Carrageenan Test Research Articles

Evaluation of the analgesic and anti-inflammatory activities of Annona senegalensis Pers. (Annonaceae) leaves aqueous extract in rats and mice

Annona Senegalensis Pers. (Annonaceae) is a medicinal plant used to treat many pathologies, including inflammatory diseases and pain. The aim of this study was to investigate the analgesic and anti-inflammatory properties of Annona Senegalensis leaves aqueous extract in mice and rats. The analgesic activity was evaluated using the acetic acid (1%) induced writhing test and formalin (1%) test. The anti-inflammatory activity was performed using the carrageenan and the dextran induced hind paw oedema in rats. The extract induced a significant (p<0.05) and dose-dependent decrease in abdominal contortions compared with control mice. The maximum inhibition was 63.36% at the dose of 200 mg/kg body weight. Only the late phase of formalin induced nociception was significantly inhibited by the extract with a maximum inhibition value of 56.96% at the dose of 200 mg/kg body weight. In the anti-inflammatory investigation, the aqueous extract of the leaves of Annona Senegalensis produced a significant (p<0.05) and dose-dependent decrease in edema induced by carrageenan and dextran. The maximum inhibition was 57.14% obtained at the fifth hour at the dose of 200mg/kg for the carrageenan test. For the dextran test, the maximum inhibition was 59.80% obtained at the second hour at the dose of 200 mg/kg body weight. Our results show that Annona Senegalensis has peripheral analgesic and anti-inflammatory properties. It could therefore be an advantage in alternative medicine. Keywords: Analgesic, Anti-inflammatory, Annona Senegalensis, Rats, Mice

5+1-Heterocyclization as preparative approach for carboxy-containing triazolo[1,5-c]quinazolines with anti-inflammatory activity

Present article is devoted to the purposeful search of novel anti-inflammatory agents among carboxyl-containing partially hydrogenated [1,2,4]triazolo[1,5-с]quinazolines and products of their tandem cyclization. It has been shown that target compound’s could be obtained via interaction between [2-(3-R-1H-1,2,4-triazol-5-yl)phenyl]amines and oxo-containing carboxylic acids and their esters of various structure. The structures of synthesized compounds were verified by appropriate methods, the features of NMR-spectra patterns were discussed as well. The low predicted toxicity of obtained compounds has been estimated using in silico methods. In vivo study on the model of acute aseptic inflammation (carrageenan test) have been revealed that synthesized compounds expose anti-inflammatory activity in the range of 0.94–52.66%. 4-(2-(Ethoxycarbonyl)-5,6-dihydro-[1,2,4]triazolo[1,5-c]quinazolin-5-yl)benzoic acid has been identified as most active compound. Additionally, the effects of some (2-R-5,6-dihydro[1,2,4]triazolo[1,5-c]quinazolin-5-yl)benzoic acids (compounds 3) on the levels of key inflammatory markers have been estimated. It has been shown that studied compounds decrease the level of neutrophils, COX-2, nitrotyrosine, IL-1b, C-reactive protein and increase level of eNOS. 4-(2-(Ethoxycarbonyl)-5,6-dihydro-[1,2,4]triazolo[1,5-c]quinazolin-5-yl)benzoic acid (3.2) has been identified as compound with most expressed anti-inflammatory activity and significant effect on the levels of marker of inflammatory processes. Molecular docking study towards СОХ-1 and СОХ-2 has been conducted to substantiate possible mechanism of obtained compounds anti-inflammatory activity. It has been found that fixation of 4-(2-(ethoxycarbonyl)-5,6-dihydro-[1,2,4]triazolo[1,5-c]quinazolin-5-yl)benzoic acid (3.2) molecule in active site of enzyme is outstandingly similar to the reference ligands. The essential value of carboxylic group for presence of anti-inflammatory activity has been estimated as result of SAR-analysis. It has been found that studied class of compounds is perspective for further structural modification aimed to the creation of novel anti-inflammatory agents.

