6,184 results match your criteria cyp2e1

Enantioselective metabolism of phenylpyrazole insecticides by rat liver microsomal CYP3A1, CYP2E1 and CYP2D2.

Pestic Biochem Physiol 2021 Jul 11;176:104861. Epub 2021 May 11.

College of Resources and Environment, Anhui Agricultural University, Key Laboratory of Agri-food Safety of Anhui Province, Hefei 230036, China. Electronic address:

The stereoselective difference of chiral pesticide enantiomers is an important factor of risk evaluation and the subject has received wide attention. In the present work, enantioselective metabolism of chiral phenylpyrazole insecticides including fipronil, ethiprole and flufiprole in rat liver microsomes was investigated in vitro. The result showed remarkable enantioselectivity for fipronil and ethiprole with the EF values of 0. Read More

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Alpha lipoic acid priming enhances the hepatoprotective effect of adipose derived stem cells in CCl4 induced hepatic injury in-vitro.

Eur J Pharmacol 2021 Jun 9;906:174201. Epub 2021 Jun 9.

National Centre of Excellence in Molecular Biology, University of Punjab, 87-West Canal Bank Road, Lahore, Pakistan; Jinnah Burn & Reconstructive Surgery Centre, Lahore, Pakistan. Electronic address:

Mesenchymal stem cells are known to support hepatic defense against liver fibrosis. However, the fibrosis induced oxidative microenvironment affects the proliferative, regenerative, and angiogenic properties of mesenchymal stem cells. Alpha lipoic acid (ALA) is a strong anti-oxidant which has been shown to ameliorate the adverse effects of fibrosis that otherwise can lead to severe liver problems like cirrhosis and liver failure. Read More

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Herbacetin Broadly Blocks the Activities of CYP450s by Different Inhibitory Mechanisms.

Planta Med 2021 Jun 11. Epub 2021 Jun 11.

School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, Zhejiang, China.

Herbacetin is a bioactive flavanol compound that has various pharmacological effects. However, the pharmacokinetic characteristics have not been thoroughly investigated. Previously, we screened a natural compound library and identified herbacetin as a potent CYP blocker. Read More

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Tryptophan Pathway-Targeted Metabolomics Study on the Mechanism and Intervention of Cisplatin-Induced Acute Kidney Injury in Rats.

Chem Res Toxicol 2021 Jun 10. Epub 2021 Jun 10.

Key Laboratory of Drug Quality Control and Pharmacovigilance (Ministry of Education), State Key Laboratory of Natural Medicine, China Pharmaceutical University, Nanjing 210009, P.R. China.

Cisplatin is a chemotherapeutic agent widely employed in the treatment of various solid tumors. However, its use is often restricted by acute kidney injury (AKI) which is the dose-limiting adverse effect of cisplatin. While numerous studies aiming to alleviate the AKI have been conducted, there are no effective remedies in clinical practice. Read More

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CD36 deficiency ameliorates drug-induced acute liver injury in mice.

Mol Med 2021 Jun 6;27(1):57. Epub 2021 Jun 6.

Department of Biotherapy, Medical Center for Digestive Diseases, Second Affiliated Hospital of Nanjing Medical University, Nanjing, 210011, China.

Background: Acetaminophen (APAP) overdose causes hepatotoxicity and even acute liver failure. Recent studies indicate that sterile inflammation and innate immune cells may play important roles in damage-induced hepatocytes regeneration and liver repair. The scavenger receptor CD36 has its crucial functions in sterile inflammation. Read More

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Solar-Powered Whole-Cell P450 Catalytic Platform for C-Hydroxylation Reactions.

ChemSusChem 2021 Jun 4. Epub 2021 Jun 4.

Korea Advanced Institute of Science and Technology, Materials Science and Engineering, 335 Science Road, 34141, Daejeon, KOREA, REPUBLIC OF.

Photobiocatalysis is a green platform for driving redox enzymatic reactions using solar energy, not needing high-cost cofactors and redox partners. Here, we present a visible light-driven whole-cell platform for human P450 photobiocatalysis using natural flavins as a photosensitizer. Photoexcited flavins mediate NADPH/reductase-free, light-driven biocatalysis by human CYP2E1 both in vitro and in the whole-cell systems. Read More

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10-Dehydrogingerdione ameliorates renal endoplasmic reticulum/oxidative stress and apoptosis in alcoholic nephropathy induced in experimental rats.

Life Sci 2021 May 31;279:119673. Epub 2021 May 31.

