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[PMID]: 29505934
[Au] Autor:Zheng H; Li L; Sun B; Gao Y; Song W; Zhao X; Gao Y; Xie Z; Zhang N; Ji J; Yuan H; Lou H
[Ad] Address:Department of Natural Products Chemistry, Key Laboratory of Natural Products & Chemical Biology, Ministry of Education, School of Pharmaceutical Sciences, Shandong University, Jinan, 250012, China.
[Ti] Title:Design and synthesis of furyl/thineyl pyrroloquinolones based on natural alkaloid perlolyrine, lead to the discovery of potent and selective PDE5 inhibitors.
[So] Source:Eur J Med Chem;150:30-38, 2018 Feb 16.
[Is] ISSN:1768-3254
[Cp] Country of publication:France
[La] Language:eng
[Ab] Abstract:Based on perlolyrine (1), a natural alkaloid with weak PDE5 potency from the traditional Chinese aphrodisiac plant Tribulus terrestris L., a series α-substituted tetrahydro-ß-carboline (THßC) derivatives were synthesized via T BF4 -mediated oxidative C-H functionalization of N-aryl THßCs with diverse potassium trifluoroborates. Following Winterfeldt oxidation afforded the corresponding furyl/thienyl pyrroloquinolones, of which 5-ethylthiophene/ethylfuran derivatives 20a-b were identified as the most potent and selective PDE5 inhibitors. Among the enantiomers, (S)-20a and (S)-20b (IC = 0.52 and 0.39 nM) were found to be more effective than their (R)-antipode, display favorable pharmacokinetic profiles, exert in vitro vasorelaxant effects on the isolated thoracic aorta, and exhibit in vivo efficacy in the anesthetized rabbit erectile model.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1803
[Cu] Class update date: 180305
[Lr] Last revision date:180305
[St] Status:Publisher

  2 / 357 MEDLINE  
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[PMID]: 29177586
[Au] Autor:Kim HS; Lee JW; Jang H; Le TPL; Kim JG; Lee MS; Hong JT; Lee MK; Hwang BY
[Ad] Address:College of Pharmacy, Chungbuk National University, Cheongju, 28160, Korea.
[Ti] Title:Phenolic amides from Tribulus terrestris and their inhibitory effects on nitric oxide production in RAW 264.7 cells.
[So] Source:Arch Pharm Res;41(2):192-195, 2018 Feb.
[Is] ISSN:0253-6269
[Cp] Country of publication:Korea (South)
[La] Language:eng
[Ab] Abstract:A new phenolic amide, named cis-terrestriamide (7), together with ten known compounds (1-6, 8-11), were isolated from the methanolic extract of the fruits of Tribulus terrestris. The structure of 7 was elucidated on the basis of extensive analyses of 1D and 2D nuclear magnetic resonance spectroscopic and high resolution mass spectrometry data. Compounds 1, 2, 5, 6, 8, 9, and 11 exhibited inhibitory effects on the lipopolysaccharide-stimulated nitric oxide production in RAW 264.7 cells, with IC values of 18.7-49.4 µM.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1711
[Cu] Class update date: 180210
[Lr] Last revision date:180210
[St] Status:In-Process
[do] DOI:10.1007/s12272-017-0984-0

  3 / 357 MEDLINE  
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[PMID]: 29261340
[Au] Autor:GamalEl Din SF
[Ad] Address:a Kasr Alainy Faculty of Medicine, Andrology and STDs , Cairo University, Cairo , Egypt.
[Ti] Title:Role of Tribulus terrestris in Male Infertility: Is It Real or Fiction?
[So] Source:J Diet Suppl;:1-4, 2017 Dec 20.
[Is] ISSN:1939-022X
[Cp] Country of publication:England
[La] Language:eng
[Ab] Abstract:Tribulus terrestris is an annual herb of the Zygophyllaceae family and is commonly known as Gokshur, Gokharu, or puncturevine. Flavonoids, alkaloids, saponins, lignin, amides, and glycosides are the main active phytoconstituents of this plant. Infertility is defined by the failure to conceive a child after one year or more of regular unprotected sexual intercourse. Infertility affects society at large and has a negative impact on the social and emotional aspects of the patient. This in-depth review presents several studies that evaluate the role of Tribulus terrestris in a chronological order to help us better understand the exact mechanism by which this herbal medicine acts in male infertility. In conclusion, the exact role of Tribulus terrestris in male infertility is still controversial and needs future double-blind placebo-controlled studies that deploy larger cohorts.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1712
[Cu] Class update date: 171220
[Lr] Last revision date:171220
[St] Status:Publisher
[do] DOI:10.1080/19390211.2017.1402843

