Anti-inflammatory activity of propolis

Propolis (bee-glue), known as a folk medicine, is a lipophilic material found in honeybee hives. In the present study on the anti-inflammatory effect of Korean propolis, it was extracted with ethanol, and used as a test material. The LD₅₀ value with the oral administration of ethanolic extract of Korean propolis (EEKP) was higher than 2 g/kg in mice. The oral administration of the propolis extract (100 mg/kg) significantly inhibited the development of hind paw edema induced by carrageenin in rats. The oral pretreatment of the propolis extract markedly inhibited the increase in vascular permeability and the number of writhing induced by acetic acid in mice. Propolis extract, 50 and 100 mg/kg p.o. per day for 7 days, produced a significant inhibitory effect on granuloma and exudate formation in rats. This inhibitory effect was enhanced with the concomitant use of prednisolone (2.5 mg/kg). These results suggest that Korean propolis apparently has a strong anti-inflammatory activity.     

Anti-inflammatory activity ofElsholtzia splendens

Elsholtzia splendens Nakai has been used in North-East Asia as an ingredient of folk medicines for treating cough, headache and inflammation. The present investigation was carried out to establish its in vivo anti-inflammatory activity using several animal models of inflammation and pain. The 75% ethanol extract of the aerial part of E. splendens significantly inhibited mouse croton oil-induced, as well as arachidonic acid-induced, ear edema by oral administration (44.6% inhibition of croton oil-induced edema at 400 mg/kg). This plant material also showed significant inhibitory activity against the mouse ear edema induced by multiple treatment of phorbol ester for 3 days, which is an animal model of subchronic inflammation. In addition, E. splendens exhibited significant analgesic activity against mouse acetic acid-induced writhing (50% inhibition at 400 mg/kg), while indomethacin (5 mg/kg) demonstrated 95% inhibition. E. splendens (5-100 microg/mL) significantly inhibited PGE2 production by pre-induced cyclooxygenase-2 of lipopolysaccharide-treated RAW 264.7 cells, suggesting that cyclooxygenase-2 inhibition might be one of the cellular mechanisms of anti-inflammation.     

Anti-inflammatory activity of ginsenoside ro

Ginsenoside Ro, an oleanane-type saponin has been screened for activity in experimental models of inflammation. Ginsenoside Ro (10,50, and 200 mg/kg, P. O.) inhibited an increase in vascular permeability in mice induced by acetic acid and reduced an acute paw edema in rats induced by compound 48/80 or carrageenin. Ginsenoside Ro did not suppress a developing adjuvant-induced edema in arthritic rats. However, ginsenoside Ro was found to be effective in hypercoagulable state, increase of connective tissue in the artery and calcium effluence from the bone in adjuvant-induced arthritic rats.     

Anti-inflammatory activity of cationic lipids

1. The effect of liposome phospholipid composition has been assumed to be relatively unimportant because of the presumed inert nature of phospholipids.
2. We have previously shown that cationic liposome formulations used for gene therapy inhibit, through their cationic component, the synthesis by activated macrophages of the pro-inflammatory mediators nitric oxide (NO) and tumour necrosis factor-α (TNF-α).
3. In this study, we have evaluated the ability of different cationic lipids to reduce footpad inflammation induced by carrageenan and by sheep red blood cell challenge.
4. Parenteral (i.p. or s.c) or local injection of the positively charged lipids dimethyldioctadecylammomium bromide (DDAB), dioleyoltrimethylammonium propane (DOTAP), dimyristoyltrimethylammonium propane (DMTAP) or dimethylaminoethanecarbamoyl cholesterol (DC-Chol) significantly reduced the inflammation observed in both models in a dose-dependent manner (maximum inhibition: 70–95%).
5. Cationic lipids associated with dioleyol- or dipalmitoyl-phosphatidylethanolamine retained their anti-inflammatory activity while cationic lipids associated with dipalmitoylphosphatidylcholine (DPPC) or dimyristoylphosphatidylglycerol (DMPG) showed no anti-inflammatory activity, indicating that the release of cationic lipids into the macrophage cytoplasm is a necessary step for anti-inflammatory activity. The anti-inflammatory activity of cationic lipids was abrogated by the addition of dipalmitoylphosphatidylethanolamine-poly(ethylene)glycol-2000 (DPPE-PEG₂₀₀₀) which blocks the interaction of cationic lipids with macrophages.
6. Because of the significant role of protein kinase C (PKC) in the inflammatory process we have determined whether the cationic lipids used in this study inhibit PKC activity. The cationic lipids significantly inhibited the activity of PKC but not the activity of a non-related protein kinase, PKA. The synthesis of interleukin-6 (IL-6), which is not dependent on PKC activity for its induction in macrophages, was not modified in vitro or in situ by cationic lipids. The synthesis of NO and TNF-α in macrophages, both of which are PKC-dependent, was downregulated by cationic lipids.
7. These results demonstrate that cationic lipids can be considered as novel anti-inflammatory agents. The downregulation of pro-inflammatory mediators through interaction of cationic lipids with the PKC pathway may explain this anti-inflammatory activity. Furthermore, since cationic lipids have intrinsic anti-inflammatory activity, cationic liposomes should be used with caution to deliver nucleic acids for gene therapy in vivo.

