Celem niniejszej pracy było zbadanie aktywności przeciwbakteryjnej i przeciwgrzybicznej czwartorzędowych N-metylopochodnych laurynianu 2-dimetyloaminoetylowego z różnymi przeciwjonami. Testowane preparaty przejawiały aktywność w zakresie stężeń 0.5- 0.02% w stosunku do wybranych szczepów Gram-(-) - Klebsiella, E.coli, Proteus, Pseudomonas i Gram-(+) Staphylococcus, Enterococcus, jak również niektórych przedstawicieli rodzaju Candida. Badane preparaty w stężeniu 0.5 i 0.25% wykazywały właściwości bójcze w odniesieniu do wszystkich szczepów. Uzyskane wyniki potwierdzają słuszność wyboru czwartorzędowych soli amoniowych jako efektywnych środków dezynfekcyjnych.
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The aim of present study was to assay antibacterial and antifungal activity of quaternary ammonium salts-DM-11C1(-), DM-11Br(-), DM-11 CH3SO4(-)(N-methyl quaternary derivatives of 2-dimethylaminoethyl laurate with different counterions). The tested antimicrobial agents at the concentration of 0.5-0.02% were found to inhibit the growth of some Gram-negative bacteria - Klebsiella, E.coli, Proteus, Pseudomonas, Gram-positive strains Staphylococcus, Enterococcus and some representatives of yeast-Candida. The investigated compounds at the concentration 0.5 and 0.25% were active against all tested microorganisms. These results may have significant implications for the future development of new group quaternary ammonium compounds as an antimicrobial agents-disinfectants. s. 241-244, bibliogr. 4 poz.
Polyether ionophore antibiotics (ionophores) represent a large group of naturally- occurring lipid-soluble compounds isolated from actinomycetes strains of Streptomyces genus. Ionophores are able to form complexes with the metal cations, especially sodium and potassium, and transport them across the lipid membranes according to electroneutral or electrogenic transport mechanism. This process disturbs the intercellular Na+/K+ concentration gradient and intracellular pH, leads to the mitochondrial injuries, cell swelling, vacuolization and finally to programmed cell death (apoptosis). For this reason, ionophore antibiotics found commercial use in veterinary medicine as coccidiostatic agents and non-hormonal growth promoters. In addition to the industrial use of ionophores, some of them effectively and selectively inhibit properties of different cancer cells as well as enhance the anti-cancer effects of radio- and/or chemotherapy. In this group, particularly interesting is salinomycin because of its potent anti-microbial and anti-cancer activity, including efficiency against multi-drug resistant cancer cells and cancer stem cells. A very interesting direction of research is the chemical modification of ionophore antibiotics, which can lead to obtaining various derivatives with better biological activity and lower toxicity than those of the starting substances. Because biological activity of ionophore antibiotics and their derivatives is strictly connected with the ability to form characteristic pseudocyclic structures around the complexed cations (host-guest complex), it is also important to establish the detailed information on these structures. In this context, our review article is focused on the possible role of salinomycin and its derivatives in anti-microbial as well as anti-cancer therapy, and gives an overview of the properties of this antibiotic.
W pracy przedstawiono wyniki badań uwalniania fluoru, chropowatości powierzchni i aktywności antybakteryjnej wypełnień stomatologicznych. Badaniom poddano dwa handlowe materiały: cement szkłojonomerowy Fuji IX i kompozyt modyfikowany polikwasem Dyract AP. Uwalnianie jonów fluorkowych mierzono metodą potencjometrii bezpośredniej. Aktywność antybakteryjną oceniano przy wykorzystaniu procesu dyfuzji w podłożu agarowym. Analizowano topografię powierzchni materiałów przy pomocy elektronowego mikroskopu skaningowego.
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This work present results of research of fluoride release, surface roughness and antibacterial activity of dental materials. Two commercial restorative materials were investigated: glassionomer cement Fuji IX and polyacid-modified composite resin Dyract AP. Fluoride release was measured using direct potentiometry method. The antibacterial activity was evaluated with agar diffusion test. The topography of materials surface was observed using electron scanning microscope.
