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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:20

Article

Dellai, Afef²  Maricic, Igor³  Kumar, Vipin³  Arutyunyan, Sergey¹  Bouraoui, Abderrahman²  Nefzi, Adel¹ 

[1] Torrey Pines Inst Mol Studies, Dept Chem, Port St Lucie, FL 34987 USA

[2] Fac Pharm, Lab Pharmacol Marine, Monastir 5000, Tunisia

[3] Torrey Pines Inst Mol Studies, Lab Autoimmun, San Diego, CA 92121 USA

关键词: Parallel synthesis;    Solid phase synthesis;    Natural cyclopeptides;    Anti-inflammatory activity;   

DOI  :  10.1016/j.bmcl.2010.08.033

来源: Elsevier

【 摘 要 】

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-alpha have been identified, some of which exhibit activity superior to that observed with the natural products. (C) 2010 Elsevier Ltd. All rights reserved.

【 授权许可】

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