Golegaonkar Sandeep B, Bhonsle Hermangi S, Boppana Ramanamurthy, Kulkarni Mahesh J
Council of Scientific and Industrial Reseach , India.
Eur J Mass Spectrom (Chichester). 2010;16(2):221-6. doi: 10.1255/ejms.1066.
An in vitro insulin glycation assay was developed for screening glycation inhibitors. The assay involves the use of matrix-assisted laser desorption/ionization time-of-flight mass spectrometry for monitoring the formation of glycated insulin. The assay is simple, rapid and amenable for high throughput screening. Using this assay we have discovered a strong anti-glycation activity for the anti-tuberculosis drug rifampicin. These results were compared with bovine serum albumin glucose fluorescence assay. In addition, the IC(50) of rifampicin was lower than that of aminoguanidine, a known anti-glycating agent, suggesting that rifampicin is a more potent glycation inhibitor.
开发了一种体外胰岛素糖基化测定法用于筛选糖基化抑制剂。该测定法涉及使用基质辅助激光解吸/电离飞行时间质谱来监测糖化胰岛素的形成。该测定法简单、快速且适用于高通量筛选。使用此测定法，我们发现抗结核药物利福平具有很强的抗糖基化活性。将这些结果与牛血清白蛋白葡萄糖荧光测定法进行了比较。此外，利福平的半数抑制浓度低于已知的抗糖基化剂氨基胍，这表明利福平是一种更有效的糖基化抑制剂。
