phytosterols and Edema

To evaluate changes on cutaneous microangiopathy in chronic venous disorder (CVD) after use of Cirkan [venotonic drug containing Ruscus aculeatus (plant extract), hesperidine methylchalcone (flavonoid) and vitamin C], elastic compression stockings (ECS) or no treatment for four weeks.. Fifty-five female patients (85 legs), 25 to 57 years, with at least one limb classified as C2,s or C2,3,s (CEAP classification), were allocated consecutively, according to entrance order, in these three groups. Ten healthy women age-matched were also investigated. Using orthogonal polarization spectral technique (noninvasive method), measurements of functional capillary density (FCD, number of capillaries with flowing red blood cells/mm(2)), capillary morphology (CM, % of abnormal capillaries/mm(2)) and diameters (mum) of dermal papilla (DDP), capillary bulk (DCB) and capillary limb (CD) were obtained on the medial perimalleolar region and later analyzed using CapImage software.. CVD patients showed significant changes on CD and CM compared to healthy subjects in agreement with our previous findings (J Vasc Surg 43:1037-1044, 2006). On Cirkan-treated patients, after 4 weeks, CD decreased on both limbs and CM improved on the left one, suggesting an amelioration of the chronic venous hypertension. No significant changes could be detected on other patient groups. These results confirm the existence of microcirculatory dysfunction in early stages of CVD, probably due to post-capillary hypertension, and further support the venotonic action of Cirkan.

Topics: Adult; Ascorbic Acid; Capillaries; Chymotrypsin; Combined Modality Therapy; Drug Combinations; Edema; Female; Hesperidin; Humans; Leg; Microcirculation; Middle Aged; Phytosterols; Plant Extracts; Stockings, Compression; Treatment Outcome; Trypsin; Venous Insufficiency; Venous Thrombosis

Despite the usefulness of glucocorticoids, they may cause hazardous side effects that limit their use. Searching for compounds that are as equally efficient as glucocorticoids, but with less side effects, the current study compared plant steroids, namely, glycyrrhetinic acid, guggulsterone, boswellic acid, withaferin A, and diosgenin with the classical glucocorticoid, fluticasone. This was approached both

Topics: Animals; Anti-Inflammatory Agents; Croton Oil; Diosgenin; Ear Diseases; Edema; Enzyme-Linked Immunosorbent Assay; Glycyrrhetinic Acid; Inflammation; Interleukin-6; Mice; Molecular Docking Simulation; Phytosterols; Pregnenediones; Rats; Receptors, Glucocorticoid; Software; Thymus Gland; Triterpenes; Tumor Necrosis Factor-alpha; Withanolides

Cycloeucalenone (1) and 24-oxo-31-norcycloartanone (2) obtained from Solanum cernuum Vell. were assayed to explore their pharmacologic roles. Previous studies showed that (2) has selective activity against lung tumor cell line (NCIH460) which expresses high levels of COX-2, suggesting its role in inflammatory process, and also a link between chronic inflammation and cancer-associated process. Dichloromethane crude extract (DCE) significantly reduced writhing and stretching induced by 0.8 % acetic acid at a dose of 100, 300, and 600 mg/kg, po; oral administration of different doses of (1) and (2) also displayed significant analgesic and anti-inflammatory effects in the writhing acetic acid test (p < 0.0001). Selected oral doses of both compounds (100 and 50 mg/kg) were assayed in the carrageenan-induced paw edema model. Compound (2) showed significant activity during the early phase (1.5-6 h) and also in the late phase (48 h) (p < 0.01). The anti-nociceptive activity observed for the compounds (1) and (2) and DCE was found to be related to the inhibition of different mediators involved in inflammation and nociceptive process. Both compounds decrease COX-2 protein expression, although only compound (2) reached a significant response (p < 0.05 vs control). However, in vitro Sirtuin 1 activity and TNF-α production in THP-1 macrophages were not affected.

