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At least 847 records · Page 47Linked to original sources
PubMed1987

Cutaneously applied erythromycin base reduces various types of inflammatory reactions in mouse ear.

Erythromycin base was tested by brushing a solution onto the skin in various models of non-immune and immune inflammation produced in mouse ear, namely inflammations induced by croton oil and cantharidin, primary irritation by picryl chloride, and contact hypersensitivity reactions to oxazolone and picryl chloride. On the non-immune inflammations, erythromycin displayed a greater effect than indomethacin, phenylbutazone or acetylsalicylic acid, though less than that of hydrocortisone acetate. It inhibited the hypersensitivity reactions less well. These results suggest some participation of an anti-inflammatory mechanism in the clinical effectiveness of cutaneously applied erythromycin base in some forms of acne.

Administration, Topical↗
PubMed1985

The effect of selected immunomodulating agents on experimental contact reactions.

A guinea pig experimental model which allows comparison of the macroscopic appearance of skin tests with the nature and degree of the dermal inflammatory cell infiltrate has been used to study the effects of cyclophosphamide, methotrexate, azathioprine and cyclosporin A on contact reactions. The immunomodulating capabilities of the agents tested are assessed by their effects on the allergic contact reaction to oxazolone, a cell-mediated delayed hypersensitivity reaction. Non-specific, anti-inflammatory actions are assessed by effects on the toxic contact reaction to croton oil. Changes are compared to findings in reference animals for each reaction. The reference materials and the uses and limitations of the experimental model are evaluated. When administered prior to sensitization, all agents enhanced the macroscopic appearance of the allergic contact reactions. Changes in the dermal cellular infiltrates were not pronounced. When administered prior to testing, cyclophosphamide, methotrexate and azathioprine caused changes compared to controls which varied in direction and degree both macroscopically and microscopically. Cyclophosphamide which was the most active agent showed non-specific, anti-inflammatory effects and caused a peripheral blood leukopenia, the level and character of which was essentially independent of the dermal cellular infiltrate of tests. Cyclosporin A demonstrated no non-specific, anti-inflammatory activity on the toxic reaction, but had by far the most pronounced immunosuppressant effect of the agents tested, with virtual quenching of both the macroscopic appearance and all aspects of the dermal cellular infiltrates of the allergic contact reaction.

Animals↗
PubMed1985

Anti-inflammatory activity of a dual inhibitor of cyclooxygenase and lipoxygenase pathways, CBS-1108 (2-acetylthiophene-2-thiazolylhydrazone).

Anti-inflammatory therapy is actually devolved to glucocorticoids which prevent the release of arachidonic acid from phospholipids and consequently its subsequent transformation into prostaglandins and leukotrienes. This activity explains in part why steroids are better anti-inflammatory agents than acetylsalicylic acid (ASA)-like drugs which only reduce prostaglandin production. Despite their superior therapeutic actions, there are many side effects associated with corticosteroids. Therefore in recent years, research of non-steroid dual inhibitors of prostaglandin and leukotriene production has been developed. The present paper investigates the pharmacological activity of such a new compound, CBS-1108 (2-acetylthiophene-2-thiazolylhydrazone), in comparison with dexamethasone, cyclooxygenase inhibitors (ASA and indomethacin) and reference dual inhibitors (nordihydroguaiaretic acid (NDGA) and 3-amino-1-(m-trifluoromethylphenyl)-2-pyrazoline (BW-755 C]. The two-pathway inhibitors and ASA-like drugs are similarly effective on paracentesis-induced disruption of the blood-aqueous barrier and on croton oil-induced ear edema. On the contrary in an animal model of leukocyte migration and on mast cell degranulation, NDGA and CBS-1108 are very active when the other tested compounds are inefficient.

Animals↗
PubMed1985

[Testing the loss of efficacy (tachyphylaxis) during external steroid application].

The steroids fluprednylidene-21-acetate (FA) and betamethasone-17-valerate (BV) were tested in comparison to their inactive bases for loss of activity (tachyphylaxis) after 2 weeks of application. In the croton oil test, both steroids produced equal inhibition of the pustular inflammatory reaction. The vasoconstriction test after 14 days of use revealed a clear decrease in the blanching reaction - which was, however, not statistically significant in the case of BV.

