Abstract
Objectives: To synthesize and evaluate the anti-inflammatory potential of fifteen naphthoquinones (NQs), determining their ability to inhibitory nitric oxide (NO•) and prostaglandin E2 (PGE2) production. Methods: NQs were screened for their inhibitory effect on NO• and PGE production using LPS-activated RAW 264.7 macrophages. Results: Three linear furanonaphthoquinones (4-6) were identified as potent inhibitors of NO• and PGE2 production, with IC50 values ranging from 0.45 to 2.86 μM (NO•) and 0.38 to 1.65 (PGE2), highlighting the potent activity showed by compound 5 with IC50 values lower than one and high selectivity indices. Conclusions: Synthesized furanonaphthoquinones constitute leading compounds for the design of new anti-inflammatory agents and provide a valuable tool for designing new NQs that might be useful to treat inflammation. The evaluation of compounds 4-6 using in vivo models is warranted.
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