193,083 results match your criteria cytochrome p450

Stigmasterol isolated from the chloroform fraction of Benth fruit induces mitochondrial-dependent apoptosis in rat liver.

J Complement Integr Med 2021 May 10. Epub 2021 May 10.

Laboratories for Biomembrane Research and Biotechnology, Department of Biochemistry, University of Ibadan, Ibadan, Nigeria.

Objectives: Decoction of fruit is used in folkloric medicine for treating dysmenorrhea and gonorrhea. Phytochemicals from may be potent in inducing mitochondrial-dependent apoptosis via the opening of the mitochondrial permeability transition (MPT) pore. Therefore, this study investigated the effects of stigmasterol isolated from the chloroform fraction of (CFAB) and also the increasing concentration of CFAB on the opening of rat liver mitochondrial permeability transition (MPT) pore. Read More

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The history, taxonomy, and geographic origins of an introduced African monkey in the southeastern United States.

Primates 2021 May 8. Epub 2021 May 8.

Biological Sciences Department, Florida Atlantic University, Boca Raton, USA.

The origins and taxonomy of the introduced vervet monkey population in Dania Beach, Florida has been unconfirmed due to a lack of documentation and genetic research. Our goal was to determine the introduction history, species identification, and geographic origins of the monkeys. Through interviews, historical archives, and popular media, we traced the monkeys to an escape from the Dania Chimpanzee Farm in 1948. Read More

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Indigo enhances wound healing activity of Caco-2 cells via activation of the aryl hydrocarbon receptor.

J Nat Med 2021 May 7. Epub 2021 May 7.

Pharmacology Laboratory, Department of Biomedical Sciences, College of Life Sciences, Ritsumeikan University, 1-1-1 Noji Higashi, Kusatsu, Shiga, 525-8577, Japan.

Indigo Naturalis, also known as Qing Dai (QD) is a compound obtained from Indigofera tinctoria, Isatis tinctoria, and Polygonum tinctoria and is known to ameliorate refractory ulcerative colitis (UC) by an unknown mechanism. QD maintains both homeostasis and the integrity of colon epithelia in mice that have experimentally induced colitis. The primary component of QD, indigo, comprises 42. Read More

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Impact of Clotrimazole Fungal Prophylaxis on Tacrolimus Exposure in Kidney Transplant Recipients: A Retrospective Study.

Transplant Proc 2021 May 4. Epub 2021 May 4.

Department of Pharmacy, Einstein Medical Center Philadelphia, Philadelphia, Pennsylvania. Electronic address:

Tacrolimus, an immunosuppressant prescribed to reduce the risk of organ rejection, is metabolized by cytochrome P450 and is a substrate for P-glycoprotein. Many medications affect tacrolimus concentrations, making it difficult to maintain exposure within its narrow therapeutic index. Clotrimazole troches, prescribed to posttransplant recipients immediately for the first 30 days for oral candidiasis prevention, are considered nonsystemic. Read More

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Transcriptome analysis provides insights into long noncoding RNAs in medaka gonads.

Comp Biochem Physiol Part D Genomics Proteomics 2021 Apr 29;39:100842. Epub 2021 Apr 29.

International Research Center for Marine Biosciences, Ministry of Science and Technology, Shanghai Ocean University, Shanghai 201306, China; Key Laboratory of Freshwater Aquatic Genetic Resources, Ministry of Agriculture and Rural Affairs, Shanghai Ocean University, Shanghai 201306, China. Electronic address:

Long non-coding RNAs (lncRNAs) are gradually regarded as regulators in sex determination and gonad development of various animals. Medaka (Oryzias latipes) is an excellent reproductive research model with sex-determining genes. However, the regulation of gonadal lncRNAs on medaka reproductive development remains unknown. Read More

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Tumour necrosis factor-α (TNF-α) enhances dietary carcinogen-induced DNA damage in colorectal cancer epithelial cells through activation of JNK signaling pathway.

Toxicology 2021 May 4:152806. Epub 2021 May 4.

Section of Biomolecular Medicine. Electronic address:

Colorectal cancer (CRC) is the third most common cancer worldwide and the second leading cause of cancer death. Benzo[a]pyrene (BaP) and 2-amino-1-methyl-6-phenylimidazol [4,5-b] pyridine (PhIP) present in cooked meat are pro-carcinogens and considered to be potential risk factors for CRC. Their carcinogenic and mutagenic effects require metabolic activation primarily by cytochrome P450 1 family enzymes (CYPs); the expression of these enzymes can be modulated by aryl hydrocarbon receptor (AhR) activation and the tumour microenvironment, involving mediators of inflammation. Read More

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Covalent Conjugation of Single-Walled Carbon Nanotube with CYP101 mutant for Direct Electrocatalysis.

