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hydroxylation metabolism
相关语句
  羟基化代谢
     Parent drug and metabolites were detected with liquid chromatography-multistage mass spectrometry, and the contribution of four CYPs in the hydroxylation metabolism of imrecoxib was evaluated by the rate of with total normalized rate (TNR) method. Imrecoxib is metabolized by CYP2C9, CYP2D6 and CYP3A4, which with the rate of as following: 62.5%, 21.1% and 16.4% respectively.
     研究结果表明CYP2C9为艾瑞昔布羟基化代谢的主要代谢酶,代谢贡献高达62.5%,CYP2D6次之,代谢贡献为21.1%;
短句来源
     CYP2C9 is the major enzyme involved in imrecoxib hydroxylation metabolism.
     CYP2C9和CYP2C19为格列齐特羟基化代谢(包括6β-羟基化代谢和甲基羟化代谢)的主要代谢酶;
短句来源
     Investigation on the hydroxylation metabolism of imrecoxib in vitro by using recombinant human CYPs
     采用重组人源CYP酶研究艾瑞昔布的体外羟基化代谢
短句来源
  羟化代谢
     CYP2C9 is the major enzyme involved in imrecoxib hydroxylation metabolism.
     CYP2C9和CYP2C19为格列齐特羟基化代谢(包括6β-羟基化代谢和甲基羟化代谢)的主要代谢酶;
短句来源
     Conclusion The data indicated that there were obvious substrate stereoselective differences in the hydroxylation metabolism of (+) and (-) Clau, which provided an explanation of the difference of pharmacokinetic characteristics of Clau enantiomers in rats.
     而其 7 羟 Clau和 5 羟 Clau的产生量很小。 结论 黄皮酰胺对映体在大鼠肝微粒体中的羟化代谢存在明显的底物立体选择性差异。
短句来源
  “hydroxylation metabolism”译为未确定词的双语例句
     Conclusion CYP2C9 is the major enzyme involved in imrecoxib hydroxylation metabolism.
     结论 CYP2C9为艾瑞昔布羟基化的主要代谢酶。
短句来源
     Conclusion CYP2C9 is the major enzyme involved in imrecoxib hydroxylation metabolism.
     结论CYP2C9为艾瑞昔布羟基化的主要代谢酶。
短句来源
     Methods Imrecoxib was incubated with heterologous expression human cytochrome P450 (rCYPs) in vitro, and metabolites and remained parent drug were detected with liquid chromatography-multistage mass spectrometry. The contribution of 4 CYPs in the hydroxylation metabolism of imrecoxib was evaluated by total normalized rate (TNR) method.
     方法 用体外重组的人源细胞色素P450(CYP)进行孵育代谢实验,液相色谱多级质谱法分析代谢产物和残留的母体药物,利用整体归一化法对4种CYP酶的代谢作用大小进行评估。
短句来源
     Methods Imrecoxib was incubated with heterologous expression human cytochrome P450 (rCYPs) in vitro, and metabolites and remained parent drug were detected with liquid chromatography-multistage mass spectrometry. The contribution of 4 CYPs in the hydroxylation metabolism of imrecoxib was evaluated by total normalized rate (TNR) method.
     方法用体外重组的人源细胞色素P450(CYP)进行孵育代谢实验,液相色谱-多级质谱法分析代谢产物和残留的母体药物,利用整体归一化法对4种CYP酶的代谢作用大小进行评估。
短句来源
  相似匹配句对
     CONCLUSION: The metabolism of (+)clausenamide were hydroxylation or dihydroxylation.
     结论:黄皮酰胺的代谢主要发生羟化或双羟化,CM3是其主要代谢产物,量较少的CM4,CM6为其进一步代谢产生的双羟基代谢产物;
短句来源
     THE METABOLISM OF PROLINE
     脯氨酸的代谢
短句来源
     Metabolism Syndrome
     代谢综合征
短句来源
     The preliminary study is performed on influencing factors of hydroxylation for drug metabolism.
     对药物由于代谢而产生的氧化羟化影响因素进行了初步探讨。
短句来源
     Direct Hydroxylation of Benzene into Phenol
     苯直接羟基化制苯酚研究进展
短句来源
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Single oral 100mg dose of phenytoin( PHT)was given to 16 healthy subjeets on different occations, urine was collected up to 24 hours. The excreted PHT and 4’-hydroxylation metabolite (4’-OH-PHT) were measured by HPLC method. The subjects were phenotyped 3 poor metabolizers (PMs) and 13 extensive metabolizers(EMs) of s-mephenytoin(S-MP) hydroxylation by metabolic ratio (MR) and hydroxylation index(HI). The log10 PHT /4’-OH-PHT of PMs and EMs were-2.27± 0.10 and-2. 17 ± 0. 26. respectively. There was no significant...

