CLINICAL STUDIES ON THE FOLLOWING INGREDIENTS:
Treatment of Erectile Dysfunction with Pycnogenol and L-arginine
Penile erection requires the relaxation of the cavernous smooth muscle, which is triggered by nitric oxide (NO). We investigated the possibility of overcoming erectile dysfunction (ED) by increasing the amounts of endogenous NO. For this purpose, we orally administered Pycnogenol, because it is known to increase production of NO by nitric oxide synthase together with L-arginine as a substrate for this enzyme. The study included 40 men, aged 25-45 years, without confirmed organic erectile dysfunction. Throughout the 3-month trial period, patients received 3 ampoules Sargenor a day, a drinkable solution of the dipeptide arginyl aspartate (equivalent to 1.7 g L-arginine per day). During the second month, patients were additionally supplemented with 40 mg Pycnogenol two times per day; during the third month, the daily dosage was increased to three 40-mg Pycnogenol tablets. We obtained a sexual function questionnaire and a sexual activity diary from each patient. After 1 month of treatment with L-arginine, a statistically nonsignificant number of 2 patients (5%) experienced a normal erection. Treatment with a combination of L-arginine and Pycnogenol for the following month increased the number of men with the restored sexual ability to 80%. Finally, after the third month of treatment, 92.5% of the men experienced a normal erection. We conclude that oral administration of L-arginine in combination with Pycnogenol causes a significant improvement in sexual function in men with ED without any side effects.
Stanislavov, R., and V. Nikolova. “Treatment of erectile dysfunction with pycnogenol and L-arginine.” Journal of Sex &Marital Therapy 29.3 (2003): 207-213.
Nitric oxide: a physiologic mediator of penile erection
Nitric oxide (NO) is a cytotoxic agent of macrophages, a messenger molecule of neurons, and a vasodilator produced by endothelial cells. NO synthase, the synthetic enzyme for NO, was localized to rat penile neurons innervating the corpora cavernosa and to neuronal plexuses in the adventitial layer of penile arteries. Small doses of NO synthase inhibitors abolished electrophysiologically induced penile erections. These results establish NO as a physiologic mediator of erectile function.
Burnett, Arthur L., et al. “Nitric oxide: a physiologic mediator of penile erection.” Science 257.5068 (1992): 401-403.
Effects of the nitric oxide synthase inhibitor NG‐nitro‐L‐arginine on the erectile response to cavernous nerve stimulation in the rabbit
Using a rabbit model, the involvement of the L‐arginine/nitric oxide pathway in penile erection was investigated. The mean basal intracavernous pressure was 21 cm H2O. Cavernous nerve stimulation (4–8 V, 20–30 Hz) increased the pressure to approximately 130 cm H2O. This response was highly reproducible and usually associated with full penile erection. The pressure increase could be quantified in terms of (1) the slope of the initial, ascending part of the pressure increase; (2) ΔP, which was defined as the maximal pressure obtained by the stimulation minus the basal pressure before the stimulation; (3) T90, which was defined as the time to reach 90 per cent of ΔP. Intrapenile administration of the L‐arginine/nitric oxide synthesis inhibitor NG‐nitro‐L‐arginine had no effect on systemic arterial blood pressure. However, NG‐nitro‐L‐arginine (0.22 and 2.19 mg), administered via the same route, abolished the erectile response induced by cavernous nerve stimulation; T90 increased and slope and ΔP decreased significantly. NG‐nitro‐D‐arginine (2.19), on the other hand, had no inhibitory effect. L‐arginine (21.07 mg), given either directly or after NG‐nitro‐L‐arginine had no consistent effect on the functional response to cavernous nerve stimulation.
The results suggest that pharmacologically induced effects on intracavernous pressure in the rabbit can be described quantitatively and that this model may be useful to study the mechanisms controlling penile erection in vivo. The pronounced inhibitory action of NG‐nitro‐L‐arginine demonstrates the important role of the arginine/nitric oxide pathway in mediating relaxation of penile smooth muscles necessary for erection.
Holmquist, F., et al. “Effects of the nitric oxide synthase inhibitor NG‐nitro‐L‐arginine on the erectile response to cavernous nerve stimulation in the rabbit.” Acta physiologica Scandinavica 143.3 (1991): 299-304.
The effectiveness of oral L-arginine in first-line treatment of erectile dysfunction in a controlled
Background and Aims: Relaxation of cavernous smooth muscle is a parasympathetic and non-adrenergic, non-cholinergic mediated process which requires nitric oxide (NO). NO is synthesized from L-arginine by NO synthase (NOS). Some studies report good clinical results under oral L-arginine medication in the treatment of erectile dysfunction. We examined the effectiveness and safety of L-arginine in the treatment of mixed-type impotence. Methods: 32 patients (mean age 51.6 years) with mixed-type impotence diagnosed according to the results of sexual history and urological examination were enrolled in a randomized, placebo-controlled, crossover comparison of an oral placebo with 3 × 500 mg L-arginine/day. A validated questionnaire (KEED) was used to define the grade of impotence with a score. The treatment consisted of two 17-day courses (50 tablets). After a 7-day washout period, the patients who initially received the placebo for 17 days were switched to L-arginine and vice versa. We assessed the efficacy with the validated questionnaire at the end of each drug period. Results: 30 patients (94%) completed the whole treatment schedule. Five (17%) patients reported a significant improvement in erectile function at the end of the L-arginine phase and 6 (20%) patients after the placebo period. 17 (56%) patients showed little improvement with L-arginine and 13 (43%) with placebo. In 8 patients (27%) of the verum group, there was either no change in the ED score or even a slight worsening. No statistical difference in the impotence scores was found. No drug-related adverse effects occurred with L-arginine treatment. Conclusion: Oral L-arginine 3 × 500 mg/day is not better than placebo as a first-line treatment for mixed-type impotence.
Klotz, T., et al. “Effectiveness of oral L-arginine in first-line treatment of erectile dysfunction in a controlled crossover study.” Urologia Internationalis 63.4 (1999): 220-223.
Efficacy and Safety of a Novel Combination of L-Arginine Glutamate and Yohimbine Hydrochloride: A New Oral Therapy for Erectile Dysfunction
Purpose: The goal of this double-blind, placebo-controlled, three-way crossover, randomized clinical trial was to compare the efficacy and safety of the combination of 6 g of L-arginine glutamate and 6 mg of yohimbine hydrochloride (AY) with that of 6 mg of yohimbine hydrochloride (YP) alone and that of placebo (PP) alone, for the treatment of erectile dysfunction (ED).