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Purpose: In this work our aim was to reveal the relationship between sodium alginate concentration and crosslinking level, also the ratio of release of the antibacterial additives: silver nanoparticles and metronidazole. Moreover, we examine obtained hydrogel as a potential dressing material for regenerative medicine. Design/methodology/approach: In the research specimens of hydrogels were tested to define their mechanical and physicochemical properties like antibacterial activity against gramnegative Escherichia coli and gram-positive Staphylococcus aureus, viscosity and conductivity. Findings: The concentration of alginate and presence of antibacterial additives influence on the crosslinking level. Mechanical properties of hydrogels are similar to human skin. Only hydrogels with addition of metronidazole and AgNP inhibits bacteria growth after 18 h. In case of gram-negative Escherichia coli both of the aseptic additives inhibits bacteria growth, but sodium alginate hydrogel with silver nanoparticles gives better results in tests with grampositive Staphylococcus aureus . Research limitations/implications: The presence of metronidazole in hydrogel, especially its incorporation and binding with mannuronic and guluronic acid residues must be clarified in more advanced research. Practical implications: Obtained results shows that sodium alginate hydrogels with 0.1mg/ml of alginate, due to its properties are proper as a dressing material. Based on the results, and more advanced tests with metronidazole, we can consider dressing design. Originality/value: Unique value of this work is that we completed the gap in knowledge about the relation of crosslinking level and mechanical properties with are crucial to proper tissue healing and addition of popular aseptic agents.
This chapter reviews the research on antibacterial functionalization of textiles with inorganic nanoparticles (Ag, MgO, Al2O3) by the sonochemical method. Sonochemistry is one of the most efficient techniques for the synthesis of nanosized materials, wherein ultrasonic waves in the frequency range of 20 kHz to 1 MHz serve as a driving force for chemical reactions. Sonochemical reactions are dependent on acoustic cavitation: the formation, growth, and explosive collapse of bubbles in irradiated liquids. Extreme conditions are developed when the bubbles collapse (temperature >5000 K, pressure >1000 atm, and cooling rates >109 K/sec), resulting in the breaking and forming of chemical bonds. The deposition of nanoparticles on the surface of natural and synthetic yarns and fabrics (wool, cotton, nylon, polyester) may be achieved using ultrasound irradiation. This process produces a uniform coating of nanoparticles on the textile surface with different functional groups. The coating can be performed by an in situ process, where the nanoparticles are formed and immediately propelled to the surface of the fabric. This approach was demonstrated with nanosilver. Alternatively, the sonochemical process can be used as a "throwing stone" technique, where previously synthesized nanoparticles are sonicated in the presence of the fabric. This process was shown with MgO and Al2O3 nanoparticles, which were propelled to the surface by microjets and adhered strongly to the textile without any additional binder. This phenomenon was explained because of the local melting of the substrate due to the high rate and temperature of nanoparticles propelled at the solid surface by sonochemical microjets. The activity of the fabric finishing with antibacterial nanoparticles was tested against Gram-negative and Gram-positive bacteria cultures. A significant bactericidal effect was demonstrated in both cases, even at a low concentration, below 1 wt.% of nanoparticles in the fabric.
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Dokonano przeglądu badań nad funkcjonalizacją antybakteryjną wyrobów włókienniczych nanocząsteczkami nieorganicznymi (Ag, MgO, Al2O3 ) metodą sonochemiczną. Sonochemia jest jedną z najskuteczniejszych technik syntezy nanomateriałów, w której fale ultradźwiękowe w zakresie częstotliwości od 20 kHz do 1 MHz służą jako siła napędowa dla reakcji chemicznych. Reakcje sonochemiczne są zależne od kawitacji akustycznej: powstawania, wzrostu i wybuchowego rozpadu pęcherzyków w napromieniowanych cieczach. Ekstremalne warunki powstają, gdy pęcherzyki zapadają się (temperatura > 5000 K, ciśnienie > 1000 atm, szybkość chłodzenia > 109 K/s), powodując pękanie i tworzenie wiązań chemicznych. Osadzanie nanocząsteczek na powierzchni przędz i tkanin naturalnych i syntetycznych (wełna, bawełna, nylon, poliester) można uzyskać za pomocą napromieniowania ultradźwiękowego. W tym procesie uzyskuje się jednolitą powłokę nanocząsteczek na powierzchni tkaniny z różnymi grupami funkcyjnymi. Powłokę można prowadzić w procesie in situ, w którym nanocząsteczki są formowane i natychmiast wyrzucane na powierzchnię tkaniny. To podejście zostało wykazane z nanosrebrem. Alternatywnie, proces sonochemiczny może być stosowany jako technika „rzucania kamieniami”, w którym wcześniej zsyntetyzowane nanocząsteczki są sonikowane w obecności tkaniny. Proces ten został przedstawiony za pomocą nanocząsteczek MgO i Al2O3, które zostały wyrzucone na powierzchnię za pomocą mikrodysz i silnie przylegały do tkaniny bez dodatkowego spoiwa. Zjawisko to tłumaczy się miejscowym topnieniem podłoża z powodu wysokiej szybkości i temperatury nanocząsteczek wyrzucanych na powierzchnię stałą przez sonochemiczne mikrodysze. Aktywność tkaniny wykończonej nanocząsteczkami przeciwbakteryjnymi badano na kulturach bakterii Gram-ujemnych i Gram-dodatnich. Znaczące działanie bakteriobójcze wykazano w obu przypadkach, nawet w niskim stężeniu, poniżej 1% wag. nanocząsteczek w tkaninie.
