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海洋海绵多溴二苯醚是适应葡萄糖饥饿的癌细胞的选择性生长抑制剂,可抑制线粒体复合物II。

Marine spongean polybrominated diphenyl ethers, selective growth inhibitors against the cancer cells adapted to glucose starvation, inhibits mitochondrial complex II.

作者信息

Arai Masayoshi, Shin Dayoung, Kamiya Kentaro, Ishida Ryosuke, Setiawan Andi, Kotoku Naoyuki, Kobayashi Motomasa

机构信息

Graduate School of Pharmaceutical Sciences, Osaka University, Yamada-oka 1-6, Suita, Osaka, 565-0871, Japan.

Department of Chemistry, Faculty of Science, Lampung University, Jl. Prof. Dr. Sumantri Brodjonegoro No. 1, Bandar Lampung, 35145, Indonesia.

出版信息

J Nat Med. 2017 Jan;71(1):44-49. doi: 10.1007/s11418-016-1025-x. Epub 2016 Jul 23.

Abstract

In the course of search for selective growth inhibitors against the cancer cells adapted to nutrient starvation, two polybrominated diphenyl ethers, 3,4,5-tribromo-2-(2',4'-dibromophenoxy)-phenol (1) and 3,5-dibromo-2-(2',4'-dibromophenoxy)-phenol (2) were isolated from an Indonesian marine sponge of Dysidea sp. Compounds 1 and 2 showed the anti-proliferative activity against PANC-1 cells under glucose-starved conditions with IC values of 2.1 and 3.8 µM, respectively, whereas no growth inhibition was observed up to 30 µM in the general culture conditions. The further mechanistic analysis indicated that compound 1 might act mainly by inhibiting complex II in the mitochondrial electron transport chain.

摘要

在寻找针对适应营养饥饿的癌细胞的选择性生长抑制剂的过程中,从印度尼西亚海绵属的一种海绵Dysidea sp.中分离出两种多溴二苯醚,即3,4,5-三溴-2-(2',4'-二溴苯氧基)-苯酚(1)和3,5-二溴-2-(2',4'-二溴苯氧基)-苯酚(2)。化合物1和2在葡萄糖饥饿条件下对PANC-1细胞显示出抗增殖活性,IC值分别为2.1和3.8 μM,而在一般培养条件下,浓度高达30 μM时未观察到生长抑制。进一步的机制分析表明,化合物1可能主要通过抑制线粒体电子传递链中的复合物II起作用。

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