Some embodiments of the invention provide a polyhydroxybenzo pyrone compound, pharmaceutically acceptable salts or prodrugs, and a pharmaceutical composition containing the compound. The compound, the salts or the prodrugs and the pharmaceutical composition can be used for regulating functions of novel estrogen acceptor ER-[alpha]36, and preventing and/or treating ER-[alpha]36 receptor-mediated tumor diseases, such as breast cancer, leukemia, liver cancer, etc.