribulus terrestris on a wide spectrum of targets and physiological processe and disorders. In particular, Tribulus terrestris can be a stimulator of male and female reproductive processes at the level of central nervous system, sexual behaviour, pituitary and gonadal hormones and their receptors, gonadal functions (including ovarian follicullogenesis and spermatogenesis), improvement of the quality and quantity of gametes (at least of sperm) and fecundity. This ability of puncture vine is applicable for the improvement of man’s sexual desire and sperm quality in vivo and in vitro, as well as of women’s libido, activation of women’s reproductive organs, fecundity, and treatment of infertility, especially that related to the polycystic ovarian syndrome.
... Tribulus terrestris (TT) is one of the most controversial plants encountered in the literature. Several studies suggest that the administration of extracts obtained from the fruits could improve sexual performance, improve the symptoms of erectile dysfunction and increase libido in animals and/or humans [1,2]. On the other hand, there is the belief that the administration has no effects on the sexual parameters. ...
... On the other hand, there is the belief that the administration has no effects on the sexual parameters. Supposedly, these extracts could increase athletic performance, but the scientific results seem to be in contradiction [2,3]. The presumed actions are attributed to the high content in steroidal saponins, which are taught to have anabolic effects. ...
... In the first herbal drug (TT-1. [2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17], the concentration of protodioscin was under the limit of quantification (<0.5 µg/g sample). This product was used in the experimental determination as the Tribulus terrestris low protodioscin content extract (TT-LPC). ...
The present project aims to evaluate Tribulus terrestris (TT) extracts by addressing various possible mechanisms of action in order to see whether the use of TT supplements in diabetes and diabetes complications is justified. Diabetic rats were divided into three groups: diabetic control group, TT extract with low protodioscin content group (TT-LPC) and TT extract with high protodioscin content group (TT-HPC). After twelve weeks of treatment, fasting blood glucose, insulin, LH, FSH and testosterone levels were measured. Both TT preparations reduced elevated blood glucose level. Insulin and luteinizing hormone levels were not significantly different compared with the control group; however, the FSH and testosterone levels were significantly higher in the TT-HPC group compared with the diabetic control group. The testosterone level is correlated in part with the protodioscin concentration in extracts and is probably mediated through an FSH-linked pathway.
... [36] Puncture vine (Tribulus Terrestris L.) Animal studies reported a significant increase in serum testosterone levels. [37,38] Selenium Improvement of sperm motility. [39,40] Vitamin D supplementation improved erectile function in middle aged men, and increased serum testosterone levels. ...
... It is widely grown in Africa, Australia, Asia, and Europe, and it is known as goat's head and bull's head. It has a long history of use by Chinese traditional Medicine, Indian medicine (Ayurveda) and traditional medicine of South Eastern Europe for improvement of sexual functions in man [38]. Today, beyond aphrodisiac use, it is commonly used by athletes and bodybuilders, as it is believed that it can enhance testosterone concentrations [37]. ...
... A limited number of animal studies displayed a significant increase in serum testosterone levels after Tribulus terrestris administration, but this effect was only noted in humans when Tribulus terrestris was part of a combined supplement administration. The literature available on the effectiveness of this supplement is surprisingly scarce and more studies for the effectiveness of this supplement are needed [37,38]. Also, there is severe safety concerning, since there are two cases of hepatonephrotoxicity following high dose ingestion in young healthy men, and so patients should be cautioned regarding supplementation with Tribulus terrestris [10]. ...
Background:
Sexual dysfunction and infertility are conditions with high prevalence in general population. Nutritional factors have been reported to have impact in sexual and reproductive health.
Objective:
The aim of this review is to summarize the data on nutritional factors that have influence in male and female sexual and reproductive function, including nutritional status, specific foods (e.g. dairy food), nutrients and other food components and dietary supplements.
Method:
A literature search was performed using Cochrane Library, Medline and ScienceDirect databases without time limitations.
Results:
Obesity has a negative influence in male fertility, and weight loss improves male fertility. Food insufficiency is associated with increased sexual risk behaviours, more significant in women. Regarding to macronutrients and group foods, trans-fatty acids, high glycemic index food, high carbohydrate diet and high animal protein intake prejudices fertility; omega-3 and omega-6 fatty acids, low glycemic index food and low carbohydrate diet, vegetable proteins and antioxidants improves fertility. Isoflavones has a negative impact on men fertility and improves sexual health of menopausal women. Whole milk improves women fertility, but men benefit from skim milk. Concerning to dietary supplements there is weak evidence sustaining efficacy, and the most promising supplements are yohimbine, vitamin B, L-arginine and vitamin D.
Conclusion:
The compiled results indicate that despite the multifactorial etiology of sexual/reproductive dysfunction, nutritional factors may affect the sexual and reproductive health in both men and women. However, it is necessary further studies to clarify this association, and simultaneously improve the approach and treatment of patients with sexual and/or reproductive problems.
... They reported that erectile function improvement is due to the conversion of Protodioscin found in TT extract to dehydroepiandrosterone (DHEA) (41). A literature review by Neychev and Mitev (2016) revealed the effect of TT in treating ED and sexual desire problems. However, the empirical evidence to support the latter hypothesis in which the desirable effects are due to androgen enhancing properties of TT is still inconclusive and largely unknown (45). ...
... A literature review by Neychev and Mitev (2016) revealed the effect of TT in treating ED and sexual desire problems. However, the empirical evidence to support the latter hypothesis in which the desirable effects are due to androgen enhancing properties of TT is still inconclusive and largely unknown (45). One of the strengths of the present study is that it is the first systematic review and meta-analysis which specifically examined the effectiveness and safety of TT on semen parameters and erectile function. ...
... TT has received great attention due to usage as widespread and indiscriminate in treatment of various diseases such as urinary infections, inflammations, sexual dysfunction and desire problems, leucorrhoea, erectile function, oedema, kidney stones, hypertension and coronary heart disease and ascites owing to possessing aphrodisiac, free-radicalscavenging, anti-inflammatory, anti-cancer, antispasmodic, anti-bacterial, antiurolithic and analgesic properties (Akram et al., 2011;Mohd et al., 2012;Hammoda et al., 2013;Kamenov et al., 2017;Ma et al., 2017). Moreover, it has potential to elevate the testosterone, testosterone precursor and luteinizing hormone levels in humans and animals (Gauthaman and Ganesan, 2008;Omitoyin et al., 2013;Neychev and Mitev, 2016;Yeganeh et al., 2017). For these reasons, many studies have been focused on masculinization, growth and reproductive performance, survival and histopathology, feed utilization, hematological, immunological, and biochemical variables in different fish species Kavitha and Subramanian, 2011;Omitoyin et al., 2013;Gültepe et al., 2014, Yilmaz et al., 2014Hassona et al., 2020). ...
... The differences may be related with ecological factors and broodstock (age and weight of the male), spawning (behavior of broodstock and stage of spawning), sampling method and term (Piironen and Hyvarinen 1983;Suquet et al. 1994;Suquet et al. 1998;Tekin et al. 2003;Kocabaş and Kutluyer 2017b). 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). ...
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
... Ștefănescu et al. also credited TT's antioxidant activity to its polyphenols and flavonoids [8]. Studies concentrating on the therapeutic effects of TT have assessed its potential effects on sexual enhancement [12], fertility [13], urinary tract stones [14,15], diabetes [16,17], cardiovascular diseases [18,19], regarding its antioxidant [20,21], and anti-inflammatory properties [22,23]. Although a wide range of clinical studies has assessed the effects of TT on the enhancement of health [12][13][14][15][16][17][18][19][20][21][22][23], there are few randomized clinical trials on the effects of TT on athletes [24] and physically active individuals [25], and also, there is no randomized controlled trial on recreational runners. ...
... Studies concentrating on the therapeutic effects of TT have assessed its potential effects on sexual enhancement [12], fertility [13], urinary tract stones [14,15], diabetes [16,17], cardiovascular diseases [18,19], regarding its antioxidant [20,21], and anti-inflammatory properties [22,23]. Although a wide range of clinical studies has assessed the effects of TT on the enhancement of health [12][13][14][15][16][17][18][19][20][21][22][23], there are few randomized clinical trials on the effects of TT on athletes [24] and physically active individuals [25], and also, there is no randomized controlled trial on recreational runners. Therefore, this study has been designed to assess the efficacy of TT supplement on the nutritional, oxidative, inflammatory, and anti-inflammatory status and sports performance of recreational runners. ...
Background
High intensity and endurance exercises lead to exercise-induced oxidative stress (EIOS), exercise-induced muscle damage (EIMD), and inflammation, which are the influencing factors on muscle soreness, localized swelling, and sports performance decrease. Therefore, the purpose of this study is to determine the effectiveness of Tribulus terrestris (TT) as an herbal supplement with antioxidant and anti-inflammatory properties on the nutritional, oxidative, inflammatory, and anti-inflammatory status, as well as the sports performance of recreational runners.
Methods/design
This study is a double-blind, randomized, placebo-controlled trial, which will be conducted among recreational runners of Tabriz stadiums, Iran. Thirty-four recreational runners will be selected, and participants will be assigned randomly to two groups: to receive 500 mg TT supplement or placebo capsules twice daily for 2 weeks. Both groups will do high-intensity interval training (HIIT) workouts during the study. Baseline and post-intervention body composition, muscle pain, and aerobic and anaerobic performance will be assessed. In addition, assessment of malondialdehyde (MDA), total antioxidant capacity (TAC), total oxidant status (TOS), superoxide dismutase (SOD), glutathione peroxidase (GPx), uric acid (UA), 8-iso-prostaglandin F2α (8-iso-PGF2α), protein carbonyl (PC), catalase (CAT), glutathione (GSH), nitric oxide (NO), high-sensitivity C-reactive protein (hs-CRP), interleukin-6 (IL-6), interleukin-10 (IL-10), tumor necrosis factor-alpha (TNF-α), creatine kinase (CK), myoglobin (MYO), lactate dehydrogenase (LDH), insulin-like growth factor-1 (IGF-1) irisin, cortisol, and brain-derived neurotrophic factor (BDNF) will be done during three blood samplings. Changes in oxidative stress, anti/inflammatory biomarkers, and sports performance will be assessed as primary outcomes.
Discussion
This study will be the first to assess the potential effects of TT on recreational runners. Our results will contribute to the growing body of knowledge regarding TT supplementation on the nutritional, oxidative, inflammatory, and anti-inflammatory status and sports performance in recreational runners.
Trial registration
Iranian Registry of Clinical Trials ( www.irct.ir ) (ID: IRCT20150205020965N8 ). Registration date: 13 February 2021.
... Goat head, hard thorns, and Tribulus are the local names associated with it. T. terrestris is considered as vital component of various countries ancient health care systems i.e., India (Ayurveda), Chinese, and Europe [11]. In China, T. terrestris fruits are considered helpful in preventing kidney problems, cough, and improves the eyesight [12]. ...
... The guidelines of the International Federation of Blood Donor Organizations (IFBDO) were followed, while collecting the blood samples and also authorized by the Bioethical Committee of Bahauddin Zakariya University, Multan, Pakistan (approval number Reg. No. [10][11][12][13][14][15][16][17][18][19][20]. This work was also carried out in conformity with the Helsinki declaration. ...
Tribulus terrestris L. belongs to the family Zygophyllaceae and integral part of various ancient medicinal systems including Chinese, Indian, and European to combat various health ailments. The aim of the present study was to assess the phytochemical constituents, in vitro antioxidant activity using DPPH, FRAP, and H2O2 assays, in vitro anticancer activity using MTT assay, and in vitro and in vivo anti-inflammatory properties of T. terrestris. The acute and sub-acute toxicity of extracts exhibiting most biological potential was examined using murine models. Liquid–liquid partitioning followed by RP–HPLC sub-fraction of crude extract was performed. After that, ESI-MS/MS analysis was done for the timid identification of bioactive metabolites responsible for bioactivities of sub-fractions and HPLC analysis to quantify the compounds using external standards. Among all extracts, T. terrestris methanol extract was noted to hold maximum phenolic (341.3 mg GAE/g) and flavonoid (209 mg QE/g) contents, antioxidant activity in DPPH (IC50 71.4 µg/mL), FRAP (35.3 mmol/g), and H2O2 (65.3% inhibition) assays, anti-inflammatory activities in vitro at 400 µg/mL (heat-induced hemolysis, % inhibition 68.5; egg albumin denaturation, % inhibition 75.6%; serum albumin denaturation, % inhibition 80.2), and in vivo at 200 mg/kg (carrageenan-induced paw edema, % inhibition 69.3%; formaldehyde-induced paw edema, % inhibition 71.3%) and anticancer activity against breast cancer cell (MCF-7) proliferation (IC50 74.1 µg/mL). Acute and sub-acute toxicity studies recorded with no change in body weight, behavior, hematological, serum, and histopathological parameters in treated rats with T. terrestris methanol extracts when compared to control group. Fraction B obtained through liquid–liquid partitioning resulted in more bioactive potential as compared to the parent methanol extract. RP–HPLC analysis of fraction B resulted with four sub-fractions (TBTMF1-TBTMF4), wherein TBTMF3 delineated notable bioactive capabilities as compared to other fractions and parent methanol extract. ESI-MS/MS analysis of TBTMF3 resulted with tentative identification of myricetin, rutin, liquitrigenin, physcion, and protodioscin. It can be stated that T. terrestris is a potential bearing herb and findings of current study further verify the claims made in ancient medicinal systems. However, after investigation of each identified compound, it must be considered for drug discovery.
... They reported that erectile function improvement is due to the conversion of Protodioscin found in TT extract to dehydroepiandrosterone (DHEA) (41). A literature review by Neychev and Mitev (2016) revealed the effect of TT in treating ED and sexual desire problems. However, the empirical evidence to support the latter hypothesis in which the desirable effects are due to androgen enhancing properties of TT is still inconclusive and largely unknown (45). ...