Materials and Methods: Forty-five patients were included in this study. During each of the 2-week, crossover periods, the drug was administered orally, one to two hours before intended sexual intercourse. The primary endpoint was changed in the Erectile Function Domain score of the International Index of Erectile Function (IIEF). The secondary endpoints were patient and investigator assessments of treatment success.
Results: At the end of each treatment period, the Erectile Function Domain scores for AY, YP, and PP were 17.2±7.17, 15.4±6.49 and 14.1±6.56, respectively. The difference between AY and PP was statistically significant (p=0.006). When stratified according to baseline scores over 14, those patients with mild to moderate MED had a better Erectile Function Domain response to treatment (AY=22.2±4.99, YP=18.2±5.59, PP=16.9±6.91, respectively) than those with scores 14 and below (AY=12.4±5.48, YP=12.7±6.25, PP=11.4±5.02, respectively). Investigators’ and patients’ assessment of efficacy was significantly improved by YP over PP.
Conclusions: This pilot study shows that the on-demand oral administration of the L-arginine glutamate 6 g and 6 mg yohimbine combination is effective in improving erectile function in patients with mild to moderate ED. It appears to be a promising addition to first-line therapy for ED.
Lebret, Thierry, et al. “Efficacy and safety of a novel combination of L-arginine glutamate and yohimbine hydrochloride: a new oral therapy for erectile dysfunction.” European Urology 41.6 (2002): 608-613.
Effect of Epimedium brevicornum Maxim extract on elicitation of penile erection in the rat
To investigate the effect and mechanism of Chinese medicine (Epimedium brevicornum Maxim [EbM]) on the elicitation of penile erection in the rat.
Adult male Sprague-Dawley rats were used. The penile intracavernous pressure (ICP) was monitored. Intracavernous administration of different doses (30, 100, 300, 1000, 3000, 6500, and 10,000 μg/0.1 mL) of EBM extract and saline 0.1 mL was done. Intracavernous NG-nitro-l-arginine methyl ester (l-NAME) (120 μg) was administered, followed by EBM extract 300 μg 10 minutes later. EBM extract (20, 10, and 10 μg) was stereotaxically delivered into the intracerebral ventricle, paraventricular nucleus of the hypothalamus, and hippocampus, respectively.
After intracavernous administration of 30 or 100 μg EBM extract, no significant change in ICP was noted. All other doses (300 to 10,000 μg) of EBM extract elicited a significant increase in ICP, with the greatest peak at 99.7 ± 0.3 mm Hg (resting 7.8 ± 1.0 mm Hg) after application of 6500 μg EBM extract. No change in ICP occurred with administration of l-NAME followed by EBM extract. Furthermore, intracavernous saline or administration of EBM extract into the intracerebral ventricle, paraventricular nucleus of the hypothalamus, or hippocampus was ineffective in inducing a significant change in ICP.
These results suggest that intracavernous administration of EBM extract may elicit penile erection in the rat. Nitric oxide may be involved in this penile erection-inducing effect. No central neural effect of EBM extract may exist in the elicitation of penile erection.
Chen, Kuang-Kuo, and Jen-Hwey Chiu. “Effect of Epimedium brevicornum Maxim extract on elicitation of penile erection in the rat.” Urology 67.3 (2006): 631-635.
Effect of lipid-based suspension of Epimedium koreanum Nakai extract on sexual behavior in rats
Herba of Epimedium koreanum is used in traditional Chinese and Korean herbal medicine as a potent enhancer of erectile function. Icariin, the main active component of Epimedium koreanum, possesses many biological effects, such as improving cardiovascular function, hormone regulation, immunological function modulation, and anti-tumor activity.
The aim of the Study
This study supports the traditional use of extracts from Epimedium species in erectile dysfunction.
Materials and Methods
The Epimedium koreanum dry extract was suspended in wheat germ oil using lecithin and bee wax for oral administration. The effect of oral administration of two compositions (E-01 and E-02) standardized by their icariin content on the number of complete intromissions, the number of ejaculations, and the latent period of ejaculation (LPE) in rats were evaluated. E-01 and E-02 were administered orally for 10 days to the experimental animals. The control animals received olive oil for 10 days. On day 10, 0.5 h after the dose was administered to male rats, one virgin female rat was placed with one male rat.
The number of complete intromissions increased to 23.3 ± 2.6 in the E-01 and E-02 group (dose 300 mg/kg body weight) (b.wt) and to 20.1 ± 2.3 in the E-02 group (dose 750 mg/kg b.wt) compared with 15.2 ± 2.4 in the control group of aged rats. The number of ejaculations increased from 1.1 ± 0.3 in the control-aged group to 2.6 ± 0.4 in the E-01 group. The LPE of male rats was 14.2 ± 1.8 min in the control-aged group. The LPE of the aged group was reduced to 9.8 ± 1.5 min, 9.8 ± 1.6 min, and 11.4 ± 1.8 min when treated with E-01 at a dose of 300 mg/kg b.wt, and E-02 at a dose of 300 mg/kg b.wt and 750 mg/kg b.wt, respectively.
It was established that oral administration of a lipid-based suspension of dry extract of Epimedium koreanum in wheat germ oil improved erectile function of aged rats.
Makarova, Marina N., et al. “Effect of lipid-based suspension of Epimedium koreanum Nakai extract on sexual behavior in rats.” Journal of Ethnopharmacology 114.3 (2007): 412-416.
The rise of Herbal and Traditional Medicine in Erectile Dysfunction Management
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.
Ho, Christopher CK, and Hui Meng Tan. “Rise of herbal and traditional medicine in erectile dysfunction management.” Current urology reports 12.6 (2011): 470-478.
Erectogenic and Neurotrophic Effects of Icariin, a Purified Extract of Horny Goat Weed (Epimedium spp.) In Vitro and In Vivo
Introduction. Epimedium species (aka horny goat weed) have been utilized for the treatment of erectile dysfunction in Traditional Chinese Medicine for many years. Icariin (ICA) is the active moiety of Epimedium species.
Aim. To evaluate the penile hemodynamic and tissue effects of ICA in cavernous nerve-injured rats. We also studied the in vitro effects of ICA on cultured pelvic ganglia.
