title: The antihypercholesterolemic effect of jatrorrhizine isolated from Rhizoma Coptidis.
abstract: Current work was conducted to evaluate the safety and antihypercholesterolemic activity of jatrorrhizine extracted from Rhizoma Coptidis (RC) and its potential mechanism on regulating cholesterol metabolism. It was found that the LD50 of jatrorrhizine in mice was more than 5,500 mg/kg and there were no influences on clinical signs, organ weight changes, urinalysis and hematological parameters, gross necropsy and histological alterations in jatrorrhizine-treated rats during the 3-month period, compared to the control group. Jatrorrhizine showed a strong lipid-lowering effect in a dose-dependent manner. Oral administration of 70.05 mg/kg of jatrorrhizine on Mesocricetus auratus (Syrian golden hamsters) exhibited significant decrease in TC, TG, and LDL-c levels by 20%, 43%, and 19%, respectively, and increase in HDL-c and total bile acids (TBA) content in feces (p<0.01), compared to high-fat and high-cholesterol (HFHC) group. Besides, jatrorrhizine dose-dependently slowed the rate of weight gain. The results of qRT-PCR, western blotting and ELISA revealed that jatrorrhizine significantly up-regulated the mRNA and protein expression of LDLR and CYP7A1, but exhibited no significant effect on mRNA and protein expression of HMGR and ASBT in hamsters. In conclusion, jatrorrhizine was a safe and potential antihypercholesterolemic agent from RC which could improve the utilization and excretion of cholesterol by up-regulating the mRNA and protein expression of LDLR and CYP7A1.
authors.affiliation: School of Life Sciences, Southwest University, Chongqing 400715, China.
authors.forename: Hao
authors.initials: H
authors.lastname: Wu
authors.affiliation: School of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China.
authors.forename: Kai
authors.initials: K
authors.lastname: He
authors.affiliation: School of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China.
authors.forename: YanZhi
authors.initials: Y
authors.lastname: Wang
authors.affiliation: School of Life Sciences, Southwest University, Chongqing 400715, China.
authors.forename: DongFang
authors.initials: D
authors.lastname: Xue
authors.affiliation: School of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China.
authors.forename: Na
authors.initials: N
authors.lastname: Ning
authors.affiliation: School of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China.
authors.forename: Zongyao
authors.initials: Z
authors.lastname: Zou
authors.affiliation: School of Life Sciences, Southwest University, Chongqing 400715, China. Electronic address: yexiaoli@swu.edu.cn.
authors.forename: Xiaoli
authors.initials: X
authors.lastname: Ye
authors.affiliation: School of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China. Electronic address: Xuegangli@swu.edu.cn.
authors.forename: Xuegang
authors.initials: X
authors.lastname: Li
authors.affiliation: School of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China.
authors.forename: DeZhen
authors.initials: D
authors.lastname: Wang
authors.affiliation: School of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China.
authors.forename: Jie
authors.initials: J
authors.lastname: Pang
mesh_terms: D000818:Animals; D000924:Anticholesteremic Agents / Q000494:pharmacology*; D001599:Berberine / Q000031:analogs & derivatives* / Q000494:pharmacology; D001647:Bile Acids and Salts / Q000378:metabolism; D002784:Cholesterol / Q000097:blood / Q000378:metabolism*; D002790:Cholesterol 7-alpha-Hydroxylase / Q000378:metabolism; D000089042:Coptis chinensis; D004305:Dose-Response Relationship, Drug; D004365:Drugs, Chinese Herbal / Q000494:pharmacology*; D005260:Female; D008297:Male; D008647:Mesocricetus; D051379:Mice; D018517:Plant Roots / Q000737:chemistry; D029626:Ranunculaceae / Q000737:chemistry; D017207:Rats, Sprague-Dawley; D011973:Receptors, LDL / Q000378:metabolism; D018675:Toxicity Tests; D014280:Triglycerides / Q000097:blood
chemical_list: D000924:Anticholesteremic Agents; D001647:Bile Acids and Salts; D004365:Drugs, Chinese Herbal; D011973:Receptors, LDL; D014280:Triglycerides; C055785:jatrorrhizine; D001599:Berberine; D002784:Cholesterol; C107393:Coptidis rhizoma extract; D002790:Cholesterol 7-alpha-Hydroxylase
keywords: Antihypercholesterolemia; CYP7A1; Jatrorrhizine; LDLR; Rhizoma Coptidis