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Alpha Male References
Eurycoma longifolia References
Ezzat SM et al. Rho-Kinase II Inhibitory Potential of Eurycoma longifolia New Isolate for the Management of Erectile Dysfunction. Evidence Based Complementary and Alternative Medicine, 15 May 2019. Background: Eurycoma longifolia Jack (Fam.: Simaroubaceae), known as Tongkat Ali (TA), has been known as a symbol of virility and sexual power. The aim of the study was to screen E. longifolia aqueous extract (AE) and isolates for ROCK-II inhibition. Results: The AE (1-10 μg/ml) showed a significant inhibition for ROCK-II activity (62.8-81%) at P < 0.001 with an IC50 (651.1 ± 32.9 ng/ml) compared to Y-27632 ([(+)-(R)-trans-4-(1-aminoethyl)-N-(4-pyridyl)cyclohexanecarboxamide dihydrochloride]) (68.15-89.9 %) at same concentrations with an IC50 (192 ± 8.37 ng/ml). Chromatographic purification of the aqueous extract (AE) allowed the isolation of eight compounds; stigmasterol T1, trans-coniferyl aldehyde T2, scopoletin T3, eurycomalactone T4, 6α- hydroxyeurycomalactone T5, eurycomanone T6, eurycomanol T7, and eurycomanol-2-O-β-D-glucopyranoside T8. This is the first report for the isolation of T1 and T3 from E. longifolia and for the isolation of T2 from genus Eurycoma. The isolates (at 10 μg/ml) exhibited maximum inhibition % of ROCK-II 82.1 ± 0.63 (T2), 78.3 ± 0.38 (T6), 77.1 ± 0.11 (T3), 76.2 ± 3.53 (T4), 74.5 ± 1.27 (T5), 74.1 ± 2.97 (T7), 71.4 ± 2.54 (T8), and 60.3 ± 0.14 (T1), where the newly isolated compound trans-coniferyl aldehyde T2 showed the highest inhibitory activity among the tested isolated compounds and even higher than the total extract AE. The standard Y-27632 (10 μg/ml) showed 89.9 ± 0.42 % inhibition for ROCK-II activity when compared to control at P < 0.0001. Conclusion: The traditional use of E. longifolia as aphrodisiac and for male sexual disorders might be in part due to the ROCK-II inhibitory potential.
Low BS et al. Standardized quassinoid-rich Eurycoma longifolia extract improved spermatogenesis and fertility in male rats via the hypothalamic-pituitary-gonadal axis. J Ethnopharmacol. 2013 Feb 13;145(3):706-14. Ethnopharmacological Relevance: Eurycoma longifolia Jack, a small Simaroubaceae tree, known locally as 'Tongkat Ali' is popularly used as a sexual tonic in traditional medicine for aphrodisiac activity and improvement of fertility and male libido. Aim of the Study: To investigate the effects of the standardized bioactive fraction of E. longifolia and its chemical constituents on the male fertility and the mechanisms of action involved. Material and Methods: The powdered roots of E. longifolia were extracted separately with methanol and water. The organic extract upon further fractionation on HP 20 resin and elution with the methanol/water mixture afforded four fractions (F1-F4). These fractions, together with the crude aqueous (W) and organic extracts were standardized following their respective major quassinoid content and profile. The effects of the fractions on the rat spermatogenesis were compared with that of the aqueous extract (W) to determine the bioactive fraction. The effects of the bioactive fraction on the sperm count and quality, the histological morphometric changes on the spermatogenesis cycle, fertility and hormonal changes of plasma testosterone, luteinizing hormone (LH), follicle stimulating hormone (FSH) and estrogen in the animals upon oral administration were