Methods. Rats were subjected to cavernous nerve injury and subsequently treated for 4 weeks with daily gavage feedings of a placebo solution of normal saline and Dimethyl sulfoxide (DMSO) vs. ICA dissolved in DMSO at doses of 1, 5, and 10 mg/kg. A separate group underwent a single dose of ICA 10 mg/kg 2 hours prior to functional testing. Functional testing with cavernous nerve stimulation and real‐time assessment of intracavernous pressure (ICP) were performed at 4 weeks. After functional testing, penile tissue was procured for immunohistochemistry and molecular studies. In separate experiments, pelvic ganglia were excised from healthy rats and cultured in the presence of ICA, sildenafil, or placebo culture media.
Main Outcome Measure. The ratio of ICP and area under the curve (AUC) to mean arterial pressure (MAP) during cavernous nerve stimulation of subject rodents. We also assayed tissue expression of neuronal nitric oxide synthase (nNOS), eNOS: endothelial nitric oxide synthase (eNOS), calponin, and apoptosis via immunohistochemistry and Western blot. Serum testosterone and luteinizing hormone (LH) were assayed using enzyme‐linked immunosorbent assay (ELISA). Differential length of neurite outgrowth was assessed in cultured pelvic ganglia.
Results. Rats treated with low‐dose ICA demonstrated significantly higher ICP/MAP and AUC/MAP ratios compared with control and single‐dose ICA animals. Immunohistochemistry and Western blot were revealing of significantly greater positivity for nNOS and calponin in penile tissues of all rats treated with ICA. ICA led to significantly greater neurite length in cultured specimens of pelvic ganglia.
Conclusion. ICA may have neurotrophic effects in addition to known phosphodiesterase type 5 inhibiting effects. Shindel AW, Xin Z‐C, Lin G, Fandel TM, Huang YC, Banie L, Breyer BN, Garcia MM, Lin C‐S, and Lue TF. Erectogenic and neurotrophic effects of icariin, a purified extract of horny goat weed (Epimedium spp.) in vitro and in vivo. J Sex Med 2010;7:1518–1528.
Shindel, Alan W., et al. “Erectogenic and neurotrophic effects of icariin, a purified extract of horny goat weed (Epimedium spp.) in vitro and in vivo.” The journal of sexual medicine 7.4pt1 (2010): 1518-1528.
Clinical study of Tribulus Terrestris Linn. in Oligozoospermia: A double-blind study
After a detailed discussion on observations made and results achieved, this present study shows significant remission in the signs and symptoms of Kshina Shukra, vis-à-vis oligozoospermia, corroborated with a definite improvement in the total sperm count. In toto, from this study it can be concluded that the Alternate Hypothesis of this study is accepted, that is, Tribulus Terrestris. Linn is effective in the management of Kshina Shukra, with lifestyle modification. Tribulus Terrestris. Linn Granules have shown superior results in the management of Kshina Shukra, as compared to placebo granules.
Thirunavukkarasu M. Sellandi, Anup B. Thakar, and Madhav Singh Baghel. Clinical study of Tribulus Terrestris Linn. in Oligozoospermia: A double-blind study. Ayu. 2012 Jul-Sep; 33(3): 356–364. doi: 10.4103/0974-8520.108822.
Identification of fruits of Tribulus terrestris Linn. and Pedalium murex Linn.: A pharmacognostical approach
Gokshura is a well-known Ayurvedic drug that is used in many preparations. Botanically it is identified as Tribulus Terrestris Linn., especially the roots and fruits of the plant. But instead the fruits of another plant Pedalium murex Linn. are commonly used and the drug is frequently substituted. The pharmacognostic study has been carried out to identify the distinguishing features, both morphological and microscopic, of the fruits of Tribulus terrestris Linn. and Pedalium murex Linn. This knowledge should help reduce the problem of substitution of the genuine drug.
Short term impact of Tribulus Terrestris intake on doping control analysis of endogenous steroids
Tribulus Terrestris is a nutritional supplement highly debated regarding its physiological and actual effects on the organism. The main claimed effect is an increase in testosterone anabolic and androgenic action through the activation of endogenous testosterone production. Even if this biological pathway is not entirely proven, T. terrestris is regularly used by athletes. Recently, the analysis of two female urine samples by GC/C/IRMS (gas chromatography/combustion/isotope-ratio-mass-spectrometry) conclusively revealed the administration of exogenous testosterone or its precursors, even if the testosterone glucuronide/epitestosterone glucuronide (T/E) ratio and steroid marker concentrations were below the cut-off values defined by the World Anti-Doping Agency (WADA). Hence, the short-term treatment with T. terrestris showed no impact on the endogenous testosterone metabolism of the two subjects.
Saudan C1, Baume N, Emery C, Strahm E, Saugy M.Short term impact of Tribulus Terrestris intake on doping control analysis of endogenous steroids.Forensic Sci Int. 2008 Jun 10;178(1):e7-10. doi: 10.1016/j.forsciint.2008.01.003. Epub 2008 Feb 20.
Evaluation of the aphrodisiac activity of Tribulus terrestris Linn. in sexually sluggish male albino rats
A dose-dependent improvement in sexual behavior was observed with the Tribulus Terrestris (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 in the 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.
Surender Singh, Vinod Nair, and Yogendra K. Gupta. Evaluation of the aphrodisiac activity of Tribulus terrestris Linn. in sexually sluggish male albino rats.J Pharmacol Pharmacother. 2012 Jan-Mar; 3(1): 43–47. doi: 10.4103/0976-500X.92512
A systematic review on the herbal extract Tribulus Terrestris and the roots of its putative aphrodisiac and performance
Randomized control trials, which included healthy human subjects ingesting TT as a sole or combined supplement, along with animal studies with TT as a sole treatment across a number of species were included. 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.
Qureshi A, Naughton DP, Petroczi A. A systematic review on the herbal extract Tribulus Terrestris and the roots of its putative aphrodisiac and performance-enhancing effect. J Diet Suppl. 2014 Mar;11(1):64-79. doi: 10.3109/19390211.2014.887602.
Phytopharmacological overview of Tribulus Terrestris
Tribulus Terrestris (family Zygophyllaceae), commonly known as Gokshur or Gokharu or puncture vine, has been used for a long time in both the Indian and Chinese systems of medicine for treatment of various kinds of diseases. It has diuretic, aphrodisiac, antiurolithic, immunomodulatory, antidiabetic, absorption enhancing, hypolipidemic, cardiotonic, central nervous system, hepatoprotective, anti-inflammatory, analgesic, antispasmodic, anticancer, antibacterial, anthelmintic, larvicidal, and anticarcinogenic activities. The aim of this review is to create a database for further investigations of the discovered phytochemical and pharmacological properties of this plant to promote research.
