Faculté de Pharmacie, Laboratoire de Pharmacologie Marine, 5000 Monastir, Tunisia.
Bioorg Med Chem Lett. 2010 Oct 1;20(19):5653-7. doi: 10.1016/j.bmcl.2010.08.033. Epub 2010 Aug 11.
We report the parallel synthesis of two natural cyclopeptides, isolated from the seeds of Annona squamosa, cyclosquamosin D (A1), and Met-cherimolacyclopeptide B (B) and their analogs. All of the compounds were screened for anti-inflammatory activity by evaluating their inhibitory effects on the production of pro-inflammatory cytokines using the lipopolysaccharide stimulated macrophage J774A.1 cell line. Compounds having significant anti-inflammatory activity in suppressing the secretion of IL-6 and TNF-α have been identified, some of which exhibit activity superior to that observed with the natural products.
我们报告了两种天然环缩肽的平行合成,它们分别从 Annona squamosa 的种子中分离出来,分别是环 Squamosin D(A1)和 Met-cherimolacyclopeptide B(B)及其类似物。所有化合物都通过评估它们对脂多糖刺激的巨噬细胞 J774A.1 细胞系中促炎细胞因子产生的抑制作用来筛选抗炎活性。已经鉴定出具有抑制 IL-6 和 TNF-α分泌的显著抗炎活性的化合物,其中一些化合物的活性优于天然产物。