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二头截短孢菌素A - C：源自深海真菌二头截短孢FS110的新型二酮哌嗪类化合物

Dichotocejpins A-C: New Diketopiperazines from a Deep-Sea-Derived Fungus Dichotomomyces cejpii FS110.

作者信息

Fan Zhen, Sun Zhang-Hua, Liu Zhong, Chen Yu-Chan, Liu Hong-Xin, Li Hao-Hua, Zhang Wei-Min

机构信息

State Key Laboratory of Applied Microbiology Southern China, Guangdong Provincial Key Laboratory of Microbial Culture Collection and Application, Guangdong Open Laboratory of Applied Microbiology, Guangdong Institute of Microbiology, Guangzhou 510070, China.

Guangdong Provincial Key Laboratory of Bioengineering Medicine, National Engineering Research Center of Genetic Medicine, College of Life Science and Technology, Jinan University, Guangzhou 510632, China.

出版信息

Mar Drugs. 2016 Sep 9;14(9):164. doi: 10.3390/md14090164.

DOI:10.3390/md14090164
PMID:27618072
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5039535/
Abstract

Three new diketopiperazines, dichotocejpins A-C (1-3), together with eight known analogues (4-11), were isolated from the culture of the deep-sea sediment derived fungus Dichotomomyces cejpii FS110. Their structures, including absolute configurations, were elucidated by a combination of HRESIMS, NMR, X-ray crystallography, and ECD calculations. Compounds 4-6, 10-11 showed significant cytotoxic activities against MCF-7, NCI-H460, HepG-2, and SF-268 tumor cell lines. Compound 1 exhibited excellent inhibitory activity against α-glucosidase with an IC50 of 138 μM.

摘要

从深海沉积物来源的真菌 Dichotomomyces cejpii FS110 的培养物中分离出三种新的二酮哌嗪，即 dichotocejpins A-C（1-3），以及八个已知类似物（4-11）。通过高分辨电喷雾电离质谱（HRESIMS）、核磁共振（NMR）、X 射线晶体学和电子圆二色光谱（ECD）计算相结合的方法阐明了它们的结构，包括绝对构型。化合物 4-6、10-11 对 MCF-7、NCI-H460、HepG-2 和 SF-268 肿瘤细胞系表现出显著的细胞毒性活性。化合物 1 对α-葡萄糖苷酶表现出优异的抑制活性，IC50 为 138 μM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd08/5039535/dbc50aecbdcc/marinedrugs-14-00164-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd08/5039535/36449555dd1f/marinedrugs-14-00164-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd08/5039535/b0d551d9dd3e/marinedrugs-14-00164-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd08/5039535/1d297a271f15/marinedrugs-14-00164-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd08/5039535/dbc50aecbdcc/marinedrugs-14-00164-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd08/5039535/36449555dd1f/marinedrugs-14-00164-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd08/5039535/b0d551d9dd3e/marinedrugs-14-00164-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd08/5039535/1d297a271f15/marinedrugs-14-00164-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd08/5039535/dbc50aecbdcc/marinedrugs-14-00164-g004.jpg

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