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钝瓣密花藤嫩枝中的细胞毒性和抗疟生物碱

Cytotoxic and Antimalarial Alkaloids from the Twigs of Dasymaschalon obtusipetalum.

作者信息

Jaidee Atchara, Promchai Thanika, Trisuwan Kongkiat, Laphookhieo Surat, Rattanajak Roonglawan, Kamchonwongpaisan Sumalee, Pyne Stephen G, Ritthiwigrom Thunwadee

出版信息

Nat Prod Commun. 2015 Jul;10(7):1175-7.

PMID:26411003
Abstract

One new p-quinonoid aporphine alkaloid, obtusipetadione (1), and eleven known compounds (2-12) were isolated from the acetone extract of the twigs of Dasymaschalon obtusipetalum. Their structures were elucidated by spectroscopic methods. The cytotoxic and antimalarial activities of the isolated compounds were evaluated. Compound 1 showed significant in vitro antiplasmodial activity against the P. falciparum strains TM4 and K1 (multidrug resistant strain) with IC50 values of 2.46 ± 0.12 and 1.38 ± 0.99 μg/mL, respectively with no cytotoxicity. Compound 9 had more modest antiplasmodial activity, but significant cytotoxicity.

摘要

从钝叶暗罗嫩枝的丙酮提取物中分离出一种新的对醌型阿朴菲生物碱——钝叶暗罗二酮(1)和11种已知化合物(2 - 12)。通过光谱方法阐明了它们的结构。对分离得到的化合物进行了细胞毒性和抗疟活性评估。化合物1对恶性疟原虫菌株TM4和K1(多药耐药菌株)显示出显著的体外抗疟活性,IC50值分别为2.46±0.12和1.38±0.99μg/mL,且无细胞毒性。化合物9的抗疟活性较弱,但具有显著的细胞毒性。

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