2. Academic Validation
  3. Antitubercular and cytotoxic tigliane-type diterpenoids from Croton tiglium

Antitubercular and cytotoxic tigliane-type diterpenoids from Croton tiglium

  • Bioorg Med Chem Lett. 2016 Oct 15;26(20):4996-4999. doi: 10.1016/j.bmcl.2016.09.002.
Bi-Qing Zhao 1,  Shuai Peng 1,  Wei-Jun He 2,  Yong-Hong Liu 3,  Jun-Feng Wang 4,  Xiao-Jiang Zhou 5
Affiliations

Affiliations

  • 1 College of Pharmacy, Hunan University of Chinese Medicine, Changsha 410208, PR China.
  • 2 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.
  • 3 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.
  • 4 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. Electronic address: wangjunfeng@scsio.ac.cn.
  • 5 College of Pharmacy, Hunan University of Chinese Medicine, Changsha 410208, PR China; State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China. Electronic address: gale9888@163.com.
PMID: 27623549 DOI: 10.1016/j.bmcl.2016.09.002
Abstract

Five new tigliane diterpene esters (1-5), highly oxygenated tetracyclic diterpenoid carbon skeleton, together with three known analogues (6-8) were isolated from the leaves of Croton tiglium. Extensive NMR and mass spectroscopic analysis were used to elucidate their structures. Most of the isolated compounds were tested for their cytotoxic and antitubercular activities. Among them, the cytotoxic activities of these tigliane-type diterpenes strongly depend on the species of the tumor cells. Especially, these bioactivity compounds showed strong cytotoxic activities against the K562 cell line, and their inhibition effects were close to the positive control Taxol. Furthermore, compounds 1, 2, 6, and 7 showed potent antitubercular activities with MIC values of 19.5, 20.9, 20.5, and 13.4μM, respectively.

Keywords

Antitubercular activity; Croton tiglium; Cytotoxicity; Diterpenoids; Tiglianes.

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