Topical Anti-inflammatory Effect Research Articles

In vivo anti-inflammatory properties of aerial parts of Nasturtium officinale

Context: Nasturtium officinale R. Br. (watercress) has long been used in Iranian folk medicine to treat hypertension, hyperglycemia, and renal colic. Moreover, anticancer, antioxidant, and hepatoprotective properties of N. officinale have been reported.Objective: In this study, anti-inflammatory activity of the hydro-alcoholic extract from aerial parts of N. officinale was investigated.Materials and methods: Oral administration of the hydro-alcoholic extract of N. officinale (250, 500 and 750 mg kg−1) was investigated on two well-characterized animal models of inflammation, including carrageenan- or formalin-induced paw edema in rats. Then, the topical anti-inflammatory effect of N. officinale (2 and 5 mg/ear) was studied on 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear edema. Finally, biopsy of the paw or ear was performed for pathological evaluation.Results: Acute toxicity tests of N. officinale in rats established an oral LD50 of >5 g kg−1. The extract of watercress (250, 500 and 750 mg kg−1) significantly inhibited carrageenan-induced paw edema 1, 2, 3 and 4 h after carrageenan challenge (p < 0.001). The extract (500 mg kg−1) also showed considerable activity against formalin-evoked paw edema over a period of 24 h (p < 0.001). Furthermore, topical application of N. officinale (5 mg/ear) reduced TPA-induced ear edema (p < 0.05). Histopathologically, the extract decreased swelling and the tissue damage induced by carrageenan or TPA.Discussion and conclusion: Our findings indicate potent anti-inflammatory activity of N. officinale in systemic and topical application and propose its potential as an anti-inflammatory agent for treatment of inflammatory conditions.

Topical anti-inflammatory and analgesic activities of standardized pomegranate rind extract in comparison with its marker compound ellagic acid in vivo

Ethnopharmacological relevanceIn Chinese traditional medicine, the peels of Punica granatum L. have been used to treat traumatic hemorrhage, burn, and ulcers. Aims of the studyThis study aimed to assess the topical anti-inflammatory and analgesic activities of a standardized pomegranate rind extract (SPRE) of which ellagic acid (EA) was the major antioxidant constituent and the marker compound. Material and methodsThe topical anti-inflammatory effects of SPRE were evaluated against acute models (croton oil-induced mouse ear edema and carrageenan-induced rat paw edema) and chronic model (complete Freund's adjuvant (CFA)-induced polyarthritis). The topical analgesic activities of SPRE were investigated in the rat punctuate mechanical hyperalgesia test and in the mouse formalin test. All studies of SPRE were carried out in parallel with its marker compound EA. ResultsSPRE (5%, 2.5%, and 1%, w/w) and the equivalent EA (0.65%, 0.325%, and 0.13%, w/w) dose-dependently reduced the croton oil-induced mouse ear edema with a maximal inhibition of 86.30% and 80.82%, respectively. SPRE dose-dependently attenuated the inflammatory responses in the carrageenan-induced rat paw edema and in the CFA-induced polyarthritis but the equivalent EA were effective only at the doses of 0.65% and 0.325%. Both SPRE (5%) and EA (0.65%) showed significant topical analgesic activities in the rat punctuate mechanical hyperalgesia test and in the mouse formalin test. ConclusionsSPRE was more active as an anti-inflammatory agent than EA. The anti-inflammatory and analgesic effects of SPRE were achieved through inhibiting the leukocyte infiltration and modulating the pro-inflammatory cytokines IL-β and TNF-α. These results clearly demonstrated that SPRE is a promising phytomedicine that could find use in the treatment of inflammatory diseases.

Anti-inflammatory activity of Salvia officinalis L.

