Crosstalk-Assisted Augmented Activity of Polyphenolic Molecules: A Study Using Fluorescence Lifetime Imaging
Pratyush Kiran Nandi1, Souvik Layek1, Ritwik Hazra1
1Department of Chemistry, Indian Institute of Technology Kharagpur, Kharagpur, West Bengal 721302, India.
The Journal of Physical Chemistry Letters
|February 13, 2025
Summary
Gallic acid and methyl gallate self-assemble into distinct structures, but form a unique fibrillar co-assembly. This cross-assembly shows enhanced anti-cancer properties compared to individual molecules.
Area of Science:
- Physical Chemistry
- Materials Science
- Biochemistry
Background:
- Small molecule self-assembly is crucial for understanding molecular behavior.
- Fluorescence lifetime imaging microscopy (FLIM) provides molecular-level insights into microenvironments.
- Polyphenols like gallic acid (GA) and methyl gallate (MG) are natural compounds with potential biological activity.
Purpose of the Study:
- To investigate the self-assembly and co-assembly mechanisms of gallic acid and methyl gallate.
- To elucidate the structural transitions and morphological changes during self-assembly using FLIM.
- To evaluate the impact of co-assembly on the biological activity, specifically cytotoxicity and cancer cell progression.
Main Methods:
- Synthesis and characterization of gallic acid (GA) and methyl gallate (MG) assemblies.
- Fluorescence lifetime imaging microscopy (FLIM) to study structural transitions and molecular packing.
- In vitro cytotoxicity assays and cancer cell progression studies under physiological conditions.
Main Results:
- GA self-assembles into rod-like structures, while MG forms cotton-like aggregates.
- Equimolar co-assembly of GA and MG results in a distinct fibrillar structure with improper molecular packing.
- FLIM revealed structural transitions and morphological differences between individual and co-assemblies.
- Co-assemblies disintegrate under physiological conditions, but individual molecules retain their architectures.
- Co-polyphenols exhibited enhanced dose-dependent cytotoxicity and mitigated cancer cell progression compared to individual polyphenols.
Conclusions:
- The co-assembly of GA and MG leads to a novel fibrillar structure with altered properties.
- FLIM is a powerful tool for understanding self-assembly mechanisms and molecular packing.
- Co-assembly of polyphenols can enhance their efficacy as drug molecules, offering a strategy to improve drug performance.