Anti-inflammatory and antinociceptive effects of sitagliptin in animal models and possible mechanisms involved in the antinociceptive activity.

Sitagliptin is an antidiabetic drug that inhibits dipeptidyl peptidase-4 enzyme. This study aimed to investigate the antinociceptive and anti-inflammatory effects of sitagliptin in formalin and carrageenan tests and determine the possible mechanism(s) of its antinociceptive activity. Male Swiss mice (25-30 g) and male Wistar rats (180-220 g) were used for formalin and carrageenan tests, respectively. In the formalin test, paw licking time and in the carrageenan test, paw thickness were considered as indexes of pain behavior and inflammation respectively. Three doses of sitagliptin (2.5, 5, and 10 mg/kg) were used in these tests. Also, several antagonists and enzyme inhibitors were used to evaluate the role of adrenergic, serotonergic, dopaminergic, and opioid receptors as well as the NO/cGMP/KATP pathway in the antinociceptive effect of sitagliptin (5 mg/kg). Sitagliptin showed significant antinociceptive and anti-inflammatory effects in the formalin and carrageenan tests respectively. In the carrageenan test, all three doses of sitagliptin significantly (P < 0.001) reduced paw thickness. Pretreatment with yohimbine, prazosin, propranolol, naloxone, and cyproheptadine could not reverse the antinociceptive effect of sitagliptin (5 mg/Kg), which indicates that adrenergic, opioid, and serotonin receptors (5HT2) are not involved in the antinociceptive effects. L-NAME, methylene blue, glibenclamide, ondansetron, and sulpiride were able to reverse this effect. NO/cGMP/KATP, 5HT3 and D2 pathways play an important role in the antinociceptive effect of sitagliptin. Additionally significant anti-inflammatory effects observed in the carrageenan test might contribute in reduction of pain response in the second phase of the formalin test.

Antinociceptive and anti-inflammatory actions of curcumin and nano curcumin: a comparative study.

Pain and inflammation can be treated by various therapies that for the most part are not effective and can result in adverse effects. The current study was proposed to compare the antinociceptive and anti-inflammatory actions of curcumin and nano curcumin in rats. Rats were randomly allocated into ten groups of six for formalin and tail-flick tests including the control group, curcumin and nano curcumin groups (20, 50, 100 mg/kg), morphine group (10 mg/kg), naloxone + 100 mg/kg curcumin group, and naloxone + 100 mg/kg nano curcumin group. There were nine groups for the carrageenan test. Groups 1-7 were the same as the previous division; groups 8 and 9 received 10 mg/kg diclofenac and 1% carrageenan, respectively. All doses of nano curcumin significantly decreased the paw-licking time in both phases of the formalin test. In the tail-flick test, curcumin 100, nano curcumin 100, naloxone + curcumin 100, and naloxone + nano curcumin 100 showed significant analgesic effects compared to the control group. In the paw edema test, at 180 s after injection, curcumin (50 and 100 mg/kg) and all doses of nano curcumin significantly inhibited carrageenan-induced edema. Myeloperoxidase activity and lipid peroxidation decreased at doses of 50 and 100 mg/kg of curcumin but at three doses of nano curcumin (20, 50, and 100 mg/kg). In conclusion, our results suggest that the nanoemulsion formulation of curcumin can be efficient in reducing pain and especially inflammation in lower doses compared to the native form of curcumin.

