Drug-metabolizing enzymes major

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). 

With respect to drug-metabolizing enzymes, the majority of the CYPs responsible for phase I metabolism are concentrated in liver. The CYPs considered here are all found in the endoplasmic reticulum (isolated as microsomes ). Of the 18 human CYP families known, the bulk of xenobiotic biotransformation processes are carried out by enzymes from the CYP1, CYP2 and CYP3 families. In humans, realistically,... 

Constitutive e3q>ression and localization of the major drug metabolizing enzyme, cytochrome P4502D in human brain. Brain Res Mol Brain Res 103 49-61. 

Microsomes Can be frozen and used on demand Contains major drug metabolizing enzymes Straighforward to use Limited enzyme complement Closed system so may not be representative of in vivo situation... 

Unlike renal function, hepatic maturation is generally believed to be a two-stage process with the major development completed at 4 weeks postpartum and tlie second stage completed by about 10 weeks of age. In sheep, for example, tlie activity of a number of hepatic drug-metabolizing enzymes was found to be relatively low in animals aged up to 6 months compared with adult individuals... 

It has only been discovered relatively recently that a natural remedy, St. John s Wort, used by millions for the treatment of depression, is a potent inducer of the major human drug-metabolizing enzyme, CYP3A4. This induction can lead to the therapeutic failure of a drug when the remedy is taken at the same time. 

Table 1 Nuclear Receptors That Play a Major Role in Regulating Human Drug-Metabolizing Enzymes ... 

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