121st General Meeting of the KCS

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