Department of Biochemistry, Faculty of Pharmacy, Horus University, Egypt.

Background: Chronic alcoholism induces kidney injury (KI), leading to increased mortality in alcoholic hepatitis patients. Endoplasmic reticulum stress (ER) represents the main initiator of kidney diseases and alcoholic nephropathy.

Aims: We used alcoholic nephropathy rat model followed by 10-dehydrogingerdione (10-DHGD) intake as potential modulator. Read More

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Times New Roman',serif;">Characterization of a novel CYP1A2 knockout rat model constructed by CRISPR/Cas9.

Drug Metab Dispos 2021 Jun 1. Epub 2021 Jun 1.

East China Normal University, China

Cytochrome P450 1A2 (CYP1A2) as one of the most important CYP isoforms is involved in the biotransformation of many important endogenous and exogenous substances. CYP1A2 plays an important role in the development of many diseases because it is involved in the biotransformation of precancerous substances and poisons. Although the generation of Cyp1a2 knockout (KO) mouse model has been reported, there are still no relevant rat models for the study of CYP1A2-mediated pharmacokinetics and diseases. Read More

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Calvaria Bone Transcriptome in Mouse Models of Osteogenesis Imperfecta.

Int J Mol Sci 2021 May 18;22(10). Epub 2021 May 18.

Shriners Hospital for Children-Canada, Montreal, QC H4A 0A9, Canada.

Osteogenesis imperfecta (OI) is a bone fragility disorder that is usually caused by mutations affecting collagen type I. We compared the calvaria bone tissue transcriptome of male 10-week-old heterozygous Jrt ( mutation) and homozygous mice ( mutation) to their respective littermate results. We found that Jrt and mice shared 185 differentially expressed genes (upregulated: 106 genes; downregulated: 79 genes). Read More

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Genetic Variants of Alcohol Metabolizing Enzymes and Alcohol-Related Liver Cirrhosis Risk.

J Pers Med 2021 May 13;11(5). Epub 2021 May 13.

Service of Gastroenterology (Liver Unit), Hospital Clínico San Carlos, Universidad Complutense Medical School, 28040 Madrid, Spain.

Alcohol-related liver disease (ARLD) is a major public health issue caused by excessive alcohol consumption. ARLD encompasses a wide range of chronic liver lesions, alcohol-related liver cirrhosis being the most severe and harmful state. Variations in the genes encoding the enzymes, which play an active role in ethanol metabolism, might influence alcohol exposure and hence be considered as risk factors of developing cirrhosis. Read More

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Probing functional interactions between cytochromes P450 with principal component analysis of substrate saturation profiles and targeted proteomics.

Arch Biochem Biophys 2021 May 28;708:108937. Epub 2021 May 28.

Department of Chemistry, Washington State University, Pullman, WA, 99164, USA. Electronic address:

We investigated the correspondence between drug metabolism routes and the composition of the P450 ensemble in human liver microsomes (HLM). As a probe, we used Coumarin 152 (C152), a fluorogenic substrate metabolized by multiple P450 species. Studying the substrate-saturation profiles (SSP) in seven pooled HLM preparations, we sought to correlate them with the P450 pool's composition characterized by targeted proteomics. Read More

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Cytochrome P450 2E1 (CYP2E1) positively regulates lipid catabolism and induces browning in 3T3-L1 white adipocytes.

Life Sci 2021 Aug 24;278:119648. Epub 2021 May 24.

Department of Biotechnology, Daegu University, Gyeongsan, Gyeongbuk 38453, Republic of Korea. Electronic address:

Aims: Browning induction (beiging) of white adipocytes is an emerging prospective strategy to defeat obesity and its related metabolic disorders. Cytochrome P450 2E1 (CYP2E1), a membrane protein which belongs to the cytochrome P450 superfamily, reportedly functions in the xenobiotic metabolism in the body, especially ethanol metabolism. Although previous studies have reported the effect of CYP2E1 on obesity in animal models, the data remains controversial. Read More

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TA allele of rs2070673 in the CYP2E1 gene is associated with lobular inflammation and nonalcoholic steatohepatitis in patients with biopsy-proven nonalcoholic fatty liver disease.

J Gastroenterol Hepatol 2021 May 24. Epub 2021 May 24.

NAFLD Research Center, Department of Hepatology, The First Affiliated Hospital of Wenzhou Medical University, Wenzhou, China.

