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Medicinal properties, phytochemistry and pharmacology of Tribulus terrestris L. (Zygophyllaceae)

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Abstract

Tribulus terrestris (puncture vine) belongs to family Zygophyllaceae and it is a herbaceous, mat forming plant in nature. It extensively grows in warm dry tropics all over the world and ecologically adaptated as a typical C4 xeromorphic plant. T. terrestris is a noxious weed along with its use in many countries as a folk medicine for different purposes from time immemorial. Ancient records describe various medicinal properties of T. terrestris as a popular source to cure variety of different disease conditions in China, India, and Greece. The plant is used directly as a herb or as a main component for production of a number of medicines and food supplements such as for physical rejuvenation, therapy for the conditions affecting liver, kidney, cardiovascular system and immune systems. Also it is used as a folk medicine for increased muscle strength, sexual potency and in treatments of urinary infections, heart diseases and cough. It is considered invigorating stimulant, aphrodisiac, and nutritive. This review discusses the most commonly recognized medicinal properties of this herb. The chemistry of T. terrestris extracts to establish the relationship between medicinal properties of this important plant will also be reviewed.

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... T. terrestr is commonly known as caltrop, is an annual species with opposite and pinnate leaves and yellow petals that grow up to 10-60cm in height (Ganzera Bedir et al., 2001;Chhatre Nesari et al., 2014). This plant is widely distributed in tropical, mild temperate areas and desert climates such as Asia, the Mediterranean region and Mexico (Dinchev Janda et al., 2008;Hussain et al., 2009;Martino-Andrade et al., 2010;Hashim et al., 2014). ...
... For example, saponins, flavonoids, alkaloids, cinammic acid amides and lignin amides were found in T. terrestris. Furostanol, spirostanol saponins and four sulphated saponins of tigogenin and diosgenin were also isolated from this plant (Ukani et al., 1997;Kostova and Dinchev, 2005;Hashim et al., 2014). The fruit and root of T. terrestris are rich in flavonoids, alkaloids, phytosteroids and glycosides (Ukani et al., 1997;Hashim et al., 2014) and its leaves contain diosgenin, gitogenin and chlorogenin (Hashim et al., 2014). ...
... Furostanol, spirostanol saponins and four sulphated saponins of tigogenin and diosgenin were also isolated from this plant (Ukani et al., 1997;Kostova and Dinchev, 2005;Hashim et al., 2014). The fruit and root of T. terrestris are rich in flavonoids, alkaloids, phytosteroids and glycosides (Ukani et al., 1997;Hashim et al., 2014) and its leaves contain diosgenin, gitogenin and chlorogenin (Hashim et al., 2014). ...
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Objective: Hypertension is an important cause of cardiovascular disorders. The angiotensin converting enzyme (ACE) plays an important role in hypertension; therefore, inhibition of ACE in treatment of chronically elevated blood pressure is an important therapeutic approach. In the current review, we have provided information from Persian Traditional Plants described by Avicenna in the Canon of Medicine and a number of more current scientific databases, with a focus on angiotensin converting enzyme inhibitory activity of the following six plants: Allium sativum, Cinnamomum zeylanicum, Jasminum grandiflorum, Tribulus terrestris, Vaccinium myrtillus and Vitis vinifera. Materials and methods: A literature search was conducted and information on different traditional plants used for hypertension was collected from the Canon of Medicine and several other databases including PubMed, Scopus, Google Scholar and Web of Science. Results: The present article highlights the antihypertensive potential of the above-noted six plants. Administered doses, manner of consumption, types of extracts, preparations and derivatives, personal habits, and other geographic and epidemiologic variables have an important role in the potential efficacy of these plants. Conclusion: Recent studies indicated a significant correlation between the traditional use of Persian plants to reduce blood pressure and angiotensin converting enzyme inhibitory activity.
... Being medicinally important the phytochemistry of T. terrestris has been extensively studied and the occurrence of saponins, flavonoids, glycosides, alkaloids, lignanamides and cinammic acid, amides and tannins has been reported ; the fruit and root contain pharmacologically important metabolites such as phytosteroids, flavonoids, alkaloids and glycosides (Jameel et al. 2012, Chhatre et al. 2014, Hashim et al. 2014). ...
... Various parts of T. terrestris are sweet, cooling, diuretic, aphrodisiac, palliative, emollient, appetizer, digestive, anthelmintic, expectorant, antihypertensive, anodyne, anti-inflammatory, alterant, laxative, cardiotonic, styptic, lithontriptic, tonic, astringent, abortifacient and depurative (Warrier et al. 2010, Jameel et al. 2012, Hashim et al. 2014, Shaheen et al. 2014. T. terrestris is one of the 46 medicinal plant species in high trade sourced mainly from wastelands for Ayurvedic Industries in India (Ved and Goraya 2007). ...
... It has been widely used in the Ayurvedic as well as traditional system of medicine in India and other parts of world for the treatment of various ailments, especially sexual dysfunction, infertility, as a testosterone booster and for the cure of various urinary disorders for centuries. In India, T. terrestris is also used extensively in folk medicine for the treatment of cancer, male infertility, painful urination, calculous affections and Bright's disease, digestive disorders, immune disorders, stress, eczema, psoriasis, angina, high blood pressure, high cholesterol, kidney stones and also improves blood circulation and as an aphrodisiac in traditional medicines (Warrier et al. 2010, Jameel et al. 2012, Kor et al. 2013, Yadav 2013, Hashim et al. 2014. The different parts of the plant has strong antibacterial and antifungal activities (Al-Bayati and Al-Mola 2008). ...
... The survey of the literature data revealed some differences in the saponins content and the saponins composition of TT growing in different geographic regions of the world [19,20]. Kostova and Dinchev (2005) reported that the high content of furostanol saponins of the diosgenin type is a characteristic feature of TT from Bulgaria [8]. ...
... Despite its traditional use as an aphrodisiac, which has been well documented for thousands of years, there is minimal evidence for the use of TT in ED, based on contemporary studies. Few studies have been conducted in recent years [9,20] and controlled clinical trials regarding the effect of TT on sexual function are lacking. ...
... and pharmaceutical interest due to its steroidal saponin content [5,6]. Tribulus terrestris L., in addition to its hypolipidemic and hypoglycemic effects, is also used for the treatment of vitiligo, urological infections, prostatic hypertrophy, eye, abdomen and cardiovascular system diseases [6][7][8]. ...
... and pharmaceutical interest due to its steroidal saponin content [5,6]. Tribulus terrestris L., in addition to its hypolipidemic and hypoglycemic effects, is also used for the treatment of vitiligo, urological infections, prostatic hypertrophy, eye, abdomen and cardiovascular system diseases [6][7][8]. There are limited in vitro studies on the effect of T. terrestris L. extracts [7], which have low cytotoxicity on normal cells, on different cancer cells [7,[10][11][12]. ...
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People, especially those living in rural environments and those who have recently been dissatisfied with traditional medicine, use medicinal plants for their therapeutic effects. In this study, ethanol, ethyl acetate and methanol extracts of Tribulus terrestris L. plant, which is used by local people as one of these medicinal plants in Kars province (Turkey), were obtained by ultrasound assisted extraction method. The cytotoxic effects of the obtained extracts on MCF-7 breast cancer cells in the concentration range of 10-1000 ppm at 24 h of exposure were investigated by the MTT method, which is a colorimetric method. T. terrestris L. ethanol extracts at 1000 ppm caused a moderate cytotoxic effect on MCF-7 breast cancer cells. It was determined that ethanolic extracts in the concentration range of 10-500 ppm and methanol and ethyl acetate extracts in the concentration of 10-1000 ppm caused cell proliferation.
... Whereas the macroscopical and the microscopical characters of the flower parts were studied [5]. Hashim et al. (2014) [6] studied the medicinal properties, phytochemistry and pharmacology of T. terrestris. The morphology and anatomy of the xerophytes (dicot) of district Karak were reported within which was T. terristris [7]. ...
... Whereas the macroscopical and the microscopical characters of the flower parts were studied [5]. Hashim et al. (2014) [6] studied the medicinal properties, phytochemistry and pharmacology of T. terrestris. The morphology and anatomy of the xerophytes (dicot) of district Karak were reported within which was T. terristris [7]. ...
... The survey of the literature data revealed some differences in the saponins content and the saponins composition of TT growing in different geographic regions of the world [19,20]. Kostova and Dinchev (2005) reported that the high content of furostanol saponins of the diosgenin type is a characteristic feature of TT from Bulgaria [8]. ...
... Despite its traditional use as an aphrodisiac, which has been well documented for thousands of years, there is minimal evidence for the use of TT in ED, based on contemporary studies. Few studies have been conducted in recent years [9,20] and controlled clinical trials regarding the effect of TT on sexual function are lacking. ...
Article
Objective: The primary objectives were to compare the efficacy of extracts of the plant Tribulus terrestris (TT; marketed as Tribestan), in comparison with placebo, for the treatment of men with erectile dysfunction (ED) and with or without hypoactive sexual desire disorder (HSDD), as well as to monitor the safety profile of the drug. The secondary objective was to evaluate the level of lipids in blood during treatment. Participants and design: Phase IV, prospective, randomized, double-blind, placebo-controlled clinical trial in parallel groups. This study included 180 males aged between 18 and 65 years with mild or moderate ED and with or without HSDD: 90 were randomized to TT and 90 to placebo. Patients with ED and hypertension, diabetes mellitus, and metabolic syndrome were included in the study. In the trial, an herbal medicine intervention of Bulgarian origin was used (Tribestan(®), Sopharma AD). Each Tribestan film-coated tablet contains the active substance Tribulus terrestris, herba extractum siccum (35-45:1) 250mg which is standardized to furostanol saponins (not less than 112.5mg). Each patient received orally 3×2 film-coated tablets daily after meals, during the 12-week treatment period. At the end of each month, participants' sexual function, including ED, was assessed by International Index of Erectile Function (IIEF) Questionnaire and Global Efficacy Question (GEQ). Several biochemical parameters were also determined. The primary outcome measure was the change in IIEF score after 12 weeks of treatment. Complete randomization (random sorting using maximum allowable% deviation) with an equal number of patients in each sequence was used. This randomization algorithm has the restriction that unequal treatment allocation is not allowed; that is, all groups must have the same target sample size. Patients, investigational staff, and data collectors were blinded to treatment. All outcome assessors were also blinded to group allocation. Results: 86 patients in each group completed the study. The IIEF score improved significantly in the TT group compared with the placebo group (Р<0.0001). For intention-to-treat (ITT) there was a statistically significant difference in change from baseline of IIEF scores. The difference between TT and placebo was 2.70 (95% CI 1.40, 4.01) for the ITT population. A statistically significant difference between TT and placebo was found for Intercourse Satisfaction (p=0.0005), Orgasmic Function (p=0.0325), Sexual Desire (p=0.0038), Overall Satisfaction (p=0.0028) as well as in GEQ responses (p<0.0001), in favour of TT. There were no differences in the incidence of adverse events (AEs) between the two groups and the therapy was well tolerated. There were no drug-related serious AEs. Following the 12-week treatment period, significant improvement in sexual function was observed with TT compared with placebo in men with mild to moderate ED. TT was generally well tolerated for the treatment of ED.