  4 / 357 MEDLINE  
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[PMID]: 29172782
[Au] Autor:Vale FBC; Zanolla Dias de Souza K; Rezende CR; Geber S
[Ad] Address:a Department of Obstetrics and Gynecology , Universidade Federal de Minas Gerais , Minas Gerais , Brazil.
[Ti] Title:Efficacy of Tribulus Terrestris for the treatment of premenopausal women with hypoactive sexual desire disorder: a randomized double-blinded, placebo-controlled trial.
[So] Source:Gynecol Endocrinol;:1-4, 2017 Nov 27.
[Is] ISSN:1473-0766
[Cp] Country of publication:England
[La] Language:eng
[Ab] Abstract:Although hypoactive sexual desire disorder (HSDD) is the most common sexual complaint, there is no consensus for the ideal treatment. Our study aimed to evaluate the efficacy of treating premenopausal women with HSDD with Tribulus terrestris and its effect on the serum levels of testosterone. We performed a prospective, randomized, double-blind, placebo-controlled trial, with 40 premenopausal women reporting diminished libido, receiving T. terrestris or placebo. The questionnaires FSFI and the QS-F were used to evaluate sexual dysfunction before and after treatment. Patients treated with T. terrestris experienced improvement in total score of FSFI (p < .001) and domains "desire" (p < .001), "sexual arousal" (p = .005), "lubrication" (p = .001), "orgasm" (p <.001), "pain" (p = .030) and "satisfaction" (p = .001). Treatment with placebo did not improve the scores for the "lubrication" and "pain". QS-F scores showed that patients using T. terrestris had improvements in "desire" (p = .012), "sexual arousal/lubrication" (p = .002), "pain" (p = .031), "orgasm" (p = .004) and "satisfaction" (p = .001). Women treated with placebo did not score improvements. Women receiving T. terrestris had increased levels of free (p = .046) and bioavailable (p < .048) testosterone. T. terrestris might be a safe alternative for the treatment of premenopausal women with HSDD as it was effective in reducing the symptoms, probably due to an increase in the serum levels of free and bioavailable testosterone.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1711
[Cu] Class update date: 171127
[Lr] Last revision date:171127
[St] Status:Publisher
[do] DOI:10.1080/09513590.2017.1409711

  5 / 357 MEDLINE  
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[PMID]: 29086839
[Au] Autor:Zhu W; Du Y; Meng H; Dong Y; Li L
[Ad] Address:School of Science, Beijing Technology and Business University, Beijing, 100048, People's Republic of China.
[Ti] Title:A review of traditional pharmacological uses, phytochemistry, and pharmacological activities of Tribulus terrestris.
[So] Source:Chem Cent J;11(1):60, 2017 Jul 11.
[Is] ISSN:1752-153X
[Cp] Country of publication:England
[La] Language:eng
[Ab] Abstract:Tribulus terrestris L. (TT) is an annual plant of the family Zygophyllaceae that has been used for generations to energize, vitalize, and improve sexual function and physical performance in men. The fruits and roots of TT have been used as a folk medicine for thousands of years in China, India, Sudan, and Pakistan. Numerous bioactive phytochemicals, such as saponins and flavonoids, have been isolated and identified from TT that are responsible alone or in combination for various pharmacological activities. This review provides a comprehensive overview of the traditional applications, phytochemistry, pharmacology and overuse of TT and provides evidence for better medicinal usage of TT.
[Pt] Publication type:JOURNAL ARTICLE; REVIEW
[Em] Entry month:1711
[Cu] Class update date: 171102
[Lr] Last revision date:171102
[St] Status:PubMed-not-MEDLINE
[do] DOI:10.1186/s13065-017-0289-x

