cytellin and Edema

Beta-sitosterol (BS) is a compound discovered to be present in numerous plants. A number of interesting biomedical properties have been attributed to BS, including immuno-modulating and anti-inflammatory activities. Therefore, the aim of this report was to evaluate its anti-inflammatory capacity by applying various rodent experimental tests.. To carry out the objective of the study we applied the methods indicated here. Two of the adopted methods were based on the passive reverse Arthus reaction: the rat paw edema test and the rat pleurisy assay. We also applied two methods related with the non-specific acute inflammation: the mouse ear edema test, and the mouse mieloperoxidase activity assay.. The results obtained in all tests established a significant anti-inflammatory potential of BS. In the rat paw edema test we found an inhibitory effect which goes from 50-70%; in the rat pleurisy assay our findings with respect to the volume of pleural exuded showed a reduction of 46%, as well as a 20% low amount of neutrophils in comparison with the level of the control group. In the mouse ear edema test we found a mean inflammatory inhibition of 75%, and with respect to mieloproxidase activity the results showed a significant inhibition induced by the three doses of BS.. In the present study we determined a potent anti-inflammatory capacity of BS in specific and non-specific types of acute inflammation in rodents.

Topics: Animals; Anti-Inflammatory Agents; Drug Evaluation, Preclinical; Edema; Humans; Male; Mice; Plant Extracts; Pleurisy; Rats; Rats, Wistar; Sitosterols

The hexanic, ethyl acetate and methanolic extracts from branches of Stenocereus stellatus were tested in both the 12-O-tetradecanoylphorbol-13-acetate (TPA) - induced ear oedema model and antimicrobial activity assay. The % of oedema inhibition, the Minimum Inhibitory Concentration (MIC), as well as the polyphenolic and flavonoid content were determined. Also, extracts were analysed by gas chromatography-mass spectrometry (GC-MS). In TPA model, the three extracts showed moderate oedema inhibition. In the antimicrobial activity assay, methanolic extract shows better MIC against all strains. The lowest MICs were for Candida albicans (31 μg/mL) and Rhizopus sp. (15 μg/mL). Also, 50.78 mg eq. of gallic acid/g extract of polyphenol and 115.12 mg eq. of catequine/g extract of flavonoids content were founded in ethyl acetate extract. In the chromatographic analysis, β-sitosterol, β-amyrine, betulin and some other molecules were identified. The results show that S. stellatus possess antimicrobial activities against some fungus species.

Topics: Animals; Anti-Infective Agents; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Cactaceae; Candida albicans; Disease Models, Animal; Edema; Flavonoids; Gas Chromatography-Mass Spectrometry; Male; Microbial Sensitivity Tests; Phorbol Esters; Plant Extracts; Polyphenols; Rhizopus; Secondary Metabolism; Sitosterols

Chemical investigation of the Red Sea sponge Dragmacidon coccinea led to the isolation of a new nucleoside, dragmacidoside (1), along with eight known compounds: adenosine (2), inosine (3), deoxycytidine (4), methyl-α-d-glucopyranoside (5), clionasterol (6), stigmasterol (7), campesterol (8) and brassicasterol (9). The compounds were isolated from chloroform and ethyl acetate fractions of the methanolic extract of the sponge, and their structures were established based on various spectroscopic data including MS, 1D and 2D NMR (COSY, HSQC and HMBC). Biological testing revealed that the chloroform fraction possesses significant anti-inflammatory activity in the carrageenan-induced hind paw oedema in rats.

