PDF(Pubmed)
Abstract：
Developing clinically meaningful nanomedicines for cancer therapy requires the drugs to be effective, safe, simple, cheap, and easy to store. In the present work, we report that a simple cationic Fe(III)-rich salt of [FeIIICl(TMPPH2)][FeIIICl4]2 (Fe-TMPP) exhibits a superior anticancer performance on a broad spectrum of cancer cell lines, including breast, colorectal cancer, liver, pancreatic, prostate, and gastric cancers, with half maximal inhibitory concentration (IC50) values in the range of 0.098-3.97 μM (0.066-2.68 μg mL-1), comparable to the best-reported medicines. Fe-TMPP can form stand-alone nanoparticles in water without the need for extra surface modification or organic-solvent-assisted antisolvent precipitation. Critically, Fe-TMPP is TME-responsive (TME = tumor microenvironment), and can only elicit its function in the TME with overexpressed H2O2, converting H2O2 to the cytotoxic •OH to oxidize the phospholipid of the cancer cell membrane, causing ferroptosis, a programmed cell death process of cancer cells.
摘要：
开发用于癌症治疗的有临床意义的纳米药物需要药物有效，安全,简单,便宜,易于存储。在目前的工作中,我们报道，[FeIIICl（TMPPH2）][FeIIIC4]2（Fe-TMPP）的简单阳离子富含Fe（III）的盐在广谱癌细胞系上表现出优异的抗癌性能，包括乳房,结直肠癌,肝脏,胰腺,前列腺,和胃癌，半最大抑制浓度（IC50）值在0.098-3.97μM（0.066-2.68μgmL-1）范围内，与报道最好的药物相当。Fe-TMPP可以在水中形成独立的纳米颗粒，而无需额外的表面改性或有机溶剂辅助的反溶剂沉淀。严重的,Fe-TMPP是TME反应性的（TME=肿瘤微环境），并且只能在过表达H2O2的TME中引发其功能，将H2O2转化为细胞毒性·OH以氧化癌细胞膜的磷脂，导致铁性凋亡，癌细胞的程序性细胞死亡过程。
