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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。
Objective To study the effect of anti-tumor Chinese medicine injection of elemene, Kanglaite, Brucea javanica oil and Eddie on the enzyme activity of cytochrome P4503A4 (CYP3A4) subtype in vitro using testosterone as probe drug. Methods The in vitro incubation of rat liver microsomes was used to determine the production of 6β-hydroxytestosterone (6-OHTS) in 4 kinds of anti-tumor traditional Chinese medicine injection by HPLC. Results Compared with the blank group, elemene had no significant effect on CYP3A4 activity. KLT and Aid induced CYP3A4. Brucea javanica oil emulsion inhibited CYP3A4 with IC50 of 0.78%. Conclusions Clinically, the potential drug-drug interactions of KLT, Aidi and Brucea javanica oil emulsion should be taken care when used in combination with CYP3A4-metabolized drugs.