Topics: Animals; Anti-Inflammatory Agents; Carrageenan; Edema; Indian Ocean; Marine Biology; Molecular Structure; Nucleosides; Porifera; Rats; Sitosterols; Stigmasterol

In Mexico Agave angustifolia has traditionally been used to treat inflammation. The aim of this study was to measure the anti-inflammatory effect of the extract of A. angustifolia, the isolation and identification of active compounds. From the acetone extract two active fractions were obtained, (AsF13 and AaF16). For the characterization of pharmacological activity, the acute inflammatory model of mouse ear edema induced with TPA was used. The tissue exposed to TPA and treatments were subjected to two analysis, cytokine quantification (IL-1β, IL-6, IL-10 and TNF-α) and histopathological evaluation. The active fraction (AaF16) consisted principally of 3-O-[(6'-O-palmitoyl)-β-D-glucopyranpsyl] sitosterol. In AaF13 fraction was identified β-sitosteryl glucoside (2) and stigmasterol (3). The three treatments tested showed a concentration-dependent anti-inflammatory effect (AaAc Emax = 33.10%, EC50 = 0.126 mg/ear; AaF13 Emax = 54.22%, EC50 = 0.0524 mg/ear; AaF16 Emax = 61.01%, EC50 = 0.050 mg/ear). The application of TPA caused a significant increase on level of IL-1β, IL-6 and TNFα compared with basal condition, which was countered by any of the experimental treatments. Moreover, the experimental treatments induced a significant increase in the levels of IL-4 and IL-10, compared to the level observed when stimulated with TPA. Therefore, the anti-inflammatory effect of Agave angustifolia, is associated with the presence of 3-O-[(6'-O-palmitoyl)-β-D-glucopyranosyl] sitosterol.

Topics: Agave; Animals; Anti-Inflammatory Agents; Cytokines; Disease Models, Animal; Ear; Edema; Male; Mice; Plant Extracts; Sitosterols

The present study describes the tracheorelaxant and anti-inflammatory effects of Polygonatum verticillatum which may support its medicinal use in hyperactive airway complaints and inflammatory disorders.. The tracheorelaxant activity of crude extract of the rhizomes of P. verticillatum (PR) was assessed in isolated guinea-pig tracheal tissues immersed in tissue organ bath filled with Tyrode's solution and a continuous supply of carbogen gas (95% O2 and 5% CO2). The contractile and relaxant responses of the tissue were measured using isometric transducers coupled with Power-Lab data acquisition system. The anti-inflammatory effect was evaluated in carrageenan-induced rat paw edema model, while the lipoxygenase inhibitory activity was performed in the in-vitro assay. Various chromatographic and spectroscopic techniques were used for the isolation and characterization of pure molecules.. In isolated guinea-pig tracheal preparations, PR caused complete inhibition of the high K+ (80 mM) and carbachol-induced contractions however, it was more potent against K+ than CCh, similar to verapamil. Pretreatment of the tissue with PR, displaced the Ca2+ concentration-response curves to the right, similar to that induced by verapamil, indicating the presence of Ca2+ channel blocking like activity. When tested on carrageenan-induced rat paw edema, PR demonstrated a marked reduction in edema with 65.22% protection at 200 mg/kg, similar to aspirin. In the in-vitro assay, PR showed lipoxygenase inhibitory activity (IC50: 102 ± 0.19 μg/mL), similar to baicalein. Bioactivity-guided fractionation led to the isolation of 2-hydroxybenzoic acid and β-sitosterol.. These results indicate that the plant possesses tracheorelaxant, mediated possibly through a Ca2+ channel blockade mechanism, and anti-inflammatory activities, which may explain the medicinal use of this plant in airway disorders and inflammation.

Topics: Animals; Anti-Inflammatory Agents; Calcium Channel Blockers; Carbachol; Carrageenan; Edema; Female; Guinea Pigs; Inflammation; Male; Muscle Contraction; Muscle, Smooth; Phytotherapy; Plant Extracts; Polygonatum; Rats; Rats, Wistar; Respiratory Tract Diseases; Rhizome; Salicylic Acid; Sitosterols; Trachea; Verapamil

