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Mitochondria-targeting fluorescent molecules for high efficiency cancer growth inhibition and imaging
Hao Chen1,2, Jing Wang1,3, Xin Feng3,4
1Department of Radiology , The First Hospital of Jilin University , Changchun , 130021 , China .
Abstract:
Fluorescent mitochondria-accumulating delocalized lipophilic cations (DLCs) for cancer therapy have drawn significant attention in the field of cancer theranostics. One of the most promising fluorescent DLCs, F16, can selectively trigger the apoptosis and necrosis of cancer cells, making it an attractive targeted theranostic drug candidate. However, it suffers from low clinical translation potential, largely due to its inefficient anti-cancer activity (IC50 in the μM range) and poorly understood structure-activity relationship (SAR). In this report, eleven indole-ring substituted F16 derivatives (F16s) were synthesized. Among these derivatives, 5BMF was identified as a highly effective theranostic agent, with in vitro studies showing a low IC50 of ∼50 nM (to H2228 cells) and high cancer to normal cell selectivity index of 225. In vivo studies revealed that tumors treated with 5BMF were significantly suppressed (almost no growth over the treatment period) compared to the PBS treated control group, and also no obvious toxicity to mice was found. In addition, the tumor imaging capability of 5BMF was demonstrated by in vivo fluorescence imaging. Finally, we report for the first time a proposed SAR for F16 DLCs. Our work lays down a solid foundation for translating 5BMF into a novel and highly promising DLC for cancer theranostics.
Insights
Researchers developed a new cancer theranostic agent, 5BMF, which selectively targets cancer cells with high efficacy and low toxicity. This fluorescent delocalized lipophilic cation (DLC) shows promise for improved cancer therapy and imaging.
Area of Science:
- Oncology
- Pharmacology
- Biomedical Engineering
Background:
- Fluorescent mitochondria-accumulating delocalized lipophilic cations (DLCs) are promising for cancer theranostics.
- The F16 DLC exhibits selective cancer cell apoptosis but has limitations in anti-cancer activity and a poorly understood structure-activity relationship (SAR).
Purpose of the Study:
- To synthesize and evaluate novel F16 derivatives for enhanced cancer theranostic applications.
- To investigate the structure-activity relationship (SAR) of these new F16 derivatives.
Main Methods:
- Synthesis of eleven indole-ring substituted F16 derivatives.
- In vitro evaluation of cytotoxicity (IC50) and cancer cell selectivity.
- In vivo anti-cancer efficacy studies and toxicity assessment in mice.
- In vivo fluorescence imaging for tumor visualization.
Main Results:
- 5BMF, an F16 derivative, demonstrated potent in vitro anti-cancer activity (IC50 ~50 nM) with high cancer to normal cell selectivity (index 225).
- In vivo studies showed significant tumor suppression with 5BMF treatment and no obvious toxicity in mice.
- 5BMF exhibited effective tumor imaging capabilities via in vivo fluorescence imaging.
Conclusions:
- 5BMF is a highly effective theranostic agent with improved anti-cancer activity and selectivity compared to F16.
- The study proposes a structure-activity relationship for F16 DLCs.
- 5BMF holds significant potential for translation into a novel clinical cancer theranostic agent.
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