4.5 Article

A new iridoid, verbascoside and derivatives with inhibitory activity against Taq DNA polymerase

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 25, 期 4, 页码 914-918

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.12.052

关键词

Natural products; Taq DNA polymerase inhibitors; 6-epi-Catalpol; Sylil derivatives; Verbascoside

资金

  1. CONICET [PIP 00360]
  2. UNSL [PROICO 2/1214]
  3. ANPCyT [PICT-2011-1416]
  4. CONICET
  5. Spanish MINECO [CTQ2011-28417-C02-01]
  6. [PCI-A/025750/09]

向作者/读者索取更多资源

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 500 mu M was assayed against Taq DNA polymerase. Compound 11 (per-O-acetyl-verbascoside) was the most active with an IC50 of 1.21 +/- 0.18 mu M; compounds 9, 2 and 8 were strong inhibitors with IC50 values of 5.57 +/- 0.70, 21.62 +/- 0.22 and 78.13 +/- 0.93 mu M, 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. (C) 2014 Elsevier Ltd. All rights reserved.

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