Evaluation of 4-alkoxychalcones as a new class of antiglycating agents: a combined experimental and docking study

Evaluation of 4-alkoxychalcones as a new class of antiglycating agents: a combined experimental... A series of 4-alkoxychalcones (1–12) has been evaluated for their in vitro antiglycation activity. Compound 2 (IC50 = 89.07 ± 1.3 μM), compound 3 (IC50 = 266.82 ± 4.6 μM), and compound 5 (IC50 = 285.79 ± 1.9 μM) showed an excellent antiglycation potential better than the standard (rutin, IC50 = 294.50 ± 1.5 μM). Additionally, all the compounds of this series were evaluated for their cytotoxicity against Artemia salina (brine shrimp) and one tumor cell line, namely human Prostate Cancer cell line (PC-3). All the compounds showed low toxicity against brine shrimp with LD50 values much lower than the standard etoposide. Similarly, a much lower toxicity was observed for all the compounds against PC-3 cell line compared to doxorubicin, a standard reference drug used for this study. The molecular docking studies were also carried out to support the experimental results. A good correlation was found between experimental and theoretical results. The compounds of this series are therefore excellent antiglycating agents with no or very little cytotoxicity and represent a new class of antiglycating agents that deserve to be focused on for further research and in vivo studies in the future. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Research on Chemical Intermediates Springer Journals

Evaluation of 4-alkoxychalcones as a new class of antiglycating agents: a combined experimental and docking study

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Publisher
Springer Netherlands
Copyright
Copyright © 2014 by Springer Science+Business Media Dordrecht
Subject
Chemistry; Catalysis; Physical Chemistry; Inorganic Chemistry
ISSN
0922-6168
eISSN
1568-5675
D.O.I.
10.1007/s11164-014-1752-0
Publisher site
See Article on Publisher Site

Abstract

A series of 4-alkoxychalcones (1–12) has been evaluated for their in vitro antiglycation activity. Compound 2 (IC50 = 89.07 ± 1.3 μM), compound 3 (IC50 = 266.82 ± 4.6 μM), and compound 5 (IC50 = 285.79 ± 1.9 μM) showed an excellent antiglycation potential better than the standard (rutin, IC50 = 294.50 ± 1.5 μM). Additionally, all the compounds of this series were evaluated for their cytotoxicity against Artemia salina (brine shrimp) and one tumor cell line, namely human Prostate Cancer cell line (PC-3). All the compounds showed low toxicity against brine shrimp with LD50 values much lower than the standard etoposide. Similarly, a much lower toxicity was observed for all the compounds against PC-3 cell line compared to doxorubicin, a standard reference drug used for this study. The molecular docking studies were also carried out to support the experimental results. A good correlation was found between experimental and theoretical results. The compounds of this series are therefore excellent antiglycating agents with no or very little cytotoxicity and represent a new class of antiglycating agents that deserve to be focused on for further research and in vivo studies in the future.

Journal

Research on Chemical IntermediatesSpringer Journals

Published: Jul 10, 2014

References

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