The Effectivity Analysis of Accumulation of Liposomal, Micellar, and Water-Soluble Forms of Diminazene in Cells and in Organs

Староверов, С. А.; Pristensky, Dmitry V.; Yermilov, D.N.; Габалов, К. П.; Жемеричкин, Д. А.; Сидоркин, В. А.; Shcherbakov, A. A.; Shchyogolev, S. Yu.; Дыкман, Л. А.

doi:10.1080/10717540500459084

Cited by 5 publications

(2 citation statements)

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“…Liposomes are a widely used successful system when targeting macrophages [39] and macrophages are the primary site for ASFV infection [40]. As such, tris-benzimidazole packaged in liposomes may potentially be engineered to show significant accumulation in macrophages and to minimize potential toxic effects [41,42].…”

Section: Resultsmentioning

confidence: 99%

Comparative in silico study of congocidine congeners as potential inhibitors of African swine fever virus

et al. 2019

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African swine fever virus (ASFV) infection is fatal in domesticated pigs, with a mortality rate approaching 100%. This may result in economic losses and threats to food security. Currently, there are no approved vaccines or antiviral therapies for ASFV. Therefore, in this study, we evaluated congocidine congeners and a tris-benzimidazole as potential inhibitors of ASFV transcription using an in silico approach. We applied redocking of congocidine and docking of its congeners and a tris-benzimidazole to a receptor containing B-DNA with AT-motifs as a target to mimic conserved ASFV late gene promoters. Subsequently, the binding scores of DNA-ligand docked complexes were evaluated and their binding affinity was estimated. Molecular dynamics (MD) simulation was then used to assess ligand behavior within the minor groove. From our results, it is evident the less toxic congocidine congeners and tris-benzimidazole could dock to AT-rich regions significantly. Additionally, the predicted binding affinities had suitable values comparable to other experimentally determined minor groove binders, MD simulation of the docked DNA-ligand complexes and subsequent molecular trajectory visualization further showed that the ligands remained embedded in the minor groove during the time course of simulation, indicating that these ligands may have potential applications in abrogating ASFV transcription.

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Section: Resultsmentioning

confidence: 99%

Comparative in silico study of congocidine congeners as potential inhibitors of African swine fever virus

et al. 2019

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show abstract

“…Those studies also were addressed to the biodynamics and toxicity of such complexes. Staroverov et al [5] probed the effectiveness of using liposomal, micellar, and watersoluble drug forms of diminazene for its cellular localization and selective accumulation at the sites of aggregation of pathogenic organisms.…”

Section: Introductionmentioning

confidence: 99%