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dc.contributor.author이화정-
dc.contributor.author권영주-
dc.contributor.author이재옥-
dc.date.accessioned2018-03-13T16:30:24Z-
dc.date.available2018-03-13T16:30:24Z-
dc.date.issued2018-
dc.identifier.issn0022-3573-
dc.identifier.issn2042-7158-
dc.identifier.otherOAK-21959-
dc.identifier.urihttps://dspace.ewha.ac.kr/handle/2015.oak/241214-
dc.description.abstractObjectives: 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.languageEnglish-
dc.publisherWILEY-
dc.subjectbenzoxanthone analogue-
dc.subjectintestinal P-glycoprotein-
dc.subjectoral administration-
dc.subjectP-glycoprotein inhibitor-
dc.subjectpharmacokinetics-
dc.titleIntestinal P-glycoprotein inhibitors, benzoxanthone analogues-
dc.typeArticle-
dc.relation.issue2-
dc.relation.volume70-
dc.relation.indexSCIE-
dc.relation.indexSCOPUS-
dc.relation.startpage234-
dc.relation.lastpage241-
dc.relation.journaltitleJOURNAL OF PHARMACY AND PHARMACOLOGY-
dc.identifier.doi10.1111/jphp.12832-
dc.identifier.wosidWOS:000419992800008-
dc.identifier.scopusid2-s2.0-85038032203-
dc.author.googleChae, Song Wha-
dc.author.googleLee, Jaeok-
dc.author.googlePark, Jung Hyun-
dc.author.googleKwon, Youngjoo-
dc.author.googleNa, Younghwa-
dc.author.googleLee, Hwa Jeong-
dc.contributor.scopusid이화정(57102029300;35069834100)-
dc.contributor.scopusid권영주(12446435600)-
dc.contributor.scopusid이재옥(57199423901)-
dc.date.modifydate20210915135234-
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약학대학 > 약학과 > Journal papers
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