Evaluation of guggulsterone derivatives as novel kidney cell protective agents against cisplatin-induced nephrotoxicity
- Authors
- Lee, Dahae; Kim, Taejung; Kim, Ki Hyun; Ham, Jungyeob; Jang, Tae Su; Kang, Ki Sung; Lee, Jae Wook
- Issue Date
- 15-Jul-2017
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Guggulsterone; Kidney protection; Click chemistry; MAPK
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.27, no.14, pp.3156 - 3161
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 27
- Number
- 14
- Start Page
- 3156
- End Page
- 3161
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/5918
- DOI
- 10.1016/j.bmcl.2017.05.033
- ISSN
- 0960-894X
- Abstract
- Guggulsterone derivatives were prepared using [3+2] click chemistry with aryl and alkyl acetylene. The series of derivatives were evaluated for their cellular protective effects on cisplatin-treated cultured LLC-PK1 kidney epithelial cells. 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. (C) 2017 Elsevier Ltd. All rights reserved.
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