Search results for: Natalia Szkaradek

Items from 1 to 12 out of 12 results

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Preliminary antifungal activity assay of selected chlorine‐containing derivatives of xanthone and phenoxyethyl amines

Karolina Klesiewicz, Dorota Żelaszczyk, Danuta Trojanowska, Bożena Bogusz, more

Chemical Biology & Drug Design > 92 > 5 > 1867 - 1875

The aim of this study was to evaluate antifungal activity in a diverse group of chlorine‐containing xanthone and phenoxyethyl amine derivatives – and to select the most promising compounds for further studies. The antifungal efficacy of 16 compounds was tested with qualitative and quantitative methods against both reference and clinical strains of dermatophytes, moulds and yeasts. The disc‐diffusion...

article

Contribution of reactive oxygen species to the anticancer activity of aminoalkanol derivatives of xanthone

Daniel Sypniewski, Natalia Szkaradek, Tomasz Loch, Anna M. Waszkielewicz, more

Investigational New Drugs > 2018 > 36 > 3 > 355-369

Summary Reactive oxygen species (ROS) are critically involved in the action of anticancer agents. In this study, we investigated the role of ROS in the anticancer mechanism of new aminoalkanol derivatives of xanthone. Most xanthones used in the study displayed significant pro-oxidant effects similar to those of gambogic acid, one of the most active anticancer xanthones. The pro-oxidant activity of...

article

Evaluation of anti-inflammatory and ulcerogenic potential of zinc–ibuprofen and zinc–naproxen complexes in rats

Magdalena Jarosz, Natalia Szkaradek, Henryk Marona, Gabriel Nowak, more

Inflammopharmacology > 2017 > 25 > 6 > 653-663

Because of numerous indications and high availability, non-steroidal anti-inflammatory drugs (NSAIDs) are among the most commonly prescribed and used medicines in the world. However, long-term therapy with and improper use of NSAIDs may lead to gastrointestinal damage. Therefore, improving the therapeutic index of the existing drugs has become a priority over the past decades. Considerable attention...

article

Anticonvulsant activity, crystal structures, and preliminary safety evaluation of N-trans-cinnamoyl derivatives of selected (un)modified aminoalkanols

Agnieszka Gunia-Krzyżak, Ewa Żesławska, Karolina Słoczyńska, Paulina Koczurkiewicz, more

European Journal of Medicinal Chemistry > 2016 > 107 > Complete > 26-37

Adequate control of seizures remains an unmet need in epilepsy. In order to identify new anticonvulsant agents, a series of N-trans-cinnamoyl derivatives of selected aminoalkanols was synthetized. The compounds were obtained in the reaction of N-acylation carried out in a two-phase system. The substances were tested in animal models of seizures induced either electrically (maximal electroshock – MES;...

article

Cardiovascular activity of the chiral xanthone derivatives

Natalia Szkaradek, Anna Rapacz, Karolina Pytka, Barbara Filipek, more

Bioorganic & Medicinal Chemistry > 2015 > 23 > 20 > 6714-6724

A series of 6 derivatives of xanthone were synthesized and evaluated for cardiovascular activity. The following pharmacological experiments were conducted: the binding affinity for adrenoceptors, the influence on the normal electrocardiogram, the effect on the arterial blood pressure, the effect on blood pressor response and prophylactic antiarrhythmic activity in adrenaline induced model of arrhythmia...

article

Antiarrhythmic activity of some xanthone derivatives with β1-adrenoceptor affinities in rats

Anna Rapacz, Jacek Sapa, Marek Bednarski, Barbara Filipek, more

European Journal of Pharmacology > 2014 > 738 > C > 14-21

A series of aminoalkanolic derivatives of xanthone with high affinity for β₁-adrenoceptors was evaluated for antiarrhythmic activity in the model of ischemia-reperfusion in isolated hearts, as well as in barium chloride- and adrenaline-induced model of arrhythmia. In order to better understand biological activity of studied compounds, the influence on β₂-adrenoceptors in guinea-pig trachea and vasorelaxant...

