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Pegylated bis-indolyl polyurethane dendrimer : Empty drug carrier with prominent anticancer activity

Bargathulla, Ibrahim ; Aadhil Ashwaq, Babu ; Sathiyaraj, S. LU ; Sultan Nasar, A. and ElangovanVellaichamy (2021) In European Polymer Journal 153.
Abstract

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... (More)

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.

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author
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organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
Apoptosis, Bis-indolyl dendrimer, Breast cancer, Cytotoxicity, Lung cancer, PEGylated dendrimer, Polyurethane dendrimer
in
European Polymer Journal
volume
153
article number
110491
publisher
Elsevier
external identifiers
  • scopus:85107651259
ISSN
0014-3057
DOI
10.1016/j.eurpolymj.2021.110491
language
English
LU publication?
yes
id
9758e0d1-9fdf-4f15-878b-d59a135a052a
date added to LUP
2021-06-28 10:11:17
date last changed
2022-04-27 02:36:33
@article{9758e0d1-9fdf-4f15-878b-d59a135a052a,
  abstract     = {{<p>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.</p>}},
  author       = {{Bargathulla, Ibrahim and Aadhil Ashwaq, Babu and Sathiyaraj, S. and Sultan Nasar, A. and ElangovanVellaichamy}},
  issn         = {{0014-3057}},
  keywords     = {{Apoptosis; Bis-indolyl dendrimer; Breast cancer; Cytotoxicity; Lung cancer; PEGylated dendrimer; Polyurethane dendrimer}},
  language     = {{eng}},
  month        = {{06}},
  publisher    = {{Elsevier}},
  series       = {{European Polymer Journal}},
  title        = {{Pegylated bis-indolyl polyurethane dendrimer : Empty drug carrier with prominent anticancer activity}},
  url          = {{http://dx.doi.org/10.1016/j.eurpolymj.2021.110491}},
  doi          = {{10.1016/j.eurpolymj.2021.110491}},
  volume       = {{153}},
  year         = {{2021}},
}