The Engagement of Cytochrome P450 Enzymes in Tryptophan Metabolism by Anna Haduch, Ewa Bromek, Wojciech Kuban, Władysława Anna Daniel

“…Recent studies indicate that serotonin can also be synthesized by cytochrome P450 (CYP), via the CYP2D6-mediated 5-methoxytryptamine O-demethylation, while melatonin is catabolized by CYP1A2, CYP1A1 and CYP1B1 via aromatic 6-hydroxylation and by CYP2C19 and CYP1A2 via O-demethylation. …”
Get full text

Duloksetyna – profil farmakologiczny i kliniczny leku z grupy inhibitorów zwrotnego wychwytu serotoniny i noradrenaliny by Marcin Wojtera, Tomasz Sobów

“…Duloksetyna wiąże się u ludzi z białkami osocza w 96%, jest intensywnie metabolizowana przez CYP1A2 i CYP2D6. Z uwagi na intensywny metabolizm przez CYP1A2 substancje hamujące ten enzym – fluwoksamina, ciprofloksacyna czy enoksacyna – zdecydowanie zwiększają stężenie duloksetyny i mogą spowodować wystąpienie objawów toksycznych. …”
Get full text

In vitro characterization of the furin inhibitor MI-1851: Albumin binding, interaction with cytochrome P450 enzymes and cytotoxicity by Erzsébet Pászti-Gere, Anna Szentkirályi-Tóth, Pál Szabó, Torsten Steinmetzer, Eszter Fliszár-Nyúl, Miklós Poór

“…Furthermore, the impacts of MI-1851 on human microsomal hepatic cytochrome P450 (CYP) 1A2, 2C9, 2C19, 2D6 and 3A4 activities were assessed based on fluorometric assays. …”
Get full text

Immunonutrition and Hepatoprotectant Aspects of <i>Moringa Oleifera</i> Leaf Nanoemulsion Syrup as an Antituberculosis Adjuvant for Children with Tuberculosis by Nyoman Budhi Wirananda Setiawan, Agus Indra Yudhistira Diva Putra, Made Indira Dianti Sanjiwani, Agung Wiwiek Indrayani, Ida Ayu Ika Wahyuniari

“…As a hepatoprotectant, Moringa oleifera leaf nanoemulsion syrup work by reducing the side effects of conventional tuberculosis drugs such as rifampicin by suppressing the action of cytochrome p450 (CYP1A2 and CYP2B), thus decreases the production of toxic hydrazine which causes liver toxicity in tuberculosis patient. …”
Get full text

Sex-dependent effects of long-term clozapine or haloperidol medication on red blood cells and liver iron metabolism in Sprague Dawley rats as a model of metabolic syndrome by Marie-Luise Bouvier, Karin Fehsel, Andrea Schmitt, Eva Meisenzahl-Lechner, Wolfgang Gaebel, Martina von Wilmsdorff

“…Liver HRI was significantly elevated in male clozapine medicated rats. CYP1A2 was significantly reduced in clozapine medicated females. …”
Get full text

Building a Human Physiologically Based Pharmacokinetic Model for Aflatoxin B1 to Simulate Interactions with Drugs by Orphélie Lootens, Marthe De Boevre, Jia Ning, Elke Gasthuys, Jan Van Bocxlaer, Sarah De Saeger, An Vermeulen

“…AFB1 is mostly metabolised by cytochrome P450 (CYP) enzymes, namely, CYP1A2 and CYP3A4. As a consequence of chronic exposure, it is interesting to check for interactions with drugs taken concomitantly. …”
Get full text

Functional evaluation of genetic and environmental regulators of p450 mRNA levels. by Dazhi Wang, Zhengwen Jiang, Zhongyang Shen, Hui Wang, Beilan Wang, Weihua Shou, Hong Zheng, Xun Chu, Jinxiu Shi, Wei Huang

“…In this study, we measured the mRNA levels of seven major P450 genes (CYP1A1, CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4 and CYP3A5) in 96 liver biopsy samples from Chinese population. …”
Get full text

