Two potent microsomal enzyme inducing agents, phenobarbital and flumecinol (Zixoryn) as well as the microsomal enzyme inhibitor chloramphenicol (Chlorocid) were given subcutaneously to newborn rats in the first 5 days of their life. Microsomal cytochrome P-450 and b5 content and various cytochrome P-450 and P-448 dependent enzyme activities were measured at the age of 20 weeks. Phenobarbital had positive imprint effect on aminopyrine N-demethylase activity in female and on aniline hydroxylase activity in male rats. Flumecinol had no imprint effect. Chloramphenicol had a positive imprint on aniline hydroxylase activity in male rats. Sex differences in microsomal enzyme activities were not affected by the xenobiotics used.
Download full-text PDF |
Source |
|---|
Publication Analysis
Top Keywords
Similar Publications
Quantitative analysis of the polar cod (Boreogadus saida) hepatic proteome highlights interconnected responses in cellular adaptation and defence mechanisms after dietary benzo[a]pyrene exposure.
Sci Total Environ
January 2025
Department of Arctic and Marine Biology, UiT The Arctic University of Norway, N-9037 Tromsø, Norway.
Increased industrial offshore activities in northern waters raise the question of impact of polycyclic aromatic hydrocarbons (PAHs) on key Arctic marine species. One of these is the ecologically important polar cod (Boreogadus saida), which is the primary food source for Arctic marine mammals and seabirds. In the present work, we have conducted the first comprehensive proteomics study with this species by exploring the effects of dietary PAH exposure on the hepatic proteome, using benzo[a]pyrene (BaP) as a PAH model-compound.
View Article and Find Full Text PDFStructure-activity relationship expansion and microsomal stability assessment of the 2-morpholinobenzoic acid scaffold as antiproliferative phosphatidylcholine-specific phospholipase C inhibitors.
RSC Med Chem
January 2025
School of Chemical Sciences, University of Auckland Auckland 1010 New Zealand
Dysregulation of choline phospholipid metabolism and overexpression of phosphatidylcholine-specific phospholipase C (PC-PLC) is implicated in various cancers. Current known enzyme inhibitors include compounds based on a 2-morpholino-5--benzylamino benzoic acid, or hydroxamic acid, scaffold. In this work, 81 compounds were made by modifying this core structure to explore the pharmacophore.
View Article and Find Full Text PDF2-Phenylbenzothiazoles featuring heteroaryl sulfonamide end-capping substructures as developable mPGES-1 inhibitors.
Arch Pharm (Weinheim)
January 2025
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, Ankara, Turkey.
The inhibition of human microsomal prostaglandin E (PGE) synthase-1 (mPGES-1) is a promising therapeutic modality for developing next-generation anti-inflammatory medications. In this study, we present novel 2-phenylbenzothiazole derivatives featuring heteroaryl sulfonamide end-capping substructures as inhibitors of human mPGES-1, with IC values in the range of 0.72-3.
View Article and Find Full Text PDFResearch on the metabolites and key metabolic enzymes of allocryptopine in chicken liver microsomes via stable isotope tracing technology.
J Pharm Biomed Anal
January 2025
Shanxi Key Lab. for modernization of TCVM, College of Veterinary Medicine, Shanxi Agricultural University, Jinzhong 030801, China; College of Veterinary Medicine, Hunan Agricultural University, Changsha 410128, China. Electronic address:
Allocryptopine (ALL), a principal active component of the novel veterinary medicine Bopu Powder®, has gained widespread application in the poultry farming sector for the effective management of Escherichia coli (E. coli) diarrhea. In order to explore the metabolites and the pivotal enzymes associated with ALL, this study was conducted employing an in vitro chicken liver microsomal incubation.
View Article and Find Full Text PDFDrug interaction evaluation of the novel phosphodiesterase type 5 inhibitor tunodafil (youkenafil): Effects of tunodafil on omeprazole pharmacokinetics based on CYP2C19 gene polymorphism, and effects of ritonavir on tunodafil pharmacokinetics.
Eur J Pharm Sci
January 2025
Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing 211198, China. Electronic address:
Purpose: To evaluate the drug-drug interactions (DDI) of tunodafil (youkenafil), a novel phosphodiesterase type 5 inhibitor, its inhibitory effects on CYP450 enzymes in vitro and its clinical trials in combination with ritonavir or omeprazole were conducted.
Methods: The inhibitory effect of tunodafil on seven major CYP450 enzymes in human liver microsomes was investigated by probe substrate method. The effect of tunodafil on the pharmacokinetics of omeprazole (CYP2C19 substrate) in 40 healthy subjects, who received a single dose of 40 mg omeprazole in combination with tunodafil on the day 8 after taking 100 mg tunodafil daily for 7 days, was assessed based on CYP2C19 genotypes.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!