Antihyperglycemia and Antihyperlipidemia Effect of Protoberberine Alkaloids From Rhizoma Coptidis in HepG2 Cell and Diabetic KK‐Ay Mice

Abstract

Preclinical Research Rhizoma Coptidis (RC), the root of Coptis chinensis Franch, a species in the genus Coptis (family Ranunculaceae), has been commonly prescribed for the treatment of diabetes in Chinese traditional herbal medicine applications. The present study is focused on the assessment of the antihyperglycemia and antidiabetic hyperlipidemia effect of five protoberberine alkaloids, berberine (BBR), coptisine (COP), palmatine (PAL), epiberberine (EPI), and jatrorrhizine (JAT), separated from R. Coptidis in hepatocellular carcinoma HepG2 cells and diabetic KK-Ay mice. Protoberberine alkaloids are effective in modulating hyperglycemia and hyperlipidemia. After adding BBR and COP to culture medium, glucose consumption of HepG2 cells was increased. In KK-Ay mice assays, suppressed fasting blood glucose level and ameliorated glucose tolerance were observed after BBR/COP administration. After treated with berberine and coptisine, in the same dose of 5 µg/mL, the glucose consumption of HepG2 cells were promoted and, respectively, reached 96.1% and 17.6%. Body weight, food consumption, water intake, and urinary output of KK-Ay mice were reduced after treated with EPI. Serum total cholesterol and triglyceride of mice were decreased after treated with palmatine and jatrorrhizine. Serum high-density lipoprotein cholesterol of mice was increased after palmatine, jatrorrhizine, and berberine administrated. Moreover, hepatomegaly was attenuated in JTR-treated mice. Suggested that these protoberberine alkaloids from R. Coptidis have potential curative effect for diabetes. Drug Dev Res 77 : 163-170, 2016. © 2016 Wiley Periodicals, Inc.

Biologically active isoquinoline alkaloids covering 2014–2018

“…Moreover, diminished hepatomegaly was found in jatrorrhizine-treated mice. 226 In a subsequent study, a combination of the five alkaloids showed synergistic cholesterol-lowering in HepG2 cells and hypercholesterolemic hamsters, which was greater than that of the single alkaloids. 227 Activation of AMPK activation and alteration of neutral lipid metabolism may explain the hypoglycemic effect of berberine in differentiated cardiomyocytes.…”

“…56 In 2016, berberine (161), coptisine (165), palmatine (166), epiberberine (163), and jatrorrhizine (162) were evaluated for antihyperglycemic, antidyslipidemic and antidiabetic hyperlipidemic effects in HepG2 cells and diabetic KK-Ay mice. 226 All five alkaloids effectively modulated hyperglycemia and hyperlipidemia. Berberine and coptisine promoted glucose consumption in vitro as well as suppressed fasting blood glucose level and improved glucose tolerance in vivo.…”

Metabolic profile of Rhizoma coptidis in human plasma determined using ultra‐high‐performance liquid chromatography coupled with high‐resolution mass spectrometry

“…Rhizoma coptidis , commonly known as Huang Lian in China, has been one of the most important medicinal plants used for the treatment of various diseases in traditional Chinese medicine for more than 2000 years. In recent years, numerous scientific studies have demonstrated that Rhizoma coptidis and its main active constituents display a variety of activities including anti‐bacterial, anti‐cancer, anti‐hyperglycemic, anti‐hyperlipidemic, anti‐diabetic, anti‐obesity, anti‐inflammatory, radio‐protective and hepato‐protective effects . Moreover, Rhizoma coptidis and its isolated alkaloids have been reported to have cardio‐protective and neuro‐protective properties.…”

Rhizoma Coptidis: A Potential Cardiovascular Protective Agent

“…Type 2 diabetes is strongly associated with significant morbidity and mortality due to cardiovascular complications. This is in part due to the impaired utilization of carbohydrate that is part of the metabolic profile of diabetes, which results in accelerated lipolysis and thus hyperlipidemia or dyslipidemia (Vijayaraghavan, 2010 ; Ma et al, 2016 ). RC has been shown to have the ability to attenuate the impaired lipid metabolism associated with diabetes.…”

“…The anti-hyperlipidemic effect of the alkaloids isolated from RC have been further tested on diabetic mice. Palmatine and jatrorrhizine were shown to decrease the concentrations of serum TC and triglyceride; while elevated HDL cholesterol levels were found in diabetic mice administered with palmatine, jatrorrhizine and berberine (Ma et al, 2016 ). In another study, there were decreased serum TC, triglyceride, LDL cholesterol and increased HDL cholesterol in diabetic rats treated with berberine (Tang et al, 2006 ), showing the ability of RC to attenuate the impaired lipid metabolism in diabetic conditions.…”