     

Anti-inflammatory activity of domestic papain

The influence of domestic papain to the course of experimental inflammation due to formalin, dextrane, histamine, serotonin and infectious arthritis has been studied. The domestic papain in doses of 0.325 and 0.75 mg/kg possesses strongly marked antiinflammatory activity and this ability is no less than that of butadion and indomethacin.     

Anti-inflammatory activity of hyaluronic acid

The results of in vivo experiments showed that hyaluronic acid possesses antiexudative activity comparable with that of nonsteroidal anti-inflammatory drugs. Hyaluronic acid exhibits antagonism with respect to histamine-induced inflammation.     

Anti-inflammatory activity of 5,7-dimethoxyflavone

The anti-inflammatory activity of 5,7-dimethoxyflavone (5,7-DMF) has been assessed. It was found to possess a comparable effect to aspirin on the rat paw edema model, and it showed no inhibition on cotton pellet-induced granuloma formation. On the rat pleurisy model, 5,7-DMF exhibited an antiexudative effect, interfered with leukocyte migration, and markedly inhibited prostaglandin biosynthesis. In addition, 5,7-DMF caused marked lowering of the rectal temperature of rats. The results obtained from Hippocratic screening revealed that 5,7-DMF possessed a weak CNS depressant activity.     

Anti-inflammatory activity of Commiphora molmol

The petroleum ether extract of the oleo-gum resin of Commiphora molmol, at a dose of 500 mg/kg body weight, produced significant inhibition of carrageenan induced inflammation and cotton pellet granuloma. The extract also showed significant antipyretic activity in mice. Further studies on the fractionation of phytoconstituents and their mechanism of action are in progress.     

Anti-inflammatory activity in human plasma

Pooled human plasma contains a fraction, separable by ultrafiltration and column chromatography, which possesses anti-inflammatory activity in the carrageenan oedema test in the rat, may be partially purified by solvent extraction, has an apparent molecular weight below 1000, and is resistant to acid and proteolytic digestion. A substance showing experimental anti-inflammatory activity has been isolated from human serum (McArthur, Smith & Freeman, 1972). The present paper describes a much simpler preparation of this material from pooled human plasma, its partial purification by extraction with acetone and ethanol, its ultrafiltration through several membranes, and its resistance to acidic, proteolytic and thermal degradation. A preliminary account of part of this work has been published (Elliott, Ford-Hutchinson & others, 1973).     