This study evaluate the effects of sage hydroalcoholic extract (SE) and sage essential oil (SO) on the inflammatory response using an experimental model of acute inflammation and a leukocyte migration assay. In the carrageenan-induced pleurisy test, SE did not reduce the exudate volume and leukocyte migration to the pleura, but SE exerted a topical anti-inflammatory effect by significantly inhibiting croton oil-induced ear edema. All SO doses tested significantly inhibited leukocyte chemotaxis induced by casein and reduced the number of rolling, adhesion, and leukocytes migration to spermatic fascia after inflammatory stimulus. Our data demonstrated that SO has anti-inflammatory activity. Key words: Salvia officinalis, essential oil, anti-inflammatory, medicinal plants.

Effects of Thymol and Carvacrol, Constituents ofThymus vulgarisL. Essential Oil, on the Inflammatory Response

Thyme (Thymus vulgaris L., Lamiaceae) is an aromatic and medicinal plant that has been used in folk medicine, phytopharmaceutical preparations, food preservatives, and as an aromatic ingredient. The effect of Thymus vulgaris essential oil (TEO) and its isolated constituents thymol and cavacrol (CVL) were studied in the following experimental models: ear edema, carrageenan-induced pleurisy, and chemotaxis in vitro. In the pleurisy model, TEO, CVL, and thymol significantly inhibited inflammatory edema. However, only TEO and CVL inhibited leukocyte migration. In the in vitro chemotaxis experiment, CVL inhibited leukocyte migration, whereas thymol exerted a potent chemoattractant effect. In the ear edema model, CVL (10 mg/ear), applied topically, reduced edema formation, exerting a topical anti-inflammatory effect. Thymol did not reduce edema formation but rather presented an irritative response, probably dependent on histamine and prostanoid release. Our data suggest that the antiinflammatory effects of TEO and CVL are attributable to the inhibition of inflammatory edema and leukocyte migration.

Attenuation of experimental TPA-induced dermatitis by acetylenic acetogenins is associated with inhibition of PLA 2 activity

Topical application of acetylenic acetogenins (AAG) from avocado (0.01–1.0 mg/ear), was effective in inhibiting both 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear edema, and in decreasing tissue myeloperoxidase activity (indicative of polymorphonuclear leukocyte influx). Maximum edema inhibition of 72% was achieved by AAG at lower concentration (0.6 mg/ear) than that of the anti-inflammatory drug indomethacin (2 mg/ear). The maximum myeloperoxidase inhibition of 60% was obtained at AAG concentration 0.1 mg/ear. Chemical reduction of unsaturated bonds in aliphatic chain of AAG molecules almost abrogated inhibition effect of AAG at high concentration. In vitro AAG administration reduced secretion of PGE 2 in TPA-induced keratinocytes, and inhibited total PLA 2 and sPLA 2 activities in HaCaT cells. The results indicate a topical anti-inflammatory effect of acetylenic acetogenins which is associated with inhibition of PLA 2 activity in skin.

Effectiveness of Vernonia scorpioides ethanolic extract against skin inflammatory processes

Ethnopharmacological relevanceVernonia scorpioides (Asteraceae) is a native Brazilian medicinal plant that is commonly used to treat skin disorders. Considering the traditional use of Vernonia scorpioides and the lack of information about its pharmacological properties, we investigated the topical anti-inflammatory effect of the ethanolic extract of Vernonia scorpioides (EEVS) on acute and chronic cutaneous inflammation models in mouse. Materials and methodsThe topical anti-inflammatory effect of EEVS was evaluated against acute models (12-O-tetradecanoylphorbol acetate (TPA)- and arachidonic acid (AA)-induced mouse ear oedema) and chronic models (multiple applications of croton oil). ResultsThe EEVS caused a dose-related inhibition of oedema in both the TPA- and AA-induced acute models (DI50=0.24 and 0.68mg/ear with an inhibition of 80±5% and 65±5%, respectively, for 1mg/ear). In addition, the TPA-induced increase in myeloperoxidase activity (MPO) in the ear was reduced (77±8%) by the topical application of EEVS. In the chronic model, the EEVS reduced all parameters evaluated: oedema formation (31±2%), epidermal hyperproliferation (histology) and MPO (25±10%). However, the topical treatment of EEVS had no effect on N-acetyl-β-d-glucosaminidase activity. The EEVS effectively interfered in the ear oedema on the delayed-type hypersensitivity reaction induced by oxazolone. The topical treatment with EEVS performed on both phases or only on the elicitation phase caused the inhibition of the ear oedema-induced by oxazolone in 42.9% and 63.4%, respectively, when compared to control animals (sensitized and challenged). ConclusionsThe results suggest that EEVS is effective as a topical anti-inflammatory agent in acute and chronic inflammatory processes and that its action is markedly influenced by the inhibition of neutrophil migration into inflamed tissue as well as by epidermal hyperproliferation.

