Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Crotonates”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 541 records · Page 30Linked to original sources

Black cumin seed essential oil, as a potent analgesic and antiinflammatory drug.

The steam-distilled essential oil of Iranian black cumin seed (Nigella sativa L.) was investigated for its composition and analgesic and antiinflammatory properties. After oil analysis by GC/MS, 20 compounds were identified in the oil, obtained in 0.4% (v/w) yield. Among them, para-cymene (37.3%) and thymoquinone (13.7%) were the major components. Acetic acid-induced writhing, formalin and light tail flick tests were used for assessment of analgesic activity. Antiinflammatory activity was evaluated using carrageenan-induced paw oedema in rats and croton oil-induced ear oedema in mice. Black cumin seed essential oil (BCSEO) was found to produce a significant analgesic effect in acetic acid-induced writhing, formalin and light tail flick tests. Naloxone, an opioid antagonist, could not reverse the analgesic effect observed in the formalin test. Although oral administration of BCSEO at doses of 100, 200 and 400 micro L/kg did not exert a significant antiinflammatory effect in the carrageenan test, i.p. injection of the same doses significantly (p < 0.001) inhibited carrageenan-induced paw oedema. BCSEO at doses of 10 and 20 micro L/ear could also reduce croton oil-induced oedema. It seems that mechanism(s) other than opioid receptors is (are) involved in the analgesic effect of BCSEO since naloxone could not reverse this effect. Both systemic and local administration of BCSEO showed antiinflammatory activity. Thymoquinone, as one of the major components of BCSEO, probably has an important role in these pharmacological effects.

Acetic Acid↗

Estragole-induced behavioural changes in rats.

Croton zehntneri is a popular plant used in the Brazilian folk medicine. Recently, the use of its essential oil showed depressive activity on the central nervous system (CNS). Chemical studies show that estragole (ES) is one of the main compounds of this oil. This work seeks to evaluate the activity of ES on behaviour models of depression and anxiety, in rats. Male rats (60 days) were distributed to four groups (n = 10) and treated with 1.0, 3.0 and 10.0 microL/100 g body weight, v.o. of ES (experimental) and saline (control). Forced swimming and open-field parameters were unaffected by the ES treatment suggesting no alterations on depression behaviour. A decrease was observed in the total time of social interaction in the 10.0 microL/100 g group in relation to other groups. This group showed a reduction in the total entries frequency on the elevated plus-maze without differences to the other parameters of this test. No differences in holeboard parameters were observed suggesting no alterations in exploratory activity. These data suggest that administration of ES induced alterations in the CNS related to anxiety behaviour, expressed by the shortest total time in the social interaction model. Exposure to ES was capable of altering the motor activity in the plus-maze test. These data are antagonistic to those observed with the Croton zehntneri essential oil in these models.

Allylbenzene Derivatives↗

Topical antiinflammatory and analgesic activities of Copaifera duckei dwyer.

The oleoresin of several Copaifera species is used widely in the Amazonian Region mainly as a topical antiinflammatory and healing agent. The topical analgesic and antiinflammatory activities of Copaifera duckei oleoresin, whose terpenoidal chemical composition has been characterized, are now examined. Antiinflammatory activity was evaluated in rats using the carrageenin-induced paw edema and the granuloma tests, and in mice by the croton oil-induced dermatitis test. Analgesic activity was determined in mice using the writhing test method. In the carrageenin-induced edema and granuloma tests the oleoresin in a dose of 1,802 mg/kg inhibited the edema by 18% and granuloma by 42% (p < 0.05), this last result similar to that observed with dexamethasone. Topical doses of 517 mg/kg, 1,035 mg/kg and 1,802 mg/kg produced 52%, 58% and 62% (p < 0.05) reduction of the edema induced by croton oil, respectively, and 48%, 56% and 65% inhibition of the writhing process (p < 0.05). These results suggest that the Copaifera duckei oleoresin has topical antiinflammatory and analgesic activities.

Administration, Cutaneous↗

Protective effect of Picroliv, the active constituent of Picrorhiza kurroa, against chemical carcinogenesis in mice.