Anti-inflammatory activity of substituted 1,3,4-oxadiazoles

Various 2-(4-biphenoxymethyl)-5-arylamino-1,3,4-oxadiazoles were synthesized by cyclization of the corresponding 1-(4-biphenoxyacetyl)-4-substituted thiosemicarbazides. These compounds were characterized by their elemental analyses and infrared, mass, and nuclear magnetic resonance spectral data. All substituted thiosemicarbazides (100 mg/kg, ip) and cyclized substituted oxadiazoles (100 mg/kg, ip) possessed anti-inflammatory activity, as reflected by their ability to provide protection against carrageenin-induced edema in the rat paw which ranged from 28 to 68% and 36 to 76%, respectively. Cyclization of the substituted thiosemicarbazides, in general, resulted in an increase in the anti-inflammatory activity of their corresponding substituted oxadiazoles, with the exception of those containing 2,4-dimethyl and 3,4-dimethyl substituents in their molecular structure. Hydrocortisone (10 mg/kg, ip) and oxyphenbutazone (40 mg/kg, ip) were used as the standard reference drugs and these provided 45 and 53% protection, respectively. All compounds (1 mM) possessed antiproteolytic activity and the in vitro inhibition of trypsin-induced hydrolysis of bovine serum albumin ranged from 13 to 75% for substituted thiosemicarbazides and 39 to 70% for substituted oxadiazoles. There was no relationship between the anti-inflammatory activity of substituted thiosemicarbazides and substituted oxadiazoles and their antiproteolytic effectiveness. The low toxicity of these compounds was reflected by their high approximate LD50 values, ranging from 500 to 1000 mg/kg.     

Anti-inflammatory activity of gallic acid.

Gallic acid was found to possess antiinflammatory activity towards zymosan-induced acute food pad swelling in mice. In vitro studies on the mode of action of gallic acid revealed that this compound interferes with the functioning of polymorphonuclear leukocytes (PMNs). Scavenging of superoxide anions, inhibition of myeloperoxidase release and activity as well as a possible interference with the assembly of active NADPH-oxidase may account for the inhibition of inflammatory process by gallic acid. Structure-activity relationship analysis showed that the o-dihydroxy group of gallic acid is important for the inhibitory activity in vitro.     

Anti-inflammatory activity of 4,4'-dihydroxy-alpha-truxillic acid

The oral anti-inflammatory activity of 4,4'-dihydroxy-alpha-truxillic acid (1) was compared with that of two other nonsteroidal anti-inflammatory drugs, loxoprofen sodium (LOX) and diclofenac sodium (DIC). The activity of 1 against the inflammatory pain response induced by formalin was comparable to that of LOX, but weaker than that of DIC. In the monosodium urate (MSU)-induced acute inflammatory model, 1 showed stronger anti-inflammatory activity than both LOX and DIC. The ED50 value for 1 was 4.5 micromol/kg, while the values for LOX and DIC were 65 and 25 micromol/kg, respectively. Otherwise, the oral single-dose toxicity of 1 was investigated in both sexes of Sprague-Dawley rats administered once at a dose of 2000 mg/kg. 1 showed no death, clinical signs, changes in body weight or pathological findings related to the treatment. In addition, no mutagenicity was observed in the reverse mutation assay. Furthermore, 1 did not show any ulcerogenic activity at doses ranging from 30 to 300 mg/kg in rat. Thus, 1 might be considered to be an effective anti-inflammatory agent with no deleterious adverse effect.     

Anti-inflammatory activity of neutrophil elastase inhibitors

Neutrophil elastase is a protease that is involved in the tissue destruction and inflammation that characterize numerous diseases, including hereditary emphysema, chronic obstructive pulmonary disease, cystic fibrosis, adult respiratory distress syndrome, ischemic-reperfusion injury and rheumatoid arthritis. Thus, elastase has been the object of extensive research to develop potent inhibitors that target its destructive and pro-inflammatory action. This review focuses on the anti-inflammatory activity of inhibitors that are currently, or were until recently in development, including purified or recombinantly produced endogenous inhibitors, genetically modified recombinant protein inhibitors and synthetic small-molecule inhibitors.     

Anti-inflammatory activity of Sapindus trifoliatus Linn

Anti-inflammatory activity of the ethanolic extract of the seeds of Sapindus trifoliatus Linn. was studied in wister rats using the carrageenan induced left hind paw edema, carrageenan induced pleurisy and cotton pellet induced granuloma model. The ethanolic extract (150 mg/kg, p.o.) produced the inhibition of carrageenan induced rat paw edema. It also showed an inhibitory effect on leukocyte migration and a reduction on the pleural exudates as well as reduction on the granuloma weight in the cotton pellet granuloma method. The results indicated that the ethanolic extract produced significant (P < 0.001) anti-inflammatory activity when compared with the standard and untreated control.