Imunita je důmyslný systém. Imunitní paměť může při správném průběhu trvat desítky let či celý život a významně ovlivňuje naše zdraví a život. Dobře fungující imunitní systém přináší organizmu zdraví a vitalitu ve formě odolnosti i při kontaktu se zákeřným protivníkem jak z řad zevních činitelů, tak vlastních buněk. Betaglukany jsou látky přírodního původu, které umí aktivovat buňky imunitního systému, tedy podpoří tělo v tom, aby si bylo schopno samo pomoci, což je vždy velmi efektivní, a navíc bez vedlejších účinků. Nedoporučují se pouze u pacientů, u kterých není žádoucí zvyšovat a podporovat imunitní procesy. Jsou celosvětově doporučovány jako základní či doplňková léčba zánětů, nádorů, diabetu, hypercholesterolemie a dalších onemocnění.
Immunity is a sophisticated system, including immune memory, which can last for decades or a lifetime if it works correctly and significantly affects our health and therefore life. A well-functioning immune system brings health and vitality to the body in the form of resistance even when in contact with an insidious enemy, both from external agents and from its own cells. Betaglucans are of natural origin and can activate the cells of the immune system, so they support the body in helping itself, which is always very effective; moreover, they are without side effects. They are not recommended only in patients in whom it is not desirable to increase support of the immune processes. They are recommended worldwide as a basic or complementary treatment for inflammation, tumors, diabetes, hypercholesterolemia and other diseases.
Production of particles and their adaptation in the pharmacology became an object of interest, and they are the currently introduced therapies based on the use of micro and nanoparticles. The use of gold particles is not an exception. This review has focused on the application of gold micro and nanoparticles in pharmacology and biomedicine. The particles can be used for diagnosis respective theranostic of cancer, rheumatoid arthritis and as antimicrobial means. Besides these applications, specifications of gold, gold particles, and colloidal gold manufacturing and their comparison with the solid gold, are described as well. This review is based on a survey of actual scientific literature.
- MeSH
- antiflogistika chemie farmakologie MeSH
- antiinfekční látky chemie farmakologie MeSH
- antitumorózní látky chemie farmakologie MeSH
- Bacteria účinky léků MeSH
- biomedicínský výzkum MeSH
- houby účinky léků MeSH
- lidé MeSH
- nádory diagnóza farmakoterapie MeSH
- nanočástice chemie MeSH
- revmatoidní artritida diagnóza farmakoterapie MeSH
- zlato chemie farmakologie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
Cryptococcosis is an invasive infection that accounts for 15% of AIDS-related fatalities. Still, treating cryptococcosis remains a significant challenge due to the poor availability of effective antifungal therapies and emergence of drug resistance. Interestingly, protease inhibitor components of antiretroviral therapy regimens have shown some clinical benefits in these opportunistic infections. We investigated Major aspartyl peptidase 1 (May1), a secreted Cryptococcus neoformans protease, as a possible target for the development of drugs that act against both fungal and retroviral aspartyl proteases. Here, we describe the biochemical characterization of May1, present its high-resolution X-ray structure, and provide its substrate specificity analysis. Through combinatorial screening of 11,520 compounds, we identified a potent inhibitor of May1 and HIV protease. This dual-specificity inhibitor exhibits antifungal activity in yeast culture, low cytotoxicity, and low off-target activity against host proteases and could thus serve as a lead compound for further development of May1 and HIV protease inhibitors.
- MeSH
- antifungální látky chemie metabolismus farmakologie MeSH
- aspartátové proteasy antagonisté a inhibitory genetika metabolismus MeSH
- Cryptococcus neoformans enzymologie MeSH
- fungální proteiny antagonisté a inhibitory genetika metabolismus MeSH
- HIV-proteasa chemie metabolismus MeSH
- HIV enzymologie MeSH
- houby účinky léků MeSH
- katalytická doména MeSH
- krystalografie rentgenová MeSH
- preklinické hodnocení léčiv MeSH
- rekombinantní proteiny biosyntéza chemie izolace a purifikace MeSH
- simulace molekulární dynamiky MeSH
- substrátová specifita MeSH
- vazebná místa MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Research Support, N.I.H., Extramural MeSH
Hydrazide-hydrazones have been described as a scaffold with antimicrobial and cytotoxic activities as well as iodinated compounds. A resistance rate of bacterial and fungal pathogens has increased considerably. That is why we synthesized and screened twenty-two iodinated hydrazide-hydrazones 1 and 2, ten 1,2-diacylhydrazines 3 and their three reduced analogues 4 for their antibacterial, antifungal, and cytotoxic properties. Hydrazide-hydrazones were prepared by condensation of 4-substituted benzohydrazides with 2-/4-hydroxy-3,5-diiodobenzaldehydes, diacylhydrazines from identical benzohydrazides and 3,5-diiodosalicylic acid via its chloride. These compounds were investigated in vitro against eight bacterial and eight fungal strains. The derivatives were found potent antibacterial agents against Gram-positive cocci including methicillin-resistant Staphylococcus aureus with the lowest values of minimum inhibitory concentrations (MIC) of 7.81 μM. Four compounds inhibited also human pathogenic fungi (MIC of ≥1.95 μM). The derivatives had different degrees of cytotoxicity for HepG2 and HK-2 cell lines (IC50 values from 11.72 and 26.80 μM, respectively). Importantly, normal human cells exhibited lower sensitivity. The apoptotic effect was also investigated. In general, the presence of 3,5-diiodosalicylidene scaffold (compounds 1) is translated into enhanced both antimicrobial and cytotoxic properties whereas its 4-hydroxy isomers 2 share a low biological activity. N'-Benzoyl-2-hydroxy-3,5-diiodobenzohydrazides 3 have a non-homogeneous activity profile. Focusing on 4-substituted benzohydrazide part, the presence of an electron-withdrawing group (F, Cl, CF3, NO2) was found to be beneficial.
