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Orange juice and its component, hesperidin, decrease the expression of multidrug resistance-associated protein 2 in
Minoru Watanabe1, Naoki Matsumoto, Yuko Takeba
1Department of Pharmacology, St. Marianna University School of Medicine, 2-16-1 Sugao, Miyamae-Ku, Kawasaki, Kanagawa 216-8511, Japan. m4wata@marianna-u.ac.jp
Journal of Biomedicine & Biotechnology
|June 11, 2011
Summary
Orange juice (OJ) and hesperidin significantly alter pravastatin (PRV) pharmacokinetics by decreasing multidrug resistance-associated protein 2 (Mrp2) expression in rats. These findings highlight hesperidin
Area of Science:
- Pharmacology and Toxicology
- Nutritional Science
Background:
- Pravastatin (PRV) is a statin medication used to lower cholesterol.
- Multidrug resistance-associated protein 2 (Mrp2) plays a role in the transport and elimination of various compounds, including statins.
- Orange juice (OJ) contains hesperidin, a flavonoid with potential biological activities.
Purpose of the Study:
- To investigate the impact of orange juice (OJ) and hesperidin on the pharmacokinetics of pravastatin (PRV).
- To examine the effect of OJ and hesperidin on the expression of multidrug resistance-associated protein 2 (Mrp2) in rats.
Main Methods:
- Male Sprague-Dawley rats were administered OJ or hesperidin orally for two days.
- A single oral dose of pravastatin (100 mg/kg) was administered post-treatment.
- Pharmacokinetic parameters (AUC, Cmax, t1/2) of PRV and Mrp2 protein/mRNA levels in the small intestine and liver were measured.
Main Results:
- Orange juice (OJ) administration significantly increased the area under the curve (AUC), maximum concentration (Cmax), and half-life (t1/2) of pravastatin (PRV).
- OJ significantly decreased Mrp2 protein and mRNA expression in both the small intestine and liver.
- Hesperidin administration yielded similar results to OJ, indicating its role in the observed effects.
Conclusions:
- Hesperidin in orange juice (OJ) is responsible for altering pravastatin (PRV) pharmacokinetics.
- The observed changes in PRV pharmacokinetics are associated with a decrease in Mrp2 expression, suggesting Mrp2's involvement in PRV transport.
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