Abstract
Chemotherapy drugs have limited efficacy in breast cancer due to multidrug resistance generated by cancer cells against anticancer drugs. In this study, we developed a novel derivative, 2, 3, 5, 4‘-tetrahydroxystilbene (TG1) by modifying 2, 3, 5, 4‘-tetrahydroxystilbene-2-O-beta-D-glucoside (THSG). In-vivo zebrafish embryo tests revealed that TG1 showed low toxicity. The equitoxic combination of DOX or DTX with TG1 in MCF-7/Adr reduced the IC50 of DOX or DTX, and the combination index (CI) showed strong synergistic effects in the 1:3 molar ratio of DTX: TG1 and 1:5 molar ratio of DOX: TG1. Moreover, fluorescence images confirmed the cellular uptake of DOX when combined with TG1 in MCF-7/Adr. Western blotting analysis indicated downregulation of p-glycoprotein (P-gp) after MCF-7/Adr treated with TG1. In conclusion, the combined therapy of DTX or DOX and TG1 increases drug efficacy via suppressing the p-glycoprotein efflux pump. These results suggest that TG1 may have potential use for breast cancer patients, especially those with multidrug resistance.
Highlights
Breast cancer is one of the most common cancers in the world, and has the highest mortality rate among all cancers in women [1]
Many chemotherapy drugs are used for breast cancer treatment, including doxorubicin (DOX), paclitaxel, docetaxel (DTX) and others
Anti-tumor efficacy is often limited by the multidrug resistance (MDR), resulting in the failure of chemotherapy [7, 8]
Summary
Breast cancer is one of the most common cancers in the world, and has the highest mortality rate among all cancers in women [1]. Previous reports have shown that approximately 12.3% of women in the US will be diagnosed with breast cancer during their lifetime, and it was predicted that it will reach up to 22 million new cases worldwide in a decade [2,3,4]. Treating breast cancer efficiently is always an important issue for researchers. Chemotherapy and radiation therapy are the major treatments for breast cancer patients currently. Chemotherapy is useful for treating various stages of breast cancer, and is used preoperatively to shrink the tumor or postoperatively to eliminate residual tumor cells after surgical removal [5, 6]. Many chemotherapy drugs are used for breast cancer treatment, including doxorubicin (DOX), paclitaxel, docetaxel (DTX) and others. MDR has become a significant problem for breast cancer treatment
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