Krzesimir Ciura

University of Gdańsk

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Joanna Nowakowska

Poznan University of Medical Sciences

Tomasz Bączek

Gdańsk Medical University

Piotr Kawczak

Gdańsk Medical University

Wiesław Sawicki

Gdańsk Medical University

Katarzyna E. Greber

Gdańsk Medical University

Hanna Kapica

Gdańsk Medical University

Karolina Jagiełło

University of Gdańsk

Szymon Dziomba

Gdańsk Medical University

Tomasz Puzyn

University of Gdańsk

Michał J. Markuszewski

Gdańsk Medical University

Cooperative Institutions

Gdańsk Medical University

University of Gdańsk

University of Helsinki

Gdańsk University of Technology

Chinese Academy of Sciences

United States Food and Drug Administration

National Center for Toxicological Research

Zhejiang University

Faculty (United Kingdom)

Medical University of Warsaw

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Lipophilicity Determination of Quaternary (Fluoro)Quinolones by Chromatographic and Theoretical Approaches

International Journal of Molecular Sciences (2019)

Krzesimir Ciura Joanna Fedorowicz Filip Andrić Katarzyna E. Greber Alina Gurgielewicz

Lipophilicity is a vital physicochemical parameter of a molecule, which affects several biological processes such as absorption, tissue distribution, and pharmacokinetic properties. In this study, evaluation of lipophilicities of a series of novel fluoroquinolone-Safirinium dye hybrids using chromatographic and computational methods is presented. Fluoroquinolone-Safirinium dye hybrids have been synthesized as new dual-acting hydrophilic antibacterial agents. Reversed phase thin-layer chromatography and micellar electrokinetic chromatography experiments were carried out. Furthermore, logP values of the target structures were predicted by means of different software platforms and algorithms. In order to assess similarities and dissimilarities of the obtained lipophilicity indexes, cluster analysis and sum of ranking differences were performed. The significant differences of calculated logP values (α = 0.05, p < 0.001) indicated that an experimental approach is necessary for lipophilicity prediction of this class of antibiotics. Chromatographic data indicated that the newly synthesized hybrid (fluoro)quinolone-based quaternary ammonium derivatives show less lipophilic character than the parent (fluoro)quinolones. Additionally, the chromatographically obtained lipophilicity indexes were evaluated for possible application in quantitative retention–activity relationships. The established lipophilicity models have the potential to predict antimicrobial activities of a series of quaternary (fluoro)quinolones against Bacillus subtilis, Escherichia coli, and Proteus vulgaris.

Lipophilicity

10.3390/ijms20215288

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Citations (36)

Sweeping of hydrophobic amines under inhomogeneous electric field and low surfactant concentration in micellar electrokinetic chromatography

Electrophoresis (2015)

Krzesimir Ciura Piotr Kowalski Joanna Nowakowska Michał J. Markuszewski Tomasz Bączek

The influence of sample matrix on sample sweeping in MEKC was examined in the presented manuscript. Significant focusing effect was observed for relatively hydrophobic cationic compounds (emetine, strychnine and quinine) using high ionic strength sample matrix (900 mM H3 PO4 /720 mM Tris) which conductivity was about ninefold higher than utilized BGE. Moreover, the results were obtained using BGE composed of comparatively low surfactant concentration (10 mM SDS) and 40 mM H3 PO4 /32 mM Tris buffer solution. About 200 to 300-fold preconcentration of analytes was reached with the presented method. Basing on experimental results and computer simulation using Simul5 software, hypothetical mechanism of observed phenomenon was proposed.

Micellar electrokinetic chromatography

Matrix (chemical analysis)

Cationic polymerization

10.1002/elps.201500436

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Citations (8)

Biopartitioning micellar electrokinetic chromatography – Concept study of cationic analytes

Microchemical Journal (2019)

Krzesimir Ciura Hanna Kapica Szymon Dziomba Piotr Kawczak Mariusz Belka

Micellar electrokinetic chromatography

Lipophilicity

10.1016/j.microc.2019.104518

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Citations (11)

The on-line preconcentration of nanoparticles in electromigration techniques

Journal of Chromatography A (2019)