... Ginger is a powerful antifungal agent that is used in shampoo to treat dandruff [24]. The antihypertensive effects of fruits of T. terrestris are similar to those of MXD, and its beneficial effects are attributed in part to its ability to release nitric oxide from the endothelium and nitrergic nerve endings [25]; however, there are no reports of its effects on human hair growth. The present study was undertaken to investigate the pharmacological effects of DA-5512 on the proliferation of human dermal papilla cells (hDPCs) in vitro and its effects on C57BL/6 mice and to evaluate its efficacy and safety when administered to human subjects. ...
... The antihypertensive effects of the T. terrestris fruit are similar to those of MXD, and its beneficial effects are attributed to vasodilator activity [25]. The mechanism of the effect of T. terrestris fruit on human hair growth is unknown, but it may act as a growth factor for hair roots. ...
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The proprietary DA-5512 formulation comprises six herbal extracts from traditional oriental plants historically associated with therapeutic and other applications related to hair. Here, we investigated the effects of DA-5512 on the proliferation of human dermal papilla cells (hDPCs) in vitro and on hair growth in C57BL/6 mice and conducted a clinical study to evaluate the efficacy and safety of DA-5512. DA-5512 significantly enhanced the viability of hDPCs in a dose-dependent manner ( p<0.05 ), and 100 ppm of DA-5512 and 1 μ M minoxidil (MXD) significantly increased the number of Ki-67-positive cells, compared with the control group ( p<0.05 ). MXD (3%) and DA-5512 (1%, 5%) significantly stimulated hair growth and increased the number and length of hair follicles (HFs) versus the controls (each p<0.05 ). The groups treated with DA-5512 exhibited hair growth comparable to that induced by MXD. In clinical study, we detected a statistically significant increase in the efficacy of DA-5512 after 16 weeks compared with the groups treated with placebo or 3% MXD ( p<0.05 ). In conclusion, DA-5512 might promote hair growth and enhance hair health and can therefore be considered an effective option for treating hair loss.
... The common name for T. terrestris is devil's eyelashes, puncture vine or cat's head. 2 T. terrestris is used in folk medicine as tonic, aphrodisiac, analgesic, astringent, stomachic, anti-hypertensive, diuretic, lithontriptic and urinary anti-infective. 3 The antimicrobial effects of T. terrestris from other countries have been reported. ...
... showed activity against all test bacteria oral pathogens 4 while the Yemeni species showed no detectable antimicrobial activity against any of the reference bacteria. 2 The T. terrestris extract is also used for urinary dysfunction, asthma and opthalmia and different, 5,6 and has been shown to have antihypertensive and vasodilatory properties. 7,8 It may also protect against oxidative stress and exhibits antitumor, cytotoxic, antifungal and antihelmentic properties. ...
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Objective: This research work focus on synergistic effect of ethnomedicinal plants namely, Tribulus terrestris and Pandiaka heudelotii methanolic and aqueous leaves extracts on two species of clinical bacterial isolates namely, Staphylococcus aureus and Escherichia coli, using disc diffusion method. Methods: The leaves were collected, air dried, pulverized and extracted by maceration. The extracts were subjected to preliminary phytochemical screening using standard procedures. The susceptibility test of individual plant as well as the synergistic effect of combinations of the plants extract was carried out using disc diffusion method. Results: Collectively the plant extracts revealed the presence of alkaloids, flavonoids, steroids, saponins, glycosides, amino acids, reducing sugars and tannins. The in-vitro antimicrobial activity of the crude extracts was examined against both the plants leaves extract showed antibacterial activity against the tested microorganisms. However, some of the eluents collected from methanolic extract fractions of column chromatography were also showed activity on tested organisms. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the leaves extract were determined within the ranges of (125 to 250 mg/ml) and (250 to 500 mg/ml) respectively, the highest synergistic activity was attained against E. coli by combined both methanolic P. heudelotii and T. terrestris extract which showed a zone of (27.54±00). Conclusions: The result indicates antibacterial activity of the leaves extract of P. heudelotii in combination with that of T. terrestris against the clinical bacterial isolates tested and laid credence to the advantage of the combination of the two plants over the two other individual forms. Statistically using, Microsoft excel version 2010.
... Therefore, a photosensitization case should be properly diagnosed whether or not the case is by measuring the levels of bilirubin, liver enzymes and bile acids (Ocal, 2013). On the other hand, Tribulus terrestris is a medicinal and pharmaceutical interest as it contains a number of steroidal saponins which may account for its use in muscle growth, health status and treatment of certain ailments (Hashim et al., 2014;Daniel, 2016). The extract is also used to treat the urinary dysfunction, asthma, antihypertensive, and vaso-dilatory properties (Hashim et al., 2014;Abubakar et al., 2016). ...
... On the other hand, Tribulus terrestris is a medicinal and pharmaceutical interest as it contains a number of steroidal saponins which may account for its use in muscle growth, health status and treatment of certain ailments (Hashim et al., 2014;Daniel, 2016). The extract is also used to treat the urinary dysfunction, asthma, antihypertensive, and vaso-dilatory properties (Hashim et al., 2014;Abubakar et al., 2016). Moreover, Tribulus terrestris is extremely rich with substances which have potential biological significances in addition to saponins, which includes: flavonoids, unsaturated fatty, alkaloids, acids, vitamins, and tannins (Heidari et al., 2007;Grigorova et al., 2017;Khazaei et al., 2018). ...
... Therefore, a photosensitization case should be properly diagnosed whether or not the case is by measuring the levels of bilirubin, liver enzymes and bile acids (Ocal, 2013). On the other hand, Tribulus terrestris is a medicinal and pharmaceutical interest as it contains a number of steroidal saponins which may account for its use in muscle growth, health status and treatment of certain ailments (Hashim et al., 2014;Daniel, 2016). The extract is also used to treat the urinary dysfunction, asthma, antihypertensive, and vaso-dilatory properties (Hashim et al., 2014;Abubakar et al., 2016). ...
... On the other hand, Tribulus terrestris is a medicinal and pharmaceutical interest as it contains a number of steroidal saponins which may account for its use in muscle growth, health status and treatment of certain ailments (Hashim et al., 2014;Daniel, 2016). The extract is also used to treat the urinary dysfunction, asthma, antihypertensive, and vaso-dilatory properties (Hashim et al., 2014;Abubakar et al., 2016). Moreover, Tribulus terrestris is extremely rich with substances which have potential biological significances in addition to saponins, which includes: flavonoids, unsaturated fatty, alkaloids, acids, vitamins, and tannins (Heidari et al., 2007;Grigorova et al., 2017;Khazaei et al., 2018). ...
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This study was conducted to investigate one of the most issues in Iraqi Awassi sheep by ingesting of Tribulus terrestris that disseminated in the Al-Najaf Desert. The Iraqi Awassi sheep is one of the most popular and economically important sheep in Iraq and the Middle East which survive on the low nutrition level. Nutrition also remains one of the major constraints to livestock production in the tropics, particularly the lack of protein during the dry season. Tribulus terrestris (Qutub) belongs to family Zygophyllaceae, it is a herbaceous, mat forming plant in nature and grows in warm dry tropics all over the world. A total of 75 blood samples were collected from jugular vein and placed into EDTA and plain tubes. Samples were divided in to two groups depending on the clinical signs, 45 sheep were clinically healthy and 30 sheep possessed clinical signs that are suggestive of photosensitization in Al-Najaf governorate, Iraq. The results showed that the total blood analyses, there were a significant increase (P > 0.05) in total leukocyte count and neutrophils, while, there was no significant difference in total red blood cells, PCV, Hb, lymphocytes, and eosinophil of affected sheep compared to the control. Furthermore, affected sheep had significantly higher levels of aspartate aminotransferase (AST), alkaline phosphatase (ALP), sorbitol dehydrogenase (SDH), total protein, total bilirubin, and serum urea nitrogen. In conclusion, the present study recorded that hematological, biochemical and pathological changes related with ingestion of toxic plant Tribulus terrestris in Al Najaf desert of Iraq, which causes photosensitization in affected sheep.
... Other steroidal saponins of furostanol and spirostanol type have been identified: prototribestin, protogracillin, etc. [6,7]. Alkaloids and flavonoids have also been identified in the extracts obtained from fruits; therefore, the extracts are considered to also have antioxidant effects (attributed mainly to di-p-coumaroylquinic acid derivatives) [8,9]. ...
... Chim.1949 Rev. Chim., 71 (4) Reported results on the antibacterial effects of Tribulus terrestris extracts are very different and it seems that this effect is correlated with the originating geographical area of the plant and consequently with the phytochemical profile [8]. An herbal preparation used for its anabolic properties but with extra antibacterial effects could be a solution for the persons who frequently use doping agents because anabolic steroids have a substantial impact on the immune function. ...
Article
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Recommendations of products with Tribulus terrestris as anabolic enhancers are based on empirical data. Exposure, especially of athletes, is very high, being among the most widely used nutritional supplements. Consumption of products containing Tribulus terrestris extracts has increased rapidly in the past few years due to the high content of sterol saponosides, compounds with presumed anabolic properties. Because of this upward surge, their efficacy and/or their safety are more and more often questioned. Commercialized dietary supplements, are often mislabelled, adulterated, or contaminated, therefore an evaluation of benefit/risk balance should always be conducted. Our study aimed to analyse an herbal drug and a food supplement frequently encountered on the market. Total polyphenolic and total saponosides content were determined. Inductively coupled plasma atomic emission spectrometry (ICP-AES) was used to determine mineral element content of Tribulus terrestris products. Antioxidant and antimicrobial activities were assayed. The extract obtained with the herbal drug had no antibacterial effect. The extract from the capsules, however, was active against all tested strains with higher activity against Methicillin-resistant Staphylococcus aureus and Escherichia coli (MIC = 0.78 mg/mL). Trace elements were quantified, and dose-related risks were outlined, raising awareness regarding the aluminum and nickel content in the herbal drug.
... The early Egyptians, Babylonians, Samarians, Greeks, Romans, Indians and Chinese all used Tribulus terrestris in their system of medicines. It posses special nutritional and healing powers that often go beyond chemotherapy (Hashim et al., 2014). It contains a number of steroidal saponins and is used for the treatment of many diseases like infertility, cardiac, muscle building, conditioning and treatment of some other microbial diseases (Al-Bayati and Al-Mola, 2008). ...