  6 / 357 MEDLINE  
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[PMID]: 29052328
[Au] Autor:Adeldust H; Farzinpour A; Farshad A; Rostamzadeh J; Lopez-Bejar M
[Ad] Address:Department of Animal Science, College of Agriculture, University of Kurdistan, Sanandaj, Iran.
[Ti] Title:Increased sperm cell production in ageing roosters by an oral treatment with an aromatase inhibitor and a natural herbal extract designed for improving fertility.
[So] Source:Reprod Domest Anim;52 Suppl 4:58-60, 2017 Oct.
[Is] ISSN:1439-0531
[Cp] Country of publication:Germany
[La] Language:eng
[Ab] Abstract:Rooster fertility peaks between 30 and 40 weeks of age and declines rapidly from 50 weeks of age. This is linked to a reduction in the number of spermatozoa in the ejaculate due to high density of spermatids in the seminiferous tubules of low-fertility roosters. In this study, we assessed the effects over spermatogenesis of both letrozole, an aromatase inhibitor, and a commercial herbal extract designed for improving fertility composed by Tribulus, Cinnamomum, Zingiber and Sativus. Forty-two-week-old Ross 308 roosters (n = 24) were distributed into four groups: control, letrozole (0.03 mg/kg), herbal extract (0.04 ml/kg) and letrozole+herbal extract. After 14 weeks of daily oral supplementation, their testes and epididymides were weighed, fixed and sectioned for assessment of spermatogenesis and quantification of sperm cells inside the lumen. Differences in seminiferous tubules measurements and density of sperm cells were tested using R software (version 3.0.1). Although body weight was not affected by the treatment, testes from animals treated with the combination of letrozole and herbal extracts were heavier than those from control animals. Animals treated with either letrozole or herbal extract, or their combination, showed a significant higher number of sperm cells inside the seminiferous tubules and epididymis than control animals (p < .05). These data suggest that the use of letrozole and the herbal extract could improve sperm cell production in ageing roosters. Future studies are needed to disclose the causal mechanisms involved and its effect on fertility and ejaculate features.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1710
[Cu] Class update date: 171020
[Lr] Last revision date:171020
[St] Status:In-Process
[do] DOI:10.1111/rda.13058

  7 / 357 MEDLINE  
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[PMID]: 28939023
[Au] Autor:Jiang YH; Guo JH; Wu S; Yang CH
[Ad] Address:Affiliated Hospital of Shandong University of Traditional Chinese Medicine, Jinan 250011, China.
[Ti] Title:Vascular protective effects of aqueous extracts of Tribulus terrestris on hypertensive endothelial injury.
[So] Source:Chin J Nat Med;15(8):606-614, 2017 Aug.
[Is] ISSN:1875-5364
[Cp] Country of publication:China
[La] Language:eng
[Ab] Abstract:Angiotensin II (Ang II) is involved in endothelium injury during the development of hypertension. Tribulus terrestris (TT) is used to treat hypertension, arteriosclerosis, and post-stroke syndrome in China. The present study aimed to determine the effects of aqueous TT extracts on endothelial injury in spontaneously hypertensive rats (SHRs) and its protective effects against Ang II-induced injury in human umbilical vein endothelial cells (HUVECs). SHRs were administered intragastrically with TT (17.2 or 8.6 g·kg ·d ) for 6 weeks, using valsartan (13.5 mg·kg ·d ) as positive control. Blood pressure, heart rate, endothelial morphology of the thoracic aorta, serum levels of Ang II, endothelin-1 (ET-1), superoxide dismutase (SOD) and malonaldehyde (MDA) were measured. The endothelial injury of HUVECs was induced by 2 × 10 mol·L Ang II. Cell Apoptosisapoptosis, intracellular reactive oxygen species (ROS) was assessed. Endothelial nitric oxide synthase (eNOS), ET-1, SOD, and MDA in the cell culture supernatant and cell migration were assayed. The expression of hypertension-linked genes and proteins were analyzed. TT decreased systolic pressure, diastolic pressure, mean arterial pressure and heart rate, improved endothelial integrity of thoracic aorta, and decreased serum leptin, Ang II, ET-1, NPY, and Hcy, while increased NO in SHRs. TT suppressed Ang II-induced HUVEC proliferation and apoptosis and prolonged the survival, and increased cell migration. TT regulated the ROS, and decreased mRNA expression of Akt1, JAK2, PI3Kα, Erk2, FAK, and NF-κB p65 and protein expression of Erk2, FAK, and NF-κB p65. In conclusion, TT demonstrated anti-hypertensive and endothelial protective effects by regulating Erk2, FAK and NF-κB p65.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1709
[Cu] Class update date: 170923
[Lr] Last revision date:170923
[St] Status:In-Process

