The Enzyme Kinetics of CYP2D6 to Six Flavonoids of Smilax glabra In Vitro
XU Jia-ming1, XIE Jing2, LIU Gui-ming2, HUANG Xiao-wei1*, SHI Yu-rui2, CHEN Rong-da2, LI Li2
1. School of Pharmaceutical Science, Changchun University of Chinese Medicine, Changchun 130032, China; 2. College of Chemistry, Changchun Normal University, Changchun 130032, China
Abstract：OBJECTIVE To investigate the enzyme kinetics of CYP2D6 to six flavonoids of Smilax glabrain vitro. METHODS The effects of incubation time and CYP2D6 enzyme concentration on the metabolism of six flavonoids including epicatechin, neoastilbin, astilbin, isoastilbin, engeletin and resveratrol from Smilax glabra were studied in vitro. RESULTS The RESULTS showed that the six flavonoids were eliminated linearly within 30-90 min, and the metabolic elimination rate increased with the increase of CYP2D6 enzyme concentration at 1.0-3.0 mg·mL-1. When epicatechin, neoastilbin, astilbin, isoastilbin, engeletin and resveratrol were used as substrates, the Km were 1.20, 2.14, 3.84, 2.84, 1.86 and 1.30 μmol·L-1, respectively, indicating that epicatechin was the most suitable substrate for CYP2D6; the maximum reaction rates were 0.01, 0.02, 0.03, 0.03, 0.02 and 0.01 μmol·L-1·min-1; and the metabolic clearance rates were 0.008 3, 0.009 3, 0.007 8, 0.010 5, 0.010 7, 0.007 6 min-1, respectively, and the RESULTS showed that CYP2D6 had the greatest scavenging ability to engeletin. CONCLUSION This study provides experimental and theoretical basis for further research on the interaction between six flavonoids and CYP2D6.
许佳明, 谢静, 刘桂明, 黄晓巍, 史玉蕊, 陈荣达, 李丽. 土茯苓6种黄酮类成分在CYP2D6中的体外酶促动力学研究[J]. 中国药学杂志, 2021, 56(6): 472-477.
XU Jia-ming, XIE Jing, LIU Gui-ming, HUANG Xiao-wei, SHI Yu-rui, CHEN Rong-da, LI Li. The Enzyme Kinetics of CYP2D6 to Six Flavonoids of Smilax glabra In Vitro. Chinese Pharmaceutical Journal, 2021, 56(6): 472-477.
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2021, Vol. 56 