Effect of Tribulus Terrestris on nicotinamide adenine dinucleotide phosphate-diaphorase activity and androgen receptors in rat brain
Administration of Tribulus Terrestris extract (TT) increased sexual behavior and intracavernous pressure both in normal and castrated rats and these effects were probably due to the androgen increasing property of TT. The objective of the present study is to evaluate the effect of TT on nicotinamide adenine dinucleotide phosphate-diaphorase (NADPH-d) activity and androgen receptor (AR) immunoreactivity in the rat brain. There was an increase in both NADPH-d (67%) and AR immunoreactivity (58%) in TT treated group and these results were statistically significant compared to the control. Chronic treatment of TT in rats increases the NADPH-d positive neurons and AR immunoreactivity in the PVN region. The mechanism for the observed increase in AR and NADPH-d positive neurons in the present study is probably due to the androgen increasing property of TT.
Gauthaman K, Adaikan PG. Effect of Tribulus Terrestris on nicotinamide adenine dinucleotide phosphate-diaphorase activity and androgen receptors in the rat brain. J Ethnopharmacol. 2005 Jan 4;96(1-2):127-32.
The Effect of Oral Feeding of Tribulus Terrestris L. on Sex Hormone and Gonadotropin Levels in Addicted Male Rats
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. Oral consumption of TT could markedly antagonize the reduction of sex hormones and gonadotropins (except for FSH) due to morphine addiction.
Ghosian Moghaddam MH, Khalili M, Maleki M, Ahmad Abadi ME. The Effect of Oral Feeding of Tribulus Terrestris L. on Sex Hormone and Gonadotropin Levels in Addicted Male Rats. Int J Fertil Steril. 2013 Apr;7(1):57-62. Epub 2013 Mar 6.
Effects and Mechanism of Action of a Tribulus Terrestris Extract on Penile Erection
Concentration-dependent relaxation effects of the extract on the corpus cavernosum (CC) were detected in the organ bath study. Relaxation of the CC by the T. terrestris extract was inhibited in both an endothelium-removed group and an L-arginine methyl ester pretreatment group. The intracavernous pressure (ICP) measured after oral administration of the T. terrestris extract for 1 month was higher than that measured in the control group, and a significant increase in cAMP was observed in the T. terrestris extract group. The T. terrestris extract induced concentration-dependent relaxation of the CC in an organ bath. The mechanism included a reaction involving the nitric oxide/nitric oxide synthase pathway and endothelium of the CC. Moreover, in an in vivo study, the T. terrestris extract showed a significant concentration-dependent increase in ICP. Accordingly, the T. terrestris extract may improve erectile function.
Jungmo Do, Seemin Choi, Jaehwi Choi, and Jae Seog Hyun. Effects and Mechanism of Action of a Tribulus Terrestris Extract on Penile Erection. Korean J Urol. 2013 Mar; 54(3): 183–188. Published online 2013 Mar 15. doi: 10.4111/kju.2013.54.3.183
The effects of Tribulus Terrestris on body composition and exercise performance in resistance-trained males
There were no changes in body weight, percentage fat, total body water, dietary intake, or mood states in either group. Muscle endurance (determined by the maximal number of repetitions at 100-200% of body weight) increased for the bench and leg press exercises in the placebo group (p <.05; bench press +/-28.4%, leg press +/-28.6%), while the Tribulus group experienced an increase in leg press strength only (bench press +/-3.1%, not significant; leg press +/-28.6%, p <.05). Supplementation with Tribulus does not enhance body composition or exercise performance in resistance-trained males.
Antonio J, Uelmen J, Rodriguez R, Earnest C. The effects of Tribulus Terrestris on body composition and exercise performance in resistance-trained males. Int J Sport Nutr Exerc Metab. 2000 Jun;10(2):208-15.
Chemical constituents from Tribulus Terrestris and screening of their antioxidant activity
Two oligosaccharides (1,2) and a stereoisomer of di-p-coumaroylquinic acid (3) were isolated from the aerial parts of Tribulus Terrestris along with five known compounds (4-8). This is the first report for the complete NMR spectral data of the known 4,5-di-p-trans-coumaroylquinic acid (4). The antioxidant activity represented as DPPH free radical scavenging activity was investigated revealing that the di-p-coumaroylquinic acid derivatives possess potent antioxidant activity so considered the major constituents contributing to the antioxidant effect of the plant.
Hammoda HM, Ghazy NM, Harraz FM, Radwan MM, ElSohly MA, Abdallah II.Chemical constituents from Tribulus Terrestris and screening of their antioxidant activity. Phytochemistry. 2013 Aug;92:153-9. doi: 10.1016/j.phytochem.2013.04.005. Epub 2013 May 2.
Sexual effects of puncturevine (Tribulus Terrestris) extract (protodioscin): an evaluation using a rat model
The weight gain and improvement in sexual behavior parameters observed in rats could be secondary to the androgen increasing property of TT (PTN) that was observed in our earlier study on primates. The increase in ICP which confirms the proerectile aphrodisiac property of TT could possibly be the result of an increase in androgen and subsequent release of nitric oxide from the nerve endings innervating the corpus cavernosum.
The hormonal effects of Tribulus Terrestris and its role in the management of male erectile dysfunction–an evaluation using primates, rabbit and rat
TT extract was administered intravenously, as a bolus dose of 7.5, 15 and 30 mg/kg, in primates for acute study. Rabbits and normal rats were treated with 2.5, 5 and 10mg/kg of TT extract orally for 8 weeks, for chronic study. In addition, castrated rats were treated either with testosterone cypionate (10mg/kg, subcutaneously; biweekly for 8 weeks) or TT orally (5mg/kg daily for 8 weeks). In primates, the increases in T (52%), DHT (31%) and DHEAS (29%) at 7.5mg/kg were statistically significant. In castrated rats, increases in T levels by 51% and 25% were observed with T and TT extract respectively that were statistically significant.
Gauthaman K, Ganesan AP.The hormonal effects of Tribulus Terrestris and its role in the management of male erectile dysfunction–an evaluation using primates, rabbit, and rat.Phytomedicine. 2008 Jan;15(1-2):44-54.
