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阿仑膦酸钠重新定位为靶向旋毛虫无机焦磷酸酶的潜在抗寄生虫剂:体外支持的分子对接和分子动力学模拟研究

Alendronate repositioning as potential anti-parasitic agent targeting Trichinella spiralis inorganic pyrophosphatase, in vitro supported molecular docking and molecular dynamics simulation study.

作者信息

Hanafy Marmar A, Nassar Doaa A, Zahran Fatima M, Mohammed Magdy M D

机构信息

Department of Parasitology, Faculty of Medicine, Ain Shams University, Cairo, Egypt.

Department of Pharmacognosy, Pharmaceutical and Drug Industries Research Institute, National Research Centre, Dokki, Cairo, 12622, Egypt.

出版信息

BMC Chem. 2025 May 6;19(1):119. doi: 10.1186/s13065-025-01468-4.

Abstract

Trichinellosis represents great public health and economic problems worldwide. Moreover, the development of parasitic resistance against conventional anthelminthic treatment led to the urgent search for new therapeutic strategies, including drug repurposing. Bisphosphonates have been used to inhibit the growth of many parasites and have also emerged as promising candidates for the treatment of cryptosporidiosis and amoebic liver abscess. Alendronate is a second-generation bisphosphonate that is widely used for the treatment and prevention of osteoporosis. Till date, there is not enough data on the effect of this drug on Trichinella spiralis and it is unknown whether the regular use of this drug in osteoporotic patients may alter the course of the infection. ALN showed a significant lethal effect on both adult worms and juveniles, with severe tegumental damage in the form of fissures in the cuticle, widening of the hypodermal gland, and flattening of the cuticular annulation, ending with the appearance of multiple vesicles and large cauliflower masses. Molecular docking outcomes unveiled the potential inhibition of ALN against T. spiralis surface proteins (i.e., Ts-SP, Ts-PPase, Ts-MAPRC2, Ts-TS, Ts-MIF, etc.), with promising results confirmed its ability to defeat T. spiralis via targeting its surface proteins. Moreover, molecular dynamics simulation, through the analysis of RMSD, RMSF, RG, SASA and cluster analysis, proved the prolonged effective inhibition of ALN on T. spiralis inorganic pyrophosphatase, as an essential surface protein required for molting and developmental process of intestinal larval stages. Thus, ALN might be a valuable drug candidate for the treatment of trichinellosis and warrant further investigation in animal models of disease.

摘要

旋毛虫病在全球范围内构成了重大的公共卫生和经济问题。此外,寄生虫对传统驱虫治疗产生耐药性,这促使人们迫切寻找新的治疗策略,包括药物重新利用。双膦酸盐已被用于抑制多种寄生虫的生长,并且也已成为治疗隐孢子虫病和阿米巴肝脓肿的有前景的候选药物。阿仑膦酸钠是第二代双膦酸盐,广泛用于治疗和预防骨质疏松症。迄今为止,关于这种药物对旋毛虫的作用尚无足够数据,并且尚不清楚骨质疏松症患者常规使用这种药物是否会改变感染进程。阿仑膦酸钠对成虫和幼虫均显示出显著的致死作用,表现为严重的体表损伤,如角质层出现裂缝、皮下腺增宽以及角质层环纹变平,最终出现多个水泡和大的菜花状肿块。分子对接结果揭示了阿仑膦酸钠对旋毛虫表面蛋白(即Ts-SP、Ts-PPase、Ts-MAPRC2、Ts-TS、Ts-MIF等)具有潜在抑制作用,有前景的结果证实了其通过靶向旋毛虫表面蛋白来战胜旋毛虫的能力。此外,分子动力学模拟通过对均方根偏差(RMSD)、均方根波动(RMSF)、回转半径(RG)、溶剂可及表面积(SASA)的分析和聚类分析,证明了阿仑膦酸钠对旋毛虫无机焦磷酸酶具有延长的有效抑制作用,无机焦磷酸酶是肠道幼虫阶段蜕皮和发育过程所需的一种重要表面蛋白。因此,阿仑膦酸钠可能是治疗旋毛虫病的一种有价值的候选药物,值得在疾病动物模型中进一步研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/54c8/12057173/d9827ef73d3a/13065_2025_1468_Fig1_HTML.jpg

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