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Study of antihypertensive mechanism of Tribulus terrestris in 2K1C hypertensive rats: role of tissue ACE activity.

Tribulus terrestris is a natural herb used for treating many diseases including hypertension. According to previous reports, aqueous extract of tribulus fruits may have some antihypertensive effect with an unknown mechanism. The present study investigated the antihypertensive mechanism of tribulus in 2K1C hypertensive rats by measurement of circulatory and local ACE activity in aorta, heart, kidney and lung. Four groups of rats were selected; control, sham, operated or hypertensive and tribulus treated hypertensive group. Hypertension was induced using silver clip on renal artery by surgery. Four weeks after surgery, a single daily dose of 10 mg/kg of lyophilized aqueous extract of tribulus fruit were given orally to 2K1C rats for four weeks. ACE activity was determined by high performance liquid chromatography (HPLC). Blood pressure was measured by the tail-cuff method. The systolic blood pressure (SBP) was significantly increased in 2K1C rats compared to control rats. The SBP of tribulus fed hypertensive rats was significantly decreased compared to hypertensive rats. The ACE activity in all tissues of 2K1C rats including: aorta, heart, kidney, lung as well as serum were significantly increased compared to normal rats. The ACE activity in all tissues of tribulus fed hypertensive rats was significantly lower than that of hypertensive rats, which was more pronounced in kidney. These results indicated that there is a negative correlation between consumption of tribulus and ACE activity in serum and different tissues in 2K1C rats.

Angiotensin-Converting Enzyme Inhibitors↗

The aphrodisiac herb Tribulus terrestris does not influence the androgen production in young men.

OBJECTIVE: The aim of the current study is to investigate the influence of Tribulus terrestris extract on androgen metabolism in young males. DESIGN AND METHODS: Twenty-one healthy young 20-36 years old men with body weight ranging from 60 to 125 kg were randomly separated into three groups-two experimental (each n=7) and a control (placebo) one (n=7). The experimental groups were named TT1 and TT2 and the subjects were assigned to consume 20 and 10 mg/kg body weight per day of Tribulus terrestris extract, respectively, separated into three daily intakes for 4 weeks. Testosterone, androstenedione and luteinizing hormone levels in the serum were measured 24 h before supplementation (clear probe), and at 24, 72, 240, 408 and 576 h from the beginning of the supplementation. RESULTS: There was no significant difference between Tribulus terrestris supplemented groups and controls in the serum testosterone (TT1 (mean+/-S.D.: 15.75+/-1.75 nmol/l); TT2 (mean+/-S.D.: 16.32+/-1.57 nmol/l); controls (mean+/-S.D.: 17.74+/-1.09 nmol/l) (p>0.05)), androstenedione (TT1 (mean+/-S.D.: 1.927+/-0.126 ng/ml); TT2 (mean+/-S.D.: 2.026+/-0.256 ng/ml); controls (mean+/-S.D.: 1.952+/-0.236 ng/ml) (p>0.05)) or luteinizing hormone (TT1 (mean+/-S.D.: 4.662+/-0.274U/l); TT2 (mean+/-S.D.: 4.103+/-0.869U/l); controls (mean+/-S.D.: 4.170+/-0.406U/l) (p>0.05)) levels. 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. The study will be extended in the clarifying the probable mode of action of Tribulus terrestris steroid saponins.

Adult↗

The effects of Tribulus terrestris on body composition and exercise performance in resistance-trained males.

The purpose of this study was to determine the effects of the herbal preparation Tribulus terrestris (tribulus) on body composition and exercise performance in resistance-trained males. Fifteen subjects were randomly assigned to a placebo or tribulus (3.21 mg per kg body weight daily) group. Body weight, body composition, maximal strength, dietary intake, and mood states were determined before and after an 8-week exercise (periodized resistance training) and supplementation period. 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.

Adult↗

[Effect of Tribulus terrestris L decoction of different concentrations on tyrosinase activity and the proliferation of melanocytes].

