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KMID : 0606920080160030190
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Biomolecules & Therapeutics
2008 Volume.16 No. 3 p.190 ~ p.196
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Characterization of Deoxypodophyllotoxin Metabolism in Rat Liver Microsomes
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Lee Sang-Kyu
Lee Seung-Ho
Jeong Tae-Cheon
Jeong Hye-Gwang
Kang Mi-Jeong
Seo Young-Min
Kim Ju-Hyun
Jeon Tae-Won
Jun In-Hye
Shin Sil
Choi Jae-Ho
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Abstract
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Deoxypodophyllotoxin (DPT) is a medicinal herb product isolated from Anthriscus sylvestris. DPT possesses beneficial activities in regulating immediate-type allergic reaction and anti-inflammatory activity through the dual inhibition of cyclooxygenase-2 and 5-lipoxygenase. In the present study, the metabolism of DPT was further characterized in rat liver microsomes isolated from male Sprague Dawley rats. The metabolism of DPT was NADPH-dependent. In addition, when liver microsomes were incubated with SKF-525A, a well-known CYP inhibitor, in the presence of -NADPH, the metabolism of DPT was significantly inhibited. Using enriched rat liver microsomes, the anticipated isoforms of cytochrome P450s (CYPs) in the metabolism of DPT were partially characterized. Phenobarbital-induced microsomes increased in the formation of metabolite M1. The metabolite M3 was only produced in the enriched microsomes isolated from dexamethasone-treated rats. The results indicated that the metabolism of DPT would be CYP-dependent and that CYP2B and CYP3A might be important in the metabolism of DPT in rats.
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KEYWORD
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Deoxypodophyllotoxin, Metabolism, Cytochrome P450, in vitro, Electrospray ionization tandem mass spectrometry, Microsome
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