Cryptococcosis is a potentially fatal fungal disease which has aggrandized with the emergence of AIDS and antifungal resistance. The currently used antifungals lack the broad-spectrum activity and result in several toxicities during long treatment regimens. Thus, the present study aims to evaluate the antifungal activity of cinnamaldehyde against Cryptococcus neoformans var. grubii, the etiological agent of the disease. Quantitative and qualitative in vitro fungal susceptibilities were carried out by minimum inhibitory concentration assay, flow cytometric analysis, and confocal microscopy. Micromorphological alterations were studied through scanning electron and light microscopies. "In vivo" antifungal efficacy of cinnamaldehyde was assessed. Cinnamaldehyde showed antifungal activity against C. neoformans in a dose-dependent manner. A concentration of 1.37 mg/mL of cinnamaldehyde was found to be inhibitory and fungicidal while the low concentration (0.68 mg/mL) was found to induce micromorphological changes and formation of giant/titan-like cells in this pathogen. The reparative activity of cinnamaldehyde and its ability to prolong the life even after the advent of cryptococcal meningitis in mice was also noticed. This study suggests potent anti-cryptococcal activity of cinnamaldehyde. Though, it has a couple of limitations like allergy and low bioavailability. However, these problems can be circumvented by developing suitable analogs of the compound. It, therefore, could be used as a therapeutic option against cryptococcosis and cryptococcal meningitis. Moreover, the evaluation of its pharmacokinetic and pharmacodynamic properties is desirable.

• MeSH
• akrolein analogy a deriváty   farmakologie   MeSH
• analýza přežití MeSH
• antifungální látky farmakologie   MeSH
• Cryptococcus neoformans účinky léků   MeSH
• fungální léková rezistence účinky léků   MeSH
• játra patologie   MeSH
• kryptokokóza farmakoterapie   mikrobiologie   patologie   MeSH
• mikrobiální testy citlivosti MeSH
• modely nemocí na zvířatech MeSH
• mozek patologie   MeSH
• mykózy farmakoterapie   MeSH
• myši MeSH
• plíce patologie   MeSH
• zvířata MeSH
• Check Tag
• myši MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH

Acrolein, a highly reactive unsaturated aldehyde, is generated in large amounts during smoking and is best known for its genotoxic capacity. Here, we aimed to assess whether acrolein at concentrations relevant for smokers may also exert immunomodulatory effects that could be relevant in allergy or cancer. In a BALB/c allergy model repeated nasal exposure to acrolein abrogated allergen-specific antibody and cytokine formation, and led to a relative accumulation of regulatory T cells in the lungs. Only the acrolein-treated mice were protected from bronchial hyperreactivity as well as from anaphylactic reactions upon challenge with the specific allergen. Moreover, grafted D2F2 tumor cells grew faster and intratumoral Foxp3+ cell accumulation was observed in these mice compared to sham-treated controls. Results from reporter cell lines suggested that acrolein acts via the aryl-hydrocarbon receptor which could be inhibited by resveratrol and 3'-methoxy-4'-nitroflavone Acrolein- stimulation of human PBMCs increased Foxp3+ expression by T cells which could be antagonized by resveratrol. Our mouse and human data thus revealed that acrolein exerts systemic immunosuppression by promoting Foxp3+ regulatory cells. This provides a novel explanation why smokers have a lower allergy, but higher cancer risk.

• MeSH
• akrolein farmakologie   MeSH
• alergeny imunologie   MeSH
• alergie imunologie   prevence a kontrola   MeSH
• cytokiny metabolismus   MeSH
• forkhead transkripční faktory metabolismus   MeSH
• imunologické faktory farmakologie   MeSH
• modely nemocí na zvířatech MeSH
• myši MeSH
• nádory imunologie   metabolismus   MeSH
• NF-kappa B metabolismus   MeSH
• plíce imunologie   metabolismus   patologie   MeSH
• receptory aromatických uhlovodíků metabolismus   MeSH
• regulační T-lymfocyty imunologie   metabolismus   MeSH
• resveratrol MeSH
• signální transdukce MeSH
• stilbeny farmakologie   MeSH
• tvorba protilátek imunologie   MeSH
• zvířata MeSH
• Check Tag
• myši MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH

Biofilmy oportunně patogenních mikroorganismů představují zdroj četných obtížně léčitelných onemocnění. Studium přírodních biologicky aktivních látek a jejich vlivu na tvorbu a stabilitu biofilmů hraje významnou roli v současném výzkumu. Přírodní produkty extrahované z nesčetného množství rostlin představují potenciální zdroj nových antimikrobiálních a antibiofilmových činidel. Ze zmíněné kategorie látek práce předkládá cinnamaldehyd a N‐‐acetylcystein.

