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dc.contributor.author
Chialva, Constanza Soledad
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dc.contributor.author
Avila, Héctor Gabriel
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dc.contributor.author
Pungitore, Carlos Rodolfo
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dc.date.available
2018-02-09T18:17:48Z
dc.date.issued
2017-05
dc.identifier.citation
Chialva, Constanza Soledad; Avila, Héctor Gabriel; Pungitore, Carlos Rodolfo; Inhibition of Taq DNA Polymerase and Human Topoisomerase I by Resveratrol Derivatives; Bentham Science Publishers; Current Bioactive Compounds; 13; 5-2017; 1-6
dc.identifier.issn
1573-4072
dc.identifier.uri
http://hdl.handle.net/11336/36329
dc.description.abstract
Background: DNA polymerases and topoisomerases are proteins that play a vital part in DNA metabolism such as replication, transcription, recombination, and chromosome segregation during mitosis. For this reason, these enzymes are appreciated targets for the development of cancer chemotherapeutic drugs. Method: All compounds evaluated in this work were obtained under the conditions and using the reagents described in the Schemes (1-3). Polymerase Chain Reaction (PCR): Sample stock solutions were prepared at a concentration of 10 mM in dimethyl sulfoxide (DMSO) using 1 ml as a final volume. The PCR master mix consisted of 2.5 μl of PCR Buffer (40 mM Tris-acetate, pH 8.3), 0.5 μl of MgCl2 at a concentration of 15 mM, 2.5 U Taq DNA polymerase, 2.5 μl of each oligonucleotide primer at a concentration of 100 mM, 0.5 μl of each deoxynucleotide triphosphates (dNTP) at a concentration of 10 mM and 0.1 μg/ml of DNA template. Topoisomerase I activity was determined by relaxation of super-coiled pBr 322 plasmid DNA. The reaction mixture in 20 ml contained 35 mM Tris-HCl, pH 8, 72 mM KCl, 5 mM MgCl2, 5 mM DTT, 5 mM spermidine, 0.01% bovine serum albumin, 0.64 mg/20 ml super-coiled pBr 322 DNA, 1.5 U human topoisomerase I and 1 ml of test compound diluted with DMSO. Results: Faithful replication of DNA molecules with the intervention of DNA polymerases and topoisomerases is essential for genome integrity and correct transmission of genetic information in all living organisms. For this reason, DNA polymerases and topoisomerases have emerged as important cellular targets for chemical intervention in the development of anti-cancer agents. Herein we report the semi-synthesis of resveratrol derivatives and similar compounds and their biological activity against Taq DNA polymerase and topoisomerases. Compound 4 was the most active against both enzymes with IC50 values equal to 18.56 and 28.37 μM, respectively. Additionally, compounds 3 and 5 showed interesting activity against Taq DNA polymerase with IC50 values equal to 76.89 and 71.65 μM, respectively. Conclusion: In summary, one compound (4) was found to have excellent inhibitory activity against human topoisomerase I and Taq DNA polymerase. This compound can be a leading molecule for the development of original anticancer treatment and an excellent instrument to explore DNA polymerase and topoisomerase activity.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Bentham Science Publishers
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dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
DIDEOXYNUCLEOTIDES
dc.subject
DNA POLYMERASES
dc.subject
HUMAN TOPOISOMERASE I
dc.subject
NATURAL PRODUCTS
dc.subject
RESVERATROL
dc.subject
STILBENE
dc.subject.classification
Otras Ciencias Químicas
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dc.subject.classification
Ciencias Químicas
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dc.subject.classification
CIENCIAS NATURALES Y EXACTAS
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dc.title
Inhibition of Taq DNA Polymerase and Human Topoisomerase I by Resveratrol Derivatives
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2017-12-04T18:22:36Z
dc.identifier.eissn
1875-6646
dc.journal.volume
13
dc.journal.pagination
1-6
dc.journal.pais
Emiratos Árabes Unidos
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dc.journal.ciudad
Sharjah
dc.description.fil
Fil: Chialva, Constanza Soledad. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Mendoza. Instituto de Biología Agrícola de Mendoza. Universidad Nacional de Cuyo. Facultad de Ciencias Agrarias. Instituto de Biología Agrícola de Mendoza; Argentina
dc.description.fil
Fil: Avila, Héctor Gabriel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Mendoza. Instituto de Biología Agrícola de Mendoza. Universidad Nacional de Cuyo. Facultad de Ciencias Agrarias. Instituto de Biología Agrícola de Mendoza; Argentina
dc.description.fil
Fil: Pungitore, Carlos Rodolfo. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Luis. Instituto de Investigaciones en Tecnología Química. Universidad Nacional de San Luis. Facultad de Química, Bioquímica y Farmacia. Instituto de Investigaciones en Tecnología Química; Argentina
dc.journal.title
Current Bioactive Compounds
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/http://www.eurekaselect.com/152769/article
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.2174/1573407213666170530085340
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