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Objective: To evaluate the role of the Cytochrome P450 3A4*22 mutation on the postoperative analgesic effects of lidocaine.
Methods: The study was conducted at the Pakistan Ordinance Factories Hospital, Wah Cantt, Pakistan, from March 2021 to December 2022, and comprised adult patients undergoing elective laparoscopic cholecystectomy. The patients were randomised into intervention group A and control group B. Patients in group A were given a bolus dose of lidocaine 2mg/kg in addition to the standard anaesthesia protocol, while the patients in group B received the standard anaesthesia protocol. Visual analog scale was used at 6 hours and 12 hours post-surgery. Blood samples for genetic analysis were taken after the start of surgery. Data was analysed using SPSS 26.
Results: Of the 300 patients, 215(71.7%) were females and 85(28.3%) were males. The overall mean age was 48.49±11.34 years and mean body mass index was 23.40±7.0546kg/m2. However, owing to unsuccessful genotyping, 42(14%) patients could not be evaluated. Patients with a GA allele sequence with GG in the Cytochrome P450 3A4*22 (rs35599367) had a higher postoperative pain threshold than those with GG and AA alleles alone (p<0.01).
Conclusions: Patients with a GA allele succession with GG in the Cytochrome P450 3A4*22 (rs35599367) had a higher postoperative aggravation edge than those with GG and AA alleles alone.
Rct No: IRCT-20220830059302N1.
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http://dx.doi.org/10.47391/JPMA.20095 | DOI Listing |
Chembiochem
September 2025
Science Center for Future Foods, Jiangnan University, 1800 Lihu Road, Wuxi, Jiangsu, 214122, China.
Natural products exhibit a wide range of biological activities and are the crucial resources for drug development and compound modification. Cytochrome P450 enzymes (P450s, CYP) are a class of multifunctional and stereoselective biocatalysts that utilize heme as a cofactor and can be employed in the biosynthesis of natural products. With the development of biotechnology, P450s have been widely applied in the synthesis of natural products.
View Article and Find Full Text PDFBioorg Chem
September 2025
Entomology Department, Faculty of Science, Ain Shams University, Abbassia, 11566, Cairo, Egypt.
A strategically engineered, eco-conscious synthetic platform was developed to access a novel library of eighteen polyfunctionalized pyridine-based heterocycles through high-efficiency multicomponent and annulation strategies, using 2-amino-4-(4-chlorophenyl)-6-(p-tolyl)nicotinonitrile (M) as a privileged core. Structural diversity was maximized by integrating potent pharmacophores, including pyrido[2,3-d]pyrimidines, naphthyridines, triazines, and fused pyrrolo/tetrazolo motifs, via both conventional and accelerated (microwave/ultrasound-assisted) routes, affording excellent yields with high structural fidelity as confirmed by IR, H/C NMR, and mass spectrometry. Biological evaluation revealed that all synthesized compounds had excellent larvicidal efficacy against Culex pipiens larvae, especially 15 and 9, emerging as lead candidates that exhibited exceptional LC₅₀ values of 0.
View Article and Find Full Text PDFSci Adv
September 2025
Biology Department, Brookhaven National Laboratory, Upton, NY 11973, USA.
Sterols are essential isoprenoid derivatives that contribute to membrane structure and function. In plants, they also serve as precursors to phytohormones and specialized metabolites important for development, defense, and health. Although the sterol biosynthetic pathway is considered well-characterized, we report the discovery of a plant-specific cytochrome -like protein, CB5LP, as a critical component of phytosterol biosynthesis.
View Article and Find Full Text PDFMol Ther Methods Clin Dev
June 2025
Eisai Co., Ltd., Tsukuba Research Laboratories, 5-1-3, Tokodai, Tsukuba, Ibaraki 300-2635, Japan.
Liver-humanized chimeric mice (PXB-mice) are widely utilized for predicting human pharmacokinetics (PK) and as human disease models. However, residual metabolic activity of mouse hepatocytes in chimeric mice can interfere with accurate human PK estimation. Lipid nanoparticle (LNP)-formulated small interfering RNA (siRNA) treatment makes it possible to eliminate the shortcomings of chimeras and create new models.
View Article and Find Full Text PDFFront Vet Sci
August 2025
College of Food Science, Guangdong Provincial Key Laboratory of Food Quality and Safety, South China Agricultural University, Guangzhou, China.
Introduction: Tenvermectin (TVM) is a novel avermectin-class drug that has attracted attention for its superior antiparasitic potency, low toxicity, and broad-spectrum activity. However, uncertainty about its interaction with cytochrome P450 enzymes (CYPs) has raised concerns about potential therapeutic failure, increased risk of toxicity, dangerous drug combinations, and prolonged discontinuation periods.
Method: To address these critical safety concerns, we conducted a systematic comparative study using a highly selective and quantitatively accurate substrate conversion assay to assess and compare the effects of TVM and ivermectin (IVM) on the activities of key CYPs (CYP1A1/2, 2B1, 2C6, 2D2, and 3A1/2).