In Vitro Antischistosomal Activity and Cytotoxicity of 5-Methoxylated Flavones fom Vochysia divergens, a Flood-Adapted Species from Brazilian Pantanal

L. P. Pimenta, K. Lc, Rhavena Graziela Liotti, M. Soares, Daniela P. Aguiar, M. Lg, P. F. Oliveira, D. Tavares, Andrade Ml, W. Cunha, P. Pauletti, J. Ah
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引用次数: 3

Abstract

Background: Vochysia divergens is native to the Amazon Basin and considered an invasive species in the Brazilian Pantanal. In this work, the ethanolic extract of V. divergens leaves was chemically investigated and evaluated in vitro against Schistosoma mansoni adult worms together with the isolated compounds. Methods: The samples were available at concentrations of 12.5, 25, 50 and 100 μM. The parasites were kept for 4 days and monitored every 24 h to evaluate their viability and motor activity comparing with the positive control praziquantel. The cell viability of isolated flavones as determined by XTT assays in V79 cells. Results: The flavones 3′,5-dimethoxy luteolin-7-O-β-glucopyranoside, 5-methoxy luteolin and 3′,5-dimethoxy luteolin were isolated from V. divergens. Flavone 5-methoxy luteolin caused the death of 25% of male and female adult S. mansoni worms in 24 h at 100 μM and also reduced their motor activity. Flavones 3′,5-dimethoxy luteolin-7-O-β-glucopyranoside and 3′,5-dimethoxy luteolin were able to slightly reduce the motor activity to 25% within 24 h at 25 μg/mL and 12.5 μg/mL, respectively, but only in male worms. The results were compared with the flavone luteolin. For XTT assay in V79 cells the IC50 values were 1468.4 ± 10.5 μM, 5946.6 ± 25,1 μM, > 7960.8 μM and 270.6 ±9.3 μM for compounds 3′,5-dimethoxy luteolin-7-O-β-glucopyranoside, 5-methoxy luteolin, 3′,5-dimethoxy luteolin and luteolin, respectively. Conclusion: To the best of our knowledge, flavones 5-methoxy luteolin and 3′,5-dimethoxy luteolin are reported for the first time as constituents of V. divergens and the Vochysiaceae family.
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巴西潘塔纳尔河流域洪水适应物种——桃蚜5-甲氧基化黄酮体外抗血吸虫活性和细胞毒性研究
背景:沃琪亚(Vochysia divergens)原产于亚马逊盆地,被认为是巴西潘塔纳尔河的入侵物种。本研究对发散叶乙醇提取物及其分离化合物进行了体外抗曼氏血吸虫作用的化学研究和评价。方法:样品浓度分别为12.5、25、50、100 μM。饲养4 d,每24 h监测一次,与阳性对照吡喹酮比较,评价寄生虫的活力和运动活性。XTT法测定分离的黄酮类化合物在V79细胞中的细胞活力。结果:分离得到3′,5-二甲氧基木犀草素-7- o -β-葡萄糖苷、5-甲氧基木犀草素和3′,5-二甲氧基木犀草素。黄酮类5-甲氧基木犀草素在100 μM下24 h内可致25%的雄性和雌性曼氏线虫死亡,并降低其运动活性。黄酮3′,5-二甲氧基木犀草素-7- o -β-葡萄糖苷和3′,5-二甲氧基木犀草素分别在25 μg/mL和12.5 μg/mL浓度下能在24 h内将运动活性略微降低25%,但仅在雄性蠕虫中有效。结果与黄酮类木犀草素进行了比较。XTT法检测V79细胞中3′,5-二甲氧基木犀草素-7- o -β-葡萄糖苷、5-甲氧基木犀草素、3′,5-二甲氧基木犀草素和木犀草素的IC50值分别为1468.4±10.5 μM、5946.6±25 μM、1 μM、> 7960.8 μM和270.6±9.3 μM。结论:据我们所知,5-甲氧基木犀草素和3,5 -二甲氧基木犀草素为首次报道的植物属。
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