anti-inflammatory properties Dotaz Zobrazit nápovědu
Jednojadrové akva-(aryloxyacetáto)zinočnaté komplexy zloženia [Zn(H2O)2(ROCH2COO)2] (R =fenyl, o-, m-, p-tolyl) boli pripravené ako potenciálne protizápalovo účinné látky. Výsledky elemen-tárnej analýzy a parametre IČ spektier dovolili uvedené zlúčeniny zaradiť do skupiny karboxyláto-zinočnatých komplexov s deformovane oktaedrickou štruktúrou. Antiedematózna aktivitaakvakomplexov bola hodnotená na karagenínovom opuchu na potkanoch a ich účinky boli porovná-vané s príslušnými voľnými kyselinami. Kyselina salicylová a jej Zn(II)- a Cu(II)-soli, boli použitéako porovnávacie štandardy. Všetky zlúčeniny boli aplikované i.p. v jednorazovej dávke 50 mmol/kg(počítané na karboxylátový fragment). Vo všeobecnosti Zn(II)-komplexy boli účinnejšie (vyjadrenéako miera redukcie edému 58 – 70 – 68 – 59 %), vrátane dihydrátu salicylanu zinočnatého (64 %),ako nekomplexované kyseliny (37 – 26 – 50 – 48 %). Aktivita tetrahydrátu salicylanu meďnatého(60 %) a kyseliny salicylovej (57 %) je za tých istých podmienok porovnateľná. Zistená aktivitakomplexov je diskutovaná vo vzťahu k ich štruktúre a ku koordinačno-chemickým vlastnostiamštudovaných acidoligandov.
Mononuclear aqua(aryloxyacetato)zinc(II) complexes of the composition [Zn(H2O)2(ROCH2COO)2](R = phenyl, o-, m-, p-tolyl) were prepared as potential anti-inflammatory agents. The results ofelemental analysis and parameters of IR spectra allow to classify the above-mentioned compoundsto the group of carboxylatozinc(II) complexes with a distorted octahedral structure. They wereassayed in rat paw carrageenan-induced edema and antiedematous effects were compared to thoseof free acids. Salicylic acid and its zinc(II) and copper(II) salts were used as the standards ofcomparison. All compounds were administered i.p. in a single dose of 50 mmol/kg body weight(calculated for the carboxylate fragment). In general, the zinc(II) complexes tested were clearly moreeffective (expressed as a mean edema reduction of 58 – 70 – 68 – 59 %), including zinc(II) salicylatedihydrate (64 %), than the uncomplexed acids (37 – 26 – 50 – 48 %). Copper(II) salicylate tetrahyd-rate (60 %) and salicylic acid (57 %) exhibited comparable effects under the same conditions. Theobserved activities of the complexes are discussed in relation to their structures as well as to thecoordination-chemical properties of the acidoligands under study.
- MeSH
- antiflogistika terapeutické užití MeSH
- edém chemicky indukované terapie MeSH
- karagenan škodlivé účinky toxicita MeSH
- krysa rodu rattus MeSH
- kyseliny karboxylové analýza chemie MeSH
- měď chemie MeSH
- sloučeniny zinku analýza chemická syntéza terapeutické užití MeSH
- spektrofotometrie infračervená metody využití MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- zvířata MeSH
V skupine dvojiadrových meďnatých komplexov zloženia [Cu2(RCOO)4(H2O)2] {R = 2,4-diacetoxyfenyl (I), 2,5-diacetoxyfenyl (II) a 2,6-diacetoxyfenyl (III)} bola hodnotená protizápalová aktivita na karagenínovom edéme na potkanoch. Ako porovnávacie štandardy boli použité: tetrahydrát salicylanu meďnatého (IV) a kyselina salicylová. Všetky zlúčeniny boli podané i.p. v dávke 50 μnol/kg, počítané na R-COO-fragment. Testované meďnaté komplexy boli zjavne účinnejšie ako príslušné voľné diacetoxybenzoové kyseliny, s výnimkou 2,5-diacetoxyderivátu. Priemerná hodnota protizápalovej aktivity meďnatých komplexov klesá v poradí: III (71,0 %) = I (70,6 %) > IV (57,4 %) salicylovej (44,9 %). Vzťah medzi koordinačno-chemickými vlastnosťami a biologickým účinkom testovaných komplexov je diskutovaný.