- MeSH
- antibakteriální látky chemie farmakologie MeSH
- antifungální látky chemie farmakologie MeSH
- antitumorózní látky chemie farmakologie MeSH
- Bacteria účinky léků MeSH
- buňky Hep G2 MeSH
- houby účinky léků MeSH
- hydraziny chemie MeSH
- hydrazony chemie MeSH
- lidé MeSH
- objevování léků MeSH
- viabilita buněk účinky léků MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
Fungal contamination in stored food grains is a global concern and affects food economics and human and animal health. It is clear that there is a need to develop new technologies with improved performances that are also eco-friendly in nature. Due to the bioactivity of essential oils (EOs) in the vapor phase, their low toxicity for humans, and their biodegradability and antifungal properties, EOs could be a suitable solution. In this study, we explored the potential of thyme, oregano, lemongrass, clove, and cajeput EOs in the vapor phase. For 17 days, inhibitory activity was assessed against five strains of postharvest pathogens-Aspergillus spp., Fusarium s. l. spp., and Penicilliumochrochloron-isolated from cereal grains. A modified disc volatilization method was used, which is more effective in comparison to traditional screening methods. Three concentrations were tested (250, 125, and 62.5 μL/L). The two highest concentrations resulted in complete inhibition of fungal growth; however, even 62.5 μL/L showed a significant antifungal effect. The efficiency of EOs followed this order: thyme > oregano > lemongrass > clove > cajeput. From our findings, it appears that the use of EOs vapors is a better option not only for laboratory experiments, but for subsequent practice.
With increasing numbers of patients needing intensive care or who are immunosuppressed, infections caused by moulds other than Aspergillus spp or Mucorales are increasing. Although antifungal prophylaxis has shown effectiveness in preventing many invasive fungal infections, selective pressure has caused an increase of breakthrough infections caused by Fusarium, Lomentospora, and Scedosporium species, as well as by dematiaceous moulds, Rasamsonia, Schizophyllum, Scopulariopsis, Paecilomyces, Penicillium, Talaromyces and Purpureocillium species. Guidance on the complex multidisciplinary management of infections caused by these pathogens has the potential to improve prognosis. Management routes depend on the availability of diagnostic and therapeutic options. The present recommendations are part of the One World-One Guideline initiative to incorporate regional differences in the epidemiology and management of rare mould infections. Experts from 24 countries contributed their knowledge and analysed published evidence on the diagnosis and treatment of rare mould infections. This consensus document intends to provide practical guidance in clinical decision making by engaging physicians and scientists involved in various aspects of clinical management. Moreover, we identify areas of uncertainty and constraints in optimising this management.
- MeSH
- houby účinky léků genetika izolace a purifikace fyziologie MeSH
- lidé MeSH
- management nemoci MeSH
- mykologie MeSH
- mykózy diagnóza farmakoterapie mikrobiologie MeSH
- směrnice pro lékařskou praxi jako téma MeSH
- společnosti lékařské MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
During our investigation on the endophytic fungi of Azadirachta indica, the strain YM 311593 was obtained from the fruit of the plant. The culture extract of the strain showed antifungal activities against four phytopathogenic fungi. Based on the morphological features and phylogenetic definition, the strain YM 311593 was identified as Paraconiothyrium sp. Four xanthones and one anthraquinone were obtained from the extract of the fermentation broth of the strain. They were characterized to be globosuxanthone A (1), vertixanthone (2), hydroxyvertixanthone (3), 3,8-dihydroxy-1-methy1-9H- xanthen-9-one (4), and danthron (5), respectively, by spectroscopic elucidation. Furthermore, the absolute configuration of 1 was deduced by X-ray diffraction analysis. Besides, compound 4 was firstly found from natural sources. The antifungal activities of compounds 1-5 towards four phytopathogens were assayed using broth microdilution method. Among them, globosuxanthone A (1) showed obvious antifungal activity towards Fusarium graminearum, Fusarium solani, and Botrytis cinerea with MIC values of 4, 8, and 16 μg/mL, respectively.
