Full metadata record
DC Field | Value | Language |
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dc.contributor.author | 이화정 | * |
dc.contributor.author | 권영주 | * |
dc.date.accessioned | 2016-08-27T04:08:17Z | - |
dc.date.available | 2016-08-27T04:08:17Z | - |
dc.date.issued | 2015 | * |
dc.identifier.issn | 0223-5234 | * |
dc.identifier.issn | 1768-3254 | * |
dc.identifier.other | OAK-14687 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/217085 | - |
dc.description.abstract | Intestinal P-glycoprotein (P-gp) is a limiting step for oral absorption of drugs. Therefore, P-gp inhibitors have been studied as enhancers of oral absorption of drugs that are P-gp substrates. We investigated the in vitro and in vivo P-gp inhibitory activity of synthesized xanthone analogues. With 3-(3-chloro-2-hydroxypropoxy)-1-hydroxy-9H-thioxanthen-9-one, compound 13, accumulation of daunomycin (DNM) increased 707% and efflux of DNM decreased 66% compared to DNM alone. Relative bioavailability (RB) of paclitaxel (PTX, 25 mg/kg) increased 2.5-fold after oral administration with 13 (5 mg/kg). In a xenograft animal model, oral administration of PTX (40 mg/kg) with 13 (10 mg/kg) significantly inhibited tumour growth and was more effective than intravenously administered PTX (10 mg/kg) alone. Therefore, the synthesized xanthone analogue 13 might have therapeutic benefits for oral absorption of P-gp substrate anticancer drugs. (C) 2015 Published by Elsevier Masson SAS. | * |
dc.language | English | * |
dc.publisher | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER | * |
dc.subject | P-glycoprotein inhibitor | * |
dc.subject | Xanthone analogue | * |
dc.subject | Paclitaxel | * |
dc.subject | Bioavailability | * |
dc.subject | Xenograft | * |
dc.title | Xanthone analogues as potent modulators of intestinal P-glycoprotein | * |
dc.type | Article | * |
dc.relation.volume | 93 | * |
dc.relation.index | SCI | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 237 | * |
dc.relation.lastpage | 245 | * |
dc.relation.journaltitle | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | * |
dc.identifier.doi | 10.1016/j.ejmech.2015.01.006 | * |
dc.identifier.wosid | WOS:000351646100024 | * |
dc.identifier.scopusid | 2-s2.0-84922797513 | * |
dc.author.google | Chae, Song Wha | * |
dc.author.google | Woo, Sangwook | * |
dc.author.google | Park, Jung Hyun | * |
dc.author.google | Kwon, Youngjoo | * |
dc.author.google | Na, Younghwa | * |
dc.author.google | Lee, Hwa Jeong | * |
dc.contributor.scopusid | 이화정(57102029300) | * |
dc.contributor.scopusid | 권영주(12446435600) | * |
dc.date.modifydate | 20240123101932 | * |