The possible anti-inflammatory properties of hydro-ethanolic extract of Oregano

Backgrounds: Plant compounds are of great value due to their analgesic, anti-inflammatory, cytotoxic, and other characteristics. This study aimed to examine the chemical composition and impact of the Origanum vulgare hydro-ethanolic extract on nociceptive behavior and anti-inflammatory properties in in vivo mice models.Methods: Gas chromatography-mass spectrometry and high-performance liquid chromatography techniques were employed to determine the major active phytochemicals of the extract. The effects of the extract on nociceptive reactions were evaluated using formalin and hot plate tests, while the anti-inflammatory effect was determined using the Carrageenan test. The methyl-thiazolyl-tetrazolium assay was applied to analyze growth-inhibiting properties of the extract on MCF-7 breast cancer cells.Results: Various flavonoids and organic acids were identified in O. vulgare hydro-ethanolic extract. The extract possessed low cytotoxicity on MCF-7 cells as only 1 mg/mL or higher concentrations of the extract induced considerable growth inhibition. The formalin and hot plate tests demonstrated some sensitizing effects of the investigated extract (5 mg/kg) on mice. Moreover, the Carrageenan test revealed pronounced anti-inflammatory properties of the O. vulgare extract.Conclusion: The potent biological activity of the wild oregano herb extract makes it a promising source for the development of medicinal preparations. Keywords: Nociceptive behavior, anti-inflammatory effect, Oregano, flavonoids, chemical composition, cytotoxicity, in vivo mice models.

Mineral composition, principal polyphenolic components, and evaluation of the anti-inflammatory, analgesic, and antioxidant properties of Cytisus villosus Pourr leaf extracts

Abstract Cytisus villosus Pourr. (C. villosus) is a medicinal plant belonging to the Fabaceae family, which grows in the Mediterranean area. It is used in traditional medicine against diseases related to inflammation. The objective of the present study was to identify the mineral and polyphenolic composition as well as to evaluate some biological properties including antioxidant, anti-inflammatory, and analgesic activities of C. villosus leaf aqueous extract. The chemical constituents were identified and quantified using ultra performance liquid chromatography-electrospray ionization tandem mass spectrometry (UPLC-ESI-MS/MS) methods. The antioxidant properties of C. villosus leaves were tested using reducing power (RP), 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS), and 2,2′-diphenyl-1-picrylhydrazyl (DPPH) assays. The anti-inflammatory potency was evaluated in vitro and in vivo using the albumin denaturation test and the carrageenan test, respectively. Furthermore, the analgesic effect was performed in vivo using tail flick, acetic acid-induced contortion, and plantar tests. Mineralogical analysis revealed that potassium and calcium were the most abundant minerals. The analysis and quantification of the phytochemical composition using UPLC-ESI-MS/MS showed that quinic acid (57.478 ± 1.72 mg/kg) was the major compound of the aqueous extract, followed by salicylic acid (17.38 ± 0.2 mg/kg), isoquercetin (16.895 ± 1.01 mg/kg), and gallic acid (15.914 ± 1.51 mg/kg). The extracts showed potent antioxidant activity for all tests used. The highest antioxidant activity was recorded for the DPPH, ABTS and RP methods, with an IC50 of 3.94 ± 0.09, 2.88 ± 0.07, and 1.94 ± 0.10 μg/mL, respectively. Additionally, using the most frequent analgesic assays, the aqueous extract at a dose of 500 mg/kg exhibited a potent analgesic activity. Notably, an interesting inhibition of albumin denaturation was recorded with an IC50 of 383.94 μg/mL, corroborating the in vivo test. Overall, the results presented here may represent a scientific basis for the traditional use of C. villosus in the treatment of inflammation-related diseases.

New NSAID Conjugates as Potent and Selective COX-2 Inhibitors: Synthesis, Molecular Modeling and Biological Investigation.

