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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Sabzevari O, Hatcher M, O'Sullivan M, Kentish P, Gibson G

Molecular Toxicology Group, School of Biological Sciences, University of Surrey, Guildford, UK.

Xenobiotica. 1995 Apr;25(4):395-403. doi: 10.3109/00498259509061860.

The influence of imidazole and triazole antifungal drugs on cytochrome P450 levels in male Wistar primary rat hepatocyte culture for 70 h has been investigated and compared with clofibrate. 2. Bifonazole, clotrimazole, geniconazole clofibrate induced total P450 in hepatocytes, whereas itraconazole, miconazole and UK-47,265 did not. 3. When the CYP4A subfamily was examined, only bifonazole and clofibrate induced CYP4A as assessed by both Western blot analysis and the 11- and 12-hydroxylation of lauric acid. 4. By analysis of concentration-response curves in hepatocyte culture, bifonazole was 160 and 40 times more potent than clofibrate for induction of the 11- and 12-hydroxylation of lauric acid respectively. 5. Taken collectively, our data have identified bifonazole as a relatively potent, non-carboxylate inducer of CYP4A and the mechanism of induction and specificity of this azole is discussed.

研究了咪唑和三唑类抗真菌药物对雄性Wistar大鼠原代肝细胞培养70小时细胞色素P450水平的影响，并与氯贝丁酯进行了比较。2. 联苯苄唑、克霉唑、吉尼康唑和氯贝丁酯可诱导肝细胞中的总P450，而伊曲康唑、咪康唑和UK-47,265则不能。3. 当检测CYP4A亚家族时，通过蛋白质印迹分析以及月桂酸的11-和12-羟基化评估，只有联苯苄唑和氯贝丁酯可诱导CYP4A。4. 通过对肝细胞培养中的浓度-反应曲线分析，联苯苄唑诱导月桂酸11-和12-羟基化的效力分别比氯贝丁酯高160倍和40倍。5. 总体而言，我们的数据已确定联苯苄唑是一种相对强效的、非羧酸盐类CYP4A诱导剂，并讨论了该唑类药物的诱导机制和特异性。

Sabzevari O, Hatcher M, O'Sullivan M, Kentish P, Gibson G

Molecular Toxicology Group, School of Biological Sciences, University of Surrey, Guildford, UK.

Xenobiotica. 1995 Apr;25(4):395-403. doi: 10.3109/00498259509061860.

The influence of imidazole and triazole antifungal drugs on cytochrome P450 levels in male Wistar primary rat hepatocyte culture for 70 h has been investigated and compared with clofibrate. 2. Bifonazole, clotrimazole, geniconazole clofibrate induced total P450 in hepatocytes, whereas itraconazole, miconazole and UK-47,265 did not. 3. When the CYP4A subfamily was examined, only bifonazole and clofibrate induced CYP4A as assessed by both Western blot analysis and the 11- and 12-hydroxylation of lauric acid. 4. By analysis of concentration-response curves in hepatocyte culture, bifonazole was 160 and 40 times more potent than clofibrate for induction of the 11- and 12-hydroxylation of lauric acid respectively. 5. Taken collectively, our data have identified bifonazole as a relatively potent, non-carboxylate inducer of CYP4A and the mechanism of induction and specificity of this azole is discussed.

研究了咪唑和三唑类抗真菌药物对雄性Wistar大鼠原代肝细胞培养70小时细胞色素P450水平的影响，并与氯贝丁酯进行了比较。2. 联苯苄唑、克霉唑、吉尼康唑和氯贝丁酯可诱导肝细胞中的总P450，而伊曲康唑、咪康唑和UK-47,265则不能。3. 当检测CYP4A亚家族时，通过蛋白质印迹分析以及月桂酸的11-和12-羟基化评估，只有联苯苄唑和氯贝丁酯可诱导CYP4A。4. 通过对肝细胞培养中的浓度-反应曲线分析，联苯苄唑诱导月桂酸11-和12-羟基化的效力分别比氯贝丁酯高160倍和40倍。5. 总体而言，我们的数据已确定联苯苄唑是一种相对强效的、非羧酸盐类CYP4A诱导剂，并讨论了该唑类药物的诱导机制和特异性。