Inhibitory effects of ursolic acid derivatives from Cynomorium songaricum, and related triterpenes on human immunodeficiency viral protease

From the stems of Cynomorium songaricum Rupr. (Cynomoriaceae), ursolic acid and its hydrogen malonate were isolated as inhibitory substances against human immunodeficiency virus (HIV‐1) protease. Their 50% inhibitory concentrations (IC50) were 8 μM and 6 μM, respectively. Of various dicarboxylic aci...

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Veröffentlicht in:	PTR. Phytotherapy research 1998, Vol.12 (S1), p.S138-S142
Hauptverfasser:	Ma, Chaomei, Nakamura, Norio, Miyashiro, Hirotsugu, Hattori, Masao, Shimotohno, Kunitada
Format:	Artikel
Sprache:	eng
Schlagworte:	betulinic acid hydrogen glutarate Biological and medical sciences Cynomorium songaricum General pharmacology HIV-protease inhibitors Human immunodeficiency virus 1 Medical sciences oleanolic acid hydrogen glutarate Pharmacognosy. Homeopathy. Health food Pharmacology. Drug treatments ursolic acid hydrogen glutarate
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Zusammenfassung:	From the stems of Cynomorium songaricum Rupr. (Cynomoriaceae), ursolic acid and its hydrogen malonate were isolated as inhibitory substances against human immunodeficiency virus (HIV‐1) protease. Their 50% inhibitory concentrations (IC50) were 8 μM and 6 μM, respectively. Of various dicarboxylic acid hemiesters of related triterpenes synthesized, the inhibitory activities tended to increase in the order of oxalic, malonyl, succinyl and glutaryl hemiesters of triterpenes such as ursolic acid, oleanolic acid and betulinic acid. The most potent inhibition was observed for the glutaryl hemiesters with IC50 of 4 μM. © 1998 John Wiley & Sons, Ltd.
ISSN:	0951-418X 1099-1573
DOI:	10.1002/(SICI)1099-1573(1998)12:1+3.0.CO;2-5