Synthetic menthyl 伪/尾-(1鈫?)-diglucopyranosides-induced cell death in human leukemia cells is dependent on caspases

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• 作者：Marí ; a Teresa Marrero^a ; Sara Tejera^b ; Sara Esté ; vez^a ; José ; Quintana^a ; Carlos Mayato^b ; Rosa L. Dorta^b ; Jesú ; s T. Vá ; zquez^b ; Francisco Esté ; vez^a ; ^{festevez@dbbf.ulpgc.es}
• 关键词：Apoptosis ; Carbohydrates ; Caspases ; Poly(ADP-ribose)polymerase ; Reactive oxygen species
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 June, 2012
• 卷：22
• 期：11
• 页码：3665-3670
• 文件大小：863 K

摘要

A series of alkyl 伪/尾-(1鈫?)-diglucopyranosides 1鈭?2 were synthesized and assessed for cytotoxicity against HL-60, U937, Molt-3 and MCF-7 cancer cell lines. The menthyl derivatives displayed strong cytotoxic properties showing IC₅₀ values between 6 and 16 渭M. Furthermore, we demonstrated that the selected synthetic (+)-menthyl 尾-(1鈫?)-diglucopyranoside 5 induces apoptotic cell death in human leukemia cells through a mechanism that involves activation of multiple caspases. Cell death was completely prevented by the non-specific caspase inhibitor z-VAD-fmk and found to be associated with the release of cytochrome c, an increase in the expression of Bax levels and a decrease in the generation of reactive oxygen species.