Anal Biochem 2021 May 4:114204. Epub 2021 May 4.

Department of Chemical Sciences, Tata Institute of Fundamental Research, Homi Bhabha Road, Colaba, Mumbai, 400 005, INDIA. Electronic address:

Covalent linkage between the single-walled carbon nanotube (SWCNT) and CYP101 through a specific site of the enzyme can provide a novel method of designing efficient enzyme electrodes using this prototype cytochrome P450 enzyme. We have chemically modified the SWCNT with linker 4-carboxy phenyl maleimide (CPMI) containing maleimide functional groups. The enzyme was covalently attached on to the SWCNT through the maleimide group of the linker (CPMI) to the thiolate group of the surface exposed Cys58 or Cys136 of the CYP101 forming a covalently immobilized protein on the nanotube. Read More

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Risk prediction of drug-drug interaction potential of phenytoin and miconazole topical formulations.

Chem Biol Interact 2021 May 4:109498. Epub 2021 May 4.

School of Life and Pharmaceutical Sciences, Dalian University of Technology, Panjin, 124221, China. Electronic address:

The drug-drug interaction (DDI) risk of phenytoin with several topical formulations of miconazole is still unclear. The present investigation conducted in vitro in vivo extrapolation to predict the potential risks. Our data indicated that miconazole potently inhibited phenytoin hydroxylation in both pooled HLMs and recombinant cytochrome P450 2C9 (CYP2C9) with the K values of 125 ±7 nM and 30 ± 2 nM, respectively. Read More

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Outcomes of a multi-ethnic Asian population on combined treatment with clopidogrel and omeprazole in 12,440 patients.

J Thromb Thrombolysis 2021 May 6. Epub 2021 May 6.

National University Heart Centre, National University of Singapore, Singapore, Singapore.

Omeprazole is commonly co-prescribed with clopidogrel. Clopidogrel requires bio-activation by cytochrome P450 CYP2C19. Omeprazole may reduce clopidogrel's antithrombotic efficacy by inhibiting CYP2C19. Read More

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Genetic Variation and Its Implication for Vivax Malaria Treatment in Madagascar.

Front Pharmacol 2021 20;12:654054. Epub 2021 Apr 20.

Center for Global Health and Diseases, Case Western Reserve University School of Medicine, Cleveland, OH, United States.

is one of the five human malaria parasite species, which has a wide geographical distribution and can cause severe disease and fatal outcomes. It has the ability to relapse from dormant liver stages (hypnozoites), weeks to months after clearance of the acute blood-stage infection. An 8-aminoquinoline drug primaquine (PQ) can clear the hypnozoites, and thus can be used as an anti-relapse therapeutic agent. Read More

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Redescription of - a ubiquitous intertidal hoplonemertean found along the West Coast of North America.

Zookeys 2021 14;1031:1-17. Epub 2021 Apr 14.

Oregon Institute of Marine Biology, University of Oregon, Charleston, OR, USA Universidade de São Paulo São Paulo Brazil.

Stimpson, 1857, a barnacle predator, is one of the most common and conspicuous intertidal nemerteans found along the West Coast of North America from Alaska to California, but it is currently referred to by the wrong name. Briefly described without designation of type material or illustrations, the species was synonymized with the Atlantic look-alike, (Johnston, 1837) by Coe. Here we present morphological and molecular evidence that is distinct from . Read More

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Architecture of the membrane-bound cytochrome c heme lyase CcmF.

Nat Chem Biol 2021 May 6. Epub 2021 May 6.

Institut für Biochemie, Albert-Ludwigs-Universität Freiburg, Freiburg, Germany.

The covalent attachment of one or multiple heme cofactors to cytochrome c protein chains enables cytochrome c proteins to be used in electron transfer and redox catalysis in extracytoplasmic environments. A dedicated heme maturation machinery, whose core component is a heme lyase, scans nascent peptides after Sec-dependent translocation for CXCH-binding motifs. Here we report the three-dimensional (3D) structure of the heme lyase CcmF, a 643-amino acid integral membrane protein, from Thermus thermophilus. Read More

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Cytochrome P450-epoxygenated fatty acids inhibit Müller glial inflammation.

