Evaluation of guggulsterone derivatives as novel kidney cell protective agents against cisplatin-induced nephrotoxicity |
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| Authors: | Dahae Lee Taejung Kim Ki Hyun Kim Jungyeob Ham Tae Su Jang Ki Sung Kang Jae Wook Lee |
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| Affiliation: | 1. College of Korean Medicine, Gachon University, Seonngman 13120, Republic of Korea;2. School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea;3. Natural Constituent Research Center, Korea Institute of Science and Technology, Gangneung 25451, Republic of Korea;4. Institute of Green Bio Science &Technology, Seoul National University, Pyeong Chang 232-916, Republic of Korea;5. Convergent Research Center for Dementia, Korea Institute of Science and Technology, Seoul 02792, Republic of Korea;6. Department of Biological Chemistry, Korea University of Science and Technology, Daejeon 34113 Republic of Korea |
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| 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. |
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| Keywords: | Guggulsterone Kidney protection Click chemistry MAPK |
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