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来自澳大利亚海绵指状希氏海绵的倍半萜类同系物作为动脉粥样硬化疾病的潜在药物先导物

Merosesquiterpene Congeners from the Australian Sponge Hyrtios digitatus as Potential Drug Leads for Atherosclerosis Disease.

作者信息

Wahab Huda A, Pham Ngoc B, Muhammad Tengku S Tengku, Hooper John N A, Quinn Ronald J

机构信息

Eskitis Institute for Drug Discovery, Griffith University, Brisbane 4111, Australia.

School of Fundamental Science, Universiti Malaysia Terengganu, Kuala Terengganu 21030, Malaysia.

出版信息

Mar Drugs. 2016 Dec 27;15(1):6. doi: 10.3390/md15010006.

Abstract

A study of the chemical constituents from the Australian Sponge has provided a perspective on the connection between the chemistry and biology of the puupehenones, a unique and unusual class of merosesquiterpenes. In this study, a new tetracyclic merosesquiterpene, 19-methoxy-9,15-ene-puupehenol () was isolated from the marine sponge along with the known 20-methoxy-9,15-ene-puupehenol (). Their structures were elucidated on the basis of spectroscopic data (¹H and C NMR) in combination with experimental electronic circular dichroism (ECD) data. Compounds and are active at 1.78 μM and 3.05 μM, respectively, on Scavenger Receptor-Class B Type 1 HepG2 (SR-B1 HepG2) stable cell lines, targeting atherosclerosis disease.

摘要

一项对澳大利亚海绵化学成分的研究,为独特且不寻常的半倍半萜类化合物——普佩海酮的化学与生物学之间的联系提供了一个视角。在这项研究中,从海洋海绵中分离出一种新的四环半倍半萜,19-甲氧基-9,15-烯-普佩海醇( )以及已知的20-甲氧基-9,15-烯-普佩海醇( )。它们的结构是根据光谱数据(¹H和¹³C NMR)并结合实验性电子圆二色光谱(ECD)数据确定的。化合物 和 分别在1.78 μM和3.05 μM时,对靶向动脉粥样硬化疾病的清道夫受体B类1型HepG2(SR-B1 HepG2)稳定细胞系具有活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba3c/5295226/a9c2fe7c5335/marinedrugs-15-00006-g001.jpg

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