Topics: Analgesics; Animals; Anti-Inflammatory Agents; Edema; Mice; Mice, Inbred BALB C; Pain; Phytosterols; Plant Extracts; Solanum; Triterpenes

Lopezia racemosa Cav. is a plant used in Mexican traditional medicine to heal inflammatory diseases. From this plant we isolated the novel compound 6-O-palmitoyl- 3-O-β-D-glucopyranosylcampesterol (1) and 6-O-palmitoyl-3-O-β-D-glucopyranosyl-β-sitosterol (2), previously reported to have cytotoxic activity on several cancer cell lines. We evaluated the anti-inflammatory activity of 1 in vivo by mouse ear edema induced with 12-O-tetradecanoylphorbol-13-acetate (TPA) and 57.14% inhibition was observed. The aim of our study was to obtain callus cultures derived from this plant species with the ability to produce the compounds of interest. Callus cultures were initiated on MS basal medium amended with variable amounts of naphthaleneacetic acid (NAA), or 2,4-dichlorophenoxyacetic acid (2,4-D), combined or not with 6-benzylaminopurine (BAP). Ten treatments with these growth regulators were carried out, using in vitro germinated seedlings as source of three different explants: hypocotyl, stem node, and leaf. Highest yield of 1 was observed on callus derived from leaf explants growing in medium containing 1.0 mg/L 2,4-D and 0.5 mg/L BAP. Selected callus lines produced less 1 than wild plants but the in vitro cultured seedlings showed higher production. So we conclude that it could be attractive to further investigate their metabolic potential.

Topics: Animals; Anti-Inflammatory Agents; Cells, Cultured; Cholesterol; Ear; Edema; Germination; Inflammation; Male; Mice; Onagraceae; Phytochemicals; Phytosterols; Plant Extracts; Seeds; Tetradecanoylphorbol Acetate

Gorgonians of the genus Eunicella are known for possessing a wide range of pharmacological activities such as antiproliferative and antibacterial effect. The aim of this study was to evaluate the anti-inflammatory and gastroprotective effect of the organic extract and its semi-purified fractions from the white gorgonian Eunicella singularis and the isolation and identification of pure compound(s) from the more effective fraction.. Anti-inflammatory activity was evaluated, using the carrageenan-induced rat paw edema test and in comparison to the reference drug Acetylsalicylate of Lysine. The gastroprotective activity was determined using HCl/EtOH induced gastric ulcers in rats. The purification of compound(s) from the more effective fraction was done by two chromatographic methods (HPLC and MPLC). The structure elucidation was determined by extensive spectroscopic analysis (1H and 13C NMR, COSY, HMBC, HMQC and NOESY) and by comparison with data reported in the literature.. The evaluation of the anti-inflammatory activity of different fractions from Eunicella singularis showed in a dependent dose manner an important anti-inflammatory activity of the ethanol fraction, the percentage of inhibition of edema, 3 h after carrageenan injection was 66.12%, more effective than the reference drug (56.32%). In addition, this ethanolic fraction showed an interesting gastroprotective effect compared to the reference drugs, ranitidine and omeprazol. The percentage of inhibition of gastric ulcer induced by HCl/ethanol in rats was 70.27%. The percentage of the reference drugs (ranitidine and omeprazol) were 65 and 87.53%, respectively. The purification and structure elucidation of compound(s) from this ethanolic fraction were leading to the isolation of five sterols: cholesterol (5α-cholest-5-en-3β-ol) (1); ergosterol (ergosta-5,22-dien-3β-ol) (2); stigmasterol (24-ethylcholesta-5,22-dien-3b-ol) (3); 5α,8α-epidioxyergosta 6,22-dien-3β-ol (4) and 3β-hydroxy-5α,8α-epidioxyergosta-6-ene (5); and one diterpenoid: palmonine D (6).. Based on data presented here, we concluded that diterpenoids and sterols detected in the ethanolic fraction can be responsible for its pharmacological activity.

Topics: Animals; Anthozoa; Anti-Inflammatory Agents; Anti-Ulcer Agents; Carrageenan; Disease Models, Animal; Diterpenes; Drug Discovery; Edema; Ethanol; Female; Hydrochloric Acid; Male; Phytosterols; Rats; Rats, Wistar; Stomach Ulcer