Topical anti-inflammatory and analgesic activity of kirenol isolated from Siegesbeckia orientalis

Ethnopharmacological relevanceSiegesbeckia orientalis has been traditionally used as a topical anti-inflammatory and analgesic agent. Aims of the studyCurrent study was designed to explore the topical anti-inflammatory and analgesic effects of a constituent isolated from Siegesbeckia orientalis (Compositae), in order to validate its folk use. Materials and methodsKirenol was isolated from ethanolic extract of Siegesbeckia orientalis. Several topical formulations containing kirenol were investigated for anti-inflammatory and analgesic activities in rat. The effects were studied using carrageenan-induced rat acute inflammation model, complete Freund's adjuvant (CFA)-induced chronic inflammation and formalin test in rats. Piroxicam gel and methyl salicylate ointment were studied as positive control for anti-inflammatory and analgesic activity, respectively. ResultsThe anti-inflammatory effect of kirenol 0.4–0.5% (w/w) was similar to the effect of piroxicam gel 4h after carrageenan injection. The analgesic activity of topical preparation with more than 0.4% (w/w) was observed in the late phase. These effects may be due, at least in part, to the pro-inflammatory cytokine production of IL-1β and TNF-α. The administration of kirenol cream at the dose of 0.3, 0.4 and 0.5% (w/w) significantly inhibited the development of joint swelling induced by CFA, which was auxiliary supported by histopathological studies. ConclusionKirenol has demonstrated its significant potential to be further investigated for its discovery as a new lead compound for management of topical pain and inflammation, although further pharmacological research is necessary to fully understand its mechanism of action. It also supports the potential beneficial effect of topically administered Siegesbeckia orientalis in inflammatory diseases.

Topical anti-inflammatory constituents of lipophilic leaf fractions of Alchornea floribunda and Alchornea cordifolia

The leaves of Alchornea floribunda and Alchornea cordifolia are used traditionally as topical anti-inflammatory agents. In this study, two highly lipophilic fractions AFLF and ACLF isolated from A. floribunda and A. cordifolia leaves respectively were investigated for topical anti-inflammatory effects using xylene-induced mice ear oedema as a model of inflammation. AFLF and ACLF at 5 mg per ear showed significant (p < 0.01) topical anti-inflammatory effect with oedema inhibitions of 64.0% and 79.0% at 2 h, respectively. When compared to indomethacin (5 mg per ear), these fractions showed significantly (p < 0.05) higher topical anti-inflammatory effect. Gas chromatography–mass spectrometry analysis revealed that AFLF is composed mainly of long chain saturated and unsaturated hydrocarbons (18.78%) and their oxygenated derivatives (1.89%); while ACLF is rich in volatile oils eugenol (21.26%) and cadinol (4.76%), and other constituents like, nanocosaine (36.86%) and steroid derivatives, ethyl iso-allocholate (4.59%) and 3-acetoxy-7,8-epoxylanostan-1-ol (15.86%). Analysis of the volatile oil (ACV) extracted from the fresh leaves of A. cordifolia revealed the presence of high concentrations of eugenol (41.7%), cadinol (2.46%), Caryophylene (1.04%), Linalool (30.59%) and (E)-α-bergamotene (4.54%). These compounds could be contributing to the topical anti-inflammatory effects of A. floribunda and A. cordifolia leaf extracts.