Cancer chemoprevention of chemically induced tumours by Picroliv, an iridoid glycoside mixture purified from Picrorhiza kurroa, was studied on 20-methylcholanthrene (20-MC)-induced sarcoma model and 7,12-dimethylbenz[a]anthracene (DMBA)-initiated papilloma formation in BALB/c mice. Administration of Picroliv (100 and 200 mg/kg, p.o) inhibited the sarcoma development by 47 and 53% as estimated on day 200 after 20-MC administration. Control animals started dying of tumour burden 76 days after 20-MC administration and all animals were dead by day 170, while 60 and 66% of the animals survived in the Picroliv treated group, 100 and 200 mg/kg, respectively. Picroliv exhibited anti-tumour-promoting activity on a two-stage carcinogenesis test on mouse skin using DMBA as an initiator and croton oil as a promoter. Topical application of Picroliv (1 and 5 mg/mouse) 30 minutes prior to that of croton oil application resulted in a 50 and 60% reduction in the number of animals that developed papillomas, and 48 and 64% reduction in the number of papillomas per mouse. There was also a delay in the onset of first skin tumour in the group of animals treated with Picroliv. Oral administration of Picroliv (150 mg/kg, p.o.) prior to DMBA application delayed the onset of papillomas and the percent of mice (60%) with tumours indicates that Picroliv inhibited the tumour initiation induced by DMBA. Picroliv administration was also found to increase the life span of transplanted Dalton's Lymphoma Ascites (DLA) and Ehrlich Ascites Carcinoma (EAC) harboring mice and reduced the volume of transplanted solid tumours.

9,10-Dimethyl-1,2-benzanthracene↗

Enhancement of the contact hypersensitivity reaction by acute morphine administration at the elicitation phase.

The present study investigated the effects of morphine on the irritant contact sensitivity (ICS) and contact hypersensitivity (CHS) reaction. ICS was induced by croton oil application on the pinnae of naïve rats. Morphine injected prior to croton oil application did not affect the ICS response when assessed by measurements of pinnae thickness. CHS was induced by applying the antigen 2,4-dinitro-1-fluorobenzene (DNFB) to the pinnae of rats sensitized to DNFB. Rats received an injection of morphine prior to either initial antigen exposure (sensitization) or antigen reexposure (challenge). Morphine prior to challenge, but not sensitization, resulted in a pronounced enhancement of the CHS response as measured by pinna thickness. Quantitative PCR also showed increased IFN-gamma mRNA levels in the inflamed tissue of morphine-treated rats. Naltrexone blocked the morphine-induced enhancement of the CHS response. The differential effects of morphine suggest that opioids have a more pronounced effect on in vivo immune responses that involve immunological memory.

Animals↗

Serum concentrations of alpha-macrofeto-protein (acute-phase alpha2-macroglobulin), a proteinase inhibitor, in pregnant and neonatal rats and in rats with acute inflammation.

Alpha macrofetoprotein (AMF) or acute-phase alpha2 macroglobulin serum concentrations are elevated in pregnant, fetal, and newborn rats and in rats with experimentally induced acute inflammation when quantitated using a double-antibody radioimmunoassay. Concentrations of AMF are 17 +/- 2 microgram/ml and 32 +/- 6 microgram/ml in normal adult rat sera. Both maternal (1.2 mg/ml) and neonatal (9.3 mg/ml) concentrations are maximal at term. AMF serum concentrations of rats injected with croton oil into the hind footpads are unchanged for the first 4 h after injection, then increase to a maximum of 10.5 mg/ml 36 h after injection. Serum AMF concentrations correlate directly with the dose of croton oil and the increase in size (swelling) of the injured foot, and remain elevated during the course of inflammation for at least two weeks. The possible function of AMF as an antiproteinase limiting the extent of inflammation after acute tissue injury is discussed.

Aging↗

Two simple methods for the evaluation of topically active anti-inflammatory steroidal ointments.

Simple laboratory methods for quantitating the topical anti-inflammatory activity of steroidal ointments are described. One is of croton oil ear edema in rats and the other is a new method using homologous passive cutaneous anaphylaxis (PCA) in rats. In order to avoid problems such as the animals' licking and/or rubbing the ointment at the applied sites, which might result in oral uptake, each rat was housed individually and fitted with a plastic collar in the croton oil experiment. The sites of ointment application in the PCA experiment were covered with adhesive plaster. Optimal experimental conditions were as follows. In the former method, ointments were applied to the inside surface of the ear 5 min after the irritant treatment and anti-edematous activity was determined after 6 h. In the latter, ointments were applied 3 h before the antigenic challenge to the dorsal area of animals which had been passively sensitized by anti-serum, and inhibition of the increased permeability was determined 45 min after the challenge. These methods were found to be reliable with respect to sensitivity and reproducibility of data. Ointments of halcinonide, betamethasone-17-valerate, hydrocortisone-17-butyrate, fluocinonide, flumethasone-21-pivalate and beclomethasone-17,21-dipropionate were evaluated by these methods.

