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基于双吲哚的小分子作为跨膜阴离子转运体和潜在的抗癌剂。

Bisindole-based small molecules as transmembrane anion transporters and potential anticancer agents.

机构信息

Department of Chemistry, Indian Institute of Science Education and Research (IISER) Pune, Dr. Homi Bhabha Road, Pashan, Pune 411008, Maharashtra, India.

Department of Biotechnology, Savitribai Phule Pune University (Formerly University of Pune), Pune 411007, Maharashtra, India.

出版信息

Org Biomol Chem. 2024 Jun 19;22(24):4987-4992. doi: 10.1039/d4ob00554f.

Abstract

Few synthetic ion transporters have been reported incorporating indole as the core moiety. We have developed a novel bisindole-based transporter capable of efficient transmembrane anion antiport. This system induced cytotoxicity in MCF-7 breast cancer cells chloride ion homeostasis disruption and the associated ROS generation, mitochondrial membrane depolarization, and lysosomal deacidification.

摘要

鲜有以吲哚为核心部分的合成离子转运体被报道。我们开发了一种新型双吲哚基转运体,能够有效地进行跨膜阴离子反向转运。该体系通过破坏 MCF-7 乳腺癌细胞内氯离子稳态和相关的 ROS 生成、线粒体膜去极化以及溶酶体去酸化,导致细胞毒性。

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