2. Academic Validation
  3. Lignans from the stems of Clematis armandii ("Chuan-Mu-Tong") and their anti-neuroinflammatory activities

Lignans from the stems of Clematis armandii ("Chuan-Mu-Tong") and their anti-neuroinflammatory activities

  • J Ethnopharmacol. 2014 May 14;153(3):737-43. doi: 10.1016/j.jep.2014.03.036.
Juan Xiong 1,  Van-Binh Bui 2,  Xin-Hua Liu 3,  Zhi-Lai Hong 1,  Guo-Xun Yang 1,  Jin-Feng Hu 4
Affiliations

Affiliations

  • 1 Department of Natural Products Chemistry, Fudan University, Shanghai 201203, China.
  • 2 Department of Chemistry, School of Science & Engineering, No. 3663 Zhongshan Road N, East China Normal University, Shanghai 200062, China; Department of Chemistry, Hoa Lu University, No. 491C Xuanthanh Road, Ninh Binh 40000, Vietnam.
  • 3 Department of Pharmacology, School of Pharmacy, Fudan University, No. 826 Zhangheng Road, Shanghai 201203, China. Electronic address: [email protected].
  • 4 Department of Natural Products Chemistry, Fudan University, Shanghai 201203, China; Department of Chemistry, School of Science & Engineering, No. 3663 Zhongshan Road N, East China Normal University, Shanghai 200062, China. Electronic address: [email protected].
PMID: 24661966 DOI: 10.1016/j.jep.2014.03.036
Abstract

Ethnopharmacological relevance: The dried stems of Clematis armandii (Caulis clematidis armandii), named "Chuan-Mu-Tong" in Chinese Pharmacopoeia, have been traditionally used as an herbal remedy mainly for inflammation-associated diseases. The Aim of the study is to identify the potential anti-neuroinflammatory components from Clematis armandii.

Materials and methods: The ethanol extract of "Chuan-Mu-Tong" was suspended in H₂O and exhaustively extracted with CH₂Cl₂. The CH₂Cl₂ fraction was successively subjected to column chromatography (CC) over silica gel, Sephadex LH-20, and semi-preparative HPLC. The structures of the isolated compounds were identified by spectroscopic methods and by comparison with those reported in the literature. Their anti-neuroinflammatory activities were evaluated by inhibitory effects on pro-inflammatory mediators [e.g. nitric oxide (NO) and tumor necrosis factor-alpha (TNF-α)] in lipopolysaccharide (LPS)-activated BV-2 cells.

Results: One new and sixteen known Lignans were isolated and characterized. The absolute configuration of the new lignan, (7R,8S)-9-acetyl-dehydrodiconiferyl alcohol (1), was elucidated by a combination of 1D/2D NMR techniques and the Electronic Circular Dichroism (ECD) spectroscopy based on the empirical helicity rules. The anti-neuroinflammatory bioassay showed that compounds 1, (7R,8S)-dehydrodiconiferyl alcohol (2), erythro-guaiacylglycerol-β-coniferyl ether (5), and threo-guaiacylglycerol-β-coniferyl ether (6) displayed significant inhibitory effects on NO production. Among them, neolignans 1 and 2 exhibited more potent activities than the positive control (N(G)-monomethyl-L-arginine, L-NMMA), with an IC₅₀ value of 9.3 and 3.9 μM, respectively. Moreover, both 1 and 2 were also found to concentration-dependently suppress the TNF-α release in LPS-stimulated BV-2 cells.

Conclusion: The results revealed that Lignans are the major components of "Chuan-Mu-Tong", and their anti-neuroinflammatory activities strongly support the traditional application of this herb medicine on inflammation. Moreover, the dihydrobenzo[b]furan neolignans 1 and 2 as well as Caulis clematidis armandii could be further exploited as new therapeutic agents to treat inflammation-mediated neurodegenerative and aging-associated diseases.

Keywords

Anti-neuroinflammation; Clamatis armandii; Lignans; NO; Ranunculaceae; TNF-α.

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