胰曲霉 BF-1613 产生的作为甾醇 O-酰基转移酶抑制剂的 Drimane 倍半萜酯。

IF 2.1 4区医学 Q3 BIOTECHNOLOGY & APPLIED MICROBIOLOGY

Journal of Antibiotics Pub Date : 2024-10-10 DOI:10.1038/s41429-024-00774-8

Elyza Aiman Azizah Nur, Keisuke Kobayashi, Rio Tejima, Yosuke Katada, Hiroshi Tomoda, Taichi Ohshiro

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引用次数: 0

摘要

从 insuetusolate 曲霉 BF-1613 的培养液中分离出了一种新的 drimane 倍半萜酯，命名为 insuetusolate（1），以及四种已报道的倍半萜酯（2-5）。通过大量光谱分析（包括质谱和核磁共振），阐明了 1 的化学结构。化合物 1 的核心是一个具有 2'E、4'E、6'E-辛三烯酸酯侧链的 drimane 型倍半萜。所有这些 drimane 倍半萜酯对甾醇 O-酰基转移酶 1（SOAT1）和 2（SOAT2）都有抑制作用，但对 SOAT1 的抑制作用略强于 SOAT2，选择性指数（SI）[对 SOAT1 的 IC50 对数/对 SOAT2 的 IC50 对数]值介于-0.24 至-0.94 之间。

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

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

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 (IC50 for SOAT1/ IC50 for SOAT2)] values ranging from −0.24 to −0.94.

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来源期刊

Journal of Antibiotics 医学-免疫学

CiteScore

6.60

自引率

3.00%

发文量

审稿时长

1 months

期刊介绍： The Journal of Antibiotics seeks to promote research on antibiotics and related types of biologically active substances and publishes Articles, Review Articles, Brief Communication, Correspondence and other specially commissioned reports. The Journal of Antibiotics accepts papers on biochemical, chemical, microbiological and pharmacological studies. However, studies regarding human therapy do not fall under the journal’s scope. Contributions regarding recently discovered antibiotics and biologically active microbial products are particularly encouraged. Topics of particular interest within the journal''s scope include, but are not limited to, those listed below: Discovery of new antibiotics and related types of biologically active substances Production, isolation, characterization, structural elucidation, chemical synthesis and derivatization, biological activities, mechanisms of action, and structure-activity relationships of antibiotics and related types of biologically active substances Biosynthesis, bioconversion, taxonomy and genetic studies on producing microorganisms, as well as improvement of production of antibiotics and related types of biologically active substances Novel physical, chemical, biochemical, microbiological or pharmacological methods for detection, assay, determination, structural elucidation and evaluation of antibiotics and related types of biologically active substances Newly found properties, mechanisms of action and resistance-development of antibiotics and related types of biologically active substances.