In a group of binuclear copper (11) complexes of the composition [Cu2(RCOO)4(H20)2] (R = 2,4-(diacetoxyphenyl (1), 2,5-diacetoxyphenyl (II) and 2,6-diacetoxyphenyl (III)), the anti-inflammatory activity was assayed in rat paw carrageenan-induced edema. Copper (II) salicylate tetrahydrate (IV) and salicylic acid were used as standards for comparison. All compounds were applied i.p. in a single dose of 50 μmol/kg body weight, calculated for the R-COO-fragment. The Cu(II) complexes tested were clearly more effective than the corresponding free diacetoxybenzoic acids, with an exception for the 2,5-diacetoxy derivative. The average anti-inflammatory activities of copper (II) complexes were decreasing in the following order: III (71.0 %)«(70.6 %) > IV (57.4 %) > II (18.0 %). Of the acids, only 2,6-diacetoxybenzoic acid (45.2 %) was effective at the level of salicylic acid (44.9 %). The relationship between the coordination-chemical properties and the biological effects of the complexes tested is discussed.
Antiedematózna aktivita monohydrátu diakva-tetrakis(o -krezotináto)dimeďnatého komplexu(Cu o K)a diakva-bis(o -krezotináto)zinočnatého komplexu (Zn o K)bola hodnotená pletyzmometrickyna dextránovom a karagenínovom edéme na potkanoch.Dihydrát diakva-bis(salicyláto)meďnatéhokomplexu (CuS)a diakva-bis(salicyláto)zinočnatý komplex (ZnS)boli použité ako porovnávacieštandardy.Všetky zlúčeniny boli podané i.p.v jednorazovej dávke 50 µmol/kg (počítané naRCOO —fragment)30 min pred injikovaním iritačných látok.Priemerná antidextránová/antikaragenínová aktivita látok (vyjadrená ako miera redukcie edému)bola zistená:Cu o K 36/54 %–Zn o K59/65 %– CuS 71//52 %– ZnS 63/10 %.Vzťahy medzi koordinačno-chemickými vlastnosťami a biologickým účinkom príslušných komplexov sú diskutované.
Using rat paw dextran-induced and carrageenan-induced edemas,the antiedematous activites ofmonohydrate of the diaquatetrakis(o -cresotato)dicopper(II)complex (Cu o C)and the diaquabis(o-cresotato)zinc(II)complex (Zn o C)were assayed plethysmometrically.Dihydrate of the diaquabis(salicylato)copper(II)complex (CuS)and the diaquabis(salicylato)zinc(II)complex (ZnS)were used asthe standards of comparison.All compounds were administered i.p.in a single dose of 50 µmol/kgbody weight (calculated for the RCOO-fragment)30 min before injecting the irritants.The antidextran/anticarrageenan activities of the species (expressed as a mean edema reduction)were found:Cu o C 36/54 %–Zn o C 59/65 %–CuS 71/52 %–ZnS 63/10 %.The relationships between thecoordination-chemical properties and the biological effects of the corresponding complexes arediscussed.
Inflammation contributes to the formation and progression of atherosclerosis and the therapeutic potential of some anti-inflammatory drugs has been evaluated for possible antiatherosclerotic effects. This review will briefly describe the mechanisms underlying the inflammation-atherosclerosis connection, the effect of various anti-inflammatory therapies on atherosclerotic disease and a sampling of the potential targets and agents under evaluation. RECENT FINDINGS: Some agents with anti-inflammatory properties appear to have beneficial effects on atherosclerosis or subsequent risk for cardiovascular events, while others have been disappointing. The anti-inflammatory actions of statins have been linked retrospectively with their favorable effects on atherosclerosis progression and clinical outcomes. The cardiovascular safety of COX-2 inhibitors is being assessed prospectively in patients with atherosclerosis. Potential new therapeutic agents targeting other inflammatory mechanisms and oxidative stress are being evaluated in animal models and clinical trials. SUMMARY: Due to the contributory inflammatory pathways in atherosclerosis, the properties of existing and novel anti-inflammatory agents are being carefully and actively evaluated in cardiovascular disease. Advances in our understanding of both atherosclerosis and the inflammatory contributors may play an important role in future strategies to decrease the incidence of atherosclerotic cardiovascular disease.
