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4'-hydroxylation of flurbiprofen by rat liver microsomes in fasting and feeding conditions. 2003

Makiko Shimizu, and Reiko Matsushita, and Yoshiaki Matsumoto, and Masamichi Fukuoka
Department of Clinical Pharmacology and Toxicology, Showa Pharmaceutical University, Japan. shimizu@ac.shoyaku.ac.jp

We examined the 4'-hydroxylation of flurbiprofen in rat hepatocytes and liver microsomes in order to know whether the metabolism of flurbiprofen is changed on its administration to experimental animals after overnight fasting, because starvation and fasting change both the composition of cytochrome P450s (CYPs) and metabolic activity. CYPs involved in the hydroxylation were determined by various CYP inhibitors and inhibitory antibodies against rat CYP2C11 and CYP2E1 using the microsomes in fasting and feeding. The results provided a possibiliy that the 4'-hydroxylation might be regulated by CYP2C11, but not by CYP2E1, at fasting rather than feeding.

UI MeSH Term Description Entries
D008297 Male Males
D008862 Microsomes, Liver Closed vesicles of fragmented endoplasmic reticulum created when liver cells or tissue are disrupted by homogenization. They may be smooth or rough. Liver Microsomes,Liver Microsome,Microsome, Liver
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D004791 Enzyme Inhibitors Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. Enzyme Inhibitor,Inhibitor, Enzyme,Inhibitors, Enzyme
D005215 Fasting Abstaining from FOOD. Hunger Strike,Hunger Strikes,Strike, Hunger,Strikes, Hunger
D005247 Feeding Behavior Behavioral responses or sequences associated with eating including modes of feeding, rhythmic patterns of eating, and time intervals. Dietary Habits,Eating Behavior,Faith-based Dietary Restrictions,Feeding Patterns,Feeding-Related Behavior,Food Habits,Diet Habits,Eating Habits,Behavior, Eating,Behavior, Feeding,Behavior, Feeding-Related,Behaviors, Eating,Behaviors, Feeding,Behaviors, Feeding-Related,Diet Habit,Dietary Habit,Dietary Restriction, Faith-based,Dietary Restrictions, Faith-based,Eating Behaviors,Eating Habit,Faith based Dietary Restrictions,Faith-based Dietary Restriction,Feeding Behaviors,Feeding Pattern,Feeding Related Behavior,Feeding-Related Behaviors,Food Habit,Habit, Diet,Habit, Dietary,Habit, Eating,Habit, Food,Habits, Diet,Pattern, Feeding,Patterns, Feeding,Restrictions, Faith-based Dietary
D005480 Flurbiprofen An anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE. 2-Fluoro-alpha-methyl-(1,1'-biphenyl)-4-acetic Acid,Ansaid,Apo-Flurbiprofen,BTS-18322,Cebutid,Dobrofen,E-7869,Flubiprofen,Flugalin,Flurbiprofen Sodium,Fluriproben,Froben,Froben SR,Neo Artrol,Novo-Flurprofen,Nu-Flurbiprofen,Ocufen,Ocuflur,Strefen,ratio-Flurbiprofen,Apo Flurbiprofen,BTS 18322,BTS18322,E 7869,E7869,Novo Flurprofen,Nu Flurbiprofen,ratio Flurbiprofen
D006900 Hydroxylation Placing of a hydroxyl group on a compound in a position where one did not exist before. (Stedman, 26th ed) Hydroxylations
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D017208 Rats, Wistar A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain. Wistar Rat,Rat, Wistar,Wistar Rats

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