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Published on: May 21, 2019
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Copper(ii) curcumin complexes for endoplasmic reticulum targeted photocytotoxicity
Atrayee Banaspati1, Vanitha Ramu2, Md Kausar Raza2
1Department of Chemistry, Gauhati University Guwahati 781014 Assam India tridibgoswami05@gmail.com.
RSC Advances
|November 9, 2022
Summary
Copper(II) complexes with curcumin exhibit potent visible light-activated chemotherapy against cervical and lung cancer cells. These complexes induce apoptosis via reactive oxygen species generation, showing low dark toxicity and high phototoxic indices.
Area of Science:
- Coordination Chemistry
- Photochemistry
- Cancer Therapeutics
Background:
- Curcumin and its derivatives are known for their biological activities.
- Copper complexes have shown promise in medicinal chemistry.
- Photodynamic therapy offers a targeted approach to cancer treatment.
Purpose of the Study:
- To synthesize and characterize novel copper(II) complexes with curcumin and nitrogen-based ligands.
- To evaluate the light-assisted chemotherapeutic potential of these complexes against cancer cells.
- To investigate the mechanism of action, including DNA binding, protein interaction, and cellular localization.
Main Methods:
- Synthesis and full physicochemical characterization of copper(II) complexes.
- Single crystal X-ray diffraction for structural determination.
- Spectroscopic analysis (UV-Vis, redox potentials).
- In vitro cytotoxicity assays (dark and light conditions).
- Flow cytometry for apoptosis and reactive oxygen species (ROS) detection.
- Confocal microscopy for cellular localization.
Main Results:
- Novel copper(II)-curcumin complexes ([Cu(cur)(L)(ClO4)], L=phen, dpq, dppz) were synthesized and characterized.
- Curcumin complexes showed significant visible light-induced cytotoxicity against HeLa and A549 cancer cells (IC50 ≈ 4 μM) with high phototoxic indices (PI).
- Complexes induced apoptosis via ROS generation upon photoactivation, with minimal dark toxicity.
- Complexes exhibited moderate binding to human serum albumin (HSA) and significant affinity for calf-thymus (CT) DNA.
- Cellular localization studies indicated predominant accumulation in the endoplasmic reticulum.
Conclusions:
- The synthesized copper(II)-curcumin complexes demonstrate remarkable potential as photochemotherapeutic agents.
- Light activation is crucial for their potent anticancer activity, mediated by ROS production and apoptosis induction.
- The complexes target specific cellular organelles, suggesting a targeted therapeutic approach.
