Transportan 10 improves the pharmacokinetics and pharmacodynamics of vancomycin

Abstract In the presented study, transportan 10 (TP10), an amphipathic cell penetrating peptide (CPP) with high translocation activity, was conjugated with vancomycin (Van), which is known for poor access to the intracellular bacteria and the brain. The antibacterial activity of the conjugates was t...

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Auteurs principaux:	Jarosław Ruczyński, Izabela Rusiecka, Katarzyna Turecka, Agnieszka Kozłowska, Magdalena Alenowicz, Iwona Gągało, Anna Kawiak, Piotr Rekowski, Krzysztof Waleron, Ivan Kocić
Format:	article
Langue:	EN
Publié:	Nature Portfolio 2019
Sujets:	Medicine R Science Q
Accès en ligne:	https://doaj.org/article/6ab41cdc1a11452badeea81901679a26
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spelling	oai:doaj.org-article:6ab41cdc1a11452badeea81901679a262021-12-02T15:08:59ZTransportan 10 improves the pharmacokinetics and pharmacodynamics of vancomycin10.1038/s41598-019-40103-w2045-2322https://doaj.org/article/6ab41cdc1a11452badeea81901679a262019-03-01T00:00:00Zhttps://doi.org/10.1038/s41598-019-40103-whttps://doaj.org/toc/2045-2322Abstract In the presented study, transportan 10 (TP10), an amphipathic cell penetrating peptide (CPP) with high translocation activity, was conjugated with vancomycin (Van), which is known for poor access to the intracellular bacteria and the brain. The antibacterial activity of the conjugates was tested on selected clinical strains of methicillin-resistant Staphylococcus aureus (MRSA) and Enterococcus sp. It turned out that all of them had superior antimicrobial activity in comparison to that of free Van, which became visible particularly against clinical MRSA strains. Furthermore, one of the conjugates was tested against MRSA - infected human cells. With respect to them, this compound showed high bactericidal activity. Next, the same conjugate was screened for its capacity to cross the blood brain barrier (BBB). Therefore, qualitative and quantitative analyses of the conjugate’s presence in the mouse brain slices were carried out after its iv administration. They indicated the conjugate’s presence in the brain in amount >200 times bigger than that of Van. The conjugates were safe with respect to erythrocyte toxicity (erythrocyte lysis assay). Van in the form of a conjugate with TP10 acquires superior pharmacodynamic and pharmacokinetic.Jarosław RuczyńskiIzabela RusieckaKatarzyna TureckaAgnieszka KozłowskaMagdalena AlenowiczIwona GągałoAnna KawiakPiotr RekowskiKrzysztof WaleronIvan KocićNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 9, Iss 1, Pp 1-15 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Jarosław Ruczyński Izabela Rusiecka Katarzyna Turecka Agnieszka Kozłowska Magdalena Alenowicz Iwona Gągało Anna Kawiak Piotr Rekowski Krzysztof Waleron Ivan Kocić Transportan 10 improves the pharmacokinetics and pharmacodynamics of vancomycin
description	Abstract In the presented study, transportan 10 (TP10), an amphipathic cell penetrating peptide (CPP) with high translocation activity, was conjugated with vancomycin (Van), which is known for poor access to the intracellular bacteria and the brain. The antibacterial activity of the conjugates was tested on selected clinical strains of methicillin-resistant Staphylococcus aureus (MRSA) and Enterococcus sp. It turned out that all of them had superior antimicrobial activity in comparison to that of free Van, which became visible particularly against clinical MRSA strains. Furthermore, one of the conjugates was tested against MRSA - infected human cells. With respect to them, this compound showed high bactericidal activity. Next, the same conjugate was screened for its capacity to cross the blood brain barrier (BBB). Therefore, qualitative and quantitative analyses of the conjugate’s presence in the mouse brain slices were carried out after its iv administration. They indicated the conjugate’s presence in the brain in amount >200 times bigger than that of Van. The conjugates were safe with respect to erythrocyte toxicity (erythrocyte lysis assay). Van in the form of a conjugate with TP10 acquires superior pharmacodynamic and pharmacokinetic.
format	article
author	Jarosław Ruczyński Izabela Rusiecka Katarzyna Turecka Agnieszka Kozłowska Magdalena Alenowicz Iwona Gągało Anna Kawiak Piotr Rekowski Krzysztof Waleron Ivan Kocić
author_facet	Jarosław Ruczyński Izabela Rusiecka Katarzyna Turecka Agnieszka Kozłowska Magdalena Alenowicz Iwona Gągało Anna Kawiak Piotr Rekowski Krzysztof Waleron Ivan Kocić
author_sort	Jarosław Ruczyński
title	Transportan 10 improves the pharmacokinetics and pharmacodynamics of vancomycin
title_short	Transportan 10 improves the pharmacokinetics and pharmacodynamics of vancomycin
title_full	Transportan 10 improves the pharmacokinetics and pharmacodynamics of vancomycin
title_fullStr	Transportan 10 improves the pharmacokinetics and pharmacodynamics of vancomycin
title_full_unstemmed	Transportan 10 improves the pharmacokinetics and pharmacodynamics of vancomycin
title_sort	transportan 10 improves the pharmacokinetics and pharmacodynamics of vancomycin
publisher	Nature Portfolio
publishDate	2019
url	https://doaj.org/article/6ab41cdc1a11452badeea81901679a26
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Transportan 10 improves the pharmacokinetics and pharmacodynamics of vancomycin

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