Abstract |
The anti-inflammatory properties of 3',4',3,5,6,7,8-heptamethoxyflavone (HMF), a citrus polymethoxylated flavone, were studied in the bacterial lipopolysaccharide (LPS)-challenge/ tumor necrosis factor-alpha ( TNFalpha) response in mice and in the carrageenan/paw edema assay in rats. In each of these trials, HMF administered by intraperitoneal (ip) injection exhibited anti-inflammatory activity, whereas HMF administered orally (po) produced no effects. The inhibition observed in the LPS-challenge/ TNFalpha assay correlated with the HMF levels in the blood sera of mice dosed (ip) with either 33 or 100 mg/kg body weight. Low levels of HMF (0.035 +/- 0.024 ppm) were detected in the blood sera of mice dosed orally [100 mg of HMF (suspended in vegetable oil)/kg], whereas ip injection led to higher levels (0.517 +/- 0.051 ppm). This may account for the different levels of anti-inflammatory effects observed in mice following ip vs oral HMF administration. HMF metabolites, including a number of mono- and di-demethylated HMF metabolites and their glucuronic acid conjugates, were also detected, but results of these studies suggest that the glucuronidated metabolites of HMF are inactive in these inflammation models.
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Authors | John A Manthey, Philip Bendele |
Journal | Journal of agricultural and food chemistry
(J Agric Food Chem)
Vol. 56
Issue 20
Pg. 9399-403
(Oct 22 2008)
ISSN: 1520-5118 [Electronic] United States |
PMID | 18816060
(Publication Type: Journal Article)
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Chemical References |
- Anti-Inflammatory Agents
- Flavonoids
- Lipopolysaccharides
- Plant Extracts
- Tumor Necrosis Factor-alpha
- 3,3',4',5,6,7,8-heptamethoxyflavone
- Carrageenan
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Topics |
- Animals
- Anti-Inflammatory Agents
(administration & dosage, metabolism)
- Carrageenan
(immunology)
- Citrus
(chemistry)
- Disease Models, Animal
- Dose-Response Relationship, Drug
- Drug Administration Routes
- Edema
(chemically induced, drug therapy, metabolism)
- Flavonoids
(administration & dosage, metabolism)
- Humans
- Inflammation
(chemically induced, drug therapy, metabolism)
- Lipopolysaccharides
(immunology)
- Male
- Mice
- Plant Extracts
(administration & dosage, metabolism)
- Rats
- Rats, Sprague-Dawley
- Tumor Necrosis Factor-alpha
(blood)
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