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Antifungal activities and action mechanisms of compounds from Tribulus terrestris l.

第二军医大学学报 2006年第5期27卷 492-492页

作者： zhang jd xu z cao yb chen hs yan l an mm gao ph wang y jia xm jiang yy Department of pharmacology College of Pharmacy Second Military Medical University Shanghai 200438 China

Antifungal activity of natural products is being studied widely. Saponins are known to be antifungal and antibacterial. We used bioassay-guided fractionation to have isolated eight steroid saponins from Tribulus terrestris l. , which were identified as hecogenin-3-O-beta-D-glucopyranosyl ( 1→4 )-beta-D-galactopyranoside ( TTS-8), tigogenin-3-O-beta-D-glucopyranosyl ( 1→4 )-beta-D-galactopyranoside ( TTS-9 ), hecogenin-3-O-beta-D-glucopyranosyl ( 1→2 )-beta-D-glucopyranosyl ( 1 4 )-beta-D-galactopyranoside ( TTS-10 ), hecogenin-3-O-beta-D-xylopyranosyl ( 1→3 )-beta-D-glucopyranosyl ( 1→4 )-beta-D-galactopyranoside ( TTS-11 ), tigogenin-3-O-beta-D-xylopyranosyl ( 1→2 )-[- beta-D-xylopyranosyl ( 1→3 ) ]-beta-D-glucopyranosyl (1→4)-[alpha-l-rhamnopyranosyl (1→2)]-beta-D-galactopyranoside (TTS-12), 3-O-Ebeta-D-xylopyranosyl (1→2)-[beta-D- xylopyranosyl (1→3)]-beta-D-glucopyranosyl ( 1→4)-[alpha-l-rhamnopyranosyl ( 1→2 )]-beta-D-galactopyranosy13-26-O-beta- D-glucopyranosyl-22-methoxy-(3beta, 5alpha, 25R)-furostan-3,26-diol (TTS-13), hecogenin-3-O-beta-D-glucopyranosyl ( 1→2)-[beta-D-xylopyranosyl ( 1→3 )]-beta-D-glucopyranosyl ( 1→4 )-beta-D-galactopyranoside ( TTS-14 ), tigogenin-3-O-beta-D- glucopyranosyl ( 1→2 )-[ beta-D-xylopyranosyl ( 1→3 )]-beta-D-glucopyranosyl ( 1→4 )-beta-D-galaetopyranoside ( TTS-15 ). The in vitro antifungal activities of the eight saponins against five yeasts, Candida albicans, Candida glabrata, Candida parapsilosis, Candida tropicalis and Cryptococcus neoformans were studied using microbroth dilution assay. In vivo activity of TTS-12 in a Candida albicans vaginal infection model was studied in particular. The results showed that TTS-12 and TTS-15 were very effective against several pathogenic candidal species and Cryptococcus neoformans in vitro. It is noteworthy that TTS-12 and TTS-15 were very active against Candida albicans (MIC50 = 10 and 2.3 microg/ml) and Cryptococcus neoformans (MIC50 = 1.7 and 6. 7 microg/ml).

关键词： Tribulus terrestris l 抗真菌活性抗菌药

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

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第二军医大学学报 2006年第6期27卷 664-664页

作者： zhang jd cao yb xu z Sun HH An mm yan l chen hs gao ph wang y jia xm jiang yy Department of pharmacology College of Pharmacy Second Military Medical University Shanghai 200438China

Antifungal activity of natural products is being studied widely。Saponins are known to be antifungal and antibacterial。We have isolated eight steroid saponins from Tribulus terrestris l。, namely TTS-8, TTS-9, TTS-10, TTS-11, TTS-12, TTS-13, TTS-14 and TTS-15。TTS-12 and TTS-15 were identified as tigogenin-3-O-β-D-xylopyranosyl(1→2)-[-β-D-xylopyranosyl( 1→3 ) 3-β- D-glucopyranosyl ( 1→4 )- 1-α-l-rhamnopyranosyl ( 1→2 ) 3-β-D-galactopyranoside and tigogenin-3-O-β-D-glucopyranpyranosyl(1→2)-[-β-D-xylopyranosyl(1→3)3-β-D-glucopyranosyl(1→4)-β-D-galactopyranoside, respectively。The in vitro antifungal activities of the eight saponins against six fluconazole-resistant yeasts, Candida albicans, Candida glabrata, Candida para psilosis , Candida tropicalis , Candida krusei , and Cryptococcus neo f ormans were studied using microbroth dilution assay。The results showed that TTS-12 and TTS-15 were very effective against several pathogenic candidal species and C。neoformans in vitro。It is noteworthy that TTS-12 and TTS-15 were very active against fluconazole-resistant C。albicans (MIC80 = 4.4, 9.4 mg/ml), C。neoformans (MIC80 =10.7, 18.7 mg/ml) and inherently resistant C。krusei (MIC80 =8.8, 18.4 mg/ml)。So in vivo activity of TTS-12 in a vaginal infection model with fluconazole-resistant C。albicans was studied in particular。Our studies revealed TTS-12 also showed in vivo activities against fluconazole-resistant yeasts。In conclusion, steroid saponins TTS-12 and TTS-15 from Tribulus terrestris l。have significant in vitro antifungal activity against fluconazole-resistant fungi, especially TTS-12 also showed in vivo activity against fluconazole-resistant C。albicans。

关键词：类固醇皂角苷抗菌活性蒺藜病理学

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