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

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• 作者：Masayoshi Arai ; Dayoung Shin ; Kentaro Kamiya…
• 关键词：Polybrominated diphenyl ether ; Marine sponge ; Cancer ; Glucose starvation ; Mitochondrial electron transport chain
• 刊名：Journal of Natural Medicines
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：71
• 期：1
• 页码：44-49
• 全文大小：
• 刊物主题：Pharmacology/Toxicology; Plant Sciences; Complementary & Alternative Medicine; Medicinal Chemistry; Pharmacy;
• 出版者：Springer Japan
• ISSN：1861-0293
• 卷排序：71

文摘

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 IC₅₀ 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.