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Volume 20, Issue 9
  • ISSN: 1573-4064
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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 three-dimensional 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.

© 2024 Bentham Science Publishers
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2024-06-05
2024-11-14

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In silico and In vitro Assessment of Dimeric Flavonoids (Brachydins) on Rhipicephalus microplus Glutathione S-transferase
Medicinal Chemistry 20, 912 (2024); https://doi.org/10.2174/0115734064298481240517072216
/content/journals/mc/10.2174/0115734064298481240517072216
/content/journals/mc/10.2174/0115734064298481240517072216
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  • Article Type:     Research Article
Keyword(s): dimeric flavonoids; Fridericia platyphylla; GST inhibition; Rhipicephalus microplus; Tick

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