Administration, Topical↗

Anti-oedematous action of some H1-receptor antagonists.

The oedema disk technique was used to study the effects of orally administered H1-receptor antagonists (cetirizine, chloropyramine, clemastine, cyproheptadine, dimethindene, loratadine, mequitazine and terfenadine) on the inflammation induced with capsaicin or croton oil in the mouse ear, and the effect of topically applied dimethindene maleate gel on the inflammation induced with croton oil in the mouse ear. In rats of the Wistar strain, oedema was induced in the hind paw by the subplantar injection of dextran or compound 48/80. Preliminary antihistamine treatment inhibited the development of oedema in the mouse ear, and of oedema in the rat paw, to statistically significant extents, in a dose-dependent manner. In all experiments, the most potent drugs were loratadine and cyproheptadine.

Animals↗

Macrolide antibiotics as antiinflammatory agents: roxithromycin in an unexpected role.

The antiinflammatory activity of a new 14-membered macrolide antibiotic, roxithromycin, was evaluated in various rat models including carrageenan- and poly-L-arginine-induced hind-paw oedema, croton oil inflamed ear assay and polyester sponge granuloma. When administered orally to animals, roxithromycin displayed an atypical profile in the assays utilized, including: (1) marked antioedema activity similar to that of indomethacin in poly-L-arginine assay, (2) significant inhibition of lambda-carrageenan hind-paw oedema and croton-oil-induced inflammation in the ear, although indomethacin was more effective, and (3) failure to reduce the development of granuloma induced by implanted polyester sponges, while indomethacin significantly reduced the chronic inflammatory reaction. Based on these results, it is concluded that roxithromycin is active in reducing the acute inflammatory reaction in rat models through mechanisms different from conventional nonsteroidal antiinflammatory agents such as indomethacin. Therefore, roxithromycin may have a favorable impact on skin inflammatory reactions accompanying microbial infections.

Analysis of Variance↗

Sporotomaculum syntrophicum sp. nov., a novel anaerobic, syntrophic benzoate-degrading bacterium isolated from methanogenic sludge treating wastewater from terephthalate manufacturing.

An anaerobic, mesophilic, syntrophic benzoate-degrading bacterium, designated strain FB(T), was isolated from methanogenic sludge which had been used to treat wastewater from the manufacture of terephthalic acid. Cells were non-motile gram-positive rods that formed spores. The optimum temperature for growth was 35-40 degrees C, and the optimum pH was 7.0-7.2. A co-culture with the hydrogenotrophic methanogen Methanospirillum hungatei converted benzoate to acetate, carbon dioxide, and methane. Butyrate transiently accumulated at a high concentration of 2.5 mM during degradation. Besides benzoate, no other compound tested supported growth of the co-culture. Crotonate supported growth of strain FB(T) in pure culture. Furthermore, the strain degraded benzoate in pure culture with crotonate as co-substrate to produce acetate and butyrate. The strain was not able to utilize sulfate, sulfite, thiosulfate, nitrate, fumarate, or Fe(III) as electron acceptor. The G+C content of the DNA was 46.8 mol%. Strain FB(T) contained MK-7 as the major quinone and C(16:1) as the major fatty acid. 16S rDNA sequence analysis revealed that the strain was a member of the genus Sporotomaculum, even though it exhibited significant differences, such as the capacity for syntrophic growth, to the known member of the genus. Hence, we propose the name Sporotomaculum syntrophicum sp. nov. for strain FB(T). The type strain is strain FB(T) (DSM 14795, JCM 11475).

Bacteria, Anaerobic↗

Anti-inflammatory activity of amylin and CGRP in different experimental models of inflammation.

The anti-inflammatory activity of amylin was studied in different models of inflammation, and compared to that of CGRP. Both peptides were active against mouse ear oedema induced by croton oil and acetic acid-induced peritonitis in the rat. CGRP was more potent than amylin in both models. Pretreatment with CGRP 8-37 fragment blocked the anti-inflammatory activity of both peptides in croton oil ear oedema. No anti-inflammatory activity was evidenced against serotonin-induced rat paw oedema and plasma protein extravasation induced by dextran in rat skin. Our results suggest that amylin exerts anti-inflammatory activity only in inflammatory models characterized by a vascular component. This effect appears to be mediated by the involvement of CGRP receptors.

