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首页> 外文期刊>European journal of pharmaceutical sciences >Inhibitory effects of selected antibiotics on the activities of alpha-amylase and alpha-glucosidase: In-vitro, in-vivo and theoretical studies
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Inhibitory effects of selected antibiotics on the activities of alpha-amylase and alpha-glucosidase: In-vitro, in-vivo and theoretical studies

机译：选定抗生素对α-淀粉酶和α-葡糖苷酶活性的抑制作用：体外，体内和理论研究

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Antibiotics are effective drugs that are used to treat infectious diseases either by killing bacteria or slowing down their growth. The well-adapted structural features of antibiotics for the inhibition/activation of enzymes include several available hydrogen bond (H-bond) acceptors and donors, flexible backbone and hydrophobic nature. The substrates of alpha-amylase and alpha-glucosidase, known as key absorbing enzymes, have functional groups (OH groups) rembling antibiotics. Given the possibility of developing in diabetics and the significant association between diabetes and infection, the present study was conducted to investigate the influences of tetracycline (TET), kanamycin (KANA), lincomycin (LIN), erythromycin (ERM) and azithromycin (AZM) on alpha-glucosidase and alpha-amylase activities with calculating IC50 and K-i values. Also, the efficacy of antibiotics after oral administration was evaluated by analysis of blood glucose concentrations in rats, as well as a molecular docking analysis was explored. alpha-glucosidase and a-amylase activities were inhibited in a dose dependent fashion by TET with an IC50 of 38.7 +/- 1.4 and 47.8 +/- 3.2 mu M respectively, by KANA with an IC50 of 46.2 +/- 1.6 and 65.1 +/- 1.6, by LIN with an IC50 of 59.1 +/- 2.1 and 51.3 +/- 4.1, by ERM with an IC50 of 94.9 +/- 4.7 and 65.7 +/- 3.8 and by AZM with an IC50 of 69.4 +/- 4.4 and 103.6 +/- 6.2. Moreover, the K-i values of TET were calculated as 4.4 +/- 0.6 and 8.4 +/- 0.8 mu M for alpha-glucosidase and alpha-amylase in a competitive-mode and mixed-mode inhibition. In addition, to communicate with the active site of alpha-glucosidase and alpha-amylase respectively, TET presented a binding energy of -9.8 and -8.8 kcal/mol, KANA -7.9 and -7.1, LIN -7.8 and -6.7, ERM -6.8 and -6.4, and AZM -6.4 and -7.5 kcal/mol. In-vivo studies also suggested a decrease in the blood glucose concentration after administering TET compared to the positive controls (P < 0.01). The results obtained from the present research can therefore help the scientific community explore the possible interconnection between the clinical side-effects of antibiotics and their alpha-glucosidase and alpha-amylase inhibitory properties, as the target enzymes in hypoglycemia conditions.
机译：抗生素是通过杀死细菌或减缓其生长来治疗传染病的有效药物。用于抑制/活化酶的抗生素的良好结构特征包括几种可用的氢键（H键）受体和供体，柔性骨架和疏水性。称为关键吸收酶的α-淀粉酶和α-葡糖苷酶的底物具有官能团（OH基团）去除抗生素。鉴于糖尿病和糖尿病和感染之间的重要关联的可能性，进行了本研究，研究了四环素（TET），卡那霉素（Kana），林霉素（LIN），红霉素（ERM）和阿奇霉素（AZM）的影响用计算IC50和Ki值的α-葡糖苷酶和α-淀粉酶活性。而且，通过分析大鼠血糖浓度来评价口服给药后的抗生素的疗效，以及探索分子对接分析。 α-葡萄糖苷酶和α-淀粉酶活性，通过TET通过TET依赖于剂量，IC50分别为38.7 +/- 1.4和47.8 +/-3.2μmm，通过Kana，IC50为46.2 +/- 1.6和65.1 + / - 1.6，Lin，IC50为59.1 +/- 2.1和51.3 +/- 4.1，ORM，IC50为94.9 +/- 4.7和65.7 +/- 3.8和AZM，IC50为69.4 +/- 4.4和103.6 +/- 6.2。此外，对于α-葡糖苷酶和α-淀粉酶，在竞争模式和混合模式抑制中，将TET的K-1值计算为4.4 +/- 0.6和8.4 +/-0.8μm。此外，为了分别与α-葡糖苷酶和α-淀粉酶的活性位点通信，TET呈现为-9.8和-8.8 kcal / mol，Kana -7.9和-7.1，Lin -7.8和-6.7，ERM - 6.8和-6.4和AZM -6.4和-7.5 kcal / mol。体内研究还表明，与阳性对照相比，施用TET后血糖浓度的降低（P <0.01）。因此，从本研究中获得的结果可以帮助科学界探讨抗生素及其α-葡糖苷酶和α-淀粉酶抑制性能的临床副作用之间的可能互连，作为低血糖条件中的靶酶。

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