Polyether ionophore antibiotics (ionophores) represent a large group of naturally- occurring lipophilic compounds which are able to form complexes with the metal cations and transport them across the lipid membranes. This process disturbs the intercellular Na+/K+ concentration gradient and intracellular pH, and leads to the mitochondrial damages, cell swelling, vacuolization and finally to apoptosis process. For this reason, ionophores are commonly used in veterinary medicine as the non-hormonal growth-promoting as well as coccidiostatic agents. In this group particularly interesting are monensin and salinomycin (Fig. 1) because of their proved anti-tumour activity, including efficiency against multidrug- -resistant cancer cells and cancer stem cells of different origin. Improved synthetic derivatives of both polyether ionophores are thus of considerable current interest. Selective derivatization of these structures whose display multiple reactive functional groups and, in the case of salinomycin, a sensitive tricyclic spiroketal ring system is however non-trivial. Even so, semi-synthetic analogs reported to date includes i.a. selective derivatization of the carboxyl group, the three hydroxyl groups, the ketone group, the alkene, and epimerization of the characteristic tricyclic salinomycin unit (for more details see: M. Antoszczak, A. Huczyński, B. Brzezinski, Wiad. Chem., 2017, 71, 629). On the other hand, as part of the original program to develop innovatory anti- -cancer pro-drugs and prompted by the idea that cancer cells may be individually effectively killed by monensin and salinomycin, a very interesting direction of research is bioconjugation of these ionophores. In this context, our review article is focused on the possible role of hybrids of both ionophore antibiotics with other biologically active substances (natural amino acids, Cinchona alkaloids, flavonoids, nucleosides) in anti-bacterial and anti-cancer treatment, and gives an overview of their properties.
Millipedes as saprophagous epigeic fauna members are involved in the decomposition of organic debris. Diplopod’s activity improve circulation of nutrients, elements and accelerate environmental reclamation. Beyond mentioned above Diplopoda can provoke sanitary and epidemiological threats especially during swarming or seasonal migrations activities. Considering following aspects: contact with defensive secretions, pseudo-parasitic activity that imitates helminthiasis or passive transmission of pathogens, we can discuss direct or distant effects on human health. Education and proper prophylactic remain neglected. Variety of substances from millipedes are checked for their medical action: direct body extracts and active chemical components from defensive secretion. Millipedes may serve as source for zoo-pharmacology and zoo-indication development. This issue review shows that both pros and cons of the Diplopod’s influences should be considered. Literature was carried out from middle of 20th century article till recent papers. The nowadays literature were found in Google Scholar, PubMed, Medline search base.
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Krocionogi jako przedstawiciele saprofagów w faunie epigeicznej odpowiadają za dekompozycję pozostałości organicznych. Aktywność dwuparców poprawia cyrkulację składników odżywczych, pierwiastków i wzmaga proces rekultywacji środowiska. Poza wyżej wymienionymi Diplopoda powodują zagrożenia sanitarne i epidemiologiczne szczególnie podczas masowych pojawów i migracji. Biorąc od uwagę następujące aspekty: kontakt z sekrecjami obronnymi, aktowość pseudo-pasożytniczą, która imituje robaczyce oraz bierną transmisję patogenów możemy mówić o bezpośrednim i odległym wpływie na ludzkie zdrowie. W zakresie edukacji i profilaktyki pozostaje nadal wiele do uzupełnienia. Różne substancje pozyskiwane z krocionogów są testowane ze względu na ich medyczne właściwości; bezpośrednie wydzieliny, płyny i fragmenty ciała oraz aktywne związki z sekrecji obronnych. Krocionogi mogą posłużyć jako źródło rozwoju zoo-farmakognozji i zoo-indykacji. Zaprezentowany przegląd zagadnień sugeruje zarówno pozytywy jak i negatywne aspekty znaczenia grupy. Zebrano literaturę z połowy dwudziestego wieku oraz współczesną. W przypadku najnowszych doniesień korzystano z baz danych Google Scholar, PubMed, Medline.
