Enhanced Cellular Uptake and Pharmacokinetic Characteristics of Doxorubicin-Valine Amide Prodrug
DC Field | Value | Language |
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dc.contributor.author | Park, Yohan | - |
dc.contributor.author | Park, Ju-Hwan | - |
dc.contributor.author | Park, Suryeon | - |
dc.contributor.author | Lee, Song Yi | - |
dc.contributor.author | Cho, Kwan Hyung | - |
dc.contributor.author | Kim, Dae-Duk | - |
dc.contributor.author | Shim, Won-Sik | - |
dc.contributor.author | Yoon, In-Soo | - |
dc.contributor.author | Cho, Hyun-Jong | - |
dc.contributor.author | Maeng, Han-Joo | - |
dc.date.available | 2020-02-28T00:42:35Z | - |
dc.date.created | 2020-02-07 | - |
dc.date.issued | 2016-10 | - |
dc.identifier.issn | 1420-3049 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/7806 | - |
dc.description.abstract | In this study, we synthesized the valine (Val)-conjugated amide prodrug of doxorubicin (DOX) by the formation of amide bonds between DOX and Val. The synthesis of the DOX-Val prodrug was identified by a proton nuclear magnetic resonance (H-1-NMR) assay. In the MCF-7 cells (human breast adenocarcinoma cell; amino acid transporter-positive cell), the cellular accumulation efficiency of DOX-Val was higher than that of DOX according to the flow cytometry analysis data. Using confocal laser scanning microscopy (CLSM) imaging, it was confirmed that DOX-Val as well as DOX was mainly distributed in the nucleus of cancer cells. DOX-Val was intravenously administered to rats at a dose of 4 mg/kg, and the plasma concentrations of DOX-Val (prodrug) and DOX (formed metabolite) were quantitatively determined. Based on the systemic exposure (represented as area under the curve (AUC) values) of DOX-Val (prodrug) and DOX (formed metabolite), approximately half of DOX-Val seemed to be metabolized into DOX. However, it is expected that the remaining DOX-Val may exert improved cellular uptake efficiency in cancer cells after its delivery to the cancer region. | - |
dc.language | 영어 | - |
dc.language.iso | en | - |
dc.publisher | MDPI AG | - |
dc.relation.isPartOf | MOLECULES | - |
dc.title | Enhanced Cellular Uptake and Pharmacokinetic Characteristics of Doxorubicin-Valine Amide Prodrug | - |
dc.type | Article | - |
dc.type.rims | ART | - |
dc.description.journalClass | 1 | - |
dc.identifier.wosid | 000389917900009 | - |
dc.identifier.doi | 10.3390/molecules21101272 | - |
dc.identifier.bibliographicCitation | MOLECULES, v.21, no.10 | - |
dc.identifier.scopusid | 2-s2.0-84988967341 | - |
dc.citation.title | MOLECULES | - |
dc.citation.volume | 21 | - |
dc.citation.number | 10 | - |
dc.contributor.affiliatedAuthor | Shim, Won-Sik | - |
dc.contributor.affiliatedAuthor | Maeng, Han-Joo | - |
dc.type.docType | Article | - |
dc.subject.keywordAuthor | amino acid transporters | - |
dc.subject.keywordAuthor | cancer cell | - |
dc.subject.keywordAuthor | cellular uptake | - |
dc.subject.keywordAuthor | doxorubicin | - |
dc.subject.keywordAuthor | valine prodrug | - |
dc.subject.keywordAuthor | amide bond | - |
dc.subject.keywordPlus | AMINO-ACID TRANSPORTERS | - |
dc.subject.keywordPlus | CANCER-THERAPY | - |
dc.subject.keywordPlus | DRUG-DELIVERY | - |
dc.subject.keywordPlus | STRATEGIES | - |
dc.subject.keywordPlus | ACCUMULATION | - |
dc.subject.keywordPlus | SOLUBILITY | - |
dc.subject.keywordPlus | METABOLISM | - |
dc.subject.keywordPlus | IRINOTECAN | - |
dc.subject.keywordPlus | INCREASES | - |
dc.subject.keywordPlus | DESIGN | - |
dc.relation.journalResearchArea | Biochemistry & Molecular Biology | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Biochemistry & Molecular Biology | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Multidisciplinary | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
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