determined. The effects of the bioactive quassinoids on the testosterone release from the isolated testicular interstitial cells rich in Leydig cells, were also described. Results: The male rats orally administered with 25mg/kg of F2 and 250mg/kg of W, significantly increased the sperm concentration when compared with that of the control animals (P < 0.05). High performance liquid chromatography analysis revealed that 25mg/kg of F2 and 250mg/kg of W were almost similar in concentration of eurycomanone, the major and most potent quassinoid. Microscopic morphometrical analysis of the rat testis following treatment with F2, showed significant increase in the number of spermatocytes and round spermatids at Stage VII of the spermatogenesis cycle when compared to that of the control (P < 0.05). The estimated spermatozoa production rate and the number of Leydig cells were also elevated (P < 0.001). The fertility index, fecundity index and the pup litter size delivered from the females after mating with the males treated with F2 were increased. The plasma testosterone level of the animals given 25mg/kg of F2 orally was significantly different at day-26 (P < 0.05) and day-52 (P < 0.01) from those of control but was not different at day-104. The testicular testosterone also peaked in the animals treated with 25mg/kg F2 and was higher than that in the plasma. The plasma LH and FSH levels of the rats treated with 25mg/kg of F2 were higher than those of the control (P < 0.001). In contrast, the plasma estrogen level was significantly lower than that of the untreated control. Amongst the isolated quassinoids of F2, eurycomanone and 13α(21)-dihydroeurycomaone significantly increased the testosterone level from the Leydig cells of the testicular interstitial cells cultured in vitro (P < 0.05). Conclusion: The standardised extract F2 of E. longifolia and its major quassinoids especially eurycomanone improved the rat spermatogenesis by affecting the hypothalamic-pituitary-gonadal axis and the potential efficacy may be worthy of further investigation.
Muhamad AS et al. Eurycoma longifolia Jack: Medicinal properties and its effects on endurance exercise performance. Asian Journal of Exercise & Sport Science, 2009, Vol. 6 (No. 1). ABSTRACT: This review article discusses the medicinal properties of a herbal plant, Eurycoma longifolia Jack, and its possible ergogenic effect on endurance exercise performance. To date, herbs or plant products that have been investigated as ergogenic aids for enhancing endurance performance are caffeine, ginseng, mahuang, ephedrine and related alkaloids. Eurycoma longifolia Jack is one of the herbs found in Malaysia. It is commonly known as ‘Tongkat Ali’ in Malaysia and as ‘Pasak Bumi’ in Indonesia. It is also referred to as ‘Malaysian ginseng’ since it is well-known among various ethnic groups in Malaysia for treating various diseases and enhancing health. Eurycoma longifolia Jack is a tall, slender shrubby tree found on sandy soil. It belongs to the Simaroubaceae family and grows wildly in Southeast Asian countries, i.e. Malaysia, Indonesia, Thailand, and Myanmar. To our knowledge, studies on Eurycoma longifolia Jack as an ergogenic aid for enhancing endurance performance is lacking. Thus, this review article highlights the available studies on its purported medicinal properties as well as studies that have been carried out to investigate its effects on physiological responses and endurance exercise performance.
