Croton Oil-induced Ear Edema Research Articles

English

Endopleura uchi (Huber) Cuatrec. (Humiriaceae), the Brazilian Amazon plant, is used in folk medicine to treat arthritis and gastric ulcer. Bergenin, one of the chemical constituents of E. uchi, has anti-inflammatory properties. Its acetylation results in acetylbergenin, which is extracted to investigate its potential anti-inflammatory and antiulcer properties using an assay for croton oil-induced ear edema, rat paw edema induced by carrageenan and dextran, carragenin-induced peritonitis, and stress-induced gastric ulcer. In ear erythema induced by croton oil, acetylbergenin presented a significant 75.60% inhibition (p<0.001). The oral administration of 6.8 mg/kg of acetylbergenin significantly inhibited the carrageenan-induced edema formation by 35.09% (p<0.05) and the dextran-induced edema by 33% (p<0.05). The migration of neutrophils toward the peritoneal cavity was inhibited in acetylbergenin (6.8 mg/kg) treated animals by 70% (p<0.01). In the stress-induced gastric ulcer, acetylbergenin inhibited 78.55% of gastric lesions. The results suggest that, the anti-inflammatory action of acetylbergenin appears to be dependent on cyclooxygenase (COX-2) inhibition. Furthermore, although the anti-inflammatory activity of acetylbergenin is a characteristic of nonsteroidal compounds, it causes little deleterious interference in the gastric mucosa. Key words: Endopleura uchi, bergenin, acetylbergenin, anti-inflammatory, antiulcerogenic activity.

Synthesis and anti-inflammatory evaluation of novel thiadiazol derivatives of Mefenamic acid

In the search for new potential non-steroidal anti-inflammatory agents, some novel Mefenamic acid derivatives were synthesized and confirmed by spectroscopic data. The anti-inflammatory activities of these compounds were evaluated by the croton oil-induced ear oedema test in mice. The preliminary pharmacological evaluations indicate that these new compounds showed potent anti-inflammatory activities compare to control and Indomethacin groups. KEY WORDS : Non-steroidal anti-inflammatory drugs, Mefenamic acid derivatives, Cyclooxygenase, Ear oedema test Bull. Chem. Soc. Ethiop. 2017 , 31(1), 171-175. DOI: http://dx.doi.org/10.4314/bcse.v31i1.15

LPS로 자극된 대식세포에서의 NF-κB와 MAPK 활성 조절을 통한 참까막살(Polyopes affinis) 에탄올 추출물의 항염증 효과

본 연구에서는 참까막살 에탄올 추출물(PAEE)의 항염증 활성을 확인하기 위하여 LPS로 자극된 RAW 264.7 세포에서의 pro-inflammatory cytokine 및 NO의 분비 생성량과 western blot으로 단백질 발현량을 측정하였다. 또한, croton oil로 유도된 귀 부종 모델을 이용하여 알아보았다. RAW 264.7 세포에서 PAEE를 0.1~100 μg/mL 농도로 처리 시 세포독성을 나타내지 않음을 확인하였다. 그 결과 PAEE는 pro-inflammatory cytokine(IL-6, TNF-α, IL-1β) 및 NO의 분비량을 농도 의존적으로 억제시켰으며, iNOS와 COX-2의 발현량도 감소시킴을 확인하였다. 이러한 항염증 활성 결과는 NF-κB와 MAPKs 전사인자의 활성 억제에 의한 것으로 확인되었다. 또한, croton oil로 유도된 귀 부종 모델에서 PAEE를 50 mg/kg body weight 처리 시 귀 부종이 prednisolone(10 mg/kg body weight)과 유사한 정도로 억제됨을 확인하였다. 귀 조직 관찰에서도 PAEE는 croton oil에 의해 증가한 진피와 경피의 두께를 감소시켰으며, 진피로 침윤된 mast cell의 수도 감소시켰다. 이 결과를 종합해 보면 참까막살 에탄올 추출물은 NF-κB와 MAPKs의 활성화 억제를 통해 염증 매개 물질의 생성을 억제시켜 항염증 활성을 나타내는 것으로 확인되었다.

Anti-inflammatory activity of rhein isolated from the flowers of Cassia fistula L. and possible underlying mechanisms.