Recently, 1,2,3-triazoles have gained an increased attention in the field of drug discovery because several derivatives have already been marketed as medications (e.g. tazobactam, cefatrizine, rufinamide) [1, 2] and many of them appeared to be very active in diverse biological studies including plinambulin 69 currently in the last stage of the clinical trials [60]. In this review very recent investigations of antibacterial, antitubercular, antifungal, antipsychotic, antiepileptic, anti-inflammatory, hypoglycemic, anticancer and antiviral properties of 1,2,3-triazole derivatives are discussed. These studies allowed to select several compounds which were found to be more active in comparison to the already used drugs.
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Garlic (Allium sativum) has historically been one of the most common vegetables to serve as a both spice and medical herb in many countries. One of the outstanding features of the chemical composition of garlic is the large amount of unique organosulfur compounds, which provide its characteristic flavor and odor and most of its potent biological activity. Two classes of primary organosulfur compounds are found in whole garlic cloves: γ-glutamyl-S-alk(en)yl-L-cysteines and S-alk(en)yl-L-cysteine sulfoxides (alliin, metiin, propiin, isallin) (Fig. 1, 2) [5-15]. When garlic is crushed or cut, S-alk(en)yl--L-cysteine sulfoxides are exposed to the enzyme alliinase and thiosulfinates, via intermediate sulfenic acids are formed (Fig. 6) [29-33]. The major thiosulfinate, allicin is a reactive intermediate species that can be transformed, into a variety of compounds including diallyl, methyl allyl and mono- di-, tri-, tetrasulfides, vinyldithiins and ajoenes (Fig. 7-9) [37-49]. Garlic belongs to the Allium species, which accumulate only fructans as their nonstructural carbohydrates [52-59]. Garlic is also known for its production of some unique furostanol saponins, e.g. proto-eruboside-B and sativoside-B1 (Fig. 10-12) [60-63]. The Allium species also contain high levels of flavonides, including apigenin, myricetin and quercetin (Fig. 13) [64, 65], moderate levels of vitamins as well as free amino acids (Arg, Gln, Asn, Glu, and Lys) [66-69]. It was found that the amino acid fraction of Aged Garlic Extract (AGE) contain Maillard reaction products, N-fructosyl glutamine (Fru-Glu), Nα-(1-deoxy-D-fructos-1-yl)-L-arginine (Fru-Arg) (Fig. 14, 15) [74-76], as well as tetrahydro-?-carboline derivatives (Fig. 16, 17) [77-82]. Recently, allixin (Fig. 18), a novel phytoalexin, with the structure 4H-pyran-4-one, as a novel substance with neurotrophic activity has been reported to by synthesized by garlic [83-85]. Garlic has the ability to accumulate the selenium from soil and the major selenium compound in both Se-enriched and unenriched garlic was identified as γ-glutamyl-Se-methyl selenocysteine along with lesser amounts of Se-methyl selenocysteine, selenocysteine, selenomethionine among other compounds (Fig. 19) [86-96]. Pharmacological investigations have shown that garlic has a wide spectrum of actions, not only it is antimicrobial [97], but it also has beneficial effects in regard to cardiovascular and cancer diseases [2, 3, 14, 42]. A number of organosulfur substances derived from garlic such as allicin, allicin-derived organosulfur compounds including sulfides, ajoene, steroidal saponins, flavonides, Fru-Arg, Fru-Glu, organic seleno-compounds and tetrahydro-?-carboline derivatives have been found to have strong antioxidant properties. It has been suggested that garlic can prevent cardiovascular disease, inhibit platelet aggregation, decrease the synthesis of cholesterol and prevent cancer. Thus it may either prevent or delay chronic diseases associated with aging.
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