[Inhibitory effects of some traditional medicines on proliferation of HIV-1 and its protease].
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 Xanthoceras sorbifolia showed inhibitory activity against HIV-1 protease. Various derivatives of oleanolic acid were synthesized and evaluated for their inhibitory activity against HIV-1 protease. Their inhibitory mechanism was also investigated.
Institute of Natural Medicine, Toyama Medical and Pharmaceutical University, Sugitani, Toyama, Japan. ikki@ms.toyama-mpu.ac.jp
Norio
N
Nakamura
D029802:Croton; D024882:Drug Resistance, Viral; D016333:HIV Protease / Q000378:metabolism*; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology; D010703:Phorbol Esters / Q000302:isolation & purification / Q000494:pharmacology*; D010936:Plant Extracts / Q000302:isolation & purification / Q000494:pharmacology*; D010946:Plants, Medicinal; D011480:Protease Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D029631:Sapindaceae; D012639:Seeds; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000302:isolation & purification / Q000494:pharmacology*
D010703:Phorbol Esters; D010936:Plant Extracts; D011480:Protease Inhibitors; D014315:Triterpenes; D016333:HIV Protease