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由黑曲霉BF-1613产生的Drimane倍半萜酯作为甾醇O-酰基转移酶的抑制剂

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

Nature 等信源发布 2024-10-10 12:15

可切换为仅中文


AbstractA 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.

摘要从Aspergillus insuetus BF-1613的培养液中分离出一种新的drimane倍半萜酯,命名为insuetusolate(1)和四个已报道的倍半萜酯(2-5)。通过广泛的光谱分析,包括MS和NMR,阐明了1的化学结构。化合物1具有具有2'E,4'E,6'E-辛三烯酸侧链的drimane型倍半萜核心。

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..

所有这些drimane倍半萜酯均抑制甾醇O-酰基转移酶1(SOAT1)和2(SOAT2),但对SOAT1的抑制作用略强于SOAT2,选择性指数(SI)[log(SOAT1的IC50/SOAT2的IC50)]值范围为-0.24至-0.94。。

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Download referencesAcknowledgementsWe are grateful to Noriko Sato, Dr. Kenichiro Nagai and Reiko Seki of Graduate School of Pharmaceutical Sciences, Kitasato University for the measurements of NMR and MS spectra and the late Prof. L.L. Rudel of Wake Forest University, Winston-Salem, NC, USA for kindly providing SOAT1-CHO and SOAT2-CHO cells.

下载参考文献致谢我们感谢北里大学药物科学研究生院的佐藤北子博士和关灵子博士测量NMR和MS光谱,以及美国北卡罗来纳州温斯顿塞勒姆威克森林大学已故教授L.L.鲁德尔(L.L.Rudel)提供SOAT1-CHO和SOAT2-CHO细胞。

This work was financially supported by JSPS KAKENHI Grant numbers 18KK0219 (Fund for the Promotion of Joint International Research (Fostering Joint International Research (B)) (HT), MEXT Scholarship (EAAN) and Kitasato University Research Grant for Young Researcher (EAAN).Author informationAuthors and AffiliationsDepartment of Microbial Chemistry, Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo, JapanElyza Aiman Azizah Nur, Keisuke Kobayashi, Rio Tejima, Hiroshi Tomoda & Taichi OhshiroMedicinal Research Laboratories, School of Pharmacy, Kitasato University, Tokyo, JapanElyza Aiman Azizah Nur, Keisuke Kobayashi, Hiroshi Tomoda & Taichi OhshiroDepartment of Microbial Chemistry, School of Pharmacy, Kitasato University, Tokyo, JapanElyza Aiman Azizah Nur, Keisuke Kobayashi, Yosuke Katada, Hiroshi Tomoda & Taichi OhshiroAuthorsElyza Aiman Azizah NurView author publicationsYou can also search for this author in.

这项工作得到了JSPS KAKENHI资助号18KK0219(促进联合国际研究基金(促进联合国际研究(B))(HT),MEXT奖学金(EAAN)和北里大学青年研究基金(EAAN)的资助。作者信息作者和附属机构东京北里大学药物科学研究生院微生物化学系,日本东京北里大学药学院微生物化学系,东京北里大学药学院微生物化学系,东京北里大学药学院Hiroshi Tomoda&Taichi OhshiroAuthorsElyza Aiman Azizah NurView作者出版物您也可以在中搜索这位作者。

PubMed Google ScholarKeisuke KobayashiView author publicationsYou can also search for this author in

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PubMed Google ScholarRio TejimaView author publicationsYou can also search for this author in

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

等人。由Aspergillus insuetus BF-1613产生的Drimane倍半萜酯作为甾醇O-酰基转移酶的抑制剂。。

J Antibiot (2024). https://doi.org/10.1038/s41429-024-00774-8Download citationReceived: 27 May 2024Revised: 28 August 2024Accepted: 10 September 2024Published: 10 October 2024DOI: https://doi.org/10.1038/s41429-024-00774-8Share this articleAnyone you share the following link with will be able to read this content:Get shareable linkSorry, a shareable link is not currently available for this article.Copy to clipboard.

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