Although serotherapy against snakebite has been discovered more than one hundred years ago, antivenom is not available all over Brazil. The use of plants from folk medicine is common mainly in the Brazilian Amazon area. One of these plants is named Humirianthera ampla (HA).. We have investigated HA extract and constituents' antiophidic activity in different experimental protocols against some Bothrops snake venoms (Bothrops jararacussu, Bothrops atrox and Bothrops jararaca). The protocols investigated include phospholipase, proteolytic, pro-coagulant, hemorrhagic, edematogenic and myotoxic activities induced by these venoms in Swiss mice.. All the venoms caused an increase in the rate of creatine kinase (CK) release from isolated muscles, indicating damage to the sarcolemma. The crude extract of HA decreased the myotoxic activity in a concentration-dependent fashion. The presence of HA 300 μg/mL decreased up to 96% of Bothrops jararacussu and 94% of Bothrops atrox myotoxicity after 90 min of exposure. In vivo myotoxicity of Bothrops atrox venom was decreased in 75% when the venom was preincubated with HA 500 mg/kg. Similar results were observed with lupeol against Bothrops jararacussu and Bothrops atrox venoms. The hemorrhagic activity was evaluated by intradermal injection of Bothrops atrox venom. Preincubation and oral pre- and posttreatment with HA decreased hemorrhage by 100%, 45% and 45%, respectively. Bothrops atrox venom also induced formation of edema, which was significantly inhibited by pre- and posttreatment with HA. All the venoms showed extensive pro-coagulating properties, and these activities were inhibited by up to 90% with HA, which presented concentration-dependent inhibition. Finally, proteolytic and phospholipase activities of the venoms were all inhibited by increasing concentrations of HA, lupeol and sitosterol. The inhibition of these activities might help explain the actions against in vivo myotoxicity and the in vivo effects observed, i.e., edema, myotoxicity, pro-coagulation and hemorrhage.. Altogether, our results give support for the popular use of HA extracts in cases of accidents with snakes, suggesting that it can be used as an adjunct in the management of venomous snakebites.

Topics: Animals; Antivenins; Bothrops; Brazil; Crotalid Venoms; Edema; Ethanol; Hemorrhage; Magnoliopsida; Male; Mice; Muscles; Pentacyclic Triterpenes; Phospholipases; Phytotherapy; Plant Extracts; Plant Roots; Sitosterols

Leaves and branches of Machaerium hirtum Vell. (Fabaceae), native to South America, were subjected to phytopharmacological investigation in order to identify its major chemical constituents and evaluate its extracts, fractions and isolated compounds in assays for anti-inflammatory activities. These were performed using mouse ear edema model, pleurisy and myeloperoxidase activity assays. Six compounds were isolated and identified as the flavanones swertisin and isovitexin, the alkaloid 4-hydroxy-N-methylproline, the triterpenes friedelin and lupeol, and the steroids sitosterol and stigmasterol. These compounds were identified by nuclear magnetic resonance of (1)H and (13)C data, in comparison with literature.

Topics: Animals; Anti-Inflammatory Agents; Apigenin; Edema; Fabaceae; Magnetic Resonance Spectroscopy; Mice; Pentacyclic Triterpenes; Plant Extracts; Plant Leaves; Proline; Sitosterols; Stigmasterol; Triterpenes

The methanol crude extract of the leaves of Ficus radicans Roxb. 'Variegata' (Moraceae) and the n-hexane, ethyl acetate and aqueous methanol fractions resulting from its fractionation were evaluated for their anti-inflammatory, molluscicidal and free-radical scavenging activities. The crude extract and fractions exhibited significant inhibition of inflammation in both croton oil (CO)-induced ear oedema in mice (p<0.001) and carrageenan-induced rat paw oedema models (p<0.01). The molluscicidal assay against Biomphalaria glabrata showed a weak activity for the n-hexane fraction (DL(50)= 400 µg mL(-1)). A moderated 1,1-diphenyl-1-picrylhydrazyl (DPPH) free-radical scavenging activity was observed for the ethyl acetate fraction (IC(50)= 66.2 µg mL(-1)). Fractionation of the extracts through chromatographic methods afforded the coumarins 7-methoxycoumarin, 7-hydroxy-6-methoxycoumarin and methoxy-3,4-dihydrocoumarin, the steroids β-sitosterol and β-sitosterol 3-O-β-glucopyranoside, as well as a cinnamic acid derivative and a flavonoid identified as trans-4-methoxy-2-β-D-glucopyranosyloxy cinnamic acid and quercetin 3-O-β-D-xylopyranosyl-(1 → 2)-α-L-rhamnopyranoside, respectively. The compounds were identified on the basis of their NMR spectral data and comparison with those previously reported in the literature.

