Cytotoxicity of electrophilic iron(II)-clathrochelates in human promyelocytic leukemia cell line

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• 作者：Jenny Blechinger^a ; Oleg A. Varzackii^b ; Vladyslava Kovalska^c ; Genrikh E. Zelinskii^d ; Yan Z. Voloshin^d ; Elisa Kinski^a ; Andriy Mokhir^a ;
• 关键词：Clathrochelate ; Iron ; Alkylation ; Glutathione ; Cancer
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 January 2016
• 年：2016
• 卷：26
• 期：2
• 页码：626-629
• 全文大小：637 K

文摘

We observed that electrophilic iron(II)–clathrochelates exhibit significant cytotoxicity in human promyelocytic leukemia cells (IC₅₀ = 6.5 ± 4.6 μM), which correlates with the enhancement of intracellular oxidative stress (17-fold increase with respect to the cells treated with the solvent only). Based on in vitro studies we suggested that this effect is caused by alkylation of glutathione leading to inhibition of the cellular antioxidative system and by catalytic generation of reactive oxygen species by products of the alkylation reaction.