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单宁酸可与驱虫剂发生直接相互作用:等温滴定量热法的研究。

Tannins Can Have Direct Interactions with Anthelmintics: Investigations by Isothermal Titration Calorimetry.

机构信息

Department of Chemistry, University of Turku, FI-20014 Turku, Finland.

School of Chemistry, Food and Pharmacy, University of Reading, Whiteknights, P.O. Box 224, Reading RG6 6AP, UK.

出版信息

Molecules. 2023 Jul 7;28(13):5261. doi: 10.3390/molecules28135261.

Abstract

Plant tannins are known for their anthelmintic and antiparasitic activities and have been increasingly studied to battle the ever-growing problem of anthelmintic resistance. While tannins have been shown to exhibit these activities on their own, one approach would be to use them as complementary nutrients alongside commercial anthelmintics. So far, research on the interactions between tannins and anthelmintics is limited, and few studies have reported both synergistic and antagonistic effects depending on the type of tannin and the method used. These interactions could either strengthen or weaken the efficacy of commercial anthelmintics, especially if tannin-rich diets are combined with anthelmintics used as oral drenches. To study these interactions, a series of hydrolysable tannins (HTs) was selected, and their direct interactions with thiabendazole (TBZ) were evaluated by isothermal titration calorimetry (ITC), which allowed the detection of the exothermic interaction but also the roles and significances of different structural features of HTs in these interactions. Our results show that HTs can have a direct interaction with the benzimidazole anthelmintic TBZ and that the interaction is strengthened by increasing the number of free galloyl groups and the overall molecular flexibility of HTs.

摘要

植物单宁以其驱虫和抗寄生虫活性而闻名,并且越来越多地被研究用于对抗日益严重的驱虫剂耐药性问题。虽然单宁本身就具有这些活性,但一种方法是将它们作为补充营养物质与商业驱虫剂一起使用。到目前为止,关于单宁和驱虫剂之间相互作用的研究有限,而且很少有研究报道根据单宁的类型和使用方法,会产生协同和拮抗作用。这些相互作用可能会增强或削弱商业驱虫剂的功效,特别是如果富含单宁的饮食与用作口服滴剂的驱虫剂结合使用的话。为了研究这些相互作用,选择了一系列可水解单宁(HTs),并通过等温热力学滴定法(ITC)评估了它们与噻苯达唑(TBZ)的直接相互作用,该方法允许检测到放热处理相互作用,还可以检测到 HTs 中不同结构特征在这些相互作用中的作用和重要性。我们的结果表明,HTs 可以与苯并咪唑类驱虫剂 TBZ 发生直接相互作用,并且通过增加游离没食子酰基的数量和 HTs 的整体分子灵活性来增强相互作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/555d/10343783/40e96450429e/molecules-28-05261-g001.jpg

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