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A new iridoid, verbascoside and derivatives with inhibitory activity against Taq DNA polymerase.
Garro, Hugo A; García, Celina; Martín, Victor S; Tonn, Carlos E; Pungitore, Carlos R.
Afiliação
  • Garro HA; INTEQUI-CONICET, Fac. Qca., Bioqca. y Fcia., Univ. Nac. de San Luis (U.N.S.L), Chacabuco y Pedernera, 5700 San Luis, Argentina. Electronic address: hugocanaya@yahoo.com.ar.
  • García C; Instituto Universitario de Bio-Orgánica 'Antonio González', Departamento de Química Orgánica, Universidad de La Laguna, Avda. Astrofísico Fco. Sánchez, 2 La Laguna 38206, Tenerife, Spain.
  • Martín VS; Instituto Universitario de Bio-Orgánica 'Antonio González', Departamento de Química Orgánica, Universidad de La Laguna, Avda. Astrofísico Fco. Sánchez, 2 La Laguna 38206, Tenerife, Spain.
  • Tonn CE; INTEQUI-CONICET, Fac. Qca., Bioqca. y Fcia., Univ. Nac. de San Luis (U.N.S.L), Chacabuco y Pedernera, 5700 San Luis, Argentina.
  • Pungitore CR; INTEQUI-CONICET, Fac. Qca., Bioqca. y Fcia., Univ. Nac. de San Luis (U.N.S.L), Chacabuco y Pedernera, 5700 San Luis, Argentina. Electronic address: carlos.pungitore@conicet.gov.ar.
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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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Fenóis / Taq Polimerase / Inibidores Enzimáticos / Glucosídeos Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2015 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Fenóis / Taq Polimerase / Inibidores Enzimáticos / Glucosídeos Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2015 Tipo de documento: Article