Identification of Mitochondria-Targeting Anticancer Drugs and Mitochondrial Membrane Potential

Author: admin     Date: February 23, 2024

Mitochondria play a pivotal role in determining the point-of-no-return in the apoptotic process. Therefore, anticancer drugs that directly target mitochondria hold great potential to evade resistance mechanisms that have developed toward conventional chemotherapeutics. Here, an in vitro strategy to quickly identify therapeutic agents that induce apoptosis by directly affecting mitochondria was reported. This result is achieved by treating isolated mitochondria with potential anticancer compounds, followed by simultaneously measuring the side scatter and mitochondrial membrane potential (ΔΨm, labeled with DiOC6(3)) fluorescence of individual mitochondria using the Flow NanoAnalyzer. The feasibility of this method was tested with eight widely used anticarcinogens. A potent mitochondrial membrane uncoupling agent, CCCP, was used as the positive control.

Figure 1. Analysis of mitochondria treated with different anticancer drugs on the Flow NanoAnalyzer.

By labeling with DiOC6(3), the Flow NanoAnalyzer can monitor the change of mitochondrial membrane potential and quickly and accurately detect whether the drug can act directly on mitochondria and its effect. This provides a new way for the detection of anticancer drugs’ mechanisms and screening.

Anal. Chem., 2014, 86(11), 5232-5237.