... A literature review by Neychev and Mitev (2016) revealed the effect of TT in treating ED and sexual desire problems. However, the empirical evidence to support the latter hypothesis in which the desirable effects are due to androgen enhancing properties of TT is still inconclusive and largely unknown (45). One of the strengths of the present study is that it is the first systematic review and meta-analysis which specifically examined the effectiveness and safety of TT on semen parameters and erectile function. ...
... Furthermore, the composition and biological activity of TT depends on growth conditions, including soil quality, but also the harvesting period [2]. As shown by Dinchev et al. [3], the highest content of saponins in the aerial parts was met during the preflowering and flowering periods. ...
... Analysis of human and animal evidence 1968-2015 [2] 2016 Phytochemistry NS Only the composition of fruits was discussed [9] 2016 Phytochemistry and pharmacology NS [10] 2017 Phytochemistry and pharmacology NS [11] 2018 ...
The general spread of Tribulus terrestris L. (South Africa, Australia, Europe, and India), the high content of active ingredients (in particular sterol saponins, as well as flavonoids, tannins, terpenoids, phenol carboxylic acids, and alkaloids), and its frequent uses in folk medicine, and as food supplements highlight the importance of evaluating its phytopharmacological properties. There are miscellaneous hypotheses that the species could have a high potential for the prevention and improvement of various human conditions such as infertility, low sexual desire, diabetes, and inflammatory diseases. Worldwide, numerous herbal supplements are commercialized with indications mostly to improve libido, sexual performance in both sexes, and athletic performance. Phytochemical studies have shown great disparities in the content of active substances (in particular the concentration of furostanol and spirostanol saponoside, considered to be the predominant active ingredients related to the therapeutic action). Thus, studies of experimental pharmacology (in vitro studies and animal models in vivo) and clinical pharmacology (efficacy and safety clinical trials) have sometimes led to divergent results; moreover, the presumed pharmacodynamic mechanisms have yet to be confirmed by molecular biology studies. Given the differences observed in the composition, the plant organ used to obtain the extract, the need for selective extraction methods which are targeted at the class of phytocompounds, and the standardization of T. terrestris extracts is an absolute necessity. This review aims to highlight the phytochemical, pharmacological, and toxicological properties of T. terrestris, with a focus on the contradictory results obtained by the studies conducted worldwide.
... 8,9 During the trial period, this preparation showed significant stimulating activity of sexual function, spermatogenesis, and libido. 8,9 According to Neychev and Mitev, 156 studies on animals to determine the stimulating effect of TT extracts can be classified in 3 ways: (1) studies of pituitary-gonadal axis hormones; (2) studies of sexual behavior; (3) studies of biophysical and biochemical aspects of the erectile function effect. Studies conducted on albino rats [157][158][159] overall have shown an increase in ovulation, an improvement of spermatogenesis, and an increase in the number of spermatozoa, spermatogonia, and spermatocytes. ...
... Consistency in saponins profile may resolve the issue with the observed variability in pharmacological action of TT extracts and products. Examples of this variation in the pharmacological action of TT were evident in the publications by Qureshi et al, 52 Neychev and Mitev, 156 Kovac et al, 53 and others. Qureshi et al 52 and Neychev and Mitev 156 reported that the herb's ability to improve erectile dysfunctions in men is incorrect. ...
Tribulus terrestris L. (TT) (puncturevine) is a common weed that grows in many countries worldwide and in some places is considered as a noxious weed. The plant has been used in traditional Chinese and Indian medicines and is now considered as one of the most popular aphrodisiacs. It is known for its healing properties for sexual difficulties, impotence, and human and animal hormonal imbalance. It is also used as a sexual booster. Because of the plant’s active substances that can be used for curing sexual and other disorders, interest in it is increasing, and it is currently one of the most studied medicinal plants. The products and preparations manufactured from the aboveground plant parts are especially popular among athletes and people with health issues and diseases such as hormonal imbalance, sexual problems, heart problems, and various kidney and skin diseases. The aim of this review is a comprehensive and critical assessment of the scientific publications involving TT, with special reference to its chemical constituents and biological properties that may facilitate current understanding and future studies of this fascinating plant species. The objectives of this review were (1) to find knowledge gaps, (2) to discuss critically relevant publications and issues with materials and methods that may be prerequisites for contradictory results, and (3) to identify research and development areas. It was found that some of the studies on TT extracts as aphrodisiacs are controversial. A significant number of research publications claim that TT extracts and nutritional supplements containing TT improve muscle tone, have a common biostimulating effect, and improve spermogenesis. However, there are a growing number of publications that dispute these claims, as there are no empirical data on commonly accepted mechanisms of action. The main biologically active substances in TT are steroidal saponins, flavonoids, alkaloids, and lignan amides, the most studied being the steroidal saponins. Multiyear data on the metabolic profile of the species are generally lacking. There are a variety of methods used for extracting plant material, differences in methodologies and saponin analyses, and scientific instruments that were used. Lack of common standards could be a reason for differences in the pharmacological activity and composition of the TT preparations. Development of standard procedures and methods for collection of plant material and analyses are recommended. Selection and breeding efforts and agronomic studies of promising clones of TT would need to be conducted in order to develop TT as a new crop. This will provide consistency of supply and quality of the feedstock for the pharmaceutical industry and could provide a new cash crop for growers.
... The main phytotherapics promoted to increase T and improve sperm characteristics in humans are: tribulus (Tribulus terrestris L., Zygophyllaceae), maca (Lepidium meyenii Walp., Brassicaceae), long Jack (Eurycoma longifolia Jack, Simaroubaceae), mucuna (Mucuna pruriens (L.) DC, Fabaceae), ashwagandha (Withania somnifera L. Dunal, Solanaceae) fenugreek (Trigonella foenum-graecum L., Fabaceae) and black seeds (Nigella sativa L., Ranunculaceae) (Bhat and Karim, 2010;Chen et al., 2014;Mahdavi et al., 2015;Khanijo and Jiraungkoorskul, 2016;Neychev and Mitev, 2016;Rehman et al., 2016;Talbott et al., 2013). Previous reviews have overestimated the effectiveness of these phytotherapics to favorably influence hormonal parameters, and, to date, the real physiological impact remains unclear (Chhatre et al., 2014;Malviya et al., 2011;Nagulapalli Venkata et al., 2017;Yadav and Baquer, 2014;Zhu et al., 2017). ...
... In addition, four sulphated saponins of tigogenin and diosgenin type have been isolated. Hence, saponin fractions from tribulus have been suggested as substances that may play a significant and favorable role in influencing T and sperm physiology (Kostova and Dinchev, 2005;Neychev and Mitev, 2016). ...
Ethno-pharmacological relevance:
Phytotherapeutic approaches have been widely proposed to improve male health. Despite the well-touted effects of tribulus (Tribulus terrestris L) on men's health, an optimal phytotherapy remains an elusive challenge.
Aim of the review:
We sought to critically analyze the evidence in the phytotherapic literature beyond the effects of tribulus on testosterone (T) concentration and sperm analysis to also include indications for prostate health.
Materials and methods:
A focused literature search was conducted to include studies published in Cochrane, Pubmed, and Web of Science databases between the years 2002 and 2018.
Results:
The use of tribulus and maca (Lepidium meyenii Walp, Brassicaceae) were not scientifically supported to improve serum T levels in men. Moderate evidence supports the use of long Jack (Eurycoma longifolia Jack, Simaroubaceae), mucuna (Mucuna pruriens (L.) DC., Fabaceae), ashwagandha (Withania somnifera (L.) Dunal, Solanaceae), fenugreek (Trigonella foenum-graceum L., Fabaceae), and black seeds (Nigella sativa L., Ranunculaceae) to increase total T and improve seminal parameters. Data suggests an increase in total T with the use of 5000 mg/d of powdered mucuna seed and ashwagandha root (151 and 143 ng/dL, respectively) over a 12-week period in patients with oligozoospermia. The use of mucuna was supported for patients with oligozoospermia to improve sperm parameters, with an increase of 83.3 million/mL observed after use of 5000 mg/d of powdered mucuna seed over a 12-week period. Evidence supporting the use of saw palmetto (Serenoa repens, (W.Bartram) Small, Arecaceae) to improve prostate health remains equivocal; whereas, evidence supporting the use of Pygeum africanum Hook.f., Rosaceae, Urtica dioica L., Urticaceae, beta-sitosterols, pollen extract, onion, garlic, and tomato, appears favorable and promising.
Conclusion:
Scientific evidence supports the use of mucuna and ashwagandha as phytotherapics for improving serum T concentrations and semen parameters. Despite inconclusive evidence for use of tribulus as a T booster, it may provide advantageous effects on sperm parameters in men with idiopathic infertility. Nutraceutical strategies and some phytotherapics may also be effective to promote prostate health. Popular foodstuffs (onion, garlic, and tomato), nutraceutical agents (pollen extract and beta-sitosterols), and herbal medicines (Pygeum africanum and Urtica dioica) are rational approaches.
... T. terrestris extracts are the main ingredients of different commercial sex enhancers, so, this study was designed to explain "Can T. terrestris be used in sexual herbal supplements as an active ingredient and if the answer is positive, which extract should be applied. There are two review articles in literatures [9,10], which have evaluated the sexual and androgen enhancing effects of T. terrestris. The first review article on studies up to 2013 concluded its ineffectiveness on testosterone level, and insufficient evidence of human studies for its effectiveness on sexual functions [9]. ...
... The first review article on studies up to 2013 concluded its ineffectiveness on testosterone level, and insufficient evidence of human studies for its effectiveness on sexual functions [9]. The second review article on clinical trials from 1982-2014 has recommended the further investigations on it [10]. In this review article, the clinical and preclinical studies were investigated up to November 2017 that opened a new window on efficacy of T. terrestris in sexual function. ...
Background
Tribulus terrestris (Zygophyllaceae family) is believed to have aphrodisiac activity in different cultures.
Objective
The aim of this study was to evaluate the efficacy of T. terrestris in the management of sexual functions in female and male patients.
Methods
We searched in PubMed Central, Science Direct, Wiley, Springer, SID, accessible books, reports, and thesis.
Results
According to the results of animal and human studies, standard T. terrestris improved erectile parameters. After administration of T. terrestris, an increase in testosterone level was observed in most animal studies, while this increase was not confirmed in male human studies. T. terrestris improved the sperm parameters in animal and human studies. T. terrestris enhanced the folliculogenesis and improved polycystic ovary syndrome (PCO) in animal studies. The human clinical studies confirmed its efficacy on female sexual disorders.
Conclusion
Therefore, standard T. terrestris extract as a valuable herbal compound can be considered an improvement of sexual functions in both sexes.
... Tribulus terrestris contains steroidal glycosides (A -trillin, B -ruskogenin monoside, C -dioscin, Ddioscinin, and longipetalosides A-C) [15][16][17], furastanol saponins (chloromaloside, terrestoneiside, trillin, dioscine, protodioscin, terfyranosides, and others) [13,[18][19][20][21][22][23] flavonoids (rutin, kaempferol-3-rutinoside, rhamnetin-3-rutinoside, isorhamnetin-3-rutinoside, tamaraxetin-3-rutinoside, azaleatin-3-rutinoside) [24,25], alkaloids, vitamin C, resinous substances, fatty oil, coumarins, and dyes [26]. Therefore, Tribulus terrestris contains various classes of compounds. ...
Furostanol saponins from Tribulus terrestris may be separated from ballast substances by liquid-liquid extraction with changing polarity of the extractant, depending on the dynamics of the process. Treatment with chloroform removed the maximum number of lipid-like compounds and showed minimal losses of furostanol saponins, and subsequent treatment with ethyl acetate retrieved low-polarity substances. Fourfold extraction with butanol was used to extract furostanol saponins from an aqueous solution. Optimal conditions were developed for spray drying of furostanol saponins. The greatest yield of "Dry extract Tribulus" was obtained with a solution feed rate of 80 l/h, a spray head rotation speed of 8000 rpm, and a heat carrier velocity of 2000 kg/h. Technology was developed for obtaining "Dry extract Tribulus" from Tribulus terrestris that contained at least 45% furostanol saponins. The reproducibility of the developed technology was shown with the obtaining of 5 series of substances that meet the requirements of regulatory and technical documentation on the lines of the Scientific and Technological Center for GMP Requirements the Institute of Chemistry of Plant Substances.
... The improvement of sexual organ weights with the co-administration of the plant extracts might be attributed to their active constituents and antioxidant potentials (El-Wakf et al., 2015;Kumari and Singh, 2015). Additionally, T. terrestris possesses aphrodisiac and pro-sexual activities because of its capability of increasing the testosterone and testosterone precursor levels which enhance the weight and size of sexual organs including the testes, epididymis, and accessory gland (Neychev and Mitev, 2016). The weight, size, and secretory function of the testis, epididymis, accessory sex organs (seminal vesicles, ventral prostate), and vasa differentia are strictly controlled by androgens (Aladakatti et al., 2011). ...
The current study is aimed at evaluating the potential health benefits of Salvia officinalis L. (sage) methanol extract on lead and nicotine hydrogen tartrate-induced sperm quality degeneration in male rats and also identifying some of the non-polar volatile bioactive compounds that might be attributed to the bioactivity of S. officinalis extract using gas chromatography-mass spectrometry (GC-MS). In the study, fifty-four mature male albino rats of about 220 - 250 g [were divided randomly and equally into 9 groups (n=6)]. Sperm quality degeneration was induced through the oral administration of 1.5 g/L of lead acetate in drinking water or peritoneal injection of 0.50 mg/kg (animal weight) nicotine hydrogen tartrate for sixty days. Two doses (200 & 400 mg/kg b.w.) of S. officinalis L. were used. Twelve major compounds were identified. Lead and nicotine toxicity had a great effect on the rats' sperm quality causing a significant (p<0.05) decrease in the quantity of sperm and sperm motility as well as an upsurge in the abnormalities of the sperm and a reduction in the length & diameter of seminiferous tubules and size & weight of sexual organs. The administration of S. officinalis L. methanol extract ameliorates the adversative effects of lead and nicotine.