New sets of ibuprofen and indomethacin conjugates comprising triazolyl heterocycle were synthesized via click chemistry, adopting an optimized protocol through the molecular hybridization approach affording the targeted agents in good yields. The new non-steroidal anti-inflammatory drug (NSAID) conjugates were designed and synthesized and could be considered as potential drug candidates for the treatment of pain and inflammation. The anti-inflammatory properties were investigated for all the synthesized conjugates. Among 14 synthesized conjugates, four (5a, 5b, 5d, and 5e) were found to have significant anti-inflammatory properties potency 117.6%, 116.5%, 93.8%, and 109.1% in comparison to reference drugs ibuprofen (97.2%) and indomethacin (100%) in the rat paw edema carrageenan test without any ulcerogenic liability. The suppression effect of cytokines IL-6, TNF-α, and iNOS in addition to NO in the LPS-induced RAW264.7 cells supports the promising anti-inflammatory properties observed in the ibuprofen conjugates. In addition, several conjugates showed promising peripheral and central analgesic activity. The selectivity index (SI) of compound 5a (23.096) indicates the significant efficacy and selectivity for COX-2 over COX-1. Molecular modeling (docking and QSAR) studies described the observed biological properties.

Rubiadin exerts an acute and chronic anti-inflammatory effect in rodents

Rubiadin is identified as a bioactive anthraquinone that exists in some quinone rich plants. The current research was carried out to evaluate the potential anti-inflammatory impact of Rubiadin in acute and chronic inflammation test models in rodents. The anti-inflammatory activity of Rubiadin was examined in cotton pellet-induced granuloma and carrageenan-induced edema as chronic and acute inflammation models in rats. TNF-α level and histopathological changes were assessed using sampled foot tissue of rat in the acute model. Also, the IL-1β level was assessed in the chronic model. One-way ANOVA (post hoc Tukey's) analysis was used for comparing the groups. Rubiadin (0.5 mg/kg, i.p.) induced a significant reduction in TNF α level and the paw edema compared to the control group in carrageenan test. Also, it was observed that the anti-inflammatory activity of Rubiadin (0.5 mg/kg, i.p.) is comparable to mefenamic acid (30 mg/kg, i.p.) as the standard drug. Rubiadin was effective in granuloma induced by cotton pellet concerning the granuloma and transudate formation amount. Rubiadin's anti-inflammatory effects were associated with a significant IL-1β decrease in this model. The results suggest that Rubiadin as a natural compound can possess significant peripheral anti-inflammatory impacts.

Physicochemical In vivo Anti-Inflammatory effect of Tablet containing Fenoprofen

Fenoprofen, a potent nonsteroidal anti-inflammatory drug, is widely used for relief of pain in patients suffering from rheumatic diseases, migraine, sore throat and primary dysmenorrheal. However, this drug has many gastrointestinal side effects produced by its oral administration, such as gastric bleeding and peptic ulcer. These effects were responsible for non-compliance among patients, which ultimately results in treatment failure. The physicochemical properties of Fenoprofen, make it a suitable candidate for transdermal drug delivery, which can overcome the drawbacks of oral administration. In this sense, tablets have been proved to increase the cutaneous absorption of lipophilic drugs when compared to conventional drug delivery systems. The carrageenan test is highly sensitive to nonsteroidal anti-inflammatory drugs and has long been accepted as a useful model to determine the anti-inflammatory effects of natural products. In the present study the anti-inflammatory activity of Fenoprofen and superdisintegrant was investigated by experimental carrageenan animal model. In our study, the induction of carrageenan in the rat hind paw started off the vascular phase of inflammation which was characterized by temporary vasoconstriction and vasodilatation that generated an increase in the size of the edema for all groups.

Synergistic antinociceptive effects of concomitant NAAA and peripheral FAAH inhibition

The intracellular lipid amidases, fatty acid amide hydrolase (FAAH) and N-acylethanolamine acid amidase (NAAA), terminate the actions of anandamide and palmitoylethanolamide (PEA), two antinociceptive and anti-inflammatory lipid-derived mediators. Here we show, confirming prior research, that small-molecule inhibitors of peripheral FAAH (compound URB937) and systemic NAAA (compound ARN19702) individually attenuate, in male CD-1 mice, pain-related behaviors and paw inflammation in the formalin and carrageenan tests. More importantly, isobolographic analyses revealed that the combination of URB937 and ARN19702 produced substantial synergistic (greater than additive) antinociceptive effects in both models as well as additive anti-inflammatory effects in the carrageenan test. Together, the findings uncover a functional interplay between FAAH and NAAA substrates in the control of nociception, which might be exploited clinically to develop safe and effective pain management strategies

