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The effect of garlic extract on human metabolism of acetaminophen
P R Gwilt1, C L Lear, M A Tempero
1College of Pharmacy, Eppley Institute, University of Nebraska Medical Center, Omaha 68131.
Abstract:
Several studies suggest that the constituents of garlic may inhibit experimentally induced carcinogenesis. To evaluate the chemopreventive properties of garlic in humans, the effects of chronic administration of an aged garlic extract on the disposition of acetaminophen and metabolites were studied. This commonly used drug was chosen because it forms a reactive electrophilic metabolite after oxidative metabolism. Sixteen subjects ingested daily doses of garlic extract (approximately equivalent to six to seven cloves of garlic) for 3 months. Before the course of garlic, at the end of each month and 1 month after termination of garlic administration, a 1-g oral dose of acetaminophen was given to each subject. Plasma and urine were measured for acetaminophen and the glucuronide, sulfate, cysteinyl, mercapturate, and methylthio metabolites. It was found that garlic treatment had no discernible effect on oxidative metabolism but was associated with a slight increase in sulfate conjugation of drug. These findings suggest that garlic extract has limited potential as a chemopreventive agent.
Insights
Aged garlic extract showed minimal impact on acetaminophen metabolism in humans. While not affecting oxidative pathways, it slightly increased sulfate conjugation, suggesting limited chemopreventive potential.
Area of Science:
- Nutritional biochemistry
- Pharmacology
- Chemoprevention research
Background:
- Garlic constituents are investigated for potential anticancer properties.
- Acetaminophen metabolism involves a reactive electrophilic metabolite, a target for chemoprevention.
- Human studies are needed to validate garlic's chemopreventive effects.
Purpose of the Study:
- To assess the chemopreventive potential of aged garlic extract in humans.
- To investigate the effect of chronic garlic extract consumption on acetaminophen metabolism.
- To determine if garlic influences the disposition of acetaminophen and its metabolites.
Main Methods:
- Aged garlic extract was administered daily to sixteen subjects for three months.
- Acetaminophen (1g) was administered orally before, during, and after garlic extract treatment.
- Plasma and urine samples were analyzed for acetaminophen and its key metabolites (glucuronide, sulfate, cysteinyl, mercapturate, methylthio).
Main Results:
- Garlic extract administration did not significantly alter the oxidative metabolism of acetaminophen.
- A slight increase in the sulfate conjugation of acetaminophen was observed during garlic treatment.
- No discernible effect on the formation of reactive electrophilic metabolites was detected.
Conclusions:
- Chronic intake of aged garlic extract has a limited impact on acetaminophen metabolism in humans.
- The study suggests a minor influence on sulfate conjugation, but not on critical oxidative pathways.
- Garlic extract demonstrates limited potential as a chemopreventive agent based on this acetaminophen metabolism model.