Rehman SU et al. Review on a Traditional Herbal Medicine, Eurycoma longifolia Jack (Tongkat Ali): Its Traditional Uses, Chemistry, Evidence-Based Pharmacology and Toxicology. Molecules, 2016, 21(3), 331. ABSTRACT: Eurycoma longifolia Jack (known as tongkat ali), a popular traditional herbal medicine, is a flowering plant of the family Simaroubaceae, native to Indonesia, Malaysia, Vietnam and also Cambodia, Myanmar, Laos and Thailand. E. longifolia, is one of the well-known folk medicines for aphrodisiac effects as well as intermittent fever (malaria) in Asia. Decoctions of E. longifolia leaves are used for washing itches, while its fruits are used in curing dysentery. Its bark is mostly used as a vermifuge, while the taproots are used to treat high blood pressure, and the root bark is used for the treatment of diarrhea and fever. Mostly, the roots extract of E. longifolia are used as folk medicine for sexual dysfunction, aging, malaria, cancer, diabetes, anxiety, aches, constipation, exercise recovery, fever, increased energy, increased strength, leukemia, osteoporosis, stress, syphilis and glandular swelling. The roots are also used as an aphrodisiac, antibiotic, appetite stimulant and health supplement. The plant is reported to be rich in various classes of bioactive compounds such as quassinoids, canthin-6-one alkaloids, β-carboline alkaloids, triterpene tirucallane type, squalene derivatives and biphenyl neolignan, eurycolactone, laurycolactone, and eurycomalactone, and bioactive steroids. Among these phytoconstituents, quassinoids account for a major portion of the E. longifolia root phytochemicals. An acute toxicity study has found that the oral Lethal Dose 50 (LD50) of the alcoholic extract of E. longifolia in mice is between 1500-2000 mg/kg, while the oral LD50 of the aqueous extract form is more than 3000 mg/kg. Liver and renal function tests showed no adverse changes at normal daily dose and chronic use of E. longifolia. Based on established literature on health benefits of E. longifolia, it is important to focus attention on its more active constituents and the constituents' identification, determination, further development and most importantly, the standardization. Besides the available data, more evidence is required regarding its therapeutic efficacy and safety, so it can be considered a rich herbal source of new drug candidates. It is very important to conserve this valuable medicinal plant for the health benefit of future generations.
Solomon MC et al. In vivo effects of Eurycoma longifolia Jack (Tongkat Ali) extract on reproductive functions in the rat. Andrologia. 2014 May;46(4):339-48. ABSTRACT: An aqueous extract of Eurycoma longifolia (Tongkat Ali; TA) roots is traditionally used to enhance male sexuality. Because previous studies are limited to only few sperm parameters or testosterone concentration, this study investigated the in vivo effects of TA on body and organ weight as well as functional sperm parameters in terms of safety and efficacy in the management of male infertility. Forty-two male rats were divided into a control, low-dose (200 mg kg(-1) BW) and high-dose (800 mg kg(-1) BW) group (n = 14). Rats were force-fed for 14 days and then sacrificed. Total body and organ weights of the prostate, testes, epididymides, gastrocnemius muscle and the omentum were recorded. Moreover, testosterone concentration, sperm concentration, motility, velocity, vitality, acrosome reaction and mitochondrial membrane potential (MMP) were assessed. Whilst TA decreased BW by 5.7% (P = 0.0276) and omentum fat by 31.9% (P = 0.0496), no changes in organ weights were found for the prostate, testes and epididymides. Testosterone concentration increased by 30.2% (P = 0.0544). Muscle weight also increased, yet not significantly. Whilst sperm concentration, total and progressive motility and vitality increased significantly, MMP improved markedly (P = 0.0765) by 25.1%. Because no detrimental effect could be observed, TA appears safe for possible treatment of male infertility and ageing male problems.
Tribulus terrestris References
Gamal El Din SF et al. Tribulus terrestris versus placebo in the treatment of erectile dysfunction and lower urinary tract symptoms in patients with late-onset hypogonadism: A placebo-controlled study. Urologia. 2019 May;86(2):74-78. doi: 10.1177/0391560318802160. Epub 2018 Sep 25. ABSTRACT: Aging is associated with a series of morphological and functional modifications that leads to reduced physiological efficiency and atrophy of various organs and systems. Tribulus terrestris induces its effect in fertility and sexual functions through the steroidal saponins, particularly the dominant saponins protodioscin. We aimed in this study to evaluate the efficacy and safety profiles of Tribulus terrestris in aging males with partial androgen deficiency who suffered from erectile dysfunction and lower urinary tract symptoms. A total of 70 randomized aging patients with erectile dysfunction and lower urinary tract symptoms were recruited from June 2017 to March 2018 from our andrology outpatient clinic. Thirty-five patients (group A) received Tribulus terrestris three times daily for 3 months and the other 35 patients (group B) received placebo. The mean of aspartate transaminase was elevated in group A after 3 months of receiving Tribulus terrestris (26.5 (before), 27.8 (after), respectively, p = 0.03). Moreover, there were significant elevations in the means of both total testosterone together with the score of the validated Arabic index of erectile function (5-item version of the International Index of Erectile Function) (2.2, 10.7 (before), 2.7, 16.1 (after), p < 0.001, p < 0.001, respectively). Finally, the mean of the total prostate-specific antigen was elevated in this group (1.4 (before), 1.7 (before), p = 0.007, respectively). Interestingly, there were no worsening of the lower urinary tract symptoms in group A as there was no change in the mean score of the international prostate symptom score, which was used to assess these symptoms before and after treatment (mean 14.4 (before), 14.6 (after), p = 0.67, respectively). In sum, this study replicates the findings of previous reports about the robust effect of this herbal medicine in elevating the testosterone level and improving the sexual function of patients who suffered from erectile dysfunction with partial androgen deficiency.
