In vitro cytotoxicity of the protoberberine-type alkaloids
- PMID: 11473418
- DOI: 10.1021/np000554f
In vitro cytotoxicity of the protoberberine-type alkaloids
Abstract
In vitro cytotoxic activities of 24 quaternary protoberberine alkaloids related to berberine have been evaluated using a human cancer cell line panel coupled with a drug sensitivity database. Extending the alkyl chain at position 8 or 13 strongly influenced the cytotoxic activity, that is, relative lipophilicity as well as the size of the substituent affects cytotoxicity. The highest level of activity was observed in 8- or 13-hexyl-substituted derivatives of berberine. Structure-activity relationships are described.
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