92340-57-3Relevant articles and documents
Evaluation of MTBH, a novel hesperetin derivative, on the activity of hepatic cytochrome P450 isoform in?vitro and in?vivo using a cocktail method by HPLC-MS/MS
Qin, Yan,Dong, Haijun,Sun, Jiayin,Zhang, Yilong,Li, Jun,Zhang, Tianci,Chen, Guanjun,Wang, Sheng,Song, Shuai,Wang, Wei,Fan, Yuru,Wang, Jie,Huang, Xiaohui,Shen, Chenlin
, p. 1389 - 1399 (2022/01/11)
1. 8-methylene-tert-butylamine-3′,5,7-trihydroxy-4′-methoxyflavanone (MTBH), a novel hesperidin derivative, has potential in the prevention of hepatic disease, however, its effects on cytochrome P450 isoforms (CYP450s) remains unexplored. The purpose was to investigate the effects of MTBH on the mRNA, protein levels, and activities of six CYP450s (1A2, 2C11/9, 2D2/6, 3A1/4, 2C13/19, and 2E1) in?vitro and in?vivo. 2. In vitro study, rat and human liver microsomes were adopted to elucidate the inhibitory effect of MTBH on six CYP450s using probe drugs. In vivo study, Sprague-Dawley male rats were treated with MTBH (25, 50, or 100 mg/kg for 28 consecutive days), phenobarbital (80 mg/kg for 12 consecutive days), or 0.5% CMC-Na solution (control group) by intragastric administration, then, the mRNA, protein levels and activities of liver CYP450s were analysed by real-time PCR, western blotting and probe-drug incubation systems, respectively. 3. The in?vitro study indicated that MTBH inhibits the activities of CYP3A1/4 and CYP2E1 in rat and human liver microsomes. In vivo data showed that MTBH inhibits mRNA, protein levels, and activities of CYP3A1 and CYP2E1 in medium- and high-dose MTBH groups. 4. MTBH has the potential to cause drug-drug interactions when co-administered with drugs that are metabolised by CYP3A1/4 and CYP2E1.
Prepare alkylene sulfonyl-1-H-benzimidazole derivatives
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Paragraph 0032; 0033; 0070; 0071, (2016/11/24)
The invention relates to a method for preparing a sulfinyl-1-hydrogen-benzimidazole derivative. According to the invention, a 2-(1H-benzimidazole-2-methylmercapto)-4-hydroxy-pyridine derivative expressed in a general formula I is dissolved in a solvent, and under the effect of a catalyst and an additive, a hydrogen peroxide aqueous solution is used as an oxidizing agent for oxidizing reaction, so that the sulfinyl-1-hydrogen-benzimidazole derivative expressed in the general formula II (refer to the Specification) is prepared. The method has the advantages that the operation is simple, a catalyst with the harmful effect on a human body is not used, no pollution to the environment is caused, and the obtained product is higher in yield and purity, so that the method is suitable for industrialization scale production, and has important practical application value.