  8 / 357 MEDLINE  
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[PMID]: 28849109
[Au] Autor:Lee HH; Ahn EK; Hong SS; Oh JS
[Ad] Address:Department of Pharmacy, College of Pharmacy, Dankook University, Cheonan, Chungcheongnam 31116, Republic of Korea.
[Ti] Title:Anti-inflammatory effect of tribulusamide D isolated from Tribulus terrestris in lipopolysaccharide-stimulated RAW264.7 macrophages.
[So] Source:Mol Med Rep;16(4):4421-4428, 2017 Oct.
[Is] ISSN:1791-3004
[Cp] Country of publication:Greece
[La] Language:eng
[Ab] Abstract:Tribulus terrestris (T. terrestris) has been used as a traditional medicine for the treatment of a variety of diseases, including inflammation, edema and hypertension. The aqueous and ethanol extracts of T. terrestris contain alkaloids, flavonoids, tannins, quinines and phenolic compounds. Tribulusamide D is a compound that has been isolated from the ethanol extract of T. terrestris. The present study investigated the anti­inflammatory effect of tribulusamide D on lipopolysaccharide (LPS)­stimulated RAW 264.7 macrophages. Tribulusamide D inhibited the production of LPS­induced nitric oxide and prostaglandin E2, by reducing the expression of inducible nitric oxide synthase and cyclooxygenase­2 expression, respectively. The expression of these genes associated with inflammation was determined using reverse transcription­polymerase chain reaction and western blot analysis. Furthermore, tribulusamide D reduced the expression of LPS­induced inflammatory cytokines, including interleukin (IL)­6, IL­10 and tumor necrosis factor­α. They were quantified using an enzyme­linked immunosorbent assay. In addition, the present study confirmed that the inhibitory effects of tribulusamide D on the inflammatory response were mediated through inactivation of mitogen­activated protein kinase p38 and inhibition of nuclear localization of nuclear factor­B, which were also determined by western blot analysis. To the best of our knowledge, the current study is the first to demonstrate that tribulusamide D exerts anti­inflammatory activity by altering the expression of inflammatory mediators and cytokines, indicating that tribulusamide D could be developed as a potential therapeutic agent for the treatment of inflammatory disorders.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1708
[Cu] Class update date: 171025
[Lr] Last revision date:171025
[St] Status:In-Process
[do] DOI:10.3892/mmr.2017.7208

  9 / 357 MEDLINE  
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[PMID]: 28849084
[Au] Autor:Park YJ; Cho YR; Oh JS; Ahn EK
[Ad] Address:Bio­center, Gyeonggi Institute of Science and Technology Promotion, Suwon, Gyeonggi 443­270, Republic of Korea.
[Ti] Title:Effects of Tribulus terrestris on monosodium iodoacetate­induced osteoarthritis pain in rats.
[So] Source:Mol Med Rep;16(4):5303-5311, 2017 Oct.
[Is] ISSN:1791-3004
[Cp] Country of publication:Greece
[La] Language:eng
[Ab] Abstract:Tribulus terrestris L. (T. terrestris) has been used as a traditional medicine for the treatment of diuretic, lithontriptic, edema and urinary infections. Previous studies have indicated that it is effective in improving inflammation by regulating tumor necrosis factor­α (TNF)­α, interleukin (IL)­6, IL­10, nitric oxide (NO) and cyclooxygenase (COX)­2. However, the effects and mechanism of action of T. terrestris on osteoarthritis (OA) remain unknown. Therefore, the present study aimed to evaluate the effects of the ethanolic extract of T. terrestris (ETT) in a monosodium iodoacetate (MIA)­induced OA animal model. OA was induced in LEW/SSNHSD rats by intra­articular injection of MIA. Morphometric changes and parameters of the tibial trabecular bone were determined using micro­computed tomography. The molecular mechanisms of ETT in OA were investigated using reverse transcription­polymerase chain reaction, western blotting and gelatin zymogram analysis. Treatment with ETT attenuated MIA­induced OA, and this effect was mediated by the downregulation of NO synthase 2, COX­2, TNF­α and IL­6. Furthermore, the ETT­mediated attenuation of OA was also dependent on the expression of matrix metalloproteinases­2 and ­9. The results of the current study indicate that further evaluation of the mechanisms underlying the attenuation of MIA­induced OA by ETT are required, and may support the development of ETT as a potential therapeutic agent for the treatment of inflammatory diseases such as OA.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1708
[Cu] Class update date: 171025
[Lr] Last revision date:171025
[St] Status:In-Process
[do] DOI:10.3892/mmr.2017.7296