Topics: Animals; Anti-Inflammatory Agents; Biomphalaria; Biphenyl Compounds; Carrageenan; Cinnamates; Croton Oil; Drug Evaluation, Preclinical; Edema; Ficus; Free Radical Scavengers; Glucosides; Male; Mice; Molecular Structure; Molluscacides; Monosaccharides; Picrates; Plant Extracts; Plant Leaves; Quercetin; Rats; Rats, Wistar; Scopoletin; Sitosterols

Nine compounds have been isolated for the first time from Celtis africana, namely trans-N-coumaroyltyramine (1), trans-N-feruloyltyramine (2), trans-N-caffeoyltyramine (3), lauric acid (4), oleic acid (5), palmitic acid (6), lupeol (7), β-sitosterol (8) and oleanolic acid (9), respectively. Their structures have been elucidated by different spectroscopic techniques. The isolated compounds were screened for their antioxidant, anti-inflammatory and acetylcholinestrease enzyme inhibitory activities. Compounds 1-3 showed significant antioxidant and anti-inflammatory activities and weak to moderate acetylcholinestrease enzyme inhibition activity.

Topics: Amines; Animals; Cannabaceae; Carrageenan; Cholinesterase Inhibitors; Edema; Fatty Acids; Female; Free Radical Scavengers; Male; Oleanolic Acid; Pentacyclic Triterpenes; Phenols; Plant Components, Aerial; Plant Extracts; Rats; Rats, Wistar; Sitosterols

The roots of Cyathula officinalis Kuan are widely used in Chinese medicine for the treatment of inflammatory disorders. Here, the ability of C. officinalis Kuan to downregulate matrix metalloproteinase (MMP)-13 was examined since MMP-13 is an important enzyme for the degradation of the cartilage collagen matrix, especially under arthritic conditions. The ethanol extract of C. officinalis Kuan as well as the N-hexane and chloroform soluble fractions were found to potently inhibit MMP-13 induction in IL-1 β-treated SW1353 cells, a human chondrosarcoma cell line, at 50-200 µg/mL. Activity-guided separation led to the isolation of six compounds, palmitic acid (1), β-sitosterol (2), α-spinasterol (3), atractylenolide I (4), 1,3-diacetoxy-tetradeca-6E,12E-dien-8,10-dyn (5), and N-trans-feruloyl-3-methyldopamine (6). Among these, 4 and 5 exhibited MMP-13 downregulating activity in IL-1 β-treated SW1353 cells. And 4 also showed anti-oedematous activity against λ-carageenan-induced paw edema in mice at 20-200 mg/kg, p. o. The results of this study provide information that can help elucidate the action mechanism of C. officinalis Kuan. In addition, the results presented here suggest that C. officinalis Kuan and its constituents may have the potential for chondroprotection against cartilage degrading disorders.

Topics: Acetates; Alkynes; Amaranthaceae; Animals; Carrageenan; Cartilage; Cell Line, Tumor; Chondrocytes; Chondrosarcoma; Disease Models, Animal; Dopamine; Down-Regulation; Edema; Humans; Hypolipidemic Agents; Interleukin-1beta; Lactones; Male; Matrix Metalloproteinase 13; Medicine, Chinese Traditional; Mice; Mice, Inbred ICR; Phytotherapy; Plant Extracts; Plant Roots; Sesquiterpenes; Sitosterols; Stigmasterol

