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 (IC50 < 1 íM) 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.
Novel Inhibitors of Mitochondrial Respiratory Chain: Endoperoxides from the Marine Tunicate Stolonica socialis / Fontana, A; Cimino, G.; Gavagnin, M.; Gonzalez, M. C.; Estornell, E.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 44:(2001), pp. 2362-2365. [10.1021/jm0011373]
Novel Inhibitors of Mitochondrial Respiratory Chain: Endoperoxides from the Marine Tunicate Stolonica socialis
Fontana A;
2001
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 (IC50 < 1 íM) 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.File | Dimensione | Formato | |
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