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Inhibitory effect of morin on aldolase 2 from Eimeria tenella

Authors :
Junjing Hu
Mingfei Sun
Nanshan Qi
Asmaa M.I. Abuzeid
Juan Li
Haiming Cai
Minna Lv
Xuhui Lin
Shenquan Liao
Guoqing Li
Source :
International Journal for Parasitology: Drugs and Drug Resistance, Vol 20, Iss , Pp 1-10 (2022)
Publication Year :
2022
Publisher :
Elsevier, 2022.

Abstract

Eimeria tenella (E. tenella) is a protozoal parasite that can cause severe cecal lesions and death in chickens, seriously harming the chicken industry. Conventional control strategies mainly rely on anticoccidial drugs. However, the emerging problems of anticoccidial resistance and drug residues necessitate exploring potential drug targets for developing new anticoccidial drugs. Fructose-1,6-bisphosphate aldolase (ALD) is an essential enzyme for parasite energy metabolism that has been considered a potential drug target. In this study, we analyzed the molecular and biochemical properties of E. tenella ALD2 (EtALD2). EtALD2 mRNA expression was highest in second-generation merozoites, whereas the protein level was highest in unsporulated oocysts. Indirect immunofluorescence showed that EtALD2 was mainly distributed in sporozoite’ cytoplasm. The natural product inhibitor (morin) was screened by computer-aided drug screening. Enzyme kinetic and inhibition kinetic assays showed that morin had a good inhibitory effect on EtALD2 activity (IC50 = 10.37 μM, Ki = 48.97 μM). In vitro inhibition assay demonstrated that morin had an inhibitory effect on E. tenella development, with an IC50 value of 3.98 μM and drug selection index of 177.49. In vivo, morin significantly improved cecal lesions (p

Details

Language :
English
ISSN :
22113207
Volume :
20
Issue :
1-10
Database :
Directory of Open Access Journals
Journal :
International Journal for Parasitology: Drugs and Drug Resistance
Publication Type :
Academic Journal
Accession number :
edsdoj.7d6bb5293c0c4ae3ae02298bfe844b47
Document Type :
article
Full Text :
https://doi.org/10.1016/j.ijpddr.2022.07.002