Administration, Topical↗
PubMed1977

Passive immunotherapy of established tumors with syngeneic antitumor serum in combination with immunopotentiators.

The possibility of passive therapy of 6 approximately 8-day established tumors with syngeneic antitumor antiserum was tested using (1) combination of the antiserum and immunopotentiators, (2) combination of the antiserum and inflammatory agents, and (3) repeated injections of antiserum. Therapeutic effect on an ascites tumor was seen using antiserum in combination with BCG or lipopolysaccharide, or less clearly with carrageenan. Combinations of antiserum and PS-K, histamine, or croton oil did not have a synergistic therapeutic effect, but repeated injection of a small amount of antiserum did have a therapeutic effect on established peritoneal and subcutaneous tumors.

Animals↗
PubMed1978

Colonic basophil hypersensitivity.

Contact hypersensitivity reactions were elicited by intraluminal application of DNCB to the colon of guinea pigs and were found sometimes to contain large infiltrates of basophils. These colonic basophil hypersensitivity reactions were accompanied by systemic sensitization and were not seen in nonspecific colonic inflammatory responses induced by croton oil. The heterogenous immune inflammatory responses induced in the colon by DNCB contact sensitivity may serve as a model for the study of inflammatory bowel disease.

Animals↗
PubMed1980

Complement-independence of the acute-phase production of serum amyloijd P-component (SAP) in mice.

Mice depleted of circulating C3 by injection of cobra factor (CoF), the C3-activating protein of cobra (Naja naja) venom, mounted the same acute-phase responses of serum amyloid P-component (SAP) to subsequent injection of casein, bacterial lipopolysaccharide or croton oil as did normal control mice. There was also evidence for accelerated synthesis of C3 itself in response to injection of these acute-phase stimulants in CoF-treated mice. On the other hand complement activation produced by injection of CoF alone did not cause any elevation of the serum SAP level. These results indicate that acute-phase plasma protein production can proceed independently of the complement system as a mediator of or participant in inflammatory reactions, and that complement activation alone is not a sufficient stimulus for an acute-phase response, at least of SAP.

Amyloid↗
PubMed1981

Acetoacetyl-CoA reductase activity of lactating bovine mammary fatty acid synthase.

Fatty acid synthase, purified from lactating bovine mammary gland, utilizes coenzyme A esters of acetoacetic, 3-hydroxybutyric, and crotonic acids as substrates for its partial reactions at micromolar concentrations. The NADPH:acetoacetyl-CoA reductase had a Km of 5 microM acetoacetyl-CoA and a Vmax of about 4 mumol of NADPH oxidized min-1 mg-1. In contrast, the Km for the model compound, acetoacetyl pantetheine was 820 microM and that of S-acetoacetyl-N-acetylcysteamine was over 40 mM. The reduction of acetoacetyl-CoA was observed with the enzyme from rat tissues also but not with those from avian tissues or yeast. With the bovine mammary enzyme, the reaction was found to oxidize 2 mol of NADPH for every mol of acetoacetyl-CoA consumed. Butyrate was the major product of reduction. The reductase activity was susceptible to inhibition by several sulfhydryl reagents; it was lost when the synthase was dissociated into one-half molecular weight subunits or when the incubation mixture was depleted of CoA. It was competitively inhibited by acetyl-CoA, butyryl-CoA, methylmalonyl-CoA, and 2-methylcrotonyl-CoA. These results as well as its use as a primer in fatty acid synthesis by the enzyme suggest that the acetoacetyl group from acetoacetyl-CoA is transferred to the enzyme, presumably to its 4'-phosphopantheine prosthetic group. The acyl group is then expected to remain attached to the enzyme while it is reduced, dehydrated, and reduced again to form a butyryl group which can either undergo chain elongation, if malonyl-CoA is present, or be released from the enzyme by hydrolysis or transfer to free CoA.

Acetoacetates↗
PubMed1982

Synthesis and topical antiinflammatory potencies of a series of 6-keto- and delta 6-6-acyloxybetamethasone derivatives.