The aphrodisiac herb Tribulus Terrestris does not influence the androgen production in young men
There was no significant difference between Tribulus Terrestris supplemented groups and controls in the serum testosterone… All results were within the normal range. The findings in the current study anticipate that Tribulus Terrestris steroid saponins possess neither direct nor indirect androgen-increasing properties
In vivo and in vitro animal investigation of the effect of a mixture of herbal extracts from Tribulus Terrestris and Cornus Officinalis on penile erection
- terrestris extract, C. officinalis extract, and the mixture of both extracts showed concentration-dependent relaxation effects of the CC. In both the endothelium-removed group and N(G)-nitro-L-arginine methyl ester pretreatment group, T. terrestris extract inhibited relaxation. ICP measured after oral administration of the extract mixture for a month was higher than that measured in the control group, and a significant increase in cAMP was observed in the mixture group. T. terrestris extract and C. officinalis extract exhibited concentration-dependent relaxation in an organ bath. In the in vivo study of the extract mixture, ICP and cAMP was significantly potentiated. Accordingly, the mixture of T. terrestris extract and C. Officinalis extract may improve erectile function.
Kam SC, Do JM, Choi JH, Jeon BT, Roh GS, Hyun JS. In vivo and in vitro animal investigation of the effect of a mixture of herbal extracts from Tribulus Terrestris and Cornus Officinalis on penile erection.J Sex Med. 2012 Oct;9(10):2544-51. doi: 10.1111/j.1743-6109.2012.02889.x. Epub 2012 Aug 20.
Proerectile pharmacological effects of Tribulus Terrestris extract on the rabbit corpus cavernosum
The relaxant responses to acetylcholine, nitroglycerin, and EFS by more than 10%, 24%, and 10% respectively compared to their control values and the lack of such effect on the contractile response to noradrenaline and histamine indicate that PTN has a proerectile activity. The enhanced relaxant effect observed is probably due to an increase in the release of nitric oxide from the endothelium and nitrergic nerve endings, which may account for its claims as an aphrodisiac. However, further study is needed to clarify the precise mechanism of its action.
The In Vitro and In Vivo Anti-Cancer Activities of a Standardized Quassinoids Composition from Eurycoma longifolia on LNCaP Human Prostate Cancer Cells.
We hypothesized that androgen could modulate CCL2 expression in hormone-responsive prostate cancer cells and thereby promote recruitment of monocytes. Dihydrotestosterone was found to induce a time-dependent (0-72 hours) and concentration-dependent (0-1 nmol/L) increase in CCL2 mRNA levels in androgen-responsive human prostate cancer cells (LNCaP). This increase in CCL2 mRNA corresponded with increased secretion of CCL2 protein. The effect of dihydrotestosterone was mediated through an androgen receptor (AR)-dependent pathway as small inhibitor RNA against AR negated the induction of CCL2. Both I3C and DIM inhibited promotional effects of dihydrotestosterone on CCL2 and migration.
Tong KL, Chan KL, Abubakar S, Low BS, Ma HQ, Wong PF. The In Vitro and In Vivo Anti-Cancer Activities of a Standardized Quassinoids Composition from Eurycoma longifolia on LNCaP Human Prostate Cancer Cells. LoS One. 2015 Mar 31;10(3):e0121752. doi: 10.1371/journal.pone.0121752. eCollection 2015.
Production of biomass and bioactive compounds from adventitious roots by optimization of culturing conditions of Eurycoma longifolia in a balloon-type bubble bioreactor system.
The effects of the type and concentration of auxin on root growth were studied, as well as the effects of the NH4(+): NO3(-) ratio on adventitious root growth and the production of phenolics and flavonoids. The adventitious roots were thin, numerous, and elongated in 3/4 MS medium supplemented with 5.0 and 7.0 mg L(-1) IBA, whereas the lateral roots were shorter and thicker with 5.0 mg L(-1) NAA compared with IBA treatment. High phenolic and flavonoid productions (38.59 and 11.27 mg L(-1) medium, respectively) were also obtained with a ratio of 15:30. These results suggest that balloon-type bubble bioreactor cultures are suitable for the large-scale commercial production of E. longifolia adventitious roots which contain high yield of bioactive compounds.
Lulu T, Park SY, Ibrahim R, Paek KY.Production of biomass and bioactive compounds from adventitious roots by optimization of culturing conditions of Eurycoma longifolia in balloon-type bubble bioreactor system.J Biosci Bioeng. 2015 Jun;119(6):712-7. doi: 10.1016/j.jbiosc.2014.11.010. Epub 2014 Dec 12.
Eurycomanone and eurycomanol from Eurycoma longifolia Jack as regulators of signaling pathways involved in proliferation, cell death, and inflammation.
Eurycomanone and eurycomanol are two quassinoids from the roots of Eurycoma longifolia Jack. The aim of this study was to assess the bioactivity of these compounds in Jurkat and K562 human leukemia cell models compared to peripheral blood mononuclear cells from healthy donors. Both eurycomanone and eurycomanol inhibited Jurkat and K562 cell viability and proliferation without affecting healthy cells. Interestingly, eurycomanone inhibited NF-κB signaling through inhibition of IκBα phosphorylation and upstream mitogen-activated protein kinase (MAPK) signaling, but not eurycomanol. In conclusion, both quassinoids present differential toxicity towards leukemia cells, and the presence of the α,β-unsaturated ketone in eurycomanone could be prerequisite for the NF-κB inhibition.
Hajjouli S, Chateauvieux S, Teiten MH, Orlikova B, Schumacher M, Dicato M, Choo CY, Diederich M.Eurycomanone and eurycomanol from Eurycoma longifolia Jack as regulators of signaling pathways involved in proliferation, cell death, and inflammation. Molecules. 2014 Sep 16;19(9):14649-66. doi: 10.3390/molecules190914649.
Supplementation of Eurycoma longifolia Jack Extract for 6 Weeks Does Not Affect Urinary Testosterone: Epitestosterone Ratio, Liver and Renal Functions in Male Recreational Athletes.
Supplementation of ElJ i.e. Physta(®) at a dosage of 400 mg/day for 6 weeks did not affect the urinary T: E ratio and hence will not breach any doping policies of the International Olympic Committee for the administration of exogenous testosterone or its precursor. In addition, the supplementation of ElJ at this dosage and duration was safe as it did adversely affect the liver and renal functions.
Chen CK, Mohamad WM, Ooi FK, Ismail SB, Abdullah MR, George A.Supplementation of Eurycoma longifolia Jack Extract for 6 Weeks Does Not Affect Urinary Testosterone: Epitestosterone Ratio, Liver and Renal Functions in Male Recreational Athletes. Int J Prev Med. 2014 Jun;5(6):728-33.
