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Berberine (BBR) is a natural compound with molecular weight of 371.8.It has been used in China in clinic for diarrhea for over 60 years with good safety record.Our recent work found that BBR effectively up-regulates the expression of the Low-Density-Lipoprotein Receptor (LDLR) as well as insulin receptor (InsR) through activation of ERK and PKC pathway,respectively.It renders the compound a new application in clinic for lipid and sugar related disorders.This presentation covers its molecular mechanism, structure-activity analysis,clinical application, as well as its significant advantage over statins in patients.