Sci Rep 2021 May 6;11(1):9677. Epub 2021 May 6.

Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, Nashville, TN, USA.

Free fatty acid dysregulation in diabetics may elicit the release of inflammatory cytokines from Müller cells (MC), promoting the onset and progression of diabetic retinopathy (DR). Palmitic acid (PA) is elevated in the sera of diabetics and stimulates the production of the DR-relevant cytokines by MC, including IL-1β, which induces the production of itself and other inflammatory cytokines in the retina as well. In this study we propose that experimental elevation of cytochrome P450 epoxygenase (CYP)-derived epoxygenated fatty acids, epoxyeicosatrienoic acid (EET) and epoxydocosapentaenoic acid (EDP), will reduce PA- and IL-1β-induced MC inflammation. Read More

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Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.

Eur J Med Chem 2021 Apr 25;220:113453. Epub 2021 Apr 25.

School of Pharmacy, Xinxiang Medical University, Xinxiang, Henan, 453003, China. Electronic address:

LSD1 and HDAC are physical and functional related to each other in various human cancers and simultaneous pharmacological inhibition of LSD1 and HDAC exerts synergistic anti-cancer effects. In this work, a series of novel LSD1/HDAC bifunctional inhibitors with a styrylpyridine skeleton were designed and synthesized based on our previously reported LSD1 inhibitors. The representative compounds 5d and 5m showed potent activity against LSD1 and HDAC at both molecular and cellular level and displayed high selectivity against MAO-A/B. Read More

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Studying genetic population structure to shed light on the demographic explosion of the rare species Barbitistes vicetinus (Orthoptera, Tettigoniidae).

PLoS One 2021 6;16(5):e0250507. Epub 2021 May 6.

Department of Agronomy, Food, Natural resources, Animals and Environment (DAFNAE), University of Padua, Legnaro, PD, Italy.

Insect outbreaks usually involve important ecological and economic consequences for agriculture and forestry. The short-winged bush-cricket Barbitistes vicetinus Galvagni & Fontana, 1993 is a recently described species that was considered rare until ten years ago, when unexpected population outbreaks causing severe defoliations across forests and crops were observed in north-eastern Italy. A genetic approach was used to analyse the origin of outbreak populations. Read More

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Redescription and molecular identification of Isospora feroxis Berto, Luz, Flausino, Ferreira & Lopes, 2009 (Eimeriidae) from tyrant-flycatchers (Tyrannoidea) in South America.

Syst Parasitol 2021 May 6. Epub 2021 May 6.

Departamento de Biologia Animal, Instituto de Ciências Biológicas e da Saúde, Universidade Federal Rural do Rio de Janeiro, BR-465 km 7, 23897-000, Seropédica, Rio de Janeiro, Brazil.

In the present study Isospora feroxis Berto, Luz, Flausino, Ferreira & Lopes, 2009 is redescribed from the photosyntypes and from new samples from a short-crested flycatcher Myiarchus ferox (Gmelin), which is the type-host in the type-locality, the Marambaia Island in Southeastern Brazil. In addition, the yellow-olive flycatcher Tolmomyias sulphurescens Spix is recorded as a new host for this species, in a new locality, the Itatiaia National Park, in the interior of Southeastern Brazil, providing a preliminary genotypic characterization via sequencing of the mitochondrial cytochrome c oxidase subunit 1 (COI) gene. Micropyle and rough oöcyst wall are added to the description of I. Read More

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Effect of GLPG1205, a GPR84 Modulator, on CYP2C9, CYP2C19, and CYP1A2 Enzymes: In Vitro and Phase 1 Studies.

Clin Pharmacol Drug Dev 2021 May 6. Epub 2021 May 6.

Galapagos Biotech Ltd, Cambridge, UK.

GLPG1205 is a novel agent being investigated for the treatment of idiopathic pulmonary fibrosis. GLPG1205 may be concomitantly administered with pirfenidone in future clinical development; therefore, the potential for GLPG1205 to interact with enzymes involved in the metabolism of pirfenidone (cytochrome P450 [CYP] 1A2, CYP2C9, 2C19) was evaluated. In vitro experiments indicated weak inhibition of CYP1A2 and moderate but reversible inhibition of CYP2C9 and CYP2C19 by GLPG1205. Read More

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Delphinidin modulates JAK/STAT3 and MAPKinase signaling to induce apoptosis in HCT116 cells.

Environ Toxicol 2021 May 6. Epub 2021 May 6.