Effects of a Proprietary Freeze-Dried Water Extract of Eurycoma longifolia (Physta) and Polygonum minus on Sexual Performance and Well-Being in Men: A Randomized, Double-Blind, Placebo-Controlled Study.
Background. Methods. Outcome measures included validated questionnaires that aimed to evaluate erectile function, satisfaction with the intervention, sexual intercourse performance, erectile hardness, mood, and overall quality of life. Results. 12 subjects in the active group and 14 in the placebo group completed the study. Significant improvements were noted in scores for the Sexual Intercourse Attempt diary, Erection Hardness Scale, Sexual Health Inventory of Men, and Aging Male Symptom scale (P < 0.05 for all). Conclusion. Supplementation for twelve weeks with Polygonum minus and the proprietary Eurycoma longifolia extract, Physta, was well tolerated and more effective than placebo in enhancing sexual performance in healthy volunteers.
Udani JK, George AA, Musthapa M, Pakdaman MN, Abas A.Effects of a Proprietary Freeze-Dried Water Extract of Eurycoma longifolia (Physta) and Polygonum minus on Sexual Performance and Well-Being in Men: A Randomized, Double-Blind, Placebo-Controlled Study. Evid Based Complement Alternat Med. 2014;2014:179529. doi: 10.1155/2014/179529. Epub 2014 Jan 12.
Four new quassinoids from the roots of Eurycoma longifolia Jack.
Seven compounds were isolated from the roots of Eurycoma longifolia and characterized by comprehensive analysis of 1D and 2D NMR experiments along with single crystal X-ray diffraction. Among them, four new quassinoids were identified and three of them were diastereomers for each other. Compounds 1-7 were evaluated for cytotoxicities against HT-29, MCF-7, LOVO, BGC-823, MGC-803, HepG2, HeLa, and A549 cancer cell lines. Compounds 2 and 5 exhibited the lowest IC50 values of 24.9 μM, 11.8 μM, and 44.1 μM, 14.1 μM towards MCF-7, MGC-803 cancer cell lines, respectively, while compound 6 exhibited moderate cytotoxicity towards all the selected cancer cell lines.
Eurycoma longifolia in Radix for the treatment of an ethanol-induced gastric lesion in rats.
The effect of treatment with Radix on ethanol-induced gastric lesions was investigated. Three groups were given 0.5 mL 100% ethanol orally. One group that was administered with ethanol was only given distilled water orally (no treatment). (Radix) and oral ranitidine 21.4 mg kg(-1) b.wt. (Ranitidine), respectively. There was no difference in ulcer index between the Radix and ranitidine group. The gastric MDA content was significantly higher in all the groups that were induced with ethanol compared to the control group but no difference between all the ethanol-induced groups.
Phytoandrogenic properties of Eurycoma longifolia as a natural alternative to testosterone replacement therapy.
This significant decline in testosterone levels is further closely linked with medical conditions such as obesity, metabolic syndrome, diabetes or hypertension. Apart from the beneficial effects of TRT, significant adverse side effects have been described, and prostate cancer (PCa) as absolute contraindication is debated. Eurycoma longifolia (Tongkat Ali; TA) is a natural alternative to TRT and has been shown to restore serum testosterone levels, thus significantly improving sexual health. This includes significant positive effects on bone health and physical condition of patients.
George A, Henkel R.Phytoandrogenic properties of Eurycoma longifolia as a natural alternative to testosterone replacement therapy.Andrologia. 2014 Sep;46(7):708-21. doi: 10.1111/and.12214. Epub 2014 Jan 6. Review.
Acute, reproductive toxicity and two-generation teratology studies of a standardized quassinoid-rich extract of Eurycoma longifolia Jack in Sprague-Dawley rats.
The roots of Eurycoma longifolia Jack are popularly sought as herbal medicinal supplements to improve libido and general health amongst the local ethnic population. The major quassinoids of E. longifolia improved spermatogenesis and fertility but toxicity studies have not been well documented. The reproductive toxicity, two generations of fetus teratology and the up-and-down acute toxicity were investigated in Sprague-Dawley rats orally treated with quassinoid-rich E. longifolia extract (TAF273). The results showed that the median lethal dose (LD50 ) of TAF273 for female and male rats was 1293 and >2000 mg/kg, respectively. Fertility index and litter size of the TAF273 treated were significantly increased when compared with those of the non-treated animals. The TAF273-treated dams decreased in percentage of pre-implantation loss, post-implantation loss, and late resorption. Any human dose derived from converting the rat doses of 100 mg/kg and below may be considered as safe for further clinical studies.
Low BS, Das PK, Chan KL.Acute, reproductive toxicity and two-generation teratology studies of a standardized quassinoid-rich extract of Eurycoma longifolia Jack in Sprague-Dawley rats. Phytother Res. 2014 Jul;28(7):1022-9. doi: 10.1002/ptr.5094. Epub 2013 Dec 6.
Evaluation of Acute 13-Week Subchronic Toxicity and Genotoxicity of the Powdered Root of Tongkat Ali (Eurycoma longifolia Jack).
Tongkat Ali (Eurycoma longifolia) is an indigenous traditional herb in Southern Asia. Its powdered root has been processed to produce health supplements, but no detailed toxicology report is available. In this study, neither mutagenicity nor clastogenicity was noted, and acute oral LD50 was more than 6 g/kg b.w. After 4-week subacute and 13-week subchronic exposure paradigms (0, 0.6, 1.2, and 2 g/kg b.w./day), adverse effects attributable to test compound were not observed with respect to body weight, hematology, serum biochemistry, urinalysis, macropathology, or histopathology. However, the treatment significantly reduced prothrombin time, partial thromboplastin time, blood urea nitrogen, creatinine, aspartate aminotransferase, creatine phosphate kinase, lactate dehydrogenase, and cholesterol levels, especially in males (P < 0.05). These changes were judged as pharmacological effects, and they are beneficial to health. The calculated acceptable daily intake (ADI) was up to 1.2 g/adult/day. This information will be useful for product development and safety management.
Li CH, Liao JW, Liao PL, Huang WK, Tse LS, Lin CH, Kang JJ, Cheng YW. Evaluation of Acute 13-Week Subchronic Toxicity and Genotoxicity of the Powdered Root of Tongkat Ali (Eurycoma longifolia Jack).Evid Based Complement Alternat Med. 2013;2013:102987. doi: 10.1155/2013/102987. Epub 2013 Aug 25.
The anti-angiogenic quassinoid-rich fraction from Eurycoma longifolia modulates endothelial cell function.