Salgado RM et al. Effect of oral administration of Tribulus terrestris extract on semen quality and body fat index of infertile men. Andrologia. 2017 Jun;49(5). doi: 10.1111/and.12655. Epub 2016 Jul 12. ABSTRACT: Male fertility can be evaluated through complete semen analysis. Plants belonging to the Tribulus genus are known for their role in enhancing sex hormone levels and semen quality. The aim of this study was to evaluate the effects of T. terrestris on semen quality and physiological parameters. Sixty-five men with abnormal semen evaluation were included in this study, in which they were prescribed with oral administration of Androsten® (250 mg of Tribulus terrestris dried extract per capsule). Body fat percentage, lean muscle mass gain, fluctuation in steroid hormone levels and all semen parameters were analysed during the period of treatment. The results demonstrated that decrease in the percentage of body fat and increase in lean mass were significant, as well as increase in dihydrotestosterone levels. Complete semen analysis evaluated at the end of treatment showed significant enhancement in sperm concentration, motility and liquefaction time. Protodioscin, the main phytochemical agent of the Tribulus genus, acts on sertoli cells, germ cell proliferation and growth of seminiferous tubules. This component is known to convert testosterone into dihydrotestosterone, which plays important roles in male attributes. Our results indicate the therapeutic use of Tribulus terrestris by men presenting altered semen parameters, and/or undergoing infertility treatment.
Wilk M et al. Endocrine Responses to Physical Training and Tribulus Terrestris Supplementation in Middle-Age Men. Central European Journal of Sports Sciences and Medicine, Vol. 13, No. 1/2016: 65-71. ABSTRACT: The aim of this study was to evaluate the effects of steroidal saponin supplementation on blood concentration of T, GH and IGF-1. The research involved 14 men between the age of 45 and 60 years. The duration of the experiment was 12 weeks. There were two series of laboratory tests. Independent tests were conducted at the beginning and after 12 weeks of the inter vention. A t wo-way repeated measures ANOVA revealed a statistically significant effect of the intervention on the following variables: T-Ch (η2 = 0.542), HDL-Ch (η2 = 0.522), LDL-Ch (η2 = 0.587), T (η2 = 0.603), IGF-1 (η2 = 0.512) and GH (η2 = 0.621). Thus, FFM significantly increased while TBF and BM decreased in comparison to pre-intervention levels. The analyzed results indicate that treatment or supplementation of individual hormone deficiencies can be a successful form of counteracting the aging process. Nevertheless, the effects of TT supplementation on the concentration of T as well as GH and IGF-1, requires further studies, especially in middle-aged and older subjects, along with different exercise programs. The analyzed results indicate that treatment or supplementation of individual hormone deficiencies can be a major form of counteracting the aging process
Haghmorad D et al. Improvement of fertility parameters with Tribulus Terrestris and Anacyclus Pyrethrum treatment in male rats. Int Braz J Urol. Sep-Oct 2019;45(5):1043-1054. doi: 10.1590/S1677-5538.IBJU.2018.0843. ABSTRACT: Objective: Anacyclus Pyrethrum (AP) and Tribulus Terrestris (TT) have been reported as male infertility treatment in several studies; however, in Iranian traditional medicine these two plants are prescribed simultaneously. In this study, we aimed to determine the effects of AP and TT extracts both separately and simultaneously on the male Wistar rat fertility parameters. Materials and methods: 32 male Wistar rats were divided into 4 groups: