Background: Cyclodextrins (CDs) have been shown to improve physicochemical and biopharmaceutical\nproperties of drugs when low solubility and low safety limit their use in the pharmaceutical field. Recently, a new\namphiphilic peptide-substituted-?-CD, hepta-(N-acetyl-Leu-Gly-Leu)-?-CD (hepta-(N-acetyl-LGL)-?-CD), is\ndeveloped which exhibited good solubility, strong inclusion ability and an appropriate average molecular weight.\nHowever, there is limited information available about its toxic effects. This study was designed to evaluate\ncytotoxic effects of the hepta-(N-acetyl-LGL)-?-CD (50, 200, 400, and 800 ?g/ml) on rat pheochromocytoma PC-12\ncells.\nResults: A significant reduction of cell viability with IC50 values of 1115.0 ?g/ml, 762.4 ?g/ml, and 464.9 ?g/ml at 6,\n12, and 24 h post-treatment, respectively, as well as increased lipid peroxide levels and DNA damage were observed.\nConclusions: In conclusion, hepta-(N-acetyl-Leu-Gly-Leu)-?-CD exhibit significant toxic properties at high concentrations,\nprobably through induction of oxidative stress and genotoxicity.
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