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Identification of 1-Furan-2-yl-3-pyridin-2-yl-propenone, an Anti-inflammatory Agent, and Its Metabolites in Rat Liver Subcellular Fractions  

Lee, Sang-Kyu (College of Pharmacy, Yeungnam University)
Jeon, Tae-Won (College of Pharmacy, Yeungnam University)
Basnet, Arjun (College of Pharmacy, Yeungnam University)
Jeong, Hye-Gwang (College of Pharmacy, Chosun University)
Lee, Eung-Seok (College of Pharmacy, Yeungnam University)
Jeong, Tae-Cheon (College of Pharmacy, Yeungnam University)
Publication Information
Archives of Pharmacal Research / v.29, no.11, 2006 , pp. 984-989 More about this Journal
Abstract
1-Furan-2-yl-3-pyridin-2-yl-propenone (FPP-3) has been characterized to have an anti-inflammatory activity through the inhibition of the production of nitric oxide and tumor necrosis $factor-{\alpha}$. In the present studies, the phase 1 metabolism of FPP-3 was investigated in rat liver microsomes and cytosols. When FPP-3 was incubated with rat liver microsomes and cytosols in the presence of NADPH. 2 major peaks were detected on a liquid chromatography/electrospray ionization-mass spectrometry. Two metabolites (i.e., M1 and M2) were characterized as reduced forms on propenone: M1 (1-furan-2-yl-3-pyridin-2-yl-propan-1-one) was the initial metabolite and M2 (1-furan-2-yl-3-pyridin-2-yl-propan-1-ol) was a secondary alcohol believed to be formed from M1.
Keywords
1-Furan-2-yl-3-pyridin-2-yl-propenone; LC-ESI/MS; Reduction; Metabolite;
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