ObjectiveAnti-inflammatory activity of rhein in animal models with potential mechanism of actions.MethodsRhein was isolated from Cassia fistula L. flowers collected in Chennai, Tamil Nadu, India. Its anti-inflammatory activity was then investigated in Wistar rats and mice using carrageenan-induced hind paw oedema, croton oil-induced ear oedema, cotton pellet-induced granuloma and acetic acid-induced vascular permeability models.ResultsAdministration of rhein (10, 20, 40 mg/kg) significantly (p < 0.05) inhibited carrageenan-induced paw oedema in rats and croton oil-induced ear oedema in mice in dose-dependent manners. Continual administration of rhein to rats using implanted cotton pellets significantly (p < 0.05) reduced granuloma formation (20 mg/kg: 17.24%; 40 mg/kg: 36.12%) compared to control group animals. Administration of rhein increased the activities of catalase (CAT), superoxide dismutase (SOD) and glutathione peroxidase (GSH-px) and decreased the levels of nitrite, interleukin-6 (IL-6), interleukin-1β (IL-1β), tumor necrosis factor-α (TNF-α), malondialdehyde (MDA) and vascular endothelial growth factor (VEGF) compared to control animals. Western blotting results revealed that rhein diminished carrageenan-induced cyclooxygenase (COX)-2 and inducible nitric oxide synthase (iNOS) and increased heme oxygenase (HO)-1, nuclear factor erythroid 2–related factor 2 (Nrf2), peroxisome proliferator-activated receptor gamma (PPAR)-γ and heat shock protein (HSP)-72 expression after 6 h in the paw oedema model.ConclusionThe anti-inflammatory mechanisms of rhein might be related to decrease in the levels of MDA, iNOS and COX-2 and the stimulation of HO-1, PPAR-γ and Nrf2 expression via increases in the activities of CAT, SOD and GSH-px through the suppression of nitrite, TNF-α, IL-6 and IL-1β.

Evaluation of Biological Activity and Computer-Aided Design of New Soft Glucocorticoids.

Soft glucocorticoids are compounds that are biotransformed to inactive and non-toxic metabolites and have fewer side effects than traditional glucocorticoids. A new class of 17β-carboxamide steroids has been recently introduced by our group. In this study, local anti-inflammatory activity of these derivatives was evaluated by use of the croton oil-induced ear edema test. Glucocorticoids with the highest maximal edema inhibition (MEI) were pointed out, and the systemic side effects of those with the lowest EC50 values were significantly lower in comparison to dexamethasone. A 3D-QSAR model was created and employed for the design of 27 compounds. By use of the sequential combination of ligand-based and structure-based virtual screening, three compounds were selected from the ChEMBL library and used as a starting point for the design of 15 derivatives. Molecular docking analysis of the designed derivatives with the highest predicted MEI and relative glucocorticoid receptor binding affinity (20, 22, 24-1, 25-1, 27, VS7, VS13, and VS14) confirmed the presence of interactions with the glucocorticoid receptor that are important for the activity.