article

Antiarrhythmic, hypotensive and α1-adrenolytic properties of new 2-methoxyphenylpiperazine derivatives of xanthone

Anna Rapacz, Karolina Pytka, Jacek Sapa, Monika Kubacka, more

European Journal of Pharmacology > 2014 > 735 > Complete > 10-16

The main goal of this study was to assess antiarrhythmic and hypotensive activity of new 2-methoxyphenylpiperazine derivatives of xanthone. In order to better understand mechanism of action of studied compounds, their abilities to antagonize the increase in blood pressure elicited by adrenaline, noradrenaline and methoxamine, as well as the antagonistic properties for α ₁ -adrenoceptors on...

article

MH-3: evidence for non-competitive antagonism towards the low-affinity site of β₁-adrenoceptors

Eberhard Schlicker, Anna Pędzińska-Betiuk, Hanna Kozłowska, Natalia Szkaradek, more

Naunyn-Schmiedeberg's Archives of Pharmacology > 2014 > 387 > 8 > 743-752

β-Adrenoceptor antagonists are important drugs for the treatment of cardiovascular diseases and some of those drugs also block the so-called low-affinity site of β₁-adrenoceptors although at much higher concentrations. This low-affinity site, also identified in vivo and in human tissue, may come into play under certain pathophysiological situations including arrhythmias. The aim of our study was to...

article

Anticonvulsant evaluation of aminoalkanol derivatives of 2- and 4-methylxanthone

Natalia Szkaradek, Agnieszka Gunia, Anna M. Waszkielewicz, Lucyna Antkiewicz-Michaluk, more

Bioorganic & Medicinal Chemistry > 2013 > 21 > 5 > 1190-1198

A series of 17 new aminoalkanol derivatives of 6-methoxy- or 7-chloro-2-methylxanthone as well as 6-methoxy-4-methylxanthone was synthesized and evaluated for anticonvulsant activity. All compounds were verified in mice after intraperitoneal (ip) administration in maximal electroshock (MES) and subcutaneous pentetrazole (scMet) induced seizures as well as neurotoxicity assessment. Eleven of the tested...

article

Synthesis and preliminary evaluation of pharmacological properties of some piperazine derivatives of xanthone

Natalia Szkaradek, Anna Rapacz, Karolina Pytka, Barbara Filipek, more

Bioorganic & Medicinal Chemistry > 2013 > 21 > 2 > 514-522

A series of 9 piperazine derivatives of xanthone were synthesized and evaluated for cardiovascular activity. The following pharmacological experiments were conducted: the binding affinity for adrenoceptors, the influence on the normal electrocardiogram, the effect on the arterial blood pressure and prophylactic antiarrhythmic activity in adrenaline induced model of arrhythmia (rats, iv). Three compounds...

article

The study of the lipophilicity of some aminoalkanol derivatives with anticonvulsant activity

Anna Waszkielewicz, Natalia Szkaradek, Elżbieta Pękala, Fabiola Galzarano, more

Biomedical Chromatography > 24 > 12 > 1365 - 1372

A series of new (phenoxyethyl)aminoalkanol derivatives were synthesized and evaluated for their anticonvulsant activity. The most promising compound seemed to be (R,S)‐1N‐[(2,6‐dimethyl)phenoxyethyl]amino‐2‐butanol, which displayed anti‐MES activity (in mice, i.p.) with protective index (TD₅₀/ED₅₀) of 5.712, corresponding to that of phenytoin (6.6), carbamazepine (4.9) and valproate (1.7). The lipophilicity...

article

Preliminary evaluation of pharmacological properties of some xanthone derivatives

Henryk Marona, Natalia Szkaradek, Anna Rapacz, Barbara Filipek, more

Bioorganic & Medicinal Chemistry > 2009 > 17 > 3 > 1345-1352

A series of xanthone derivatives were synthesized and examined for electrocardiographic, antiarrhythmic, hypotensive and anticonvulsant activities as well as for α ₁ - and β ₁ -adrenergic binding affinities. Among the investigated compounds, some of them exhibited significant antiarrhythmic and/or hypotensive activity. The data obtained via receptor binding assay are in agreement with...

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