Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 이화정 | * |
dc.contributor.author | 권영주 | * |
dc.contributor.author | 이재옥 | * |
dc.date.accessioned | 2018-03-13T16:30:24Z | - |
dc.date.available | 2018-03-13T16:30:24Z | - |
dc.date.issued | 2018 | * |
dc.identifier.issn | 0022-3573 | * |
dc.identifier.issn | 2042-7158 | * |
dc.identifier.other | OAK-21959 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/241214 | - |
dc.description.abstract | Objectives: The inhibitors of P-glycoprotein (P-gp) which limits an access of exogenous compounds in the luminal membrane of the intestine have been studied to enhance the intestinal P-gp-mediated absorption of anticancer drugs. Methods: Inhibition of the efflux pump by synthesized benzoxanthone derivatives was investigated in vitro and in vivo. MCF-7/ADR cell line was used for cytotoxicity assay and [H-3]-daunomycin (DNM) accumulation/efflux study. Eight benzoxanthone analogues were tested for their effects on DNM cytotoxicity. Among them, three analogues were selected for the accumulation/efflux and P-gp ATPase studies. Paclitaxel (PTX), a P-gp substrate anticancer drug, was orally administered to rats with/without compound 1 (8,10-bis(thiiran-2-ylmethoxy)-7H-benzo[c]xanthen-7-one). The pharmacokinetic parameters of PTX in the presence/absence of compound 1 were evaluated from the plasma concentration-time profiles. Key-findings: Compound 1 increased the DNA accumulation to 6.5-fold and decreased the DNM efflux to approximately 1/2 in the overexpressing P-gp cell line. Relative bioavailability (RB) of PTX in rats was significantly increased up to 3.2-fold by compound 1 (0.5 or 2 mg/kg). Conclusions: Benzoxanthone analogue, compound 1 is strongly suggested to be a promising inhibitor of P-gp to improve an oral absorption of compounds for cancer therapy. | * |
dc.language | English | * |
dc.publisher | WILEY | * |
dc.subject | benzoxanthone analogue | * |
dc.subject | intestinal P-glycoprotein | * |
dc.subject | oral administration | * |
dc.subject | P-glycoprotein inhibitor | * |
dc.subject | pharmacokinetics | * |
dc.title | Intestinal P-glycoprotein inhibitors, benzoxanthone analogues | * |
dc.type | Article | * |
dc.relation.issue | 2 | * |
dc.relation.volume | 70 | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 234 | * |
dc.relation.lastpage | 241 | * |
dc.relation.journaltitle | JOURNAL OF PHARMACY AND PHARMACOLOGY | * |
dc.identifier.doi | 10.1111/jphp.12832 | * |
dc.identifier.wosid | WOS:000419992800008 | * |
dc.identifier.scopusid | 2-s2.0-85038032203 | * |
dc.author.google | Chae, Song Wha | * |
dc.author.google | Lee, Jaeok | * |
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.contributor.scopusid | 이재옥(57199423901) | * |
dc.date.modifydate | 20240422124907 | * |