The biofilms of opportunistic pathogens are a source of numerous difficult‐‐to‐‐treat infections. Exploration of natural biologically active compounds and their influence on the formation and stability of biofilms plays an important role in current research. Natural compounds isolated from plants can be viewed as a potential source of new anti‐‐microbial and anti‐‐biofilm agents. From this category, cinnamaldehyde and N‐‐acetylcysteine are presented.

• Klíčová slova
• cinnamaldehyd, antibiofilmová aktivita,
• MeSH
• acetylcystein * farmakologie   MeSH
• akrolein analogy a deriváty   farmakologie   MeSH
• antibakteriální látky MeSH
• Bacteria účinky léků   MeSH
• biofilmy * účinky léků   MeSH
• Candida albicans účinky léků   MeSH
• quorum sensing účinky léků   MeSH
• Publikační typ
• práce podpořená grantem MeSH

x

• MeSH
• akrolein analogy a deriváty   farmakologie   škodlivé účinky   MeSH
• chemické bojové látky * farmakologie   škodlivé účinky   MeSH
• chloracetáty chemie   škodlivé účinky   MeSH
• dráždivé látky * dějiny   škodlivé účinky   MeSH
• fosgen analogy a deriváty   farmakologie   škodlivé účinky   MeSH
• lidé MeSH
• sloučeniny bromu chemie   škodlivé účinky   MeSH
• slzné plyny chemie   škodlivé účinky   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• práce podpořená grantem MeSH
• přehledy MeSH

Cronobacter sakazakii and C. malonaticus are opportunistic pathogens that cause infections in children and immunocompromised adults. In the present study, the antibacterial activity of 19 plant-derived compounds, 5 essential oils, and an extract of propolis were assessed against C. sakazakii and C. malonaticus. The effects of most of these antimicrobials have not been reported previously. Both strains were susceptible to thymol, carvacrol, thymoquinone, p-cymene, linalool, camphor, citral, eugenol, and trans-cinnamaldehyde as well as cinnamon, lemongrass, oregano, clove, and laurel essential oils; their minimum inhibitory concentrations varied between 0.1 and 2.0 mg/mL. As an alternative treatment method, vapors of the volatiles were tested as an indirect treatment. Vapors of trans-cinnamaldehyde, eugenol, oregano, and cinnamon essential oils inhibited both tested strains, while vapors of linalool were only active against C. sakazakii. To our knowledge, this study is the first time that the inhibitory activity of the vapors of these compounds and essential oils has been reported against Cronobacter spp.

• MeSH
• akrolein analogy a deriváty   chemie   farmakologie   MeSH
• antibakteriální látky chemie   farmakologie   MeSH
• benzochinony chemie   farmakologie   MeSH
• Cronobacter sakazakii účinky léků   MeSH
• Cronobacter účinky léků   MeSH
• Cymbopogon chemie   MeSH
• dobromysl (rod) chemie   MeSH
• eugenol chemie   farmakologie   MeSH
• kafr chemie   farmakologie   MeSH
• mikrobiální testy citlivosti MeSH
• monoterpeny chemie   farmakologie   MeSH
• oleje prchavé chemie   farmakologie   MeSH
• oleje rostlin chemie   farmakologie   MeSH
• rostlinné extrakty chemie   farmakologie   MeSH
• seskviterpeny chemie   farmakologie   MeSH
• skořicovník ceylonský chemie   MeSH
• Syzygium chemie   MeSH
• thymol chemie   farmakologie   MeSH
• vztah mezi dávkou a účinkem léčiva MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH

• MeSH
• akrolein * farmakologie   kontraindikace   škodlivé účinky   terapeutické užití   MeSH
• antibakteriální látky izolace a purifikace   terapeutické užití   MeSH
• fytoterapie MeSH
• kůra rostlin * chemie   MeSH
• lidé MeSH
• skořicovník ceylonský * chemie   MeSH
• Check Tag
• lidé MeSH

