2. Academic Validation
  3. Five new phorbol esters with cytotoxic and selective anti-inflammatory activities from Croton tiglium

Five new phorbol esters with cytotoxic and selective anti-inflammatory activities from Croton tiglium

  • Bioorg Med Chem Lett. 2015 May 1;25(9):1986-9. doi: 10.1016/j.bmcl.2015.03.017.
Jun-Feng Wang 1,  Sheng-Hui Yang 2,  Yan-Qun Liu 2,  Din-Xiang Li 3,  Wei-Jun He 2,  Xiao-Xiao Zhang 2,  Yong-Hong Liu 4,  Xiao-Jiang Zhou 5
Affiliations

Affiliations

  • 1 College of Pharmacy, Hunan University of Chinese Medicine, Changsha 410208, PR China; CAS Key Laboratory of Tropical Marine Bio-resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica/RNAM Center for Marine Microbiology, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, PR China.
  • 2 College of Pharmacy, Hunan University of Chinese Medicine, Changsha 410208, PR China.
  • 3 Key Laboratory of Hunan Province for Integrated Traditional Chinese and Western Medicine on Prevention and Treatment of Cardio-Cerebral Diseases, Hunan University of Chinese Medicine, Changsha 410208, PR China.
  • 4 CAS Key Laboratory of Tropical Marine Bio-resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica/RNAM Center for Marine Microbiology, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, PR China. Electronic address: yonghongliu@scsio.ac.cn.
  • 5 College of Pharmacy, Hunan University of Chinese Medicine, Changsha 410208, PR China. Electronic address: gale9888@163.com.
PMID: 25819096 DOI: 10.1016/j.bmcl.2015.03.017
Abstract

Five new phorbol esters, (four phorbol diesters, 1-4, and one 4-deoxy-4α-phorbol diester, 5), as well as four known phorbol esters analogues (6-9) were isolated and identified from the branches and leaves of Croton tiglium. Their structures were elucidated mainly by extensive NMR spectroscopic, and mass spectrometric analysis. Among them, compound (1) was the first example of a naturally occurring phorbol ester with the 20-aldehyde group. Compounds 2-5, and 7-9 showed potent cytotoxicity against the K562, A549, DU145, H1975, MCF-7, U937, SGC-7901, HL60, Hela, and MOLT-4 cell lines, with IC50 values ranging from 1.0 to 43 μM, while none of the compounds exhibited cytotoxic effects on normal human cell lines 293T and LX-2, respectively. In addition, compound 3 exhibited moderate COX-1 and COX-2 inhibition, with IC50 values of 0.14 and 8.5 μM, respectively.

Keywords

Anti-inflammatory activity; Croton tiglium; Cytotoxicity; Phorbol esters.

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