ArticleDrug design, development and therapy2025
Dolutegravir Derivatives Alleviate LPS-Induced Microglial Inflammation by Suppressing STAT1/3 Nuclear Translocation.
Article in Drug design, development and therapy, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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6 authors.
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Abstract
Purpose: Microglial inflammation plays a significant role in a variety of neurological disorders. Dolutegravir as a antiretroviral drug has been reported to inhibit the secretion of pro-inflammatory cytokines. Meanwhile, compounds containing 1,2,3-triazole have shown potential anti-inflammatory properties. Therefore, this study aims to investigate the anti-inflammatory potential of dolutegravir-1,2,3-triazole structural derivatives and elucidate its associated mechanisms of action. Methods: Dolutegravir-1,2,3-triazole derivatives were synthesized through click chemistry reactions. The anti-inflammatory activity against microglial inflammation and cytotoxicity of these derivatives were evaluated using the Griess assay and MTT assay. In vitro, the effects of the compounds on the expression of inflammatory mediators in LPS-stimulated BV-2 microglial cells were assessed using Real-time PCR, ELISA, and Western blot. In vivo, the effects of the compounds on microglial inflammation and synaptic deficits in the hippocampus of LPS-challenged mice were evaluated using Real-time PCR, immunofluorescence, and Western blot. Results: We discovered compound Conclusion: Compound
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