Imazalil

一种咪唑类杀菌剂，可抑制麦角固醇的生物合成；以pH依赖性方式抑制各种真菌的体外生长，包括P.italicum、A.niger、U.maydis、B.alii和C.cucumerinum（pH7时MIC=0.005-2μg/ml）；抑制酿酒酵母，但不抑制大鼠肝微粒体CYP（IC50分别为0.088和80μM）以及人胎盘微粒体的芳香酶CYP19（IC50=0.34μM）；在细胞报告基因检测中以浓度依赖性方式激活小鼠PXR；在100mg/kg剂量下增加小鼠肝脏CYP3A11和CYP2B10mRNA水平；与mCAR激动剂TCPOBOP联合使用时，可增加小鼠肝切片中Ki-67阳性细胞核和肝脏MCM2mRNA水平（细胞增殖标志物）。An imidazole fungicide that inhibits ergosterol biosynthesis; inhibits the growth of various fungi in vitro including P. italicum, A. niger, U. maydis, B. alii, and C. cucumerinum in a pH-dependent manner (MICs = 0.005-2 μg/ml at pH 7); inhibits S. cerevisiae, but not rat liver microsomal, CYPs (IC50s = 0.088 and 80 μM, respectively), as well as aromatase CYP19 from human placental microsomes (IC50 = 0.34 μM); activates the murine PXR in a concentration-dependent manner in a cell-based reporter assay; increases hepatic CYP3A11 and CYP2B10 mRNA levels in mice at 100 mg/kg; increases Ki-67-positive nuclei in liver sections and hepatic MCM2 mRNA levels, markers of cell proliferation, in mice when co-administered with the mCAR agonist TCPOBOP.