化学
细胞毒性
顺铂
选择性
A549电池
铂金
免疫印迹
癌细胞
细胞凋亡
生物化学
癌症研究
立体化学
体外
癌症
化疗
内科学
生物
催化作用
基因
医学
作者
Aleen Khoury,Elias Elias,Stephanie Mehanna,Wassim N. Shebaby,K. Deo,Najwa Mansour,Christian Khalil,Katia Sayyed,Jennette A. Sakoff,Jayne Gilbert,Costantine F. Daher,Christopher P. Gordon,Robin I. Taleb,Janice R. Aldrich‐Wright
标识
DOI:10.1021/acs.jmedchem.2c01310
摘要
A novel platinum(II) complex 47OMESS(II) and its platinum(IV) derivative 47OMESS(IV) were synthesized and characterized. Cytotoxicity studies against mesenchymal cells (MCs) and lung (A549), breast (MDA-MB-231), and melanoma (A375) cancer cells demonstrated 7–20-fold superior activity for both complexes relative to cisplatin. Remarkably, 47OMESS(IV) demonstrated 17–22-fold greater selectivity toward the cancerous cells compared to the non-cancerous MCs. Western blot analysis on A549 cells showed the involvement of the intrinsic apoptotic pathway. Cellular fractionation and uptake experiments in A549 cells using ICP-mass spectrometry (MS) indicated that 47OMESS(II) and 47OMESS(IV) cross the cellular membrane predominantly via active transport mechanisms. The significant improvement in selectivity that is exhibited by 47OMESS(IV) is reported for the first time for this class of complexes.
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