Amyloid↗

Effect of RU 486 on the atrophogenic and antiinflammatory effects of glucocorticoids in skin.

Clobetasol-17-propionate (CP), a synthetic glucocorticoid (GC), reduced skin thickness in rats. Both the subcutaneous injection and topical applications of RU 486 counteracted CP-induced reduction in skin thickness. Topical application of the CP cream completely inhibited the ear edema produced by croton oil. A less potent GC, hydrocortisone-17-butyrate, also inhibited ear edema. This antiinflammatory effect was not abolished by the subcutaneous injection or topical application of RU 486. These observations suggest that GC-induced skin atrophy is mediated by glucocorticoid receptors (GRs), while the inhibition of croton oil-induced inflammation by GC is primarily related to the direct effects of GC, which are not mediated by GRs. Our findings suggest that RU 486 inhibits the atrophogenic effect of GCs without interfering with their antiinflammatory effect. Dissociation of antiinflammatory and atrophogenic activity of GC seems favorable in treating inflammatory skin diseases lacking epidermal proliferation.

Animals↗

Dynamic swelling behavior of gamma-radiation induced polyelectrolyte poly(AAm-co-CA) hydrogels in urea solutions.

The aim of this study was to investigate the equilibrium swelling properties in urea solutions of gamma-radiation induced polyelectrolyte copolymeric hydrogels consisting of acrylamide (AAm) and crotonic acid (CA). Poly(acrylamide-co-crotonic acid), poly(AAm-co-CA) hydrogels containing different amounts of CA were obtained in the form of rods after radiation. Swelling experiments were performed in aqueous urea solutions at 25 degrees C, gravimetrically. The hydrogels showed large extents of swelling in aqueous (urea/water) media the swelling being highly dependent on the chemical composition of the hydrogels and irradiation dose. The percentage swelling of poly(AAm-co-CA) hydrogels was between 1160 and 4250%, while that of the AAm hydrogels was between 670 and 900%. The diffusional exponent values (n) are between 0.51 and 0.66, hence the diffusion of urea/water into the hydrogels is non-Fickian. Equilibrium urea/water contents of the hydrogel systems were changed between 0.870 and 0.977.

Acrylamides↗

In vivo anti-inflammatory activity of Alchornea cordifolia (Schumach. & Thonn.) Müll. Arg. (Euphorbiaceae).

Alchornea cordifolia (Schumach. & Thonn.) Müll. Arg. (Euphorbiaceae) is a widely distributed plant in Africa. It is used in the traditional medicine of many African countries for the treatment of bacterial, fungal, parasitic and inflammatory disorders. Aqueous decoction and methanol leaf extracts were tested for their ability to reduce Croton oil-induced oedema in the mouse ear, after topical application. The methanol leaf extract dose-dependently inhibited the Croton oil-induced ear oedema in mice (ID(50)<500 microg/cm(2)). A bio-assay guided liquid-liquid fractionation of this methanol extract gave four active fractions: water insoluble (F1), hexane (F2), ethyl acetate (F3) and water (F4). The hexane fraction showed a very high activity (42% inhibition at 0.7 microg/cm(2)) as compared to the control. The other fractions were less active (F1: 56% at 506.2 microg/cm(2); F3: 57% at 289.3 microg/cm(2); F4: 32% for 203.8 microg/cm(2)) while indomethacin gave 49% of inhibition at 90 microg/cm(2). The activity of F1 and F3 may be at least in part explained by the presence of anti-inflammatory flavonoids (hyperoside and quercitrin, quercitrin being identified in the plant for the first time) while the activity was not correlated to the tannin contents. None of these compounds were detected in the most active F2 fraction. These results support the reported traditional use of this plant against topical inflammatory disorders.

Administration, Topical↗

Studies on the immune status of patients with renal adenocarcinoma.

Thirty-one patients with renal carcinoma were divided into 3 groups according to the stage of the disease and evaluated with skin tests to determine cell-mediated immunity and an in vitro chemostaxis assay to measure monocyte function. The patients demonstrated a significant defect in monocyte function, that is the ability to undergo chemotaxis when compared to healthy controls and patients with non-neoplastic disease (p less than 0.001). The defect tended to be more severe in patients with advanced disease. Improvements in monocyte function occurred following nephrectomy in patients with localized disease. The patients were skin tested with recall antigens and dinitrochlorobenzene to determine the presence of a delayed cutaneous hypersensitivity response. Croton oil was used to evaluate the non-specific inflammatory response. These studies indicate that a defect exists in cellular immunity as well as the inflammatory response. Patients with advanced disease tend to be unresponsive to these skin tests while those with localized disease are more likely to react to dinitrochlorobenzene and croton oil.

