中国药师
中國藥師
중국약사
CHINA PHARMACIST
2014年
10期
1613-1619
,共7页
舒舟%翟学佳%刘金梅%吕永宁
舒舟%翟學佳%劉金梅%呂永寧
서주%적학가%류금매%려영저
辣椒素%CYP450%探针药物%Cocktail
辣椒素%CYP450%探針藥物%Cocktail
랄초소%CYP450%탐침약물%Cocktail
Capsaicin%CYP450%Probedrug%Cocktail
目的：：采用cocktail 探针药物法研究辣椒素在体外对大鼠肝微粒体CYP 450四种亚型的影响。方法：分为试验组和对照组,试验组采用大鼠肝微粒体孵育体系、探针药物和系列浓度的辣椒素(对照组仅加入缓冲液)共同孵育20 min,反应终止后用HPLC方法检测代谢产物的生成量以代表酶的活性。采用Graphpad prism 5.0计算辣椒素对各亚型的IC50值。将辣椒素与大鼠肝微粒体分别预孵育0,5,10,15,20,30 min,计算不同预孵育时间下各亚型的相对活性百分比。结果：辣椒素对大鼠肝微粒体CYP1A2、CYP2C11、CYP2E1和CYP3A2的IC50值分别为36.21,17.19,51.64,18.86μmol·L-1。预孵育没有增强辣椒素对CYP450的抑制作用。结论：辣椒素在体外对大鼠肝微粒CYP1A2、CYP2C11、CYP2E1和CYP3A2具有抑制作用,且未呈现出预孵育时间依赖性。
目的：：採用cocktail 探針藥物法研究辣椒素在體外對大鼠肝微粒體CYP 450四種亞型的影響。方法：分為試驗組和對照組,試驗組採用大鼠肝微粒體孵育體繫、探針藥物和繫列濃度的辣椒素(對照組僅加入緩遲液)共同孵育20 min,反應終止後用HPLC方法檢測代謝產物的生成量以代錶酶的活性。採用Graphpad prism 5.0計算辣椒素對各亞型的IC50值。將辣椒素與大鼠肝微粒體分彆預孵育0,5,10,15,20,30 min,計算不同預孵育時間下各亞型的相對活性百分比。結果：辣椒素對大鼠肝微粒體CYP1A2、CYP2C11、CYP2E1和CYP3A2的IC50值分彆為36.21,17.19,51.64,18.86μmol·L-1。預孵育沒有增彊辣椒素對CYP450的抑製作用。結論：辣椒素在體外對大鼠肝微粒CYP1A2、CYP2C11、CYP2E1和CYP3A2具有抑製作用,且未呈現齣預孵育時間依賴性。
목적：：채용cocktail 탐침약물법연구랄초소재체외대대서간미립체CYP 450사충아형적영향。방법：분위시험조화대조조,시험조채용대서간미립체부육체계、탐침약물화계렬농도적랄초소(대조조부가입완충액)공동부육20 min,반응종지후용HPLC방법검측대사산물적생성량이대표매적활성。채용Graphpad prism 5.0계산랄초소대각아형적IC50치。장랄초소여대서간미립체분별예부육0,5,10,15,20,30 min,계산불동예부육시간하각아형적상대활성백분비。결과：랄초소대대서간미립체CYP1A2、CYP2C11、CYP2E1화CYP3A2적IC50치분별위36.21,17.19,51.64,18.86μmol·L-1。예부육몰유증강랄초소대CYP450적억제작용。결론：랄초소재체외대대서간미립CYP1A2、CYP2C11、CYP2E1화CYP3A2구유억제작용,차미정현출예부육시간의뢰성。
Objective:To investigate the in vitro effect of capsaicin on four major rat cytochrome P450 ( CYP) enzymes using a cocktail probe drug method. Methods:The in vitro incubation was divided into capsaicin group and the control group. Rat liver micro-somes, probe drugs, capsaicin at various concentration ( buffer solution in the control group) and cofactors were cultured altogether for 20 min. After the culture, the concentration of metabolites was determined by HPLC to assess the activities of enzymes. IC50 value of capsaicin on every isoform was calculated using Graphpad prism 5. 0. Capsaicin and hepatic microsomess were pre-incubated respec-tively for 0, 5, 10, 15, 20 and 30 min, and then the relative activity of the four isoforms at different time was calculated. Results:The activity of the rat liver microsomes enzyme CYP450 isoforms (CYP1A2, CYP2C11, CYP2E1 and CYP3A2) was all inhibited by capsaicin in vitro with IC50 value of 36. 21, 17. 19, 51. 64 and 18. 86 μmol·L-1 , respectively. Pre-incubation could not increase cap-saicin inhibitory activity against the four CYP enzymes. Conclusion:Capsaicin shows inhibition on CYP1A2, CYP2C11, CYP2E1 and CYP3A2 in rat liver microsomes in vitro without pre-incubation time-dependent property.