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The experiments were conducted to see the impact of drying methods and extraction solvents on the yield of steroidal saponins of Tribulus terrestris. The plant was dried by three different drying methods namely,solar collector drying, open sun drying and shade drying. After drying different levels (25-100%) of extracting solvent in the form of ethanol, methanol and distilled water were used for extraction. Soxhlet apparatus was used for extraction, while the gas chromatography apparatus was used in the experiment for detecting steroidal saponins in Tribulus terrestris. After extraction, four saponins identified were Tigogenin, Gitogenin, Hecogenin and Neohecogenin. The maximum yield of 61.2% was recorded for flat plate solar drying with 75% ethanol solution, followed 49.5% in shade drying with the same extraction solvent level. The lowest value of 3.1% yield was recorded for distilled water with open sun drying method. It was concluded that Both the drying methods and extraction solvent have a direct effect on the yield of steroidal saponins extracted from Tribulus terrestris. A maximum yield of almost 60% saponins may be achieved, if Tribulus terrestris is dried using a flat plate solar collector and extorted with 75% ethanol solution using GC-MS technique. Open sun drying minimizes saponins in Tribulus terrestris, while distilled water is the worse extracting solvent for extraction of steroidal saponins from Tribulus terrestris.
... Usually phytoconstituents found in T. terrestris are alkaloids, resins, tannins, sugars, sterols, fl avonoids like rutin, quercetin, cinammic acid, amides, lignanamides (tribulusamides A and B), kaempferol, protodioscin and prototribestin (Evstatieva et al. 2011). Hashim et al. (2014) reported phytosteroids and glycosides. However major phytochemicals produced by this plant are steroidal saponins such as prototribestin, dioscin, protodioscin (Gauthaman et al. 2003), furostanol (De Combarieu et al. 2003), (1 2)]-β-D-galactopyranoside (Tandan and Sharma 2010) gitogenin, beta-Sitosterol, spirosta 3,5-diene, stigmasterol, hecogenin, neohecogenin, ruscogenin (Akram et al. 2011), tribulosaponin B, metilprotodiostsin, terrestrozin H, prototribestin, gracillin (Kozlova et al. 2011. ...
... Seeds are enclosed in a woody star-shaped structure (carpels). Each plant can have up to 2000 seeds (Hashim et al., 2014). This plant has long been used for medicinal purposes and, therefore, the seeds would be a valuable by-product in industries extracting its active components. ...
Article
In the Mediterranean Basin, petroleum energy resources are scarce. For an environmentally sustainable solution, the seeds collected from wild plants indigenous to this area could be used as biodiesel producers to meet the energy demand. For this, the fatty acid profiles of seed oils from 127 species belonging to 30 plant families, all native of the Mediterranean Basin, were surveyed in a search for fossil-fuel substitutes. The saponification number (SN, mg KOH/g), iodine value (IV, g I2/100 g), cetane number (Ф), higher heating value (δ, MJ/kg), cold filter-plugging point (CFPP, ºC), density (ρ, g/cm³), induction period (IP, h) and kinematic viscosity (η, mm²/s) were empirically determined and then used to establish the suitability of the different seed oils for biodiesel production. The aptness to serve as biodiesel was determined by applying the specification for biodiesel standard made by several organizations. In addition to three already well-characterized species, the fatty acid methyl esters from the seeds of Conium maculatum (Ф= 53.7; δ= 40.1), Eryngium maritimum (Ф= 53.2; δ= 40.2), Nigella damascena (Ф= 58.1; δ= 40.1), Portulaca oleracea (Ф= 62.9; δ= 40.5), Prangos uechtritzii (Ф= 52.8; δ= 40.1), and Tribulus terrestris (Ф= 59.4; δ= 40.1), meet the major quality standards set by several organizations, and thus are suitable for biodiesel production. Data from empirical models used for estimating biodiesel properties was compared with experimental data from biodiesel prepared with available seeds, and good correlations between the two methodologies were found.
... [40] KK fruit contains steroidal saponins, teresterosin A, teresterosin E, and tribulosin which on hydrolysis give rise to steroidal sapogenin, namely, diosgenin (having pyroketone ring), gitogenin, chlorogenin, ruscogenin, and 25 D-spirosta-3,5-diene, hecogenins. Other Steroidal saponin includes gitonin, protodioscin, tribulosaponins A and B, tribulosin, and terrestrosins A-K, [7,41] considering that this HPTLC study was done and a fingerprinting was set in for future work including estimation of diosgenin which is a nonsugar component of saponin present in the formulation obtained after hydrolysis. Diosgenin, a sapogenin from TT, was taken as a reference standard which is an essential component. ...
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Background and Objectives Mudabbar/Tadbeere advia is referred to the processes performed on the drugs to detoxify, purify, and enhance therapeutic action and to reduce its doses before making the formulations in Unani medicine. It improves quality of drugs either by optimizing its desirable characteristics or minimizing the undesirable ones; it makes drug effective, safe, and specific. There is a need of comparative evaluation to understand its significance. Tadbeer of Kharekhasak (KK) khurd (Tribulus terrestris Linn. fruit) is described by Rabban Al-Tabari in Firdausul Hikmat, Akbar Arzani in Qarabadeene Qadri, etc., during the compounding of aphrodisiac formulations. Mudabbar Kharekhasak (MKK) used in Safoofe Kharekhasak mentioned in Al-Qarabadeene was evaluated in this work. Methods Mudabbar/Tadbeer process was carried out by blending fresh KK. Juice with powdered dry KK and drying it under the sun. Juice used for process is thrice the weight of dry KK powder. The KK before and after the process was evaluated using physicochemical tests: powder characterization, extractive value, alcohol and water soluble matter, ash value, loss on drying (LOD) at 105°C, pH, high-performance thin layer chromatography (HPTLC) fingerprinting, and diosgenin content. Results Powder characterizations were set in. Increase in successive and nonsuccessive extractive values in various solvents, water/alcohol-soluble content, total ash, acid-insoluble ash, water-soluble ash, and sulfated ash of MKK was noted in comparison with KK. Decrease in LOD at 105°C and pH of MKK powder was observed. HPTLC fingerprinting data were developed for the identification and evaluation. Quantification of diosgenin content increased to 432.1 g/g in MKK as compared to 144.5 g/g in KK, suggesting significant increase in saponin content. Conclusion Data obtained clearly indicated changes in MKK validating the classical Mudabbar process, probably to enhance/modify the action of drug. Standards for crude and MKK were established for future reference. SUMMARY Mudabbar process on Tribulus terrestris Linn (KK) have been validated. Physicochemical data for Mudabbar and non mudabbar Kharekhasak (KK) powder have been set in. Diosgenin content was increased significantly in mudabbar KK. Abbreviations Used: KK: Kharekhasak, TT: Tribulus terrestris, MKK: mudabbar Kharekhasak, SK: Safoofe Kharekhasak, LOD: loss of weight on drying, HPTLC: High performance thin layer chromatography, BSS: British standard sieve, μl: microliter, SEM: Standard error of mean, nm: nanometer, g: gram.
... Usually phytoconstituents found in T. terrestris are alkaloids, resins, tannins, sugars, sterols, fl avonoids like rutin, quercetin, cinammic acid, amides, lignanamides (tribulusamides A and B), kaempferol, protodioscin and prototribestin (Evstatieva et al. 2011). Hashim et al. (2014) reported phytosteroids and glycosides. However major phytochemicals produced by this plant are steroidal saponins such as prototribestin, dioscin, protodioscin (Gauthaman et al. 2003), furostanol (De Combarieu et al. 2003), (1 2)]-β-D-galactopyranoside (Tandan and Sharma 2010) gitogenin, beta-Sitosterol, spirosta 3,5-diene, stigmasterol, hecogenin, neohecogenin, ruscogenin (Akram et al. 2011), tribulosaponin B, metilprotodiostsin, terrestrozin H, prototribestin, gracillin (Kozlova et al. 2011. ...
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Tribulus terrestris extract are traditionally curable medicines used by several nations such as India, China, European nations and America. It is extensively used for severe ailments of cardiovascular, urinary tract diseases and induced spermatogenesis. The complete plant has tremendous medicinal and pharmacological activities such as a diuretic, aphrodisiac, antiurolithic, immunomodulatory, antihypertensive, antidiabetic, anticancer, anthelmintic, antibacterial, analgesic and anti infl ammatory.
... In traditional medicine, T. terrestris is well known to treat various diseases in many countries. It can be applied directly or used as the main ingredient in many medicines and food supplements (Hashim et al., 2014). Dighe et al. (2020) stated that the plant is used for healing purposes such as strengthening, nutrition, rejuvenation, diuretic, anti-inflammatory, or aphrodisiac agent, and renal calculi. ...
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ETHNO-PHYTOTECHNOLOGY combines ethnobotany and biotechnology. This study evaluated the ethnobotanical role, anticancer potential, and allelopathy of Tribulus terrestris L. The ethnobotanical survey of twenty informants used an open-ended questionnaire. T. terrestris contains steroids, saponins, antioxidants, flavonoids, alkaloids, phenolics, proteins, and amino acids. The study investigated cytotoxic effects using six carcinoma cell lines. Hordeum vulgare and Lepidium sativum were used as recipient species in the allelopathy experiments. We found that 95% of the informants stated that T. terrestris is an aggressive species that injures livestock, reduces biodiversity, leads to soil dryness, consumes large amounts of space during the vegetative season, and affects soil pH and the absorption of minerals. Ethanolic extracts produced a significant effect on the prostate (PC3), breast (MCF 7), lung (A549), and liver (HEP-G2) carcinoma cell lines, with IC50 values of 19, 22, 33, and 33μg/mL, respectively. The intestinal carcinoma cell line (CAco2) had an IC50 60μg/mL. The colon (HCT) carcinoma cell line had an IC50 value of 68 μg/mL. Water extracts inhibited the seed germination, plumule length, radicle growth, and fresh and dry matter production of the recipient species. This study demonstrated that T. terrestris is potentially valuable as an anticancer agent and an herbicide against harmful weeds.
... (Ajwain); Hussain et al., [31] performed a pharmacological study on Thymus linearis Benth and Thymus serpyllum L.; Wadood et al., [32] conducted a pharmacological study of Acacia nilotica (L.) Delile, Psidium guajava L., Luffa cylindrical (L.) Roxb., Morus alba L., Morus nigra L., Momordica charantia L., Fagonia cretica L., Punica granatum L., Ficus palmate Forssk. and Prunus persica (L.) Batsch; Hashim et al., [33] did experiments on Tribulus terrestris L. to study its chemical and pharmacological importance; Atta et al., [34] studied five selected vegetable plants to know their chemistry and pharmacognosy. ...
