Methylsalicylate 2-O-D-lactoside, a novel salicylic acid analogueacts as an antiinflammatoryagent on microglia and astrocytes

中国药理学与毒理学杂志
中国药理学与毒理学杂志 ›› 2011, Vol. 25 ›› Issue (增刊) : 32-32.
心脑血管药理

Methylsalicylate 2-O-D-lactoside, a novel salicylic acid analogueacts as an antiinflammatoryagent on microglia and astrocytes

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Methylsalicylate 2-O-D-lactoside, a novel salicylic acid analogueacts as an antiinflammatoryagent on microglia and astrocytes

  • LAN Xi, LIU Rui , SUN Lan, ZHANG Tian-tai , DU Guan-hua
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OBJECTIVE Neuroinflammation has been known to play a critical role in the pathogenesis of alzheimer′s disease (AD). Activation of microglia and astrocytes is a characteristic of brain inflammation. Epidemiological studies have shown that longterm use of nonsteroidal antiinflammatory drugs (NSAIDs) delays the onset of AD and suppresses its progression. Methylsalicylate-2-O-β-D-lactoside (DL0309) is a new molecule chemically related to salicylic acid. The present study aimed to evaluate the antiinflammatory effects of DL0309. METHODS Cells were pretreated for 1 h with DL0309 at the concentration of 0.1, 1 and 10 μmol·L-1 respectively, and then stimulated by lipopolysaccharide (LPS, 0.5 μg·ml-1) for 24 h. Pro-inflammatory cytokines (IL-6, IL-1β and TNF-α) levels, NO production and COX1/2 expression were measured. After exposing to LPS (0.5μg·ml-1) for 10min or 45 min, the activation of NF-κB signal pathway was measured by western blotting. RESULTS Our studies showed that DL0309 significantly inhibited LPSinduced the release of pro-inflammatory cytokines (IL-6, IL-1β, and TNF-α) and the expression of inflammatory related proteins (iNOS, COX-1, and COX-2) in microglia and astrocytes. At the concentration of 10 μmol·L-1, DL0309 prominently inhibited LPS-induced the activation of NF-κB in glia cells via blocking the phosphorylation of IKK, p65 and IκB degradation. CONCLUSION We have first demonstrated that DL0309 exerts antiinflammatory effects in glia cells by inhibiting different proinflammatory cytokines and iNOS/NO. Furthermore, it also regulates the NF-κB signaling pathway by blocking IKK, IκB and p65 activation. It also acts as a non-selective COX inhibitor in glia cells. These studies suggest that DL0309 may be effective in the treatment of neuroinflammatory disorders including AD.

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Methylsalicylate 2-O-D-lactoside, a novel salicylic acid analogueacts as an antiinflammatoryagent on microglia and astrocytes. 中国药理学与毒理学杂志. 2011, 25(增刊): 32-32
LAN Xi;LIU Rui;SUN Lan;ZHANG Tian-tai;DU Guan-hua. Methylsalicylate 2-O-D-lactoside, a novel salicylic acid analogueacts as an antiinflammatoryagent on microglia and astrocytes. Chinese Journal of Pharmacology and Toxicology. 2011, 25(增刊): 32-32

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