Recent studies manifest an increase of inflammatory diseases at an alarming rate due to gut microbiota dysbiosis, genetic and other environmental factors. Lactic acid bacteria (LAB) are known for their antimicrobial properties and their extensive applications in food and pharmaceutical industries. Cyclic peptides are receiving increased attention due to their remarkable stability to withstand variations in temperature and pH. LAB produces anti-inflammatory that can inhibit lipopolysaccharide-induced production of proinflammatory cytokines in macrophages. The structural backbones of cyclic peptides offer a promising approach for the treatment of chronic inflammatory conditions. The current review aims to present the overview of anti-inflammatory and wound healing properties of LAB-derived cyclic peptides.
- MeSH
- antiflogistika farmakologie MeSH
- cyklické peptidy MeSH
- hojení ran MeSH
- Lactobacillales * MeSH
- peptidy MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
Cudraflavone B (1) is a prenylated flavonoid found in large amounts in the roots of Morus alba, a plant used as a herbal remedy for its reputed anti-inflammatory properties. The present study shows that this compound causes a significant inhibition of inflammatory mediators in selected in vitro models. Thus, 1 was identified as a potent inhibitor of tumor necrosis factor α (TNFα) gene expression and secretion by blocking the translocation of nuclear factor κB (NF-κB) from the cytoplasm to the nucleus in macrophages derived from a THP-1 human monocyte cell line. The NF-κB activity reduction resulted in the inhibition of cyclooxygenase 2 (COX-2) gene expression. Compound 1 acts as a COX-2 and COX-1 inhibitor with higher selectivity toward COX-2 than indomethacin. Pretreatment of cells by 1 shifted the peak in an regulatory gene zinc-finger protein 36 (ZFP36) expression assay. This natural product has noticeable anti-inflammatory properties, suggesting that 1 potentially could be used for development as a nonsteroidal anti-inflammatory drug lead.
- MeSH
- aktiny účinky léků MeSH
- antiflogistika nesteroidní chemie izolace a purifikace farmakologie MeSH
- cyklooxygenasa 1 účinky léků MeSH
- flavonoidy chemie izolace a purifikace farmakologie MeSH
- inhibitory cyklooxygenasy 2 chemie izolace a purifikace farmakologie MeSH
- kořeny rostlin chemie MeSH
- lidé MeSH
- makrofágy účinky léků MeSH
- molekulární struktura MeSH
- Morus chemie MeSH
- NF-kappa B antagonisté a inhibitory MeSH
- TNF-alfa antagonisté a inhibitory genetika MeSH
- tristetraprolin účinky léků genetika MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
BACKGROUND: Salivary glands from blood-feeding arthropods secrete several molecules that inhibit mammalian hemostasis and facilitate blood feeding and pathogen transmission. The salivary functions from Simulium guianense, the main vector of Onchocerciasis in South America, remain largely understudied. Here, we have characterized a salivary protease inhibitor (Guianensin) from the blackfly Simulium guianense. MATERIALS AND METHODS: A combination of bioinformatic and biophysical analyses, recombinant protein production, in vitro and in vivo experiments were utilized to characterize the molecula mechanism of action of Guianensin. Kinetics of Guianensin interaction with proteases involved in vertebrate inflammation and coagulation were carried out by surface plasmon resonance and isothermal titration calorimetry. Plasma recalcification and coagulometry and tail bleeding assays were performed to understand the role of Guianensin in coagulation. RESULTS: Guianensin was identified in the sialotranscriptome of adult S. guianense flies and belongs to the Kunitz domain of protease inhibitors. It targets various serine proteases involved in hemostasis and inflammation. Binding to these enzymes is highly specific to the catalytic site and is not detectable for their zymogens, the catalytic site-blocked human coagulation factor Xa (FXa), or thrombin. Accordingly, Guianensin significantly increased both PT (Prothrombin time) and aPTT (Activated partial thromboplastin time) in human plasma and consequently increased blood clotting time ex vivo. Guianensin also inhibited prothrombinase activity on endothelial cells. We show that Guianensin acts as a potent anti-inflammatory molecule on FXa-induced paw edema formation in mice. CONCLUSION: The information generated by this work highlights the biological functionality of Guianensin as an antithrombotic and anti-inflammatory protein that may play significant roles in blood feeding and pathogen transmission.
