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Updated: Sep 5, 2025

Simultaneous Measurement of Mitochondrial Calcium and Mitochondrial Membrane Potential in Live Cells by Fluorescent Microscopy
Published on: January 24, 2017
A red-light activatable and mitochondrion-targeting PtIV complex to overcome drug resistance
Yanran Li1,2, Zigui Wang1,2, Yanxin Qi1
1Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China.
Abstract:
The therapeutic effects of platinum anticancer drugs are commonly whittled away by drug resistance, which is associated with drug efflux and the nucleotide excision repair (NER) pathway. Activation of drugs in a spatiotemporally controllable manner in the mitochondria of cancer cells is a very promising strategy to alleviate these problems. In this work, PtIV-PS2, a cisplatin-based PtIV prodrug, was designed to release cisplatin inside the mitochondria on red light exposure. This PtIV complex could be effectively reduced to PtII species under irradiation. PtIV-PS2 very effectively accumulates in the mitochondria of cancer cells through active transport. After photoactivation, PtIV-PS2 showed higher cytotoxicity than cisplatin in the cisplatin-resistant carcinoma cells and the amount of Pt in genomic DNA was elevated. Moreover, PtIV-PS2 decreased the cellular mitochondrial membrane potential (MMP) and the cellular content of ATP. This work developed a promising window for the design of controllably activated and mitochondrion-targeting PtIV prodrugs to overcome drug resistance of chemotherapy.
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