In vitro cytotoxicity of the protoberberine-type alkaloids

  • J Nat Prod. 2001 Jul;64(7):896-8. doi: 10.1021/np000554f.
K Iwasa  1 ,  M Moriyasu ,  T Yamori ,  T Turuo ,  D U Lee ,  W Wiegrebe
Affiliations
  • 1. Kobe Pharmaceutical University, 4-19-1 Motoyamakita, Higashinada-ku, Kobe 658-8558, Japan. [email protected]
PMID: 11473418 DOI: 10.1021/np000554f
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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