摘要
Berberine(BBR)is an alkaloid from plants like Coptis chinensis and is for many years an OTC drug in China for bacterial-caused diarrhea.We have identified BBR to be an effective drug in treating hyperlipidemia as well as hyperglycemia.Clinical studies showed that oral administration of BBR caused significant reduction of blood cholesterol,triglyceride as well as glucose in patients with hyperlipidemia and T2D,with no obvious side-effect.Mechanism studies have identified several molecular mechanisms involving in the mode of action of BBR.The cholesterol-lowering effect was associated with the extracellular-signalregulated kinase(ERK)mediated LDLR mRNA up-regulation;the glucose-lowering effect mainly resulted from the protein kinase D mediated InsR expression and the activation of AMPK.The observed reduction of triglyceride by BBR might reflect its synergistic effect on both sugar and lipid metabolism.The interaction between gut microbiota and BBR explained the molecular mechanism of BBR′s intestinal absorption.BBR concentrated in liver after oral administration with a level many times more than that in blood.At least three CYP450 subtypes were responsible for BBR phase-Ⅰ metabolism.Structure-activity relationship of BBR was analyzed,and the clinical advantage of BBR was demonstrated.We consider BBR a new medicine for metabolic disorders.
Berberine(BBR)is an alkaloid from plants like Coptis chinensis and is for many years an OTC drug in China for bacterial-caused diarrhea.We have identified BBR to be an effective drug in treating hyperlipidemia as well as hyperglycemia.Clinical studies showed that oral administration of BBR caused significant reduction of blood cholesterol,triglyceride as well as glucose in patients with hyperlipidemia and T2D,with no obvious side-effect.Mechanism studies have identified several molecular mechanisms involving in the mode of action of BBR.The cholesterol-lowering effect was associated with the extracellular-signalregulated kinase(ERK)mediated LDLR mRNA up-regulation;the glucose-lowering effect mainly resulted from the protein kinase D mediated InsR expression and the activation of AMPK.The observed reduction of triglyceride by BBR might reflect its synergistic effect on both sugar and lipid metabolism.The interaction between gut microbiota and BBR explained the molecular mechanism of BBR′s intestinal absorption.BBR concentrated in liver after oral administration with a level many times more than that in blood.At least three CYP450 subtypes were responsible for BBR phase-Ⅰ metabolism.Structure-activity relationship of BBR was analyzed,and the clinical advantage of BBR was demonstrated.We consider BBR a new medicine for metabolic disorders.
出处
《中国药理学与毒理学杂志》
CAS
CSCD
北大核心
2015年第S1期6-6,共1页
Chinese Journal of Pharmacology and Toxicology
