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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Song, Won Young Ji, Hye Young Baek, Nam-In Jeong, Tae-Sook Lee, Hye Suk |
| Description | Author Affiliation: Song WY ( Drug Metabolism & Bioanalysis Laboratory, College of Pharmacy, Wonkwang University, Iksan 570-749, Korea.) |
| Abstract | Jaceosidin is an active component in Artemisia species as well as Eupatorium species and it exhibits antiallergic, anticancer, antioxidant, anti-inflammatory, and antimutagenic activities. Jaceosidin was metabolized to jaceosidin glucuronide, 6-O-desmethyljaceosidin, hydroxyjaceosidin, 6-O-desmethyljaceosidin glucuronide, and hydroxyjaceosidin glucuronide in human liver microsomes. This study characterized the human liver cytochrome P450 (CYP) and UDPglucuronosyltransferase (UGT) enzymes responsible for the metabolism of jaceosidin. CYP1A2 was identified as the major enzyme responsible for the formation of 6-O-desmethyljaceosidin and hydroxyjaceosidin from jaceosidin on the basis of a combination of correlation analysis and experiments including immuno-inhibition, chemical inhibition in human liver microsomes, and metabolism by human cDNA-expressed CYP enzymes. Jaceosidin glucuronidation was catalyzed by UGT1A1, UGT1A3, UGT1A7, UGT1A8, UGT1A9, and UGT1A10. These results suggest that the pharmacokinetics of jaceosidin may be dramatically affected by polymorphic CYP1A2, UGT1A1, and UGT1A7 responsible for the metabolism of jaceosidin or by the coadministration of relevant CYP1A2 or UGT inhibitors or inducers. |
| File Format | HTM / HTML |
| ISSN | 02536269 |
| Issue Number | 12 |
| Volume Number | 33 |
| e-ISSN | 19763786 |
| Journal | Archives of Pharmacal Research |
| Language | English |
| Publisher | Springer |
| Publisher Date | 2010-12-01 |
| Publisher Place | Korea (South) |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Pharmacology Artemisia Cytochrome P-450 Enzyme System Metabolism Flavonoids Glucuronosyltransferase Microsomes, Liver Enzymology Plant Preparations Pharmacokinetics Cytochrome P-450 Cyp1a2 Cytochrome P-450 Cyp1a2 Inhibitors Cytochrome P-450 Enzyme Inhibitors Antagonists & Inhibitors Humans Plant Components, Aerial Journal Article Research Support, Non-u.s. Gov't |
| Content Type | Text |
| Resource Type | Article |
| Subject | Organic Chemistry Drug Discovery Molecular Medicine |
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