Garro Hugo A, García Celina, Martín Victor S, Tonn Carlos E, Pungitore Carlos R
INTEQUI-CONICET, Fac. Qca., Bioqca. y Fcia., Univ. Nac. de San Luis (U.N.S.L), Chacabuco y Pedernera, 5700 San Luis, Argentina.
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.
Bioorg Med Chem Lett. 2015 Feb 15;25(4):914-8. doi: 10.1016/j.bmcl.2014.12.052. Epub 2014 Dec 23.
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.
DNA聚合酶是在DNA代谢过程中发挥关键作用的酶，这些代谢过程包括复制、修复、转录、重组以及有丝分裂期间的染色体分离。在此，我们报告了从灰叶醉鱼草（醉鱼草科）地上部分分离出一种新的环烯醚萜（6-表梓醇，2）和全-O-乙酰毛蕊花糖苷（11）。从化合物2出发，我们通过化学转化得到了8种化合物。对这组浓度为500μM的化合物针对Taq DNA聚合酶进行了测定。化合物11（全-O-乙酰毛蕊花糖苷）活性最强，IC50为1.21±0.18μM；化合物9、2和8是强抑制剂，IC50值分别为5.57±0.70、21.62±0.22和78.13±0.93μM。化合物11和9可能是开发新型抗癌化疗药物的先导结构，也是研究DNA聚合酶活性的有用工具。
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