Pharmacokinetics and Pharmacogenetics of Apixaban by A. V. Savinova, M. M. Petrova, N. A. Shnayder, E. N. Bochanova, R. F. Nasyrova

“…Apixaban is mainly metabolized by CYP3A4 with minor contributions from CYP1A2, CYP2C8, CYP2C9, CYP2C19 and CYP2J2 isoenzymes. …”
Get full text

Prospective Prediction of Dapaconazole Clinical Drug–Drug Interactions Using an In Vitro to In Vivo Extrapolation Equation and PBPK Modeling by Natalícia de Jesus Antunes, Fernanda de Lima Moreira, Karin Kipper, Lewis Couchman, Daniel Temponi Lebre, Atholl Johnston, Gilberto De Nucci

“…The in vitro dapaconazole inhibition was observed for all isoforms investigated, including CYP1A2 (IC₅₀ of 3.68 µM), CYP2A6 (20.7 µM), 2C8 (104.1 µM), 2C9 (0.22 µM), 2C19 (0.05 µM), 2D6 (0.87 µM), and 3A4 (0.008–0.03 µM). …”
Get full text

Protein Abundance of Drug Metabolizing Enzymes in Human Hepatitis C Livers by Marek Drozdzik, Joanna Lapczuk-Romanska, Christoph Wenzel, Lukasz Skalski, Sylwia Szeląg-Pieniek, Mariola Post, Arkadiusz Parus, Marta Syczewska, Mateusz Kurzawski, Stefan Oswald

“…In the Child–Pugh class C livers, CYP1A2 was found to be reduced (to 52%). A significant trend in down-regulation of the protein abundance was documented for CYP1A2, CYP2C9, CYP3A4, CYP2E1, UGT2B7, and UGT2B15. …”
Get full text

Study on the liver Drug’s dominant metabolic enzymes for six effective components of the Huang qi Liuyi decoction by Qun Wang, Tiantian Tang, Zengguang Wu, Hong Yang, Yuan Gao, Yuan Gao, Shiyu Zhang, Xinli Song, Xinli Song, Xiaolan Chen, Xiaolan Chen

“…The chemical inhibitors of CYP2E1 and CYP1A2 inhibit the metabolism of calycosin-glucuronide. …”
Get full text

Age-associated changes of cytochrome P450 and related phase-2 gene/proteins in livers of rats by Shang-Fu Xu, An-Ling Hu, Lu Xie, Jia-Jia Liu, Qin Wu, Jie Liu

“…The protein expression of CYP1A2, CYP2B1, CYP2E1, CYP3A1, CYP4A1, and CYP7A1 corresponded the trend of mRNA changes. …”
Get full text

In vitro evaluation suggests fenfluramine and norfenfluramine are unlikely to act as perpetrators of drug interactions by Parthena Martin, Maciej Czerwiński, Pallavi B. Limaye, Brian W. Ogilvie, Steven Smith, Brooks Boyd

“…FFA and nFFA were direct in vitro inhibitors of CYP2D6 (IC50, 4.7 and 16 µM, respectively) but did not substantially inhibit CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, or CYP3A4/5. …”
Get full text

Effects of cigarette smoking on older chinese men treated with clopidogrel monotherapy or aspirin monotherapy: a prospective study by Yulun Cai, Weihao Xu, Hongbin Liu, Fan Wang, Lei Duan, Huiying Li, Man Li, Yuerui Li, Lina Han, Hunan Xiao

“…Long-term cigarette smoking may contribute to increased variations in CYP1A2*1F, but the variations do not fully explain the smoking paradox.…”
Get full text

piR-39980 mediates doxorubicin resistance in fibrosarcoma by regulating drug accumulation and DNA repair by Basudeb Das, Neha Jain, Bibekanand Mallick

“…The authors reported that its inhibition lead to attenuated intracellular DOX accumulation, DOX-indued apoptosis and anti-proliferative effects in parental HT1080 cells, as well as DNA damage by regulating RRM2 and CYP1A2.…”
Get full text