ANTIOXIDANT AND ANTI-INFLAMMATORY ACTIVITIES OF RUBUS FRUTICOSUS AND ZIZYPHUS VULGARIS METHANOL EXTRACTS

&lt;p class="Default"&gt;&lt;strong&gt;Objective&lt;/strong&gt;:&lt;strong&gt; &lt;/strong&gt;This report is an attempt to study the phenolic composition of &lt;em&gt;Rubus fruticosus &lt;/em&gt;(RFE) and&lt;em&gt; Zizyphus vulgaris (&lt;/em&gt;ZVE&lt;em&gt;) &lt;/em&gt;methanol&lt;em&gt; &lt;/em&gt;extracts&lt;em&gt; and &lt;/em&gt;evaluate their antioxidant and anti-inflammatory effects &lt;em&gt;in-vitro&lt;/em&gt; and &lt;em&gt;in-vivo&lt;/em&gt;.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Methods: &lt;/strong&gt;Total phenolic and total flavonoids contents of extracts were determined by spectrophotometric methods. Phenolic compounds were identified by&lt;strong&gt; &lt;/strong&gt;HPLC-TOF/MS. The antioxidant activities were evaluated &lt;em&gt;in vitro&lt;/em&gt; using DPPH, ABTS and FRAP assays. The effect of RFE and ZVE&lt;em&gt; &lt;/em&gt;on DNA cleavage induced by H&lt;sub&gt;2&lt;/sub&gt;O&lt;sub&gt;2&lt;/sub&gt; UV-photolysis was also investigated. The antioxidant effect of RFE and ZVE was tested &lt;em&gt;in vivo&lt;/em&gt; using the blood total antioxidant capacity test in mice. On the other hand, the anti-inflammatory activity was assessed &lt;em&gt;in vivo&lt;/em&gt; using two models of acute inflammation ear edema and vascular permeability.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Results: &lt;/strong&gt;The phytochemical analysis of these extracts showed that RFE possesses higher polyphenolic and flavonoid content than ZVE. in the same way RFE exerted the highest antioxidant capacity with IC&lt;sub&gt; 50 &lt;/sub&gt;value of 14 µg/ml in DPPH assay, 1.58 mmol of Trolox E/mg extract and 3.39 of mmol FesO&lt;sub&gt;4&lt;/sub&gt;/mg extract in ABTS, and FRAP assay respectively. The studied extracts showed a concentration-dependent protective effect on DNA cleavage induced by H&lt;sub&gt;2&lt;/sub&gt;O&lt;sub&gt;2&lt;/sub&gt; UV-photolysis. The daily oral administration of 200 mg/kg of RFE or ZVE during three weeks showed an improvement of the blood total antioxidant capacity; the HT&lt;sub&gt;50&lt;/sub&gt; values were151.45 min and 146.72 min for the groups treated with RFE and ZVE, respectively &lt;em&gt;versus&lt;/em&gt; 122.5 min for the control group. The topical application of 2 mg/ear of RFE inhibited the croton oil-induced ear edema by 75.72%, while the inhibition exerted by ZVE was 64.24%. These inhibitions were higher than that of indomethacin, used as a reference. Moreover, the oral administration of 400 mg/kg of RFE inhibited significantly (33.57%) acetic acid induced vascular permeability in mice. However, this effect was lower than this of indomethacin. The inhibition effect exerted by ZVE was not significant.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Conclusion&lt;/strong&gt;&lt;strong&gt;:&lt;/strong&gt;&lt;strong&gt; &lt;/strong&gt;The results obtained in this investigation showed that RFE possesses strong antioxidant and anti-inflammatory potential in comparison with ZVE, which may be attributed to the presence of polyphenolic phytoconstituents.&lt;/p&gt;

Solanum paranense Extracts and Solanine Present Anti-Inflammatory Activity in an Acute Skin Inflammation Model in Mice.

The aim of the study was to evaluate the anti-inflammatory activity of the S. paranense crude extract, S. paranense alkaloid fraction, and solanine alkaloid. These samples reduce the croton oil-induced ear edema in a dose-dependent manner and a maximum inhibition of 81%, 98%, and 80% in the doses of 1.0, 0.73, and 0.37 mg/ear, respectively. Moreover, the samples inhibit the MPO activity with an inhibition maximum of 51%, 40%, and 46% in the doses of 1.0, 0.73, and 0.37 mg/ear, respectively. Similar results were found for dexamethasone 0.10 mg/ear (positive control), which showed inhibitions of ear edema and MPO activity of 100% and 65%, respectively. These results found probably are related to the presence of solanine which is present in significant quantity in the alkaloid fraction and others as rutin and rosmarinic, chlorogenic, and gallic acids. These results support the use of S. paranense for the treatment of inflammatory skin disorders.

Anti-Inflammatory Effect of Chondria crassicaulis Harvey Ethanol Extract in a Mouse Model of Croton Oil-Induced Ear Edema and LPS-Induced RAW 264.7 Cells

Anti-Inflammatory Effect of Chondria crassicaulis Harvey Ethanol Extract in a Mouse Model of Croton Oil-Induced Ear Edema and LPS-Induced RAW 264.7 Cells

Evaluation of the anti-inflammatory properties of the aqueous extract of &lt;i&gt;Albizia zygia&lt;/i&gt; stem bark

