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

✍ Scribed by Chaomei Ma; Norio Nakamura; Hirotsugu Miyashiro; Masao Hattori; Kunitada Shimotohno


Publisher
John Wiley and Sons
Year
1998
Tongue
English
Weight
104 KB
Volume
12
Category
Article
ISSN
0951-418X

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✦ Synopsis


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 (IC 50 ) were 8 mM and 6 mM, 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 IC 50 of 4 mM.