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
2014年
9期
800-802
,共3页
杨旭平%冯碧敏%黄毅岚%钟小燕
楊旭平%馮碧敏%黃毅嵐%鐘小燕
양욱평%풍벽민%황의람%종소연
抗肿瘤中药注射液%肝微粒体%细胞色素P4503 A4%药-药相互作用
抗腫瘤中藥註射液%肝微粒體%細胞色素P4503 A4%藥-藥相互作用
항종류중약주사액%간미립체%세포색소P4503 A4%약-약상호작용
anti -tumor traditional Chinese medicine injections%liver microsomes%cytochrome P4503 A4%drug-drug interaction
目的:以睾酮为探针药物体外研究抗肿瘤中药注射液榄香烯、康莱特、鸦胆子油、艾迪对大鼠细胞色素P4503A4(CYP3A4)亚型酶活性的影响。方法用大鼠肝微粒体体外孵育法,用高效液相色谱法测定4种抗肿瘤中药注射液在孵育体系中6β-羟基睾酮(6-OHTS)生成量,反映其对CYP3A4酶活性的影响。结果与空白组相比,榄香烯对CYP3A4酶活性无明显影响;康莱特与艾迪对CYP3A4有诱导作用;鸦胆子油乳对CYP3A4有抑制作用,半数抑制率IC50值为0.78%。结论临床上在与经CYP3A4代谢的药物联合应用时,应警惕康莱特、艾迪及鸦胆子油乳潜在的药-药相互作用。
目的:以睪酮為探針藥物體外研究抗腫瘤中藥註射液欖香烯、康萊特、鴉膽子油、艾迪對大鼠細胞色素P4503A4(CYP3A4)亞型酶活性的影響。方法用大鼠肝微粒體體外孵育法,用高效液相色譜法測定4種抗腫瘤中藥註射液在孵育體繫中6β-羥基睪酮(6-OHTS)生成量,反映其對CYP3A4酶活性的影響。結果與空白組相比,欖香烯對CYP3A4酶活性無明顯影響;康萊特與艾迪對CYP3A4有誘導作用;鴉膽子油乳對CYP3A4有抑製作用,半數抑製率IC50值為0.78%。結論臨床上在與經CYP3A4代謝的藥物聯閤應用時,應警惕康萊特、艾迪及鴉膽子油乳潛在的藥-藥相互作用。
목적:이고동위탐침약물체외연구항종류중약주사액람향희、강래특、아담자유、애적대대서세포색소P4503A4(CYP3A4)아형매활성적영향。방법용대서간미립체체외부육법,용고효액상색보법측정4충항종류중약주사액재부육체계중6β-간기고동(6-OHTS)생성량,반영기대CYP3A4매활성적영향。결과여공백조상비,람향희대CYP3A4매활성무명현영향;강래특여애적대CYP3A4유유도작용;아담자유유대CYP3A4유억제작용,반수억제솔IC50치위0.78%。결론림상상재여경CYP3A4대사적약물연합응용시,응경척강래특、애적급아담자유유잠재적약-약상호작용。
Objective To investigate the influence of elemene , kang-laite, brucea jananica oil and Aidi injection on CYP 3A4 of liver micro-somes in vitro with testosterone as probe.Methods HPLC method was used to detect the production of 6β-hydroxytestosterone (6-OHTS) to study the effects of 4 anti-tumor traditional Chinese medicine injections on the activities of CYP 3 A4 enzymes in the microsomal incubation sys-tem.Results Compared with blank control group , elemene have no sig-nificant effects on CYP3A4; kanglaite, Aidi have a induction on CYP3A4;brucea jananica oil have a inhibition on CYP3A4, IC50 of bru-cea jananica oil on CYP3A4 was 0.78%.Conclusion Potential drug-drug interaction should be vigilant when kanglaite , aidi and brucea ja-nanica oil co -administered with the substrates which mainly undergo CYP3A4-mediated metabolism.