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Novel inhibitors of mitochondrial respiratory chain: endoperoxides from the marine tunicate Stolonica socialis.

Abstract：

:The Mediterranean tunicate Stolonica socialis contains a new class of powerful cytotoxic acetogenins, generically named stolonoxides. In this paper, which also details the isolation and chemical characterization of a minor component (3a) of the tunicate extract, we report the potent inhibitory activity (IC(50) < 1 microM) of stolonoxides (1a and 3a) on mitochondrial electron transfer. The compounds affect specifically the functionality of complex II (succinate:ubiquinone oxidoreductase) and complex III (ubiquinol:cytochrome C oxidoreductase) in mammalian cells, thereby causing a rapid collapse of the whole energetic metabolism. This result, which differs from the properties of similar known products (e.g., 6), reflects the molecular features of stolonoxides.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Fontana A,Cimino G,Gavagnin M,González MC,Estornell E

doi

10.1021/jm0011373

keywords:

subject

Has Abstract

pub_date

2001-07-05 00:00:00

pages

2362-5

issue

14

eissn

0022-2623

issn

1520-4804

pii

jm0011373

journal_volume

44

pub_type

杂志文章

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