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Novel antiplasmodial agents from christia vespertilionis

机译:Christia vespertilionis的新型抗血浆药物

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The roots, leaves and stems of Christia vespertilionis were separately and successively extracted with methanol and aqueous-methanol (1:4, v/v) and were evaluated in vitro for their antiplasmodial potential against Plasmodium falciparum NF-54. The aqueous-methanolic stem (AS) extract was the most active (IC~(50) 7.5 μg/mL) followed by the methanolic leaf (ML) extract (IC~(50) 32.0 μg/mL). The in vivo antimalarial activity of the combined plant extract of C. vespertilionis was also assessed in P. berghei infected mice, which showed 87.8% suppression of parasitaemia as compared with complete suppression by chloroquine on day 8. Finally, detailed chemical investigation of C. vespertilionis resulted in the isolation and characterization of fifteen compounds (1-15), of which two (1 and 4) are being reported for the first time from nature. The novel compound 1 possesses potent antiplasmodial activity (IC~(50) = 9.0 μg/mL).
机译:分别用甲醇和甲醇水溶液(1:4,v / v)分别提取和连续提取Christia vespertilionis的根,叶和茎,并在体外评估其对恶性疟原虫NF-54的抗血浆活性。水-甲醇茎(AS)提取物的活性最高(IC〜(50)7.5μg/ mL),其次是甲醇叶(ML)提取物(IC〜(50)32.0μg/ mL)。还对伯氏疟原虫感染的小鼠评估了C. vespertilionis合并植物提取物的体内抗疟活性,与第8天用氯喹完全抑制相比,寄生虫抑制了87.8%。最后,对C.进行了详细的化学研究。 vespertilionis导致了15种化合物(1-15)的分离和表征,其中两种(1和4)是自然界首次报道。新化合物1具有有效的抗疟原虫活性(IC〜(50)= 9.0μg/ mL)。

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