Background And Aim: Cytochrome P450 2E1 (CYP2E1) plays a role in lipid metabolism, and by increasing hepatic oxidative stress and inflammation, the upregulation of CYP2E1 is involved in development of nonalcoholic steatohepatitis (NASH). We aimed to explore the relationship between CYP2E1-333A>T (rs2070673) and the histological severity of nonalcoholic fatty liver disease (NAFLD).

Methods: We studied 438 patients with biopsy-proven NAFLD. Read More

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The p53/p21/p16 and PI3K/Akt signaling pathways are involved in the ameliorative effects of maltol on D-galactose-induced liver and kidney aging and injury.

Phytother Res 2021 May 24. Epub 2021 May 24.

College of Chinese Medicinal Materials, Jilin Agricultural University, Changchun, China.

Successive evidence has established that maltol, a flavor-enhancing agent, could provide resistance to oxidative stress-induced tissue injury in various animal models though its benefits for aging-induced liver and kidney injuries are still undetermined. In the present work, for demonstrating maltol's ameliorative effect and probable mechanism against aging-induced liver and kidney injuries, D-galactose (D-Gal)-induced animal in vivo and HEK293 cells in vitro models were established and results demonstrated that long-term D-Gal treatment increases the accumulation of advanced glycation end products (AGEs) in liver and kidney tissues, mitigates cell viability, and arrests the cycle. Interestingly, 4-weeks maltol treatment at 50 and 100 mg/kg activated aging-associated proteins including p53, p21, and p16 followed by inhibiting malondialdehyde (MDA)'s over-production and increasing the levels of antioxidant enzymes. Read More

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Drug-induced-acute liver failure: A critical appraisal of the thioacetamide model for the study of hepatic encephalopathy.

Toxicol Rep 2021 30;8:962-970. Epub 2021 Apr 30.

Department of Hepatology CA-3163, Rigshospitalet, Copenhagen University Hospital, Blegdamsvej 9, 2100, Copenhagen, Denmark.

Hepatic encephalopathy (HE) following acute and chronic liver failure is defined as a complex of neuropsychiatric abnormalities, such as discrete personal changes, sleep disorder, forgetfulness, confusion, and decreasing the level of consciousness to coma. The use and design of suitable animal models that represent clinical features and pathological changes of HE are valuable to map the molecular mechanisms that result in HE. Among different types of animal models, thioacetamide (TAA) has been used extensively for the induction of acute liver injury and HE. Read More

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Mechanism of Huo-Xue-Qu-Yu Formula in Treating Nonalcoholic Hepatic Steatosis by Regulating Lipid Metabolism and Oxidative Stress in Rats.

Evid Based Complement Alternat Med 2021 29;2021:6026319. Epub 2021 Apr 29.

School of Chinese Materia Medica, Zhejiang Pharmaceutical College, Ningbo 310053, China.

Huo-Xue-Qu-Yu formula (HXQYF) is a prescription consisting of leaf and Pall. for treating hyperlipidemia and NAFLD in China. Here, we investigated the hepatic and renal function, oxidative stress and lipid metabolism, and potential mechanisms of HXQYF on nonalcoholic fatty liver disease (NAFLD) rat models. Read More

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Effect of fucoidan on ethanol-induced liver injury and steatosis in mice and the underlying mechanism.

Food Nutr Res 2021 20;65. Epub 2021 Apr 20.

Department of Biochemistry and Molecular Biology, Basic Medical College, Qingdao University of Medicine, Qingdao, PR China.

Background: Alcoholic liver disease is caused as a result of chronic alcohol consumption. In this study, we used an alcoholic liver injury mouse model to investigate the effect of fucoidan on ethanol-induced liver injury and steatosis and the underlying mechanisms.

Methods: All mice were randomly divided into four groups: 1) control group, 2) model group, 3) diammonium glycyrrhizinate treatment group (200 mg/kg body weight), and 4) fucoidan treatment group (300 mg/kg body weight). Read More

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A Decade's Review of miRNA: a Center of Transcriptional Regulation of Drug-Metabolizing Enzymes and Transporters Under Hypoxia.

Curr Drug Metab 2021 May 13. Epub 2021 May 13.

Medical college, Qinghai University, Xining, China.

Background: Hypoxia has a negative effect on the cardiovascular system, nervous system, and metabolism, which contributes to potential changes in drug absorption, distribution, metabolism, and excretion (ADME). However, hypoxia can also alter the expression of microRNA (miRNA), thereby regulating drug-metabolizing enzymes, transporters, and ADME genes, such as hypoxia-inducible factor, inflammatory cytokine, nuclear receptor, etc. Therefore, it is crucial to study the role of miRNA in the regulation of drug-metabolizing enzymes and transporters under hypoxia. Read More

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Spatial Reconstruction of the Early Hepatic Transcriptomic Landscape after an Acetaminophen Overdose using Single-cell RNA Sequencing.

