(R)-α-Lipoyl-Gly-l-Pro-l-Glu dimethyl ester as dual acting agent for the treatment of Alzheimer's disease.

Marinelli L., Fornasari E., Di S., Turkez H., Arslan M., Eusepi P., ...Daha Fazla

Neuropeptides, cilt.66, ss.52-58, 2017 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 66
  • Basım Tarihi: 2017
  • Doi Numarası: 10.1016/j.npep.2017.09.001
  • Dergi Adı: Neuropeptides
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.52-58
  • Anahtar Kelimeler: Alzheimer's disease, Gly-pro-Glu, Lipoic acid, Tripeptides, NEURODEGENERATIVE DISEASES, AMYLOID-BETA, IN-VITRO, ANALOGS, PEPTIDES, CELLS, GPE, EPTASTIGMINE, DERIVATIVES, HYPOTHESIS
  • Atatürk Üniversitesi Adresli: Hayır

Özet

In this study, effects of LA-GPE dimethyl ester) and GPE (Gly-L-Pro-L-Glu) on the cytotoxic action of A beta(1-42) were tested with differentiated human neuroblastoma SH-SY5Y cells as cellular Alzheimer model via measurements of mitochondria) viability (MTT assay) and lactate dehydrogenase release (LDH assay). Effects of LA-GPE and GPE on acetylcholinesterase (AChE) activity, total antioxidant capacity (TAC) and total oxidative status (TOS) levels, and neural cell apoptosis and necrosis were also determined. In addition, biological safety of these novel formulations was evaluated in human blood cells using different cytotoxicity and genotoxicity assays. Our results indicated that both compounds could block A beta(1-42) induced cell death. LA-GPE reduced A beta-induced AChE activity and oxidative stress, suggesting it as a multifunctional compound potentially valuable for the treatment of Alzheimer's disease (AD).