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This review article is an effort to summarize the medicinal plant status, history, research, prospects and limitation in Pakistan. Therapeutic plants are the important part of the healthcare system. Over 400.000 higher plants species are identified so far; of which about 10% are utilized by different communities for medicinal purposes. In Pakistan, the majority of the people depend on therapeutic plants for curing minor ailments and in certain circumstances major ailments too. All over the world, there various treatment systems exist like Ayurvedic, Allopathic medicine, Chinese treatment system and Homeopathic medicine. China and Indo-Pakistan are at the center of the international herbal market. According to an estimate, the global trade of herbal drugs values 25-30 billion US$ per annum. Because of over-collection many medicinal plants are near extinction. Native plant gatherers and sellers are the main cause of threat to the Pakistan medicinal flora. Although the medicinal flora is the income source for indigenous people, this resource is not managed properly, which may result in habitat destruction, as well as species extinction. It is high time to find sustainable ways for harvesting medicinal plants from the wild, to educate native collectors in suitable collection methods, to train the local community how to grow therapeutic herbs, and to eliminate the middle-men from the trading chain.
... The fruits and roots of T. terrestris have been used as a folk medicine for thousands of years in China, India, Sudan, and Pakistan (Table 1). Modern researches demonstrated that the chemical constituents such as steroidal saponins and flavonoids from T. terrestris were the main contributors to the traditional pharmacological activities such as antioxidant, antiaging, antiurolithic, immunomodulatory, absorption enhancing, hypolipidemic, hepatoprotective, anti-inflammatory, analgesic, antispasmodic, anticancer, antibacterial, antifungal, anthelmintic, and larvicidal (Anand et al., 1994;Adaikan et al., 2001;Al-Bayati et al., 2008;Chhatre et al., 2014;Hashim et al., 2014;Sivapalan, 2016;Zhu et al., 2017). In addition, in the therapeutic protocols, it has been reported that high doses of the aqueous extracts of the T. terrestris fruits had genotoxic efficacy (Qari and El-Assouli, 2019). ...
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Background: Tribulus terrestris L. (T. terrestris) positive performance on the male sexual system has been confirmed, but little is known about its effects on the female reproductive system. Purpose: This review discussed in detail the beneficial impact of T. terrestris and its secondary metabolites on the female reproductive system. Study design and methods: In this review, the scientific Databases of Science direct, Pubmed, Web of Science, Google, Google Scholar, Researchgate, EMBASE, Scientific Information (SID), and Elsevier were searched profoundly. Studies about the pharmacological activities of T. terrestris on the female reproductive system in each aspect of investigations: human, in vivo, and in vitro studies, in the period from 1998 to 2020 were admitted. Our study was not limited by the language of publications. Results: 23 articles about the effects of T. terrestris on the female reproductive system were found. These studies approved the T. terrestris efficacy on improvements in histological features of the ovary and uterus of polycystic ovary syndrome patients as well as the well-working of normal ovaries, enhancements in the sexual desire of postmenopausal syndrome, improve ovarian and breast cancers. Conclusion: These studies showed that the positive effect of T. terrestris on the female reproductive system was due to the presence of a secondary metabolite called protodioscin; a steroidal saponin compound, as the dominant active component of this plant.
... The plant has been used as a folk medicine in Iraq as tonic, aphrodisiac, analgesic, astringent, stomachic, diuretic, lithotriptic, and as a urinary anti-infective (Pandey, 2014). Wang (1989) and Hashim et al. (2014) gave a detailed review on phytochemistry and pharmacology of Tribulus terrestris. ...
... When the literature data are examined, T. terrestris of Chinese, Indian and Bulgarian origin has been studied extensively. However, the phytochemical studies on T. terrestris located in Turkey, Russia, South Africa, Australia, Azerbaijan and Romania is inadequate (Hashim, 2014). T. terrestris is a plant known effects in Turkey and consumed among the people. ...
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For a long time, many cultures around the world have used Tribulus terrestris L. in the prevention and treatment of various diseases. In this study, the antioxidant activity and total phenolic and flavonoid content of extracts obtained with various solvents from T. terrestris plant collected from different localities in Kahramanmaraş were investigated. In addition, the fixed oil content of the extracts was examined by GC-MS analysis and as a result, 26 different fatty acids were determined. The main fatty acid components of plant extracts are linoleic acid, oleic acid and palmitic acid. The total phenolic substance value of plant extracts varies between 2.20-18-77 mg g-1, total flavonoid amount varies between 0.06-0.50 mg g-1, FRAP value varies between 6.16-23.50 µg g-1 and DPPH value varies between 1.54-10.54 µg mL-1. It was observed that the solvents used in extraction affected the bioactivity values rather than the locations. Although the absorbance values of the extracts obtained with hexane were high, low extract yield affected the results. The highest values in all characters examined were obtained from ethanolic extracts.
... Diosgenin (3b-hydroxy-5-spirostene) is a steroidal saponin with abroad therapeutic applications in cardiovascular protection and evaluated in the past extensively (14). This Chinese T. terrestris is also predominant with steroidal saponin gitogenin (15). Gitogenin has been reported as an alpha-glucosidase-inhibitor (16) and as a regulator of thyrotoxicosis in rats (17). ...
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Background/objectives: Steroidal saponins are widely distributed in medicinal plants with potential applications in cardiovascular disorders. Gitogenin, a saponin, has not been explored as antihypertensive; this investigation was aimed to explore its blood pressure lowering potential and underlying mechanisms. Methodology: The effect of gitogenin was evaluated on blood pressure in vivo, using normotensive rat model and the underlying cardiovascular mechanism(s) in vitro, in isolated rat aorta and in atria preparations using PowerLab data acquisition system (ADInstrument, Australia). Results: Intravenous injection of gitogenin decreased mean arterial pressure (MAP) in anesthetized rats. Atropine (1 mg/kg) and L-NAME (100 mg/kg) pretreatment significantly (*p < .05) attenuated effect on MAP to gitogenin. In isolated intact aortic rings, gitogenin induced endothelium-dependent vasodilatation (maximum 65%), which was ablated (maximum 22%) with L-NAME (100 mg/kg) and atropine (1 μM) pretreatment or endothelium removal. Gitogenin was found more potent against angiotensin II precontractions without effect on high K⁺ and low K⁺ precontractions. In isolated rat right atria, gitogenin suppressed rate and force of contractions. Atropine (1 μM) pretreatment partially inhibited effect of gitogenin on force and eliminated its effect on rate. Combined atropine (10 μM) and atenolol (0.5 μM) pretreatment was without effect on force of contractions but eliminated effect of gitogenin on rate with 25% increase. Conclusion: These findings indicate that antihypertensive effect of gitogenin is the outcome of vascular and cardiac effects; agonistic effect on vascular M3 and cardiac M2 receptors; and being more selective for M2. Increase in the rate of atrial contraction might be of clinical importance.
... T. terrestris grows rapidly along roads and waste places; its seed bank remains in the soil for its successful spread; it punctures bicycle tires and injures feet (Donaldson 2011) with its seeds having three hard and long spines. T. terresteris an aggressive and hardy invasive species, widely known as a noxious weed, because of its small woody fruit -the bur -having long sharp and strong spines which easily penetrate surfaces, such as the bare feet or thin shoes of crop workers and other pedestrians, the rubber of bicycle tires, and the mouths and skin of grazing animals (Hashim 2014). ...
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The present research work is based on the identification of Invasive Alien Plant Species (IAPS) distributed in Potohar Plateau, which are threat to indigenous flora. To confirm the invasive and alien status of these species, we investigated the flora of Potohar plateau. The target population sampling method was used for the collection and listing of IAPS present in all districts of Potohar Region. Invasion status of IAPS was recorded from wastelands, roadsides, crop fields, banks of canals, mismanaged gardens and housing colonies. Our results revealed that Broussonetia papyrifera Vent., Cannabis sativa L., Eucalyptus camaldulensis Dehnh., Lantana camara L., and Parthenium hysterophorus L. are highly invasive species. Whereas seventeen IAPS were found in naturalized, ten recently escaped from controlled cultivation, three were newly introduced while fifteen grown casually in the study area. The common life form of IAPS was herbs and are used for medicinal and ornamental purposes. These species have invaded maximum area to obstruct the distribution of native flora including medicinal and economically important plants, which are now found in patches. We tend to use eradication methods to control further replacement of indigenous vegetation. This study suggests that the Government of Pakistan should take possible steps to prevent natural habitat of local flora and make separate zones for IAPS. The present study will help the researchers and policymakers to control invasion and alien species.
... Our results coincides with [24] were they showed that species Amranthus viridis was used as anti-inflammatory agent, vermifuse, diuretics and for the treatment in kidney stones a anti-urolithiatic agent. [25], also reported phytochemical and antimicrobial activity of Tribulus terrestris in experimental animal R. norvigicus to reduce the percentage of calcification. [26], reported the phyto-remedial impact of Amranthus cruentus leading to significantly reduction of calcium oxalate crystals which has direct impact on regulation of excretory system and urine formation. ...
... Table 1 comprises all the reviews related to TT found in the scientific literature. 2014 Phytochemistry and pharmacology short review [7] 2014 Phytochemistry and pharmacology NS short review [8] 2016 ...
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The general spread of Tribulus terrestris L. (South Africa, Australia, Europe, and India), the high content of active ingredients (in particular sterol saponins, as well as flavonoids, tannins, terpenoids, phenol carboxylic acids, and alkaloids), and its frequent uses in folk medicine, and as food supplements highlight the importance of evaluating its phytopharmacological properties. There are miscellaneous hypotheses that the species could have a high potential for the prevention and improvement of various human conditions such as infertility, low sexual desire, diabetes, and inflammatory diseases. Worldwide, numerous herbal supplements are commercialized with indications mostly to improve libido, sexual performance in both sexes, and athletic performance. Phytochemical studies have shown great disparities in the content of active substances (in particular the concentration of furostanol and spirostanol saponoside, considered to be the predominant active ingredients related to the therapeutic action). Thus, studies of experimental pharmacology (in vitro studies and animal models in vivo) and clinical pharmacology (efficacy and safety clinical trials) have sometimes led to divergent results; moreover, the presumed pharmacodynamic mechanisms have yet to be confirmed by molecular biology studies. Given the differences observed in the composition, the plant organ used to obtain the extract, the need for selective extraction methods which are targeted at the class of phytocompounds, and the standardization of T. terrestris extracts is an absolute necessity. This review aims to highlight the phytochemical, pharmacological, and toxicological properties of T. terrestris, with a focus on the contradictory results obtained by the studies conducted worldwide.
... Herbal medicines are utilized by humans for general health and specific diseases since ancient times and are complex,based on various plants including weeds. 8,9 According to world health organization, majority (80%) of the inhabitants of rural areas depend on herbal medicine in their healthcare in developing countries. 10 An estimate of thousands of plant species are widely used for medicinal purposes worldwide. ...
