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제126회 대한화학회 학술발표회 및 총회 The synthesis and biological evaluation of chalcone derivatives as a neuroprotective agent against glutamate-induced HT22 mouse hippocampal neuronal cell death

등록일
2020년 9월 15일 10시 26분 51초
접수번호
1060
발표코드
MEDI.P-433 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
10월 21일(수) 17:30~18:00
발표형식
포스터
발표분야
Medicinal Chemistry
저자 및
공동저자
Gyuwon Huh, Heesu Lee1, Ae Nim Pae2, Jae Wook Lee3,*
Natural Products Research Center, Korea Institute of Science and Technology, Korea
1Department of Dentistry, Gangneung-Wonju National University, Korea
2Korea Institute of Science and Technology, Korea
3Convergence Research Center for Dementia DTC, Korea Institute of Science and Technology, Korea
17 chalcone analogues were synthesized from 7-methoxy-3,4-dihydronaphthalen1(2H)-one and various aromatic aldehydes under basic condition. These chalcone analogues were evaluated for the neuroprotective effects against glutamate-induced neurotoxicity. In the cell based assay, we have identified a compound C01 as neuronal cell protection agent. This compound inhibits the Ca2+ influx and cellular ROS accumulation inside the cell and the FACS analysis using annexin V and PI shows that C01 significantly reduced apoptotic or dead cell death induced by 5 mM glutamate. Further, western blot analysis indicates that glutamate induced activation of MAPKs were inhibited by compound C01 treatment. Also, the C01 increases the anti-apoptotic protein Bcl-2 and decreases pro-apoptotic protein Bax. C01 protects neuronal cells from apoptosis by preventing the translocation of AIF into nucleus. Taken together, treatment of C01 results in decreasing the neurotoxicity induced by 5 mM of glutamate. As a result, we confirm that C01 has neuroprotective effects against glutamate induced toxicity in HT22 hippocampal neuronal cells.

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