Toxicological profile, phytochemical analysis and anti-inflammatory properties of leaves of Vitex doniana Sweet. (Verbenaceae)

BackgroundNatural herbal compounds are a source and alternative for new compounds with anti-inflammatory properties. Therefore, in-depth studies should be carried out to assess their safety and efficacy in order to avoid or prevent toxicological risks of these natural plant-based substances. V. doniana is a species of food plant used for the treatment of inflammatory diseases in Burkina Faso. This study aimed to estimate the anti-inflammatory properties in vitro and in vivo of the ethyl acetate fraction of the leaves of V. doniana. MethodsTo do this, acute toxicity was first evaluated on the animal model. Biological activities (carrageenan test, formalin and xylene induced oedemas) were used to assess the anti-inflammatory power. ResultsRegarding the dietary toxicology of the extracts, visual and clinical signs showed that the extracts are not at the end of the 15-day (acute toxicity) and 45-day (subacute toxicity) tests. In terms of anti-inflammatory activity in vivo, it was observed that the bioactive fraction (50, 100 and 200 mg/kg.b.w) had effective neurogenic anti-inflammatory properties. All of these effects observed were all dose-dependent. ConclusionThe results of this present research have proven that V. donania extracts can be used as anti-inflammatories.

Approaches to synthesis of ([1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzoic acids as potential anti-inflammators

Despite their high efficacy NSAIDs have significant side effects due to non-selective inhibition of COX-1 and COX-2. Due to this, medical chemists still pay considerable attention to their design and synthesis, in particular the creation of hybrid molecules that combine in their structure a fragment with anti-inflammatory activity and the quinazoline heterocycle.&#x0D; The aim of the present study is to develop methods for the synthesis of [1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzoic acids as potential anti-inflammatory agents.&#x0D; Quinazolin-4(3H)-ylidene)hydrazides (hydrazones) of benzenedicarboxylic acids, their esters, products of their heterocyclization and nucleophilic degradation were the subjects of the study. The structure of the synthesized compounds was confirmed by elemental analysis and NMR spectroscopy. Anti-inflammatory activity was studied in a model of acute aseptic inflammation («carrageenan test») in rats.&#x0D; Possibilities and limitations of synthesis of [1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzoic acids and their esters via hetero­cyclization of the corresponding hydrazides and hydrazones oxidative cyclization are shown. It was found that the hydrolysis of 4-[(1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzoic acid esters is not a preparative method for the synthesis of the target acids, due to the hydrolytic cleavage of the pyrimidine cycle. Compounds 3, 4 and 6 with moderate anti-inflammatory activity have been identified, which can be used for further structural modification.&#x0D; Conclusions. It was found that quinazolin-4(3H)-ylidene)hydrazides (hydrazones) of benzenedicarboxylic acids and their esters under the conditions of heterocyclization and oxidative cyclization form [1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzoic acids and their esters. The synthesized compounds are carriers of anti-inflammatory activity and promising for further research.

Convenient Synthesis of 4-pyridinyloxy-Modified imidazo[2,1-b][1,3]thiazines as Potential Anti-inflammatory Agents

Novel imidazo[2,1-b][1,3]thiazine derivatives modified with 4-pyridinyloxyl moiety, as potential anti-inflammatory agents are described. Synthetic approach to the preparation of (6-((pyridin-4-yl)oxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazines 3a-f and their benzoanelated analogues 3g-j is based on the interaction of substituted 4-fluoropyridines with 3-hydroxy(benzo)imidazo[2,1-b][1,3]thiazines. The nucleophilic substitution reaction of the fluorine atom occurs selectively at position 4 of the pyridine ring. The drug-like properties of the first synthesized (4-pyridinyloxy)imidazo[2,1-b][1,3]thiazines were predicted in silico using SwissADME. Anti-inflammatory activity was studied in vivo using hind paw edema in white rats (carrageenan test). Compounds with satisfactory drug-like and pharmacological properties have been identified as promising for further structure optimization and in-depth research.