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Khella (Ammi visnagais) was used in Ancient Egypt as a herbal remedy for renal colic. Khella contains group of coumarins, xanthotoxin, ammidin, furoquinoline alkaloids and, dihydroseselins with varying cytotoxic activity. The most common is Khellin and visnagin. Khellin was found to be a smooth muscle relaxant, induces diuresis, increases excretion of citrate and decreases the excretion of oxalate in urine, which improves nephrolithiasis and passage of ureteric stones. Synthetic derivatives of khellin include amiodarone, the anti-arrhythmic drug, and cromolyn, an anti-asthma drug. Khellin is not as safe as it seems to be. Its oral use is limited by its potential toxicity (eg, elevated liver enzymes, phototoxicity, dermatitis). In experimental animals, the median lethal dose (LD50) was 3.6 g/kg for intra-peritoneal administration and 10.1 g/kg for oral administration. In humans, nausea and vomiting were observed frequently in 29% and transaminitis in 7-14% of the patients. Other potential adverse reactions include dizziness, constipation, headache, itching, insomnia, photosensitivity and lack of appetite. We report for the first-time, acute kidney injury following use of khella in a CKD patient with a 5-fold increase in his serum creatinine level from 1.9 to 9.2 mg/dl. His renal biopsy revealed eosinophilic interstitial nephritis. He responded well to pulse methylprednisolone followed by short course of oral steroids. We believe this is the first case describing Khella nephropathy. Herbal nephropathy is not uncommon and herbal remedies are not as safe as it is believed. Accurate diagnosis and early management are the key in improving the renal outcome.
... Tribulus terrestris (zygophyllaceae) grows mainly in North China. The fruit of Tribulus terrestris helps to improve erectile function, increases androgen ability and does not enhance serum testosterone levels as an aphrodisiac property in many animal experiments [49,50] . Hence, it needs to be investigated further for the pro-erectile property mechanism. ...
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Erectile dysfunction (ED) or male impotence is described as an inability to maintain penile erection primarily endothelial and neuronal dysfunction which is partly characterized by decreased production of nitric oxide (NO). Male impotence can be caused by androgen deficiency in aging men, atherosclerosis, diabetes mellitus, spinal cord injury, high level of cholesterol, hypertension, prostate surgery, prostate and heart disease, penis anatomical deformity, social and psychological conditions as unhappy marital relationship, depression, and stress. Aphrodisiac is a drink or food that arouse sexuality. It can be categorized into three groups according to their action mode as follows: increase sexual pleasure substances, increase libido substances (arousal, sexual desire), and increase sexual potency (erection effectiveness). Various extracts of medicinal plants and orally active drugs such as vardenafil, sildenafil, and tadalafil are used to increase arterial blood flow for treating (ED) in southwest Asia. Hence, this paper review focuses on medicinal plants used as aphrodisiacs for scientific validation and management of erectile dysfunction (ED).
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Introduction Fruit extract of Tribulus terrestris (TT) bears aphrodisiac and antioxidative properties. Antimicrobial drug, metronidazole (MTZ) impairs the spermatogenic activity and fertility in males. Objective Validation of the use of fruit extract of TT as a supplement against MTZ-induced fertility impairment in males. Methods Adult Swiss strain male mice were administered with 500mg/kgBW/day of MTZ for 28 days. Low (100mg/kgBW/day) and high (200mg/kgBW/day) doses of TT were administered simultaneously with MTZ (500mg/kgBW/day) for same duration. All males were cohabited with virgin proestrus females. Vaginal plug formation was observed to calculate the libido index. Cohabited females were sacrificed on fifteenth day of gestation to dissect out the ovaries and uteri. Fertility index, quantal pregnancy, pre-implantation and post-implantation losses were calculated. Results MTZ-treated males showed unaltered mating ability, however, the females impregnated by such males exhibited marked alterations in the fertility index, quantal pregnancy and pre- and post-implantation losses. Supplementation with low dose of TT failed to restore such reproductive toxicities exhibited by administration of MTZ. However, the altered reproductive toxicities were reinstated to control values following supplementation with high dose of TT. Conclusion The fruit extract of TT may emerge as an effective herbal remedy, correcting the drug-induced fertility impairments in males.
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The recent focus is on the analysis of biological activities of extracts from thirteen folk medicinal plants from arid and semi-arid zones of Balochistan, Pakistan. Only a small proportion of them have been scientifically analyzed. Therefore the present investigation explores the biochemical and bioactive potential of different plant parts. Superoxide dismutase was detected maximum in Fagonia indica, (184.7±5.17 units/g), ascorbate peroxidase in Tribulus pentandrus (947.5±12.5 units/g), catalase and peroxidase were higher in Peganum harmala (555.0±5.0 and 2597.8±0.4 units/g, respectively). Maximum esterase and α-amylase activity was found in Zygophyllum fabago (14.3±0.44 and 140±18.8 mg/g, respectively). Flavonoid content was high in T. pentandrus (666.1±49 μg/ml). The highest total phenolic content and tannin was revealed in F. olivieri (72125±425 and 37050±1900 μM/g, respectively). The highest value of ascorbic acid was depicted in F. bruguieri (F.b.N) (448±1.5 μg/g). Total soluble proteins and reducing sugars were detected higher in P. harmala (372.3±54 and 5.9±0.1 mg/g, respectively). The maximum total antioxidant capacity was depicted in Tetraena simplex (16.9±0.01 μM/g). The highest value of lycopene and total carotenoids exhibited in T. terrestris (7.44±0.2 and 35.5±0.0 mg/g, respectively). Chlorophyll contents were found maximum in T. pentandrus var. pterophorus (549.1±9.9, 154.3±10, and 703.4±20.2 ug/g, respectively). All taxa exhibited anti-inflammatory activity and anti-diabetic potential. Z. eurypterum seeds exhibited the highest anti-inflammatory potential (96%), along with other taxa indicated (96–76%) activity when compared with the standard drug diclofenac sodium (79%). Seeds of T. pentandrus (85%) exhibited the highest anti-diabetic activity. The other taxa also exhibited inhibitory activity of α-amylase ranging from (85–69%) compared with Metformin (67%) standard drug. Phytochemical screening revealed that selected taxa proved to be the potential source of natural antioxidants and could further be explored for in-vivo studies and utilized in pharmaceutical industries as potent therapeutic agents validating their ethno-pharmacological uses.
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The purpose of this study was to illustrate the mechanism of “enzyme inactivation and toxicity reduction” of Fructus Tribuli (FT) after being heating processed. Ultra-high performance liquid chromatography coupled with triple quadrupole tandem mass spectrometry (UHPLC-MS/MS) was used to quantitatively analyze the contents of four steroidal saponins in crude Fructus Tribuli (CFT) and stir-fried Fructus Tribuli (SFT) under different storage times at room temperature. The enzyme activity of β-D-glucosidase in CFT and SFT were determined and calculated by ultraviolet–visible spectrometry (UV-VIS spectrometry). In addition, the enzyme hydrolysates of FOT and tribuluside A were qualitatively analyzed by ultra-high-performance liquid chromatography coupled with quadruple-time-of-flight mass spectrometry (UHPLC-Q-TOF/MS). The hepatorenal toxicity of spirostanol saponins in FT were further confirmed by in vivo and in vitro experiment. This study confirmed that “enzyme inactivation and toxicity reduction” was one of the reasons why the stir-frying can reduce hepatorenal toxicity of FT, and further enriched the exploration on the mechanism of processing toxicity reduction.
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The main objective of the present study was to indorse specific herbal formula as supplements in polluted human societies to minimize the harmful effect of the prevailing heavy metals. The concentration of different heavy metals in Abu Qir, Amreyya and Abis districts was determined and the different methods by which these metals were introduced to the body system was recognized. An herbal assemblage (ACOSTU) was prepared based on the types of heavy metals and their concentrations. The results of the application of the herbal assembly for six sustained months showed a significant improvement in the medical examined cases recorded in the study areas. The study concluded that initiation of health care specific programs for the human living in polluted districts is urgently necessary as a part of a sustainable development plan to save endangered rural communities.
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Ammi visnaga (bisnaga, toothpick weed or khella) belongs to the family Apiaceae and it is a herbaceous medicinal plant. It is found mainly in the Mediterranean regions and also distributed abundantly throughout the world as introduced species. Many times, A. visnaga is weed as well as used in many countries as herbal medicine for different purposes. Ancient records reveal various medicinal properties of A. visnaga as a popular source to cure variety of different ailments. The plant is used directly as a herb or as a component for production of a number of herbal medicines used in the cure of renal colic, ureteric stones, angina pectoris, the coronary vessels, cardiovascular disorders and asthma. Also it is used as a folk medicine for vitiligo and psoriasis. This review highlights the commonly recognized medicinal uses of A. visnaga, its chemistry and ethnobotanical uses and will also serve as ready reference for future research.
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Tribulus terrestris is well known for its medicinal importance in curing urino-genital disorders. Amplified fragment length polymorphism (AFLP), selec-tive amplification of microsatellite polymorphic loci (SAMPL), inter-simple sequence repeat (ISSR) and ran-domly amplified polymorphic DNA (RAPD) markers were used for the first time for the detection of genetic poly-morphism in this medicinal herb from samples collected from various geographical regions of India. Six assays each of AFLP and SAMPL markers and 21 each of ISSR and RAPD markers were utilized. AFLP yielded 500 scorable amplified products, of which 82.9% were polymorphic. SAMPL primers amplified 488 bands, 462 being poly-morphic (94.7%). The range of amplified bands was 66 [(TC) 8 G + M-CAG] to 98 [(CA) 6 AG + M-CAC] and the percentage polymorphism, 89.9 [from (CT) 4 C (AC) 4 A + M-CTG] to 100 [from (GACA) 4 + M-CTA]. The ISSR primers amplified 239 bands of 0.4–2.5 kb, 73.6% showed polymorphism. The amplified products ranged from 5 to 16 and the percentage polymorphism 40–100. RAPD assays produced 276 bands, of which 163 were polymorphic (59%). Mantel test employed for detection of goodness of fit established cophenetic correlation values above 0.9 for all the four marker systems. The dendrograms and PCA plots derived from the binary data matrices of the four marker systems are highly concordant. High bootstrap values were obtained at major nodes of phenograms through WINBOOT software. The relative efficiency of the four molecular marker systems calculated on the basis of multiplex ratio, marker index and average heterozygosity revealed SAMPL to be the best. Distinct DNA finger-printing profile, unique to every geographical region could be obtained with all the four molecular marker systems. Clustering can be a good indicator for clear separation of genotypes from different regions in well-defined groups that are supported by high bootstrap values.
