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Anti-metastasis effects of a major green tea polyphenol - (-)-epigallocatechin-3-gallate (EGCG) has been reported, but the fully acetylated form of EGCG, peracetylated EGCG (AcEGCG), a postulated prodrug form of EGCG with improved bioavailability, remains unexplored. In human breast carcinoma, upregulation of matrix metalloproteinases (MMPs) and fatty acid synthase (FAS) involved in tumor metastasis are associated with tumor cell aggressiveness and a poor prognosis. In this study, we have investigated the anti-metastatic potential of AcEGCG in breast cancer cells. Herein we showed that AcEGCG was more effective than EGCG in preventing the epidermal growth factor (EGF)-induced cell motility, transformation and epithelial to mesenchymal transition (EMT)-mesenchymal to epithelial transition (MET) in both estrogen receptor positive and negative breast cancer cells. We found that AcEGCG was more potent than EGCG in reducing EGF-induced MMP-2 and MMP-9 activities in MCF-7 and MDA-MB-231 cells. In addition, AcEGCG also inhibited the expression of FAS by EGF in MCF-7 cells. In conclusion, AcEGCG exerted a more inhibitory effect on the intracellular lipid accumulation than that of EGCG. Taken together, our results suggest for the first time that molecular targets of MMPs and FAS by AcEGCG may be a potential strategy for breast cancer therapy.

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