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The Safety and Anti‐Hypercholesterolemic Effect of Coptisine in Syrian Golden Hamsters
Author(s) -
He Kai,
Ye Xiaoli,
Wu Hao,
Wang YanZhi,
Zou Zongyao,
Ning Na,
Hu Yinran,
Chen Biao,
Fang Xuedong,
Li Xuegang
Publication year - 2015
Publication title -
lipids
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.601
H-Index - 120
eISSN - 1558-9307
pISSN - 0024-4201
DOI - 10.1007/s11745-014-3983-7
Subject(s) - coptisine , clinical chemistry , medicine , lipidology , cholesterol , endocrinology , gemfibrozil , cholesterol 7 alpha hydroxylase , ldl receptor , chemistry , pharmacology , lipoprotein , biology , berberine , palmatine
Current work was conducted to evaluate the cholesterol‐lowering effect of coptisine extracted from Rhizoma coptidis in Syrian golden hamsters. The safety results indicated that coptisine was a safe and low‐toxic compound. Coptisine showed a beneficial effect in the abnormal serum lipid levels induced by a high‐fat and high‐cholesterol diet (HFHC): at a concentration of 70.05 mg/kg, coptisine significantly led to a decrease in total cholesterol, triglycerides, and low‐density lipoprotein cholesterol (LDL‐c) levels by 26.70, 15.38, and 22.22 %, respectively, and high‐density lipoprotein cholesterol (HDL‐c) was increased by 41.74 % in serum of hamsters ( p < 0.01). In addition, total bile acid (TBA) levels in feces of hamsters were elevated after coptisine administration. Further investigation has suggested that the mRNA and protein expression of 3‐hydroxy‐3‐methyl‐glutaryl‐CoA reductase (HMGCR) in the liver of hamsters was down‐regulated by high‐dosage coptisine treatment ( p < 0.05); mRNA and protein expression of low‐density lipoprotein receptor (LDLR) and cholesterol 7α‐hydroxylase (CYP7A1) were dramatically up‐regulated by coptisine administration. The apical sodium‐dependent bile salt transporter expression was down‐regulated in the coptisine‐treated animals, but showed no significant differences from the HFHC groups. Taken together, our results demonstrate that a high dosage of coptisine could inhibit cholesterol synthesis via suppressing the HMGCR expression and promoting the use and excretion of cholesterol via up‐regulating LDLR and CYP7A1 expression. These findings suggest a critical role for coptisine in anti‐ hypercholesterolemia, and thus it needs to be considered as a potential natural cholesterol lowering agent.