2. Academic Validation
  3. Natural potential neuroinflammatory inhibitors from Alhagi sparsifolia Shap

Natural potential neuroinflammatory inhibitors from Alhagi sparsifolia Shap

  • Bioorg Med Chem Lett. 2017 Feb 15;27(4):973-978. doi: 10.1016/j.bmcl.2016.12.075.
Di Zhou 1,  Hongyan Wei 2,  Zhe Jiang 3,  Xuezheng Li 3,  Kun Jiao 4,  Xiaoguang Jia 2,  Yue Hou 5,  Ning Li 6
Affiliations

Affiliations

  • 1 School of Traditional Chinese Materia Medica, 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, Urumqi 830002, China.
  • 3 Department of Pharmacy, Affiliated Hospital of Yanbian University, Yanji 133000, China.
  • 4 College of Life and Health Sciences, Northeastern University, Shenyang 110819, China.
  • 5 College of Life and Health Sciences, Northeastern University, Shenyang 110819, China. Electronic address: [email protected].
  • 6 School of Traditional Chinese Materia Medica, 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].
PMID: 28073678 DOI: 10.1016/j.bmcl.2016.12.075
Abstract

Neuroinflammation is a key contributor to neuronal damage in neurodegenerative diseases. In our previous work on natural effective neuroinflammatory inhibitors, Alhagi sparsifolia Shap. (Leguminosae), a folk medicine widely distributed in Xinjiang, attracted our attention because of its significant anti-neuroinflammatory effect. Therefore, further investigation of the bioactive material basis was carried out. As a result, 33 major components were characterized and identified by chromatographic and spectral methods, respectively. Furthermore, the anti-neuroinflammatory effects of the extract and purified constituents were evaluated in LPS-induced N9 cells in vitro. The results displayed that compounds 1, 2, 3, 5, 6, 8, 11, 15, 16, 17, 22, 23, 25, 26, 28, 30, 33 could exhibit significant inhibitory activities without obvious cytotoxicities at their effective concentrations. Especially, isorhamnetin (1) (IC50 17.87μM), quercetin (2) (10.22μM), 3',7-dihydroxyl-4'-methoxylisoflavone (5) (17.43μM), 3',7-dihydroxyl-4',6-dimethoxylisoflavone (6) (11.21μM), syringgaresinol (16) (2.68μM), bombasinol A (17) (7.61μM), aurantiamide (23) (14.91μM) and 1,3,3,4-tetramethyl cyclopentene (33) (2.63μM) showed much stronger inhibiting effect than that of the positive control minocycline (19.89μM). Therefore, the effective compositions might be responsible for the significant neuroinflammation inhibitory activities exhibited by the herb. Moreover, compounds 16 and 33 could be good leading compounds for the development of potential therapeutic agents against neurodegenerative diseases.

Keywords

Alhagi sparsifolia Shap.; Effective chemical composition; Neurodegenerative diseases; Neuroinflammatory inhibitors; Overactivated microglial cells.

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