Department of Gastroenterology, First Affiliated Hospital of Xi'an Jiaotong University, Xi'an, Shaanxi, China.

Delphinidin is an anthocyanin that belongs to the group of flavonoids that exert numerous biological activities. However, the molecular mechanisms underlying the anticancer effects of delphinidin remain poorly understood. In our study we analyzed delphinidin modulate STAT-3 and MAPKinase signaling thereby inhbits cell proliferation and promote apoptosis. Read More

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Molecular Species Identification of Six Forensically Important Iranian Flesh Flies (Diptera).

J Arthropod Borne Dis 2020 Dec 31;14(4):416-424. Epub 2020 Dec 31.

Department of Cell and Molecular Biology, Faculty of Life Sciences and Biotechnology, Shahid Beheshti University, Tehran, Iran.

Background: Flesh flies (Diptera: Sarcophagidae) are considered as myiasis agents and important evidences in forensic investigations. However, their use has been restricted because, at all larval stages and female adults, morphological species identification is difficult or very challenging. This study investigated to test utility of mitochondrial cytochrome oxidase subunit I (mt-COI) sequences for differentiation of six forensically important Iranian flesh flies namely, , , , , and . Read More

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December 2020

Melatonin ameliorates myocardial injury by reducing apoptosis and autophagy of cardiomyocytes in a rat cardiopulmonary bypass model.

PeerJ 2021 15;9:e11264. Epub 2021 Apr 15.

Department of Cardiac Surgery, First Affiliated Hospital of Sun Yat-Sen University, Guangzhou, China.

Background: Myocardial injury is a frequent complication after cardiac surgery with cardiopulmonary bypass (CPB). This study aimed to test the hypothesis that melatonin could attenuate myocardial injury in a rat CPB model.

Methods: Eighteen male Sprague-Dawley rats were randomly divided into three groups,  = 6 for each group: the sham operation (SO) group, CPB group and melatonin group. Read More

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, a commonly consumed food, affects sirolimus level in a renal transplant recipient: a case report.

Ther Adv Drug Saf 2021 19;12:20420986211009358. Epub 2021 Apr 19.

Department of Nephrology, Hacettepe University Faculty of Medicine, Altindag, Ankara, Turkey.

Sirolimus is an immunosuppressive drug used to prevent graft rejection. Therapeutic drug monitoring is required as with other immunosuppressive drugs. Previous studies have shown the interactions between sirolimus and drugs that affect the activity of cytochrome P450 3A4 and P-glycoprotein. Read More

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Molecular identification of Uronema marinum (Protozoa, Ciliophora, Scuticociliatia) in cultured turbot (Psetta maxima) larvae.

Mustafa Türe

Vet Res Forum 2021 15;12(1):121-124. Epub 2021 Mar 15.

Department of Fisheries Health, Central Fisheries Research Institute, Trabzon, Turkey .

Scuticociliates are dangerous parasitic pathogens causing systemic tissue destruction and high mortality in marine fish worldwide. In this study, the first identification of (Ciliophora, Scuticociliatida) from cultured turbot () larvae using mitochondrial cytochrome c oxidase 1 (1) gene sequence as well as species-specific primers was reported. The mean prevalence values of infected fish were calculated, and partial sequencing obtained from the mitochondrial 1 gene region was also compared with isolates registered in the Genbank database. Read More

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Down regulation of lactate dehydrogenase initiates apoptosis in HeLa and MCF-7 cancer cells through increased voltage-dependent anion channel protein and inhibition of BCL2.

Oncotarget 2021 Apr 27;12(9):923-935. Epub 2021 Apr 27.

Department of Pathology, College of Medicine & Health Sciences, United Arab Emirates University, AlAin, UAE.

Malignant cells commonly use aerobic glycolysis for ATP production; this is known as the Warburg effect, where pyruvate is converted to lactate, by enzyme lactate dehydrogenase A (LDH-A). In this study, we have investigated the effect of inhibition of LDH-A on cells viability and identifying the mechanism of cell death in HeLa and MCF-7 cancer cells. Human cervical cancer HeLa cell line and breast cancer MCF-7 cell line were used to investigate the effect of inhibition of LDH-A by sodium oxamate on cell survival and proliferation using western blot, spectrophotometry, and immunofluorescent study. Read More

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Creation of a new class of radiosensitizers for glioblastoma based on the mibefradil pharmacophore.

Oncotarget 2021 Apr 27;12(9):891-906. Epub 2021 Apr 27.

Department of Therapeutic Radiology, Yale University School of Medicine, New Haven, CT 06510-8034, USA.

