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卡比林胺,一种来自冲绳甲藻的新型环状亚胺。

Kabirimine, a New Cyclic Imine from an Okinawan Dinoflagellate.

机构信息

Graduate School of Engineering and Science, University of the Ryukyus, Senbaru 1, Nishihara, Okinawa 903-0213, Japan.

OP Bio Factory Co., Ltd., Okinawa Life Science Center 107, 5-8 Suzaki, Uruma, Okinawa 904-02234, Japan.

出版信息

Mar Drugs. 2019 Jun 13;17(6):353. doi: 10.3390/md17060353.

DOI:10.3390/md17060353
PMID:31200525
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6627061/
Abstract

On our quest for new bioactive molecules from marine sources, two cyclic imines (, ) were isolated from a dinoflagellate extract, inhibiting the growth of the respiratory syncytial virus (RSV). Compound was identified as a known molecule portimine, while was elucidated to be a new cyclic imine, named kabirimine. The absolute stereochemistry of was determined by crystallographic work and chiral derivatization, whereas the structure of was elucidated by means of spectroscopic analysis and computational study on all the possible isomers. Compound showed potent cytotoxicity (CC < 0.097 µM) against HEp2 cells, while exhibited moderate antiviral activity against RSV with IC = 4.20 µM (95% CI 3.31-5.33).

摘要

在我们从海洋来源中寻找新的生物活性分子的过程中,从一种甲藻提取物中分离出两种环亚胺(、),它们抑制呼吸道合胞病毒(RSV)的生长。化合物被鉴定为已知的分子波替霉素,而被阐明为一种新的环亚胺,命名为卡比林霉素。通过晶体学工作和手性衍生化确定了的绝对立体化学,而通过光谱分析和所有可能异构体的计算研究阐明了的结构。化合物对 HEp2 细胞表现出很强的细胞毒性(CC < 0.097 µM),而对 RSV 表现出中等的抗病毒活性,IC = 4.20 µM(95% CI 3.31-5.33)。

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