OBJECTIVE: To study the effects of the decoction of Tribulus terrestris L on tyrosinase activity and melanogenesis. METHODS: MTT was employed to study the proliferation of human melanocytes cultured in vitro, and tyrosinase activity was estimated by measuring the rate of oxidation of DL-dopa, after the cells were treated with different concentrations of decoction of Tribulus terrestris L. RESULTS: The treatment with the decoction increased the amount of melanin at higher concentrations but act to the reverse effect at lower concentrations, with the best concentrations for promoting and inhibiting the cell growth being 1.5 mg/ml (P<0.05) and 0.5 mg/ml (P<0.05) respectively. At high concentrations the decoction enhanced the tyrosinase activity that was inhibited at low concentrations. The best concentrations for enhancing and inhibiting tyrosinase activity were 100 mg/ml (P<0.05) and 10 mg/ml (P<0.05) respectively. CONCLUSION: Tribulus terrestris L decoction exercises a two-way regulation on the activity of tyrosinase and the proliferation of melanocytes.

Cell Division↗

Chemopreventive potential of Tribulus terrestris against 7,12- dimethylbenz (a) anthracene induced skin papillomagenesis in mice.

In the present investigation, the chemopreventive potential of aqueous extracts of the root and fruit of Tribulus terrestris (an Ayurvedic medicinal plant) on 7, 12 - dimethylbenz (a) anthracene (DMBA) induced papillomagenesis in male Swiss albino mice was studied. A significant reduction in tumor incidence, tumor burden and cumulative number of papillomas was observed, along with a significant increase in average latent period in mice treated orally with Tribulus terrestris suspension continuously at pre, peri and post-initiation stages of papillomagenesis as compared to the control group treated with DMBA and croton oil alone. Treatment with Tribulus terrestris suspension by oral gavage for 7 days resulted in a significant increase in the reduced glutathione content in the liver (P< 0.001 for both root and fruit extracts). Conversely, lipid peroxidation levels were significantly decreased (P< 0.001).

9,10-Dimethyl-1,2-benzanthracene↗

Locomotor effects in sheep of alkaloids identified in Australian Tribulus terrestris.

Fresh, mature, ungrazed Tribulus terrestris plant material was subjected to a standard alkaloid extraction procedure. The extract was fractionated by thin layer chromatography (TLC) and high performance liquid chromatography (HPLC). Two major alkaloid fractions were demonstrated. These fractions were identified by means of TLC, ultraviolet spectrofluorimetry (UVS) and HPLC, as the beta-carboline indoleamines harmane and norharmane. The extractable alkaloid content was determined to be 44 mg/kg dry matter. Synthetic harmane and norharmane were administered subcutaneously to sheep at a dose rate of 54 mg/kg. Both compounds caused similar nervous effects. The main effect observed was limb paresis, which in some sheep was body side blased. The clinical signs observed in the experimental sheep were consistent with those described for naturally occurring cases of Tribulus terrestris staggers. It was proposed that harmane and norharmane accumulate in tryptamine-associated neurones of the central nervous system, during months of tribulus ingestion, and gradually interact irreversibly with a specific neuronal gene DNA sequence.

Animals↗

Effect of Tribulus terrestris on nicotinamide adenine dinucleotide phosphate-diaphorase activity and androgen receptors in rat brain.

Tribulus terrestris L. (Zygophyllaceae) have been used as an aphrodisiac both in the Indian and Chinese traditional systems of medicine. Administration of Tribulus terrestris extract (TT) increased sexual behaviour 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 rat brain. Twenty-four adult male Sprague-Dawley rats were divided into two groups of twelve each. Group I was treated with distilled water and Group II was treated with TT at the dose of 5mg/kg body weight orally, once daily for 8 weeks. Following treatment transcardiac perfusion was done with Ringer lactate, 4% paraformaldehyde and 30% sucrose. The brain tissue was removed and sections of the paraventricular (PVN) area of hypothalamus were taken for NADPH-d and AR immunostaining. 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. Androgens are known to increase both AR and NADPH-d positive neurons either directly or by its conversion to oestrogen. 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. The findings from the present study add further support to the aphrodisiac claims of TT.