In the present study, the antiangiogenic potential of partially purified quassinoid-rich fraction (TAF273) of E. longifolia root extract was evaluated using ex vivo and in vivo angiogenesis models and the anti-angiogenic efficacy of TAF273 was investigated in human umbilical vein endothelial cells (HUVEC). TAF273 caused significant suppression in sprouting of microvessels in rat aorta with IC50 11.5μg/ml. TAF273 (50μg/ml) showed remarkable inhibition (63.13%) of neovascularization in the chorioallantoic membrane of a chick embryo. In vitro, TAF273 significantly inhibited the major angiogenesis steps such as proliferation, migration, and differentiation of HUVECs. Phytochemical analysis revealed a high content of quassinoids in TAF273.
Al-Salahi OS, Kit-Lam C, Majid AM, Al-Suede FS, Mohammed Saghir SA, Abdullah WZ, Ahamed MB, Yusoff NM. The anti-angiogenic quassinoid-rich fraction from Eurycoma longifolia modulates endothelial cell function. Microvasc Res. 2013 Nov;90:30-9. doi: 10.1016/j.mvr.2013.07.007. Epub 2013 Jul 27.
Eurycomanone, the major quassinoid in Eurycoma longifolia root extract increases spermatogenesis by inhibiting the activity of phosphodiesterase and aromatase in steroidogenesis.
Eurycomanone enhanced testosterone steroidogenesis at the Leydig cells by inhibiting aromatase conversion of testosterone to estrogen, and at a high concentration may also involve phosphodiesterase inhibition. The quassinoid may be worthy for further development as a phytomedicine to treat testosterone-deficient idiopathic male infertility and sterility.
Low BS, Choi SB, Abdul Wahab H, Das PK, Chan KL.Eurycomanone, the major quassinoid in Eurycoma longifolia root extract increases spermatogenesis by inhibiting the activity of phosphodiesterase and aromatase in steroidogenesis. J Ethnopharmacol. 2013 Aug 26;149(1):201-7. doi: 10.1016/j.jep.2013.06.023. Epub 2013 Jun 27.
Tongkat Ali as a potential herbal supplement for physically active male and female seniors–a pilot study.
Thirteen physically active male and 12 physically active female seniors (57-72 years) were supplemented with 400-mg TA extract daily for 5 weeks. After treatment, hemoglobin, testosterone, and dehydroepiandrosterone concentrations, and the ratio of total testosterone/cortisol and muscle force remained significantly lower in female seniors than in male seniors. Treatment resulted in significant increases in total and free testosterone concentrations and muscular force in men and women. The study affirms the ergogenic benefit of TA through enhanced muscle strength.
Henkel RR, Wang R, Bassett SH, Chen T, Liu N, Zhu Y, Tambi MI.Tongkat Ali as a potential herbal supplement for physically active male and female seniors–a pilot study.Phytother Res. 2014 Apr;28(4):544-50. doi: 10.1002/ptr.5017. Epub 2013 Jun 11.
In vivo effects of Eurycoma longifolia Jack (Tongkat Ali) extract on reproductive functions in the rat.
An aqueous extract of Eurycoma longifolia (Tongkat Ali; TA) roots is traditionally used to enhance male sexuality. 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). 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. Testosterone concentration increased by 30.2% (P = 0.0544). Muscle weight also increased, yet not significantly.
Solomon MC, Erasmus N, Henkel RR.In vivo effects of Eurycoma longifolia Jack (Tongkat Ali) extract on reproductive functions in the rat. Andrologia. 2014 May;46(4):339-48. doi: 10.1111/and.12082. Epub 2013 Mar 6.
Standardized quassinoid-rich Eurycoma longifolia extract improved spermatogenesis and fertility in male rats via the hypothalamic-pituitary-gonadal axis.
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 was almost similar in the concentration of eurycomanone, the major and most potent quassinoid. 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). 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). The standardized 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.
Low BS, Das PK, Chan KL.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. doi: 10.1016/j.jep.2012.11.013. Epub 2012 Dec 20.
Randomized Clinical Trial on the Use of PHYSTA Freeze-Dried Water Extract of Eurycoma longifolia for the Improvement of Quality of Life and Sexual Well-Being in Men.
A randomized, double-blind, placebo-controlled, parallel group study was carried out to investigate the clinical evidence of E. longifolia in men. Primary endpoints were the Quality of Life investigated by SF-36 questionnaire and Sexual Well-Being investigated by International Index of Erectile Function (IIEF) and Sexual Health Questionnaires (SHQ); Seminal Fluid Analysis (SFA), fat mass and safety profiles. The E. longifolia (EL) group significantly improved in the domain Physical Functioning of SF-36, from baseline to week 12 compared to placebo (P = 0.006) and in between group at week 12 (P = 0.028). All safety parameters were comparable to placebo.
Ismail SB, Wan Mohammad WM, George A, Nik Hussain NH, Musthapa Kamal ZM, Liske E.Randomized Clinical Trial on the Use of PHYSTA Freeze-Dried Water Extract of Eurycoma longifolia for the Improvement of Quality of Life and Sexual Well-Being in Men. Evid Based Complement Alternat Med. 2012;2012:429268. doi: 10.1155/2012/429268. Epub 2012 Nov 1.
Eurycoma longifolia upregulates osteoprotegerin gene expression in androgen- deficient osteoporosis rat model.
Supplementation with Eurycoma longifolia (EL) extract elevated the testosterone levels, reduced the bone resorption marker and upregulated OPG gene expression of the orchidectomised rats. These actions may be responsible for the protective effects of EL extract against bone resorption due to androgen deficiency.
Shuid AN, El-arabi E, Effendy NM, Razak HS, Muhammad N, Mohamed N, Soelaiman IN. Eurycoma longifolia upregulates osteoprotegerin gene expression in an androgen-deficient osteoporosis rat model.BMC Complement Altern Med. 2012 Sep 12;12:152. doi: 10.1186/1472-6882-12-152.
Effects of Eurycoma longifolia on Testosterone Level and Bone Structure in an Aged Orchidectomised Rat Model.
Testosterone replacement is the choice of treatment in androgen-deficient osteoporosis. Thirty-six male Sprague-Dawley rats aged 12 months were divided into normal control, normal rat supplemented with EL, sham-operated, orchidectomised-control, orchidectomised with testosterone replacement, and orchidectomised with EL supplementation groups. Testosterone replacement was able to raise the testosterone level and restore the bone volume of orchidectomised rats. EL supplementation failed to emulate both these testosterone actions.