Albizia zygia is used in folk medicine for treatment of a wide variety of ailments including wounds, toothache and inflammation. Its acclaimed local use in the treatment of inflammation prompted the investigation into its antiinflammatory activity. The effect of the aqueous stem bark extract of Albizia zygia on inflammation was investigated using acute (carrageenan induced-, dextran induced-, histamine induced-paw oedema, carrageenan-induced exudate formation and croton oil induced ear oedema) and chronic (formalin induced arthritis) models of inflammation in rats and mice. The extract caused significant (p<0.05), inhibitions of croton oil-induced ear oedema, carrageenanand dextran-induced paw oedema without any appreciable effect on histamine induced oedema. The extract also significantly inhibited leucocyte migration without affecting the volume of exudate formation. The antiinflammatory effects of the extract on these acute models of inflammation were not dose-dependent as greatest activity was seen at the dose of 200mg/kg. This same dose also caused a significant reduction in ankle, but not paw, oedema in the formaldehyde-induced arthritis model. The aqueous stem bark extract of Albizia zygia possesses antiinflammatory activity on acute and chronic inflammatory models in rats and mice. Keywords: Albizia zygia ; Arthritis; Carrageenan; Formaldehyde; Oedema

Anti-Inflammatory Potential of Hecogenin in Experimental Animals: Possible Involvement of Inflammatory Cytokines and Myeloperoxidase.

Hecogenin is a steroidal sapogenin plays important role in treatment of variety of inflammatory diseases. We have investigated the anti-inflammatory effects of Hecogenin (50 µg/animal) (HG), Fluticasone (50 µg/animal) (FC) and Hecogenin+Fluticasone (HG+FC) combination (25 µg/animal, each) on various inflammatory models. The anti-inflammatory effect of HG, FC and HG+FC combination was studied on % inhibition of dry weight of granuloma tissue, Δ ear weight, myeloperoxidase assay, serum pro-inflammatory cytokines, colon weight to length ratio, macroscopic lesions, adhesion score, diarrhoea score and histopathological analysis of ear and colon tissue on Cotton pellets induced granuloma in rats, Croton oil induced ear edema in mice and TNBS induced granuloma in rats. Topical administration of HG and its combination with FC showed significant decrease (p<0.001) in the % inhibition of dry weight of granuloma tissue, Δ ear weight, myeloperoxidase level, serum pro-inflammatory cytokines levels, colon weigh to length ratio as compared with Cotton pellets treated with acetone groups and Croton oil treated animals. Further histopathological analysis of ear tissue showed significant decrease in dermal thickness and epidermal hyperplasia and colon tissue showed reduction of edema, infiltration of inflammatory cells and normalization of crypt structure compared to DC animals. Thus, the findings of present study suggest the possible role of HG in the treatment of inflammation by reducing the dose of FC in combination with HG.

Ethnopharmacological study and topical anti-inflammatory activity of crude extract from Poikilacanthus glandulosus (Nees) Ariza leaves

Ethnopharmacological relevanceEthnopharmacological studies are important tools as records and documentation of the empirical uses of medicinal plants in traditional communities with the purpose of generating useful knowledge to lead to the development of new medicines, biodiversity conservation and enhancement of knowledge and local culture. Poikilacanthus glandulosus is widely used by the population of City of Santiago, in Brazil, nevertheless, it does not have any validation regarding its use and its medicinal effects. AimThe objective of this study was to perform one ethnopharmacological survey about P. glandulosus in the City of Santiago and determine the anti-inflammatory activity in order to prove its uses in popular medicine. MethodsPersonal and ethnopharmacological data were collected through a prepared questionnaire. The phytochemical analysis was performed observing the individual methodology for each reaction and by HPLC-UV. The antiedematogenic and anti-inflammatory (cell infiltration and histological procedure) activities of the P. glandulosus (0.01–1000μg/ear) were evaluated in the ear edema model induced by topical application of croton oil. ResultsP. glandulosus is known in City of Santiago as “Gaiana” and its macerated leaves and branches are prepared with alcohol or sugarcane liquor especially for insect bites, cicatrization and inflammation. HPLC analysis revealed the presence of maslinic acid (2.024±0.10mg/g), uvaol (0.124±0.02mg/g) and sitosterol (0.502±0.05mg/g). The topical application of crude extract of P. glandulosus reduced in a dose-dependent manner the croton oil-induced ear edema and myeloperoxidase activity (neutrophils infiltration marker) with maximum inhibition of 87±2% and 64±12%, respectively at 1000µg/ear. Dexamethasone (100µg/ear), used as a positive control, inhibited croton oil-induced ear edema in 89±3% and decreased myeloperoxidase activity in 50±3%. Both P. glandulosus as dexamethasone reduced cell infiltration when evaluated by histological procedure ConclusionThis work allowed us to understand the specie P. glandulosus through ethnopharmacological study and it showed that the crude extract presented antiedematogenic and anti-inflammatory actions, proving their traditional use as anti-inflammatory.