Animals↗

Antihypertensive and vasodilator effects of methanolic and aqueous extracts of Tribulus terrestris in rats.

The effects of methanolic and aqueous extracts of Tribulus terrestris on rat blood pressure (BP) and the perfused mesenteric vascular bed were investigated. The extracts dose-dependently reduced BP in spontaneously hypertensive rats (SHRs) with the aqueous fraction being more potent than the methanolic fraction at all doses tested. In vitro, the methanolic but not aqueous extract produced a dose-dependent increase in perfusion pressure of the mesenteric vascular bed. When perfusion pressure was raised with phenylephrine (10(-5) M), the aqueous extract produced a dose-dependent reduction in perfusion pressure at all doses. A low dose of the methanolic extract produced a vasoconstrictor effect while higher doses produced dose-dependent reduction in perfusion pressure. L-NAME (10(-4) M) significantly reduced but did not abolish vasodilation induced by the extracts. Vasodilator responses to aqueous and methanolic fractions were significantly reduced in preparations where perfusion pressure was raised with KCl (60 mM). A combination of KCl and L-NAME abolished the vasodilator responses induced by the extracts. It was concluded that methanolic and aqueous extracts of Tribulus terrestris possess significant antihypertensive activity in spontaneously hypertensive rats. The antihypertensive effects appeared to result from a direct arterial smooth muscle relaxation possibly involving nitric oxide release and membrane hyperpolarization.

Animals↗

Abnormal turning behaviour, GABAergic inhibition and the degeneration of astrocytes in ovine Tribulus terrestris motor neuron disease.

OBJECTIVE: To observe the clinical signs of sheep affected by Tribulus terrestris motor neuron disease, to ascertain their response to striatal dopamine reducing drugs, and to examine their brains and spinal cords for microscopic changes. PROCEDURES: Twenty-eight sheep displaying well developed clinical signs of the disorder were observed. Twenty-two of these and 22 normal sheep were then randomly allocated to three groups and treated with diazepam, chlorpromazine, or xylazine. The time that it took an animal to return to a standing position following drug administration was recorded. The brain and complete spinal cord were removed from each of the other six affected sheep and fixed in formalin. Brains were sectioned throughout at 5 mm intervals and spinal cords at 10 mm intervals. All tissues were paraffin embedded and examined by light microscopy. A few samples were examined by electron microscopy. RESULTS: Clinical signs included postural asymmetry with a right:left body-side dominance within the group of 50:50, unequal flaccid paresis in the pelvic limbs, extensor muscle atrophy and adduction of the weaker pelvic limb, and concurrent abduction of the stronger. Forward motion followed either a fixed left or right hand curved trajectory, the sheep no longer being able to choose which. Twelve animals intermittently displayed rotational behaviour that involved loss of postural balance without locomotor activation. The administration of diazepam, chlorpromazine, or xylazine caused limb paresis and sedation, with affected sheep being slower than normal sheep by factors of 8, 3 and 2 respectively, to return to a standing position. There were scattered areas of mild Wallerian degeneration throughout the spinal cord, and in both the brain and the cord there were small numbers of degenerate astrocytes containing novel cytoplasmic pigment granules. CONCLUSIONS: Affected sheep had a dysfunction in the control of directional change and this provides a new insight into the normal mechanism for 'turning' in quadrupeds. Directional change requires a functional asymmetry or lateralisation within the upper motor neuron to accommodate a difference in the rate of forward progression of each body side and, simultaneously, a lateral shift of the centre of gravity. The sensitivity of affected sheep to diazepam is consistent with a pre-existing elevation in GABAergic neuronal inhibition, probably as a result of a reduction in glutamatergic neuronal excitation. The cytoplasmic pigment found in degenerate astrocytes was novel and its presence in the brain nuclei known to contribute to turning behaviour could have aetiological significance. The motor output of the basal ganglia in Tribulus neurotoxicity appeared to be excessively inhibitory to the pelvic limb extensor muscles and was asymmetric, causing fixation of the turning posture but not locomotor activation. An intoxication of specific purine sensitive, glutamate releasing astrocytes, located in nuclei controlling turning, was suspected.