Selected Thiadiazine-Thione Derivatives Attenuate Neuroinflammation in Chronic Constriction Injury Induced Neuropathy.

Neuropathic pain refers to a lesion or disease of peripheral and/or central somatosensory neurons and is an important body response to actual or potential nerve damage. We investigated the therapeutic potential of two thiadiazine-thione [TDT] derivatives, 2-(5-propyl-6-thioxo-1, 3, 5-thiadiazinan-3-yl) acetic acid [TDT1] and 2-(5-propyl-2-thioxo-1, 3, 5-thiadiazinan-3-yl) acetic acid [TDT2] against CCI (chronic constriction injury)-induced neuroinflammation and neuropathic pain. Mice were used for assessment of acute toxicity of TDT derivatives and no major toxic/bizarre responses were observed. Anti-inflammatory activity was assessed using the carrageenan test, and both TDT1 and TDT2 significantly reduced carrageenan-induced inflammation. We also used rats for the induction of CCI and performed allodynia and hyperalgesia-related behavioral tests followed by biochemical and morphological analysis using RT-qPCR, immunoblotting, immunohistochemistry and immunofluorescence. Our findings revealed that CCI induced clear-cut allodynia and hyperalgesia which was reversed by TDT1 and TDT2. To determine the function of TDT1 and TDT2 in glia-mediated neuroinflammation, Iba1 mRNA and protein levels were measured in spinal cord tissue sections from various experimental groups. Interestingly, TDT1 and TDT2 substantially reduced the mRNA expression and protein level of Iba1, implying that TDT1 and TDT2 may mitigate CCI-induced astrogliosis. In silico molecular docking studies predicted that both compounds had an effective binding affinity for TNF-α and COX-2. The compounds interactions with the proteins were dominated by both hydrogen bonding and van der Waals interactions. Overall, these results suggest that TDT1 and TDT2 exert their neuroprotective and analgesic potentials by ameliorating CCI-induced allodynia, hyperalgesia, neuroinflammation and neuronal degeneration in a dose-dependent manner.

Anti-inflammatory Effect of the Alkaloid-rich Fraction of Landolphia owarensis

Background: Plants have several chemical compounds acclaimed to be responsible for the pharmacological actions produced when herbal products are administered to biological systems.Objectives: This study was designed to investigate the anti-inflammatory effect of the alkaloid-rich fraction of the ethanol leaf extract of Landolphia owariensis.Methods: Qualitative phytochemical analyses were carried on the crude extract using standard methods. The alkaloid-rich fraction was obtained from the crude ethanol extract, using the classical acid/base shake-up method and the obtained fraction tested positive to Dragendorf’s reagent. Oral acute toxicity was evaluated by OECD method (No 423). Anti-inflammatory effect of the fraction was evaluated using xylene-induce ear oedema and carrageenan-induced paw inflammation in mice at doses of 100, 200 and 400 mg/kg.Results: Phytochemical screening revealed presence of alkaloids, flavonoids, tannins, saponins, steroids/terpenes and glycosides. Acute toxicity studies showed no adverse symptoms of toxicity during the 14-day observation period and no mortality was recorded, thus the LD50 was estimated to be greater than 2000 mg/kg. The alkaloid-rich fraction dose-dependently inhibited inflammation induced by xylene and carrageenan. In the xylene test, the fraction produced significant inhibition of 41.70 % at 400 mg/kg (p ≤ 0.05) while in the carrageenan test 55.69 % significant inhibition (p ≤ 0.001) was recorded with 400 mg/kg at 60 mins after induction of inflammation.Conclusion: This study showed the anti-inflammatory potentials of the alkaloid-rich fraction of Landophia owariensis.

