ent-Abietane-type diterpenoids from the roots of Euphorbia ebracteolata with their inhibitory activities on LPS-induced NO production in RAW 264.7 macrophages

  • Bioorg Med Chem Lett. 2016 Jan 1;26(1):1-5. doi: 10.1016/j.bmcl.2015.11.080.
Zhi-guo Liu  1 Zhan-lin Li  1 Da-Hong Li  1 Ning Li  1 Jiao Bai  1 Feng Zhao  2 Da-li Meng  3 Hui-ming Hua  4
Affiliations
  • 1. Department of Natural Products Chemistry, Shenyang Pharmaceutical University, Shenyang 110016, PR China; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
  • 2. School of Pharmacy, Yantai University, Yantai 264005, PR China.
  • 3. Department of Natural Products Chemistry, Shenyang Pharmaceutical University, Shenyang 110016, PR China; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China. Electronic address: [email protected].
  • 4. Department of Natural Products Chemistry, Shenyang Pharmaceutical University, Shenyang 110016, PR China; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China. Electronic address: [email protected].
Abstract

Ten ent-abietane Diterpenoids (1-10), including four new (1-4) and six known ones (5-10) were isolated from the roots of Euphorbia ebracteolata. Their structures were determined by 1D, 2D NMR, and HRESIMS. Compounds 2, 4, and 7 exhibited significant inhibitory activities on lipopolysaccharide (LPS)-induced nitric oxide production in RAW 264.7 macrophages with IC50 values of 0.69, 1.97, and 0.88μM, respectively. A primary structure-activity relationship was also discussed.

Keywords
Anti-inflammation; Ent-abietane diterpenoids; Euphorbia ebracteolata.