Leea macrophylla (Leeaceae) is a wild edible plant with ethomedicinal importance as anti-inflammatory agent. However, no systematic studies on its anti-inflammatory activity and mechanisms have been reported. Present study was undertaken to evaluate anti-inflammatory activity of methanol extract of L. macrophylla leaves. Phytochemical investigation revealed presence of sterols, triterpenoids and ascorbic acid in extract. Methanol extract inhibited lipopolysaccharide stimulated production of inflammatory mediators viz. prostaglandin E2, tumor necrotic factor-α, interleukin-6 and interleukin-1β in vitro in mouse peritoneal macrophages. Additionally, the in vivo anti-inflammatory activity of this extract was evaluated by using carrageenan induced paw edema and cotton pellet granuloma assays in experimental rats. Oral administration of extract (100 and 200 mg/kg) exhibited dose dependant inhibition of carrageenan induced inflammation (p<0.05) and the reduction of the granuloma tissue formation (p<0.05-0.01). The extract (100 and 200 mg/kg, orally) exhibited significant central and peripheral analgesic activity in hot-plate test (p<0.01) and acetic acid induced writhing test (p<0.05-0.01) respectively in experimental mice. Treatment with extract (100 and 200 mg/kg, orally) significantly reduced the yeast provoked elevated body temperature (p<0.05-0.01) in experimental rats. These results confirmed the traditional anti-inflammatory indication of L. macrophylla leaves.

Topics: Animals; Anti-Inflammatory Agents; Ascorbic Acid; Cells, Cultured; Dietary Supplements; Edema; Ethnopharmacology; Granuloma; India; Macrophages, Peritoneal; Medicine, Traditional; Mice; Mice, Inbred Strains; Phytosterols; Plant Extracts; Plant Leaves; Rats; Rats, Wistar; Toxicity Tests, Acute; Toxicity Tests, Subacute; Triterpenes; Vitaceae

With reference to the ethnopharmacological significance of Vitex doniana Sweet (Lamiaceae) leaves in the treatment of stomach and rheumatic pains as well as inflammatory disorders, biological studies on its stem bark extracts have also reported anti-inflammatory and analgesic activities, with no attempt to identify the active components. Chromatographic and spectroscopic procedures identified three new phytoecdysteroids: 21-hydroxyshidasterone (1), 11β-hydroxy-20-deoxyshidasterone (2), and 2,3-acetonide-24-hydroxyecdysone (3) from the stem bark methanol extracts along with known ecdysteroids shidasterone (4), ajugasterone C (5), 24-hydroxyecdysone (6), and 11β,24-hydroxyecdysone (7). The compounds (1-7) showed significant (p ≤ 0.05) inhibitory effect at 100 mg/kg dose on rat paw oedema development due to carrageenan-induced inflammation in Sprague Dawley rats. These results suggest a possible contribution of ecdysteroids to the anti-inflammatory effect of some V. doniana stem bark extracts.

Topics: Administration, Oral; Animals; Anti-Inflammatory Agents; Carrageenan; Ecdysteroids; Edema; Female; Lethal Dose 50; Male; Phytosterols; Plant Bark; Plant Extracts; Plant Stems; Random Allocation; Rats; Rats, Sprague-Dawley; Toxicity Tests, Acute; Vitex

Alchornea floribunda (Euphorbiaceae) leaves are widely used in African ethnomedicine for the management of acute and chronic inflammatory disorders. In the present study, bioactivity-guided fractionation led to the isolation of two known (1 and 3) and one new (2) stigmastane steroids from the hexane extract of Alchornea floribunda leaves. The anti-inflammatory activities of these compounds were evaluated using IN VITRO and IN VIVO animal models. The compounds 1, 2, and 3 at 50 and 100 microg/ear significantly (p < 0.05) inhibited xylene-induced ear edema in mice in a dose-dependent manner. The topical anti-inflammatory effect of 1 and 2 are significantly (p < 0.05) higher than that of indomethacin and prednisolone. At 20 mg/kg (i. p.), all the compounds significantly (p < 0.05) inhibited acute inflammation induced by subplantar injection of egg albumen in rats. Compound 1 exhibited an anti-inflammatory effect (50.9 % edema inhibition) comparable (p < 0.05) to that of prednisolone (48.0 % edema inhibition) at 3 h. Compounds 1, 2, and 3 (50 microg/mL) significantly (p < 0.05) inhibited heat-induced haemolysis of human erythrocytes in vitro, but had no effect on hypotonicity-induced hemolysis. The compounds were elucidated as (24R)-5alpha-stigmast-3,6-dione ( 1), 5alpha-stigmast - 23-ene-3,6-dione ( 2), and 3beta-hydroxy-5alpha-stigmast-24-ene ( 3) by spectral analysis. The results of this study show that these compounds may, in part, account for the anti-inflammatory effect of Alchornea floribunda leaves. This is the first report on the isolation and structure elucidation of these anti-inflammatory steroids from Alchornea floribunda leaves.

