DL-111-1T对雌鼠肝脏及人羊膜细胞混合功能氧化酶活性的选择性诱导  

SELECTIVE INDUCING ABILITY OF DL-111-1T TOWARDS MIXED FUNCTION OXIDASE IN FEMALE RAT LIVER AND HUMAN AMNION FLUID CELL

作　　者：刘志强[1] 林志英[1] 孙路 余应年 

机构地区：[1]浙江医科大学药学系,杭州310006

出　　处：《药学学报》1989年第9期641-646,共6页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金

摘　　要：以抗早孕药3-(2-ethylphenyl)-5-(3-methoxyphenyl)-1H-1,2,4-triazole(DL-111-1T)20 mg/(kg.d)预处理♀大鼠2 d,即可使动物肝微粒体MFO与UDPGT达到稳态诱导,其诱导特征为多环芳烃型。以0.1μmol/L DL-111-1T与人羊膜FL细胞孵育24 h,可使细胞内AHH活性诱导增高3.5倍左右,此诱导能力三倍于PB,但仅为3-MC的1/2左右,即DL-111-1T对人羊膜FL细胞中依赖于P-448的MFO呈现中等程度的选择性诱导作用。UDS试验则证明DL-111-1T本身无致突变性。Following pretreatment of adult female rats with contragestational agent 3-(2-ethylphenyl)-5-(3-methoxyphenyl)-1H-1,2,4-triazol(DL111-1T) 20 mg/kg.d for 2 consecutive days, the hepatic microsomal MFO and UDPGT activities were induced to a constant level,being chacacteristic of arylhydrocarbon type of induction. Coincubation of human amnion FL cell with 0.1 μmol/L of DL-111-1T for 24 h produced a 4.5-fold induction of AHH activity of the cell. This inducing ability was 3 times that of PB, but 1/2 that of 3-MC. According to these observations, DL-111-1T may also be considered as a polycyclic arylhydrocarbon type inducer toward human amnion FL cell's MFO which contains mainly of cytochrome P-448. UDS test showed that DL-111-1T itself could not induce UDS of FL cell.

关 键 词：DL-111-1T 抗早孕药 致突变试验 

分 类 号：R963[医药卫生—微生物与生化药学]