  10 / 357 MEDLINE  
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[PMID]: 28846699
[Au] Autor:Kaushik J; Tandon S; Gupta V; Nayyar J; Singla SK; Tandon C
[Ad] Address:Amity Institute of Biotechnology, Amity University, Noida, India.
[Ti] Title:Response surface methodology based extraction of Tribulus terrestris leads to an upsurge of antilithiatic potential by inhibition of calcium oxalate crystallization processes.
[So] Source:PLoS One;12(8):e0183218, 2017.
[Is] ISSN:1932-6203
[Cp] Country of publication:United States
[La] Language:eng
[Ab] Abstract:Tribulus terrestris has significant antilithiatic efficacy established via both in vitro as well as in vivo studies and is used in numerous anti-urolithiatic herbal formulations viz. Cystone, Uriflow, Uritone and Neeri. However, to fully utilize its antilithiatic potential, the influence of different extraction parameters on antilithiatic ability of T. terrestris aqueous extract needs elucidation. Thus, the current study was undertaken using statistically optimized extraction conditions for aqueous extract preparation. Response surface methodology was employed to observe the influence of three variables i.e. temperature (°C), time (h) and solid: liquid ratio (S: L) on the extraction yield (%) and protein content (mg/g) of T. terrestris aqueous extract. RSM results revealed that the high S:L ratio, low temperature and reduced incubation time were optimal conditions for aqueous extraction. Under such extraction conditions the protein content reached the value of 26.6±1.22 mg/g and the obtained extraction yield was 27.32±1.62%. The assessment of antilithiatic activity of 4 selected extracts (AE1-4), revealed enhanced nucleation and aggregation inhibition of calcium oxalate crystals with AE1 and AE2, which in addition significantly altered the size and morphology of calcium oxalate monohydrate (COM) crystals compared to AE3 and AE4. In vitro cell culture based studies on renal epithelial cells (MDCK, NRK-52E and PK 15) proved that the AE1 showed higher cytoprotective potency by increasing cell viability as compared to the oxalate treated group. The free radical scavenging activity of aqueous extract lowered the reactive oxygen specie's induced damage and potentially reduced the signals of programmed cell death due to oxalate injury. In addition, modulation of the COM crystal morphology was enhanced by AE1 as compared to AE2. The FTIR and GC-MS analysis of AE1, showed the presence of biomolecules which could aid in the attenuation of lithiatic process. In the light of these results the utility of the RSM approach to fully optimize the antilithiatic potential of T. terrestris cannot be undermined.
[Mh] MeSH terms primary: Calcium Oxalate/metabolism
Cell Survival/drug effects
Epithelial Cells/drug effects
Kidney/drug effects
Plant Extracts/pharmacology
Tribulus
[Mh] MeSH terms secundary: Animals
Cell Line
Crystallization
Dogs
Epithelial Cells/metabolism
Kidney/metabolism
Rats
Swine
[Pt] Publication type:JOURNAL ARTICLE
[Nm] Name of substance:0 (Plant Extracts); 2612HC57YE (Calcium Oxalate)
[Em] Entry month:1710
[Cu] Class update date: 171019
[Lr] Last revision date:171019
[Js] Journal subset:IM
[Da] Date of entry for processing:170829
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0183218


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