Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 남태규 | - |
dc.date.accessioned | 2018-12-17T06:05:06Z | - |
dc.date.available | 2018-12-17T06:05:06Z | - |
dc.date.issued | 2018-01 | - |
dc.identifier.citation | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v. 28, No. 2, Page. 107-112 | en_US |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | https://www.sciencedirect.com/science/article/pii/S0960894X17311575 | - |
dc.identifier.uri | https://repository.hanyang.ac.kr/handle/20.500.11754/80900 | - |
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. | en_US |
dc.description.sponsorship | This work was supported by the Yeungnam University Research Grant. | en_US |
dc.language.iso | en_US | en_US |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | en_US |
dc.subject | Retinal pigment epithelium | en_US |
dc.subject | Apoptosis | en_US |
dc.subject | NADPH oxidase 4 | en_US |
dc.subject | 6-Ureido/thioureido-2,4,5-trimethylpyridin-3-ol | en_US |
dc.subject | 4-Hydroxynonenal | en_US |
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 | en_US |
dc.type | Article | en_US |
dc.relation.no | 2 | - |
dc.relation.volume | 28 | - |
dc.identifier.doi | 10.1016/j.bmcl.2017.11.046 | - |
dc.relation.page | 107-112 | - |
dc.relation.journal | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.contributor.googleauthor | Bae, Dawon | - |
dc.contributor.googleauthor | Gautam, Jaya | - |
dc.contributor.googleauthor | Jang, Hyeonjin | - |
dc.contributor.googleauthor | Banskota, Suhrid | - |
dc.contributor.googleauthor | Lee, Sang Yeul | - |
dc.contributor.googleauthor | Jeong, Min-Ji | - |
dc.contributor.googleauthor | Kim, A-Sol | - |
dc.contributor.googleauthor | Kim, Hong Chul | - |
dc.contributor.googleauthor | Lee, Iyn-Hyang | - |
dc.contributor.googleauthor | Nam, Tae-gyu | - |
dc.contributor.googleauthor | Kim, Jung-Ae | - |
dc.contributor.googleauthor | Jeong, Byeong-Seon | - |
dc.relation.code | 2018000599 | - |
dc.sector.campus | E | - |
dc.sector.daehak | COLLEGE OF PHARMACY[E] | - |
dc.sector.department | DEPARTMENT OF PHARMACY | - |
dc.identifier.pid | tnam | - |
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