Animals↗

In vitro and in vivo antifungal activities of the eight steroid saponins from Tribulus terrestris L. with potent activity against fluconazole-resistant fungal pathogens.

Antifungal activity of natural products is being studied widely. Saponins are known to be antifungal and antibacterial. We have isolated eight steroid saponins from Tribulus terrestris L., namely TTS-8, TTS-9, TTS-10, TTS-11, TTS-12, TTS-13, TTS-14 and TTS-15. TTS-12 and TTS-15 were identified as tigogenin-3-O-beta-D-xylopyranosyl(1-->2)-[beta-D-xylopyranosyl(1-->3)]-beta-D-glucopyranosyl(1-->4)-[alpha-L-rhamnopyranosyl(1-->2)]-beta-D-galactopyranoside and tigogenin-3-O-beta-D-glucopyranosyl(1-->2)-[beta-D-xylopyranosyl(1-->3)]-beta-D-glucopyranosyl(1-->4)-beta-D-galactopyranoside, respectively. The in vitro antifungal activities of the eight saponins against six fluconazole-resistant yeasts, Candida albicans, Candida glabrata, Candida parapsilosis, Candida tropicalis, Candida krusei, and Cryptococcus neoformans were studied using microbroth dilution assay. The results showed that TTS-12 and TTS-15 were very effective against several pathogenic candidal species and C. neoformans in vitro. It is noteworthy that TTS-12 and TTS-15 were very active against fluconazole-resistant C. albicans (MIC(80)=4.4, 9.4 microg/ml), C. neoformans (MIC(80)=10.7, 18.7 microg/ml) and inherently resistant C. krusei (MIC(80)=8.8, 18.4 microg/ml). So in vivo activity of TTS-12 in a vaginal infection model with fluconazole-resistant C. albicans was studied in particular. Our studies revealed TTS-12 also showed in vivo activities against fluconazole-resistant yeasts. In conclusion, steroid saponins TTS-12 and TTS-15 from Tribulus terrestris L. have significant in vitro antifungal activity against fluconazole-resistant fungi, especially TTS-12 also showed in vivo activity against fluconazole-resistant C. albicans.

Animals↗

[Studies on the chemical constituents from Tribulus terrestris].

AIM: To investigate the chemical constituents of the fruit of Tribulus terrestris J.. METHODS: Various chromatographic techniques were used to separate the chemical constituents. ESIMS, IR, 1HNMR, 13CNMR and HMBC were used to determine the structures of the isolated constituents. RESULTS: Two new compounds were isolated from the fruits of Tribulus terrestris J. and were identified as neohecogenin-3-O-beta-D-glucopyranosyl (1-->2)-beta-D-glucopyranosyl (1-->4)-beta-D-galactopyranoside (I); neohecogenin-3-O-beta-D-glucopyranosyl (1-->4)-beta-D-galactopyranoside (II). CONCLUSION: Compounds I and II are new steroidal saponins.

Fruit↗

[Hypoglycemic effect of saponin from Tribulus terrestris].

OBJECTIVE: To study the hypoglycemic effect of saponin from Tribulus terrestris L. METHOD: Alloxan was used to establish the diabetic model in mice. Phenformin Hydrochlride Tables was used as the positive control. The level of glucose, triglyceride, cholesterol and SOD in serum were determined. RESULTS: The level of serum glucose could be significantly reduced by saponin from Tribulus terrestris, which was the rate of 26.25% and 40.67% in normal mice and diabetic mice in respectively. The level of serum triglyceride could be reduced 23.35%. The saporin could also decrease the content of serum cholesterol. Serum SOD activity of the mice was increased by the saponin. CONCLUSION: Saponin from Tribulue terrestris could significantly reduce the level of serum glucose.

Animals↗

Some effects of feeding Tribulus terrestris, Ipomoea lonchophylla and the seed of Abelmoschus ficulneus on fetal development and the outcome of pregnancy in sheep.

