Abstract

Resveratrol, as a broad-spectrum anticancer agent, has significant inhibitory effects on many tumor cells such as murine liver cancer, human liver cancer, gastric cancer, breast cancer, ovarian cancer and leukemia. In this study, resveratrol was used as an inhibitor of ABCG2 to influence the efflux cells of protoporphyrin IX (PpIX) by inhibiting BCRP/ABCG2, and to investigate the effect of resveratrol on enhancing phototherapy (PDT) of human glioma cells treated with 5-aminolevulinic acid (5-ALA).Firstly, four kinds of malignant glioma cells U87MG, U251, A172 and T98G were treated with 5-ALA (1 mmol/L) . Resveratrol at different concentrations (0.01~1.0μmol/L) as a modulator was incubated with glioma cells. The levels of PpIX, BCRP/ABCG2mRNA and ABCG2 protein in vivo and vitro and the effects of PDT in vitro were evaluated. The results showed that resveratrol decreased the expression of BCRP/ABCG2mRNA and thus decreased the expression of BCRP/ABCG2 protein on the cell membrane. Then, resveratrol at or above the concentration of 0.1μmol/L inhibited PpIX efflux in malignant brain glioma cells, and increased PpIX level in all cells with the increase of concentration. Resveratrol can not only inhibit the efflux of PpIX in malignant glioma cells, but also enhance the effect of PDT by increasing the content of PpIX in the cells.

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