Toxicol Sci 2021 May 12. Epub 2021 May 12.

Department of Pharmacology, Toxicology & Therapeutics, University of Kansas Medical Center, Kansas City, KS 66160, USA.

An acetaminophen (APAP) overdose is the most common cause of acute liver failure in the United States. A hallmark characteristic of APAP hepatotoxicity is centrilobular necrosis. General, innate mechanisms such as lower amounts of GSH and higher Cyp2e1 expression in pericentral (PC) hepatocytes are known to contribute to the differences in susceptibility to cell injury between periportal (PP) hepatocytes and PC hepatocytes. Read More

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, , and genetic polymorphisms and their associations with susceptibility to antituberculosis drug-induced liver injury in Thai tuberculosis patients.

Heliyon 2021 Apr 20;7(4):e06852. Epub 2021 Apr 20.

Department of Biochemistry, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand.

Antituberculosis drug-induced liver injury (ATDILI) is the common adverse reaction of antituberculosis drugs. Glutathione S-transferases (GSTs), which are phase II metabolizing enzymes for detoxification, are recognized as potential mediators of hepatotoxicity. However, role of s polymorphisms in ATDILI pathogenesis has never been observed in Thais. Read More

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Effects of Real-Ambient PM Exposure on Lung Damage Modulated by Nrf2.

Front Pharmacol 2021 23;12:662664. Epub 2021 Apr 23.

School of Public Health, Qingdao University, Qingdao, China.

Previous studies have shown that long-term exposure to fine particulate matter (PM) increases the morbidity and mortality of pulmonary diseases such as asthma, chronic obstructive pulmonary disease and pulmonary emphysema. Oxidative stress and inflammation play key roles in pulmonary damage caused by PM. Nuclear factor erythroid 2-related factor 2 (Nrf2) could regulate the expression of antioxidant and anti-inflammatory genes and is pivotal for protection against PM-induced oxidative stress. Read More

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In vitro study on the effect of cornin on the activity of cytochrome P450 enzymes.

BMC Complement Med Ther 2021 May 9;21(1):138. Epub 2021 May 9.

Clinical research center, Shanghai Baoshan Luodian Hospital, No.121 Luoxi Road, Baoshan District, Shanghai, 201908, China.

Background: Cornin is a commonly used herb in cardiology for its cardioprotective effect. The effect of herbs on the activity of cytochrome P450 enzymes (CYP450s) can induce adverse drug-drug interaction even treatment failure. Therefore, it is necessary to investigate the effect of cornin on the activity of CYP450s, which can provide more guidance for the clinical application of cornin. Read More

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Hepatic Cytochrome P450 Abundance and Activity in the Developing and Adult Göttingen Minipig: Pivotal Data for PBPK Modeling.

Front Pharmacol 2021 15;12:665644. Epub 2021 Apr 15.

Comparative Perinatal Development, Department of Veterinary Sciences, Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, University of Antwerp, Wilrijk, Belgium.

The Göttingen Minipig is gaining ground as nonrodent species in safety testing of drugs for pediatric indications. Due to developmental changes in pharmacokinetics and pharmacodynamics, physiologically based pharmacokinetic (PBPK) models are built to better predict drug exposure in children and to aid species selection for nonclinical safety studies. These PBPK models require high quality physiological and ADME data such as protein abundance of drug metabolizing enzymes. Read More

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Ovariectomy-Induced Hepatic Lipid and Cytochrome P450 Dysmetabolism Precedes Serum Dyslipidemia.

Int J Mol Sci 2021 Apr 26;22(9). Epub 2021 Apr 26.

Centre for Experimental Medicine, Institute for Clinical and Experimental Medicine, 14021 Prague, Czech Republic.

Ovarian hormone deficiency leads to increased body weight, visceral adiposity, fatty liver and disorders associated with menopausal metabolic syndrome. To better understand the underlying mechanisms of these disorders in their early phases of development, we investigated the effect of ovariectomy on lipid and glucose metabolism. Compared to sham-operated controls, ovariectomized Wistar female rats markedly increased whole body and visceral adipose tissue weight ( ˂ 0. Read More

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Pogostone inhibits the activity of CYP3A4, 2C9, and 2E1 .

