2. Academic Validation
  3. Natural neuro-inflammatory inhibitors from Caragana turfanensis

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

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: liningsypharm@163.com.
  • 6 College of Life and Health Sciences, Northeastern University, Shenyang 110004, China. Electronic address: houyue@mail.neu.edu.cn.
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.

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