Inhibitory Effects of Triterpenoids and Sterols on Human Immunodeficiency Virus-1 Reverse Transcriptase

Overview

Journal Lipids

Specialty Biochemistry

Date 2001 Jul 4

PMID 11432464

Citations 18

Authors

T Akihisa

J Ogihara

J Kato

K Yasukawa

M Ukiya

S Yamanouchi

K Oishi

Affiliations

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Abstract

Fifty-five triterpenoids consisting of 19 tetracyclic, 32 pentacyclic, and 4 incompletely cyclized triterpenoids, and 2 sterols, mostly isolated from various plant and fungal materials, were examined for their inhibitory effects on a purified human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. Twenty triterpenoids and one sterol showed inhibitory effects with 50% inhibition concentration (IC50) values less than 5.0 microM. Among these cycloartenol ferulate (IC50 = 2.2 microM), 24-methylenecycloartanol ferulate (1.9 microM), lupenone (2.1 microM), betulin diacetate (1.4 microM), and karounidiol 29-benzoate (2.2 microM) inhibited most effectively. Some of the triterpenoids and sterols may be potential new lead compounds to find still more potent HIV-1 reverse transcriptase inhibitors.

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