Glioblastoma (GBM) is the most common primary malignant tumor of the central nervous system with a dismal prognosis. Locoregional failure is common despite high doses of radiation therapy, which has prompted great interest in developing novel strategies to radiosensitize these cancers. Our group previously identified a calcium channel blocker (CCB), mibefradil, as a potential GBM radiosensitizer. Read More

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Metformin Attenuates ROS FOXO3 Activation in Immune Cells.

Front Immunol 2021 19;12:581799. Epub 2021 Apr 19.

Institute of Medical Immunology, Charité-Universitätsmedizin Berlin, Corporate Member of Freie Universität (FU) Berlin, Humboldt-Universität zu Berlin and Berlin Institute of Health (BIH), Berlin, Germany.

Forkhead box O 3 (FOXO3) is a transcription factor involved in cell metabolism, inflammation and longevity. Here, we investigated if metformin can activate FOXO3 in human immune cells and affects the subsequent level of reactive oxygen/nitrogen species (ROS/RNS) in immune cells. AMP-activated protein kinase (AMPK) and FOXO3 activation were investigated by immunoblot or flow cytometry (FC) analysis, respectively. Read More

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Evaluation of Gene Polymorphisms in Patients with Acid Peptic Disorders Treated with Esomeprazole.

Pharmgenomics Pers Med 2021 29;14:509-520. Epub 2021 Apr 29.

Basic Medical Science Department, Faculty of Health Sciences, Universidad Icesi, Cali, Colombia.

Background: is a highly polymorphic gene that encodes an enzyme with the same name and whose function is associated with the metabolism of many important drugs, such as proton pump inhibitors (such as esomeprazole, which is used for the treatment of acid peptic disease). Genetic variants in alter protein function and affect drug metabolism. This study aims to genotypically and phenotypically characterize the genetic variants in the gene in 12 patients with acid peptic disorders and different therapeutic profiles to proton pump inhibitor (PPI) drugs. Read More

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The first detection of Dicrocoelium chinensis sporocysts from the land snail Aegista vulgivaga in Gifu Prefecture, Japan.

J Vet Med Sci 2021 Apr 30. Epub 2021 Apr 30.

Faculty of Applied Biological Science, Gifu University.

Trematodes of the genus Dicrocoelium are one of the most common parasites in ruminant animals; however, their life cycles in Japan are unclear. To find the sporocysts of D. chinensis in the natural field, we sampled 269 land snails (14 species) at a location with high level infection of sika deer in Gifu Prefecture, Honshu Island, Japan in autumn between 2017 and 2019. Read More

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A graph theoretic model to understand the behavioral difference of PPCA among its paralogs towards recognition of DXCA.

J Biosci 2021 ;46

Advanced Computing and Microelectronics Unit, Indian Statistical Institute, Kolkata 700 108, India.

Among all the proteins of Periplasmic C type Cytochrome family obtained from cytochrome found in , only the Periplasmic C type Cytochrome A (PPCA) protein can recognize the deoxycholate (DXCA), while its other paralogs do not, as observed from the crystal structures. Though some existing works have used graph-theoretic approaches to realize the 3-D structural properties of proteins, its usage in the rationalisation of the physiochemical behavior of proteins has been very limited. To understand the driving force towards the recognition of DXCA exclusively by PPCA among its paralogs, in this work, we propose two graph theoretic models based on the combinatorial properties, namely, and , of the nucleotide bases and the amino acid residues, respectively. Read More

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January 2021


Drug Metab Dispos 2021 May 5. Epub 2021 May 5.

Novartis Institute for Biomedical Research, East Hanover, United States, United States.

Tropifexor (NVP-LJN452) is a highly potent, selective, non-steroidal, non-bile acid farnesoid X receptor (FXR) agonist for the treatment of nonalcoholic steatohepatitis (NASH). Its absorption, metabolism, and excretion were studied following a 1-mg oral dose of [C]tropifexor to four healthy male subjects. Mass balance was achieved with ~94% of the administered dose recovered in excreta through 312 hours collection period. Read More

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Drug Metab Dispos 2021 May 5. Epub 2021 May 5.

Department of Pharmaceutical Sciences, Washington State University, United States

The increasing incidence of ocular diseases has accelerated research into therapeutic interventions needed for the eye. Ocular enzymes play important roles in the metabolism of drugs and endobiotics. Various ocular drugs are designed as prodrugs that are activated by ocular enzymes. Read More

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