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Parallel synthesis and anti-inflammatory activity of cyclic peptides cyclosquamosin D and Met-cherimolacyclopeptide B and their analogs

✍ Scribed by Afef Dellai; Igor Maricic; Vipin Kumar; Sergey Arutyunyan; Abderrahman Bouraoui; Adel Nefzi

Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 393 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.08.033

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✦ Synopsis

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-a have been identified, some of which exhibit activity superior to that observed with the natural products.

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