Synergistic Effect of Compounds from a Chinese Herb: Compatibility and Dose Optimization of Compounds from N-Butanol Extract of Ipomoea stolonifera.

The herbal medicine Ipomoea stolonifera (I. stolonifera) has previously been shown to have considerable anti-inflammatory potential in vivo and in vitro. To establish a method for exploring the synergistic effects of multiple compounds, we study the compatibility and dose optimization of compounds isolated from n-butanol extract of I. stolonifera (BE-IS). Raw264.7 cell was treated with lipopolysaccharide (LPS) in the presence of compounds from BE-IS, namely scopoletin, umbelliferone, esculetin, hesperetin and curcumin, using the orthogonal design, uniform design and median-effect method. To verify the best efficacy of principal constituents in vivo, the uniform design was used in the croton oil-induced mouse ear edema model. The results from LPS-induced the production of prostaglandin E2 (PGE2) show that, esculetin, curcumin and hesperetin were the principal constituents that had synergistic effects when used at the optimal ratio. Additionally, the principal constituents were found to work synergistically in the croton oil-induced mouse ear edema model at low doses. It turned out that the three experimental optimization and analysis methods (orthogonal design, uniform design and median-effect method) can be effectively used to solve both compatibility and dose optimization for combined use of multiple compounds.

Anti-inflammatory effect of a resveratrol derivative 3,4,5-trimethoxy-4′,5′-dihydroxy-trans-stilbene (WL-09-5) via ROS-mediated NF-κB pathway

Inflammation derived from macrophages activation leads to various diseases. Synthetic modifications of resveratrol have been shown to have better anti-inflammatory activities. In this study, croton oil-induced mouse ear edema and lipopolysaccharides (LPS)-stimulated RAW264.7 macrophages were used to evaluate the anti-inflammatory effects of WL-09-5, a derivative of resveratrol. Furthermore, the activation of NF-κB was determined. Results showed that WL-09-5 significantly reduced the croton oil-induced ear edema, scavenged NO and ROS production, and reduced the levels of TNF-α, IL-6, and IL-1β. Furthermore, WL-09-5 may significantly inhibit the translocation of NF-κB in macrophage cells stimulated by LPS in a dose-dependent manner, which is a potent mechanism of its anti-inflammatory effects. In conclusion, WL-09-5 is an underlying candidate for inflammatory diseases that need further investigations.

Phytochemical screening and anti-inflammatory properties of Algerian Hertia cheirifolia methanol extract

Context: Hertia cheirifolia L. (Asteraceae) is traditionally used in Northern Africa to treat various inflammatory infections. However, few studies on this plant have been reported.Objective: The anti-inflammatory activity of methanol extract of H. cheirifolia leaves was investigated using different experimental models.Materials and methods: Phytochemical analysis was performed to determine phenolic compounds. Acute toxicity of the extract (2000 mg/kg) was examined in Swiss albino mice for 14 days, before croton oil-induced ear oedema in mice, carrageenan-induced paw oedema in Swiss albino rats, cotton pellet-induced granuloma in rats and carrageenan-induced air pouch in mice were conducted. The IL-1β and TNF-α release from concanavalin A-stimulated monocytes was measured by ELISA.Results: Methanol extract of H. cheirifolia is rich in polyphenols and flavonoids. Cinnamic acid and rutin represent the major constituents. Methanol extract up to 2000 mg/kg did not produce any toxic effects. Topical application of 2 mg/ear of the extract produced 78.7% of inhibition on ear swilling. Oral pre-treatment of rats with 200 and 400 mg/kg of the extract inhibited paw oedema by 70% and 89%, respectively. At 200 mg/kg, granuloma dry and wet weights were reduced by 41.85% and 61.72%, respectively. Moreover, the treatment with methanol extract at 1 mg/kg exerted 62.7% of inhibition on leucocytes migrated into the ear pouch. TNF-α and IL-1β release was reduced by 69% and 78%, respectively, with 1 μg/mL of the extract.Conclusion: Methanol extract of H. cheirifolia possesses a strong anti-inflammatory activity and may be considered an interesting source of effective anti-inflammatory compounds.

