2. Academic Validation
  3. Bioactive diterpenoids from Trigonostemon chinensis: Structures, NO inhibitory activities, and interactions with iNOS

Bioactive diterpenoids from Trigonostemon chinensis: Structures, NO inhibitory activities, and interactions with iNOS

  • Bioorg Med Chem Lett. 2016 Oct 1;26(19):4785-4789. doi: 10.1016/j.bmcl.2016.08.026.
Jing Xu 1,  Maoqin Peng 2,  Xiaocong Sun 2,  Xingyu Liu 2,  Ling Tong 3,  Guochen Su 2,  Yasushi Ohizumi 4,  Dongho Lee 5,  Yuanqiang Guo 6
Affiliations

Affiliations

  • 1 State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300350, People's Republic of China. Electronic address: xujing611@nankai.edu.cn.
  • 2 State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300350, People's Republic of China.
  • 3 State Key Laboratory of Core Technology in Innovative Chinese Medicine, Pharmaceutical Analysis Institute, Tasly Academy, Tianjin 300410, People's Republic of China.
  • 4 Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai 980-8578, Japan.
  • 5 Department of Biosystems and Biotechnology, College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea.
  • 6 State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300350, People's Republic of China. Electronic address: victgyq@nankai.edu.cn.
PMID: 27570243 DOI: 10.1016/j.bmcl.2016.08.026
Abstract

A phytochemical investigation to obtain new NO inhibitors led to the isolation of two new (1 and 2) and four known (3-6) Diterpenoids from Trigonostemon chinensis. Their structures were elucidated on the basis of extensive 1D and 2D NMR spectroscopic data analyses, and the absolute configurations of new compounds were established by experimental and calculated ECD spectra. The inhibitory activities on lipopolysaccharide-induced NO production in murine microglial BV-2 cells of these Diterpenoids were evaluated, and all of the compounds showed inhibitory effects. The interactions of bioactive compounds with iNOS protein were also studied by molecular docking.

Keywords

Diterpenoids; Molecular docking; NO inhibitory activities; Trigonostemon chinensis; iNOS.

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