... It is used to re-cover visual sharpness and epilepsy in Traditional Chinese Medicine (TCM) while used for its applications as diuretic, stimulant, and aphrodisiac properties in Indian herbal medicine. The TCM name of T. terrestris fruit is ''Ji Li" which holds for several activities, such as activities against heart diseases (Neychev and Mitev 2016), eye inflammation, skin irritation (Reshma et al., 2016), and abdominal distention. The main use of the plant in Europe and the USA is for the increase in muscle strength and improvement of sexual function (Saleem et al., 2020;Angelova et al., 2013), whereas in China, it is used for the treatment of cardiovascular diseases (Ștefa˘nescu et al., 2020). ...
Metabolomics has been used as a powerful tool for the analysis, and drug-lead identification in medicinal plants and herbal medicines. For the coverage of a broader range of plant-based metabolites using LC-MS, one of the important parameters is the selection of analysis mode and data processing for identification. This paper describes the utility of two distinctive acquisition modes in combination, a classic data-dependent acquisition (DDA) mode and a data-independent acquisition (DIA) mode for obtaining the mass spectrometry data of plant extracts using LC-ESI-QTOF/MS. Tribulus terrestris plant was used as a case study. We have applied three-step data analysis pipeline 1-annotation and putative identification of metabolites, 2-validation, and relative quantification, and 3-multivariate analysis using open-access MS-DIAL, Skyline, and Perseus software. A total of four samples of T. terrestris (aqueous extracts), two fruits, and two whole plant samples, from two different regions, were used. By combining data analysis results of plant fruit samples from two different regions, a total of 95 and 77 metabolites were identified in positive and negative ionization modes, respectively. Similarly, in the analysis of the whole plant from two different regions, 75 and 76 metabolites were identified in positive and negative ionization modes, respectively. We suggested the use of DDA mode for annotation, identification of metabolites, and generation of transition lists in MS-DIAL, furthermore, the use of DIA acquisition mode for enhancing metabolites sensitivity in complex samples, deconvolute MS1/MS2 spectra in Skyline for the quantitative performance and analytical reliability. The developed protocol can be used for the broader coverage of plant-based metabolites.
... Medicinal plants have been traditionally employed for their health-improving characteristics for many years. The belief that natural medicines might improve general health and help people overcome chronic diseases has fueled a global interest in plant-based supplements (Neychev and Mitev, 2016). There is a strong interest in plants that enhance male fertility due to the widespread male fertility deficiency caused by multiple factors, including environmental pollutants. ...
... Tribulus Terrestris is an herb belonging to the Zygophyllaceae family distributed across the regions of southern Europe, southern Asia, throughout Africa, New Zealand, and Australia. It possesses various pharmacological properties and roots and fruits have been used for thousands of years in China as a folk medicine [12]. Tribulus Terrestris is rich in steroidal saponins, flavonoids, glycosides, phytosterols, tannins, terpenoids, and among them, steroidal saponins (spirostanol, furostanol) and flavonoids (quercetin, kaempferol, isorhamnetin) are considered to be the most important metabolites with various bioactivities. ...
... The improvement of sexual organ weights with the co-administration of the plant extracts might be attributed to their active constituents and antioxidant potentials (El-Wakf et al., 2015;Kumari and Singh, 2015). Additionally, T. terrestris possesses aphrodisiac and pro-sexual activities because of its capability of increasing the testosterone and testosterone precursor levels which enhance the weight and size of sexual organs including the testes, epididymis, and accessory gland (Neychev and Mitev, 2016). The weight, size, and secretory function of the testis, epididymis, accessory sex organs (seminal vesicles, ventral prostate), and vasa differentia are strictly controlled by androgens (Aladakatti et al., 2011). ...
Ethnopharmacological relevance
The use of herbal and medicinal plants to treat male infertility is well known in history. Tribulus terrestris L. (TT) belongs to the Zygophyllaceae family and it is used in folk medicine to vitalize and also improve both physical performance and sexual function in men in addition to the protective effect of the gross saponins of TT against ischemic stroke and its clinical anti-inflammatory property.
Aim of the study: This study aimed to investigate the effects of methanol extract of T. terrestris on nicotine hydrogen tartrate and lead-induced degeneration of sperm quality in male rats and to identify the volatile bioactive non-polar compounds thought to be responsible for its activity using gas chromatography-mass spectrometry (GC-MS).
Materials and methods
The effect of T. terrestris on nicotine hydrogen tartrate and lead-induced infertility was evaluated in male rats. Fifty-four mature male albino rats weighing 220–250 g body weight were used. The rats were randomly divided into 9 equal groups (n = 6). Infertility was induced by administering nicotine hydrogen tartrate (0.50 mg/kg) through peritoneal injection (i.p.) or lead acetate (1.5 g/L) orally with drinking water for sixty days. Two doses (50 and 100 mg/kg body weight of the animal) of T. terrestris were also used. At the end of the experimental period, the rats were anesthetized and sacrificed. Blood samples were collected. Hormonal analyses were carried out on the serum. The testicle, epididymis, and accessory sex organs (seminal vesical and prostates) were removed for histopathological analysis. Gas chromatography-mass spectrometry (GC-MS) analysis of the methanol extract was also carried out to identify major volatile compounds in T. terrestris methanol extract.
Results
Nicotine and lead toxicity caused a significant (p < 0.05) decrease in the number of sperm, motility, and an increase in the sperm abnormalities such as the reduction in weight and size of sexual organs (testis, epididymis, and accessory sex glands), reduction of diameter and length of seminiferous tubules. The administration of T. terrestris methanol extract, however, improved the semen quantity and quality, sexual organ weights, and fertility of male rats and, thus, ameliorated the adverse effects of nicotine and lead. Ten major compounds were found from the GC-MS analysis of the extract of T. terrestris methanol extract.
Conclusion
Findings showed that T. terrestris plant methanolic extracts ameliorated nicotine hydrogen tartrate and lead-induced degeneration of sperm quality in male rats. The GC-MS analysis of the T. terrestris plant methanolic extracts revealed the presence of several important bioactive compounds which were thought to be responsible for the ameliorative effect. Further isolation and evaluation of the individual components would provide relevant lead to finding new drugs.
... T. terrestris consists of active extracts and constituents which could effectively improve sexual function through activating aphrodisiac and improves fertility in men. T. terrestris has the ability to increase testosterone or testosterone precursor levels (Neychev and Mitev, 2016). ...
... Tribulus terrestris grows in south-eastern Europe, tropical Asia and Africa [13]. TT is a common medicinal plant from ancient times [14]; in China, fruits of TT are usually used as a tonic for the kidney, also, it can be used as a cough expectorant, a medicine that improves eyesight as well as treatment of pruritus and vertigo [13]. In Indian folk medicine, the TT fruits are utilized for treating infertility, impotence, erectile dysfunction and poor libido. ...
Tribulus terrestris saponins (TTS) have been longley used as an overall tonic and recent studies showed they influence inflammatory conditions. We examined the ameliorative effect of a commercial formula of a saponin-rich extract of TT in a model of dietary obesity in female rats focusing on their ability to control the inflammatory burden, insulin resistance (IR), adipokine expression and the related reproductive system pathologies. Female rats were fed with high fat diet (HFD) for 14 weeks to launch diet-induced obesity; they were assigned as: the obese control female rats (OFR) which received no treatment and TTS (5 and 10 mg/kg/day) treated rats; they were compared to a normal rat group. We determined the IR index, serum/tissue inflammatory cytokines, and adipose tissue adipokine expression and examined the secondary ovarian pathologies. Body weight gain, serum triglycerides and IR (>5-fold) in the OFR group were greater than the normal group; TTS lessened these parameters compared with the OFR group. TTS, at 10 mg/kg dose, ameliorated mRNA expression of leptin and visfatin genes in addition to serum inflammatory cytokine levels. Moreover, TTS corrected the hyperprolactinemia and other hormonal disturbances and ameliorated the ovarian pathologies. This study highlighted that the anti-inflammatory properties of TTS helped in alleviation of IR and body weight gain in OFR. Upon correction of obesity manifestations, the gonadal hormone dysregulations and ovarian pathologies were subsequently ameliorated. We can consider TTS as a promising candidate that may alleviate the inflammatory burden, IR and adipokine expression in obesity and hence prevent the secondary gonadal complications in female subjects if appropriate clinical studies are available.
... It is generally assumed that the aphrodisiac and sexual function enhancement properties of Tribulus terrestris can be attributed to its ability to increase testosterone or its precursor levels (Neychev and Mitev, 2016). In animal studies of Tribulus terrestris, a significant increase was observed in serum testosterone levels in tandem with an improvement in sexual function (Sahin et al., 2016;Singh et al., 2012). ...
Background
: Female sexual dysfunction (FSD) includes female orgasmic disorder, female sexual interest or arousal disorder, and genito-pelvic pain or penetration disorder. FSD affects 40% of women worldwide, but it is understudied and likely undertreated. Natural products are frequently used by women to treat FSD, but scientific evidence of their efficacy is lacking.
Objective
: This systematic review and meta-analysis focused on the study of the efficacy of natural products on FSD.
Study design
: Systematic review and meta-analysis of existing studies on natural products in the treatment of FSD.
Methods
: The literature search included MEDLINE, EMBASE, PsycINFO, and the Cochrane Central Register of Controlled Trial databases for studies published from January 2000 to February 2020. The quality and the level of evidence of the studies were assessed. The association between natural products and FSD was summarized using standardized mean differences (SMD) with a 95% confidence interval (CI).
Results
: A total of 536 studies were identified, with 20 of them meeting the criteria. According to this meta-analysis, Tribulus terrestris showed a significant positive effect in improving overall female sexual function (SMD = 1.12, 95% CI = 0.46 - 1.79, p = 0.001) and individual sexual arousal (SMD = 1.03, 95% CI = 0.22 - 1.84, p = 0.013), sexual desire (SMD = 1.08, 95% CI = 0.52 - 1.63, p = <0.001) and sexual orgasm (SMD = 0.51, 95% CI = 0.02 - 1.00, p = 0.040) domains compared to placebo. Panax ginseng was found to be effective in treating sexual arousal (SMD = 0.54, 95% CI = 0.11 - 0.97, p = 0.014) and sexual desire (SMD = 0.59, 95% CI = 0.27 - 0.90, p < 0.001) compared to placebo. Meanwhile, other natural products reviewed in this study, such as Trifolium pretense, did not differ significantly from placebo in terms of improving FSD.
Conclusion
: Preliminary evidence suggests that Tribulus terrestris and Panax ginseng may be effective as alternative treatments for FSD in a clinical setting.
... De acordo com os efeitos possivelmente gerados pelos fitoterápicos, encontra-se a ação ergogênica, no qual, tem acarretado esperança para os indivíduos que se encontram com um dos problemas de saúde mais significativos pela população, à infertilidade e disfunção sexual(Sahin et al., 2016). Medicamentos à base de plantas medicinais tem obtido um grande espaço nas opções de tratamento, passando a cooperar juntamente com medicamentos alopáticos, como exemplo, Tribulus terrestris (TT), um fitoterápico que apresenta atributos afrodisíacos capazes de reproduzir a função dos hormônios sexuais, com isso, a procura do TT pelos indivíduos que buscam uma melhoria na relação sexual vem aumentando atualmente(Neychev et al., 2015). ...
... De acordo com os efeitos possivelmente gerados pelos fitoterápicos, encontra-se a ação ergogênica, no qual, tem acarretado esperança para os indivíduos que se encontram com um dos problemas de saúde mais significativos pela população, à infertilidade e disfunção sexual(Sahin et al., 2016). Medicamentos à base de plantas medicinais tem obtido um grande espaço nas opções de tratamento, passando a cooperar juntamente com medicamentos alopáticos, como exemplo, Tribulus terrestris (TT), um fitoterápico que apresenta atributos afrodisíacos capazes de reproduzir a função dos hormônios sexuais, com isso, a procura do TT pelos indivíduos que buscam uma melhoria na relação sexual vem aumentando atualmente(Neychev et al., 2015). ...
... Tribulus terrestris L. (TT, Zygophyllaceae family), which contains active components including alkaloids, steroidal saponins, flavonoids, tannins, amino acids, quinines, and phenolic compounds, is a commonly used traditional Chinese herbal medicine, also known as Bai Jili in Chinese, for treating various diseases including hypertension, edema, eye problems, sexual dysfunction, and rheumatoid arthritis in clinics for thousands of years [13,14]. e prosexual, cardiac-protective, muscle protective, neuroprotective, and osteoprotective effects of TT were most studied in the recent years [14][15][16][17][18][19], and the anti-inflammatory effect of TT might contribute to these broad range of biological effects [13]. In our previous studies, we have established multiple drug screening models using zebrafish, such as proangiogenesis [20,21], antiangiogenesis [22], cerebral hemorrhage [23,24], and neuroprotection [25,26]. ...
