TY - JOUR
T1 - Pegylated bis-indolyl polyurethane dendrimer
T2 - Empty drug carrier with prominent anticancer activity
AU - Bargathulla, Ibrahim
AU - Aadhil Ashwaq, Babu
AU - Sathiyaraj, S.
AU - Sultan Nasar, A.
AU - ElangovanVellaichamy, null
PY - 2021/6/15
Y1 - 2021/6/15
N2 - Blocked isocyanate-terminated, bioactive bis-indole based polyurethane dendrimers of generation G0 – G3 were subjected to urethane interchange reaction with poly(ethylene glycol) monomethyl ether; the reactions yielded corresponding PEGylated dendrimers. The structures of the PEGylated dendrimers were confirmed using spectroscopic and SEC-MALS techniques. The PDI of the polymers were found between 1.24 and 1.49 and these values were on par with 1.46 of poly(ethylene glycol) monomethyl ether used. All the PEGylated dendrimers were found to have a prominent cytotoxicity in human breast (MDA MB-231) and lung (A549) cancer cells. Based on the MTT, AO/EtBr staining and ROS assay results, PEGylated G2 and G3 dendrimers were further subjected to determination of apoptosis using protein markers; the pro-apoptotic markers BaX and caspase-3 were found up regulated and the anti-apoptotic marker Bcl-2 was down regulated. The results confirmed that the PEGylated bis-indolyl G3 polyurethane dendrimer – an empty drug carrier – itself had strong tendency to activate apoptosis type cell death in human cancer cells.
AB - Blocked isocyanate-terminated, bioactive bis-indole based polyurethane dendrimers of generation G0 – G3 were subjected to urethane interchange reaction with poly(ethylene glycol) monomethyl ether; the reactions yielded corresponding PEGylated dendrimers. The structures of the PEGylated dendrimers were confirmed using spectroscopic and SEC-MALS techniques. The PDI of the polymers were found between 1.24 and 1.49 and these values were on par with 1.46 of poly(ethylene glycol) monomethyl ether used. All the PEGylated dendrimers were found to have a prominent cytotoxicity in human breast (MDA MB-231) and lung (A549) cancer cells. Based on the MTT, AO/EtBr staining and ROS assay results, PEGylated G2 and G3 dendrimers were further subjected to determination of apoptosis using protein markers; the pro-apoptotic markers BaX and caspase-3 were found up regulated and the anti-apoptotic marker Bcl-2 was down regulated. The results confirmed that the PEGylated bis-indolyl G3 polyurethane dendrimer – an empty drug carrier – itself had strong tendency to activate apoptosis type cell death in human cancer cells.
KW - Apoptosis
KW - Bis-indolyl dendrimer
KW - Breast cancer
KW - Cytotoxicity
KW - Lung cancer
KW - PEGylated dendrimer
KW - Polyurethane dendrimer
UR - http://www.scopus.com/inward/record.url?scp=85107651259&partnerID=8YFLogxK
U2 - 10.1016/j.eurpolymj.2021.110491
DO - 10.1016/j.eurpolymj.2021.110491
M3 - Article
AN - SCOPUS:85107651259
SN - 0014-3057
VL - 153
JO - European Polymer Journal
JF - European Polymer Journal
M1 - 110491
ER -
