Synergetic effect and structure-activity relationship of 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors from Crataegus pinnatifida Bge

Journal of Agricultural and Food Chemistry
Xiaoli YeXin Chen

Abstract

The 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR) inhibitors from hawthorn fruit ( Crataegus pinnatifida Bge.) were isolated and evaluated for their antihyperlipidemic effect induced by high-fat diet in mice. After being further purified with silica and polyamide column chromatography from the fractions (fractions A, F, H, and G) with a high inhibitory rate (IR) to HMGR, 24 chromatographic fractions were obtained, including 8 active fractions with a high IR to HMGR. However, the total inhibitory activity of 24 fractions was decreased by about 70%. From eight active fractions, four compounds were obtained by recrystallization and identified as quercetin (a), hyperoside (b), rutin (c), and chlorogenic acid (d), the contents of which in hawthorn EtOH extract were 0.16, 0.32, 1.45, and 0.95%, respectively. The IR values of compounds a-d to HMGR were 6.28, 9.64, 23.53, and 10.56% at the corresponding concentrations of 0.16, 0.32, 1.45, and 0.95 mg/mL, respectively. It was discovered that the IR of a mixture (2.85 mg/mL) matching the original percentage of compounds a-d in hawthorn EtOH extract was up to 79.5%, much higher than that of the single compound and the total IR of these four compounds (50.01%). The in vivo results...Continue Reading

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Citations

May 17, 2014·Evidence-based Complementary and Alternative Medicine : ECAM·Miao HuBrian Tomlinson
Apr 11, 2012·Journal of the Science of Food and Agriculture·Baoru Yang, Pengzhan Liu
Dec 12, 2012·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Tunde JurikovaRene Kizek
Jul 25, 2019·Natural Product Research·Alejandra Orona-OrtizAndrés Navarrete
Jul 1, 2016·Journal of Food and Drug Analysis·Mei-Yin ChienChao-Hsiang Chen
Dec 18, 2020·Journal of Asian Natural Products Research·Peng ZhaoShao-Jiang Song

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