Inflammation response is a regulated cellular process and excessive inflammation has been recognized in numerous diseases, such as cardiovascular disease, neurodegenerative disease, inflammatory bowel disease, and cancer. Tribulus terrestris L. (TT), also known as Bai Jili in Chinese, has been applied in traditional Chinese medicine for thousands of years while its anti-inflammatory activity and underlying mechanism are not fully elucidated. Here, we hypothesize Tribulus terrestris L. extract (BJL) which presents anti-inflammatory effect, and the action mechanism was also investigated. We employed the transgenic zebrafish line Tg(MPO:GFP), which expresses green fluorescence protein (GFP) in neutrophils, and mice macrophage RAW 264.7 cells as the in vivo and in vitro model to evaluate the anti-inflammatory effect of BJL, respectively. The production of nitric oxide (NO) was measured by Griess reagent. The mRNA expression levels of inflammatory cytokines and inducible nitric oxide synthase (iNOS) were measured by real-time PCR, and the intracellular total or phosphorylated protein levels of NF-κB, Akt, and MAPKs including MEK, ERK, p38, and JNK were detected by western blot. We found that BJL significantly inhibited fin transection or lipopolysaccharide- (LPS-) induced neutrophil migration and aggregation in zebrafish in vivo. In mice macrophage RAW 264.7 cells, BJL ameliorated LPS-triggered excessive release of NO and transcription of inflammatory cytokine genes including tumor necrosis factor-alpha (TNF-α), interleukin-6 (IL-6), and interleukin-1 beta (IL-1β). BJL also reduced the LPS-induced elevations of intracellular iNOS and nuclear factor kappa B (NF-κB) which mediate the cellular NO and inflammatory cytokine productions, respectively. Moreover, LPS dramatically increased the phosphorylation of Akt and MAPKs including MEK, ERK, p38, and JNK in RAW 264.7 cells, while cotreatment BJL with LPS suppressed their phosphorylation. Taken together, our data suggested that BJL presented potent anti-inflammatory effect and the underlying mechanism was closely related to the inhibition of Akt/MAPKs and NF-κB/iNOS-NO signaling pathways.
1. Background
Inflammatory response defenses the foreign attacks including tissue injury, pathogens, infections, and irritants and restores normal tissue function [1]. It plays a pivotal role in the physiological process of immunomodulation [2], and excessive inflammation response is also the main pathological feature in numerous chronic diseases, including cardiovascular disease, neurodegenerative disease, inflammatory bowel disease, rheumatoid arthritis, and cancer [3]. Many types of inflammatory cells, such as neutrophils, eosinophils, macrophages and mononuclear phagocytes, are involved in the inflammatory response [1]. The blood resident neutrophil is commonly the primary cell that migrates to the inflammatory position and initiates inflammatory action [4]. It is well-known that macrophages interact with neutrophils and clean the damage tissue and the other inflammatory cells by phagocytosis and consequently suppress the inflammation action [5, 6]. However, macrophages produce proinflammatory cytokines, such as TNF-α, IL-6, and IL-1β, which mediate by the transcript factor NF-κB during the tissue repairing process [7, 8]. The production of NO is an important feature of inflammatory response mediated by macrophages, which causes cell oxidative damage and is dramatically regulated by iNOS [9]. The transcription of iNOS gene is regulated by various transcript factors including NF-κB, activator protein-l (AP-l), interferon regulatory factor 1 (IRF1), and signal transducer and activator of transcription 1 (STAT1) [10]. Moreover, the activation of Akt/MAPKs signaling cascade was considered as one of the important physiological procedures on LPS-induced inflammation both in macrophage and zebrafish [11, 12]. Thus, pharmacological inhibition of Akt/MAPKs and NF-κB/iNOS-NO signaling pathways might be effective for the suppression of tissue injury during inflammatory response.
Tribulus terrestris L. (TT, Zygophyllaceae family), which contains active components including alkaloids, steroidal saponins, flavonoids, tannins, amino acids, quinines, and phenolic compounds, is a commonly used traditional Chinese herbal medicine, also known as Bai Jili in Chinese, for treating various diseases including hypertension, edema, eye problems, sexual dysfunction, and rheumatoid arthritis in clinics for thousands of years [13, 14]. The prosexual, cardiac-protective, muscle protective, neuroprotective, and osteoprotective effects of TT were most studied in the recent years [14–19], and the anti-inflammatory effect of TT might contribute to these broad range of biological effects [13]. In our previous studies, we have established multiple drug screening models using zebrafish, such as proangiogenesis [20, 21], antiangiogenesis [22], cerebral hemorrhage [23, 24], and neuroprotection [25, 26]. Zebrafish also has been supposed as one of the wildly used anti-inflammatory drug screening in vivo models, with several advantages including low cost, easy observation, and short test period [4, 27, 28]. In the present study, we evaluated the anti-inflammatory effect of BJL in zebrafish in vivo and mice macrophage RAW 264.7 cells in vitro, and the action mechanisms were also partially elucidated.
2. Materials and Methods
2.1. Ethic Statement
Zebrafish were kindly provided by Prof. Simon Lee from University of Macau and maintained by the Laboratory Animal Service Center, Longhua Hospital, Shanghai University of Traditional Chinese Medicine. All experiments were in accordance with the Longhua Hospital-Animal Experimentation Ethics Committee of Shanghai University of Traditional Chinese Medicine.
2.2. Chemicals
Lipopolysaccharide (LPS) was bought from Sigma Aldrich (St. Louis, USA). Nitric oxide (NO) detection kit was supplied by Beyotime Biotechnology (Shanghai, China). Primary and secondary antibodies were bought from Cell Signaling Technology (MA, USA). The whole plant of Tribulus terrestris L. (TT) was identified by the Pharmacy Department, Longhua Hospital. Tribulus terrestris L. extract (BJL) was prepared by Shanghai Institute of Materia Medica, Chinese Academy of Sciences (Shanghai, China). Briefly, TT was dried and smashed. 100 g TT powder was boiled within 1200 ml distilled water for 1 h and the supernatant was collected. The TT powder was continually boiled with 800 ml distilled water for 1 h and the supernatant was collected. These two supernatants were combined and stored at 5–10°C for 12 h. Then, the crude TT extract was filtered and absorbed by macroporous resin (1400, 2 : 1). Finally, the macroporous resin was washed by 60% ethanol, and the eluate was concentrated and sprayed to avoid dehydration. The yield of TT extract (BJL) was 4.92%. The chemical profile of BJL was analyzed by high performance liquid chromatography (HPLC) and is presented in supplementary materials (Figure S1). BJL was dissolved in dimethyl sulfoxide (DMSO) while other drugs were prepared in MiliQ water.
2.3. Zebrafish Maintenance and Morphological Observation
The transgenic zebrafish line Tg (MPO:GFP), which expresses green fluorescence protein (GFP) in neutrophils [29], was employed for anti-inflammatory activity evaluation. Zebrafish were maintained under a stander condition according to the zebrafish book (A guide for the laboratory use of zebrafish Danio (Brachydanio) rerio, by Monte Westerfield, Institute of Neuroscience, University of Oregon). Zebrafish embryos were generated by natural breeding and culture in embryo media at 28.5°C in an incubator. Three DPF (day post fertilization) zebrafish embryos were distributed in a 12-well plastic plate with 10 embryos in each group. On the fin transection model, zebrafish embryos were treated with various concentrations (3, 10, and 30 µg/ml) of BJL for 2 h, and then zebrafish embryos were cut fins using a sharp needle. Then, zebrafish embryos were incubated with BJL for another 2 h, and the number of fluorescent cells migrated to wound was observed under a fluorescent stereoscopic microscope (Nikon SMZ18, Japan). On the LPS-injection model, zebrafish embryos were injected with LPS (0.3 µg/ml), and then zebrafish embryos were treated with various concentrations (3, 10, and 30 µg/ml) of BJL for 24 h. The fluorescence intensity of injection site in each embryo was calculated by Image J.
2.4. Cell Viability and Nitric Oxide (NO) Release Assay in RAW 264.7 Macrophage
The mice macrophage RAW 264.7 cell line was purchased from the American Type Culture Collection (ATCC) and cultured in Dulbecco’s modified Eagle’s medium (DMEM) supplemented with 10% FBS and 1% penicillin/streptomycin at 37°C in a humidified atmosphere of 5% CO2 in air. RAW 264.7 cells were seeded in a 96-well plate with a density of 2 × 10⁴ cells/well and further cultured for 24 h. RAW 264.7 cells were treated LPS (0.3 µg/ml) with various concentrations (3, 10, and 30 μg/ml) of BJL for 24 h. The cell viability was measured by MTT assay. The supernatant medium was used for NO release assay by total NO detection kit (Griess reagent, Beyotime Biotechnology). The results were presented as the percentage or folds of the control group.
2.5. Western Blot Analysis
RAW 264.7 cells were seeded in 60 mm × 15 mm Petri dish with a density of 5 × 10⁵ cells/dish and incubated for 24 h and then treated BJL (30 μg/ml) with or without LPS (0.3 μg/ml) for 24 h. After drug treatment, the RAW 264.7 cells were washed with ice cool PBS 3 times and lysed by RIPA buffer (Beyotime Biotechnology) on ice. The cell samples were collected and centrifuged (12000 g) for 15 min at 4°C. The supernatant of each sample was transferred to a new ice cool tube and its protein concentration was determined by BCA kit (Thermo Fisher). Each sample was denatured for 5 min at 95°C after adding the 5 × loading buffer (Beyotime Biotechnology). 30 μg protein of each sample was applied for the protein separation by SDS-PAGE electrophoresis (Bio-Rad). Then, the separated protein was transferred to a PVDF membrane (0.22 μm) by the semidry transfer system (Bio-Rad). The membrane was blocked by 5% skim milk in PBST for 2 h and then followed by primary antibodies including NF-κB, Akt, Phospho-Akt, ERK1/2, Phospho-ERK1/2, p38, Phospho-p38, JNK, Phospho-JNK, and GAPDH (1 : 1000, Cell Signaling Technology) incubation over night with gentle shacking at 4°C. The membrane was washed with PBST 3 times and incubated with HRP-linked secondary antibody for 2 h at room temperature. Finally, the membrane was washed with PBST 3 times and imaged by the AM600 image system (GE Healthcare) after adding the ECL chemiluminescence substrate (Bio-Rad). The intensity of each band was calculated by Image J.
2.6. Real-Time PCR Analysis
RAW 264.7 cells were seeded in 60 mm Petri dish with a density of 5 × 10⁵ cells/well and incubated for 24 h at 37°C in a humidified atmosphere of 5% CO2 in air. RAW 264.7 cells were treated BJL (30 μg/ml) with or without LPS (0.3 μg/ml) for 24 h. The total RNA of each group was extracted by the TriPure Isolation Reagent (Roche, Manneheim, Germany) and their RNA concentrations were detected and calculated by absorbance at 260 nm using Microplate Reader (Tecan M200, NanoQuant). The first stranded cDNA was synthesized by cDNA synthesis kit (Roche, Manneheim, Germany). Finally, the mRNA expression level of interested gene was detected by real-time PCR with specific primers (Table 1) under the SYBR green-based real-time PCR system (Roche, LC96). The mRNA expression level of each gene was calculated by 2−∆∆Ct relative quantification method with 3 independent replicates.
Accession number
Gene
Forward primer
Reverse primer
NM_013693.3
TNF-α
5′-TTC TCA TTC CTG CTT GTG G-3′
5′-ACT TGG TGG TTT GCT ACG-3′
NM_031168.2
NM_001314054.1
IL-6
5′-GAG GAT ACC ACT CCC AAC AGA CC -3′
5′-AAG TGC ATC ATC GTT GTT CAT ACA-3′
NM_008361.4
IL-1β
5′-AGA GCA TCC AGC TTC AAA T-3′
5′-CAT CTC GGA GCC TGT AGT G-3′
NM_001313922.1
NM_001313921.1
NM_010927.4
iNOS
5′-CATTGATCTCCGTGACAGCC-3′
5′-CATGCTACTGGAGGTGGGTG-3′
NM_008084.3
NM_001289726.1
GAPDH
5′-CCT TCC GTG TTC CTA CCC-3′
5′-CAA CCT GGT CCT CAG TGT AG-3′
... В предыдущем исследовании нами было показано, что прием Правенора ® Форте в течение 1 мес достоверно и клини чески значимо повышает все домены шкалы МИЭФ 5, улуч шает показатели пенильной гемодинамики, увеличивает кон центрацию общего тестостерона и снижает концентрацию эс традиола у пациентов с ЭД. Указанные клинические эффекты Правенора ® Форте можно объяснить сразу несколькими био логическими механизмами, а именно: повышением доступно сти субстрата для NO синтаз -L аргинина [3], проандроген ной активностью экстракта якорцов стелющихся (Tribulus terrestris) [4], замедлением апоптоза клеточных элементов пе щеристой ткани и оптимизацией обменных процессов в NO продуцирующих нервных волокнах под влиянием гинкго би лоба (Ginkgo biloba) [5], антиадренергическим и эндотеллин подобным действием йохимбины гидрохлорид (Pausinystalia yohimbe) [6]. Кроме перечисленных выше компонентов в со став Правенор ® Форте входят экстракты крапивы двудомной (Urtica dioica) и ягод карликовой пальмы (Saw palmetto), дав но и успешно применяющиеся у пациентов с ДГПЖ. ...
... Low androgen levels or abnormalities in androgen receptors were partially account for ED (19). Testosterone as the most important androgen in men, plays an effective role in the treatment of ED (20,21). About 44% of testosterone combined to serum sex hormone-binding globulin (SHBG) to form testosterone without biological activity and bioavailable testosterone (Bio-T) did affect sexual function (22). ...
Background:
To investigate the relationship between serum sex hormones and erectile dysfunction (ED), changes in erectile function and sex hormones were studied in patients with chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS).
Methods:
A total of 171 patients with CP/CPPS who met the inclusion criteria from January 2016 to June 2019 were retrospectively analyzed. The level of patient's testosterone (TT), estradiol (E2), luteinizing hormone (LH), follicle stimulating hormone (FSH), prolactin (PRL), premature ejaculation diagnostic tool (PEDT) score and international index of erectile function (IIEF-5) score were separately observed and compared.
Results:
Among 171 eligible patients, 131 (76.61%) cases were diagnosed as ED and 40 (23.39%) cases were normal. Between the ED and No-ED groups, the PRL and PEDT score were statistically significant (P<0.01) based on the test results. ED-dependent and PEDT-dependent receiver operating characteristic (ROC) analysis and decision curve analysis (DCA) were performed on different degrees of ED to determine the predictive performance and clinical applicability. The results showed that PRL can better predict the possibility of ED in CP/CPPS patients than PEDT.
