两色金鸡菊在人肝微粒体的体外代谢研究
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摘要
目的考察两色金鸡菊在人肝微粒体的体外代谢。方法将肝微粒体空白对照、两色金鸡菊醇提物乙醇溶液、灭活肝微粒体加两色金鸡菊醇提物及肝微粒体加两色金鸡菊醇提物进行体外共孵育,采用高效液相色谱法测定,通过对比色谱峰,阐明两色金鸡菊在肝微粒体的体外代谢规律。结果两色金鸡菊醇提物在人肝微粒体药物代谢酶作用下,各成分含量均降低,其中4种物质被代谢而未被检出,分别为黄酮奥卡宁(Flavanokanin)、3,4′,5,6,7-pentahydroxyflavanone、橙酮金鸡菊苷(Maritimein)、马里苷(Marein)、奥卡宁(Okanin)。结论两色金鸡菊醇提物在人肝微粒体药物代谢酶作用下可较快地代谢消除。
Objective To examine the two color coreopsis main ingredients in human liver microsomal degradation.Methods The liver microsomes control,two-color ethanol extract of chrysanthemum,inactivated liver microsomes and ethanol extract of two-color chrysanthemum and liver microsomes plus twocolor Chrysanthemum alcohol extract were incubated in vitro.High performance liquid chromatography(HPLC)was used to determine the metabolites of Chrysanthemum indicum in liver microsomes by comparing the chromatographic peaks.Results The two colors coreopsis alcohol extract in human liver microsomes under the action of drug metabolic enzymes,each component content was reduced.Four kinds of material metabolisms(Flavanokanin,3,4′,5,6-pentahydroxyflavanone,Maritimein,Marein,Okanin)can not be checked out.Conclusion The two colors coreopsis alcohol extract in human liver microsomal under the action of drug metabolism enzymes can be rapidly eliminated.
Objective To examine the two color coreopsis main ingredients in human liver microsomal degradation.Methods The liver microsomes control,two-color ethanol extract of chrysanthemum,inactivated liver microsomes and ethanol extract of two-color chrysanthemum and liver microsomes plus twocolor Chrysanthemum alcohol extract were incubated in vitro.High performance liquid chromatography(HPLC)was used to determine the metabolites of Chrysanthemum indicum in liver microsomes by comparing the chromatographic peaks.Results The two colors coreopsis alcohol extract in human liver microsomes under the action of drug metabolic enzymes,each component content was reduced.Four kinds of material metabolisms(Flavanokanin,3,4′,5,6-pentahydroxyflavanone,Maritimein,Marein,Okanin)can not be checked out.Conclusion The two colors coreopsis alcohol extract in human liver microsomal under the action of drug metabolism enzymes can be rapidly eliminated.
引文
[1]张振清.我国药物代谢与药代动力学学科发展与展望[J].中国药理学与毒理学杂志,2015,29(5):752-754.
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[8]刘松灿,张亮,裘福荣,等.9种常用含丹参中成药对人肝微粒体CYP3A的体外抑制作用[J].中成药,2013,35(8):1776
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[2]刘妍妍,程雨晴,谭桢,等.药物代谢细胞色素酶催化活性检测新技术进展[J].化学研究,2015,26(6):551-560.
[3]叶娜,罗红丽,李容,等.丹参注射液对大鼠肝微粒体CYP450亚型酶体外抑制作用[J].中成药,2015,37(5):948-953.
[4]李维亮,辛华雯,苏明威.体外探讨五味子乙素对大鼠肝微粒体悦再孕猿粤的影响及其作用机制[J].中国药理学通报,2010,26(12):1616-1621.
[5]周建财,高署,鲁晓蓉,等.CPUHY002对人肝微粒体CYP450酶体外抑制作用研究[J].蚌埠医学院学报,2014,39(4):421-425.
[6]Yi W,Cao R,Wen H,et a1.Bioorg synthesis and biological evaluation of helicid analogues as mushroom tyrosinase inhibitors[J].Med Chem Lett,2008,18(24):6490-6493.
[7]秦梦楠,刘蕊,刘高峰,等.灯盏花素注射液对大鼠体外肝微粒体细胞色素P450酶活性的影响[J].中国药师,2012,15(2):147-150.
[8]刘松灿,张亮,裘福荣,等.9种常用含丹参中成药对人肝微粒体CYP3A的体外抑制作用[J].中成药,2013,35(8):1776
[9]徐勤,丁黎,刘文英,等.苯环喹溴铵在大鼠肝微粒体中的代谢转化研究[J].中国药房,2010,21(41):3872-3874.