- MeSH
- Ascomycota chemie izolace a purifikace MeSH
- Azadirachta mikrobiologie MeSH
- endofyty chemie izolace a purifikace MeSH
- fungicidy průmyslové izolace a purifikace farmakologie MeSH
- fylogeneze MeSH
- houby účinky léků MeSH
- kultivační média chemie MeSH
- ovoce mikrobiologie MeSH
- xantony izolace a purifikace farmakologie MeSH
- Publikační typ
- časopisecké články MeSH
Research groups have put significant emphasis on the evaluation of nutritional, health-promoting, and other biological activities of secondary metabolites from buckwheat. Among these phytochemicals, phenolic and lipophilic antioxidants, particularly, phenolic acids, flavonoids, and tocopherols, have been the focus of the latest studies since antioxidant activity has recently been associated with the possibility of inhibiting fungal growth and mycotoxin biosynthesis. The mycotoxin contamination of cereal and pseudocereal grains caused primarily by Fusarium, Penicillium, and Aspergillus species poses a significant hazard to human health. Therefore, efforts to examine the involvement of plant antioxidants in the biosynthesis of mycotoxins at the transcriptional level have emerged. In addition, hydrophobic interactions of buckwheat phenolics with cell membranes could also explain their capacity to reduce fungal development. Eventually, possibilities of enhancing the biological activity of cereal and pseudocereal phytochemicals have been studied, and sourdough fermentation has been proposed as an efficient method to increase antioxidant activities. This effect could result in an increased antifungal effects of sourdough and bakery products. This review reports the main advances in research on buckwheat phenolics and other antioxidant phytochemicals, highlighting possible mechanisms of action and processes that could improve their biological activities.
- MeSH
- Fagopyrum chemie metabolismus MeSH
- fenoly chemie metabolismus farmakologie MeSH
- fungicidy průmyslové chemie metabolismus farmakologie MeSH
- houby účinky léků růst a vývoj MeSH
- lidé MeSH
- nemoci rostlin mikrobiologie MeSH
- rostlinné extrakty chemie metabolismus farmakologie MeSH
- sekundární metabolismus MeSH
- semena rostlinná chemie metabolismus MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
Electron-deficient chlorine covalently immobilised on an amido group of hyaluronic acid (HA) can be potentially exceptional for applications requiring biodegradable and biocompatible polymers with enhanced antibacterial or antiviral activity. This expectation is supported by the assumption that a small amount of HA chloramide (HACl) is formed in the extracellular matrix under inflammatory conditions by a reaction of endogenous HA with hypochlorous acid (HClO) generated by a myeloperoxidase/H2O2/Cl- system. HACl synthesis optimisation showed significant limitations of HClO as an oxidative agent where only lower degrees of substitution (DS) was achieved. Commercially available oxidative agents based on chlorinated isocyanuric acid were successfully tested, producing the HA chain with almost entirely chlorinated amidic groups. The structure of the final HACl was thoroughly studied using advanced 2-dimensional NMR methodologies and LC/MS. Stability of HACl at different temperatures was monitored over 12 months. Preliminary antimicrobial and antiviral tests demonstrated the potential of HACl for applications in biomedicine.
- MeSH
- antibakteriální látky chemie farmakologie MeSH
- antifungální látky chemie farmakologie MeSH
- antivirové látky chemie farmakologie MeSH
- Bacteria účinky léků MeSH
- chloraminy chemie farmakologie MeSH
- halogenace MeSH
- houby účinky léků MeSH
- kyselina chlorná chemie MeSH
- kyselina hyaluronová chemie MeSH
- viry účinky léků MeSH
- Publikační typ
- časopisecké články MeSH
Nosocomial infections, which greatly increase morbidity among hospitalized patients, together with growing antibiotic resistance still encourage many researchers to search for novel antimicrobial compounds. Picolinium salts with different lengths of alkyl chains (C12, C14, C16) were prepared by Menshutkin-like reaction and evaluated with respect to their biological activity, i.e., lipophilicity and critical micellar concentration. Picolinium salts with C14 and C16 side chains achieved similar or even better results when in terms of antimicrobial efficacy than benzalkoniums; notably, their fungicidal efficiency was substantially more potent. The position of the methyl substituent on the aromatic ring does not seem to affect antimicrobial activity, in contrast to the effect of length of the N-alkyl chain. Concurrently, picolinium salts exhibited satisfactory low cytotoxicity against mammalian cells, i.e., lower than that of benzalkonium compounds, which are considered as safe.
- MeSH
- antibakteriální látky farmakologie MeSH
- antiinfekční látky farmakologie MeSH
- antivirové látky farmakologie MeSH
- Candida účinky léků MeSH
- CHO buňky MeSH
- Cricetulus MeSH
- gramnegativní bakterie účinky léků MeSH
- grampozitivní bakterie účinky léků MeSH
- houby účinky léků MeSH
- kvartérní amoniové sloučeniny chemie farmakologie MeSH
- kyseliny pikolinové chemická syntéza chemie farmakologie MeSH
- mikrobiální testy citlivosti MeSH
- povrchově aktivní látky chemie farmakologie MeSH
- viabilita buněk účinky léků MeSH
- virus varicella zoster účinky léků MeSH
- vztahy mezi strukturou a aktivitou MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