Conclusions:
For CP/CPPS patients, the Prolactin level decreases as the degree of ED increases. Prolactin can be used as a predictor to better predict the possibility of ED in CP/CPPS patients.
... Among these, protodioscin and protogracillin are thought to confer TT's unique biological activities [46]. The main pharmacological activities of saponins in TT include its effects on lowering blood pressure, lowering blood lipid, and protecting the cardiovascular system against myocardial ischemia [47][48][49]; improving the apoptosis rate of ischemic brain nerve cells, protecting brain nerve, enhancing memory and antidepressant effect, reducing blood glucose and diabetes-induced apoptosis of optic nerve cells in diabetic mice [50][51][52][53]. Some studies have reported that the saponins from TT could improve primary mice retinal ganglion cells (RGCs) survival when cultured in vitro [38,54]. ...
Oxidative stress on retinal pigment epithelial (RPE) cells has been confirmed to play a crucial role in the development and progression of age-related macular degeneration (AMD) or other retinal degenerative diseases. Tribulus terrestris (TT) is a Chinese traditional herb medicine, which has been used for the treatment of ocular diseases for many centuries. In this study, we investigated the underlying mechanisms of TT and examined its ability to protect and restore the human retinal pigment epithelial cells (ARPE-19) against H2O2-induced oxidative stress. Our data show that 200 μg/mL of ethanol extract of Tribulus terrestris (EE-TT) significantly increased the cell viability and prevented the apoptosis of H2O2-treated ARPE-19 cells through the regulation of Bcl2, Bax, cleaved caspase-3, and caspase-9. Treatment with EE-TT also significantly decreased the upregulated reactive oxygen species (ROS) activities and increased the downregulated superoxide dismutase (SOD) activities induced by H2O2 in ARPE-19 cells. Additionally, H2O2 at 1 mM significantly decreased the mRNA expression levels of Nrf2, CAT, SOD1, SOD2, HO-1, GST-pi, NQO1, and GLCM in ARPE-19 cells; however, treatment with EE-TT reversed the downregulated mRNA expression levels of all these genes induced by H2O2. Furthermore, treatment with 200 μg/mL EE-TT alone for 24 h significantly increased Nrf2, HO-1, NQO1, and GCLM mRNA expressions in ARPE-19 cells when compared with untreated control cells. Pretreatment with the inhibitor of PI3K/Akt signaling (LY294002) completely blocked these EE-TT-upregulated mRNA expressions and abolished the improvement of cell viability in H2O2-treated ARPE-19 cells. These findings all suggest that Tribulus terrestris has significant antioxidant effects on oxidative stressed ARPE-19 cells through regulating PI3K/Akt-Nrf2 signaling pathway.
... Because of its content in steroidal saponins the extracts from Tribulus terrestris (TT) are consumed as anabolic and sexual enhancers (Zhu et al., 2017). Protodioscin is thought to be responsible for the main pharmacologiocal actions of TT products, although contradictory results have been obtain in the recent years regarding the pharmacological effects, especially the anabolic effect (Neychev & Mitev, 2016). This suggest either that the herbal drugs collected from different regions contain significantly different compounds, or that the experiments were performed with extracts with different organs from TT. ...
Tribulus terrestris L. (TT) became a very popular plant due to its effects in sexual disorders. The pharmacological actions seem to be related with its content in sterolic saponins. Protodioscin has been reported to be the main compound from TT products with anabolic effects. Because of the popularity of the plant, numerous herbal supplements are consumed around the world. Quantification of steroidal saponins through HPLC methods is sometimes difficult. Several methods have been proposed but not all are reproducible. The aim of this study was to validate a LC MS/MS method for quantification of protodioscin in herbal supplements. Two herbal supplements found on the Romanian market have been chosen for this study. The compounds were separated on a C18 column with ammonium acetate buffer and acetonitrile as mobile phase. The ionization was performed in electrospray negative mode and detection of protodioscin was made by monitoring the sum of ions m/z 737.41, m/z 739.42 and m/z 755.42. In one of the herbal supplements, protodioscin was under the limit of quantification. In conclusion a simple and rapid method is proposed for the quantification of protodioscin in herbal supplements.
... The hallucinogenic and narcotic properties associated with symbolic cultural rituals clearly depend on the brain and nervous system activities that are mediated by brunfelsamidine [19], cuscohygrine [23], scopolamine [24], and even scopoletin [27][28][29], the last two sometimes exerting opposite effects. With respect to the traditional custom of associating this plant with increasing energy, wisdom, or marksmanship, the authors had to take into consideration the activity currently being studied in the furostan saponines (i.e., about their capacity to induce pro-sexual and androgenic enhancing effects [34]). ...
This study’s objective was to evaluate the rescued traditional knowledge about the
chiricaspi (Brunfelsia grandiflora s.l.), obtained in an isolated Canelo-Kichwa Amazonian community in the Pastaza province (Ecuador). This approach demonstrates well the value of biodiversity conservation in an endangered ecoregion. The authors describe the ancestral practices that remain in force today. They validated them through bibliographic revisions in data megabases, which presented activity and chemical components. The authors also propose possible routes for the development of new bioproducts based on the plant. In silico research about new drug design based on traditional knowledge about this species can produce significant progress in specific areas of childbirth, anesthesiology, and neurology.
... Recently, male reproductive functions are widely improved through phytotherapeutic approaches [56]. Tribulus (Tribulus terrestris L., Zygophyllaceae) is the main phytotherapics which is promoted to increase testosterone and improve sperm characteristics in humans [57][58][59][60], long Jack (Eurycoma longifolia Jack, Simaroubaceae) [61,62], fineleaf fumitory (Fumaria parviflora Lam. Ranunculales) [11]., Onion (Allium cepa L. Amaryllidaceae) [63] and black seeds (Nigella sativa L., Ranunculaceae) [64,65]. ...
Background:
Infertility and gonadal dysfunction are well known side-effects by cancer treatment in males. In particularly, chemotherapy and radiotherapy induced testicular damage, resulting in prolonged azoospermia. However, information regarding therapeutics to treat spermatogenesis disturbance after cancer treatment is scarce. Recently, we demonstrated that Goshajinkigan, a traditional Japanese medicine, can completely rescue severe busulfan-induced aspermatogenesis in mice. In this study, we aimed to detect the effects of Goshajinkigan on aspermatogenesis after irradiation.
Methods:
This is animal research about the effects of traditional Japanese medicine on infertility after cancer treatment. C57BL/6 J male mice received total body irradiation (TBI: a single dose of 6Gy) at 4 weeks of age and after 60 days were reared a Goshajinkigan (TJ107)-containing or TJ107-free control diet from day 60 to day 120. Then, two untreated females were mated with a single male from each experimental group. On day 60, 120 and 150, respectively, the sets of testes and epididymis of the mice in each group after deep anesthetization were removed for histological and cytological examinations.
Results:
Histological and histopathological data showed that 6Gy TBI treatment decreased the fertility rate (4/10) in the control diet group; in contrast, in the TJ107-diet group, the fertility rate was 10/10 (p < 0.05 vs. 6Gy group). Supplementation with TJ107 was found to rescue the disrupted inter-Sertoli tight junctions via the normalization of claudin11, occludin, and ZO-1 expression and reduce serum anti-germ cell autoantibodies.
Conclusions:
These findings show the therapeutic effect on TBI-induced aspermatogenesis and the recovering disrupted gonadal functions by supplementation with TJ107.
... Tribulus terrestris (Zygophyllaceae) is a perennial plant native to Southern Europe and both tropical and temperate climates across Africa and Asia [61,62]. The herb has been used in Indian and Chinese medicine for centuries and has recently garnered the attention of European and North American markets [1]. ...
Purpose of Review
In this review, we revisit and evaluate empirical research on six herbal supplements purported to affect sexual and/or reproductive function in men and women.
Recent Findings
We summarize and critically review recent evidence—both human and non-human—supporting the role of six commonly cited herbs on men’s and women’s sexual health, identifying possible mechanisms of action, as well as gaps in the literature.
Summary
Burgeoning interest in phytochemical research over the past decade has helped to elucidate potential mechanisms of action through which these plant-derived supplements may exert pro-sexual benefits. More methodologically rigorous, large-scale clinical trials are still needed to determine the extent to which encouraging findings in rodent, cell culture, and ex vivo models are generalizable to human populations.
... By contrast, Roaiah and co-workers [23] assert that Tribulus may be considered as a therapeutic option for ED patients with PADAM syndrome (partial androgen deficiency in aging male) because it can increase both the IIEF-15 score and serum testosterone levels. A recent review has also reported that Tribulus has a positive effect on both libido and erectile function, although data on its androgenic properties are still partial and not conclusive [24]. ...
... Claims are frequently made that Tribulus improves testosterone production; however, clinical trials have not supported this assumption except in intravenous use in primates. [103][104][105][106] Animal studies have shown that Tribulus may improve erectile function and NO production. 107,108 One RCT of 180 men with mildto-moderate ED using 500 mg of standardized T. terrestris taken three times daily reported improved libido, ED, intercourse satisfaction, and orgasm quality. ...
Erectile dysfunction (ED) is common with aging. Formerly ED treatment was offered mainly by urologists, but the approval and widespread use of phosphodiesterase inhibitors has enabled primary care clinicians to provide targeted ED treatment. Although large, multicenter clinical trials have shown efficacy and safety with these drugs, they are ineffective in 30–35% of men, may cause sideeffects, and do not improve the underlying pathology. A thorough understanding of erectile physiology and causes of ED and a comprehensive treatment plan addressing all contributing factors may be more effective than pharmaceutical management and may improve aspects of psychological and physical health beyond erectile problems.
... The hallucinogenic and narcotic properties associated with symbolic cultural rituals clearly depend on the brain and nervous system activities that are mediated by brunfelsamidine [19], cuscohygrine [23], scopolamine [24], and even scopoletin [27][28][29], the last two sometimes exerting opposite effects. With respect to the traditional custom of associating this plant with increasing energy, wisdom, or marksmanship, the authors had to take into consideration the activity currently being studied in the furostan saponines (i.e., about their capacity to induce pro-sexual and androgenic enhancing effects [34]). ...
This study's objective was to evaluate the rescued traditional knowledge about the chiricaspi (Brunfelsia grandiflora s.l.), obtained in an isolated Canelo-Kichwa Amazonian community in the Pastaza province (Ecuador). This approach demonstrates well the value of biodiversity conservation in an endangered ecoregion. The authors describe the ancestral practices that remain in force today. They validated them through bibliographic revisions in data megabases, which presented activity and chemical components. The authors also propose possible routes for the development of new bioproducts based on the plant. In silico research about new drug design based on traditional knowledge about this species can produce significant progress in specific areas of childbirth, anesthesiology, and neurology.
The use of nutraceutical products to enhance male sexual performance has a long history, especially with regard to the treatment of erectile dysfunction (ED). Alternative treatments for ED are becoming increasingly popular, with growing interest from consumers, as well as increased revenue for manufacturers. Dietary supplements (DSs), which are a mixture of active ingredients, are mainly sold online. In randomized controlled trials, the molecules contained in DSs have demonstrated varying degrees of effectiveness, or even have no evidence to support their use. However, none of the studies carried out provided sufficient evidence to consider these products a first-line therapy. Therefore, the combination of the various active ingredients, especially in relation to the daily dose, leaves doubts about the real effectiveness. In order to evaluate the potential efficacy of DS formulations, we analyzed the products marketed in Italy using a scoring approach. A systematic review of the literature was performed to evaluate the effect of DS and to detect the active ingredients able to improve erectile function—called effective ingredients (EIs)—and their minimal effective daily dose (mED). A metanalysis identified some nutraceuticals, such as Panax ginseng, Tribulus terrestris and L-arginine, that are able to improve male sexual function. Based on the scoring system, 2 (8%) supplements matched with the cluster of higher expected efficacy, 3 (12%) with the lower efficacy cluster and 20 (80%) matched with the criterion of no expected efficacy. DSs marketed in Italy are usually blends of many substances that are frequently employed at a negligible dose or without any evidence.
Tribulus terrestris L. seems to be a globally grown annual shrub pertaining to family Zygophyllaceae and worldwide used as aphrodisiac and boosting physical performance in men as it upregulates the testosterone levels that are involved in enhanced muscular growth and physical performance. From centuries it has been successfully used for formulating various folk and herbal medicines in Pakistan, Sudan, India, and China. It contains rich blend of some rare and scientifically captivating bioactive phytochemicals, like flavonoids and saponins that possess tremendous therapeutic potential. This review will cover different aspects of TT in terms of its traditional use, biochemistry and pharmacological effects related to its use that will help in extending the medicinal use of this herb.Keywords
Tribulus terrestris
Medicinal plantTherapeutic potentialPhytochemicalsPharmacology
Tribulus terrestris L. is an herbaceous plant native to India, widely used as a natural sexual stimulant by traditional medicine in China, India, and Greece, and also for the treatment of various diseases for example low blood pressure, cardiovascular diseases, kidney, and skin diseases, etc. Tribulus extracts are rich in numerous biologically active compounds, such as steroidal saponins, alkaloids, lignan amides, and flavonoids, which are useful for the effective treatment of sexual performance, hormonal and sexual problems. The main goal of our in vitro study was to demonstrate the potential consequences of Tribulus terrestris L. extract on TM3 cell parameters such as cell viability, membrane integrity, lysosomal activity, and steroid hormone secretion. The extract was applied to mice Leydig cells at various concentrations (ranging from 37.5 µg/mL to 600 µg/mL) for 24 h. Based on the obtained data, we may claim statistically significant inhibition of cell viability at 300 µg/mL (P < 0.0001) and 600 µg/mL (P < 0.0001). At the same concentrations, there was a statistically significant decline in both cell membrane integrity (P < 0.05; P < 0,0001) and lysosomal activity (P < 0.05; P < 0.001). Hormone secretion was significantly increased at 200 µg/mL (P < 0.05). To better understand how Tribulus terrestris L. affects the reproductive systems of animals or humans, further research must be done.