Control, TT, AP, and AT treated groups. Treatment continued for 25 days and rats were weighed daily. Their testes were dissected for histological studies. Sperm analysis including sperm count, viability and motility were performed. Serum was obtained to evaluate testosterone, LH and FSH levels. Histological studies were conducted to study Leydig, and Sertoli cells, spermatogonia and spermatid cell numbers, and to measure seminiferous diameter and epithelium thickness. Results: Sperm count increased in all the treatment groups. Sperm viability and motility in AT and AP groups were elevated. TT and AT groups showed signifi cantly increased testosterone level compared to control group (P=004, P=0.000, respectively) and TT, AP and AT treatment groups showed increased LH level (P=0.002, P=0.03 and P=0.000, respectively) compared to control, while only AT group showed increased FSH (p=0.006) compared to control. Histological studies showed signifi cant increase of spermatogonia, Leydig and Sertoli cell numbers and epithelial thickness in AT group compared to other groups. All the treatment groups had higher number of Leydig, spermatogonia and spermatid cells. Conclusion: TT and AP improved sexual parameters; however, their simultaneous administration had higher improving effects on studied parameters.
Adaikan G et al. History of herbal medicines with an insight on the pharmacological properties of Tribulus terrestris September 2001. The Aging Male 4(3):163-169. DOI:10.1080/tam.184.108.40.206. ABSTRACT: 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 administration orally (for 8 weeks at doses of 2.5, 5 and 10 mg/kg body weight) and had a proerectile effect on the corpus cavernosum smooth muscle of rabbits (orally for 8 weeks at doses of 2.5, 5 and 10 mg/kg body weight). In this article, the various pharmacological effects of TT have been reviewed and our studies based on TT extract in relation to male erectile dysfunction have been summarized.
Godard MP et al. Body composition and hormonal adaptations associated with forskolin consumption in overweight and obese men. Obesity Research. August 2005. DOI: 10.1038/oby.2005.162. Objective: This study examined the effect of forskolin on body composition, testosterone, metabolic rate, and blood pressure in overweight and obese (BMI > or = 26 kg/m(2)) men. Research methods and procedure: Thirty subjects (forskolin, n = 15; placebo, n = 15) were studied in a randomized, double-blind, placebo-controlled study for 12 weeks. Results: Forskolin was shown to elicit favorable changes in body composition by significantly decreasing body fat percentage (BF%) and fat mass (FM) as determined by DXA compared with the placebo group (P < or = 0.05). Additionally, forskolin administration resulted in a change in bone mass for the 12-week trial compared with the placebo group (P < or = 0.05). There was a trend toward a significant increase for lean body mass in the forskolin group compared with the placebo group (p = 0.097). Serum free testosterone levels were significantly increased in the forskolin group compared with the placebo group (P < or = 0.05). The actual change in serum total testosterone concentration was not significantly different among groups, but it increased 16.77 +/- 33.77% in the forskolin group compared with a decrease of 1.08 +/- 18.35% in the placebo group. Discussion: Oral ingestion of forskolin (250 mg of 10% forskolin extract twice a day) for a 12-week period was shown to favorably alter body composition while concurrently increasing bone mass and serum free testosterone levels in overweight and obese men. The results indicate that forskolin is a possible therapeutic agent for the management and treatment of obesity.
