Synthesis and antiageing properties of antioxidant pseudopeptides designed based on the bioisostere principle. Issue 6 (13th May 2019)

• Record Type: Journal Article
• Authors: Li, Yanbing; Zhang, Chao; Wang, Huailing; Zhou, Fan; Liu, Jie; Tang, Yinying; Jiang, Zhenlei; Liu, Zhijun; Chen, Heru
• Is Part Of: Archiv der Pharmazie. Volume 352:Issue 6(2019)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2019-05-13
• Subjects: antiageing -- antioxidant peptide -- C. elegans -- Cat‐1 -- Nhr‐8 -- stress resistance; Pharmaceutical chemistry -- Periodicals; Pharmacology -- Periodicals; 615.19
• DOI: 10.1002/ardp.201800354
• Languages: English
• ISSNs: 0365-6233

Abstract

Abstract: Nineteen antioxidant pseudopeptides were designed and synthesized. They were confirmed as mild antioxidants, in whichL1‐11 was the most active antioxidant with a cellular antioxidant activity (CAA) value of 5.65 ± 0.64 μmol QE/g, andL1‐12 was the second most active one (5.58 ± 0.66 μmol QE/g). The existence of nonnatural amino acids inL1‐12 increased its stability. Pretreatment withL1‐12 dose‐dependently extended the lifespan of Caenorhabditis elegans .L1‐12 improved resistance against UVB irradiation, oxidative stress induced by paraquat, and thermal shock. It decreased the reactive oxygen species level and upregulated the superoxide dismutase activity inside C. elegans . This pseudopeptide sensitively enhanced the expressions of the Cat‐1 and Nhr‐8 genes to reduce oxidative damage, leading to an extension of the lifespan. All the evidence support thatL1‐12 may probably be a potential antiageing agent. Abstract : Nineteen antioxidant pseudopeptides were designed, synthesized, and confirmed as mild antioxidants.L1‐11 andL1‐12 were the two most active antioxidants with activity values of 5.65 ± 0.64 and 5.58 ± 0.66 μmol QE/g. The existence of nonnatural amino acids inL1‐12 increased its stability. Pretreatment withL1‐12 as a potential antiageing agent dose‐dependently extended the lifespan of Caenorhabditis elegans .