Correlation between antitumor activity of berberine and the inhibition of Wnt/?-catenin signal pathway / 中国药理学通报

ABSTRACT

Aim To investigate the relationship between the antitumor activity of berberine and the inhibition of Wnt/?-catenin signaling pathway. Methods The antitumor activities of berberine and total alkaloids of Coptis were assessed for their ability to inhibit the proliferation and to induce apopotosis of human colon cancer lines. A well-established Tcf-4 responsive reporter was introduced into human colon cancer lines to test whether berberine and total alkaloids inhibited the ?-catenin/Tcf4 activity in these cancer cells.Results The proliferation of HCT116 and SW480 cells was inhibited substantially within the concentration ranges of 5 to 40 mg?L~(1) of berberine. 72 hours after treament both HCT116 and SW480 cells underwent apparent apopotosis as demonstrated by Hoechst 33258 staining. Total alkaloids of Coptis had similar effects to berberine when comparable concentrations of it with berberine were used.Berberine effectively and specifically inhibited the Tcf4 reporter activity, but not the positive control reporter at the same experimental conditions. Conclusion Our findings suggest that berberine may be mainly responsible for the antitumor activity of total alkaloids of Coptis and this effect may be mediated at least in part by its inhibitory effect on the Wnt/?-catenin signaling pathway, which is aberrantly activated in many types of human cancer.