Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 김현영 | - |
dc.date.accessioned | 2019-11-26T05:48:37Z | - |
dc.date.available | 2019-11-26T05:48:37Z | - |
dc.date.issued | 2017-06 | - |
dc.identifier.citation | CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY, v. 44, no. 6, page. 671-679 | en_US |
dc.identifier.issn | 1440-1681 | - |
dc.identifier.uri | https://onlinelibrary.wiley.com/doi/abs/10.1111/1440-1681.12757 | - |
dc.identifier.uri | https://repository.hanyang.ac.kr/handle/20.500.11754/114620 | - |
dc.description.abstract | Excessive activation of poly (ADP-ribose) polymerase-1 (PARP-1) is known to develop neuronal apoptosis, necrosis and inflammation after ischaemic brain injury. Therefore, PARP-1 inhibition after ischaemic stroke has been attempted in successful animal studies. The purpose of present work was to develop a novel water soluble PARP-1 inhibitor (JPI-289) and explore its neuroprotective effect on ischaemic injury in an in vitro model. The half-life of JPI-289 after intravenous or oral administration in rats was relatively long (1.4-1.5 hours) with 65.6% bioavailability. The inhibitor strongly inhibited PARP-1 activity (IC50=18.5 nmol/L) and cellular PAR formation (IC50=10.7 nmol/L) in the nanomolar range. In rat cortical neuronal cells, JPI-289 did not affect cell viability up to 1 mmol/L as assayed by Trypan blue staining (TBS) and lactate dehydrogenase (LDH) assay. Treatment of JPI-289 for 2 hours after 2 hours of oxygen glucose deprived (OGD) rat cortical neuron attenuated PARP activity and restored ATP and NAD+ levels. Apoptosis-associated molecules such as apoptosis inducing factor (AIF), cytochrome C and cleaved caspase-3 were reduced after JPI-289 treatment in the OGD model. The present findings suggest that the novel PARP-1 inhibitor, JPI-289, is a potential neuroprotective agent which could be useful as a treatment for acute ischaemic stroke. | en_US |
dc.description.sponsorship | Korea Drug Development Fund, Grant/Award Number: KDDF-201410-08; Korea Health Industry Development Institute; Ministry of Health & Welfare, Korea, Grant/Award Number: A100453 | en_US |
dc.language.iso | en_US | en_US |
dc.publisher | WILEY | en_US |
dc.subject | cerebral ischaemia | en_US |
dc.subject | PARP-1 inhibitor | en_US |
dc.subject | stroke | en_US |
dc.title | Neuroprotective effects of a novel poly (ADP-ribose) polymerase-1 inhibitor, JPI-289, in hypoxic rat cortical neurons | en_US |
dc.type | Article | en_US |
dc.relation.no | 6 | - |
dc.relation.volume | 44 | - |
dc.identifier.doi | 10.1111/1440-1681.12757 | - |
dc.relation.page | 671-679 | - |
dc.relation.journal | CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY | - |
dc.contributor.googleauthor | Kim, Youngchul | - |
dc.contributor.googleauthor | Kim, Young S. | - |
dc.contributor.googleauthor | Noh, Min-Young | - |
dc.contributor.googleauthor | Lee, Hanchang | - |
dc.contributor.googleauthor | Joe, Boyoung | - |
dc.contributor.googleauthor | Kim, Hyun Y. | - |
dc.contributor.googleauthor | Kim, Jeongmin | - |
dc.contributor.googleauthor | Kim, Seung H. | - |
dc.contributor.googleauthor | Park, Jiseon | - |
dc.relation.code | 2017001337 | - |
dc.sector.campus | S | - |
dc.sector.daehak | COLLEGE OF MEDICINE[S] | - |
dc.sector.department | DEPARTMENT OF MEDICINE | - |
dc.identifier.pid | hyoungkim1 | - |
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