Single oral 100mg dose of phenytoin( PHT)was given to 16 healthy subjeets on different occations, urine was collected up to 24 hours. The excreted PHT and 4’-hydroxylation metabolite (4’-OH-PHT) were measured by HPLC method. The subjects were phenotyped 3 poor metabolizers (PMs) and 13 extensive metabolizers(EMs) of s-mephenytoin(S-MP) hydroxylation by metabolic ratio (MR) and hydroxylation index(HI). The log10 PHT /4’-OH-PHT of PMs and EMs were-2.27± 0.10 and-2. 17 ± 0. 26. respectively. There was no significant difference in PMs and EMs of log10 PHT /4’-OH-PHT (p>0. 05).No correlations were found between the log10 PHT/4’-OH-PHT of PHT and the log10 MR and log10 HI of S-MP.These findings suggested that they are antiepileptic drugs of hydantoinis and 4’-hydroxylation metabolism, but dissociation of S-MP polymorphism and PHT hydroxlation.

16名汉族健康志愿者进行S-美芬妥英4’-羟化代谢分型,13名为强代谢者(EMs),3名为弱代谢者(PMs)。口服苯妥英100mg,应用HPLC法测定服药后24h尿中苯妥英和4’-羟苯妥英(4’-OH-PHT)的排泄量。13名S-美芬妥英强代谢者Lg苯妥英/4’-羟苯妥英比值为-2.17±0.26;3名弱代谢者为-2.27±0.10,两组无显著性差异P>0.05)。16名受试者S-美芬妥英和苯妥英的羟化代谢比值无相关性(r=-0.108,P>0.005)。本文结果表明,S-美芬妥英和苯妥英虽同为乙内酰脲类抗癫痫药,化学结构和羟化反应均相似,但在人体内不属同一羟化途径代谢,无交叉代谢障碍。

AIM: Catechol estrogens and 16a-hydroxy estrogen are important metabolites that cause carcinogenesis. This study was aimed to study the role of cytochrome P450 in estradiol metabolism. METHODS: The estradiol metabolites were determined with HPLC-ECD. Correlation of estradiol metabolites production between cytochrome P450 activity, the inhibitory effect of specific inhibitors and enzyme catalyzing kinetics were studied in cDNA-expressed P450 or human liver microsomes. RESULT: CYP1A2, CYP3A4, and CYP2C9 catalyze...

AIM: Catechol estrogens and 16a-hydroxy estrogen are important metabolites that cause carcinogenesis. This study was aimed to study the role of cytochrome P450 in estradiol metabolism. METHODS: The estradiol metabolites were determined with HPLC-ECD. Correlation of estradiol metabolites production between cytochrome P450 activity, the inhibitory effect of specific inhibitors and enzyme catalyzing kinetics were studied in cDNA-expressed P450 or human liver microsomes. RESULT: CYP1A2, CYP3A4, and CYP2C9 catalyze the estradiol 2-hydroxylation. CYP2C9, CYP2C19, and CYP2C8 have high activity in catalyzing 17β-hydroxy de-hydrogenation in cDNA expressed P450, but CYP1A2 is the most important enzyme in catalyzing estradiol 2-hydroxylation. Using furafyllin and troleandomycin to inhibit CYP1A2 and CYP3 A4 in liver microsomes, it was found that the 2-hydroxylation had been inhibited about the same amount. This result suggests that in human liver microsomes CYP1A2 and CYP3A4 play an important role in 2-hydroxy estradiol formation. At low substrate concentration, 17 β-hydroxy dehydrogenation dominated the estradiol metabolism, but at high substrate concentration, 2-hydroxylation exceeded 17β-hydroxy dehydrogenation to become the important mechanism. CONCLUSION: CYP1A2 and CYP3A4 are two important enzymes catalyzing the main estradiol 2-hydroxylation metabolism pathway at high substrate concentrations. 17β-hydroxy dehydrogenation is the main metabolism pathway at low concentrations, and CYP2C9, CYP2C19, and CYP2C8 may have high catalyzing activity.

目的:研究雌二醇在cDNA表达的P450和人肝微粒体中的代谢机制,为在体内研究细胞色素P450活性与肿瘤发生的关系提供依据。方法:用HPLC-ECD法测定雌二醇的代谢产物。通过雌二醇在不同cDNA表达的P450中代谢,13例人肝微粒体中相关性研究,抑制剂对代谢的影响以及微粒体中17β-羟基脱氢化和2-羟基化代谢的催化动力学的研究来推断雌二醇的代谢机理。结果:在cDNA表达的P450中,催化2-羟基化代谢的P450按活性排列依次为CYP1A2、CYP3A4、CYP2C9。CYP2C9、CYP2C19和CYP2C8均具有较高的催化17β-羟基脱氢化活性。抑制CYP1A2与抑制CYP3A4对2-羟基化代谢产物生成的影响相似,可认为CYP1A2和CYP3A4在人肝微粒体中催化2-羟基化代谢的作用相近。雌二醇代谢的途径与底物浓度有关,低浓度时(1,10μmol/L)17β-羟基脱氢化为主要代谢途径;高浓度时(100μmol/L),2-羟基化成为主要代谢途径。结论:高底物浓度时,雌二醇主要由CYP1A2和CYP3A4催化代谢为2-羟基化产物。低底物浓度时,主要由CYP2C9、CYP2C19和CYP2C8催化生成17β-羟...