Characteristics of Kappaphycus alvarezii carrageenan from different cultivation locations

This research aimed to determining physical and chemical characteristics of Kappaphycus alvarezii carrageenan from Bontang and and East Kutai. The method carrageenan extraction process was carried out in the water bath equipped by stirrer. Furthermore, the extraction process was conducted with a constant ratio of seaweed weight to distilled water volume (10:100 g/ml) at 75 o C for an hour. The extract was precipitated in Potassium hydroxide (KOH) 6%, potassium chloride 0.2% and ethanol which increase the speed of carrageenan formation. They were dried in an oven at 60 o C for 24 hours. The chemical carrageenan test results showed the water content seaweed from Bontang (12.7%), East Kutai (12.74%), ash content seaweed from Bontang (32.49 %) and East Kutai (33.80%), pH seaweed from Bontang (8.58) and East Kutai (8.52); the physical characteristic results showed the fiber seaweed from Bontang (7.45 %) and East Kutai (9.78%), the viscocity of carrageenan seaweed from Bontang (16.38 cPs) and East Kutai (11.19 cPs) and gel strength of carrageenan seaweed from Bontang (408.00 g/cm 2 ) and East Kutai (411.67 g/cm 2 ). This physical and hemical characteristics of Kappaphycus alvarezii , meet the quality standard regulated by FAO, FCC and EEC

Phytochemical Analysis and Antinociceptive Properties of Hydroalcoholic Extracts of Aleurites moluccanus Bark.

Aleurites moluccanus is used in folk medicine to treat many diseases including pain and inflammatory processes in general. Considering the potential of the leaf extract, evidenced in a previous study, the present study investigates the antinociceptive and anti-inflammatory properties of the hydroethanolic extract of A.moluccanus bark and isolated compounds in animal models of pain. The antinociceptive and anti-inflammatory activities of A.moluccanus bark were evaluated through hyperalgesia induced by carrageenan, PGE2, cytokines, bradykinin, epinephrine, Freund's complete adjuvant, and lipopolysaccharide. Five compounds were isolated from the dichloromethane bark extract: acetyl aleuritolic acid, atraric acid, spruceanol, (5β,10α)-12-hydroxy-13-methoxy-8,11,13-podocarpatrien-3-one and sonderianol. To optimize the extraction conditions, ethanol 50, 70, and 90°GL were used as extracting solvent, in a 1 : 20 (w/v) drug : solvent ratio, under stirring at room temperature for 4 h. The extracts were named AMC50, AMC70, and AMC90, respectively. These extracts were administered to mice (250 mg/kg, p. o.) with reduced mechanical hyperalgesia activity in the carrageenan test. Of these, AMC90 showed the best results. Pure (5β,10α)-12-hydroxy-13-methoxy-8,11,13-podocarpatrien-3-one showed a beneficial effect for up to 48 hours after the administration of carrageenan, while acetyl aleuritolic acid was effective only in the first hour. AMC90 was able to reverse the analgesia induced only by prostaglandin E2 and tumor necrosis factor. We also induced hyperalgesia using the lipopolysaccharide and Freund's complete adjuvant models, with positive results. These results support the antinociceptive and anti-inflammatory activity of A.moluccanus bark extract. The observed effects are partly due to the presence of acetyl aleuritolic acid, atraric acid, and (5β,10α)-12-hydroxy-13-methoxy-8,11,13-podocarpatrien-3-one.

