Abstract
Purpose: To investigate the anti-inflammatory activity of Symplocos sumuntia Buch.-Ham. ex D. Don and identify the main secondary metabolites responsible for this effect. Methods: The in vitro anti-inflammatory activity of the plant extract and isolated compounds was determined in terms of the ability to inhibit the production of nitric oxide (NO), and expressions of iNOS and COX-2 proteins in RAW264.7 cells stimulated by lipopolysaccharide (LPS). Compounds were isolated and identified by spectroscopic methods. Results: The methanol extract of S. sumuntia leaves showed strong inhibitory effects on nitric oxide (NO) production and expression of iNOS and COX-2 in LPS-induced RAW264.7 cells. A phytochemical assay-guided fractionation of the methanol extract of S. sumuntia leaves led to the isolation of four lignans which are arctigenin (1), matairesinol (2), monomethylpinoresinol (3) and pinoresinol (4). These compounds were identified for the first time from S. sumuntia . All four compounds inhibited the production of nitric oxide (NO), with arctigenin showing the most potent activity with half-maximal inhibitory concentration (IC 50 ) value of 4.08 μM. Conclusion: S. sumuntia is a promising source of anti-inflammatory agents, which may clarify to the therapeutic use of this plant in Vietamese traditional medicine. Keywords: Symplocos sumuntia , Symplocos caudata , Lignan, Arctigenin, Anti-inflammatory
Highlights
Symplocos is a genus of flowering plants with about 300 species distributed in Asia, Australia and America [1]
In our continuing search for anti-inflammatory agents of natural origin, we found that a methanol extract of Symplocos sumuntias trongly suppressed the production of nitric oxide (NO) in LPS-induced RAW264.7 cells
Bioassay-guided fractionation of the methanol extract of S. sumuntia led to the isolation of four lignans (Figure 3)
Summary
Symplocos is a genus of flowering plants with about 300 species distributed in Asia, Australia and America [1]. It is known that inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), two major inflammatory mediators, are expressed in a variety of cells including macrophages in response to pro-inflammatory stimuli such as lipopolysaccharide (LPS), ILs, and TNF-α [10] They are responsible for the production of NO and prostaglandins, which have been implicated in the tissue destruction and pathogenesis of a number of immunological and inflammatory diseases [10]. In our continuing search for anti-inflammatory agents of natural origin, we found that a methanol extract of Symplocos sumuntias trongly suppressed the production of NO in LPS-induced RAW264.7 cells (with 60.1% at a concentration of 30 μg/mL). In Western blot analysis, SS prevented the LPS-induced expressions of COX-2 and iNOS at 10 and 30 μg/mL (Figure 2) These results suggested that S. sumuntia might contain strong anti-inflammatory compounds. Means were checked for statistical differences by Student’s t-test with error probability set at p < 0.05
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