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Tribulus terrestris is a valuable herb known for its application in the folk medicine in many parts of the world. Furostanol and spirostanol saponins of tigogenin, neotigogenin, gitogenin, neogitogenin, hecogenin, neohecogenin, diosgenin, chlorogenin, ruscogenin and sarsasapogenin type are frequently found in this plant. Four sulphated saponins of tigogenin and diosgenin type are also isolated. Extracts and steroidal saponins have been found to possess various pharmacological activities. Preparations based on the saponin fraction of T. terrestris are used for treatment of infertility and libido disorders in men and women, as well as for treatment of cardiac diseases. Food supplements containing T. terrestris extracts are on sale in USA and Europe with claim of a general stimulating action.
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The effectiveness of an androgenic nutritional supplement designed to enhance serum testosterone concentrations and prevent the formation of dihydrotestosterone and estrogen was investigated in healthy 3 to 58 year old men. Subjects were randomly assigned to consume a nutritional supplement (AND-HB) containing 300-mg androstenediol, 480-mg saw palmetto, 450-mg indole-3-carbinol, 300-mg chrysin, 1,500 mg gamma-linolenic acid and 1.350-mg Tribulus terrestris per day (n = 28), or placebo (n = 27) for 28 days. Subjects were stratified into age groups to represent the fourth (30 year olds, n = 20), fifth (40 year olds, n = 20) and sixth (50 year olds, n = 16) decades of life. Serum free testosterone, total testosterone, androstenedione, dihydrotestosterone, estradiol, prostate specific antigen and lipid concentrations were measured before supplementation and weekly for four weeks. Basal serum total testosterone, estradiol, and prostate specific antigen (PSA) concentrations were not different between age groups. Basal serum free testosterone concentrations were higher (p < 0.05) in the 30- (70.5 +/- 3.6 pmol/L) than in the 50 year olds (50.8 +/- 4.5 pmol/L). Basal serum androstenedione and dihydrotestosterone (DHT) concentrations were significantly higher in the 30- (for androstenedione and DHT, respectively, 10.4 +/- 0.6 nmol/L and 2198.2 +/- 166.5 pmol/L) than in the 40- (6.8 +/- 0.5 nmol/L and 1736.8 +/- 152.0 pmol/L) or 50 year olds (6.0 +/- 0.7 nmol/L and 1983.7 +/- 147.8 pmol/L). Basal serum hormone concentrations did not differ between the treatment groups. Serum concentrations of total testosterone and PSA were unchanged by supplementation. Ingestion of AND-HB resulted in increased (p < 0.05) serum androstenedione (174%), free testosterone (37%), DHT (57%) and estradiol (86%) throughout the four weeks. There was no relationship between the increases in serum free testosterone, androstenedione, DHT, or estradiol and age (r2 = 0.08, 0.03, 0.05 and 0.02, respectively). Serum HDL-C concentrations were reduced (p < 0.05) by 0.14 mmol/L in AND-HB. These data indicate that ingestion of androstenediol combined with herbal products does not prevent the formation of estradiol and dihydrotestosterone.
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This paper describes the first analytical method suitable for the determination of steroidal saponins in Tribulus terrestris. A separation by high performance liquid chromatography (HPLC) was achieved by using a reversed-phase (RP-18) column, evaporative light scattering (ELS) detection, and a water/acetonitrile gradient as the mobile phase. The marker compound, protodioscin, was detected at a concentration as low as 10.0 microg/mL. Several different samples of plant material were successfully analyzed, and depending on origin and plant part used for extraction, significant differences in the composition of the saponins were observed. The analysis of market products showed considerable variations of 0.17 to 6.49% in the protodioscin content.
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The known furostanol saponins methylprotodioscin and protodioscin and two new sulfated saponins, sodium salt of 26-O-beta-glucopyranosyl-22alpha-methoxy-(25R)-furost-5-ene-3beta,26-diol-3-O-alpha-rhamnopyranosyl-(1-->2)-beta-4-O-sulfo-glucopyranoside (methylprototribestin) and sodium salt of 26-O-beta-glucopyranosyl-22alpha-hydroxy-(25R)-furost-5-ene-3beta,26-diol-3-O-alpha-rhamnopyranosyl-(1-->2)-beta-4-O-sulfo-glucopyranoside (prototribestin) have been isolated from the aerial parts of Tribulus terrestris L. growing in Bulgaria. The structures of the new compounds were elucidated on the basis of 1D and 2D (DQF-COSY, TOCSY, HSQC-TOCSY, HSQC, HMBC, ROESY) NMR data, ESI mass spectra and chemical transformation.
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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.
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The preventive and therapeutic effects of saponin from Tribulus terrestris L. on diet-induced hyperlipidemia in mice have been studied. It showed that in preventive experiment the saponin could significantly low the levels of serum TC (P < 0.05), LDL-c (P < 0.01) and liver TC (P < 0.05), TG (P < 0.05), and increase the activities of superoxide-dismutase (SOD) in liver. The therapeutic experiment showed that the saponin could significantly reduce the contents of serum TC (P < 0.05) and liver TC (P < 0.01).
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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.
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The steroidal saponins of Tribulus terrestris L. (Zygophyllaceae) are considered to be the factor responsible for biological activity of products derived from this plant. The activity depends on the concentration and the composition of active saponins, which in turn is influenced by the geographical origin of plant material. Samples of T. terrestris collected in Bulgaria, Greece, Serbia, Macedonia, Turkey, Georgia, Iran, Vietnam and India were analyzed by LC-ESI/MS/MS for the presence and the concentration of protodioscin (1), prototribestin (2), pseudoprotodioscin (3), dioscin (4), tribestin (5) and tribulosin (6). The flavonoid rutin (7) was also included in the comparison. The results revealed distinct differences in the content of these compounds depending on region of sample collection, plant part studied and stage of plant development. The samples from Bulgaria, Turkey, Greece, Serbia, Macedonia, Georgia and Iran exhibited similar chemical profile and only some quantitative difference in the content of 1-7 with protodioscin (1) and prototribestin (2) as main components. The Vietnamese and Indian samples exhibit totally different chemical profile. They lack 2 and 5, while tribulosin (6) is present in high amounts. Compounds different from 1 to 7 are dominating in these 3 samples. The presented results suggested the existence of one chemotype common to the East South European and West Asian regions. Most probably, the Vietnamese and Indian samples belong to other chemotypes which are still to be studied and characterized. No clear correlation between the burrs morphology and the chemical composition of the samples has been found.
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The structure of glycoside „C” (I) from the overground part of Tribulus terrestris L., was established by enzymatic hydrolysis and oxidatJve degradation as the furostanol bisglycoside protodioscin. Acid hydrolysis yielded the spirostanol diosgenin, a trace of tigogenin, glucose and rhamnose.
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Steroid saponins isolated from various plants are reviewed. The newer techniques used in their isolation and structure elucidation are discussed. A compilation of the saponins isolated up to 1980 along with their available physical data is included. The basic steroidal saponins isolated after 1972 are also compiled.
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Successive extracts of Tribulus terrestris prepared using petroleum ether, chloroform, 50% methanol and water were tested for anthelmintic activity in-vitro using the nematode Caenorhabditis elegans. The activity could be detected only in 50% methanol extract which on further bioactivity guided fractionation and chromatographic separation yielded a spirostanol type saponin, tribulosin and β-sitosterol-D-glucoside. Both the compounds exhibited anthelmintic activity with ED50 of 76.25 and 82.50 μg/ml respectively.
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Since the beginning of civilization, and perhaps as early as Neanderthal man, people have used plants as medicine. Evidence indicates that people used plants to cure themselves, e.g. Chinese Emperor (2800 BC); Babylon (1770 BC); Ancient Egypt (1550 BC). Islamic and Indian physicians also wrote many works prior to 1100 AD and the Seals from the Harappan site in Pakistan (2000 BC) also indicate use of plants. New aspects of medicinal plants need to be studied. For example, we should address the question "why plant diversity declines, when plants with weedy traits become more abundant". This is consequently followed by, species that have traits permitting their persistence in degraded and speciespoor ecosystems which are likely to carry high pathogen and vector burdens. Indigenous communities of Pakistan play a vital role in conservation of medicinal plants. Intentionally or unintentionally, people have evolved strategies for doing so in the form of rituals, beliefs and taboos. Various traditional harvesting methods described in one of the study suggest that they were efficient to utilize the natural resources. Our efforts are towards not only providing food security, nutrition and health care to the tribal people, but also to recover, record and diffuse local botanical knowledge and wisdom.
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Three new steroid sapogenins, 25(R)-spirostane-3,5-diene-12-one (3), 25(R)-spirostane-2β, 3α-diol-4-ene-12-one (4), 25(R)-spirostane-24β-ol-4-ene-3, 12-dione (5), together with two known compounds, hecogenin (1), and 25(R)-spirostane-4-ene-3, 12-dione (2), were isolated from Tribulus terrestris L. Their structures were elucidated by the spectral analyses.
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Crystalloid material soluble in acetic acid was isolated from the bile of lambs with alveld (a hepatogenous photosensitization disease which develops after grazing Narthecium ossifragum). The main components of these bile extracts were shown by hydrolysis, GC-MS, TLC, LSIMS, H-1 and C-13 NMR, and X-ray analysis to be salts of a 4:1 mixture of episarsasapogenin beta-D-glucuronide (1) and epismilagenin beta-D-glucuronide (2). The C-13 NMR spectrum of 1 was fully assigned by comparison with the NMR spectra of model compounds. A metabolic route for conversion of the sarsasapogenin saponins of N. ossifragum into 1 is proposed. Saponins were extracted from the foliage of N. ossifragum, Tribulus terrestris, and Panicum miliaceum. The saponins were hydrolyzed to sapogenins, which were examined by NMR spectroscopy and GC-MS. P. miliaceum afforded a 4:1 mixture of diosgenin and yamogenin, T. terrestris gave a 5:1 mixture of diosgenin and tigogenin, and N. ossifragum yielded a mixture (82:9:5:4) of sarsasapogenin, smilagenin, yamogenin, and another spirostanol, tentatively identified as neotigogenin.
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The aim of this study was to investigate the pleotropic effects of an extract of a traditional herb, Tribulus terrestris (TT), on the lipid profile and vascular endothelium of the abdominal aorta in New Zealand rabbits fed a cholesterol-rich diet. Eighteen rabbits were randomly divided into three groups (n=6 for each). One experimental group (EG-I) was given a cholesterol-rich diet, a second experimental group (EG-II) was treated with TT following a cholesterol-rich diet, and a control group (CG) was fed a standard diet. Blood samples were collected on day 0 and then at weeks 4 and 12 to determine total serum cholesterol (TC), high density lipid-cholesterol (HDL-C), low density lipid-cholesterol (LDL-C) and triglyceride (TG) levels. Tissues were collected from the abdominal aorta for immunohistochemistry and transmission and scanning electron microscopy. In EG-II, the serum lipid profile was significantly lower than that of EG-I at week 12 with a reduction of TC: 65%; LDL-C: 66%; HDL-C: 64%; TG: 55%. Ultrastructural analysis revealed that endothelial damage was more prominent in EG-I compared to EG-II. The ruptured endothelial linings and damaged cellular surfaces increased in EG-I compared to EG-II. Our data indicate that dietary intake of TT can significantly lower serum lipid profiles, decrease endothelial cellular surface damage and rupture and may partially repair the endothelial dysfunction resulting from hyperlipidemia.
