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Naturalne i syntetyczne pochodne 5,8-chinolinodionu wykazujące aktywność biologiczną

Kadela-Tomanek M., Chrobak E., Bębenek E., Boryczka S.

Wiadomości Chemiczne

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2017

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[Z] 71, 11-12

795--815

EN

The compounds produced by a living organisms are most commonly used as medicinal agents and starting materials to the preparation of new semi-synthetic derivatives. It is estimated that over 23% of currently used medicinal products are natural substances. Natural compounds and their semisynthetic derivatives are most often used in the treatment of cancer and the treatment of infectious diseases. One of the groups of compounds obtained from Gram-positive bacterium are 5,8-quinolinedione antibiotics, like: streptonigrin, lavendamycin and streptonigron. The all compounds exhibit high anticancer, antimicrobial and antiviral activity. Unfortunately due to high toxicity this alkaloids did not find place in the therapy. The mechanism of action depends on interaction of compounds with the nicotinamide quinone oxidoreductase 1 (NQO1). The 5,8-quinolinedione can be reduced by the NAD(P)H as a cofactor to form the semiquinone or hydroquinone intermediates. These compounds can react with oxygen yielding a regenerated 5,8-quinolinedione fragment and creating the hydroxyl radicals, which are ultimately responsible for the DNA strands cleavage. The structure–activity relationship study has shown that the most important part of the molecule is the 5,8-quinolinedione moiety. Furthermore, it was found, that the introduction of amine, hydroxyl or thiol substituents at position 6 or 7 of the 5,8-quinolinedione moiety results in an enhanced biological activity. A lot of synthetic derivatives of 5,8-quinolinediones which containing amine, alkoxyl and thiol groups at the C-6 or/and C-7 positions have been obtained during the last few years. Commonly this compounds are obtained in the reaction of 6,7-dichloro-5,8-quinolinedione with nucleophilic factor. Depending on the reaction conditions, mono- or di-substituted derivatives are obtained. Most of synthesized compounds exhibit high biological activity, like: anticancer, antibacterial, antiviral, anti-inflammatory.

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Aktywność biologiczna związków acetylenowych pochodzenia naturalnego

Kadela-Tomanek M., Chrobak E., Bębenek E., Lubczyńska A., Siudak S., Wójcik A., Otulakowska A.

Wiadomości Chemiczne

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2016

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[Z] 70, 9-10

613--632

EN

The natural acetylenic products containing at least one a carbon-carbon triple bond, are important class of compounds widely distributed in the environment. Development of spectroscopic techniques and methods for the isolation of metabolites allowed the extraction of natural acetylenic compounds. The most of these substances have been obtained from marine organisms, such as: cyanobacteria, algae and sponges. The next source of metabolites are herbal plants, which were used in the Chinese traditional medicine. A many of them show interesting biological activity. The first isolated natural compound possessing an acetylenic unit was dehydromatricaria ester, which was obtained from rhizome European goldenrod (Solidago virgaurea). To present day have been found and researched more than 2000 natural acetylenic metabolites. Due to the chemical structure, natural acetylenic compounds were divided into six groups: peptides, aromatic compounds, enediyne antibiotics, sterols, carotenoids, and poliacetylenic compounds . This article focuses natural acetylenic substances, which exhibit interesting biological properties, particularly anticancer ones. The review presents many of such metabolites, including fatty alcohols, ketones, acids, ethers, and carotenoids.

3

Eliminacja clostridium perfringens podczas kondycjonowania osadu czynnego nadmiernego

Grűbel K, Chrobak E, Rusin A, Machnicka A.

Inżynieria Ekologiczna

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2013

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Nr 32

40--47

PL

Praca przedstawia możliwość eliminacji Clostridium perfringens w procesie kondycjonowania osadu czynnego nadmiernego z wykorzystaniem promieniowania mikrofalowego. Na podstawie wyników badań stwierdzono, że promieniowanie mikrofalowe (700W i 900W) wykazuje dezintegrujące działanie wyrażone wzrostem wartości ChZT w cieczy nadosadowej: 12 krotny wzrost wartości ChZT przy mocy 700W i 13 krotny przy mocy promieniowania 900W. Fala elektromagnetyczna przyczyniła się do częściowej higienizacji osadu. Spowodowała redukcję liczby Clostridium perfringens odpowiednio o 52% i 56% w czasie 120s oddziaływania, przy mocy 700W i 900W. Redukcja ogólnej liczby bakterii pod wpływem mikrofal wyniosła 42% i 51% (odpowiednio dla 700W i 900W), a pałeczek z rodziny Enterobacteriaceae od 54% do 70% w zależności od mocy promieniowania, czasu działania i własności biochemicznej.

EN

The work presents the possibility of elimination of Clostridium perfringens in surplus activated sludge handling by microwave radiation. An assessment of the impact of microwave radiation as a disintegration and higienisation method of surplus activated sludge was based on an analysis of the value of COD and changes in population of the bacteria Clostridium perfringens and overall sticks in the family Enterobacteriaceae. Basis on the results of the research was concluded that microwave radiation (700W and 900W) shows disintegration action expressed in COD value in the supernatant increase: 12 times increase value of COD with power 700W and 13 times for 900W radiation power. Electromagnetic wave contributed to partial higienisation of surplus activated sludge. The number of Clostridium perfringens decrease about 52% and 56% during the 120s of higienisation process with power 700W and 900W, respectively. Reduction of the overall number of bacteria under the influence of microwave radiation was 42% and 51% (respectively for 700W and 900W), and sticks from the family Enterobacteriaceae from 54% to 70% depending on the power of radiation, the time of operation and biochemical properties

4

Microstructure, magnetic and elastic properties of electrodeposited Cu+Ni nanocomposites coatings

Chrobak A., Kubisztal M., Kubisztal J., Chrobak E, Haneczok G.

Journal of Achievements in Materials and Manufacturing Engineering

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2011

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Vol. 49, nr 1

17--26

EN

Purpose: The paper presents systematic studies of fabrication and properties of Cu+Ni nanocomposite coatings obtained by electrodeposition technique. Special attention is paid to establish the influence of fabrication conditions and microstructure of the coating material on its magnetic and elastic properties. Design/methodology/approach: The results were obtained by applying electrochemical impedance spectroscopy (EIS, PARSTAT 2273, roughness factor), magnetization versus temperature measurements (2

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Lipophilicity indexes of some 3-alkylthio and 3-alkylsulfinyl 4(1H)-quinolones

Rudnik M., Chrobak E., Maślankiewicz M. J.

Acta Chromatographica

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2003

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No. 13

243-247

EN

RPTLC retention characteristics have been determined for two series of 1-alkyl-4(1H)-quinolinones with 3-alkylthio and 3-alkylsulfinyl groups. Experimentally obtained measures of lipophilicity, expressed as RM0 values, were compared with values of log P calculated by a computational method.