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Covalent Organic Framework Material Bearing Phloroglucinol Building Units as a Potent Anticancer Agent
Piyali Bhanja1, Snehasis Mishra2, Krishnendu Manna2
1Department of Materials Science, Indian Association for the Cultivation of Science , Jadavpur, Kolkata 700 032, India.
ACS Applied Materials & Interfaces
|August 24, 2017
Summary
A novel biodegradable nitrogen-containing covalent organic framework (COF), EDTFP-1, demonstrates significant anticancer potential. This COF material effectively induces apoptosis in various cancer cells, suggesting its promise as a new chemotherapeutic agent.
Area of Science:
- Materials Science
- Nanotechnology
- Medicinal Chemistry
Background:
- Covalent organic frameworks (COFs) offer tunable nanoscale pores for designing functional materials.
- Existing chemotherapy faces limitations, necessitating novel therapeutic agents.
- Biodegradable COFs present an attractive platform for targeted drug delivery and cancer therapy.
Purpose of the Study:
- To synthesize and characterize a new biodegradable nitrogen-containing COF, EDTFP-1.
- To investigate the anticancer potential and mechanism of action of EDTFP-1.
- To evaluate EDTFP-1 as a novel chemotherapeutic agent.
Main Methods:
- Synthesis of EDTFP-1 via Schiff base condensation of ethylenedianiline and triformylphloroglucinol.
- Characterization of EDTFP-1's 3D-hexagonal porous structure (1.5 nm pores).
- In vitro cytotoxicity assays against HCT 116, HepG2, A549, and MIA-Paca2 cancer cell lines.
Main Results:
- EDTFP-1 exhibited significant cytotoxicity against tested cancer cells, with notable efficacy against HCT116.
- EDTFP-1 induced apoptosis via cell membrane blebbing, DNA fragmentation, and mitochondrial dysfunction.
- Increased ROS generation correlated with mitochondrial-dependent apoptosis and p53 phosphorylation.
Conclusions:
- EDTFP-1 is a promising biodegradable COF with potent anticancer activity.
- The mechanism involves ROS generation, mitochondrial-dependent apoptosis, and p53 pathway modulation.
- EDTFP-1 represents a novel chemotherapeutic agent for cancer treatment.