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The availability of detailed environmental data, together with inexpensive and powerful computers, has fueled a rapid increase in predictive modeling of species environmental requirements and geographic distributions. For some species, detailed presence/absence occurrence data are available, allowing the use of a variety of standard statistical techniques. However, absence data are not available for most species. In this paper, we introduce the use of the maximum entropy method (Maxent) for modeling species geographic distributions with presence-only data. Maxent is a general-purpose machine learning method with a simple and precise mathematical formulation, and it has a number of aspects that make it well-suited for species distribution modeling. In order to investigate the efficacy of the method, here we perform a continental-scale case study using two Neotropical mammals: a lowland species of sloth, Bradypus variegatus, and a small montane murid rodent, Microryzomys minutus. We compared Maxent predictions with those of a commonly used presence-only modeling method, the Genetic Algorithm for Rule-Set Prediction (GARP). We made predictions on 10 random subsets of the occurrence records for both species, and then used the remaining localities for testing. Both algorithms provided reasonable estimates of the species’ range, far superior to the shaded outline maps available in field guides. All models were significantly better than random in both binomial tests of omission and receiver operating characteristic (ROC) analyses. The area under the ROC curve (AUC) was almost always higher for Maxent, indicating better discrimination of suitable versus unsuitable areas for the species. The Maxent modeling approach can be used in its present form for many applications with presence-only datasets, and merits further research and development.
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Further studies on the constituents of the fruits of Tribulus terrestris led to the isolation of six new furostanol saponins, 26-O-β- d-glucopyranosyl (25R)-furostane-2α,3β,22α,26-tetrol-3-O-β-d-glucopyranosyl (1–4)-β-d-galactopyranoside, 26- O-β-d-glucopyranosyl (25R,S)-5α-furostane-2α,3β,22α,26-tetrol-3-O-β-d-galactopyranosyl(1–2)-β-d- glucopyranosyl(1–4)-β-d-galactopyranoside, 26-O-β-d-glucopyranosyl (25R,S)-5α-furostane-3β,22α,26-triol-3- O-β-d-galactopyranosyl(1–2)-β-d-glucopyranosyl(1–4)-β-d-galactopyranoside, 26-O-β-d-glucopyranosyl (25 R,S)-5α-furostan-12-one-3β,22α,26-triol-3-O-β-d-galactopyranosyl(1–2)-β-d-glucopyranosyl (1–4)-β-d- galactopyranoside, 26-O-β-d-glucopyranosyl (25R,S)-furost-5-ene-3β,22α,26-triol-3-O-β-d-galactopyranosyl(1–2)- β-d-glucopyranosyl(1–4)-β-d-galactopyranoside, 26-O-β-d-glucopyranosyl (25R)-5α-furost-20(22)-en-12-one-3β,26- diol-3-O-β-d-galactopyranosyl(1–2)-β-d-glucopyranosyl(1–4)-β-d-galactopyranoside, named terrestrosin F—K, respectively. The structures were elucidated on the basis of spectroscopic studies of the isolated compounds and their hydrolysed products.
Article
Twenty-five flavonoid glycosides were detected in Tribulus pentandrus and T. terrestris. The glycosides belong to the common flavonols, kaempferol, quercetin and isorhamnetin, with the 3-gentiobiosides as the major glycosides. Traces of a flavone (tricin) glycoside was also present in T. pentandrus. The separation of Tribulaceae as a distinct family from Zygophyllaceae is discussed.
Article
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.
Article
In addition to hecogenin 3-O-beta-D-glucopyranosyl(1--> 4)-beta-D-galactopyranoside, two new steroidal saponins were isolated from the aerial parts of Tribulus terrestris L. On the basis of chemical and spectroscopic evidence, especially 2D NMR spectroscopic techniques, the structures of the new saponins were established as 26-O-beta-D-glucopyranosyl-3-O-[-beta-D-xylopyranosyl(1--> 3)--beta-D-galactopyranosyl(1-->2)--beta-D-glucopyranosyl (1--> 4)-beta-D-glucopyranosyl]-5 alpha-furost-20(22)-en-12-one-3 beta,26-diol and 26-O-beta-D-glucopyranosyl-3-O-[{beta-D-xylopyranosyl (1-->3)--beta-D-galactopyranosyl(1-->2)--beta-D-glucopyranosyl(1 -->4)-beta-D-glucopyranosyl]-5 alpha-furostan-12-one-3 beta,22,26-triol.
Article
By activity-guided fractionation, three known steroidal saponins, prosapogenin A of dioscin, dioscin and gracillin, were isolated from the total saponin fraction of Dioscorea coiletti var. hypoglauca as active compounds causing morphological abnormality of Pyricularia oryzae mycelia. The compounds also exhibited cytotoxic activity against the cancer cell line K562 in vitro. The structures of the compounds were elucidated on the basis of chemical evidence and IR, FAB-MS, 1H-NMR, 13C-NMR, and two-dimensional NMR (2D-NMR) analysis.
Article
Tribulus terrestris L. is an annual plant which has been commonly used in folk medicine as diuretic and against colic pains, hypertension and hypercholesterolemia in Turkey. This study investigated the effects of liophilized saponin mixture of this plant on several smooth muscle preparations in vitro. The liophilized material was obtained from dried and powdered T. terrestris L. by specific extraction method for saponins. Median lethal dose (LD50) of saponin mixture on Swiss albino mice was calculated according to Litchfield-Wilcoxon method via i.p. route. LD50 and its 95% confidence limits were 813 and 739-894 mg.kg-1 respectively. Saponin mixture has caused a significant decrease on peristaltic movements of isolated sheep ureter and rabbit jejunum preparations in a dose-dependent manner (p < 0.05). However it has been observed no effect on isolated rabbit aorta and its contractile response to KCl or noradrenaline (p > 0.05). According to these results it has been suggested that T. terrestris L. or its saponin mixture may be useful on some smooth muscle spasms or colic pains.
Article
A rapid 96-well plate assay using sulphorhodamine B (SRB) protein stain for cell number has been adopted to screen herbs used in traditional treatments of vitiligo for substances capable of stimulating melanocyte proliferation. Its applicability to melan-a cells, a mouse pigmented cell line, has been validated. SRB assay produced good linearity up to 11 x 10(4) cells/well and interference by melanin present in the cells accounted for less than 10% of the total optical density readings. The intra-assay variation was small but interassay variation was marked. For better assay precision, it is recommended that the results to be compared should be performed on the same day and controls should be plated in the same experiment, ideally in the same plate. Optimum conditions for exponential melan-a cell growth were established: viz. initial plating density (3-8 x 10(3) cells/well), incubation period (4 days) and foetal bovine serum concentration (5%). Under these conditions cells were responsive to the mitogen tetradecanoyl phorbol acetate (TPA). Out of 28 herbal extracts screened in this assay, significant stimulation (P < 0.05) of melanocyte proliferation was observed, in the absence of TPA, using aqueous extracts of Astragalus membranaceous root, Citrus reticulata peel, Dictamnus dasycarpus root bark. Ophiopogon japonicus root, Poria cocos sclerotium and Tribulus terrestris fruit.
Article
The objective of the present study was to investigate the effect of oral treatment of Tribulus terrestris (TT) extract on the isolated corpus cavernosal tissue of New Zealand white (NZW) rabbits and to determine the mechanism by which protodioscin (PTN), a constituent of the TT, exerts its pharmacological effects. Twenty-four NZW rabbits were randomly assigned to 4 experimental groups of 6 each. Group I served as control. Groups II to IV were treated with the extract at different dose levels, i.e. 2.5 mg/kg, 5 mg/kg and 10 mg/kg body weight, respectively. The TT extract was administered orally, once daily, for a period of 8 weeks. The rabbits were then sacrificed and their penile tissue isolated to evaluate the responses to both contracting and relaxing pharmacological agents and electrical field stimulation (EFS). PTN on its own had no effect on the isolated corpus cavernosal strips. The relaxant responses to EFS, acetylcholine and nitroglycerin in noradrenaline precontracted tissues from treated groups showed an increase in relaxation of a concentration dependent nature compared to that of the tissues from control group. However, the contractile, anti-erectile response of corpus cavernosal tissue to noradrenaline and histamine showed no significant change between the treatment and the control groups. 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 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.
Article
Traditional herbs have been a revolutionary breakthrough in the management of erectile dysfunction and have become known world-wide as an 'instant' treatment. The modern view of the management of erectile dysfunction subscribes to a single etiology, i.e. the mechanism of erection. A large number of pharmacological agents are orally consumed and vasoactive agents inserted intraurethrally or injected intrapenially to regain good erection. Modern phytochemicals have developed from traditional herbs. Phytochemicals focus their mechanism of healing action to the root cause, i.e. the inability to control the proper function of the whole body system. Hence phytochemicals manage erectile dysfunction in the frame of sexual dysfunction as a whole entity. Protodioscin is a phytochemical agent derived from Tribulus terrestris L plant, which has been clinically proven to improve sexual desire and enhance erection via the conversion of protodioscine to DHEA (De-Hydro-Epi-Androsterone). Preliminary observations suggest that Tribulus terrestris L grown on different soils does not consistently produce the active component Protodioscin. Further photochemical studies of many other herbal plants are needed to explain the inconsistent results found with other herbal plants, such as in diversities of Ginseng, Eurycoma longifolia, Pimpinella pruacen, Muara puama, Ginkgo biloba, Yohimbe etc.
Article
Three new steroidal saponins 1-3, together with five known steroidal saponins, L-mannitol and an inorganic salt were isolated from Tribulus terrestris L. (Zygophyllaceae). The structures of the new steroidal saponins were elucidated as hecogenin 3-O-beta-xylopyranosyl(1-->3)-beta-glucopyranosyl(1-->4)-beta-galactopyr anoside (1), hecogenin 3-O-beta-glucopyranosyl(1-->2)-beta-glucopyranosyl(1-->4)- beta-galactopyranoside (2) and 3-O-[beta-xylopyranosyl(1-->2)-[beta-xylopyranosyl(1-->3)]-beta- glucopyranosyl(1-->4)-[alpha-rhamnopyranosyl(1-->2)]-beta-galactopyranos yl]- 26-O-beta-glucopyranosyl-22-methoxy-(3 beta,5 alpha,25R)-furostan-3,26-diol (3). Structure elucidation was accomplished by 1D and 2D NMR spectra (13C-1H COSY, HMQC, HMBC, 1H-1H COSY, TOCSY, and NOESY), mass spectrometry (FABMS, ESIMS) and chemical methods.