- MeSH
- antiflogistika farmakologie MeSH
- endoteliální buňky MeSH
- hemostatika * MeSH
- hemostáza MeSH
- lidé MeSH
- myši MeSH
- savci MeSH
- Simuliidae * MeSH
- slinné proteiny a peptidy farmakologie MeSH
- zánět MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- myši MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Research Support, N.I.H., Intramural MeSH
Extensive phytochemical analysis of the CHCl3-soluble part of an ethanolic extract of branches and twigs of Broussonetia papyrifera led to the isolation of fourteen compounds, including a novel 5,11-dioxabenzo[b]fluoren-10-one derivative named broussofluorenone C (12). The isolated compounds 1-14 were characterized based on their NMR and HRMS data, and examined for their anti-inflammatory activities in LPS-stimulated THP-1 cells as well as for their cellular antioxidant effects. Compounds 7-10 and 12 showed inhibitory effects on NF-κB/AP-1 activation and compounds 7-9 were subsequently confirmed to suppress the secretion of both IL-1β and TNF-α in LPS-stimulated THP-1 cells more significantly than the prednisone used as a positive control. In the CAA assay, compound 10 exhibited the greatest antioxidant effect, greater than that of the quercetin used as a positive control. The results show possible beneficial effects and utilization of B. papyrifera wood in the treatment of inflammatory diseases as well as oxidative stress.
- MeSH
- antiflogistika chemie izolace a purifikace farmakologie MeSH
- antioxidancia chemie izolace a purifikace farmakologie MeSH
- Broussonetia chemie MeSH
- interleukin-1beta antagonisté a inhibitory biosyntéza MeSH
- kultivované buňky MeSH
- lidé MeSH
- lipopolysacharidy antagonisté a inhibitory farmakologie MeSH
- molekulární struktura MeSH
- NF-kappa B analýza antagonisté a inhibitory biosyntéza MeSH
- oxidační stres účinky léků MeSH
- THP-1 buňky MeSH
- TNF-alfa antagonisté a inhibitory biosyntéza MeSH
- transkripční faktor AP-1 analýza antagonisté a inhibitory biosyntéza MeSH
- viabilita buněk účinky léků MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
Nejslibnějším směrem v léčbě chronické prostatitidy je využití léčivých rostlin a přípravků na jejich bázi, které obsahují přírodní látky se širokým spektrem farmakologické aktivity: protizánětlivé, antimikrobiální, reparační, imunomodulační, hormonálně regulační, antisklerotické atd. a které mohou poskytnout komplexní terapeutický účinek na průběh chronické prostatitidy. Slibnou surovinou v tomto směru je Tribulus terrestris L., rostlinný přípravek tradičně používaný k léčbě erektilní dysfunkce a aterosklerózy. Cílem této experimentální práce je studium protizánětlivé aktivity hustého extraktu z trávy Tribulus terrestris (zbaveného plodů) na modelech zánětu vyvolaného karagenanem a zymosanem u potkanů. Na modelech karagenanového a zymosanového edému u potkanů vykazuje hustý extrakt Tribulus terrestris L. v dávkách od 50 mg/kg do 200 mg/kg protizánětlivou aktivitu, jejíž účinnost v rozmezí dávek 150–200 mg/g není v počátečních stadiích karagenanového zánětu horší než u diklofenaku sodného v dávce 8,0 mg/kg, respektive v počátečních stadiích zymosanového zánětu, a není lepší než účinek referenčního léčiva korvitinu v dávce 10 mg/kg. To svědčí o anticyklogenázových a antilipoxygenázových vlastnostech tohoto hustého extraktu.