Adenocarcinoma↗

New steroidal antiinflammatory antedrugs: Methyl 3,20-dioxo-9 alpha-fluoro-11 beta,17 alpha,21-trihydroxy-1,4-pregnadiene-16 alpha-carboxylate and its 21-O-acyl derivatives.

In a continuing effort to increase local to systemic activity ratios of potent steroidal antiinflammatory antedrugs, a series of 21-O-acyl derivatives of methyl 3,20-dioxo-9 alpha-fluoro-11 beta,17 alpha,21-trihydroxy-1,4-pregnadiene-16 alpha-carboxylate, FP16CM, were synthesized. These derivatives were evaluated for antiinflammatory activity and their adverse effects in an acute and semi-chronic croton oil-induced ear edema bioassay. Following a single topical application in the croton oil-induced ear edema bioassay, treatment with all the compounds resulted in dose-dependent inhibition of edema. From these dose-response profiles, the following ID(50) values (nmol/ear resulting in a 50% reduction of edema) were calculated: prednisolone (Pred); 454, FP16CM; 255, 21-acetate (FP16CM-acetyl); 402, 21-propionate (FP16CM-propionyl); 474, 21-valerate (FP16CM-valeryl); 446 and 21-pivalate (FP16CM-pivalyl); 219 nmol. In a 5-day semi-chronic study at the equipotent doses, the novel steroidal antedrugs did not significantly alter body weight gain, thymus weights or plasma corticosterone levels unlike the parent compound Pred. The compounds were assessed for high-affinity glucocorticoid receptor binding and glucocorticoid-mediated inhibition of nitric oxide (NO) generation in an in vitro RAW 264.7 macrophage cell culture system. Binding affinities for cytosolic glucocorticoid receptors were Pred; 85, FP16CM-acetyl; 86, FP16CM-propionyl; 169, FP16CM-valeryl; 149, FP16CM-pivalyl; 126 nM, respectively. Concomitant potencies for inhibition of NO generation by macrophages stimulated with lipopolysaccharide were Pred; 159, FP16CM-acetyl; 377, FP16CM-propionyl; 405, FP16CM-valeryl; 344, FP16CM-pivalyl; 311 nM, respectively. Collectively, results of these investigations suggest that esterification of 21-OH with various anhydrides did not improve receptor binding, inhibition of NO generation and ear edema inhibition, however, serum corticosterone level and local over systemic activities (L/S) were markedly improved.

Animals↗

Clinicopathologic spectrum of primary uveal melanocytic lesions in an animal model.

BACKGROUND: Currently, there are no animal models of primary uveal melanoma in an eye large enough to allow documentation of the clinical evolution of the lesion by either funduscopy or fundus photography. METHODS: The authors induced primary uveal melanocytic lesions in the eyes of Dutch (pigmented) rabbits using a two-stage carcinogenesis protocol involving initiation with 4 weekly topical applications of 10 microliters of a 1% solution of 7,12-dimethyl-benz[a]anthracene (DMBA) in acetone (21 eyes) followed by 12 weekly topical applications of a 10 microliters solution of either 0.25% or 0.5% croton oil in acetone. They also investigated the effect of initiation with DMBA without promotion and the effects of chronic topical exposure to acetone and proparacaine. RESULTS: Exposure to DMBA followed by promotion with croton oil in either concentration was the most effective means of inducing clinically detectable fundus lesions. Histologically, a spectrum of melanocytic proliferations developed including benign nevi, nevi with varying grades of cytologic atypia, and clusters of confluent atypical melanocytes that may represent early melanomas. Although clinical regression of fundus lesions was noted in eight eyes after promotion had been stopped, five of these eyes showed unequivocal histologic evidence of a residual uveal melanocytic lesion. Chronic ocular irritation is capable of inducing cytologically benign subclinical uveal melanocytic proliferations. CONCLUSIONS: The conventional classification of human uveal melanocytic lesions includes only nevi and melanomas, but a comparison of the results of this study with descriptions of human uveal melanocytic nevi suggests the existence of a spectrum of intermediate atypical precursor lesions in humans.

9,10-Dimethyl-1,2-benzanthracene↗