Topics: Animals; Anti-Inflammatory Agents; Cell Membrane; Cholestenones; Dose-Response Relationship, Drug; Edema; Erythrocytes; Euphorbiaceae; Hemolysis; Humans; Mice; Molecular Structure; Phytosterols; Phytotherapy; Plant Extracts; Plant Leaves; Rats; Rats, Wistar; Xylenes

Bioassay-guided fractionation of the anti-inflammation fractions of the Red Sea sponges Scalarispongia aqabaensis and Callyspongia siphonella yielded two new sterols from chloroform fractions of methanol extracts, namely scalaristerol (5alpha,8alpha-dihydroxycholest-6-en-3beta-ol) (1) from Scalarispongia aqabaensis, and callysterol (ergosta-5,11-dien-3beta-ol) (2) from Callyspongia siphonella. Structure determination was based on extensive NMR studies and mass spectrometry. The antiinflammatory activity of compounds 1 and 2 was assessed using the rat-hind paw edema method and by study of their effect on the release of O2(-) and TXB2 from LPS-activated rat neonatal microglia.

Topics: Animals; Anti-Inflammatory Agents; Callyspongia; Edema; Microglia; Molecular Structure; Phytosterols; Rats; Superoxides; Thromboxane B2

A new nor-pregnane derivative (2,6-dideoxy-3- O-methylpyranosylillustrol) (1), isolated from the ethyl acetate extract of Mandevilla illustris rhizomes, was identified by conventional spectral analysis and by chemical means. It markedly inhibited the rat paw oedema induced by carrageenan and, to a lesser extent, those induced by dextran, without affecting that caused by bradykinin.

Topics: Animals; Anti-Inflammatory Agents; Apocynaceae; Bradykinin; Carrageenan; Dextrans; Edema; Hindlimb; Magnetic Resonance Spectroscopy; Male; Molecular Structure; Phytosterols; Phytotherapy; Plant Extracts; Pregnanes; Rats; Rats, Wistar; Rhizome

The marine green alga, Ulva lactuca, was shown to contain 3-O-beta-D glucopyranosyl-stigmasta-5,25-dien. The structure of the compound was established on the basis of its spectroscopic data and it was extracted for the first time from this alga. The topical antiinflammatory activity of this compound was examined using the mouse ear oedema assay as an experimental model of topical inflammation. Also, the antimicrobial activity of the isolated compound was tested against 10 various microorganisms (G+, G-, fungi and yeast strains).

Topics: Administration, Topical; Animals; Anti-Bacterial Agents; Anti-Infective Agents; Anti-Inflammatory Agents; Chlorophyta; Chromatography, Gel; Chromatography, Thin Layer; Dose-Response Relationship, Drug; Edema; Egypt; Fungi; Gram-Negative Bacteria; Gram-Positive Bacteria; Magnetic Resonance Spectroscopy; Mass Spectrometry; Mice; Phytosterols; Yeasts

Eryngium foetidum L. (Apiaceae) is a Caribbean endemic plant, used in folk medicine for the treatment of several antiinflammatory disorders. A preliminary phytochemical study showed that the hexane extract is rich in terpenic compounds. Chromatographic fractionation of this extract yielded: alpha-cholesterol, brassicasterol, campesterol, stigmasterol (as the main component, 95%) clerosterol, beta-sitosterol, delta 5-avenasterol, delta (5)24-stigmastadienol and delta 7-avenasterol. The topical antiinflammatory activity of the hexane extract and of stigmasterol was evaluated by auricular oedema, induced by 12-0-tetradecanoylphorbol acetate (TPA), in the mouse, using single and multiple applications of the phlogistic agent. Both reduced the oedema in a similar proportion in the two model assays (acute and chronic). Meloperoxidase activity was strongly reduced by both the extract and the compound, in the acute but not the chronic model. These results indicate that the leaves of Eryngium foetidum L may be effective against topical inflammation processes. Stigmasterol also exerts a significant topical antiinflammatory activity although it cannot be considered to be a major antiinflammatory agent, therefore other bioactive components are probably involved in the activity of the hexane extract.

