Berberine, an alkaloid isolated from the plant Berberis aristata, has been found to inhibit significantly the carcinogenesis induced by 20-methylcholanthrene (200 microg/0.1 mL/mouse) or N-nitrosodiethylamine (NDEA; 0.02% NDEA in distilled water, 2.5 mL/animal by gavage, five days a week for 20 weeks) in a dose-dependent manner in small animals. Administration of berberine (0.5, 2.5 or 5.0 mg kg(-1)) could reduce significantly the incidence of tumour in animals after an injection of 20-methylcholanthrene and increased their life span compared with the control. When berberine (10, 25 or 50 mg kg(-1)) was administered simultaneously with NDEA, the markers of liver injury (liver weight, gamma-glutamyl transpeptidase activity and glutathione S-transferase level) were reduced significantly compared with animals treated with NDEA only, which resulted in all the values being elevated. A similar decrease was noted in the serum levels of lipid peroxide, bilirubin and glutamate pyruvate transaminase. Morphology of liver tissue and levels of marker enzymes indicated that berberine offered protection against chemical carcinogenesis.
The cytotoxicity and antitumour activity of the isoquinoline alkaloid berberine was studied in-vitro and in-vivo.Berberine was cytotoxic to L929 cells in culture (IC50 40 mg mL À1 ), and to mice when given as an acute (LD50 50 mg kg À1 , i.p) or chronic (LD50 15 mg kg À1 for 10 days, i.p) dose. At a non-toxic concentration berberine dose-dependently inhibited the tumours induced by Dalton's lymphoma ascites tumour cells in mice. Berberine was more active when given intraperitoneally than orally. The simultaneous administration of berberine potentiated the therapeutic effects of radiation, cyclophosphomide and hyperthermia with a decrease in volume of solid tumours in mice.The results indicate the bene®cial use of berberine as an adjuvant response modi®er in cancer therapy.
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