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来自圆锥花单室茱萸的抗疟异黄酮和紫檀烷。

Antiplasmodial Isoflavanes and Pterocarpans from Apoplanesia paniculata.

作者信息

Su Qingxi, Krai Priscilla, Goetz Michael, Cassera Maria B, Kingston David G I

机构信息

Department of Chemistry and Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, Virginia, United States.

Department of Biochemistry and Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, Virginia, United States.

出版信息

Planta Med. 2015 Aug;81(12-13):1128-32. doi: 10.1055/s-0035-1546036. Epub 2015 May 27.

Abstract

Bioassay-guided fractionation of an EtOH extract of the roots of the plant Apoplanesia paniculata (Fabaceae) led to the isolation of the three known compounds amorphaquinone (1), pendulone (2), and melilotocarpan C (3), and the two new pterocarpans 4 and 5. Compounds 1 and 2 exhibited good antiplasmodial activity with IC50 values of 5.7 ± 1.5 and 7.0 ± 0.8 µM, respectively. Compound 3 exhibited weak antiplasmodial activity (41.8 ± 5.2 µM), while compounds 4 and 5 were inactive. Compound 6 was synthesized to confirm the structure of 5, and it showed enhanced antiplasmodial activity (15.8 ± 1.4 µM) compared to its analogues 3-5.

摘要

对豆科植物圆锥花翅子树(Apoplanesia paniculata)根的乙醇提取物进行生物测定导向的分级分离,得到了三种已知化合物紫穗槐醌(1)、垂铃儿茶素(2)和草木犀香豆素C(3),以及两种新的紫檀素4和5。化合物1和2表现出良好的抗疟活性,IC50值分别为5.7±1.5和7.0±0.8μM。化合物3表现出较弱的抗疟活性(41.8±5.2μM),而化合物4和5无活性。合成了化合物6以确认5的结构,与类似物3 - 5相比,它表现出增强的抗疟活性(15.8±1.4μM)。

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