中国临床药理学杂志
中國臨床藥理學雜誌
중국림상약이학잡지
THE CHINESE JOURNAL OF CLINICAL PHARMACOLOGY
2009年
4期
322-325
,共4页
关小彬%叶玲%夏笔军%刘中秋
關小彬%葉玲%夏筆軍%劉中鞦
관소빈%협령%하필군%류중추
黄芩素%微粒体%代谢
黃芩素%微粒體%代謝
황금소%미립체%대사
baicalein%microsomes%metabolism
目的 观察大鼠微粒体代谢酶对黄芩素(治疗呼吸道感染中药)代谢作用的影响.方法 用体外微粒体药物代谢酶孵育法;用HPLC法测定黄芩素及其葡萄糖醛酸化代谢物的含量,在不同孵育时间和不同浓度下,观察大鼠肝肠不同微粒体对黄芩素葡萄糖醛酸化代谢产物生成速率的影响.结果 5种不同微粒体药物代谢酶对黄芩素均有代谢作用,且随孵育时间延长,代谢作用也相应增加,呈较好的时间和剂量依赖关系.在5种微粒体中,十二指肠微粒体代谢作用最强;而肝代谢作用最弱.结论 黄芩素主要代谢部位是肠道.
目的 觀察大鼠微粒體代謝酶對黃芩素(治療呼吸道感染中藥)代謝作用的影響.方法 用體外微粒體藥物代謝酶孵育法;用HPLC法測定黃芩素及其葡萄糖醛痠化代謝物的含量,在不同孵育時間和不同濃度下,觀察大鼠肝腸不同微粒體對黃芩素葡萄糖醛痠化代謝產物生成速率的影響.結果 5種不同微粒體藥物代謝酶對黃芩素均有代謝作用,且隨孵育時間延長,代謝作用也相應增加,呈較好的時間和劑量依賴關繫.在5種微粒體中,十二指腸微粒體代謝作用最彊;而肝代謝作用最弱.結論 黃芩素主要代謝部位是腸道.
목적 관찰대서미립체대사매대황금소(치료호흡도감염중약)대사작용적영향.방법 용체외미립체약물대사매부육법;용HPLC법측정황금소급기포도당철산화대사물적함량,재불동부육시간화불동농도하,관찰대서간장불동미립체대황금소포도당철산화대사산물생성속솔적영향.결과 5충불동미립체약물대사매대황금소균유대사작용,차수부육시간연장,대사작용야상응증가,정교호적시간화제량의뢰관계.재5충미립체중,십이지장미립체대사작용최강;이간대사작용최약.결론 황금소주요대사부위시장도.
Objective To investigate the different roles of metabolism of baicalein in rat,especial liver and intestine. Methods The enzyme re-actions by microsome incubations were employed. The content of baica-lein and baicalein- glucuronide were determined by HPLC. The glucu-ronidation rates of baicalein at different time points and at various con-centrations were measured by using 5 UGT microsomes. Results Five different microsomes are important common microsomes for glucuronida-tion of baicalein with the manner of time and concentration-dependences.Furthermore, the results also showed that jejunum microsome is the main microsome for metabolizing baicalein, and the colon microsome would be a weakest microsome for the contribution of baicalein metabolism. Con-clusion Different microsomes are responsible for the metabolism of ba-icalein in different organs/regions of the digestive system. The glucuroni-dation of baicalein in the intestine contributes significantly to that of ba-icalein in the liver.