Pregnant ewes and their fetuses were chronically catheterized using aseptic procedures under general anaesthesia, and the ewes were then fed either lucerne chaff alone, or lucerne mixed with dried plant material obtained from one of three forb species, Tribulus terrestris (caltrop), Abelmoschus ficulneus (native rosella) or Ipomoea lonchophylla (cowvine), from 103-112 days gestation until term. Ingestion of the forb material was not associated with changes in maternal blood gases, plasma glucose concentrations, or the length of gestation. However, ingestion of rosella seed was associated with a significantly greater fall of fetal arterial pO2 with advancing gestation, and ingestion of either rosella or cowvine was associated with significantly lower fetal mean arterial pressure at 127-131 days, compared with the Tribulus and lucerne groups. Also, the incidence of fetal breathing movements was significantly lower, and did not show a normal day-night variation, in each of the forb-fed groups compared with the lucerne-fed group. The results indicate that these forb plants may contain substances that affect the functional development of the fetal brain. Although ingestion of these plants did not appear to affect the outcome of pregnancy in this study, the possibility that these forbs have a greater impact in sheep populations with poor nutrition and in more extreme environmental conditions is discussed.

Animal Feed↗

[406 cases of angina pectoris in coronary heart disease treated with saponin of Tribulus terrestris].

Coronary heart disease (CHD) was treated with saponin of Tribulus terrestris. According to 406 cases of clinical observation and a cross test (67 cases treated with Yufen Ningxin Pian as control), the results showed that the total efficacious rate of remission angina pectoris was 82.3%. It was higher than the control group with a total effective rate of 67.2% (P less than 0.05). The total effective rate of ECG improvement (52.7%) was even higher than that of the control group (35.8%). It is shown that saponin of Tribulus terrestris has the action of dilating coronary artery and improving coronary circulation, and thus has better effects on improving ECG of myocardial ischemia. If taken for a long time, it has no adverse reaction on blood system and hepatic and renal functions. Neither does it have side effects. It is one of the ideal medicines to treat angina pectoris.

Adult↗

Scanning electron microscopic observations on micro-organisms in the root nodules of Tribulus terrestris L. (Zygophyllaceae).

Scanning electron microscopic observations were made on the micro-organisms of root nodules of Tribulus terrestris L. The results showed that nodules of T. terrestris contained dual infection consisting of Rhizobium sp. and Newmania karachiensis. Based on these observations, T. terrestris should be grouped with nonlegume Parasponia-type bacterial nodules.

Bacteria↗

Inhibition of the growth of urinary calcium hydrogen phosphate dihydrate crystals with aqueous extracts of Tribulus terrestris and Bergenia ligulata.

Urinary type calcium hydrogen phosphate dihydrate (CHPD) or Brushite crystals were grown by the single diffusion gel technique in silica hydro-gels. The gel framework acts as a three dimensional crucible in which the crystal nuclei are delicately held in the position of their formation and nutrients are supplied for their growth. This technique can be utilized as a simplified screening model to study the growth and dissolution of urinary stones in vitro. The action of the putatively litholytic medicinal plants Tribulus terrestris and Bergenia ligulata on the growth of CHPD crystals was studied . The effects of artificial reference urine (ARU) and human urine (HU), along with the plant extracts, are also reported. Attempts were made to understand the role of these inhibitors on urinary crystal formation. HU, ARU, extracts of B. ligulata and T. terrestris exhibit appreciable amounts of inhibition, but B.ligulata and T.terrestris with ARU and HU do not show inhibition at all.

Calcium Phosphates↗

A novel furostanol saponin from Tribulus terrestris of Bulgarian origin.

The phytochemical investigation of the aerial parts of Tribulus terrestris of Bulgarian origin has resulted in the isolation of the novel furostanol saponin 1, named tribol, together with the known spirostanol saponins 2 and 3 and sitosterol glucoside. The structure of tribol was determined as (25R)-furost-5(6)-ene-3beta,16,26-triol-3-O-alpha-rhamnopyranosyl-(1-->2)-[alpha-rhamnopyranosyl-(1-->4)]-beta-glucopyranoside (1) by spectral analysis, including extensive 1D and 2D-NMR experiments.

Bulgaria↗