Extracts of Helleborus roots were traditionally used in the Balkan area for their analgesic action. We report that the pure natural product MCS-18 isolated from this source is a potent, specific and reversible antagonist of the capsaicin receptor, TRPV1, expressed in rat dorsal root ganglion (DRG) neurons. TRPV1 is a nonselective cation channel expressed in a subset of cutaneous and visceral sensory nerve endings and activated by noxious heat, acidity and fatty acid metabolites of arachidonic acid, with a decisive role in inflammatory heat hyperalgesia. MCS-18 inhibited the increase in intracellular calcium concentration evoked in DRG neurons by capsaicin (300 nM) and low pH (5.5) but not by heat (43 oC). The substance had no effect on the responses mediated by acid-sensing ion channels (ASICs) or the irritant receptor TRPA1. Whole-cell patch-clamp was used to confirm the inhibition of capsaicin-induced currents by MCS-18 which was dose-dependent. The mechanism of inhibition does not require an intact cell, as capsaicin-induced currents were also inhibited in the excised outside-out configuration. The antagonism of the capsaicin and proton action on native TRPV1 by MCS-18 may be of interest for pain therapy.

• MeSH
• akrolein analogy a deriváty   farmakologie   MeSH
• biologické přípravky farmakologie   MeSH
• bolest farmakoterapie   metabolismus   MeSH
• financování organizované MeSH
• Helleborus MeSH
• kapsaicin metabolismus   MeSH
• kationtové kanály TRPV antagonisté a inhibitory   metabolismus   MeSH
• krysa rodu rattus MeSH
• kultivované buňky MeSH
• kyseliny farmakologie   MeSH
• membránové potenciály účinky léků   MeSH
• metoda terčíkového zámku MeSH
• nervové receptory cytologie   metabolismus   účinky léků   MeSH
• spinální ganglia cytologie   MeSH
• vápník metabolismus   MeSH
• vysoká teplota MeSH
• vztah mezi dávkou a účinkem léčiva MeSH
• zvířata MeSH
• Check Tag
• krysa rodu rattus MeSH
• zvířata MeSH

Two representative strains of Gram-negative rumen bacteria from the genus Prevotella were used as model organisms in order to evaluate the effect of cinnamaldehyde (the secondary metabolite found in extracts of the Cinnamomum family) vs. sodium monensin on growth, cell size and cell protein production. Prevotella bryantii B(1)4 was found to be remarkably more resistant to the action of both compounds than Prevotella ruminicola 23. The approximate IC(50) concentrations of sodium monensin influenced the increase in cell size of both strains during growth, which was much more pronounced in the case of the B(1)4 strain. A similar effect was observed in strain B(1)4 when 1.438 mmol/L cinnamaldehyde was added to the growth medium, indicating a possible interference with cell division. The action of cinnamaldehyde on P. bryantii B(1)4 was concentration-dependent, in contrast to the effect observed on P. ruminicola 23.

• MeSH
• akrolein analogy a deriváty   farmakologie   MeSH
• antiprotozoální látky farmakologie   MeSH
• bachor mikrobiologie   MeSH
• fenotyp MeSH
• inhibiční koncentrace 50 MeSH
• monensin farmakologie   MeSH
• parazitické testy citlivosti MeSH
• Prevotella ruminicola klasifikace   metabolismus   účinky léků   MeSH
• Prevotella klasifikace   metabolismus   růst a vývoj   účinky léků   MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH

The inhibitory effect of some plant oil aromatics against three strains of Arcobacter butzleri, two strains of Arcobacter cryaerophilus, and one strain of Arcobacter skirrowii was evaluated. When MICs were determined using the broth macrodilution method, cinnamaldehyde was most inhibitory followed by thymol, carvacrol, caffeic acid, tannic acid, and eugenol (P < 0.001). Sublethal concentrations of the three most potent plant oil aromatics also were examined. Overall, cinnamaldehyde was the most bacteriostatic against all arcobacters tested except A. butzleri when these strains were exposed to the MIC25 of this aromatic aldehyde. The bacteriostatic activities of thymol and carvacrol were concentration and species dependent.

• MeSH
• akrolein analogy a deriváty   farmakologie   MeSH
• Arcobacter růst a vývoj   účinky léků   MeSH
• druhová specificita MeSH
• eugenol farmakologie   MeSH
• financování organizované MeSH
• konzervace potravin metody   MeSH
• kyseliny kávové farmakologie   MeSH
• lidé MeSH
• mikrobiální testy citlivosti MeSH
• monoterpeny farmakologie   MeSH
• oleje rostlin farmakologie   chemie   MeSH
• počet mikrobiálních kolonií MeSH
• potravinářské konzervační látky farmakologie   MeSH
• spotřebitelská bezpečnost produktů MeSH
• taniny farmakologie   MeSH
• thymol farmakologie   MeSH
• vztah mezi dávkou a účinkem léčiva MeSH
• Check Tag
• lidé MeSH