title: Evaluation of in vitro toxicity of peptide (N-acetyl-Leu-Gly-Leu-COOH)-substituted-β-cyclodextrin derivative, a novel drug carrier, in PC-12 cells.
abstract: BACKGROUND
  Cyclodextrins (CDs) have been shown to improve physicochemical and biopharmaceutical properties of drugs when low solubility and low safety limit their use in the pharmaceutical field. Recently, a new amphiphilic peptide-substituted-β-CD, hepta-(N-acetyl-Leu-Gly-Leu)-β-CD (hepta-(N-acetyl-LGL)-β-CD), is developed which exhibited good solubility, strong inclusion ability and an appropriate average molecular weight. However, there is limited information available about its toxic effects. This study was designed to evaluate cytotoxic effects of the hepta-(N-acetyl-LGL)-β-CD (50, 200, 400, and 800 μg/ml) on rat pheochromocytoma PC-12 cells.
  
  
  RESULTS
  A significant reduction of cell viability with IC50 values of 1115.0 μg/ml, 762.4 μg/ml, and 464.9 μg/ml at 6, 12, and 24 h post-treatment, respectively, as well as increased lipid peroxide levels and DNA damage were observed.
  
  
  CONCLUSIONS
  In conclusion, hepta-(N-acetyl-Leu-Gly-Leu)-β-CD exhibit significant toxic properties at high concentrations, probably through induction of oxidative stress and genotoxicity.
authors.forename: Hamid Reza
authors.initials: HR
authors.lastname: Sadeghnia
authors.forename: Faezeh
authors.initials: F
authors.lastname: Vahdati Hassani
authors.forename: Hamid
authors.initials: H
authors.lastname: Sadeghian
authors.forename: Maryam
authors.initials: M
authors.lastname: Miandehi
authors.forename: Farzin
authors.initials: F
authors.lastname: Hadizadeh
authors.affiliation: Medical Toxicology Research Center, Pharmacy School, Mashhad University of Medical Sciences, Mashhad, Iran. karimig@mums.ac.ir.
authors.forename: Gholamreza
authors.initials: G
authors.lastname: Karimi