TY - JOUR
T1 - Covalent Organic Framework Material bearing Phloroglucinol Building Units as a Potent Anticancer Agent
AU - Bhanja, Piyali
AU - Mishra, Snehasis
AU - Manna, Krishnendu
AU - Mallick, Arijit
AU - Das Saha, Krishna
AU - Bhaumik, Asim
N1 - KAUST Repository Item: Exported on 2020-10-01
Acknowledgements: PB thanks to CSIR, New Delhi for a senior research fellowship. AB wishes to thank DST, New Delhi for instrumental facilities through DST Unit on Nanoscience.
PY - 2017/9/5
Y1 - 2017/9/5
N2 - Covalent organic frameworks (COFs) having periodicity in pores of nanoscale dimensions can be suitably designed for the organic building units bearing reactive functional groups at their surfaces. Thus, they are an attractive option as an anticancer agent to overcome the limitations of chemotherapy. Herein, we first report a new porous biodegradable nitrogen containing COF material, EDTFP-1 (ethylenedianiline-triformyl phloroglucinol), synthesized using 4,4'-ethylenedianiline and 2,4,6-triformylphloroglucinol via Schiff base condensation reaction. EDTFP-1 exhibited 3D-hexagonal porous structure with average pores of ca. 1.5 nm dimension. Here, we have explored the anti-cancer potentiality of EDTFP-1. Result demonstrated an enhanced cytotoxicity was observed against four cancer cells HCT 116, HepG2, A549, and MIA-Paca2 with significant lower IC50 on HCT116 cells. Additionally, EDTFP-1-induced cell death was associated with the characteristic apoptotic changes like cell membrane blebbing, nuclear DNA fragmentation, externalization of phosphatidylserine from the cell membrane followed by a loss of mitochondrial membrane potential as well as modulation of pro and anti-apoptotic proteins. Further, the result depicted a direct correlation between the generations of ROS with mitochondrial-dependant apoptosis through the involvement of p53 phosphorylation upon EDTFP-1 induction, suggesting this COF material is a novel chemotherapeutic agent for cancer treatment.
AB - Covalent organic frameworks (COFs) having periodicity in pores of nanoscale dimensions can be suitably designed for the organic building units bearing reactive functional groups at their surfaces. Thus, they are an attractive option as an anticancer agent to overcome the limitations of chemotherapy. Herein, we first report a new porous biodegradable nitrogen containing COF material, EDTFP-1 (ethylenedianiline-triformyl phloroglucinol), synthesized using 4,4'-ethylenedianiline and 2,4,6-triformylphloroglucinol via Schiff base condensation reaction. EDTFP-1 exhibited 3D-hexagonal porous structure with average pores of ca. 1.5 nm dimension. Here, we have explored the anti-cancer potentiality of EDTFP-1. Result demonstrated an enhanced cytotoxicity was observed against four cancer cells HCT 116, HepG2, A549, and MIA-Paca2 with significant lower IC50 on HCT116 cells. Additionally, EDTFP-1-induced cell death was associated with the characteristic apoptotic changes like cell membrane blebbing, nuclear DNA fragmentation, externalization of phosphatidylserine from the cell membrane followed by a loss of mitochondrial membrane potential as well as modulation of pro and anti-apoptotic proteins. Further, the result depicted a direct correlation between the generations of ROS with mitochondrial-dependant apoptosis through the involvement of p53 phosphorylation upon EDTFP-1 induction, suggesting this COF material is a novel chemotherapeutic agent for cancer treatment.
UR - http://hdl.handle.net/10754/625421
UR - http://pubs.acs.org/doi/abs/10.1021/acsami.7b07343
UR - http://www.scopus.com/inward/record.url?scp=85029695108&partnerID=8YFLogxK
U2 - 10.1021/acsami.7b07343
DO - 10.1021/acsami.7b07343
M3 - Article
C2 - 28831795
SN - 1944-8244
VL - 9
SP - 31411
EP - 31423
JO - ACS Applied Materials & Interfaces
JF - ACS Applied Materials & Interfaces
IS - 37
ER -