Topical anti-inflammatory effect of hypocholesterolaemic drugs

The topical anti-inflammatory effect of simvastatin, atorvastatin, pravastatin, ezetimibe and combined ezetimibe + simvastatin was investigated, using the croton oil model of ear oedema in mice. Simvastatin, atorvastatin, pravastatin, ezetimibe and ezetimibe + simvastatin combination (dissolved in 20 µl of 70% acetone) were topically applied simultaneously with croton oil (200 µg/ear, dissolved in 20 µl of 70% acetone) at the inner surface of each ear. Ear oedema and myeloperoxidase activity, indicative of polymorphonuclear cell migration, were assessed 6 h after inflammatory stimuli. It was found that statins can act as topical anti-inflammatories, but the pharmacological effect is dependent on statin polarity. At 0.3 mg/ear inhibition of ear oedema was 79%, 67% and 40% for simvastatin, atorvastatin and pravastatin, respectively. Simvastatin and atorvastatin also remarkably diminished myeloperoxidase activity, even at low concentrations (0.03 mg/ear). Pravastatin, the most polar statin, however, did not cause any reduction in ear oedema or myeloperoxidase activity at low doses. The order of topical anti-inflammatory activity was pravastatin < < < atorvastatin ≤ simvastatin. Ezetimibe, another hypocholesterolaemic drug, also presented anti-inflammatory effects, inhibiting ear oedema by 64% at 0.3 mg/ear. However, when used in combination with simvastatin, no further beneficial effect was observed. These results consistently support current evidence showing that statins can be used for treatment of dermatological disorders. Polarity of the molecule, however, is a factor that should be considered before recommending use.

Effects of the black tea polyphenol theaflavin‐2 on apoptotic and inflammatory pathways in vitro and in vivo

Theaflavin-2 (TF-2), a major component of black tea extract, induces apoptosis of human colon cancer cells and suppresses serum-induced cyclooxygenase-2 (COX-2) expression 1. Here, we explored the mechanisms for activation of apoptosis, evaluated the impact on inflammatory genes in a broader panel of cells and tested whether topical anti-inflammatory effects could be observed in vivo. TF-2 triggered apoptosis in five other transformed cancer cell lines, inducing cell shrinkage, membrane blebbing, and mitochondrial clustering within 3 h of treatment. Among a set of pro-apoptotic genes, TF-2 quickly induced the up-regulation of P53 and BAX, suggesting mitochondria as the primary target. Using a cell model for inflammatory response, we showed that TF-2 suppressed the 12-O-tetradecanoylphorbol-13-acetate-induced COX-2 gene expression, and also down-regulated TNF-α, iNOS, ICAM-1, and NFκB. A reporter gene assay showed that TF-2 down-regulated COX-2 at the transcriptional level. We also demonstrated that TF-2 exhibited anti-inflammatory activity in two mouse models of inflammation. Topical application with TF-2 significantly reduced ear edema and produced a pattern of gene down-regulation similar to that observed in the cell model. These results suggest that the anti-inflammatory and pro-apoptotic activity of TF-2 may be exploited therapeutically in cancer and other diseases associated with inflammation.

Analysis of the Potential Topical Anti‐Inflammatory Activity of Averrhoa carambola L. in Mice