Topics: Acute Disease; Administration, Topical; Animals; Anti-Inflammatory Agents; Caribbean Region; Chronic Disease; Edema; Female; Inflammation; Mice; Peroxidase; Phytosterols; Plants, Medicinal; Tetradecanoylphorbol Acetate

The alcoholic extracts of the aerial portion and fruits of Aglaia roxburghiana (W.& A.) Miq. var. beddomei and the triterpenes roxburghiadiol A and B isolated from this plant were investigated for their anti-inflammatory activity in rats by carrageenin induced rat paw oedema and cotton pellet granuloma methods. They were also studied for their effect on mast cell degranulation induced by compound 48/80. Potent anti-inflammatory activity was observed for the extracts of the aerial portion and fruits of A. roxburghiana as well as for the triterpenes roxburghiadiol A and B. The mast cell degranulation induced by compound 48/80 was significantly reduced by A. roxburghiana extracts and the triterpenes. The triterpenes roxburghiadiol A and B may play a significant role in the observed anti-inflammatory effect of A. roxburghiana.

Topics: Analysis of Variance; Animals; Anti-Inflammatory Agents; Cell Degranulation; Edema; Hindlimb; India; Lethal Dose 50; Male; Mast Cells; Medicine, Ayurvedic; Mice; Phytosterols; Plant Extracts; Plants, Medicinal; Rats; Rats, Wistar

The plant Crataegus monogyna has action against cardiac insufficiency, angina and arrhythmia. The anti-inflammatory properties of the cycloartenol fraction from this plant have been investigated. Chromatographic fractionation of the hexane extract of Crataegus monogyna Jacq. (Rosaceae) furnished a triterpene fraction containing cycloartenol as the main component (80.87%). The anti-inflammatory activity of the fraction was tested against hind-paw oedema induced by carrageenan in rats. At the highest oral dose (40 mg kg-1) inhibition was 61.5 and 52.5% at 3 and 5 h respectively. In the mouse carrageenan peritonitis test, the triterpene fraction given orally inhibited peritoneal leucocyte infiltration (41.9, 64.7 and 89.4% at 10, 20 and 40 mg kg-1, respectively). The fraction also showed weak inhibition of phospholipase A2 (PLA2) in-vitro. These results suggest that the fraction containing cycloartenol as the main component exerts an important anti-inflammatory action in-vivo by reducing the oedema.

Topics: Animals; Anti-Inflammatory Agents; Anti-Inflammatory Agents, Non-Steroidal; Carrageenan; Cell Migration Inhibition; Edema; Indomethacin; Leukocytes; Male; Mice; Peritonitis; Phospholipases A; Phospholipases A2; Phytosterols; Plant Extracts; Plants, Medicinal; Prednisolone; Rats; Spain; Triterpenes

The oxygenated stigmastane-type sterols stigmastane-3 beta, 6 alpha-diol, stigmastane-3 beta, 6 beta-diol, 7 alpha-hydroxysitosterol and its diacetyl derivative, 7 beta-hydroxysitosterol and its diacetyl derivative, 7-oxositosterol, 4 beta-hydroxysitosterol, and stigmast-4-ene-3 beta, 6 beta-diol were evaluated with respect to their anti-inflammatory activity against 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation in mice. All of the sterols, with the exception of 7 alpha-hydroxysitosterol and its diacetyl derivative, were found to possess marked inhibitory activity. The 50% inhibitory dose of these compounds for TPA-inflammation (1 microgram) was 0.5--1.0 mg/ear.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Chromatography, High Pressure Liquid; Ear, External; Edema; Female; Inflammation; Mice; Mice, Inbred ICR; Phytosterols; Tetradecanoylphorbol Acetate

Topics: Animals; Anti-Inflammatory Agents; Capillary Permeability; Edema; Female; Foot Diseases; Male; Mice; Phytosterols; Rats; Stigmasterol

Topics: Animals; Ascorbic Acid; Chymotrypsin; Drug Combinations; Edema; Flavonoids; Male; Peptide Hydrolases; Phytosterols; Rats; Trypsin