Characterization of semi-refined kappa-carrageenan from Kappaphycus alvarezii with different solvents in Tanjung Sumenep

The quantity and quality of carrageenan produced is influenced by the method of extraction and the solvent. Characterization of the carrageenan products necessary to get certain standards so the carrageenan product acceptable to consumers both locally and internationally. The purpose of this research was to determine the solvents that can produce carrageenan from Kappaphycus alvarezii with the best characteristics and to compare the results of the extraction of carrageenan with international standards in order to obtain a standardized carrageenan. The results showed that the solvent produce a kappa-carrageenan from K. alvarezii with the best characteristics is NaOH 0.5 N. Kappa-carrageenan has been able to compared FAO, FCC and Marine Science Co., Ltd. standards for parameters : Gel strength, viscosity, sulfate content and ash content. Alkali able to extract and modify mu-carrageenan (precursor) into a kappa-carrageenan. The extraction process uses alkali caused the event ion exchange between cations in the solvent (K+ or Na+) ions with sulphate in the sea grass that reduced sulfate content. Need to do more research on the characterization of carrageenan include microbiological tests as well as the shelf life of carrageenan test.

Anti-inflammatory and Antinociceptive Activities of the Hydroalcoholic Extract and the Volatile Fraction of Southeastern Brazilian Brown Propolis

The analgesic and anti-inflammatory activities of a Southeastern Brazilian brown propolis were evaluated using the formalin test and carrageenan-induced mechanical hypernociception. The hydroalcoholic extract and the volatile fraction were evaluated at doses of 50, 100, and 200 mg/kg. In the formalin test, the crude extract reduced the response by 73, 83, and 89% for the first phase and 48, 65, and 75% for the second phase, respectively. The volatile fraction reduced the response by 75, 94, and 99% and 30, 53, and 91% for the first and second phases. For the carrageenan test, the hydroalcoholic extract and volatile fraction showed mechanical sensitization reductions of 57, 67, and 79% and 62, 79, and 88%, respectively, after 48 h. Indomethacin and morphine showed inhibitions of 42 and 88%, respectively. In the tail-flick assay, the results showed evidence of analgesic activities; the animals treated with crude extract increased the nociceptive threshold by 58 ± 8% and 70 ± 6% and 77 ± 10%, respectively, for evaluated doses, and 55 ± 6% and 73 ± 7% and 82 ± 14% for the volatile fraction, compared with control. The coadministration of naloxone altered the antinociceptive effect of morphine and propolis, suggesting that brown propolis has an action on the central nervous system.

Effect of a Selection of Skin Penetration Enhancers on Topical Anti-Inflammatory Effect of Boswellic Acids in Carrageenan-Induced Paw Edema in Rats.

Background:Boswellia species have been used for treatment of chronic inflammatory disease. Several studies have documented the anti-inflammatory effect of Boswellic acids (BAs) after systemic administration. This study was aimed to evaluate the effect of some skin penetration enhancers on topical anti-inflammatory effect of BAs in rats.Materials and Methods:Male Wistar rats weighting 180–220 were used. Anti-inflammatory activity was assessed using carrageenan test. BAs dissolved in ethanol, propylene glycol 2%, 5%, olive oil and applied topically. Menthol, D-limonene, or eucalyptus oil 0.5%, 1% were also tested as other skin penetration enhancers and applied topically 30 min prior to subplantar injection of carrageenan into the right hind paw of rats. The volume of the paw was measured at 0 and 4 h after carrageenan with a digital plethysmometer and the difference was used as an index of inflammation. Piroxicam gel was used as a standard drug.Results:A 4% ethanolic solution of BAs showed significant anti-inflammatory effect. Propylene glycol (2% and 5%) in alcohol did not change the effect. Olive oil also enhanced penetration of BAs. Menthol 0.5%, 1% and D-limonene 0.5%, 1% did not show any significant change compared to olive oil alone. In the present study, eucalyptus oil 1% in olive oil was known as the best carrier for transdermal delivery of BAs.Conclusion:BAs have considerable topical anti-inflammatory effects and olive oil alone or especially in combination with eucalyptus oil can be promising vehicles for skin penetration of topical BAs.