Article
Three new steroidal saponins (1-3) were isolated from the fruits of Tribulus terrestris. Their structures were assigned by spectroscopic methods (IR, HRESIMS, 1D- and 2D-NMR) as 26-O-beta-D-glucopyranosyl-(25S)-5beta-furost-20(22)-en-3bet a, 26-diol-3-O-alpha-L-rhamnopyranosyl-(1-->2)-[alpha-L-rhamnopyranosyl- (1-->4)]-beta-D-glucopyranoside (1), 26-O-beta-D-glucopyranosyl-(25S)-5beta-furost-20(22)-en-3bet a, 26-diol-3-O-alpha-L-rhamnopyranosyl-(1-->2)-[beta-D-glucopyranosyl-(1 -->4)]-beta-D-galactopyranoside (2), and 25(S)-5beta-spirostan-3beta-ol-3-O-alpha-L-rhamnopyranosyl-( 1-->2)-[b eta-D-glucopyranosyl-(1-->4)]-beta-D-galactopyranoside (3). Compound 3 showed cytotoxicity against a human malignant melanoma cell line (SK-MEL).
Article
Three new steroidal saponins were isolated from the fruits of Tribulus terrestris, and their structures were elucidated as (25R,S)-5 alpha-spirostane-12-one-3 beta-ol-3-O-beta-xylopyranosyl(1-->2)- [beta-xylopyranosyl(1-->3)]-beta-glucopyranosyl(1-->4)-[alpha-rhamno- pyranosyl(1-->2)]-beta-galactopyranoside; 26-O-beta-glucopyranosyl-(25S)-5 alpha-furostane-12-one-3 beta,22 alpha,26-triol-3-O-beta-glucopyranosyl(1-->2)-beta-galactopyranoside; 26-O-beta-glucopyranosyl-(25S)-5 alpha-furostane-12-one-3 beta,22 alpha,26-triol-3-O-beta-glucopyranosyl(1-->4)-[alpha- rhamnopyranosyl(1-->2)]-beta-galactopyranoside, respectively, by spectroscopic analysis and color reaction.
Article
Protodioscin (NSC-698 796) is a furostanol saponin isolated from the rhizome of Dioscorea collettii var. hypoglauca (Dioscoreaceae), a Chinese herbal remedy for the treatment of cervical carcinoma, carcinoma of urinary bladder and renal tumor for centuries. To systematically evaluate its potential anticancer activity, protodioscin was tested for cytotoxicity in vitro against 60 human cancer cell lines in the NCI's (National Cancer Institute, USA) anticancer drug screen. As a result, protodioscin was cytotoxic against most cell lines from leukemia and solid tumors in the NCI's human cancer panel, especially selectively against one leukemia line (MOLT-4), one NSCLC line (A549/ATCC), two colon cancer lines (HCT-116 and SW-620), one CNS cancer line (SNB-75), one melanoma line (LOX IMVI), and one renal cancer line (786 - 0) with GI50 < or = 2.0 microM. In the general view of mean graphs, leukemia, colon cancer and prostate cancer are the most sensitive subpanels, while ovarian cancer is the least sensitive subpanel. Based on an analysis of COMPARE computer program with protodioscin as a seed compound, no compounds in the NCI's anticancer drug screen database have cytotoxicity patterns (mean graphs) similar to those of protodioscin, indicating that a potential novel mechanism of anticancer action is involved.
Article
Tribulus terrestris (TT) has long been used in the traditional Chinese and Indian systems of medicine for the treatment of various ailments and is popularly claimed to improve sexual functions in man. Sexual behaviour and intracavernous pressure (ICP) were studied in both normal and castrated rats to further understand the role of TT containing protodioscin (PTN) as an aphrodisiac. Adult Sprague-Dawley rats were divided into five groups of 8 each that included distilled water treated (normal and castrated), testosterone treated (normal and castrated, 10 mg/kg body weight, subcutaneously, bi-weekly) and TT treated (castrated, 5 mg/kg body weight, orally once daily). Decreases in body weight, prostate weight and ICP were observed among the castrated groups of rats compared to the intact group. There was an overall reduction in the sexual behaviour parameters in the castrated groups of rats as reflected by decrease in mount and intromission frequencies (MF and IF) and increase in mount, intromission, ejaculation latencies (ML, IL, EL) as well as post-ejaculatory interval (PEI). Compared to the castrated control, treatment of castrated rats (with either testosterone or TT extract) showed increase in prostate weight and ICP that were statistically significant. There was also a mild to moderate improvement of the sexual behaviour parameters as evidenced by increase in MF and IF; decrease in ML, IL and PEI. These results were statistically significant. It is concluded that TT extract appears to possess aphrodisiac activity probably due to androgen increasing property of TT (observed in our earlier study on primates).
Article
The steroidal saponin constituents obtained from Tribulus terrestris were tested for their antimicrobial and cytotoxic effects. The spirostanol-based steroidal saponins 1-3 exhibited remarkable activity against fungal organisms (Candida albicans and Cryptococcus neoformans) and cancer cell lines [human malignant melanoma (SK-MEL), human oral epidermoid carcinoma (KB), human breast ductal carcinoma (BT-549), and human ovary carcinoma (SK-OV-3)], while none of the compounds possessing the furostanol framework 4-7 showed activity. The most active spirostanol glycoside, compound 3 exhibited a broad range of anticancer activity against cell lines, SK-MEL, KB, BT-549 and SK-OV-3 at IC50s of 6.0, 7.0, 6.0 and 8.2 micrograms/ml, respectively, while compounds 1 and 2 showed selective cytotoxicity against SK-MEL at 6.7 and 9.1 micrograms/ml, respectively. The minimum inhibitory concentrations (MIC) in antifungal bioassay for compounds 1-3 varied from 1.5 to 6.2 micrograms/ml, which prompted to conclude certain structural features are required for these bioactivities.
Article
To investigate the chemical constituents of the fruit of Tribulus terrestris J.. 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. 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). Compounds I and II are new steroidal saponins.
Article
To study the hypoglycemic effect of saponin from Tribulus terrestris L. 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. 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. Saponin from Tribulue terrestris could significantly reduce the level of serum glucose.
Article
Tribulus terrestris L. (Zygophyllaceae) which is called Al-Gutub (in Iraqi dialect) or Quti;ba (in classical Arabic medicine), and Zea mays were both used alone or in combination by Iraqi herbalists to propel urinary stones. We studied the aqueous extract of the leaves and fruits of T. terrestris and the hair of Z. mays, to determine their diuretic activity and the contractile effect of T. terrestris. The aqueous extract was filtered and the solvent was evaporated to produce a dry crude extract. The dry extract was then dissolved in physiological saline to make the required concentrations. Wistar male rats were used for the diuresis test and strips of isolated Guinea pig ileum were used for the contractility test. The aqueous extract of T. terrestris, in oral dose of 5g/kg elicited a positive diuresis, which was slightly more than that of furosemide. Z. mays aqueous extract did not result in significant diuresis when given alone in oral dose of 5g/kg, while combination of Z. mays and T. terrestris extracts produced the same extent of diuresis as that produced by T. terrestris alone. Na(+), K(+) and Cl(+) concentrations in the urine had also much increased. In addition to its diuretic activity T. terrestris had evoked a contractile activity on Guinea pig ileum. T. terrestris has long been used empirically to propel urinary stones. The diuretic and contractile effects of T. terrestris indicate that it has the potential of propelling urinary stones and merits further pharmacological studies.
Article
An HPLC-ELSD-ESI-MS method has been developed for the analysis of the steroidal saponins in the aerial parts of Tribulus terrestris. Protodioscin, a new saponin (5,6-dihydroprotodioscin, neoprotodioscin) and their respective sulfates were detected. The structure of the new compound was elucidated on the basis of NMR and ESI-MS spectral analysis.
Article
Viagra has had a profound influence on the search for natural products with erectile-dysfunction activity. To date the "natural" equivalent is not in existence but several pure compounds from nature, e.g., Yohimbine, Citrulline, two pyrano-isoflavones, berberine, forskolin and others, have either been re-examined or are new potential candidates. Intense activity exists in the area of testing semi-purified plant extracts for erectile dysfunction activity.
Article
Methyl protodioscin (NSC-698790) was a furostanol saponin isolated from the rhizome of Dioscorea collettii var. hypoglauca (Dioscoreaceae), a Chinese herbal remedy for the treatment of cervical carcinoma, carcinoma of the urinary bladder, and renal tumors for centuries. To systematically evaluate its potential anticancer activity, methyl protodioscin was tested cytotoxicity in vitro against human cancer cell lines by the NCI's (National Cancer Institute) anticancer drug screen. As a result, methyl protodioscin showed strong cytotoxicity against most cell lines from solid tumors with GI50 < or = 10.0 microM, especially selectively against one colon cancer line (HCT-15) and one breast cancer line (MDA-MB-435) with GI50 < 2.0 microM but moderate cytotoxicity was shown against leukemia cell lines with GI50 10-30 microM. The data are consistent with the fact that the rhizome of D. collettii var. hypoglauca has been employed for the treatment of solid tumors rather than leukemia in China for centuries. Based on an analysis using the COMPARE computer program with methyl protodioscin as a seed compound, no compounds in the NCI's anticancer drug screen database have cytotoxicity patterns similar to those of methyl protodioscin, indicating a potential novel mechanism of anticancer action.
Article
Antimicrobial activity of organic and aqueous extracts from fruits, leaves and roots of Tribulus terrestris L., an Iraqi medicinal plant used as urinary anti-infective in folk medicine, was examined against 11 species of pathogenic and non-pathogenic microorganisms: Staphylococcus aureus, Bacillus subtilis, Bacillus cereus, Corynebacterium diphtheriae, Escherichia coli, Proteus vulgaris, Serratia marcescens, Salmonella typhimurium, Klebsiella pneumoniae, Pseudomonas aeruginosa and Candida albicans using microdilution method in 96 multiwell microtiter plates. All the extracts from the different parts of the plant showed antimicrobial activity against most tested microorganisms. The most active extract against both Gram-negative and Gram-positive bacteria was ethanol extract from the fruits with a minimal inhibitory concentration (MIC) value of 0.15 mg/ml against B. subtilis, B. cereus, P. vulgaris and C. diphtheriae. In addition, the same extract from the same plant part demonstrated the strongest antifungal activity against C. albicans with an MIC value of 0.15 mg/ml.