Inflammatory skin disorders, such as psoriasis and atopic dermatitis, are very common in the population; however, the treatments currently available are not well tolerated and are often ineffective. Averrhoa carambola L. (Oxalidaceae) is an Asian tree that has been used in traditional folk medicine in the treatment of several skin disorders. The present study evaluates the topical anti-inflammatory effects of the crude ethanolic extract of A. carambola leaves, its hexane, ethyl acetate, and butanol fractions and two isolated flavonoids on skin inflammation. Anti-inflammatory activity was measured using a croton oil-induced ear edema model of inflammation in mice. Topically applied ethanolic extract reduced edema in a dose-dependent manner, resulting in a maximum inhibition of 73 ± 3% and an ID50 value of 0.05 (range: 0.02–0.13) mg/ear. Myeloperoxidase (MPO) activity was also inhibited by the extract, resulting in a maximum inhibition of 60 ± 6% (0.6 mg/ear). All of the fractions tested caused inhibition of edema formation and of MPO activity. Treatment with the ethyl acetate fraction was the most effective, resulting in inhibition levels of 75 ± 5 and 54 ± 8% for edema formation and MPO activity, respectively. However, treatment of mice with isolated compounds [apigenin-6-C-β-l-fucopyranoside and apigenin-6-C-(2″-O-α-l-rhamnopyranosyl)-β-l-fucopyranoside] did not yield successful results. Apigenin-6-C-(2″-O-α-l-rhamnopyranosyl)-β-l-fucopyranoside caused only a mild reduction in edema formation (28 ± 11%). Taken together, these preliminary results support the popular use of A. carambola as an anti-inflammatory agent and open up new possibilities for its use in skin disorders.

Evaluation of Glycofurol-Based Gel as a New Vehicle for Topical Application of Naproxen

In view of the good skin tolerability, glycofurol was used as a vehicle-based gel, and its effect in the topical penetration of Naproxen (NAP) was investigated. The aims of this study were to develop a suitable gel with bioadhesive property, spreadability, and viscosity for topical anti-inflammatory effect. Three gelling and adhesive agents were examined: Carbopol 974P, Gantrez AN 119, and polyvinylpyrollidone K30. Skin permeation rates and lag times of NAP were evaluated using the Franz-type diffusion cell in order to optimize the gel formulation. The permeation rate of NAP-based gel across the excised rat skin was investigated. A significant increase in permeability parameters such as steady-state flux (J(ss)), permeability coefficient (K(p)), and penetration index (PI) was observed in optimized formulation containing 2% Transcutol as an permeation enhancer. From skin irritation test, it was concluded that the optimized novel glycofurol-based gel formulation was safe to be used for topical drug delivery. The developed glycofurol-based gel appeared promising for dermal and transdermal delivery of naproxen and could be applicable with water-insoluble drugs, which would circumvent most of the problems associated with drug therapy.

Topical anti-inflammatory effect of Caryocar coriaceum Wittm. (Caryocaraceae) fruit pulp fixed oil on mice ear edema induced by different irritant agents

Caryocar coriaceum Wittm. fruit pulp fixed oil (CCFO) has been widely employed by communities from Brazil Northeastern in the treatment of skin inflammation, respiratory affections, wound healing and muscle pain. In this study, we evaluated the topical effect of CCFO against different irritant agents in vivo, in order to verify its antiedematous effect as well to unravel its tentative mechanisms of action. CCFO was obtained from Caryocar coriaceum fruits using ethyl acetate as solvent. Ear edema provoked by the application of Croton oil (single and multiple applications), arachidonic acid (AA), capsaicin, phenol and histamine to Swiss mice was used to evaluate the topical anti-inflammatory effect of CCFO. Histological analysis from mice ears sensitized with Croton oil and AA single application was also performed. Crude CCFO (20μL/ear) demonstrated significant topical antiedematous effect against Croton oil single (inhibition of 32.0%; P<0.05) and multiple (41.4% after 9 days, P<0.001) applications, AA (inhibition of 49.7%; P<0.01) and phenol (inhibition of 38.8%; P<0.001). In contrast, CCFO did not antagonize the edema caused by topical treatment with capsaicin and histamine when compared to control group (P>0.05). Histological analysis also revealed that CCFO was able to reduce the edema and the influx of inflammatory cells in mice ears sensitized with Croton oil and AA. CCFO exhibited a similar profile of topical anti-inflammatory activity to that of drugs that classically modulate the production of arachidonic acid metabolites. The study also indicates the potential application of CCFO as an important herbal medicine to be used against skin inflammatory diseases.