The most promising direction in the treatment of chronic prostatitis is the use of medicinal plants and preparations based on them, which contain natural compounds with a broad spectrum of pharmacological activity: anti-inflammatory, antimicrobial, reparative, immunomodulatory, hormone-regulating, antisclerotic, etc., and which can provide a complex therapeutic effect on the course of chronic prostatitis. A promising raw material in this direction is Tribulus terrestris L., a herbal preparation traditionally used to treat erectile dysfunction and atherosclerosis. This experimental work aims to study the anti-inflammatory activity of a thick extract of the Tribulus terrestris grass (freed from fruits) on the models of carrageenan and zymosan inflammation in rats. In the models of carrageenan and zymosan edema in rats, a thick extract of Tribulus terrestris L. in doses from 50 mg/kg to 200 mg/kg shows anti-inflammatory activity, the efficacy of which in the dose range of 150–200 mg/g in the initial stages of carrageenan inflammation is not inferior to sodium diclofenac at a dose of 8.0 mg/kg, and in the initial stages of zymosan inflammation, respectively, before the reference drug corvitin at a dose of 10 mg/kg. It indicates the anticyclogenase and antilipoxygenase properties of this thick extract.
- MeSH
- antiflogistika MeSH
- diklofenak aplikace a dávkování terapeutické užití MeSH
- flavonoidy aplikace a dávkování terapeutické užití MeSH
- léčivé rostliny MeSH
- modely u zvířat MeSH
- potkani Wistar MeSH
- prostatitida * farmakoterapie MeSH
- rostlinné extrakty aplikace a dávkování terapeutické užití MeSH
- Tribulus * MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
BACKGROUND: Obesity is a risk factor for non-alcoholic fatty liver disease (NAFLD). The disease is associated with impairment of pro/antioxidant equilibrium and the inflammation in liver tissue. The aim of the work was to investigate the anti-inflammatory properties of the nanocrystalline cerium dioxide (nCeO2) on the rat model of NAFLD associated with monosodium glutamate (MSG)-induced obesity. METHODS: The study was carried out on three groups of rats: control, MSG- and MSG+nCeO2. They were injected with saline (control) or MSG. A month after born MSG-rats had been treated with water in a volume of 2.9ml/kg, MSG+CeO2groups - with CeO2intragastrically (i.g.). The anthropometric and carbohydrate metabolism parameters, content of proinflammatory cytokines (interleukin (IL)-1β, IL-12Bp40, interferon-γ (INF-γ)) and anti-inflammatory cytokines (IL-4, IL-10, tumor growth factor-β (TGF-β)) were measured by ELISA. RESULTS: We have demonstrated the anti-obesity effect of nanocrystalline cerium dioxide and for the first time its anti-inflammatory properties. Nanoparticles reduced the content of pro-inflammatory cytokines (IL-1β, IL-12Bp40) in rat serum and restored the level of anti-inflammatory cytokines (IL-4, IL-10, TGF-β) to the control values. CONCLUSION: The precise mechanisms of this phenomenon remain to be unclear but we suppose they are at least partially associated with the strong anti-oxidant action of studied substance. Nanocrystalline cerium dioxide attenuates the inflammatory processes in rat blood that can prevent obesity complications and liver injury.
- MeSH
- antiflogistika farmakologie MeSH
- antioxidancia metabolismus MeSH
- cer farmakologie MeSH
- interferon gama metabolismus MeSH
- interleukin-10 metabolismus MeSH
- interleukin-4 metabolismus MeSH
- krysa rodu rattus MeSH
- nanočástice aplikace a dávkování MeSH
- nealkoholová steatóza jater farmakoterapie metabolismus MeSH
- obezita farmakoterapie metabolismus MeSH
- transformující růstový faktor beta metabolismus MeSH
- zánět farmakoterapie metabolismus MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- mužské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
