Natural neuro-inflammatory inhibitors from Caragana turfanensis

  • Bioorg Med Chem Lett. 2017 Oct 15;27(20):4765-4769. doi: 10.1016/j.bmcl.2017.08.047.
Yan Song  1 ,  Lan Pan  2 ,  Wenjie Li  3 ,  Yingying Si  1 ,  Di Zhou  1 ,  Chengjian Zheng  4 ,  Xiaofang Hao  1 ,  Xinyue Jia  2 ,  Yuemei Jia  2 ,  Minghui Shi  2 ,  Xiaoguang Jia  2 ,  Ning Li  5 ,  Yue Hou  6
Affiliations
  • 1. Traditional Chinese Materia Medica Academy, Shenyang Pharmaceutical University, Wenhua Road 103, Shenyang 110016, China; Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University), Ministry of Education, Wenhua Road 103, Shenyang 110016, China.
  • 2. Xinjiang Institute of Chinese Materia Medica and Ethnodrug, Xinming Road 9, Urumqi 830002, China.
  • 3. Women And Children's Hospital of Shenyang, Shenyang City, China.
  • 4. Department of Pharmacognosy, School of Pharmacy, Second Military Medical University, Shanghai 200433, China.
  • 5. Traditional Chinese Materia Medica Academy, Shenyang Pharmaceutical University, Wenhua Road 103, Shenyang 110016, China; Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University), Ministry of Education, Wenhua Road 103, Shenyang 110016, China. Electronic address: [email protected].
  • 6. College of Life and Health Sciences, Northeastern University, Shenyang 110004, China. Electronic address: [email protected].
PMID: 28911817 DOI: 10.1016/j.bmcl.2017.08.047
Abstract

Because of the critical role of over-activated microglia in the progress of neurodegenerative diseases, it has been selected as a potential therapeutic target for drug discovery. In order to find natural neuroinflammatory inhibitors, we carried out a bioactivity-oriented phytochemical research of Caragana turfanensis Kom. (Krassn.), which is a folk medicine widely distributed in Xinjiang. As a result, a new coumarin lactone caraganolide A (1) and 35 known components were characterized from the effective extract of C. turfanensis. Furthermore, their anti-neuroinflammatory effects were evaluated in LPS-induced BV2 microglial cells using Griess assay to determine the release of nitric oxide (NO). Compounds 1, 2, 4-6, 9, 13-15, 20, 29 and 30 exhibited significant inhibitory activities and no obvious cytotoxicities were observed at their effective concentrations. It is noteworthy, the new compound caraganolide A (1) (IC50 1.01±1.57µM) and 3',7,8-trihydroxy-4'-methoxyisoflavone (5) (IC506.87±2.23µM) exhibited more excellent action than that of positive control minocycline (IC50 9.07±0.86μM).

Keywords
Caragana turfanensis (Krassn.) Kom.; Caraganolide A; Chemical profile; Neuroinflammatory inhibitors.