Beta-sitosterol and beta-sitosteryl-beta-D-glucoside were isolated as analgesic constituents from the leaves of Mentha cordifolia Opiz. The acetic acid-induced writhing test showed that beta-sitosterol and beta-sitosteryl-beta-D-glucoside decreased the number of squirms induced by acetic acid by 70.0% and 73.0%, respectively, at a dose of 100 mg / kg mouse. Statistical analysis using the Kruskall Wallis one-way analysis of variance by ranks showed that these isolates approximate the analgesic activity of mefenamic acid at a 0.001 level of significance. The hot plate method confirmed their analgesic activities, as beta-sitosterol and beta-sitosteryl-beta-D-glucoside exhibited a 300% and 157% increase in pain tolerance, respectively, while mefenamic acid, a known analgesic, showed a 171% increase. Neither isolate exhibited antiinflammatory activity using the carrageenan-induced mouse paw oedema assay. Beta-sitosterol also exhibited anthelminthic and antimutagenic activities. In vitro tests using live Ascaris suum as test animals showed that the behaviour of worms treated with beta-sitosterol approximated that of the positive controls, Combantrin and Antiox. An in vivo micronucleus test showed that beta-sitosterol inhibited the mutagenicity of tetracycline by 65.3% at a dose of 0.5 mg /kg mouse. At the same dose, it did not exhibit chromosome-breaking activity.

Topics: Acetic Acid; Analgesics; Animals; Anthelmintics; Anti-Inflammatory Agents; Ascaris suum; Drug Evaluation, Preclinical; Edema; Extremities; Gas Chromatography-Mass Spectrometry; Hot Temperature; Mefenamic Acid; Mentha; Mice; Micronucleus Tests; Pain; Pain Threshold; Plant Extracts; Plant Leaves; Plants, Medicinal; Sitosterols

We have produced a chloroform extract from Achillea which includes stigmasterol and sitosterol. By comparing it with the pure compounds an anti-inflammatory effect (with mouse ears) is assumed. The topical anti-inflammatory effect of the chloroform extract from Achillea ageratum (Asteraceae) and of stigmasterol and beta-sitosterol, isolated of this extract has been evaluated, against to 12-0-tetradecanoylphorbol acetate (TPA)-induced mouse ear edema, using simple (acute model) and multiple applications (chronic model) of the phlogistic agent. Myeloperoxydase activity also was studied in the inflamed ears. In the acute model the extract exerted a dose-dependent effect. All the doses assayed (1, 3 and 5 mg/ear) significantly reduced the edema (50%, 66% and 82%, respectively). The isolated sterols stigmasterol and beta-sitosterol (with doses of 0.5 mg/ear) had similar effect as the extract with doses of 1 and 3 mg (59% and 65% respectively). In the chronic model the anti-inflammatory effect generally was a more moderate one. The highest dose of the extract decreased the edema reduction to 26% with the highest dose of the extract applied. With the compounds the effect decreased to 36% with stigmasterol, and 40.6% with beta-sitosterol. Myeloperoxydase activity (MPO) was reduced by the extract and the compounds in the acute model, however, in the chronic edema, the enzyme inhibition was very weak with all treatments even with the standard substance. These results indicate that the chloroform extract of Achillea ageratum and some of the its components stigmasterol and beta-sitosterol are more effective as topical anti-inflammatory agents in acute than in the chronic process and their action is markedly influenced by the inhibition of neutrophil migration into inflamed tissue.

Topics: Acute Disease; Animals; Anti-Inflammatory Agents; Chloroform; Chronic Disease; Dexamethasone; Disease Models, Animal; Ear; Edema; Indomethacin; Mice; Peroxidase; Plant Extracts; Plants, Medicinal; Sitosterols; Stigmasterol; Tetradecanoylphorbol Acetate

Topics: Adenosine Diphosphate; Animals; Anti-Inflammatory Agents, Non-Steroidal; Arachidonic Acid; Areca; Aspirin; Chromatography, Liquid; Edema; Humans; Plants, Medicinal; Platelet Activating Factor; Platelet Aggregation; Platelet Aggregation Inhibitors; Rats; Sitosterols; Triterpenes

Topics: Animals; Anti-Inflammatory Agents; Anti-Inflammatory Agents, Non-Steroidal; Edema; Female; Fever; Male; Rats; Sitosterols; Stomach Ulcer