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首页> 外文期刊>Journal of Tropical Medicine >Andrographolide: A Novel Antimalarial Diterpene Lactone Compound from Andrographis paniculata and Its Interaction with Curcumin and Artesunate
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Andrographolide: A Novel Antimalarial Diterpene Lactone Compound from Andrographis paniculata and Its Interaction with Curcumin and Artesunate

机译:穿心莲内酯:穿心莲的新型抗疟疾二萜内酯化合物及其与姜黄素和青蒿琥酯的相互作用

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摘要

Andrographolide (AND), the diterpene lactone compound, was purified by HPLC from the methanolic fraction of the plant Andrographis paniculata. The compound was found to have potent antiplasmodial activity when tested in isolation and in combination with curcumin and artesunate against the erythrocytic stages of Plasmodium falciparum in vitro and Plasmodium berghei ANKA in vivo. IC50s for artesunate (AS), andrographolide (AND), and curcumin (CUR) were found to be 0.05, 9.1 and 17.4?μM, respectively. The compound (AND) was found synergistic with curcumin (CUR) and addictively interactive with artesunate (AS). In vivo, andrographolide-curcumin exhibited better antimalarial activity, not only by reducing parasitemia (29%), compared to the control (81%), but also by extending the life span by 2-3 folds. Being nontoxic to the in vivo system this agent can be used as template molecule for designing new derivatives with improved antimalarial properties.
机译:二萜内酯化合物穿心莲内酯(AND)是通过HPLC从植物穿心莲的甲醇级分中纯化的。当该化合物与姜黄素和青蒿琥酯组合使用时,在体外和体内对恶性疟原虫的红细胞生成阶段进行测试时,发现该化合物具有有效的抗疟原虫活性。青蒿琥酯(AS),穿心莲内酯(AND)和姜黄素(CUR)的IC50分别为0.05、9.1和17.4?M。发现该化合物(AND)与姜黄素(CUR)协同作用,并与青蒿琥酯(AS)上瘾地相互作用。在体内,穿心莲内酯-姜黄素表现出更好的抗疟疾活性,不仅与对照组(81%)相比,降低了寄生虫血症(29%),而且还使寿命延长了2-3倍。该试剂对体内系统无毒,可以用作模板分子,用于设计具有改善的抗疟疾特性的新衍生物。

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