Synthesis and Anti-Inflammatory Effect of Sinomenine 4-Hydroxy Esters
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In order to find more active anti-neuroinflammatory sinomenine derivatives, 17 sinomenine 4-hydroxy esters were designed and prepared. All synthesized derivatives were structurally confirmed by ESI-MS and PMR. Their anti-neuroinflammatory effects were evaluated using LPS-stimulated BV-2 microglia cells. Among them, four compounds presented more than 80% of cell viability. Compound 8 showed remarkable inhibition of nitric oxide (NO) release by the Griess method. Furthermore, esters 5–9 were tested to check their suppressive effects on xylene-induced ear edema. It was observed that 8 was more active and less toxic than 5–7 with shorter aliphatic chains.
This work was partly supported by National Natural Science Foundation of China (81373480, 81573529, 21372056), Zhenjiang Social Development Project (SH2014062), and Jiangsu University Graduate Innovation Fund (Y13A096).
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