Anti-inflammatory effect of crude extract and isolated compounds from Baccharis illinita DC in acute skin inflammation

Ethnopharmacologycal relevance The tea from the leaves of Baccharis illinita DC ( Asteraceae family) is commonly used by the population as anti-inflammatory (including topically), protective gastric and anti-infectious. However, no studies have been done with this species to confirm its topical anti-inflammatory action. Aim This study evaluated he topical effects of crude extract of leaves (CE) and its active constituents in 12-O-tetradecanoilforbol acetate (TPA)-induced ear oedema. Methodology CE and compounds effects were tested in commonly used models of TPA-, arachidonic acid (AA)- and capsaicin-ear oedema. Polymorphonuclear (PMN) cell migration was evaluated by mieloperoxidase and analyzed histologically. Results CE (0.1–1 mg/ear) caused a dose-related inhibition of TPA-induced ear oedema and PMN influx similarly to that produced by topical application of the steroidal anti-inflammatory drug dexamethasone. The active constituents of the AcOEt fraction kaurenoic acid, α-spinasterol, oleanolic acid and baurenol also inhibited TPA-induced ear edema. Histological analysis of the ear of CE-treated animals confirmed the reduction of edema and of PMN infiltration. Both CE and the nosteroidal anti-inflammatory drug indomethacin inhibited the AA-induced ear oedema, but did not change capsaicin-induced oedema. Conclusion These results indicate that the CE and the active constituents have a topical anti-inflammatory effect and the possible mechanisms for the pharmacological effects are discussed.

Anti-inflammatory efficiency of levobupivacaine in an experimental colitis model

To investigate the efficiency of levobupivacaine in treating experimentally induced colitis in rats. Colitis was induced by trinitrobenzene sulfonic acid and ethanol in 30 rats under general anesthesia, and 10 rats were used as a sham group. Subsequent to induction of colitis, rats were divided into three groups; budesonide group received 0.1 mg/kg budesonide, levobupivacaine group received 10 mg/kg levobupivacaine and saline group received 1 mL saline solution via rectal route for 7 d. In the sham group, only routine rectal catheterization was performed without use of any material. At the end of 7 d, laparotomy and total colectomy were performed for histopathological examination in all rats and blood samples were drawn for measurement of tumor necrosis factor (TNF)-alpha and interleukin (IL)-6 following cardiac puncture. Macroscopic and microscopic evaluations of the specimens were performed by a pathologist blinded to group assignment of the rats. Weight loss (P = 0.016) and macroscopic examination scores (P = 0.001) were significantly higher in saline group than others. Histopathological scoring was comparable between all colitis groups (P = 0.350). There was no significant difference in TNF-alpha levels and IL-6 levels (P = 0.150). The significant improvement in macroscopic scores suggests that levobupivacaine may have topical anti-inflammatory effects in an experimental colitis model; however, this finding was not supported by microscopic findings.

Anti-inflammatory and Membrane-stabilizing Stigmastane Steroids fromAlchornea floribundaLeaves

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.

Topical anti-inflammatory effect of tirucallol, a triterpene isolated from Euphorbia lactea latex

Latex from Euphorbia lactea (Euphorbiaceae), a native Dominican medicinal plant, is claimed to be useful in the treatment of inflammation. Topical application of tirucallol, a tetracyclic triterpene isolated from Euphorbia lacteal latex, suppressed ear edema in the mouse model in a dose-dependent manner, as well as affecting the influx of polymorphonuclear cells in response to topical application of 12-O-tetradecanoylphorbol-acetate (TPA) in the mouse ear. In addition, the effect of tirucallol, on some macrophage functions was analyzed in vitro. Non-toxic concentrations of tirucallol potently inhibited nitrite production in lipopolysaccharide-stimulated macrophages. Western blot analysis showed that nitric oxide reduction was a consequence of the inhibition of inducible nitric oxide synthetase expression although tirucallol slightly affected to prostaglandin E(2) (PGE(2)) generation. The results of the study revealed that tirucallol (0.3%), present in Euphorbia lactea latex, exerts a topical anti-inflammatory effect in vivo, via a mechanism of action related to the neutrophil migration. On the other hand, it can be deduced that the mechanism of the anti-inflammatory activity of this triterpene is related to the control of the production of NO and its effect on the expression of iNOS.

