Abstract
Purpose : To investigate the lipid-lowering activity of two metabolites of galangin, namely, galangin-3-O-β-D-glucuronic acid (GG-1) and galangin-7-O-β-D-glucuronic acid (GG-2). Methods : Female Sprague-Dawley rats were orally administered with galangin. The two metabolites of galangin were isolated from urine sample and purified using Sephadex LH-20 and semi-preparative high performance liquid chromatography (HPLC). The structures of the metabolites were identified by analyzing spectroscopic data. Hypolipidemic activity was evaluated in HepG2 cells. The down- or upregulation of lipogenic genes was detected using real-time quantitative polymerase chain reaction (qPCR). Results : Both metabolites of galangin showed hypolipidemic activity. These activities are closely associated with the down-regulation of lipogenic genes such as SREBP-1a, SREBP-1c, and SREBP-2 transcription factors, and the downstream genes such as FAS, ACC, and HMGR were revealed by realtime qPCR data. Conclusion : The results show that both metabolites possess better lipid-lowering activities than galangin. These hypolipidemic activities are closely associated with inhibiting key genes or proteins that regulated the biosynthesis of both cholesterol and triglycerides. Keywords : Galangin, Galangin-3-O-β-D-glucuronic acid, Galangin-7-O-β- D-glucuronic acid, Hypolipidemic, Lipogenic genes, Metabolites
Highlights
Obesity is becoming a serious threat to human beings [1]
Further analysis of nuclear magnetic resonance (NMR) data showed that a glucuronic acid group existed in compound 1
Comparing the 13C-NMR data of compound 1 with galangin revealed the downfield shifts of C-2 and C-4 were +10.6 and 1.8, respectively, whereas the upfield shift of C-3 (-1.6 ppm) indicating the glucuronic acid group was located at C-3
Summary
Obesity is becoming a serious threat to human beings [1]. More accumulation of lipids in liver is a key cause for insulin resistance [2]. Decreasing lipid deposition in liver through inhibition of lipogenesis or stimulation of lipolysis is an effective way for the prevention and treatment of obesity and diabetes [3,4] Natural products such as cordycepin [5], resveratrol [6], and berberine [7] have showed ability in suppressing lipogenesis and accumulation of fat, and are considered to be the potential candidates in developing new therapeutic agents. A natural flavonoid obtained from Alpinia officinarum, has been found to possess various biological activities [8,9] This compound showed a significant decrease in serum lipids, liver weight, peroxidation of lipids, and accumulation of hepatic triglycerides, which suggested that galangin has the potential for controlling obesity [10].
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