The effects of eight components from six commonly consumed spices on P-glycoprotein (P-gp) transport and CYP3A4 metabolism were evaluated in vitro. P-gp-mediated [(3)H]digoxin fluxes across the L-MDR1 (LLC-PK1 cells transfected with human MDR1 gene) and Caco-2 (human colon carcinoma) cell monolayers showed a marked asymmetry compared with that in the LLC-PK1 (porcine kidney epithelial cells) ce...

BACKGROUND Whole-grain (WG) intake is important for human health, but accurate intake estimation is challenging. Use of a biomarker for WG intake provides a possible way to validate dietary assessment methods. OBJECTIVE Our aim was to validate WG intake from 2 diets reported by children, using plasma alkylresorcinol (AR) concentrations, and to investigate the 3-mo reproducibility of AR concen...

Cinobufagin (CB), a major bioactive component of the traditional Chinese medicine Chansu, has been reported to have potent antitumor activity. In this study, in vitro metabolism of CB among species was compared with respect to metabolic profiles, enzymes involved, and catalytic efficiency by using liver microsomes from human (HLM), mouse (MLM), rat (RLM), dog (DLM), minipig (PLM), and monkey (C...

These lecture notes present some basic intuitions underlying structural equations modeling (SEM). If you find this technique useful in your research, I suggest that you take a semester-long course on SEM and/or hierarchical linear model (HLM). It turns out that SEM and HLM are essentially the same technique but some things are easier to implement in one versus the other so disciplines tend to f...

در این مقاله یک مدل ریاضی برای مسئله سیستم تولیدی همکارانه ساخت بر اساس سفارش با رعایت انصاف تخصیص بار‌های تولید طراحی شده است. اهداف اصلی مدل، کمینه‌سازی هزینه‌‌های کل و حداکثر استفاده از منابع به‌منظور عادلانه شرایط عدم­قطعیت کنترل پارامتر‌های غیرقطعی روش برنامه‌ریزی فازی ‌شده نتایج نشان می‌دهد افزایش نرخ عدم‌قطعیت، می­یابد. ازآنجاکه ظرفیت کارخانه‌ها ثابت است، مقدار تقاضا، هر کارخانه نیز می­ی...

This study determined the cytochrome P450 (P450) isoforms responsible for metabolism of isoflavones using human liver microsomes (HLM) and expressed P450s. The primary metabolite of genistein is 3'-OH-genistein, as identified with an authentic chemically synthesized standard. CYP1A2 was predominantly responsible for 3'-OH-genistein formation since its formation was inhibited (>50%, p < 0.05) by...

Lorcaserin, a selective serotonin 5-hydroxytryptamine 2C receptor agonist, is being developed for weight management. The oxidative metabolism of lorcaserin, mediated by recombinant human cytochrome P450 (P450) and flavin-containing monooxygenase (FMO) enzymes, was examined in vitro to identify the enzymes involved in the generation of its primary oxidative metabolites, N-hydroxylorcaserin, 7-hy...

Tamoxifen, an antiestrogen used in the prevention and treatment of breast cancer, is extensively metabolized by cytochrome P450 enzymes. Its biotransformation to α-hydroxytamoxifen (α-OHT), which may be genotoxic, and to N-desmethyltamoxifen (N-DMT), which is partially hydroxylated to 4-hydroxy-N-DMT (endoxifen), a potent antiestrogen, is mediated by CYP3A enzymes. However, the potential contri...

Bovine serum albumin (BSA) and fatty acid-free human serum albumin (HSAFAF) reduce the K(m) values for UGT2B7 substrates by sequestering inhibitory long-chain fatty acids released by incubations of human liver microsomes (HLM) and HEK293 cells expressing this enzyme. However, the scope of the "albumin effect" is unknown. In this investigation we characterized the effects of albumin on the kinet...

Phenacetin was withdrawn from the market because it caused renal failure in some patients. Many reports indicated that the nephrotoxicity of phenacetin is associated with the hydrolyzed metabolite, p-phenetidine. Acetaminophen (APAP), the major metabolite of phenacetin, is also hydrolyzed to p-aminophenol, which is a nephrotoxicant. However, APAP is safely prescribed if used in normal therapeut...