产品
编 号:F028486
分子式:C16H22ClN3O
分子量:307.82
产品类型
结构图
CAS No: 107534-96-3
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产品详情
生物活性:
Tebuconazole is an agricultural azole fungicide which can also inhibit CYP51 with IC50s of 0.9 and 1.3 μM for Candida albicans CYP51 (CaCYP51) and truncated Homo sapiens CYP51 (Δ60HsCYP51), respectively. Tebuconazole induces lipid accumulation and oxidative stress in HepG2 Cells. Tebuconazole decreases MAC-T cells viability and proliferation, induces ER-stress-mediated apoptosis and increases oxidative stress levels in MAC-T cells.
体内研究:
Tebuconazole (TEB) (每天一次,10-50 mg/kg,连续 28 天) 可诱导大鼠多种 CYPs 和肝脏氧化应激,抑制睾丸 P450 和谷胱甘肽 S 转移酶活性,并对雄性大鼠产生抗雄激素作用。Tebuconazole (25-100 mg/kg,每天给药,持续 10 天) 引起妊娠期大鼠中胎儿睾丸间质细胞增殖,增加胎儿血清睾酮和孕酮水平.Animal Model:Male Wistar rats
Dosage:10, 25, and 50 mg/kg
Administration:p. o. once daily for 28 days
Result:Induced CYP1A1/2, CYP2B1/2, CYP2E1, and CYP3A proteins in liver.Decreased glutathione content and increased glutathione S-transferase, superoxide dismutase, catalase, and glutathione peroxidase activities in liver . Increased superoxide dismutase activities in kidney and testis.Decreased glutathione S-transferase activity in testis .Decreased serum testosterone concentration and cauda epididymal sperm count .
Animal Model:Male and female Sprague-Dawley rats
Dosage:25, 50, and 100 mg/kg
Administration:Oral gavage (p.o.), for 10 days
Result:Increased fetal serum testosterone and progesterone levels.Increased the number of fetal Leydig cells per testis without inducing cell aggregation. Up-regulated the expression levels of Star, Cyp11a1, Hsd17b3, and Fshr.Increased phosphorylation of AKT1, ERK1/2, and mTOR, the level of BCL2, as well as the decrease of Beclin1, LC3B, and BAX.
体外研究:
Tebuconazole (TEB) (20–80 μM,24 小时) 使 HepG2 细胞出现脂质积累。Tebuconazole (20-80 μM,12 小时) 增加了 HepG2 细胞中过氧化物酶体增殖激活受体的核转位以及脂质摄取和氧化相关标志物的表达。Tebuconazole (20-80 μM,24 小时) 使氧化应激水平升高,导致 HepG2 细胞线粒体膜电位丧失和微粒体甘油三酯转移蛋白水平降低。Tebuconazole (0-750 μM,24 小时) 可降低 MAC-T 细胞活力和增殖,并通过激活 ER 应激诱导线粒体介导的 MAC-T 细胞凋亡。Tebuconazole (0-100 μM,24 小时) 可诱导 H9c2 心肌细胞和成年大鼠心室肌细胞 (ARVM) 发生剂量依赖性细胞死亡。Tebuconazole (30-60 μM,24 小时) 诱导 H9c2 细胞的 DNA 损伤、活性氧的产生和脂质过氧化。