2-Aryl-3-(2-morpholinoethyl)thiazolidin-4-ones: Synthesis, anti-inflammatory in vivo, cytotoxicity in vitro and molecular docking studies

Seven new 4-thiazolidinones bearing the morpholino moiety were easily synthesized by one-pot reactions of 4-(2-aminoethyl)morpholine (2-morpholinoethylamine), arenealdehydes and mercaptoacetic acid refluxing toluene for 19 h with moderate to good yields (45–97%). These novel compounds were fully identified and characterized by NMR spectroscopy and mass spectrometry. Thiazolidin-4-ones in vivo anti-inflammatory activities were determined using a croton oil-induced ear edema model of inflammation in BALB C mice. The best results were found for compounds 4c (49.20 mmol/kg), 4d (49.20 mmol/kg) and 4f (52.48 mmol/kg), which showed the ability to decrease the ear edema in mice by 50%, 48% and 54%, respectively, when compared to the standard drug indomethacin. In addition, the in vitro cytotoxicity activity of thiazolidin-4-ones against Vero cells was also performed and four compounds (4a, 4c, 4d and 4f) showed no toxic effect at 500 μg/mL. A docking simulation of compounds into the 1Q4G (COX-1) and 4PH9 (COX-2) enzymes binding site was conducted. This preliminary result will guide us in for further studies to improve the anti-inflammatory activity.

Phenolic content, anti-inflammatory and antioxidant activities of Anacyclus clavatus extracts

The anti-inflammatory and the antioxidant activities of methanol (ME) and aqueous (AE) extracts of Anacyclus clavatus were evaluated. Phenolic constituents in the extracts were screened. Croton oil-induced ear edema in mice, carrageenan-induced paw edema and pleurisy in rats were evoked. The antioxidant effect was tested by 1,1-diphenyl-2-picrylhydrazyl, ion chelating, lipid peroxidation tests. Both extracts are rich in phenolic compounds. The application of 2 mg per ear of ME or AE inhibited ear edema by 84 and 83 %, respectively. The oral treatment of rats with 200 or 400 mg kg –1 of ME reduced paw edema by 64 and 74%, respectively, whereas the inhibition by AE was by 65 and 80%, respectively. At 400 mg kg–1, the extracts decreased exudation and neutrophil migration into the pleural cavity by 64 and 66%, respectively, while the inhibition by AE was 42 and 55%, respectively. On the other hand, ME exerted scavenging activity higher than AE, while the AE chelating activity was more than that of ME. However, both extracts had similar inhibitory effect on lipid peroxidation. In general, A. clavatus may be used as a source of anti-inflammatory and anti-oxidant agents.

Selective Activator of the Glucocorticoid Receptor Compound A Dissociates Therapeutic and Atrophogenic Effects of Glucocorticoid Receptor Signaling in Skin.

Background:Glucocorticoids are effective anti-inflammatory drugs widely used in dermatology and for the treatment of blood cancer patients. Unfortunately, chronic treatment with glucocorticoids results in serious metabolic and atrophogenic adverse effects including skin atrophy. Glucocorticoids act via the glucocorticoid receptor (GR), a transcription factor that causes either gene transactivation (TA) or transrepression (TR). Compound A (CpdA), a novel non-steroidal GR ligand, does not promote GR dimerization and TA, retains anti-inflammatory potential but induces fewer metabolic side effects compared to classical glucocorticoids when used systemically. As topical effects of CpdA have not been well studied, this work goal was to compare the anti-inflammatory and side effects of topical CpdA and glucocorticoids and to assess their effect on GR TA and TR in keratinocytes.Methods:We used murine immortalized keratinocytes and F1 C57BlxDBA mice. Effect of glucocorticoid fluocinolone acetonide (FA) and CpdA on gene expression in keratinocytes in vitro and in vivo was evaluated by reverse transcription-PCR. The anti-inflammatory effects were assessed in the model of tumor promoter 12-O-tertradecanoyl-acetate (TPA)-induced dermatitis and in croton oil-induced ear edema test. Skin atrophy was assessed by analysis of epidermal thickness, keratinocyte proliferation, subcutaneous adipose hypoplasia, and dermal changes after chronic treatment with FA and CpdA.Results:In mouse keratinocytes in vitro and in vivo, CpdA did not activate GR-dependent genes but mimicked closely the inhibitory effect of glucocorticoid FA on the expression of inflammatory cytokines and matrix metalloproteinases. When applied topically, CpdA inhibited TPA-induced skin inflammation and hyperplasia. Unlike glucocorticoids, CpdA itself did not induce skin atrophy which correlated with lack of induction of atrophogene regulated in development and DNA damage response 1 (REDD1) causatively involved in skin and muscle steroid-induced atrophy.Conclusions:Overall, our results suggest that CpdA and its derivatives represent novel promising class of anti-inflammatory compounds with reduced topical side effects.

