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Therapeutic Potential of Sulindac Hydroxamic Acid Against Human Pancreatic and Colonic Cancer Cells by Stefano Fogli; Irene Banti; Fabio Stefanelli; Luca Picchianti; Maria Digiacomo; Marco Macchia; Maria Cristina Breschi; Annalina Lapucci is a Chemistry article available to read on EtoBox.
What is Therapeutic Potential of Sulindac Hydroxamic Acid Against Human Pancreatic and Colonic Cancer Cells about?
The non-steroidal anti-inflammatory drug (NSAID) sulindac exhibits cyclooxygenase (COX)-dependent and COX-independent chemopreventive properties in human cancer. The present study was aimed at investigating whether the hydroxamic acid substitution for the carboxylic acid group could enhance the in vitro antitumor and antiangiogenic activities of sulindac. Characterization tools used on this study included analyses of cell viability, caspase 3/7 induction, DNA fragmentation, and gene expression. Our findings demonstrate that the newly synthesized hydroxamic acid derivative of sulindac and its sulfone and sulfide metabolites were characterized by a good anticancer activity on human pancreatic and colon cancer cells, both in terms of potency (IC 50 mean values from 6 AE 1.1 mM to 64 AE 1.1 mM) and efficacy (E max of w100%). Hydroxamic acid derivatives trigger a higher degree of apoptosis than carboxylic acid counterparts, increase bax/bcl-2 expression ratio and induce caspase 3/7 activation. Most notably, these compounds significantly inhibit proangiogenic growth factor-stimulated proliferation of vascular endothelial cell (HUVEC) at sub-micromolar concentrations. Our data also provid
Who reads Therapeutic Potential of Sulindac Hydroxamic Acid Against Human Pancreatic and Colonic Cancer Cells?
It is typically read by researchers, students, and practitioners in Chemistry.
- Author
- Stefano Fogli; Irene Banti; Fabio Stefanelli; Luca Picchianti; Maria Digiacomo; Marco Macchia; Maria Cristina Breschi; Annalina Lapucci
- Publisher
- Elsevier Science; Elsevier ; Elsevier BV (ISSN 0223-5234)
- Published
- 2010
- Language
- EN
- Field
- Chemistry (Physical Sciences)