Tribulus terrestris, L. (puncture vine) have been used as a folk medicine for five thousands of years, but its targets, effects, their mechanisms and application requires further studies. This paper reviews the provenance, constituents and properties of Tribulus terrestris, L., its general physiological and health effects, as well as the currently available knowledge concerning its influence on male and female reproductive processes and their dysfunctions. Analysis of the available publications demonstrated the influence of Tribulus terrestris on a wide spectrum of targets and physiological processe and disorders. In particular, Tribulus terrestris can be a stimulator of male and female reproductive processes at the level of central nervous system, sexual behaviour, pituitary and gonadal hormones and their receptors, gonadal functions (including ovarian follicullogenesis and spermatogenesis), improvement of the quality and quantity of gametes (at least of sperm) and fecundity. This ability of puncture vine is applicable for the improvement of man’s sexual desire and sperm quality in vivo and in vitro, as well as of women’s libido, activation of women’s reproductive organs, fecundity, and treatment of infertility, especially that related to the polycystic ovarian syndrome.
The oral administration of Tribulus terrestris and Lepidium meyenii extracts on reproductive, biochemical and body parameters was evaluated in rats. Thirty-six male Wistar rats weighting 210 ± 18 g were divided into six experimental groups (n = 6). Each group received, daily for 28 days, different solutions: T. terrestris (100 mg/kg), L. meyenii (1 g/kg) and T. terrestris at doses of 75, 50 and 25 mg/kg combined with L. meyenii at doses of 0.25, 0.5 and 0.75 g/kg, respectively, and distilled water (control). T. terrestris increased (p < 0.05) the serum testosterone, regardless of dose. Combined use of the extracts increased (p < 0.05) the diameter of the epididymal duct and epididymis lumen. The combinations of T. terrestris (75 and 50 mg/kg) with L. meyenii increased (p < 0.05) the sperm concentration. There were no differences (p > 0.05) in the other semen characteristics; relative weight of organs; and serum levels of urea, creatinine, alanine and aspartate transaminase, gamma glutamyl transferase, cholesterol, triglycerides, glucose, follicle-stimulating hormone and luteinizing hormone. No histopathological changes were observed (p > 0.05). It is concluded that the association of T. terrestris and L. meyenii has positive effects on serum testosterone, sperm concentration and epididymal morphology, with no evidence of effects in the testis, liver, spleen and kidneys.
Ethnopharmacological relevance
Fructus Tribuli (FT) has been commonly used as a traditional medicine for thousands of years. With the diverse uses of FT, more attention has been paid to its hepatorenal toxicity. However, the compounds causing the hepatorenal toxicity of FT remain undetermined. Terrestrosin D (TED), a major spirostanol saponin isolated from FT, may exert hepatorenal toxicity.
Aim of the study
This study aimed to evaluate the potential hepatorenal toxicity of TED, and preliminarily explore the possible mechanism of TED-induced hepatorenal toxicity.
Materials and methods
Cytotoxicity assays, a repeated-dose 28-day in-vivo study, a toxicokinetic study, and a tissue distribution study were used to evaluate the potential hepatorenal toxicity of TED. Furthermore, network pharmacology was applied to preliminarily explore the possible mechanism of TED-induced hepatorenal toxicity.
Results
Both the in vitro and in vivo studies showed that the spirostanol saponin TED had potential hepatorenal toxicity. Nonetheless, hepatorenal toxicity induced by oral treatment with TED at a dosage range of 5 – 15 mg/kg daily for 28 consecutive days to Sprague-Dawley (SD) rats was reversible after 14 days of TED withdrawal. The toxicokinetic study demonstrated that the systematic exposure of SD rats to TED had an accumulation phenomenon and a dose-dependent trend after a 28-day repeated-dose oral administration. The tissue distribution study revealed that TED had a targeted distribution in the liver and kidneys accompanied by a phenomenon of accumulation in SD rats. Network pharmacology combined with molecular docking methods was used to screen for the key targets (HSP90AA1, CNR1, and DRD2) and the key pathways of TED-induced hepatorenal toxicity.
Conclusions
The spirostanol saponin TED, a major spirostanol saponin isolated from FT, had potential hepatorenal toxicity.
Tribulus (Tribulus terrestris) is an annual plant in the caltrop family with small woody fruit having long sharp and strong spines. Both the root and fruit of the plant have been used medicinally in traditional Chinese medicine and Ayurvedic medicine for their phytochemical and pharmacological activities. Tribulus may be beneficial for hypertension, coronary artery disease, hyperlipidemia, diabetes, polycystic ovary syndrome, and male and female sexual dysfunction; however, it does not improve athletic performance or bodybuilding. Because this herb’s target symptoms render it more prone to overdosing, it is important to educate patients about its potential toxicities. This chapter examines some of the scientific research conducted on tribulus, both alone and in combination formulas, for treating numerous health conditions. It summarizes results from several human studies of tribulus’ use in treating cardiovascular, cardiometabolic, genitourinary, and vitality disorders. Finally, the chapter presents a list of tribulus’ active constituents, different Commonly Used Preparations and Dosage, and a section on “Safety and Precaution” that examines side effects, toxicity, and disease and drug interactions.
Background: High intensity and endurance exercises lead to exercise-induced oxidative stress (EIOS), exercise-induced muscle damage (EIMD), and inflammation, which are the influencing factors on muscle soreness, localized swelling, and sport performance. Therefore, the purpose of this study is to determine the effectiveness of Tribulus terrestris (TT) as an herbal supplement with antioxidant and anti-inflammatory properties on the nutritional, oxidative stress, and anti/inflammatory status, as well as the sport performance of recreational runners.
Methods/design: This study is a double-blind, randomized, placebo-controlled trial, which will be conducted among recreational runners of Tabriz stadiums, Iran. Thirty-four recreational runners will be selected, and participants will be assigned randomly to two groups: to receive 500 mg TT supplement or placebo capsules twice daily for two weeks. Both groups will do the high-intensity interval training (HIIT) workouts during the study. Baseline and post-intervention body composition, muscle fatigue, and soreness parameters will be assessed. In addition, assessment of malondialdehyde (MDA), total antioxidant capacity (TAC), superoxide dismutase (SOD), high-sensitivity C-reactive protein (hs-CRP), interleukin-6 (IL-6), interleukin-10 (IL-10), creatine kinase (CK), lactate dehydrogenase (LDH), insulin-like growth factor-1 (IGF-1) and brain-derived neurotrophic factor (BDNF) will be done during three blood samplings.
Discussion: This study will be the first to assess the potential effects of TT in recreational runners. Our results will contribute to the growing body of knowledge regarding TT supplementation on the nutritional, oxidative stress, anti/inflammatory status and sport performance in recreational runners.
Trial registration: Iranian Registry of Clinical Trials (www.irct.ir) (ID: IRCT20150205020965N8). Registration date: 13 February 2021.
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.
We evaluated the efficacy of Tribulus terrestris in two different dosage regimes for the treatment of sexual dysfunction in pre and postmenopausal women and its effect on the vascular resistance of the clitoral artery using Power Doppler. A total of 104 women were randomly assigned to receive 94mg, three times/day (TT3) or 280mg once/day for 90 days (TT1). Evaluation was performed using FSFI and QS-F questionnaires, serum levels of prolactin, TSH, total testosterone and SHBG, and clitoral artery assessment with Power Doppler ultrasound. FSFI results demonstrated an improvement in all domains in both groups (P < 0.05) except for the “Satisfaction” in the TT3 premenopausal group. QS-F results showed a significant improvement in the mean total score in women of both reproductive phases, for both groups. Postmenopausal patients improved in all sexual domains, except for “orgasm” in the TT1 group. PI of the clitoral artery showed no difference in both reproductive phases, in both groups. We conclude that TTerrestris can be a safe alternative for the treatment of sexual dysfunction in pre and postmenopausal women as it is effective in reducing the symptoms with no side effects. Moreover, its use, increased total, free and bioavailable testosterone.
Just as natural saponins transform into aglycones, secondary glycosides, and their derivatives using biotransformation technology, steroidal saponins may also undergo similar transformation after stir‐frying. Purpose of this study was to elucidate the variations and its reasons in contents of steroidal saponins in Fructus Tribuli (FT) during a stir‐frying treatment. Stir‐fried FT was processed in different time‐temperature conditions. An UHPLC‐MS/MS method was established and fully validated for quantitative analysis. In addition, the simulation processing products of tribuluside A, terrestroside B, terrestrosin K, terrestrosin D, and 25R‐tribulosin were carried out for the qualitative analysis using UHPLC‐Q‐TOF‐MS. The established UHPLC‐MS/MS method provides a rapid, flexible, and reliable method for quality assessment of FT. The present study revealed that furostanol saponins with a C22‐OH group (FSOH) could transform into corresponding furostanol saponins with a C‐20‐C‐22 double bond (FSDB) via dehydroxylation. Additionally, FSDB could be successively converted into its secondary glycosides via a deglycosylation reaction. The transformation of spirostanol saponins into corresponding aglycones via deglycosylation led to a decrease in spirostanol saponins and an increase in aglycones. The results of this research provided scientific evidence of variation and structural transformation among steroidal saponins. These findings might be helpful for elucidating the processing mechanism of FT.
Tribulus terrestris (TT) Linn. is an annual medicinal plant that belongs to the Zygophyllaceae family. TT has been mainly planted in the subtropical regions of Pakistan, India, China, Mexico, Spain and South America. It has been extensively used to improve physical performance and sexual functions in men. All parts of the plant have been used as a traditional medicine in various regions of the world. The plant contains phytochemicals like flavonoids and saponins that possess pharmacological activities. As an example, the saponins present in TT possess anti-proliferative and anti-tumor function. The fruit of the plant is used for the treatment of abdominal and urogenital infections. The present study aims to summarize the pharmacological, traditional, medicinal and therapeutic potential of TT.
Background
Tribulus terrestris Linn. (TT) is reported for its ability to improve male sexual performance, and protodioscin is responsible for the activity. This study was designed to correlate and compare various extracts of Indian TT with Bulgarian TT, and also the effect of protodioscin content on the activity.
Methods
Bulgarian TT extract (BT) and prepared solvent extracts [aqueous (WIT), supercritical fluid (SIT) and methanol (MIT)] of Indian TT were standardized and compared using UV spectrophotometric method. Forty male rats were randomized into 5 groups of 8 each. Group I served as untreated control and group II to V were treated with 100 mg/Kg b.wt. of MIT, WIT, BT and SIT, respectively. The groups received the respective treatment for fourteen days. Sexual behavior of the rats was observed on Day-1&14. Serum testosterone was estimated after the last observation.
Results
It was found that there was a statistically significant difference between the treatment groups. However, based on the mean values/ranking analysis of all the parameters, the order of potency was WIT > SIT ≥ BT > MIT.
Conclusion
These findings indicate that the aqueous extract of Indian TT which contains lesser protodioscin showed comparatively better sex stimulant activity in comparison to the other tested extracts.
This study was conducted on (30) consecutive male patients presenting to Kasr-Al Ainy Andrology outpatient clinic complaining of manifestations of Partial Androgen Deficiency in Aging Males (PADAM). Here in this study (750 mg/day) of Tribulus terrestris in 3 divided doses, each of (250 mg/dose) as an endogenous testosterone enhancer had been tried for (3 months) duration and the evaluation of its effect had been monitored for each patient concerning its effect on serum testosterone (Total & Free) & LH, as well as its Impact on erectile function that was evaluated by International index of erectile function -5 (IIEF-5) Questionnaire for those patients. Results showed statistically significant difference in the level of testosterone (Total & Free) & IIEF-5, but no statistically significant difference in the level of LH before & after treatment. Also, it showed statistically significant correlation between Testosterone (Total & Free) & IIEF-5, but no statistically significant correlation between the level of LH & IIEF-5 before & after treatment.
We aimed to evaluate the efficacy of oral therapy with alga Ecklonia bicyclis, Tribulus terrestris, and glucosamine oligosaccharide (Tradamix TX1000) in patients with erectile dysfunction (ED) at 3 months of follow-up. From January 2013 to September 2013, 177 patients diagnosed with mild-moderate ED (IIEF-EF< 26) were enrolled in this multicenter, single-blinded, placebo-controlled study and randomized in Group A (Tradamix, n = 87) and Group B (placebo, n = 90). Penile color Doppler ultrasound measures, IIEF-15 questionnaire, male sexual health questionnaire-ejaculation disorder (MSHQ-EjD), and sexual quality of life (SQoL-M) were collected. We observed significant changes of the IIEF-15 in Group A (mean difference: 11.54; P < 0.05) at 3 months versus Group B (P < 0.05). PSV (P < 0.05), IIEF-intercourse satisfaction (P < 0.05), IIEF-orgasmic function (mean P < 0.05), IIEF-sexual desire (P < 0.05), IIEF-overall satisfaction (P < 0.05), MSHQ-EjD (mean difference: 1.21; P < 0.05), and SQoL-M(mean difference: 10.2; P < 0.05) were significantly changed in Group A versus baseline and Group B. Patients with moderate arterial dysfunction showed significant increase of PSV (P < 0.05), IIEF-EF (P < 0.05), MSHQ-EjD (P < 0.05), and SQoL-M (P < 0.05) in Group A. Therapy with Tradamix improves erectile and ejaculation function and sexual quality of life in patients with mild-moderate ED and in particular for those with moderate arterial dysfunction.