6-keto- and delta 6-6-acyloxybetamethasone esters were synthesized, and tested for topical antiinflammatory potency using a modification of the Tonelli croton ear assay. The introduction of a 6-keto group generally led to retention of topical antiinflammatory potencies when compared to the corresponding 6-desoxycorticoids. In contrast, introduction of the delta 6-6-acyloxy moiety into betamethasone 17,21-dipropionate reduced antiinflammatory potency.

Administration, Topical↗
PubMed1995

Effect of glycyrrhetinic acid on DNA damage and unscheduled DNA synthesis induced by benzo(a)pyrene.

Glycyrrhetinic acid (GA) is an active component of Glycyrrhiza uraleusis fisch. In this study, GA was found to inhibit ear edema and ornithine decarboxylase (ODC) activity induced by croton oil in mice. GA could also protect rapid DNA damage and decrease the unscheduled DNA synthesis induced by benzo(a)pyrene. The results demonstrate that GA has a potential cancer chemopreventive activity.

Animals↗
PubMed1995

Peripheral effects of naloxone in mice with acute diarrhea associated with intestinal inflammation.

The aim of the study was to evaluate the effects of centrally and peripherally acting opioid antagonists such as naloxone (NX), naloxone methiodide, (+)-naloxone [(+)NX], (-)-a-5,9-diethyl-2'-hydroxy-2 (3-furylmethyl)-6,7-benzomorphan and naltrindole on gastrointestinal (GI) transit in mice with diarrhea associated with intestinal inflammation. Our hypothesis was that diarrhea/inflammation could induce a release of endogenous opioid peptides that would play an inhibitory role in the physiological response to intestinal inflammation; the administration of opioid antagonists would uncover the effects of the endogenous opioid peptides on the gut. Diarrhea associated with inflammation was induced in mice by administration of croton oil (CO) although control animals received saline (SS); GI transit was evaluated with a charcoal meal. The i.p. administration of 0.1 mg/kg NX or NXME, induced a significant increase in GI transit in CO but not in SS-treated animals (P < .005). At the same dose, (+)NX had no effect either in CO or SS groups. The kappa antagonist MR-2266 (1 and 3 mg/kg) had no effect on GI transit in SS or CO animals. However, the delta antagonist naltrindole (3 mg/kg), caused a small but significant (P < .01) increase in GI transit in the CO group. These results suggest that endogenous opioid peptides are released in CO-treated animals and exert an inhibitory control of intestinal motility, which is unmasked by opioid antagonists.(ABSTRACT TRUNCATED AT 250 WORDS)

Acute Disease↗
PubMed1994

[The antiinflammatory activity of shikonin and its inhibitory effect on leukotriene B4 biosynthesis].

Shikonin is one of the active components isolated from the dry root of Arnebia euchroma (Royle) Johnst (AERJ). It has been shown to have anti inflammatory activity on formaldehyde induced paw swelling in rats. Preparations of AERJ has been used clinically in curing phlebitis and vascular purpura. In the present study, sc administered shikonin was shown to have significant inhibitory effects on ear edema induced by croton oil in mice and paw swelling induced by yeast in rats. In order to investigate the influence of shikonin on biosynthesis of LTB4 and 5-HETE, an in vitro leukocyte incubation system was adopted. The results showed that shikonin has fairly strong inhibitory effects on LTB4 and 5-HETE biosynthesis. Its effects and concentrations fit a positive relationship within the range of 10(-7)-10(-4) mol.L-1. The equations of inhibition (Y) versus concentration (X, LogC) obtained by linear regression were Y = 166 + 18.7X (r = 0.9319) for LTB4 and Y = 173 + 18.7X (r = 0.9856) for 5-HETE. The IC50 were 6.2 x 10(-7) and 2.6 x 10(-7) mol.L-1, respectively. The results also indicate that natural shikonin derivatives have similar inhibitory effects on LTB4 biosynthesis. These results suggest that inhibition of LTB4 and 5-HETE may play a major role in the mechanism of anti inflammatory effects of shikonin.

Animals↗
PubMed1994

Anti-inflammatory activity of rolipram in a rat ear edema model.