Tajul Ariff AS, Soelaiman IN, Pramanik J, Shuid AN.Effects of Eurycoma longifolia on Testosterone Level and Bone Structure in an Aged Orchidectomised Rat Model. Evid Based Complement Alternat Med. 2012;2012:818072. doi: 10.1155/2012/818072. Epub 2012 Aug 26.
Combined Effects of Eurycoma longifolia and Testosterone on Androgen-Deficient Osteoporosis in a Male Rat Model.
Forty male Sprague-Dawley rats were divided into sham-operated (SHAM), orchidectomized-control (ORX), orchidectomized with testosterone (ORX + T), orchidectomized with EL (ORX + EL), and orchidectomized with combined T and EL therapy (ORX + T + EL). T was injected intramuscularly at 8 mg/kg and 4 mg/kg for the ORX + T and ORX + T + EL groups, respectively. Biomechanically, the strain parameter of the ORX + T + EL group was significantly higher than the ORX group (P < 0.05). Thus, the combination therapy of EL and low-dose T has the potential for treatment of androgen-deficient osteoporosis.
Saadiah Abdul Razak H, Shuid AN, Naina Mohamed I.Combined Effects of Eurycoma longifolia and Testosterone on Androgen-Deficient Osteoporosis in a Male Rat Model. Evid Based Complement Alternat Med. 2012;2012:872406. doi: 10.1155/2012/872406. Epub 2012 Aug 9.
Eurycoma longifolia: Medicinal Plant in the Prevention and Treatment of Male Osteoporosis due to Androgen Deficiency.
Osteoporosis in elderly men is now becoming an alarming health issue due to its relation with a higher mortality rate compared to osteoporosis in women. Androgen deficiency (hypogonadism) is one of the major factors of male osteoporosis and it can be treated with testosterone replacement therapy (TRT). However, one medicinal plant, Eurycoma longifolia Jack (EL), can be used as an alternative treatment to prevent and treat male osteoporosis without causing the side effects associated with TRT. EL exerts pro-androgenic effects that enhance testosterone level, as well as stimulate osteoblast proliferation and osteoclast apoptosis. This will maintain bone remodeling activity and reduce bone loss. Phytochemical components of EL may also prevent osteoporosis via its antioxidative property. Hence, EL has the potential as a complementary treatment for male osteoporosis.
Mohd Effendy N, Mohamed N, Muhammad N, Naina Mohamad I, Shuid AN.Eurycoma longifolia: Medicinal Plant in the Prevention and Treatment of Male Osteoporosis due to Androgen Deficiency. Evid Based Complement Alternat Med. 2012;2012:125761. doi: 10.1155/2012/125761. Epub 2012 Jul 15.
Effect of Eurycoma longifolia Jack (Tongkat Ali) extracts on human spermatozoa in vitro.
A sample without addition of TA served as control. For washed spermatozoa, significant dose-dependent trends were found for vitality, total motility, acrosome reaction, and reactive oxygen species-positive spermatozoa. Contrary, the increase in the percentage of acrosome-reacted spermatozoa with increasing TA concentrations is very significant (P < 0.0001), and a significant difference (P = 0.0069) to the control could even be recorded at 20 μg TA per ml. Results indicate that the TA extract has no deleterious effects on sperm functions at therapeutically used concentrations (<2.5 μg ml(-1) ). However, at very high concentrations, TA may have harmful effects in vitro.
Erasmus N, Solomon MC, Fortuin KA, Henkel RR. Effect of Eurycoma longifolia Jack (Tongkat Ali) extracts on human spermatozoa in vitro. Andrologia. 2012 Oct;44(5):308-14. doi: 10.1111/j.1439-0272.2012.01282.x. Epub 2012 Feb 15.
Standardized water-soluble extract of Eurycoma longifolia, Tongkat Ali, as a testosterone booster for managing men with late-onset hypogonadism?
Considering that human studies are not available, 76 of 320 patients suffering from late-onset hypogonadism (LOH) were given 200 mg of a standardized water-soluble extract of Tongkat Ali for 1 month. The Ageing Males’ Symptoms (AMS) according to the standardized rating scale and the serum testosterone concentration were taken. Results show that treatment of LOH patients with this Tongkat Ali extract significantly (P < 0.0001) improved the AMS score as well as the serum testosterone concentration.
Tambi MI, Imran MK, Henkel RR.Standardized water-soluble extract of Eurycoma longifolia, Tongkat Ali, as a testosterone booster for managing men with late-onset hypogonadism?Andrologia. 2012 May;44 Suppl 1:226-30. doi: 10.1111/j.1439-0272.2011.01168.x. Epub 2011 Jun 15.
The effect of Eurycoma longifolia on sperm quality of male rats.
The standardized MeOH extract at doses of 50, 100 and 200 mg/kg, the EtOAc fraction (70 mg/kg), and standardized MeOH extract at 200 mg/kg co-administered with the EtOAc fraction of A. paniculata at 70 mg/kg were each given orally to male Sprague-Dawley albino rats for 48 consecutive days. The spermatozoa count, morphology, motility, plasma testosterone level and Leydig cell count of the animals were statistically analyzed by ANOVA with a post-hoc Tukey HSD test. The plasma testosterone level of the rats treated with the standardized MeOH extract at 200 mg/kg was significantly increased (p < 0.01) when compared with that of the control and infertile animals.
Influence of Eurycoma longifolia on the copulatory activity of sexually sluggish and impotent male rats.
Concerning the copulatory activity of sexually sluggish rats, both acute (dosed at 500 and 1000 mg/kg) and subacute treatments with the root powder significantly reduced ejaculation latencies, increasing also the percentage of mounting and ejaculating animals; in addition, the subacute administration reduced post-ejaculatory interval. In impotent rats, both subacute and subchronic treatments increased the percentage of mounting and ejaculating rats. The motivational behavior of sluggish rats during the partner preference test was not affected by the treatments. Testosterone serum levels were increased in rats subacutely treated in comparison with controls.
Eurycoma longifolia root improved sexual performance but not the motivation in sluggish rats after acute or subacute administration. The effect could be mainly ascribed to increased testosterone levels.
Zanoli P, Zavatti M, Montanari C, Baraldi M.Influence of Eurycoma longifolia on the copulatory activity of sexually sluggish and impotent male rats. J Ethnopharmacol. 2009 Nov 12;126(2):308-13. doi: 10.1016/j.jep.2009.08.021. Epub 2009 Aug 22.