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来自巴西红厚壳树叶的HIV-1抑制化合物。

HIV-1 inhibitory compounds from Calophyllum brasiliense leaves.

作者信息

Huerta-Reyes Maira, Basualdo Maria Del Carmen, Abe Fumiko, Jimenez-Estrada Manuel, Soler Carmen, Reyes-Chilpa Ricardo

机构信息

Department of Natural Products, Institute of Chemistry, National University of Mexico, Ciudad Universitaria, 04510, Mexico D. F., Mexico.

出版信息

Biol Pharm Bull. 2004 Sep;27(9):1471-5. doi: 10.1248/bpb.27.1471.

DOI:10.1248/bpb.27.1471
PMID:15340243
Abstract

The hexane, acetone and methanol extracts of Calophyllum brasiliense leaves were fractionated following a three bioassay guide: high HIV-1 RT inhibition, low cytotoxicity on MT2 cells and high inhibition of HIV-1 IIIb/LAV replication. This led to the isolation of three anti HIV-1 dipyranocoumarins: calanolides A and B and soulattrolide. In contrast, other isolated compounds such as apetalic acid, isoapetalic acid, a structural isomer of isoapetalic acid, friedelin, canophyllol and amentoflavone were devoid of HIV-1 RT inhibitory activity. Calanolide C was also obtained as a natural product and showed moderate inhibitory properties.

摘要

按照三项生物测定指标对巴西红厚壳树叶的己烷、丙酮和甲醇提取物进行分级分离:高HIV-1逆转录酶抑制活性、对MT2细胞低细胞毒性以及对HIV-1 IIIb/LAV复制的高抑制活性。由此分离出三种抗HIV-1二吡喃香豆素:红厚壳内酯A和B以及苏劳内酯。相比之下,其他分离出的化合物,如无花瓣酸、异无花瓣酸、异无花瓣酸的结构异构体、木栓酮、卡诺酚和穗花杉双黄酮,均无HIV-1逆转录酶抑制活性。红厚壳内酯C也作为一种天然产物获得,且显示出中等抑制特性。

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