In the present study the anti-inflammatory activity of the phosphodiesterase inhibitor rolipram (ZK 62,711, CAS 61413-54-5) was tested in a rat model where edema was induced in the ears of the animals by the epicutaneous application of croton oil in ethanol (5%, by volume). The administration of 0.015, 0.15 and 1.5 mg rolipram per ear dose-dependently inhibited the formation of edema. Concomitantly, the body temperature of the rats was decreased. 4-14% of rolipram was percutaneously absorbed within a 5-h interval. The absorbed proportion, represented by the area under the plasma level-time curve, correlated with the inhibition of edema formation and with the decrease in body temperature.

Administration, Topical↗
PubMed1993

[Anti-inflammatory effect of Caragana microphylla Lam].

Caragana microphylla can antagonize the inflammation induced by carrageenin, hot water and croton oil. It can also inhibit the proliferation of granuloma, blood capillary permeability, phagocytic function of mononuclear phagocyte system, and synthesis or release of PGE2 at the inflamed part.

Animals↗
PubMed1996

Antiinflammatory activity of topically applied sertaconazole nitrate.

The antiinflammatory activity of topically applied sertaconazole nitrate was investigated. The dermal administration of 2% sertaconazole to rats, in which edema was induced by application of croton oil in the external ear, induced a 39.8% reduction of edema. The results show that sertaconazole applied by topical route at the concentration at which it is used in clinic, has antiinflammatory action in this experimental model.

Administration, Topical↗
PubMed1997

Antiinflammatory activities of procyanidin-containing extracts from Pinus pinaster Ait. after oral and cutaneous application.

Orally in liquid diet administered procyanidin-containing extracts from Pinus pinaster Ait. decreased the croton oil-induced ear edema in mice or the compound 48/80-induced hind paw edema in rats to a statistically significant extent. Most effective were the extracts containing mainly oligomeric procyanidins with chain lengths greater then 4 units (extracts A or B). Further, the different extracts incorporated in various concentrations (1.0, 3.0 or 0.1%) in 5% hydroxyethylcellulose gel and applied topically on the shaved back of rats, inhibited significantly the ultraviolet radiation-induced increased capillary permeability. In these experiments, normalisation of capillary permeability was not correlated with the content of the extracts on higher oligomeric procyanidins.

Administration, Oral↗
PubMed1999

Selective requirements for leukocyte adhesion molecules in models of acute and chronic cutaneous inflammation: participation of E- and P- but not L-selectin.

Adhesion molecules borne by both endothelial cells and circulating leukocytes are in large measure responsible for guiding the process of extravasation. The selectin family has been primarily associated with the early stages of adhesion involving initial contact and rolling. A significant body of evidence has accumulated indicating a fundamental role for the endothelial members of this family, E- and P-selectin, in a variety of inflammatory states and models. Although originally identified as the lymph node-specific lymphocyte homing receptor, L-selectin has also been suggested to play an important role in leukocyte recruitment to sites of inflammation. We have recently demonstrated, using L-selectin-deficient mice, that defects in contact hypersensitivity (CHS) responses are in essence due to the inability of T cells to home to and be sensitized within peripheral lymph nodes, whereas nonspecific effector cells are fully capable of entry into sites of cutaneous inflammation (Catalina et al, J Exp Med 184:2341, 1996). In the present study, we perform an analysis of adhesion molecule usage in two models of skin inflammation and show in both L-selectin-deficient as well as wild-type mice that a combination of P- and E-selectin is crucial for the development of both acute (croton oil) and chronic (contact hypersensitivity) inflammation at sites of the skin, whereas L-selectin does not appear to play a significant role. Moreover, alpha4 integrins are shown to be integral to a CHS but not an acute irritant response, whereas CD44 does not significantly contribute to either. These results provide a systematic examination in one study of major adhesion molecules that are critical in acute and chronic skin inflammation. They reinforce the essential role of the collaboration of E- and P-selectin in both specific and nonspecific skin inflammatory responses and the importance of alpha4 in the specific response only. In addition, they substantiate only a limited role, if any, for L-selectin in these cutaneous effector mechanisms and demonstrate the essential equivalence in this analysis of L-selectin-deficient mice compared with normal mice treated with blocking antibodies.

Animals↗