抗HIV活性を有する伝統薬物の研究

概要

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In attempts to discover anti-HIV agents from natural sources, various traditional medicine extracts were tested for their inhibitory effects on HIV-1 proliferation and its protease. An extract of the seeds of Croton tiglium showed potent inhibitory effects on the proliferation of HIV-1. The active principle was determined to be phorbol esters. Several derivatives of phorbol ester were evaluated for inhibition of proliferation as well as activation of protein kinase C (PKC). Of these compounds, 12-O-acetylphorbol 13-decanoate (6) showed the most potent inhibition of proliferation without activating PKC. Some triterpenes from the stems of Cynomorium songaricum and the woody part of Xan- thoceras sorbifolia showed inhibitory activity against HIV-1 protease. Various derivatives of oleanolic acid were synthe- sized and evaluated for their inhibitory activity against HIV-1 protease. Their inhibitory mechanism was also investigated.
公益社団法人日本薬学会の論文
2004-08-01