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Life Sci. 2016 Apr 15;151:50-60. doi: 10.1016/j.lfs.2016.02.046. Epub 2016 Feb 11.

Synergetic cholesterol-lowering effects of main alkaloids from Rhizoma Coptidis in HepG2 cells and hypercholesterolemia hamsters.

Author information

1
Chongqing Engineering Research Centre for Sweet Potato, School of Life Sciences, Southwest University, Chongqing 400715, China.
2
Chongqing productivity promotion center for the modernization of Chinese traditional medicine, School of Pharmaceutical Sciences, Southwest University, Chongqing 400716, China.
3
Chongqing Engineering Research Centre for Sweet Potato, School of Life Sciences, Southwest University, Chongqing 400715, China; Chongqing Engineering Research Center for Pharmaceutical Process and Quality Control, Chongqing 400716, China. Electronic address: yexiaoli@swu.edu.cn.
4
Chongqing productivity promotion center for the modernization of Chinese traditional medicine, School of Pharmaceutical Sciences, Southwest University, Chongqing 400716, China; Chongqing Engineering Research Center for Pharmaceutical Process and Quality Control, Chongqing 400716, China. Electronic address: xuegangli@swu.edu.cn.

Abstract

AIMS:

Hyperlipidemia contributes to the progression of cardiovascular diseases. Main alkaloids from Rhizoma Coptidis including berberine (BBR), coptisine (COP), palmatine (PAL), epiberberine (EPI) and jatrorrhizine (JAT), improved dyslipidemia in hypercholesterolemic hamsters to a different degree. In this study, HepG2 cells and hypercholesterolemic hamsters were used to investigate the synergetic cholesterol-lowering efficacy of these five main alkaloids.

MAIN METHODS:

The cellular lipid and cholesterol accumulation and in HepG2 cells were evaluated by Oil Red O staining and HPLC analysis. LDL receptor, 3-Hydroxy-3-methylglutaryl CoA reductase (HMGCR) and cholesterol 7-alpha-hydroxylase (CYP7A1) that involving cholesterol metabolism in HepG2 cells were measured by qRT-PCR, western blot and immunofluorescence analysis. The serum profiles including total cholesterol (TC), triglyceride (TG), low-density lipoprotein cholesterol (LDL-c) and high-density lipoprotein cholesterol (HDL-c), as well as TC and total bile acids (TBA) of feces in hypercholesterolemic hamsters were also measured.

KEY FINDING:

As compared to single alkaloids, the combination of five main alkaloids (COM) reduced the lipid and cholesterol accumulation in HepG2 cells more effectively and performed an advantageous effect on controlling TC, TG, LDL-c and HDL-c in hypercholesterolemic hamsters. More effective reduction of TBA and TC levels in feces of hamsters were achieved after the administration of COM. These effects were derived from the up-regulation of LDL receptor and CYP7A1, as well as HMGCR downregulation.

SIGNIFICANCE:

Our results demonstrated that COM showed a synergetic cholesterol-lowering efficacy, which was better than single alkaloids and it might be considered as a potential therapy for hypercholesterolemia.

KEYWORDS:

CYP7A1; HMGCR; Hypercholesterolemia; LDL receptor; Rhizoma Coptidis; Synergetic effect

PMID:
26876917
DOI:
10.1016/j.lfs.2016.02.046
[Indexed for MEDLINE]

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