|
Type |
Poster Presentation |
Area |
Medicinal Chemistry |
Room No. |
Event Hall |
Time |
4월 19일 (목요일) 11:00~12:30 |
Code |
MEDI.P-650 |
Subject |
Click Reaction of Guggelsterone Derivatives and its kidney protective effect |
Authors |
TAEJUNG KIM, Jungyeob Ham, Heesu lee1, Jae Wook Lee2,* Natural Products Research, Korea Institute of Science and Technology, Korea 1Department of Dentistry, Gangneung-Wonju National University, Korea 2Convergence Research Center for Dementia DTC, Korea Institute of Science and Technology, Korea |
Abstract |
Guggulsterone is known as anti-inflammatory activity by inhibiting activation of NF-kB signal. Therefore, it is assumed that it may have a protective activity toward kidney injury. Here, we synthesized six guggulsterone derivatives using [3+2] click reaction with aryl and alky acetylene with relatively high yields. These six guggulsterone derivatives were evaluated for kidney protection effects to cisplatin injury. Among the guggulsterone-triazole derivatives, compound 6g, which contains a hydroxyl methyl group, was the most active of all the derivatives. In an additional study, we determined that inhibition of the mitogen-activated protein kinase/caspase-3 signaling cascade by 6g mediates its protective effects against cytotoxicity in cultured LLC-PK1 cells. |
E-mail |
jwlee5@kist.re.kr |
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