Pharm Biol 2021 Dec;59(1):532-536

Department of Pharmacy, People's Hospital of Rizhao, Rizhao, China.

Context: Pogostone possesses various pharmacological activities, which makes it widely used in the clinic. Its effect on the activity of cytochrome P450 enzymes (CYP450s) could guide its clinical combination.

Objective: To investigate the effect of pogostone on the activity of human CYP450s. Read More

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December 2021

Drug-drug interaction potential and clinical pharmacokinetics of enerisant, a novel potent and selective histamine H receptor antagonist.

Xenobiotica 2021 Jul 28;51(7):786-795. Epub 2021 Apr 28.

Drug Metabolism and Pharmacokinetics, Drug Safety and Pharmacokinetics Laboratories, Research Headquarters, Taisho Pharmaceutical Co., Ltd., Saitama, Japan.

We evaluated the drug-drug interaction (DDI) potential of enerisant (TS-091), a histamine H receptor antagonist/inverse agonist, mediated by cytochrome P450 (CYP) and transporters, as well as the pharmacokinetics of enerisant in healthy male subjects.Enerisant did not inhibit CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4 and did not induce CYP1A2, CYP2B6, or CYP3A4. Enerisant inhibited organic cation transporter 2, multidrug and toxin extrusion protein (MATE) 1, and MATE2-K, but not P-glycoprotein (P-gp), breast cancer resistance protein, organic anion transporting polypeptide (OATP) 1B1, OATP1B3, organic anion transporter (OAT) 1, or OAT3. Read More

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PPARα agonist WY-14,643 enhances ethanol metabolism in mice: Role of catalase.

Free Radic Biol Med 2021 Jun 20;169:283-293. Epub 2021 Apr 20.

Department of Biomedical Sciences, Joan C. Edwards School of Medicine, Marshall University, 1700 3rd Avenue, Huntington, WV, 25755, USA; Department of Clinical and Translational Sciences, Joan C. Edwards School of Medicine, Marshall University, Huntington, WV, 25755, USA. Electronic address:

Peroxisome proliferator-activated receptor α (PPARα), a fatty acid oxidation regulator, inhibits alcohol-induced fatty liver (AFL). PPARα agonist WY-14,643 ameliorates AFL. Nicotine enhances AFL. Read More

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Plasma cholinesterase activity is influenced by interactive effect between omethoate exposure and CYP2E1 polymorphisms.

J Environ Sci Health B 2021 19;56(5):477-482. Epub 2021 Apr 19.

Department of Occupational Health and Occupational Disease, College of Public Health, Zhengzhou University, Zhengzhou, Henan, P.R. China.

The aim of this study was to explore the association between metabolizing enzyme gene polymorphisms and the decrease in cholinesterase activity induced by omethoate exposure. A total of 180 workers exposed to omethoate over an extended period were recruited along with 115 healthy controls. Cholinesterase activity in whole blood, erythrocyte, and plasma was detected using acetylthiocholine and the dithio-bis-(nitrobenzoic acid) method. Read More

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Structural characterization and hepatoprotective activity of a galactoglucan from Poria cocos.

Carbohydr Polym 2021 Jul 24;263:117979. Epub 2021 Mar 24.

School of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui, 230012, China; Anhui Province Key Laboratory of Chinese Medicinal Formula, Hefei, Anhui, 230012, China; Institute of Pharmaceutics, Anhui Academy of Chinese Medicine, Hefei, Anhui, 230012, China. Electronic address:

To find the polysaccharide with hepatoprotective activity from Poria cocos and clarify its structure, a galactoglucan (PCP-1C) with a molecular weight of 17 kDa was purified from the Poria cocos sclerotium by column chromatography and activity evaluation in the present work. It was composed of galactose, glucose, mannose, and fucose in a molar percentage of 43.5: 24. Read More

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Obesity alters the ovarian proteomic response to zearalenone exposure.

Biol Reprod 2021 Apr 14. Epub 2021 Apr 14.

Department of Animal Science and Interdepartmental Toxicology Graduate Program, Iowa State University, Ames IA 50011.

Zearalenone (ZEN), a non-steroidal estrogenic mycotoxin, is detrimental to female reproduction. Altered chemical biotransformation, depleted primordial follicles and a blunted genotoxicant response have been discovered in obese female ovaries, thus, this study investigated the hypothesis that obesity would enhance ovarian sensitivity to ZEN exposure. Seven week old female wild type non-agouti KK. Read More

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