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Turning a Quinoline-based Steroidal Anticancer Agent into Fluorescent Dye for its Tracking by Cell Imaging
René Maltais1, Jenny Roy1, Donald Poirier1,2
1Laboratory of Medicinal Chemistry, Endocrinology and Nephrology Unit, CHU de Québec Research Center, Québec, Québec G1V 4G2, Canada.
ACS Medicinal Chemistry Letters
|May 31, 2021
Summary
Researchers developed a fluorescent version of the cancer drug RM-581 (RM-581-Fluo). This new probe accumulates in the endoplasmic reticulum, aiding the study of RM-581
Area of Science:
- Medicinal Chemistry
- Cell Biology
- Fluorescence Microscopy
Background:
- RM-581 is an aminosteroid derivative with potent cytotoxic activity against cancer cells.
- Its precise mechanism of action (MoA) is not fully understood.
- Quinoline derivatives can be made fluorescent by adding an N-dimethyl group.
Purpose of the Study:
- To create a fluorescent probe based on RM-581 for MoA studies.
- To investigate the cellular localization of the fluorescent probe.
- To confirm the cytotoxic activity of the fluorescent probe.
Main Methods:
- Chemical synthesis of the N-dimethyl analogue of RM-581 (RM-581-Fluo).
- Confirmation of fluorescent properties and cytotoxic activity in MCF-7 breast cancer cells.
- Confocal microscopy and colocalization studies with ER-Tracker dye.
Main Results:
- RM-581-Fluo was successfully synthesized and exhibited fluorescence.
- The probe retained cytotoxic activity against MCF-7 cells.
- RM-581-Fluo was found to accumulate in the endoplasmic reticulum (ER) of MCF-7 cells.
Conclusions:
- RM-581-Fluo serves as a valuable tool for investigating the MoA of RM-581.
- This study demonstrates a method for creating fluorescent versions of bioactive quinoline derivatives.
- The endoplasmic reticulum is a key cellular target for RM-581 or its metabolites.
