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Inhibitory effects of triterpenoids and sterols on human immunodeficiency virus-1 reverse transcriptase.

Authors
  • Akihisa, T
  • Ogihara, J
  • Kato, J
  • Yasukawa, K
  • Ukiya, M
  • Yamanouchi, S
  • Oishi, K
Type
Published Article
Journal
Lipids
Publication Date
May 01, 2001
Volume
36
Issue
5
Pages
507–512
Identifiers
PMID: 11432464
Source
Medline
License
Unknown

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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