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sleep promoting effect of luteolin in mice via adenosine A1 and A2A receptorsoa mark
  • Kim, Tae Ho ;
  • Custodio, Raly James ;
  • Cheong, Jae Hoon ;
  • Kim, Hee Jin ;
  • Jung, Yi Sook
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dc.contributor.authorKim, Tae Ho-
dc.contributor.authorCustodio, Raly James-
dc.contributor.authorCheong, Jae Hoon-
dc.contributor.authorKim, Hee Jin-
dc.contributor.authorJung, Yi Sook-
dc.date.issued2019-01-01-
dc.identifier.issn2005-4483-
dc.identifier.urihttps://aurora.ajou.ac.kr/handle/2018.oak/30999-
dc.identifier.urihttps://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85074666381&origin=inward-
dc.description.abstractLuteolin, a widespread flavonoid, has been known to have neuroprotective activity against various neurologic diseases such as epilepsy, and Alzheimer’s disease. However, little information is available regarding the hypnotic effect of luteolin. In this study, we evaluated the hypnotic effect of luteolin and its underlying mechanism. In pentobarbital-induced sleeping mice model, luteolin (1, and 3 mg/kg, p.o.) decreased sleep latency and increased the total sleep time. Through electroencephalogram (EEG) and electromyogram (EMG) recording, we demonstrated that luteolin increased non-rapid eye movement (NREM) sleep time and decreased wake time. To evaluate the underlying mechanism, we examined the effects of various pharmacological antagonists on the hypnotic effect of luteolin. The hypnotic effect of 3 mg/kg of luteolin was not affected by flumazenil, a GABAA receptorbenzodiazepine (GABAAR-BDZ) binding site antagonist, and bicuculine, a GABAAR-GABA binding site antagonist. On the other hand, the hypnotic effect of 3 mg/kg of luteolin was almost completely blocked by caffeine, an antagonist for both adenosine A1 and A2A receptor (A1R and A2AR), 8-Cyclopentyl-1,3-dipropylxanthine (DPCPX), an A1R antagonist, and SCH-58261, an A2AR antagonist. From the binding affinity assay, we have found that luteolin significantly binds to not only A1R but also A2AR with IC50 of 1.19, 0.84 µg/kg, respectively. However, luteolin did not bind to either BDZ-receptor or GABAAR. From these results, it has been suggested that luteolin has hypnotic efficacy through A1R and A2AR binding.-
dc.description.sponsorshipThis research was supported by the Commercialization Promotion Agency for R and D Outcomes (COMPA) funded by the Ministry of Science and ICT (MSIT) (2018K000277), the Korea Health Technology RandD Project through the Korea Health Industry Development Institute (KHIDI), funded by the Ministry of Health and Welfare, Republic of Korea (HI18C0920), and the Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education (2018R1D1A1B07048729), Republic of Korea.-
dc.description.sponsorshipThis research was supported by the Commercialization-
dc.language.isoeng-
dc.publisherKorean Society of Applied Pharmacology-
dc.titlesleep promoting effect of luteolin in mice via adenosine A1 and A2A receptors-
dc.typeArticle-
dc.citation.endPage590-
dc.citation.number6-
dc.citation.startPage584-
dc.citation.titleBiomolecules and Therapeutics-
dc.citation.volume27-
dc.identifier.bibliographicCitationBiomolecules and Therapeutics, Vol.27 No.6, pp.584-590-
dc.identifier.doi2-s2.0-85074666381-
dc.identifier.scopusid2-s2.0-85074666381-
dc.identifier.urlhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC6824624/pdf/bt-27-584.pdf-
dc.subject.keywordAdenosine A1 receptor-
dc.subject.keywordAdenosine A2A receptor-
dc.subject.keywordElectroencephalogram-
dc.subject.keywordInsomnia-
dc.subject.keywordLuteolin-
dc.subject.keywordSleep-
dc.type.otherArticle-
dc.identifier.pissn1976-9148-
dc.description.isoatrue-
dc.subject.subareaBiochemistry-
dc.subject.subareaMolecular Medicine-
dc.subject.subareaPharmacology-
dc.subject.subareaDrug Discovery-
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