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. 2001 Jul;64(7):896-8.
doi: 10.1021/np000554f.

In vitro cytotoxicity of the protoberberine-type alkaloids

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In vitro cytotoxicity of the protoberberine-type alkaloids

K Iwasa et al. J Nat Prod. 2001 Jul.

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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