A new iridoid, verbascoside and derivatives with inhibitory activity against Taq DNA polymerase.
Bioorg Med Chem Lett
; 25(4): 914-8, 2015 Feb 15.
Article
em En
| MEDLINE
| ID: mdl-25582597
DNA polymerases are enzymes that play a crucial role in DNA metabolism such as replication, repair, transcription, recombination, and chromosome segregation during mitosis. Herein we report the isolation of a new iridoid (6-epi-catalpol, 2) and per-O-acetyl-verbascoside (11) from aerial part of Buddleja cordobensis Grisebach (Buddlejaceae). From compound 2, we have obtained eight compounds by chemical transformation. This group of compounds at a concentration of 500µM was assayed against Taq DNA polymerase. Compound 11 (per-O-acetyl-verbascoside) was the most active with an IC50 of 1.21±0.18µM; compounds 9, 2 and 8 were strong inhibitors with IC50 values of 5.57±0.70, 21.62±0.22 and 78.13±0.93µM, respectively. Compounds 11 and 9 could be a leader structures to development new anticancer chemotherapy medicines and a useful tool to investigate DNA polymerase activity.
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Base de dados:
MEDLINE
Assunto principal:
Fenóis
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Taq Polimerase
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Inibidores Enzimáticos
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Glucosídeos
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
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QUIMICA
Ano de publicação:
2015
Tipo de documento:
Article