Tribulus terrestris as a herbal remedy has shown beneficial aphrodisiac effects in a number of animal and human experiments. This study was designed as a randomized double-blind placebo-controlled trial to assess the safety and efficacy of Tribulus terrestris in women with hypoactive sexual desire disorder during their fertile years. Sixty seven women with hypoactive sexual desire disorder were randomly assigned to Tribulus terrestris extract (7.5 mg/day) or placebo for 4 weeks. Desire, arousal, lubrication, orgasm, satisfaction, and pain were measured at baseline and after 4 weeks after the end of the treatment by using the Female Sexual Function Index (FSFI). Two groups were compared by repeated measurement ANOVA test.
Thirty women in placebo group and thirty women in drug group completed the study. At the end of the fourth week, patients in the Tribulus terrestris group had experienced significant improvement in their total FSFI (p < 0.001), desire (p < 0.001), arousal (p = 0.037), lubrication (p < 0.001), satisfaction (p < 0.001) and pain (p = 0.041) domains of FSFI. Frequency of side effects was similar between the two groups.
Tribulus terrestris may safely and effectively improve desire in women with hypoactive sexual desire disorder. Further investigation of Tribulus terrestris in women is warranted.
Tribulus terrestris has long been used as a tonic and aphrodisiac in Unani system of medicine. It has been used in India and Pakistan as a treatment for impotence and as a stimulant to enhance sexual drive and performance (Brown et al., 2001). T. terrestris has diuretic and uricosuric effects. In this review article introduction, description, active constituents and medicinal uses of T. terrestris have been given herewith.
Background:
Opioids can exert adverse effects on the body. Morphine, an opioid drug, reduces hormone levels and fertility, and causes sexual activity disorders. Tribulus terrestris (TT) is a traditional herbal medicine used to enhance sexual activities. This study investigates the possible role of TT on sex hormones and gonadotropins with the intent to show its usefulness in treating fertility disorders in opioid users.
Materials and methods:
In this experimental study, we randomly divided 48 rats into four groups: i. control, ii. TT-treated, iii. addicted and iv. TT-treated addicted. Watersoluble morphine was administrated orally for 21 days to induce addiction, after which the treated groups 2 and 4 received plant-mixed pelleted food (6.25%) orally for four weeks. At the end of the treatment period, the sex hormone and gonadotropin levels of all rats' sera were determined by radioimmunoassay and Elisa kits. The data obtained were statistically analyzed using the one-way analysis of variance, followed by post-hoc Tukey test. P<0.05 was considered significant.
Results:
The addicted group had a significantly lower luteinizing hormone (LH) level than the control group (p<0.027). LH levels increased significantly in the TT-treated addicted group (p<0.031). The testosterone level in the treated addicted group was lower than the treated control group. The addicted group had a significantly low testosterone level (p<0.001). The estrogen level was significantly (p<0.002) lower in the addicted group than in the control group. In addition, there was a significant difference between the treated addicted group and the treated control group (p<0.048). The treated control group had a significant increase in its progesterone level (p<0.002). Overall, except for follicle-stimulating hormone (FSH), morphine reduced most of the gonadotropins and sexual hormones. Whereas TT caused a considerable increase (p<0.05) in the hormones in the treated addicted group, there was only a slight increase in the treated control group.
Conclusion:
Oral consumption of TT could markedly antagonize the reduction of sex hormones and gonadotropins (except for FSH) due to morphine addiction.
The effectiveness of a nutritional supplement designed to enhance serum testosterone concentrations and prevent the formation of dihydrotestosterone and estrogens from the ingested androgens was investigated in healthy 30- to 59-year old men. Subjects were randomly assigned to consume DION (300 mg androstenedione, 150 mg dehydroepiandrosterone, 540 mg saw palmetto, 300 mg indole-3-carbinol, 625 mg chrysin, and 750 mg Tribulus terrestris per day; n = 28) or placebo (n = 27) for 28 days. Serum free testosterone, total testosterone, androstenedione, dihydrotestosterone, estradiol, prostate-specific antigen (PSA), and lipid concentrations were measured before and throughout the 4-week supplementations period. Serum concentration of total testosterone and PSA were unchanged by supplementation. DION increased (p < 0.05) serum androstenedione (342%), free testosterone (38%), dihydrotestosterone (71%), and estradiol (103%) concentrations. Serum HDL-C concentrations were reduced by 5.0 mg/dL in DION (p < 0.05). Increased in serum free testosterone (r(2) = 0.01), androstenedione (r(2) = 0.01), dihydrotestosterone (r(2) = 0.03), or estradiol (r(2) = 0.07) concentrations in DION were not related to age. While the ingestion of androstenedione combined with herbal products increased serum free testosterone concentrations in older men, these herbal products did not prevent the conversion of ingested androstenedione to estradiol and dihydrotestosterone.
Tribulus terrestris is a valuable herb known for its application in the folk medicine in many parts of the world. Furostanol and spirostanol
saponins of tigogenin, neotigogenin, gitogenin, neogitogenin, hecogenin, neohecogenin, diosgenin, chlorogenin, ruscogenin
and sarsasapogenin type are frequently found in this plant. Four sulphated saponins of tigogenin and diosgenin type are also
isolated. Extracts and steroidal saponins have been found to possess various pharmacological activities. Preparations based
on the saponin fraction of T. terrestris are used for treatment of infertility and libido disorders in men and women, as well as for treatment of cardiac diseases.
Food supplements containing T. terrestris extracts are on sale in USA and Europe with claim of a general stimulating action.
To study the effect of acute and repeated dose administration of lyophilized aqueous extract of the dried fruits of Tribulus terrestris (LAET) on sexual function in sexually sluggish male albino rats.
Aphrodisiac activity of the test drug was evaluated in terms of exhibited sexual behavior. In order to assess the effect of chronic T. terrestris exposure on the hypothalamus--pituitary--gonadal axis, testosterone level estimation and sperm count were carried out. Twenty-eight-day oral toxicity studies were carried out to evaluate the long-term effects of the LAET administration on different body systems.
A dose-dependent improvement in sexual behavior was observed with the LAET treatment as characterized by an increase in mount frequency, intromission frequency, and penile erection index, as well as a decrease in mount latency, intromission latency, and ejaculatory latency. The enhancement of sexual behavior was more prominent on chronic administration of LAET. Chronic administration of LAET produced a significant increase in serum testosterone levels with no significant effect on the sperm count. No overt body system dysfunctions were observed in 28-day oral toxicity study.
Findings of the present study validate the traditional use of T. terrestris as a sexual enhancer in the management of sexual dysfunction in males.
Sexual dysfunction is very serious problem in human being. Inability to achieve normal sexual intercourse called sexual dysfunction, which include premature ejaculation, retrograded, retarded or inhibited ejaculation, erectile dysfunction, arousal difficulties (reduced libido), compulsive sexual behavior, orgasmic disorder, failure of detumesence in males and Desire disorders, Arousal disorders, Orgasmic disorders, Sexual pain disorders in females. The trends of herbal medicine is running in the market to cure specific diseases due to its less adverse drug reaction, toxicity and other injurious effects. There is huge variety of plant which capable to cure and treat specific type of disease. Researchers further studying to identify plant activity. Many plants have ability to correct sexual dysfunction in male and female. Among them some plants Panax quinquefolius L. (American giseng), Eurycoma longifolia, Corynanthe yohimbe, Maca, Ginkgo biloba, Turnera diffusa (Damiana), Terminalia catappa L., Tribulus terrestris, Euphorbia Hirta L., Passiflora incarnata L., Ptychopetalum olacoides, Cnidium monnier have discussed in this article.
Herbal medicine long has been used in the management of sexual dysfunction, including erectile dysfunction. Many patients have attested to the efficacy of this treatment. However, is it evidence-based medicine? Studies have been done on animal models, mainly in the laboratory. However, randomized controlled trials on humans are scarce. The only herbal medications that have been studied for erectile dysfunction are Panax ginseng, Butea superba, Epimedium herbs (icariin), Tribulus terrestris, Securidaca longipedunculata, Piper guineense, and yohimbine. Of these, only Panax ginseng, B. superb, and yohimbine have published studies done on humans. Unfortunately, these published trials on humans were not robust. Many herbal therapies appear to have potential benefits, and similarly, the health risks of various phytotherapeutic compounds need to be elucidated. Properly designed human trials should be worked out and encouraged to determine the efficacy and safety of potential phytotherapies.
This article presents the development of a brief, self-report measure of female sexual function. Initial face validity testing of questionnaire items, identified by an expert panel, was followed by a study aimed at further refining the questionnaire. It was administered to 131 normal controls and 128 age-matched subjects with female sexual arousal disorder (FSAD) at five research centers. Based on clinical interpretations of a principal components analysis, a 6-domain structure was identified, which included desire, subjective arousal, lubrication, orgasm, satisfaction, and pain. Overall test-retest reliability coefficients were high for each of the individual domains (r = 0.79 to 0.86) and a high degree of internal consistency was observed (Cronbach's alpha values of 0.82 and higher) Good construct validity was demonstrated by highly significant mean difference scores between the FSAD and control groups for each of the domains (p < or = 0.001). Additionally, divergent validity with a scale of marital satisfaction was observed. These results support the reliability and psychometric (as well as clinical) validity of the Female Sexual Function Index (FSFI) in the assessment of key dimensions of female sexual function in clinical and nonclinical samples. Our findings also suggest important gender differences in the patterning of female sexual function in comparison with similar questionnaire studies in males.
Herbs have been used throughout history to enhance physical performance, but scientific scrutiny with controlled clinical trials has only recently been used to study such effects. The following herbs are currently used to enhance physical performance regardless of scientific evidence of effect: Chinese, Korean, and American ginsengs; Siberian ginseng, mahuang or Chinese ephedra; ashwagandha; rhodiola; yohimbe; CORDYCEPS: fungus, shilajit or mummio; smilax; wild oats; Muira puama; suma (ecdysterone); Tribulus terrestris; saw palmetto berries; beta-sitosterol and other related sterols; and wild yams (diosgenin). Controlled studies of Asian ginsengs found improvements in exercise performance when most of the following conditions were true: use of standardized root extracts, study duration (>8 wk, daily dose >1 g dried root or equivalent, large number of subjects, and older subjects. Improvements in muscular strength, maximal oxygen uptake, work capacity, fuel homeostasis, serum lactate, heart rate, visual and auditory reaction times, alertness, and psychomotor skills have also been repeatedly documented. Siberian ginseng has shown mixed results. Mahuang, ephedrine, and related alkaloids have not benefited physical performance except when combined with caffeine. Other herbs remain virtually untested. Future research on ergogenic effects of herbs should consider identity and amount of substance or presumed active ingredients administered, dose response, duration of test period, proper experimental controls, measurement of psychological and physiologic parameters (including antioxidant actions), and measurements of performance pertinent to intended uses.
The effectiveness of an androgenic nutritional supplement designed to enhance serum testosterone concentrations and prevent the formation of dihydrotestosterone and estrogen was investigated in healthy 3 to 58 year old men.
Subjects were randomly assigned to consume a nutritional supplement (AND-HB) containing 300-mg androstenediol, 480-mg saw palmetto, 450-mg indole-3-carbinol, 300-mg chrysin, 1,500 mg gamma-linolenic acid and 1.350-mg Tribulus terrestris per day (n = 28), or placebo (n = 27) for 28 days. Subjects were stratified into age groups to represent the fourth (30 year olds, n = 20), fifth (40 year olds, n = 20) and sixth (50 year olds, n = 16) decades of life.
Serum free testosterone, total testosterone, androstenedione, dihydrotestosterone, estradiol, prostate specific antigen and lipid concentrations were measured before supplementation and weekly for four weeks.
Basal serum total testosterone, estradiol, and prostate specific antigen (PSA) concentrations were not different between age groups. Basal serum free testosterone concentrations were higher (p < 0.05) in the 30- (70.5 +/- 3.6 pmol/L) than in the 50 year olds (50.8 +/- 4.5 pmol/L). Basal serum androstenedione and dihydrotestosterone (DHT) concentrations were significantly higher in the 30- (for androstenedione and DHT, respectively, 10.4 +/- 0.6 nmol/L and 2198.2 +/- 166.5 pmol/L) than in the 40- (6.8 +/- 0.5 nmol/L and 1736.8 +/- 152.0 pmol/L) or 50 year olds (6.0 +/- 0.7 nmol/L and 1983.7 +/- 147.8 pmol/L). Basal serum hormone concentrations did not differ between the treatment groups. Serum concentrations of total testosterone and PSA were unchanged by supplementation. Ingestion of AND-HB resulted in increased (p < 0.05) serum androstenedione (174%), free testosterone (37%), DHT (57%) and estradiol (86%) throughout the four weeks. There was no relationship between the increases in serum free testosterone, androstenedione, DHT, or estradiol and age (r2 = 0.08, 0.03, 0.05 and 0.02, respectively). Serum HDL-C concentrations were reduced (p < 0.05) by 0.14 mmol/L in AND-HB.
These data indicate that ingestion of androstenediol combined with herbal products does not prevent the formation of estradiol and dihydrotestosterone.
The known furostanol saponins methylprotodioscin and protodioscin and two new sulfated saponins, sodium salt of 26-O-beta-glucopyranosyl-22alpha-methoxy-(25R)-furost-5-ene-3beta,26-diol-3-O-alpha-rhamnopyranosyl-(1-->2)-beta-4-O-sulfo-glucopyranoside (methylprototribestin) and sodium salt of 26-O-beta-glucopyranosyl-22alpha-hydroxy-(25R)-furost-5-ene-3beta,26-diol-3-O-alpha-rhamnopyranosyl-(1-->2)-beta-4-O-sulfo-glucopyranoside (prototribestin) have been isolated from the aerial parts of Tribulus terrestris L. growing in Bulgaria. The structures of the new compounds were elucidated on the basis of 1D and 2D (DQF-COSY, TOCSY, HSQC-TOCSY, HSQC, HMBC, ROESY) NMR data, ESI mass spectra and chemical transformation.
