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The evaluation of inhibitive effectiveness of the tumour necrosis factor-α converting enzyme selective inhibitors by HPLC

机译:高效液相色谱法评价肿瘤坏死因子-α转化酶选择性抑制剂的抑制作用

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A novel high-performance liquid chromatography (HPLC) method based on the internal standard method was established for assaying the tumour necrosis factor-α converting enzyme (TACE) activity and matrix metalloprotease-9 (MMP-9) activity, and was used to evaluate the inhibitive effectiveness of inhibitors to TACE and MMP-9. In the assay method for TACE and MMP-9, peptides labelled with the ultraviolet group-Dpa were used as substrates. Alanine-Dpa was synthesised and was used as the internal standard for quantitative analysis. After the peptide substrates were hydrolysed by TACE (MMP-9) for 15min (25min) at 37°C, the amount of remaining substrates were determined by reversed-phased HPLC with UV detection at 353nm. The relative peak area of the substrate was linearly dependent on the substrate concentration. This method was then applied to determine the 50% inhibitory concentration (IC50) of GM6001 and inhibitor A for both TACE and MMP-9.
机译:建立了一种基于内标法的高效液相色谱法,用于测定肿瘤坏死因子-α转化酶(TACE)活性和基质金属蛋白酶-9(MMP-9)活性,并用于评价抑制剂对TACE和MMP-9的抑制作用。在TACE和MMP-9的测定方法中,将标记有紫外线基-Dpa的肽用作底物。合成了丙氨酸-Dpa,并将其用作定量分析的内标。在TACE(MMP-9)在37°C下将肽底物水解15分钟(25分钟)后,通过反相HPLC在353nm处检测UV来测定残留底物的量。底物的相对峰面积与底物浓度线性相关。然后将该方法用于测定GM6001和抑制剂A对TACE和MMP-9的50%抑制浓度(IC 50 )。

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