Effect of Betanin, the Major Pigment of Red Beetroot (<i>Beta vulgaris</i> L.), on the Activity of Recombinant Human Cytochrome P450 Enzymes by Sung Ho Lim, Seoungpyo Bae, Ho Seon Lee, Hyo-Kyung Han, Chang-Ik Choi

“…Furthermore, betanin had no significant effect on CYP1A2, CYP2B6, or CYP2C9 induction in HepG2 cells. …”
Get full text

The Development and Validation of a Novel “Dual Cocktail” Probe for Cytochrome P450s and Transporter Functions to Evaluate Pharmacokinetic Drug-Drug and Herb-Drug Interactions by Mihwa Kwon, Ji-Hyeon Jeon, Min-Koo Choi, Im-Sook Song

“…This study was designed to develop and validate a 10 probe drug cocktail named “Dual Cocktail”, composed of caffeine (Cyp1a2 in rat and CYP1A2 in human, 1 mg/kg), diclofenac (Cyp2c11 in rat and CYP2C9 in human, 2 mg/kg), omeprazole (Cyp2c11 in rat and CYP2C19 in human, 2 mg/kg), dextromethorphan (Cyp2d2 in rat and CYP2D6 in human, 10 mg/kg), nifedipine (Cyp3a1 in rat and CYP3A4 in human, 0.5 mg/kg), metformin (Oct1/2 in rat and OCT1/2 in human, 0.5 mg/kg), furosemide (Oat1/3 in rat and OAT1/3 in human, 0.1 mg/kg), valsartan (Oatp2 in rat and OATP1B1/1B3 in human, 0.2 mg/kg), digoxin (P-gp in rat and human, 2 mg/kg), and methotrexate (Mrp2 in rat and MRP2 in human, 0.5 mg/kg), for the evaluation of pharmacokinetic drug–drug and herb-drug interactions through the modulation of a representative panel of CYP enzymes or transporters in rats. …”
Get full text

Inhibition of Cytochrome P450 Activities by Extracts of Hyptis verticillata Jacq.: Assessment for Potential HERB-Drug Interactions by David Picking, Bentley Chambers, James Barker, Iltaf Shah, Roy Porter, Declan P Naughton, Rupika Delgoda

“…Individual screening of these phytochemicals against the activity of CYP1A2 identified yatein as a moderate inhibitor (71.9 μM), likely to contribute to the plant extract’s potent bioactivity. …”
Get full text

Data‐driven personalization of a physiologically based pharmacokinetic model for caffeine: A systematic assessment by Rebekka Fendt, Ute Hofmann, Annika R. P. Schneider, Elke Schaeffeler, Rolf Burghaus, Ali Yilmaz, Lars Mathias Blank, Reinhold Kerb, Jörg Lippert, Jan‐Frederik Schlender, Matthias Schwab, Lars Kuepfer

“…In the third step, virtual twins matching individual demography, physiology, and CYP1A2 activity considerably improved the simulation results. …”
Get full text

ROLE OF GENETIC FACTORS IN THE DEVELOPMENT OF CLOPIDOGREL RESISTANCE AMONG PATIENTS REFERRED FOR PERCUTANEOUS CORONARY INTERVENTIONS by S. T. Matskeplishvili, E. B. Prokhorchuk, Ya. E. Arutyunova, I. V. Koksheneva, L. S. Shakhnazaryan, B. R. Sandukhadze, K. G. Skryabin, A. V. Melerzanov, Yu. I. Buziashvili

“…No significant inter-group differences were observed for other polymorphisms (CYP2C9 (rs1057910*3); CYP3A4 (rs2242480); CYP2B6 (rs3211371 (5*)); CYP3A5 (rs28365083*2, rs776746); and CYP1A2 (rs762551)).Conclusion. The degree of platelet aggregation in patients on DAT is related to their genetic status. …”
Get full text