The International Index of Erectile Function (IIEF) is a widely used, multi-dimensional self-report instrument for the evaluation of male sexual function. It is has been recommended as a primary endpoint for clinical trials of erectile dysfunction (ED) and for diagnostic evaluation of ED severity. The IIEF was developed in conjunction with the clinical trial program for sildenafil, and has since been adopted as the 'gold standard' measure for efficacy assessment in clinical trials of ED. It has been linguistically validated in 32 languages and used as a primary endpoint in more than 50 clinical trials. This review summarizes early stages in the psychometric validation of the instrument, its subsequent adoption in randomized clinical trials with sildenafil and other ED therapies, and its use in classifying ED severity and prevalence. The IIEF meets psychometric criteria for test reliability and validity, has a high degree of sensitivity and specificity, and correlates well with other measures of treatment outcome. It has demonstrated consistent and robust treatment responsiveness in studies in USA, Europe and Asia, as well as in a wide range of etiological subgroups. Although only one direct comparator trial has been performed to date, the IIEF is also sensitive to therapeutic effects with treatment agents other than sildenafil. A severity classification for ED has recently been developed, in addition to a brief screening version of the instrument. This review includes the strengths as well as limitations of the IIEF, along with some potential areas for future research.
Fall-planted longspine sandbur began to emerge in April, peaked in late April or May, and continued at low levels through October. During the first year after seeding, 98% of the total seedlings emerged prior to June. Fall-planted puncturevine began to emerge in late April or May and continued through October. Puncturevine emergence was multipeaked and 75% of each season's total emerged prior to mid-July. A similar number of puncturevine seedlings emerged the second and third years after planting as in the first. The emergence pattern for a species was similar each year regardless of how long the seed had lain in the soil. Longspine sandbur required 7 to 13 weeks from emergence to heading and produced approximately 2600, 1300, 180, and 3 spikes per plant when planted in May, June, July, and August, respectively. Puncturevine flowered within 3 to 4 weeks after emergence when temperatures were favorable and produced an average of 5600, 5200, 3600, and 200 burs per plant when planted in May, June, July, and August, respectively.
A comparative investigation in respect to qualitative and quantitative composition of raw materials from Tribulus terretris L. and a variety of preparations from different origin have been performed. The results obtained concerning furostanol saponins indicate that most of the raw materials are either impurified products derived from Trihulus terristris or from the powdered plant itself. The content of protodioscin and protogracillin in the preparations except for the Bulgarian Tribestan film tablets (Sopharma) are in insignificant amount.
This chapter summarizes the progress made in understanding how hormones, the central nervous system, and the periphery interact to regulate male sexual behavior, focusing on how that understanding developed, and where it is incomplete. It summarizes recent research on the neural mechanisms by which males integrate hormonal and sensory inputs to produce adaptive behavioral and physiological responses, not only in the context of mating, but also in other contexts. It describes the copulatory behaviors of species commonly studied in the laboratory, the paradigms and measures used to study them, and the conceptual contexts in which the research takes place. It also reviews the behavioral effects of gonadal steroids, and systemically or intraventricularly administered drugs. It summarizes the information about the functions of the brain areas implicated in the control of male sexual behavior, including effects of lesions and stimulation, local hormonal and pharmacological manipulations, and measures of neural activity. Further, it describes the interconnections among the neural structures that mediate sexual behavior.
The aqueous extract of Tribulus terrestris was evaluated for its activity on the reproductive system of mature albino female mice. Two experiments involved maternal treatment with the extract (orally) for two and four weeks with two dose levels (100 and 200 mg/kg/day) at each period were conducted. Different ovarian and uterine parameters were studied in addition to determination of follicle stimulating hormone (FSH), luteinizing hormone( LH) and estradiol hormone levels during the estrus phase. The two weeks period experiment revealed no significant differences in maternal body weight or reproductive organs weight. A significant increase in the number of growing follicles, diameter of mature follicles, endometrial lining cells height and endometrial glands diameter was obtained in both dose levels. The four weeks period experiment showed a remarkable increase in body weight and reproductive organs weight in both dose levels. No significant differences on the levels of ovarian parameters, whereas, a significant increase was obtained in the endometrial lining cells height on both dose levels and a significant increase in endometrial glands diameter in the highest dose level. As concerning the levels of reproductive hormones, although the differences were not significant, but an obvious increase was obtained in FSH and LH and a decrease in estradiol was detected in both dose levels. In conclusions, although there was some fluctuation, a dose dependent activity was obtained with the two weeks period seems to be more effective on both ovarian and uterine parameters, whereas the four weeks period was more effective on uterine parameters.
In this study the extracts of the Iraqi herb Tribulus terrestris (Al-Hassage or Al-Kutub) was done by using of polar and non polar solvents, then the biological activity of these extractants was studied in three fields, First, the antibacterial activity (in vitro) on gram positive bacteria (Staphylococcus aureus), and gram negative bacteria (E. coli, Proteus vulgaris, Pseudomonas aerugiuosa, and Klebsiella), all extracts showed considerable activity against all bacteria. Second, the effect of extracts on free serum testosterone level in male mice (in vivo), the alcoholic, and acetonitrilic extracts showed significant (P < 0.05) increase in free serum testosterone level, and we found that the extracts contained compounds with less genotoxic effects in mice germ cells. 3 rd, was to study the effect of methanolic extract of T. terrestris in diabetes management.
To evaluate the possible effects of Tribulus terrestris herbal medicine in the erectile dysfunction treatment and to quantify its potential impact on serum testosterone levels.
Prospective, randomized, double-blind and placebo-controlled study including thirty healthy men selected from 100 patients who presented themselves spontaneously complaining of erectile dysfunction, ≥ 40 years of age, nonsmokers, not undergoing treatment for prostate cancer or erectile dysfunction, no dyslipidemia, no phosphodiesterase inhibitor use, no hormonal manipulation and, if present hypertension and/or diabetes mellitus should be controlled. International Index of Erectile Function (IIEF-5) and serum testosterone were obtained before randomization and after 30 days of study. Patients were randomized into two groups of fifteen subjects each. The study group received 800mg of Tribulus terrestris, divided into two doses per day for thirty days and the control group received placebo administered in the same way.
The groups were statistically equivalent in all aspects evaluated. The mean (SD) age was 60 (9.4) and 62.9 (7.9), P=.36 for intervention and placebo groups, respectively. Before treatment, the intervention group showed mean IIEF-5 of 13.2 (5-21) and mean total testosterone 417.1ng/dl (270.7-548.4ng/dl); the placebo group showed mean IIEF-5 of 11.6 (6-21) and mean total testosterone 442.7ng/dl (301-609.1ng/dl). After treatment, the intervention group showed mean IIEF-5 of 15.3 (5-21) and mean total testosterone 409.3ng/dl (216.9-760.8ng/dl); the placebo group showed mean IIEF-5 of 13.7 (6-21) and mean total testosterone 466.3ng/dl (264.3-934.3ng/dl). The time factor caused statistically significant changes in both groups for IIEF-5 only (P=.0004), however, there was no difference between the two groups (P=.7914).
At the dose and interval studied, Tribulus terrestris was not more effective than placebo on improving symptoms of erectile dysfunction or serum total testosterone.
Objectives
To evaluate the possible effects of Tribulus terrestris herbal medicine in the erectile dysfunction treatment and to quantify its potential impact on serum testosterone levels.
Design and methods
Prospective, randomized, double-blind and placebo-controlled study including thirty healthy men selected from 100 patients who presented themselves spontaneously complaining of erectile dysfunction, ≥ 40 years of age, nonsmokers, not undergoing treatment for prostate cancer or erectile dysfunction, no dyslipidemia, no phosphodiesterase inhibitor use, no hormonal manipulation and, if present hypertension and/or diabetes mellitus should be controlled. International Index of Erectile Function (IIEF-5) and serum testosterone were obtained before randomization and after 30 days of study. Patients were randomized into two groups of fifteen subjects each. The study group received 800 mg of Tribulus terrestris, divided into two doses per day for thirty days and the control group received placebo administered in the same way.
Results
The groups were statistically equivalent in all aspects evaluated. The mean (SD) age was 60 (9.4) and 62.9 (7.9), P = .36 for intervention and placebo groups, respectively. Before treatment, the intervention group showed mean IIEF-5 of 13.2 (5-21) and mean total testosterone 417.1 ng/dl (270.7-548.4 ng/dl); the placebo group showed mean IIEF-5 of 11.6 (6-21) and mean total testosterone 442.7 ng/dl (301-609.1 ng/dl). After treatment, the intervention group showed mean IIEF-5 of 15.3 (5-21) and mean total testosterone 409.3 ng/dl (216.9-760.8 ng/dl); the placebo group showed mean IIEF-5 of 13.7 (6-21) and mean total testosterone 466.3 ng/dl (264.3-934.3 ng/dl). The time factor caused statistically significant changes in both groups for IIEF-5 only (P = .0004), however, there was no difference between the two groups (P = .7914).
Conclusions
At the dose and interval studied, Tribulus terrestris was not more effective than placebo on improving symptoms of erectile dysfunction or serum total testosterone.
ABSTRACT Tribulus terrestris (TT) is a dicotyledonous herbal plant of the Zygophyllaceae family. In ancient medicine, extracts of the aerial parts and fruits have been used for its diuretic, tonic, and aphrodisiac properties. Today, TT is widely used by athletes and bodybuilders based on the belief, fueled by claims in marketing information, that it can enhance testosterone concentrations. To assess TT's effect on testosterone levels in human and animals, an electronic literature search out using seven databases and the patent database up to August 2013 was carried out. Randomized control trials, which included healthy human subjects ingesting TT as sole or combined supplement, along with animal studies with TT as a sole treatment across a number of species were included. Eleven studies met the inclusion criteria, including one patent application. The results showed that trials varied in duration, dosage and supplementation with TT as sole or combined treatment, rendering meta-analysis impossible. A limited number of animal studies displayed a significant increase in serum testosterone levels after TT administration, but this effect was only noted in humans when TT was part of a combined supplement administration. Literature available for the effectiveness of TT on enhancing testosterone concentrations is limited. Evidence to date suggests that TT is ineffective for increasing testosterone levels in humans, thus marketing claims are unsubstantiated. The nitric oxide release effect of TT may offer a plausible explanation for the observed physiological responses to TT supplementation, independent of the testosterone level.
Tribulus terrestris Linn. is a flowering plant belongs to the family of zygophyllaceae, native to warm temperate and tropical regions of southern Asia, Africa and Australia. It is commonly known as “Ghokhru” and is constituent in many traditional medicine formulations for its medicinal properties. It has been used traditionally as aphrodisiac due to its putative positive influence on sexual performance in humans. In the present study, the lyophilized powder of the dried fruits of Tribulus terrestris was studied for sexual behavior effects of acute and subchronic administration in male albino rats, and comparison has been made with standard sexual stimulant drug, sildenafil citrate. The animals were evaluated on various parameters of sexual behavior, anabolic effects, testosterone level and in-vitro sperm counts.Oral administration of 100 mg/kg of test drug has proven anabolic effect as evidenced by body weight gain in the body and reproductive organs. Improvement in sexual behavior of male rats was characterized by increased amount and intromission frequency. Penile erection index (PEI) was also considerably enhanced without any noticeable toxicity, and the testosterone level and sperm count also significantly increased, and the results are comparable to that of standard drug, sildenafil citrate. Findings of the present study validate the traditional use of Tribulus terrestris for its role in enhancing sexual behavior and potential to be used in the treatment of Erectile Dysfunction (ED).
From the overground part of Tribulus terrestris L. a saponine mixture was isolated in a quantity of 2,8 % containing 10 steroid substances (from A to K). A small admixture of phenol was also proved (fig. 1).
With the help of repeated column chromatography and thin-layer chromatography the saponines C, F and G were isolated (Fig. 2).
Saponine F proved to be a new product: tigogenine–3–diglucorhamnoside, named by us terrestroside F, the partial structure of which was determined on the basis of the hydrolytic products: aglykon tigogenine (identified by m. p., mixed m. p., IR– and mass spectrum, acetyl derivative) and an oligosaccharide part – rhamnose : glucose (2:1).
The saponines C and G proved to be a mixture of two tigogenine and diosgenine glycosides each. The mixture of aglykons was separated by column chromatography on silica gel containing silver nitrate and identified by the above mentioned indices as tigogenine and diosgenine (Table I). In the hydrolysates the sugars glucose and rhamnose were proved.
A flavonoide was also isolated which was identified as astragaline (caempferol–3–glucoside).
Phytochemicals have played a vital role in the past and will continue to do so in the future. Although synthetic drugs can produce dramatic results in most cases, the side-effects associated with them are a major concern. The source of many compounds used in modern medicine today can be traced down to plant origin. Whether or not scientific justification is available for the use of most plant products, the continued use of these compounds is due to their safety profile, ease of availability and also economic reasons. Each medicinal plant that has been used in the traditional system of medicine must be scientifically tested in order to bring forth its active principle that might be effectively used as a phytomedicine. In this vast resource of phytoproducts there are various plants that are claimed to improve the sexual deficiency in man. Tribulus terrestris Linn. (TT) is one such plant that has been used for a long time in both the Indian and Chinese systems of medicine. The plant is also said to possess various other pharmacological properties. The extract obtained from the air-dried aerial parts of this plant contains mainly steroidal glycosides, the major saponin being protodioscin (PTN). In our study on this plant product it was observed that PTN produced a moderate increase in testosterone, dihydrotestosterone and dehydroepiandrosterone sulfate levels in primates following bolus intravenous administration of the TT extract at doses of 7.5, 15 and 30 mg/kg body weight. It also improved libido, sexual activity and intracavernous pressure in rats following TT extract administrat