Szymon Dziomba Krzesimir Ciura Marta Dawid

Electromigration

Nanomaterials

Characterization

10.1016/j.chroma.2019.06.053

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Citations (9)

A bibliometric analysis of the recent achievements in pulmonary safety of nanoparticles

Figshare (2023)

Karina Falkiewicz Izabela Fryca Krzesimir Ciura Alicja Mikołajczyk Karolina Jagiełło

Assessing research activity is an important step for planning future initiatives oriented toward filling the remaining gaps in a field. Therefore, the objective of the current study was to review recently published research on pulmonary toxicity caused by nanomaterials. However, here, instead of reviewing possible toxic effects and discussing their mode of action, the goal was to establish trends considering for example examined so far nanomaterials or used testing strategies. A total of 2316 related articles retrieved from the three most cited databases (PubMed Scopus, Web of Science), selected based on the title and abstract requirements, were used as the source of the review. Based on the bibliometric analysis, the nano-meter metal oxides, and carbon-based nanotubes were identified as the most frequently studied nanomaterials, while quantum dots, which might induce possible harmful effects, were not considered so far. The majority of testing of pulmonary safety is based on in vitro studies with observed growth of the contribution of novel testing strategies, such as 3D lung model, air-liquid interface system, or omic analysis.

10.6084/m9.figshare.24572758

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Citations (0)

Green-Friendly Synthesis of 1,3,5-Triazine Derivatives Using a Sonochemical Protocol

Damian Kułaga Anna K. Drabczyk Przemysław Zaręba Jolanta Jaśkowska Julia Chrzan

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Triazine

10.2139/ssrn.4792562

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Use of biomimetic chromatography and in vitro assay to develop predictive GA-MLR model for use in drug-property prediction among anti-depressant drug candidates

Microchemical Journal (2022)

Szymon Ulenberg Krzesimir Ciura Paweł Georgiev Monika Pastewska Grzegorz Ślifirski

Molecular descriptor

Lipophilicity

Drug Development

10.1016/j.microc.2022.107183

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Citations (13)

Exploration and optimisation of structure-activity relationships of new triazole-based C-terminal Hsp90 inhibitors towards in vivo anticancer potency

Biomedicine & Pharmacotherapy (2024)

Jaka Dernovšek Živa Zajec Goran Poje Dunja Urbančič Caterina Sturtzel

The development of new anticancer agents is one of the most urgent topics in drug discovery. Inhibition of molecular chaperone Hsp90 stands out as an approach that affects various oncogenic proteins in different types of cancer. These proteins rely on Hsp90 to obtain their functional structure, and thus Hsp90 is indirectly involved in the pathophysiology of cancer. However, the most studied ATP-competitive inhibition of Hsp90 at the N-terminal domain has proven to be largely unsuccessful clinically. Therefore, research has shifted towards Hsp90 C-terminal domain (CTD) inhibitors, which are also the focus of this study. Our recent discovery of compound C has provided us with a starting point for exploring the structure-activity relationship and optimising this new class of triazole-based Hsp90 inhibitors. This investigation has ultimately led to a library of 33 analogues of C that have suitable physicochemical properties and several inhibit the growth of different cancer types in the low micromolar range. Inhibition of Hsp90 was confirmed by biophysical and cellular assays and the binding epitopes of selected inhibitors were studied by STD NMR. Furthermore, the most promising Hsp90 CTD inhibitor 5x was shown to induce apoptosis in breast cancer (MCF-7) and Ewing sarcoma (SK-N-MC) cells while inducing cause cell cycle arrest in MCF-7 cells. In MCF-7 cells, it caused a decrease in the levels of ERα and IGF1R, known Hsp90 client proteins. Finally, 5x was tested in zebrafish larvae xenografted with SK-N-MC tumour cells, where it limited tumour growth with no obvious adverse effects on normal zebrafish development.

Hsp90 inhibitor

Structure–activity relationship

10.1016/j.biopha.2024.116941

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Citations (2)

Chromatographic analysis of ivabradine on polar, nonpolar and chemically modified adsorbents by HPTLC

Journal of Food and Drug Analysis (2013)

Piotr Pikuł Joanna Nowakowska Krzesimir Ciura

Ivabradine

10.1016/j.jfda.2013.05.006

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Citations (22)