Topical anti-inflammatory effect of lipophilic constituents from Alchornea floribunda and Alchornea cordifolia leaves

The leaves of Alchornea floribunda and Alchornea cordifolia are used traditionally as topical anti-inflammatory agents. Several studies have shown that the hexane extracts of the plant materials exhibited significant anti-inflammatory activity [1,2,3]. In the present study, we subjected the hexane extracts of Alchornea floribunda and Alchornea cordifolia leaves to column chromatographic separation and isolated two highly lipophilic fractions AFLF and ACLF respectively. The anti-inflammatory effects of these fractions were investigated using xylene – induced oedema as a model of inflammation. AFLF and ACLF at 5mg/ear showed significant (P&lt;0.001) topical anti-inflammatory effect with oedema inhibitions of 64.0 and 79.0% at 2h respectively. These fractions showed significantly higher topical anti-inflammatory effect than 5mg/ear indomethacin (oedema inhibition of 48% at 2h). GC/MS analysis of these fractions revealed that AFLF is composed mainly of long chain saturated and unsaturated hydrocarbons (18.78%) and their oxygenated derivatives (1.89%), long chain carboxylic (fatty) acids (2.72%) and their esters (5.53%); while ACFL is rich in volatile oils euginol (21.26%) and cadinol (4.76%) and other constituents like long chain primary alcohols (4.78%), long chain saturated hydrocarbon, nanocosane (36.86) and steroid derivatives, ethyl iso-allocholate (4.59%) and 3-acetoxy-7,8-epoxylanostan-1-ol (15.86%). These constituents are highly lipophilic and can easily permeate lipoidal layers of skin. They may contribute significantly to the observed topical anti-inflammatory effect of Alchornea floribunda and Alchornea cordifolia leaf extracts.

Topical anti-inflammatory effects of Ocimum basilicum leaf extract in the phorbol-12,13-dibutyrate model of mouse ear inflammation

Topical anti-inflammatory effects of Ocimum basilicum leaf extract in the phorbol-12,13-dibutyrate model of mouse ear inflammation

Anti-inflammatory effects of ethanolic extract and alkamides-derived from Heliopsis longipes roots

Ethnopharmacological relevance Heliopsis longipes (A. Gray) Blake (Asteraceae) is a broadly used species in the Mexican, Central and South American Traditional Medicine for its anaesthetic, analgesic, anti-inflammatory and anti-ulcerative properties. The ethanolic extract contains alkamides, mainly affinin (spilanthol). This family of compounds exerts an in vitro inhibitory action on the cyclooxygenase and lipoxygenase enzymes. Aim of the study The present study approaches the anti-inflammatory effect of the extract and its main bioactive component affinin and derived isobutyl-decanamide. Materials and methods The anti-inflammatory effect was evaluated through the mouse ear oedema test by means of two irritating agents, arachidonic acid (AA) and phorbol myristate acetate (PMA). Results Heliopsis longipes, affinin and isobutyl-decanamide displayed a marked anti-inflammatory effect on the AA model with ED 50 = 0.8, 1.2 and 0.9 mg/ear, respectively. Nimesulide (1 mg/ear) was used as a reference drug. In PMA model, the extract and two alkamides also showed a dose-dependent anti-inflammatory effect with ED 50 = 2.0, 1.3 and 1.1 mg/ear, respectively. Indomethacin (3 mg/ear) was used as reference drug. Conclusions These results could represent an important contribution to explain the anti-inflammatory ethnobotanical effects reported for Heliopsis longipes and other species containing affinin (spilanthol). For the first time the topical anti-inflammatory effects of Heliopsis longipes, affinin and isobutyl-decanamide were studied.