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新型 Terpendole 同系物,胆固醇酰基转移酶抑制剂,由 BF-0440 产生。

New Terpendole Congeners, Inhibitors of Sterol -Acyltransferase, Produced by BF-0440.

机构信息

Department of Microbial Chemistry, Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo 108-8641, Japan.

Medicinal Research Laboratories, School of Pharmacy, Kitasato University, Tokyo 108-8641, Japan.

出版信息

Molecules. 2020 Jul 6;25(13):3079. doi: 10.3390/molecules25133079.

Abstract

New terpendoles N-P () were isolated along with 8 structurally related known compounds including terpendoles and voluhemins from a culture broth of the fungus BF-0440. The structures of were elucidated using various spectroscopic experiments including 1D- and 2D-NMR. All compounds contained a common indole-diterpene backbone. Compounds and had 7 and 6 consecutive ring systems with an indole ring, respectively, whereas had a unique indolinone plus 4 consecutive ring system. Compounds and inhibited both sterol -acyltransferase 1 and 2 isozymes, but lost the inhibitory activity. Structure-activity relationships of fungal indole-diterpene compounds are discussed.

摘要

新型萜品 N-P() 与 8 种结构相关的已知化合物(包括萜品和 voluhemins)一起从真菌 BF-0440 的发酵液中分离出来。通过包括 1D- 和 2D-NMR 在内的各种光谱实验阐明了的结构。所有化合物都含有一个共同的吲哚二萜骨架。化合物和分别具有 7 个和 6 个连续的环系和一个吲哚环,而具有独特的吲哚啉酮和 4 个连续的环系。化合物和抑制甾醇酰基转移酶 1 和 2 同工酶,但失去了抑制活性。讨论了真菌吲哚二萜化合物的结构-活性关系。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6cab/7411735/4a434b1efee0/molecules-25-03079-g001.jpg

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