ANTITUMOR ACTIVITY OF BERBERRUBINE DERIVATIVES

  • 1 January 1976
    • journal article
    • research article
    • Vol. 67  (2) , 321-325
Abstract
The antitumor activity of berberine, berberrubine and their derivatives against mouse ascites sarcoma 180 was determined by the total packed cell volume method. Berberine and tetrahydroberberine derivatives had no antitumor activity, but berberrubine (9-demethylberberine) and the ester derivatives of berberrubine had strong antitumor activity. ED90 of berberrubine, its acetate and benzoate, were 15, 23 and 44 mg/kg, respectively. The therapeutic indices (LD10/ED90 by the present method) of these compounds were as follows: Berberrubine hydrochloride, 6.7 .apprx. 9.4; 9-acetyl-9-demethylberberine (9-acetylberberrubine) chloride, 7.6 s 8.7; 9-benzoyl-9-demethylberberine (9-benzoylberberrubine) chloride, 3.4 .apprx. 4.9.

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