111 research outputs found

    Dvojni lijekovi primakina i nesteroidnih protuupalnih lijekova: Sinteza, hvatanje slobodnih radikala, antioksidativno djelovanje i keliranje Fe2+ iona

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    Novel primaquine conjugates with non-steroidal anti-inflammatory drugs (PQ-NSAIDs, 4a-h) were prepared, fully chemically characterized and screened for radical scavenging and antioxidant activities. The synthetic procedure leading to twin drugs 4a-h involved two steps: i) preparation of NSAID benzotriazolides 3a-h from the corresponding NSAID (ibuprofen, ketoprofen, fenoprofen, ketoprofen hydroxy and methylene analogues, diclofenac or indomethacin) and benzotriazole carboxylic acid chloride (BtCOCl, 1), ii) reaction of intermediates 3a-h with PQ. The prepared PQ-NSAIDs exerted moderate activities in the DPPH free radical test and -carotene-linoleic acid assay. Moreover, ketoprofen derivatives 4d and 4b demonstrated a notable Fe2+ chelating ability as well. On the other hand, negligible antiproliferative and antituberculotic effects of conjugates 4a-h were observed.U radu je opisana sinteza novih konjugata primakina s nesteroidnim protuupalnim lijekovima (PQ-NSAIDs, 4a-h), njihova potpuna karakterizacija te testiranje sposobnosti hvatanja slobodnih radikala i antioksidativnog djelovanja. Sintetski postupak za pripravu dvojnih lijekova 4a-h uključuje dva koraka: i) pripravu NSAID-benzotriazolida 3a-h iz odgovarajućih nesteroidnih protuupalnih lijekova (ibuprofena, ketoprofena, fenoprofena, hidroksi i metilenskih analoga ketoprofena, diklofenaka i indometacina) i klorida 1-benzotriazol karboksilne kiseline (BtCOCl, 1), ii) reakciju intermedijera 3a-h s primakinom. Novi PQ-NSAID konjugati pokazuju umjerenu sposobnost hvatanja slobodnih radikala u DPPH testu te umjereno antioksidativno djelovanje u pokusu s -karotenom i linoleinskom kiselinom. Osim toga, derivati ketoprofena 4d i 4b imaju primjetnu sposobnost keliranja Fe2+ iona. Svi konjugati 4a-h pokazuju vrlo slabo antiproliferativno i antituberkulotsko djelovanje

    Antioxidant, antimicrobial and anticancer activity of the lichens Cladonia furcata, Lecanora atra and Lecanora muralis

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    <p>Abstract</p> <p>Background</p> <p>The aim of this study is to investigate in vitro antioxidant, antimicrobial and anticancer activity of the acetone extracts of the lichens <it>Cladonia furcata, Lecanora atra </it>and <it>Lecanora muralis</it>.</p> <p>Methods</p> <p>Antioxidant activity was evaluated by five separate methods: free radical scavenging, superoxide anion radical scavenging, reducing power, determination of total phenolic compounds and determination of total flavonoid content. The antimicrobial activity was estimated by determination of the minimal inhibitory concentration by the broth microdilution method against six species of bacteria and ten species of fungi. Anticancer activity was tested against FemX (human melanoma) and LS174 (human colon carcinoma) cell lines using MTT method.</p> <p>Results</p> <p>Of the lichens tested, <it>Lecanora atra </it>had largest free radical scavenging activity (94.7% inhibition), which was greater than the standard antioxidants. Moreover, the tested extracts had effective reducing power and superoxide anion radical scavenging. The strong relationships between total phenolic and flavonoid contents and the antioxidant effect of tested extracts were observed. Extract of <it>Cladonia furcata </it>was the most active antimicrobial agent with minimum inhibitory concentration values ranging from 0.78 to 25 mg/mL. All extracts were found to be strong anticancer activity toward both cell lines with IC<sub>50 </sub>values ranging from 8.51 to 40.22 μg/mL.</p> <p>Conclusions</p> <p>The present study shows that tested lichen extracts demonstrated a strong antioxidant, antimicrobial and anticancer effects. That suggest that lichens may be used as as possible natural antioxidant, antimicrobial and anticancer agents to control various human, animal and plant diseases.</p

