The versatile biological activity of gallotannins has been investigated for a long time, including their use as α‐amylase inhibitors for the treatment of diabetes and its complications. The effectiveness of gallotannins on a wide range of enzymes refers to promiscuity. We proved that gallotannins are non‐specific promiscuous α‐amylase inhibitors, which exert their effect through their aggregates. A gallotannin of Aleppo oak origin fulfilled all the criteria for aggregators; significant changes could be observed in the IC₅₀ values in the presence of Triton^™ X‐100 detergent (from 2.3 to 110 μg/ml) and after enzyme–inhibitor preincubation (from 2.3 to 0.65 μg/ml). Increasing the enzyme concentration also led to the moderation of the inhibition by gallotannin. In addition, we observed that gallotannin molecules are those, which are involved in aggregation, and discrete protein molecules are adsorbed to the aggregates. This was revealed by the increasing particle size of gallotannin, which became three orders of magnitude higher after 150 min, whereas the size of α‐amylase remained unchanged. Consequently, gallotannins should be used as anti‐diabetic drugs only if the necessity of higher dose due to their promiscuity is taken into account. Aggregation propensity should not be ignored in case of in vivo applications.

中文翻译：

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没食子单宁是 α-淀粉酶的非特异性抑制剂：聚集体是参与抑制的活性物质

长期以来，人们一直在研究没食子单宁的多功能生物活性，包括它们作为α-淀粉酶抑制剂用于治疗糖尿病及其并发症。没食子单宁对多种酶的有效性是指滥交。我们证明了没食子单宁是非特异性混杂α-淀粉酶抑制剂，它们通过它们的聚集体发挥作用。源自阿勒颇橡木的没食子单宁满足了聚合器的所有标准；在 Triton ^™存在的情况下，IC ₅₀值可以观察到显着变化X-100 去污剂（2.3 至 110 μg/ml）和酶抑制剂预孵育后（2.3 至 0.65 μg/ml）。增加酶浓度也导致了没食子单宁的抑制作用的缓和。此外，我们观察到没食子单宁分子是那些参与聚集的分子，离散的蛋白质分子被吸附到聚集体上。这是由棓单宁的粒径增加所揭示的，在 150 分钟后增加了三个数量级，而α-淀粉酶的大小保持不变。因此，只有在考虑到由于其滥交而需要更高剂量的情况下，才应将没食子单宁用作抗糖尿病药物。在体内应用的情况下不应忽视聚集倾向。