title: A new iridoid, verbascoside and derivatives with inhibitory activity against Taq DNA polymerase.
abstract: 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.
authors.affiliation: 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.
authors.forename: Hugo A
authors.initials: HA
authors.lastname: Garro
authors.affiliation: 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.
authors.forename: Celina
authors.initials: C
authors.lastname: García
authors.affiliation: 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.
authors.forename: Victor S
authors.initials: VS
authors.lastname: Martín
authors.affiliation: INTEQUI-CONICET, Fac. Qca., Bioqca. y Fcia., Univ. Nac. de San Luis (U.N.S.L), Chacabuco y Pedernera, 5700 San Luis, Argentina.
authors.forename: Carlos E
authors.initials: CE
authors.lastname: Tonn
authors.affiliation: 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.
authors.forename: Carlos R
authors.initials: CR
authors.lastname: Pungitore
mesh_terms: D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005960:Glucosides / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D010636:Phenols / Q000494:pharmacology*; D019914:Taq Polymerase / Q000037:antagonists & inhibitors*; D059808:Polyphenols
chemical_list: D004791:Enzyme Inhibitors; D005960:Glucosides; D010636:Phenols; D019914:Taq Polymerase; C058956:acteoside; D059808:Polyphenols
keywords: 6-epi-Catalpol; Natural products; Sylil derivatives; Taq DNA polymerase inhibitors; Verbascoside