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首页> 外文期刊>Anti-infective agents >Antiplasmodial activity and some active compounds from Stachytarpheta cayennensis Vahl. (Verbenaceae) leaf fractions
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Antiplasmodial activity and some active compounds from Stachytarpheta cayennensis Vahl. (Verbenaceae) leaf fractions

机译：水飞蓟宾的抗血浆活性和一些活性化合物。 （马鞭草科）叶级分

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摘要

Background: New antimalarial drugs are required to fight resistant parasites and plantderived natural products are a robust source for identifying active lead compounds. Stachytarpheta cayennensis (Verbenaceae) is traditionally used in west and central Africa as malaria remedy. Objective: This study was undertaken to evaluate antiplasmodial activity of S. cayennensis leaf fractions and to isolate and identify some active constituents. Method: A dried, powdered batch of S. cayennensis leaf was extracted with hexane, dichloromethane and methanol. The methanol extract was partitioned with ethyl acetate and water. Solvent portions and ethyl acetate column fractions were investigated in early infection in mice, against chloroquine-sensitive (HB3) and chloroquine-resistant (FCM29) P. falciparum. Compounds I, II and III isolated from active fractions were identified based on their spectroscopic data and further evaluated for antioxidant and heme biomineralization inhibitory activity. Results: Column fractions 6-7, 10-11 significantly (P 0.01) reduced parasitaemia in vivo and in vitro (IC50 50 μg/ml). At a dose of 2.5 mg/kg, compounds I -III significantly (P 0.05) suppressed infection by 54.91 -88.95 %. Compound III also displayed strong antioxidant effect (EC50 = 0.05 mg/ml) comparable to equivalent concentrations of ascorbic acid (EC50 = 0.03 mg/ml), whereas compound I elicited stronger inhibitory effect (67.93%) on heme biomineralization than compound III (38.67%). The compounds were identified as apigenin (I), stigmasterol glucoside (II) and verbascoside (III). Conclusion: The findings showed that S. cayennensis leaves contain antiplasmodial-active compounds which show potential for further development.
机译：背景：需要新的抗疟药来对抗抗药性寄生虫，而来源于植物的天然产物是鉴定活性先导化合物的可靠来源。在非洲西部和中部，传统上使用非洲水草科（马鞭草科）作为疟疾的补救措施。目的：本研究旨在评估沙门氏菌叶级分的抗血浆活性，并分离和鉴定一些活性成分。方法：用己烷，二氯甲烷和甲醇萃取干燥的粉状沙门氏菌叶。甲醇萃取液用乙酸乙酯和水分配。研究了小鼠在早期感染中针对氯喹敏感性（HB3）和耐氯喹（FCM29）恶性疟原虫的溶剂部分和乙酸乙酯柱级分。从活性级分中分离出的化合物Ⅰ，Ⅱ和Ⅲ根据其光谱数据进行鉴定，并进一步评估其抗氧化剂和血红素生物矿化抑制活性。结果：色谱柱级分6-7、10-11在体内和体外均显着降低了寄生虫血症（IC50 <50μg/ ml）。在2.5mg / kg的剂量下，化合物I-III显着（P ＜0.05）抑制感染54.91-88.95％。与抗坏血酸当量浓度（EC50 = 0.03 mg / ml）相比，化合物III还显示出强大的抗氧化作用（EC50 = 0.05 mg / ml），而化合物I对血红素生物矿化的抑制作用强于化合物III（38.67（67.93％））。 ％）。该化合物被鉴定为芹菜素（I），豆甾醇甾醇糖苷（II）和马齿bas苷（III）。结论：研究结果表明，沙棘叶片含有抗疟原活性的化合物，具有进一步发展的潜力。

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