Faculty of Science, Department of Chemistry, Ataturk University, Erzurum, Turkey.
Department of Food Technology, Oltu Vocational School, Ataturk University, Oltu, Erzurum, Turkey.
Arch Pharm (Weinheim). 2018 Dec;351(12):e1800263. doi: 10.1002/ardp.201800263. Epub 2018 Nov 27.
Aldose reductase converts glucose to sorbitol in the polyol pathway. It is an important enzyme to prevent diabetic complications. In this study, we studied the inhibitory effects of bromophenol derivatives on aldose reductase (AR), α-glucosidase, and α-amylase enzymes. In the bromophenols series, compound 1f showed the maximum inhibition effect against AR with a K value of 0.05 ± 0.01 μM, while compound 1d showed the lowest inhibition effect against AR with a K value of 1.13 ± 0.99 μM. In addition, α-amylase from porcine pancreas and α-glucosidase from Saccharomyces cerevisiae were used as enzymes. In this study, all compounds were tested for the inhibition of the α-glucosidase enzyme and demonstrated efficient inhibition profiles with K values in the range of 43.62 ± 5.28 to 144.37 ± 16.37 nM against α-glucosidase. Additionally, these compounds were tested against the α-amylase enzyme, which determined an effective inhibition profile with IC values in the range of 9.63-91.47 nM. These compounds can be selective inhibitors of AR, α-glucosidase, and α-amylase enzymes as antidiabetic agents.
醛糖还原酶在多元醇途径中将葡萄糖转化为山梨糖醇。它是预防糖尿病并发症的重要酶。在这项研究中，我们研究了溴酚衍生物对醛糖还原酶（AR）、α-葡萄糖苷酶和α-淀粉酶的抑制作用。在溴酚系列中，化合物 1f 对 AR 的抑制作用最大，K 值为 0.05±0.01μM，而化合物 1d 对 AR 的抑制作用最低，K 值为 1.13±0.99μM。此外，还使用了来自猪胰腺的α-淀粉酶和来自酿酒酵母的α-葡萄糖苷酶作为酶。在这项研究中，所有化合物都被测试了对α-葡萄糖苷酶的抑制作用，并表现出有效的抑制作用，K 值在 43.62±5.28 到 144.37±16.37nM 范围内。此外，这些化合物还被测试了对α-淀粉酶的抑制作用，其 IC 值在 9.63-91.47nM 范围内确定了有效的抑制作用。这些化合物可以作为抗糖尿病药物，选择性抑制 AR、α-葡萄糖苷酶和α-淀粉酶。
