Drimane sesquiterpene esters produced by Aspergillus insuetus BF-1613 as inhibitors of sterol O-acyltransferase.

Autor: Nur EAA; Department of Microbial Chemistry, Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.; Medicinal Research Laboratories, School of Pharmacy, Kitasato University, Tokyo, Japan.; Department of Microbial Chemistry, School of Pharmacy, Kitasato University, Tokyo, Japan., Kobayashi K; Department of Microbial Chemistry, Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.; Medicinal Research Laboratories, School of Pharmacy, Kitasato University, Tokyo, Japan.; Department of Microbial Chemistry, School of Pharmacy, Kitasato University, Tokyo, Japan., Tejima R; Department of Microbial Chemistry, Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan., Katada Y; Department of Microbial Chemistry, School of Pharmacy, Kitasato University, Tokyo, Japan., Tomoda H; Department of Microbial Chemistry, Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.; Medicinal Research Laboratories, School of Pharmacy, Kitasato University, Tokyo, Japan.; Department of Microbial Chemistry, School of Pharmacy, Kitasato University, Tokyo, Japan., Ohshiro T; Department of Microbial Chemistry, Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan. ohshirot@pharm.kitasato-u.ac.jp.; Medicinal Research Laboratories, School of Pharmacy, Kitasato University, Tokyo, Japan. ohshirot@pharm.kitasato-u.ac.jp.; Department of Microbial Chemistry, School of Pharmacy, Kitasato University, Tokyo, Japan. ohshirot@pharm.kitasato-u.ac.jp.
Jazyk: angličtina
Zdroj: The Journal of antibiotics [J Antibiot (Tokyo)] 2024 Dec; Vol. 77 (12), pp. 837-841. Date of Electronic Publication: 2024 Oct 10.
DOI: 10.1038/s41429-024-00774-8
Abstrakt: A new drimane sesquiterpene ester, designated insuetusolate (1), and four reported ones (2-5) were isolated from a culture broth of Aspergillus insuetus BF-1613. The chemical structure of 1 was elucidated by extensive spectroscopic analyses, including MS and NMR. Compound 1 has a drimane-type sesquiterpene core with a 2'E,4'E,6'E-octatrienoate side chain. All these drimane sesquiterpene esters inhibited both sterol O-acyl transferase 1 (SOAT1) and 2 (SOAT2), but exhibited slightly potent inhibition against SOAT1 than SOAT2 with selectivity index (SI) [log (IC 50 for SOAT1/ IC 50 for SOAT2)] values ranging from -0.24 to -0.94.
Competing Interests: Compliance with ethical standards. Conflict of interest: The authors declare no competing interests.
(© 2024. The Author(s), under exclusive licence to the Japan Antibiotics Research Association.)
Databáze: MEDLINE
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