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DPU: INTERDISCIPLINARY CONFERENCE
Year : 2020  |  Volume : 7  |  Issue : 5  |  Page : 30-35

Designing novel quercetin derivatives as matrix metalloproteinase-9 inhibitors in colon carcinoma: An In vitro and in silico approach


1 Cancer and Translational Research Laboratory, Dr. D. Y. Patil Biotechnology and Bioinformatics Institute, Dr. D. Y. Patil Vidyapeeth, Pune, Maharashtra, India
2 Bioinformatics Research Laboratory, Dr. D. Y. Patil Biotechnology and Bioinformatics Institute, Dr. D. Y. Patil Vidyapeeth, Pune, Maharashtra, India
3 Cancer and Translational Research Laboratory; Bioinformatics Research Laboratory, Dr. D. Y. Patil Biotechnology and Bioinformatics Institute, Dr. D. Y. Patil Vidyapeeth, Pune, Maharashtra, India

Correspondence Address:
Soumya Basu
Cancer and Translational Research Laboratory, Dr. D. Y. Patil Biotechnology and Bioinformatics Institute, Dr. D. Y. Patil Vidyapeeth, Pune - 411 033, Maharashtra
India
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Source of Support: None, Conflict of Interest: None


DOI: 10.4103/jdrr.jdrr_67_19

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Background: Matrix metalloproteinase-9 (MMP-9) plays an important role in activating several signaling molecules and pathways during inflammation, wound healing, and cancer progression. Since flavonoids have been shown to exhibit anti-inflammatory properties, we assessed the antiproliferative activity of quercetin, a flavonoid on colon carcinoma cell line through in vitro assays, and in order to design more specific MMP-9 inhibitors, we have used insilico approach to obtain potent quercetin derivatives. Materials and Methods: The aim of the present study was to investigate the effect of quercetin on cell viability and migration on cultured HCT-15 cells using 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide assay and wound healing assay. The docking analysis of quercetin and its derivatives with the crystal structure of MMP-9 (PDB ID: 3OE9) was performed using FlexX software. Result: Quercetin showed an antiproliferative and antimigratory activity on HCT-15 cells in time- and dose-dependent manner. Conclusion: Novel quercetin derivatives targeting MMP-9 have been identified for further synthesis and validation.


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