Study on the Pharmacokinetics and Tissue Distribution of Tangeretin in Rat
Date Issued
2012
Date
2012
Author(s)
Chang, Wei-Shan
Abstract
There is a special group of flavonoids called polymethoxyflavones (PMFs) which is rich in citrus fruits. Since the special bioactivity has been studied extensively, this group of compounds are receiving more popularity recently. PMF is a general term for flavones bearing two or more methoxy groups on their basic benzo-γ- pyrone (C6－C3－C6) skeleton with a carbonyl group at the C4 position. PMFs exist almost exclusively in citrus plants, especially in citrus peels. Tangeretin is one of the most abundant and representative polymethoxyflavones in citrus peels, especially in tangerines and oranges, It’s also known as 5,6,7,8,4’-pentamethoxyflavone. Recent studies have shown that tangeretin exhibits anti-inflammatory, antifungal, anticancer activities and hypolipidemic effect. However, the oral bioavailability and metabolism of this compound are still lacking. The aim of this study is to investigate the bioavailability of tangeretin in Sprague-Dawley rats. In the pharmacokinetic study, after tube feeding 50mg/kg BW of tangeretin, the pharmacokinetic parameter Cmax and T1/2 were 0.87 ± 0.33 μg/mL and 342.43 ± 71.27 min, respectively. After intravenous injection of 5 mg/kg BW of tangeretin, our results showed that Cmax and T1/2 were 1.11 ± 0.41 μg/mL and 69.87 ± 15.72 min, respectively. The bioavailability of tangeretin is 27.11 % , much higher than other polyphenolic compounds. It is suggested that, the lipophilic nature of the multiple methoxy groups on the tangeretin structure, results in the lower solubility in water and higher cell membrane permeability, therefore tangeretin has higher bioavailability. In the tissue distribution study, higher concentration of tangeretin was found in the gastrointestinal tract after tube feeding 50 mg/kg BW of tangeretin for 4 hours. It was especially in stomach which contained up to 20% of dosing. Furthermore, in the excretion study, the major excretion period of tangeretin occurred 0-8 hours in urine excretion and 8-24 hours in fecal excretion after tube feeding 50 mg/kg BW of tangeretin, and 7.5% tangeretin was excreted to feces after 48 hours. On the other hand, the metabolites of tangeretin should be further studied in order to understand the health potential of tangeretin and its metabolites.
Subjects
bioavailability
pharmacokinetics
polymethoxyflavones(PMFs)
tangeretin
SDGs
Type
thesis
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