Drug metabolism, enzymes and

Agarwal DK, Seth PK, Gupta PK. 1978. Effect of endosulfan on drug metabolizing enzymes and lipid peroxidation in rat. J Environ Sci Health C13(l) 49-62. 

E (1997) Mechanism of action of dietary chemoprotective agents in rat liver induction of phase I and II drug metabolizing enzymes and aflatoxin B1 metabolism . Carcinogenesis, 18 1729-38. 

Each plant tissue tends to have an obviously distinctive profile of flavonoids. The flavonoid content can reach about 0.5% in pollen, 10% in propolis, and about 6 mg/kg in honey. Havonoid aglycones appear to be present only in propolis and honey, while pollen contains flavanols in herosidic forms. The flavonoids in honey and propolis have been identified as flavanones and flavanones/flavanols (Campos et ah, 1990). The antimi-crobially active flavanone pinocembrine was foimd to be a major flavonoid in honey (Bogdanov, 1989). Amiot et ah (1989) studied two blossom and two honeydew Swiss honey samples and foimd that pinocembrine was the main flavonoid. Pinocembrine concentration varied between 2 and 3 mg/kg (Bogdanov, 1989). Berahia et ah (1993) analyzed sunflower honey samples and detected six flavone/flavols, four flavanone/ flavols, and pinocembrin, of which pinocembrin is the main flavonoid. The flavonoids in sunflower honey and propolis were characterized and assessed for their effects on hepatic drug-metabolizing enzymes and benzo [fl]pyrene-DNA adduct formation (Sabatier et ah, 1992 Siess et ah, 1996). 

Siess, M. H., Le Bon, A. M., Canivenc-Lavier, M. C., Amiot, M. ]., Sabatier, S., Yaubert, S. Y., and Suschetet, M. (1996). Flavonoids of honey and propolis Characterization and effects on hepatic drug-metabolizing enzymes and benzoja] pyrene-DNA.. Agric. Food Chem. 44, 2297-2301. 

The original humanized mice bear the expression hPXR exclusively in the liver [10]. As both drug-metabolizing enzymes and xenobiotic receptors are also highly expressed in the intestinal tracts, it is conceivable that mouse models with the humanized receptors expressed in both the liver and the intestine would represent a... 

Mills, J.B., Rose, K.A., Sadagopan, N., Sahi, J. and de Morais, S.M. (2004) Induction of drug metabolism enzymes and MDR1 using a novel human hepatocyte cell line. The Journal of Pharmacology and Experimented Therapeutics, 309, 303-309. 

Kuzuya Y, Adachi T, Hara H, Anan A, Izuhara K, Nagai H (2004) Induction of drug-metabolizing enzymes and transporters in human bronchial epithelial cells by beclomethasone dipropionate. IUBMB Life 56(6) 355-359. 

Passive transcellular transport across the intestinal epithelium involves three discrete steps (1) uptake across the apical membrane, (2) diffusion through the cytoplasm, and (3) efflux across the basolateral membrane. Occasionally, drug molecules without favorable physicochemical properties traverse the intestinal epithelium using endogenous membrane transporters.6-8 In addition, the intestinal mucosa, with its numerous drug-metabolizing enzymes and efflux transporters, such as P-glycoprotein (Pgp), functions as a biochemical barrier.9... 

Pharmacogenomics of Drug-Metabolizing Enzymes and Drug Transporters in Chemotherapy... 

Moreover individuals were found who had multiple copies of the gene (up to 12 copies has been described in one Swedish family), and in these people a substance such as debrisoquine is metabolized so rapidly that virtually no therapeutic effect would be seen, as the hydroxy-metabolite is not pharmacologically active. These variants are inherited, and so it is possible to characterize families by their inherited drug-metabolizing enzymes, and the genes that code for them. 

It must be recognized that developmental differences in hepatic drug metabolism occur consequent to reductions in the activity of specific drug-metabolizing enzymes and their respective isoforms. For most enzymes, the greatest reduction of activity is seen in premature infants where immature function may also reflect continued organogenesis. This... 

Besides the examples listed above, there are numerous exploratory association studies that have identified many potential polymorphism biomarkers for treatment response in membrane transporter, drug-metabolizing enzyme, and drug target genes. The methodology and statistical analysis for the candidate gene approach are simple the results are easy to interpret. 

Piperine Piperine, molecular formula C17H19NO3, a component of black pepper (Piper nigrum), has been used in various traditional medicine preparations, and also as an insecticide. Piperine has various effects on human drug metabolizing enzymes, and is marketed under the brand name, Bioperine , as an adjunct for increasing bioavailability of various dietary supplements, especially curcumin, one of the active ingredients of turmeric (Curcuma longa). 

Morgan ET et al Regulation of drug-metabolizing enzymes and transporters in infection, inflammation, and cancer. Drug Metab Dispos 2008 36 205. [PMID 18218849]... 

Goldstein, J.A., Friesen, M., Linder, R.E., Hickman, P, Hass, J.R. Bergman, H. (1977) Effects of pcntachlorophenol on hepatic drug-metabolizing enzymes and porphyria related to contamination with chlorinated dibenzo-/i-dioxins and dibenzo-furans. Biochem. Phamiacol., 26, 1549-1557... 

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