Neuroprotective oleanane triterpenes from the roots of Bupleurum chinense

  • Bioorg Med Chem Lett. 2016 Mar 15;26(6):1594-1598. doi: 10.1016/j.bmcl.2016.02.004.
Dan-Qi Li  1 Le Zhou  1 Di Wang  1 Jie Wu  1 Ling-Zhi Li  1 Xiao-Xiao Huang  1 Qing-Bo Liu  1 Ying-Ying Wu  1 Song Lin  2 Jing-Yu Yang  3 Shao-Jiang Song  4 Chun-Fu Wu  5
Affiliations
  • 1. School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, 103 Wenhua Rd., Shenyang 110016, People's Republic of China; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
  • 2. School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, 103 Wenhua Rd., Shenyang 110016, People's Republic of China; Department of Pharmacy, General Hospital of Shenyang Military Area Command, Shenyang 110840, People's Republic of China.
  • 3. Department of Pharmacology, Shenyang Pharmaceutical University, 103 Wenhua Rd., Shenyang 110016, People's Republic of China.
  • 4. School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, 103 Wenhua Rd., Shenyang 110016, People's Republic of China; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China. Electronic address: [email protected].
  • 5. Department of Pharmacology, Shenyang Pharmaceutical University, 103 Wenhua Rd., Shenyang 110016, People's Republic of China. Electronic address: [email protected].
Abstract

The discovery of new natural compounds with pharmacological properties is an increasingly important field, and a continuous phytochemical investigation of the roots of Bupleurum chinense D.C. has led to the isolation of 17 triterpenoids, including three new oleanane Triterpenes (1-3) together with 14 known ones. Their structures were determined on the basis of 1D and 2D NMR spectra as well as HR-ESI-MS data. The cytotoxicities of all compounds against five selected human Cancer cell lines were assayed. Only compounds 9 and 14 exhibited moderate activities. Recently, a number of investigations have focused on the neuroprotective properties of triterpenoids in B. chinense. In order to expand our knowledge about this herb, the neuroprotective effects of compounds 1-17 against hydrogen peroxide (H2O2)-induced neuronal cell damage in human neuroblastoma SH-SY5Y cells were evaluated. Compounds 1-3, 6-7 showed significant neuroprotective effects against H2O2-induced SH-SY5Y cell death. Preliminary structure-activity relationships (SARs) between neuroprotective effects and the isolates were also discussed.

Keywords
Bupleurum chinense D.C.; Cytotoxicity; Neuroprotective effects; Triterpenoids.