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

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Lipids

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 μM. Among these cycloartenol ferulate (IC50=2.2 μM), 24-methylenecycloartanol ferulate (1.9 μM), lupenone (2.1 μM), betulin diacetate (1.4 μM), and karounidiol 29-benzoate (2.2 μM) 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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Abbreviations

AIDS:

acquired immunodeficiency syndrome

DMSO:

dimethylsulfoxide

DTT:

dithiothreitol

HIV:

human immunodeficiency virus

methyl-dTTP:

methyl thymidine 5′-triphosphate

RT:

reverse transcriptase

TPA:

12-O-tetradecanoylphorbol-13-acetate

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Authors and Affiliations

  1. College of Bioresource Sciences, Nihon University, 154-8513, Tokyo, Japan

    Jun Ogihara, Jun Kato & Kunio Oishi

  2. College of Pharmacy, Nihon University, 274-8555, Chiba, Japan

    Ken Yasukawa & Sakae Yamanouchi

  3. College of Science and Technology, Nihon University, 1-8 Kanda Surugadai, Chiyoda-ku, 101-8308, Tokyo, Japan

    Toshihiro Akihisa & Motohiko Ukiya

Authors
  1. Toshihiro Akihisa
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  2. Jun Ogihara
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  3. Jun Kato
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  4. Ken Yasukawa
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  5. Motohiko Ukiya
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  6. Sakae Yamanouchi
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  7. Kunio Oishi
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Correspondence to Toshihiro Akihisa.

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Akihisa, T., Ogihara, J., Kato, J. et al. Inhibitory effects of triterpenoids and sterols on human immunodeficiency virus-1 reverse transcriptase. Lipids 36, 507–512 (2001). https://doi.org/10.1007/s11745-001-0750-4

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  • DOI: https://doi.org/10.1007/s11745-001-0750-4

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