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对布洛芬具有对映选择性的 DNA 适体的分离与表征。

Isolation and characterization of enantioselective DNA aptamers for ibuprofen.

机构信息

School of Life Sciences and Biotechnology, Korea University, Anam-dong, Seongbuk-Gu, Seoul 136-701, South Korea.

出版信息

Bioorg Med Chem. 2010 May 15;18(10):3467-73. doi: 10.1016/j.bmc.2010.03.074. Epub 2010 Apr 3.

Abstract

Single stranded DNA aptamers that can bind to ibuprofen, a widely used anti-inflammation drug, were selected from random DNA library of 10(15) nucleotides by FluMag-SELEX process. Five different sequences were selected and their enantioselectivity and affinity were characterized. Three out of five aptamer candidates did not show any affinity to (S)-ibuprofen, but only to racemic form of ibuprofen, suggesting that they are (R)-ibuprofen specific aptamers. Another two aptamer candidates showed affinity to both racemic form and (S)-ibuprofen, which were considered as (S)-ibuprofen specific aptamers. The affinity of five ssDNA aptamers isolated was in a range of 1.5-5.2microM. In addition, all of these five aptamers did not show any affinity to analogues of ibuprofen in its profen's group (fenoprofen, flubiprofen, and naproxen) and the antibiotics of oxytetracycline, another control.

摘要

通过 FluMag-SELEX 过程,从 10(15)个核苷酸的随机 DNA 文库中筛选出可与布洛芬(一种广泛使用的抗炎药物)结合的单链 DNA 适体。从文库中筛选出五个不同的序列,并对其对映选择性和亲和力进行了表征。五个适体候选物中有三个对(S)-布洛芬没有亲和力,而只对布洛芬的外消旋形式有亲和力,这表明它们是(R)-布洛芬特异性适体。另外两个适体候选物对外消旋和(S)-布洛芬均有亲和力,被认为是(S)-布洛芬特异性适体。分离得到的五个 ssDNA 适体的亲和力在 1.5-5.2μM 范围内。此外,这五个适体都没有与布洛芬的前体(芬布芬、氟比洛芬和萘普生)和另一种抗生素土霉素的类似物以及其他对照物(氧四环素)产生任何亲和力。

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