Suppr超能文献

二聚体类黄酮(短梗菌素)对谷胱甘肽S-转移酶的作用及评估

and Assessment of Dimeric Flavonoids (Brachydins) on Glutathione S-transferase.

作者信息

Dos Santos Bezerra Wallyson André, Tavares Caio Pavão, Lima Victor Antônio Silva, da Rocha Cláudia Quintino, da Silva Vaz Junior Itabajara, Michels Paul A M, Costa Junior Livio Martins, Dos Santos Soares Alexandra Martins

机构信息

Programa de Pós-Graduação em Biodiversidade e Biotecnologia da Amazônia - Bionorte, Universidade Federal do Maranhão, São Luís, MA, Brazil.

Laboratório de Controle de Parasitos, Departamento de Patologia, Universidade Federal do Maranhão, São Luís, MA, Brazil.

出版信息

Med Chem. 2024;20(9):912-919. doi: 10.2174/0115734064298481240517072216.

Abstract

INTRODUCTION

, an important cattle ectoparasite, is responsible for a substantial negative impact on the economy due to productivity loss. The emergence of resistance to widely used commercial acaricides has sparked efforts to explore alternative products for tick control.

METHODS

To address this challenge, innovative solutions targeting essential tick enzymes, like glutathione S-transferase (GST), have gained attention. Dimeric flavonoids, particularly brachydins (BRAs), have demonstrated various biological activities, including antiparasitic effects. The objectives of this study were to isolate four dimeric flavonoids from roots and to evaluate their potential as inhibitors of GST.

RESULTS

assays confirmed the inhibition of GST by BRA-G, BRA-I, BRA-J, and BRA-K with IC values of 0.075, 0.079, 0.075, and 0.058 mg/mL, respectively, with minimal hemolytic effects. Molecular docking of BRA-G, BRA-I, BRA-J, and BRA-K in a threedimensional model of GST revealed predicted interactions with MolDock Scores of - 142.537, -126.831, -108.571, and -123.041, respectively. Both and analyses show that brachydins are potential inhibitors of GST.

CONCLUSION

The findings of this study deepen our understanding of GST inhibition in ticks, affirming its viability as a drug target. This knowledge contributes to the advancement of treatment modalities and strategies for improved tick control.

摘要

引言

蜱虫是一种重要的牛体外寄生虫,由于生产力损失,对经济造成了重大负面影响。对广泛使用的商业杀螨剂产生抗药性的出现,引发了探索替代蜱虫控制产品的努力。

方法

为应对这一挑战,针对蜱虫必需酶(如谷胱甘肽S-转移酶(GST))的创新解决方案受到了关注。二聚体黄酮类化合物,特别是短柄黄酮(BRAs),已显示出多种生物活性,包括抗寄生虫作用。本研究的目的是从[植物名称]根部分离出四种二聚体黄酮类化合物,并评估它们作为GST抑制剂的潜力。

结果

实验证实BRA-G、BRA-I、BRA-J和BRA-K对GST有抑制作用,IC50值分别为0.075、0.079、0.075和0.058mg/mL,溶血作用最小。BRA-G、BRA-I、BRA-J和BRA-K在GST三维模型中的分子对接显示预测的相互作用,MolDock分数分别为-142.537、-126.831、-108.571和-123.041。[具体分析方法1]和[具体分析方法2]分析均表明短柄黄酮是GST的潜在抑制剂。

结论

本研究结果加深了我们对蜱虫中GST抑制作用的理解,确认了其作为药物靶点的可行性。这一知识有助于推进治疗方式和策略,以改善蜱虫控制。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验