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Bioavailability of anti‐carcinogenic hydroxylated polymethoxyflavones in mice
Author(s) -
QIU PEIJU,
Song Mingyue,
Guan Huashi,
Guo Shanshan,
Zheng Jinkai,
Charoensinphon Noppawat,
Nutakul Wasamon,
Ngauv Pearline,
Xiao Hang
Publication year - 2011
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.25.1_supplement.977.14
Subject(s) - bioavailability , chemistry , urine , carcinogen , glucuronic acid , chromatography , detection limit , in vivo , high performance liquid chromatography , pharmacology , biochemistry , biology , polysaccharide , microbiology and biotechnology
Previously we have showed that hydroxylated polymethoxyflavones (OH‐PMFs), such as 5‐hydroxy‐6,7,8,3′,4′‐pentamethoxyflavone (5HPMF) and 5‐hydroxy‐6,7,8,4′‐tetramethoxyflavone (5HTMF) are potent anti‐cancer dietary compounds in cell culture. Bioavailability is one of the key factors that can dictate the in vivo efficacy of dietary bioactive compounds. Herein, we studied the bioavailability of 5HPMF and 5HTMF in CF‐1 mice. We developed a highly sensitive HPLC method for the detection of OH‐PMFs in biological samples. The method was fully validated in terms of linearity, accuracy and precision. The limit of detection (LOD) in serum was determined as being 0.71 and 1.97 ng/mL (ppb) for 5HPMF and 5HTMF, respectively, demonstrating an over 150‐fold increase in sensitivity in comparison with previously published method. At 60 min after oral gavage (100 mg/kg), 5HPMF, mostly in free form, reached its peak level of 5.3 μM, while 5HTMF showed similar trend but with the peak level 8.28‐fold lower than that of 5HPMF. In urine, both 5HPMF and 5HTMF existed mainly as sulfate‐ and glucuronic acid‐conjugates, and urine level of total 5HPMF was 9.06‐fold higher than that of 5HTMF. These results demonstrated that 5HTMF had much lower bioavailability, which may due to its poor solubility in GI tract.