目的:研究雌二醇在cDNA表达的P450和人肝微粒体中的代谢机制,为在体内研究细胞色素P450活性与肿瘤发生的关系提供依据。方法:用HPLC-ECD法测定雌二醇的代谢产物。通过雌二醇在不同cDNA表达的P450中代谢,13例人肝微粒体中相关性研究,抑制剂对代谢的影响以及微粒体中17β-羟基脱氢化和2-羟基化代谢的催化动力学的研究来推断雌二醇的代谢机理。结果:在cDNA表达的P450中,催化2-羟基化代谢的P450按活性排列依次为CYP1A2、CYP3A4、CYP2C9。CYP2C9、CYP2C19和CYP2C8均具有较高的催化17β-羟基脱氢化活性。抑制CYP1A2与抑制CYP3A4对2-羟基化代谢产物生成的影响相似,可认为CYP1A2和CYP3A4在人肝微粒体中催化2-羟基化代谢的作用相近。雌二醇代谢的途径与底物浓度有关,低浓度时(1,10μmol/L)17β-羟基脱氢化为主要代谢途径;高浓度时(100μmol/L),2-羟基化成为主要代谢途径。结论:高底物浓度时,雌二醇主要由CYP1A2和CYP3A4催化代谢为2-羟基化产物。低底物浓度时,主要由CYP2C9、CYP2C19和CYP2C8催化生成17β-羟基去氢化产物。

Aim To investigate the enzyme kinetics of (-) 3 S ,4 R ,5 R ,6 S clausenamide[(-) Clau] and (+) 3 R ,4 S ,5 S ,6 R clausenamide[(+) Clau] catalyzed by rat liver microsomes and compare their stereoselective differences. Methods An in vitro metabolic system was built by using rat liver microsomes and NADPH generating system. Clau and its metabolites were determined simultaneously by a reversed phase high performance liquid chromatography. The kinetic parameters, K m, V ...

Aim To investigate the enzyme kinetics of (-) 3 S ,4 R ,5 R ,6 S clausenamide[(-) Clau] and (+) 3 R ,4 S ,5 S ,6 R clausenamide[(+) Clau] catalyzed by rat liver microsomes and compare their stereoselective differences. Methods An in vitro metabolic system was built by using rat liver microsomes and NADPH generating system. Clau and its metabolites were determined simultaneously by a reversed phase high performance liquid chromatography. The kinetic parameters, K m, V max , and metabolic rate, V max / K m, were calculated by Eadie Hofstee plot. Results In the metabolic system, (-) Clau was found to be mainly metabolized to 7 hydroxy , 5 hydoxy and 4 hydroxy Clau, and 7 hydroxylation was a preferential pathway which exhibited higher V max / K m value (0 135 μL·min -1 ·mg -1 ) than those of 5 and 4 hydroxylation (0 063 and 0 068 μL·min -1 ·mg -1 , respectively). For (+) Clau, it was mainly metabolized to 4 hydroxy Clau, whereas 7 hydroxy and 4 hydroxy Clau were so small that they could not be detected systematically. 4 Hydroxylation of (+) Clau showed highest V max / K m value (0 547 μL·min -1 ·mg -1 ) among all the metabolites tested, which was 8 0 times higher than that of 4 hydroxylation of its antipode. Conclusion The data indicated that there were obvious substrate stereoselective differences in the hydroxylation metabolism of (+) and (-) Clau, which provided an explanation of the difference of pharmacokinetic characteristics of Clau enantiomers in rats.

目的 研究黄皮酰胺 (clausenamide ,Clau)对映体在大鼠肝微粒体中的酶促反应动力学并比较其立体选择性差异。方法 应用反相HPLC法测定Clau对映体在体外代谢系统中的产物 ,并用Eadie Hofstee作图法分析数据、求算酶促反应动力学参数Km 和Vmax以及肝代谢速率Vmax Km。结果 在体外代谢系统中 ,左旋黄皮酰胺主要生成 7 羟 Clau、5 羟 Clau和 4 羟 Clau ,其优势代谢途径为 7位羟化 ;7位羟化代谢的Vmax Km 值高于 5位和 4位。右旋黄皮酰胺的 4位羟化反应Km 最小、Vmax最大 ,因此代谢速率最高 ,是左旋体 4位羟化的 8倍 ;而其 7 羟 Clau和 5 羟 Clau的产生量很小。结论 黄皮酰胺对映体在大鼠肝微粒体中的羟化代谢存在明显的底物立体选择性差异。

 
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