    Організаційно-економічне забезпечення розвитку електронної промисловості

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    Розкрито питання організаційно-економічного забезпечення електронної промисловості в рамках організаційно-економічного механізму розвитку електронної промисловості на інноваційній основі, який регламентує діяльність державних, галузевих і підприємницьких структур, що забезпечують розвиток електронної промисловості. Ключові слова: електронна промисловість, організаційне забезпечення розвитку електронної промисловості, організаційно-економічний механізм, інноваційний розвиток.  Раскрываются вопросы организационно-экономического обеспечения электронной промышленности в рамках организационно-экономического механизма развития электронной промышленности на инновационной основе, который регламентирует деятельность государственных, отраслевых и предпринимательских структур, обеспечивающих развитие электронной промышленности. Ключевые слова: электронная промышленность, организационное обеспечение развития электронной промышленности, организационно-экономический механизм, инновационное развитие.  The paper deals with the issues of organizational and economic support of electronic industry in the framework of the organizational and economic mechanism of the above industry development on the basis of innovation. It regulates the activities of the government, sectoral and business organizations, which provide the development of the electronic industry. The proposalsare as follows: to work out a State Program of Development of the Electronic Industry, andto create a sectoral information system, a cluster “development of the electronic industry”, holding the electronic industry, a sectoral technology transfer system, training educational and scientific centres for the engineering staff. It is shown that at a corporate level the development of electronic industry is promoted by establishment of production facilities with the use of well-known brands and foreign electronic productions, technologies transfer with consideration of supply channels, introduction of business market mechanisms, IPC standards, and production information systems PDM/PLM. A specific feature of these measures is that to develop the issues of financial and economic, technical and technological, innovation and market support of the electronic industry development the methods of grouping, generalization of economic indicators received from the enterprises of this industry, and economic mathematical modelling using a correlation regression and structural logical analysis have been used. The application of these methods suggests that the use of the organizational and economic support contributes to promising development of the electronic industry in Ukraine which consists in formation of the core of the electronic industry and its integration in the world electronic space in the future. Keywords: electronic industry, organizational support of electronic industry development, organizational and economic mechanism, innovation-based development

    Isolation of an Antibacterial Flavonoid Glycoside from the Leaves of Cineraria abyssinica

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    The leaf extract of Cineraria abyssinica Sch. Bip. exA. Rich (Asteraceae) is locally used for the treatment of various ailments including diarrhoea. Previous study has shown that the total hydroalcoholic extract of the leaves of the plant possesses genuine antibacterial activity. The main aim of this study was, therefore, to determine the active principle(s) of the plant. Thus, chloroform, acetone and methanol fractions of the leaves of C. abyssinica were prepared and investigated for their in vitro antibacterial activities against 21 Gram-positive and Gram-negative bacterial strains by agar disc diffusion method. It was found that all the fractions possess various degrees of antimicrobial activities against most of the bacteria tested. Among the bacterial strains tested Bacillus species were less sensitive. Bioactivity-guided fractionation of the most active methanol fraction resulted in the isolation of the flavonoidal glycoside, rutin the structure of which was assigned on the basis of spectroscopic methods. Rutin showed potent antibacterial activity against the majority of the tested bacteria which was comparable to that of the standard drug ciprofloxacin. Therefore, the present study revealed for the first time the presence of an antimicrobial phytochemical in the leaves of C. abyssinica that scientifically validated the traditional use and its potential for the treatment of infectious diarrhoea.Keywords: Cineraria abyssinica, Asteraceae, antibacterial, agar diffusion, ruti

    Essential Oil of Otostegia integrifolia Benth: Composition, Antimicrobial and Antioxidant Activities

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    Composition, antioxidant and antimicrobial activities of the essential oil of Otostegia integrifolia Benth. were studied. GC/MS analyses revealed the presence of 37 constituents representing 84.88% of the oil with α- pinene (31.33%), 1-octen-3-ol (11.78%) and trans-caryophyllene (11.35%) constituting more than 50% of its components. When tested for its antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl (DPPH), the oil reduced DPPH in a concentration dependent manner with an EC50 value of 5.32 μl/ml. Similarly, the oil was shown to possess strong and broad spectrum antimicrobial activity against several Gram-positive and Gram -negative bacterial strains as well as fungal pathogens. The minimum inhibitory concentration (MIC) of the oil ranged from 5 to 100 μg/ml and 50 to 100 μg/ml against the bacterial and fungal strains tested, respectively. The oil (MIC=5 μg/ml) was found to be more potent than ciprofloxacin (MIC=10 μg/ml) against some E. coli strains. The antifungal activity of the oil was either comparable to or better than griseofulvin against most of the fungal pathogens tested. The study provides evidence for an excellent broadspectrum antimicrobial and significant antioxidant activity of O. integrifolia essential oil, a possible explanation for the traditional use of the plant.Keywords: essential oil, Otostegia integrifolia, α-pinene, 2,2-diphenyl-1-picrylhydrazyl, antimicrobial activit
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