Coptidis Rhizoma: a comprehensive review of its traditional uses, botany, phytochemistry, pharmacology and toxicology

Wang, Jin; Wang, Lin; Lou, Guan-Hua; Zeng, Hai-Rong; Hu, Ju; Huang, Qin-Wan; Peng, Wei; Yang, Xiang-Bo

Hyperlipidemia, characterized by increased levels of blood lipids, has been implicated as a contributing factor to the development of cardiovascular diseases. The main mechanism of resisting hyperlipidemia is related to inhibiting lipogenesis and promoting the use, conversion and excretion of lipid (Iii et al. 2014 ). Alkaloids derived from CR, including berberine, coptisine, palmatine, epiberberine and jatrorrhizine, appeared to prevent body weight gain, reduce serum levels of total cholesterol (TC), triglyceride (TG) and low-density lipoprotein-cholesterol (LDL-c) and increase high-density lipoprotein-cholesterol (HDL-c) and promoted the excretion of total bile acids (TBA) in faeces (He et al. 2016; Yang W et al. 2016 ). The effect of berberine is mainly related to upregulating the LDL receptor (LDLR) and Cytochrome P450 7A1 (CYP7A1), while downregulating 3hydroxy-3-methyl-glutaryl-coenzyme A reductase (HMGCR) ). In addition, palmatine and epibeberine, which could also be beneficial to treat hyperlipidaemia and downregulate apical sodium dependent bile acid transporter (ASBT) He et al. 2017) . The sterol regulatory element-binding proteins (SREBPs) are transcription factors that regulate cholesterol by binding to the promoters of genes such as those encoding LDLR and HMG-CoA synthase. Interestingly, administration of coptisine, berberine and palmatine could activate SREBP2 . Besides these main alkaloids of CR, some minor alkaloids, such as berbamine, could also exert effects on hypercholesterolemic zebrafish by upregulating cholesterol transport and bile acid synthesis .