Breast cancer the most common cancer among women in the United States and is the second leading cause of cancer-related death in women. The majority of diagnosed breast cancers are estrogen receptor (ER) positive providing a favorable target for endocrine therapy. Currently tamoxifen (TAM) is administered as first-line endocrine therapy and its development represents a major advancement in the treatment of ER positive breast carcinoma (1, 3-4). Despite the advances in chemotherapeutic agents for breast and prostate cancer, an acquired resistance to endocrine therapy still remains a major obstacle in the treatment of breast and prostate cancer. Studies have shown that phytochemical, Berberine, a benzyl-tetra isoquinoline alkaloid extracted from plants of the Berberidaceae family, has been extensively used for many centuries, in the traditional Chinese and Native American medicine. Several evidences suggest that berberine possesses therapeutic uses, including anti-tumoral, antidiabetic and anticancer activity. We hypothesizethat structural modifications of berberine may be lead to effective anticancer agents used to overcome endocrine resistance in both breast and prostate cancer. About 20 analogues have been synthesized and the preliminary data shows that berberine analogs could effectively inhibit the growth of breast cancer cell lines to about 50% at a micromolar range.

Design, synthesis, and biological evaluation of berberine and its analogs as novel drugs for breast cancer

247th National Meeting (2014)

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