Scarpace PJ, Matheny M. Thermogenesis in brown adipose tissue with age: post-receptor activation by forskolin. Pflugers Arch. 1996 Jan;431(3):388-94. ABSTRACT: beta3-Adrenergic-stimulated thermogenesis in brown adipose tissue (BAT) is diminished with age. beta3-Adrenergic receptors are positively coupled to adenylyl cyclase in BAT. To determine whether thermo- genesis, in response to direct activation of adenylyl cyclase, is also impaired with age, we examined whole body oxygen consumption, mitochondrial guanosine diphosphate (GDP) binding and BAT mitochondrial uncoupling protein (UPC) mRNA levels in 4- and 24-month-old F-344 rats following forskolin administration. We also examined the forskolin-induced change in body temperature in 4-month-old rats. In some instances, the results were compared with administration of the specific beta3-adrenergic agonist, CGP-12177. Forskolin (3.5 mg/kg) increased oxygen consumption but decreased body temperature. In subsequent experiments the BAT was unilaterally denervated. In these rats, the forskolin-(1.8 mg/kg) stimulated increase in oxygen consumption was similar in young and old rats. Forskolin increased GDP binding and UCP mRNA levels in both the denervated and innervated BAT pads. The increases were equal or greater in the BAT from senescent rats. These findings, coupled with our previous report of an impaired CGP-12177-stimulated increase in GDP binding in senescent rats, suggests beta3-adrenergic-stimulated, but not post-receptor-stimulated, thermogenesis is diminished with age.
Majeed M et al. Diterpene forskolin: A possible new compound for reduction of body weight by increasing lean body mass. Nutraceuticals, March/April 2002, pp. 6-7. ABSTRACT: Maintaining or increasing lean body mass should be one of the important considerations of any weight loss strategy for the following reasons: 1. increase in lean body mass is proportionate to an increase in the body’s thermogenic response to food and the basic metabolic rate (BMR); 2. food induced thermogenesis controls body weight by an increase in catabolism of body fat (thermogenesis is preferentially fueled by fatty acids derived from body fat and/or from food); and 3. enhanced thermogenesis contributes to a buildup of lean body mass. An extract of Coleus forskohlii root, Benth. (Fam. Labiatae) standardized for diterpene forskolin was tested in an open-field study for weight loss and lean body mass increase. The study’s hypothesis was based on the recognized role of diterpene forskolin as the plant derived compound which stimulates enzyme adenylate cyclase and subsequently cyclic AMP (3’5’adenosine monophosphate) (1,2). Cyclic AMP may release fatty acids from the adipose tissue depots which may result in enhanced thermogenesis (3), loss of body fat, and theoretically increased lean body mass. Six overweight, but otherwise healthy, women were selected for the trial. Each participant was informed about the purpose of the study and was asked to sign an informed consent before entering the study. Each participant was examined by a physician at the inception and after 4 and 8 weeks of the study. The body composition was determined by bioelectrical impedance analysis. The forskolin formula was prepared in the form of two piece hard shell capsules. Each capsule contained 250 mg of the extract standardized for 10% forskolin, and each bottle contained 60 capsules. Participants were instructed to take one capsule in the morning and one in the evening, half an hour before a meal. Each participant was asked to maintain their previous daily physical exercise habits and eating habits. In addition, physical activity was monitored based on a questionnaire before and during the trial. The study was performed in an outpatient bariatric clinic at Hilton Head, S.C. and supervised by a physician specializing in bariatric medicine for over 30 years. During the eight week trial the mean values for body weight, and fat content were significantly decreased, whereas lean body mass was significantly increased as compared to the baseline (Wilcoxon matched pairs test). Weight loss was statistically significant.
Kamath. Efficacy and Safety of Forslean in Increasing Lean Body Mass. Department of Ayurvedic Medicine, Kasturba Medical College, Manipal, India, 2005.
Tsugiyoshi. Clinical report on root extract of Perilla Plant (coleus forskohlii) in reducing body fat. Asanto Institute, Tokyo, Japan, 2001.