Protective effects of 6-ureido/thioureido-2,4,5-trimethylpyridin-3-ols against 4-hydroxynonenal-induced cell death in adult retinal pigment epithelial-19 cells
DC Field | Value | Language |
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dc.contributor.author | Bae, Dawon | - |
dc.contributor.author | Gautam, Jaya | - |
dc.contributor.author | Jang, Hyeonjin | - |
dc.contributor.author | Banskota, Suhrid | - |
dc.contributor.author | Lee, Sang Yeul | - |
dc.contributor.author | Jeong, Min-Ji | - |
dc.contributor.author | Kim, A-Sol | - |
dc.contributor.author | Kim, Hong Chul | - |
dc.contributor.author | Lee, Iyn-Hyang | - |
dc.contributor.author | Nam, Tae-gyu | - |
dc.contributor.author | Kim, Jung-Ae | - |
dc.contributor.author | Jeong, Byeong-Seon | - |
dc.date.accessioned | 2021-06-22T12:22:18Z | - |
dc.date.available | 2021-06-22T12:22:18Z | - |
dc.date.created | 2021-01-21 | - |
dc.date.issued | 2018-01 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/6860 | - |
dc.description.abstract | Dysfunction or progressive degeneration of retinal pigment epithelium (RPE) contributes in the initial pathogenesis of age-related macular degeneration (AMD) causing irreversible vision loss, which makes RPE the prime target of the disease. The present study aimed to identify compounds to protect 4-hydroxynonenal (4-HNE)-induced RPE cell death by inhibiting NADPH oxidase 4 (NOX4) activity, not just as free radical scavengers, using ARPE-19, a human adult retinal pigment epithelial cell line, as a RPE representative. Novel thirty-two 6-ureido/thioureido-2,4,5-trimethylpyridin-3-ol derivatives 17 were synthesized and tested. We found that there was a strong correlation between level of protective effect of compounds 17 against 4-HNE-induced APRE-19 cell death and that of inhibitory activity against 4-HNE-induced superoxide production, and that most of the compounds 17 showed minimal DPPH radical scavenging activity. Compound 17-28 showed the best protective activity against 4-HNE-induced superoxide production (79.5% inhibition) and cell death (85.1% recovery) at 10 mu M concentration, which was better than that of VAS2870, a NOX2/4 inhibitor. In addition, compound 17-28 blocked 4-HNE-induced apoptosis of ARPE-19 cells in a concentration-dependent manner. The results indicate that compound 17-28 may be a lead compound to develop AMD therapeutics. (C) 2017 Elsevier Ltd. All rights reserved. | - |
dc.language | 영어 | - |
dc.language.iso | en | - |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.title | Protective effects of 6-ureido/thioureido-2,4,5-trimethylpyridin-3-ols against 4-hydroxynonenal-induced cell death in adult retinal pigment epithelial-19 cells | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Nam, Tae-gyu | - |
dc.identifier.doi | 10.1016/j.bmcl.2017.11.046 | - |
dc.identifier.scopusid | 2-s2.0-85036539316 | - |
dc.identifier.wosid | 000423658000009 | - |
dc.identifier.bibliographicCitation | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.28, no.2, pp.107 - 112 | - |
dc.relation.isPartOf | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.citation.title | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.citation.volume | 28 | - |
dc.citation.number | 2 | - |
dc.citation.startPage | 107 | - |
dc.citation.endPage | 112 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.isOpenAccess | N | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Organic | - |
dc.subject.keywordPlus | MACULAR DEGENERATION | - |
dc.subject.keywordPlus | OXIDATIVE STRESS | - |
dc.subject.keywordPlus | ANTIANGIOGENIC ACTIVITY | - |
dc.subject.keywordPlus | IN-VITRO | - |
dc.subject.keywordPlus | 6-AMINO-2,4,5-TRIMETHYLPYRIDIN-3-OLS | - |
dc.subject.keywordPlus | RESVERATROL | - |
dc.subject.keywordPlus | QUERCETIN | - |
dc.subject.keywordPlus | MELATONIN | - |
dc.subject.keywordPlus | DAMAGE | - |
dc.subject.keywordAuthor | Retinal pigment epithelium | - |
dc.subject.keywordAuthor | Apoptosis | - |
dc.subject.keywordAuthor | NADPH oxidase 4 | - |
dc.subject.keywordAuthor | 6-Ureido/thioureido-2,4,5-trimethylpyridin-3-ol | - |
dc.subject.keywordAuthor | 4-Hydroxynonenal | - |
dc.identifier.url | https://www.sciencedirect.com/science/article/pii/S0960894X17311575?via%3Dihub | - |
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