12 - O - 乙酰佛波醇 - 13 - 癸酸酯能有效抑制1型人类免疫缺陷病毒（HIV - 1）的细胞病变效应，且不激活蛋白激酶C。

12-O-acetylphorbol-13-decanoate potently inhibits cytopathic effects of human immunodeficiency virus type 1 (HIV-1), without activation of protein kinase C.

作者信息

el-Mekkawy S, Meselhy M R, Nakamura N, Hattori M, Kawahata T, Otake T

机构信息

Institute of Natural Medicine, Toyama Medical and Pharmaceutical University, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1999 Sep;47(9):1346-7. doi: 10.1248/cpb.47.1346.

DOI:10.1248/cpb.47.1346

PMID:10517016

Abstract

Through bioactivity-guided fractionation, eight phorbol diesters, including five new ones (1-5), were isolated from the seeds of Croton tiglium collected in Egypt. 12-O-Acetylphorbol-13-decanoate (6) and 12-O-decanoylphorbol-13-(2-methylbutyrate) (4) potently inhibited the HIV-1-induced cytopathic effect on MT-4 cells (IC100 values of 7.6 ng/ml and 7.81 micrograms/ml, and CC0 values of 62.5 micrograms/ml and 31.3 micrograms/ml, respectively) without activating protein kinase C.

摘要

通过生物活性导向的分级分离，从埃及采集的巴豆种子中分离出8种佛波酯，包括5种新的佛波酯（1-5）。12-O-乙酰佛波醇-13-癸酸酯（6）和12-O-癸酰佛波醇-13-（2-甲基丁酸酯）（4）可有效抑制HIV-1对MT-4细胞诱导的细胞病变效应（IC100值分别为7.6 ng/ml和7.81μg/ml，CC0值分别为62.5μg/ml和31.3μg/ml），且不激活蛋白激酶C。