Topical anti-inflammatory activity of Solanum corymbiflorum leaves

Solanum corymbiflorum is popularly known as “baga-de-veado” and its leaves are applied on inflamed legs, scabies, tick bite, boils, mastitis, low back pain and otitis. The aim of this study was evaluate anti-inflammatory in vivo activity and relate this activity with antioxidant compounds present in the extract of S. corymbiflorum leaves. The extract from S. corymbiflorum leaves topically applied was able to reduce the croton oil-induced ear edema and myeloperoxidase (MPO) activity with maximum inhibition of 87±3% and 45±7%, rescpectively in the dose of 1mg/ear. Similar results were found for positive control dexamethasone, which presented inhibitions of ear edema and MPO activity of 89±3% and 50±3%, respectively in a dose of 0.1mg/ear. These findings are due, at least in part, the presence of polyphenols (195.28mg GAE/g) and flavonoids, as chlorogenic acid (59.27mg/g), rutin (12.72mg/g), rosmarinic acid, caffeic acid and gallic acid found by high performance liquid chromatography (HPLC) analysis. This species showed potencial antioxidant by 1,1-diphenyl-2-picrylhydrazyl (DPPH), and carbonyl groups in proteins methods which may be related with the presence of this compounds. This species possess anti-inflammatory activity confirming their popular use for the local treatment of skin inflammatory disorders.

양파껍질 열수추출물의 in vitro 및 in vivo 항염증 효과

Onion (Allium cepa) is one of the flavonoids-rich materials in human diet and onion peel, which is the onion byproducts, contains over 20 times more quercetin than the flesh. In this study, to examine the anti-inflammatory effects of onion peel hot water extract (OPHWE), the cell viability, nitric oxide (NO), pro-inflammatory cytokines, such as interluekin-6 (IL- 6), tumor necrosis factor-α (TNF-α), and IL-1β, were measured using the murine macrophage cell line RAW 264.7 cells. The Balb/c mice were used for an in vivo acute toxicity test and ICR mice were used for measurement of inhibition effects of croton oil-induced mouse ear edema. As a result, NO levels decreased in a dose-dependent manner. The production of IL-6, TNF-α, and IL-1β was suppressed by 38%, 41%, and 34% respectively, compared with that of the LPS only group, without any cytotoxicity. The edema formation in the ICR mouse ear was also reduced compared to that in control. Moreover, there were no mortalities occurred in mice administered 5,000 mg/kg body weight of OPHWE. These results suggest that OPHWE has considerable anti-inflammatory activities and can be regarded as a potent candidate material to treat inflammatory diseases.

LPS로 유도된 RAW264.7 Cell과 마우스모델에 대한 잘피 에탄올 추출물의 항염증 효과

The Zostera marina ethanolic extract (ZMEE) was tested in this study to investigate the anti-inflammatory activity in LPS-induced RAW 264.7 cells and mouse model. Nitric oxide production and inducible nitiric oxide synthase expression in cells treated with ZMEE was reduced significantly in a dose-dependent manner. Similarly, the secretion of pro-inflammatory cytokines such as interleukin (IL)-6, IL-1β, and TNF- α was inhibited markedly. In addition, the expression of nuclear factor kappa B (NF-κB) and the phosphorylation of JNK, ERK, and p38 MAPKs was suppressed by ZMEE as well. In vivo test, ZMEE attenuated the croton oil-induced mouse ear edema and there were no mortalities in mice administered 5,000 mg/kg body weight of ZMEE during the observation periods. The results in photomicrograph of mice ear tissue showed the reduction of dermal thickness and the number of infiltrated mast cells. These results indicate that ZMEE inhibits the production of LPS-induced pro-inflammatory mediators, suggesting that ZMEE may be a potential material for anti-inflammatory therapies.