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Antiinflammatory Properties (antiinflammatory + property)

Distribution by Scientific Domains

Medical Sciences	71%
Life Sciences	14%
Chemistry	14%

Selected Abstracts

Nonsteroidal antiinflammatory drugs as therapeutic agents for Alzheimer's disease

DRUG DEVELOPMENT RESEARCH, Issue 3 2002
Todd E. Golde
One feature of the end-stage pathology of Alzheimer's disease (AD) is the presence of numerous inflammatory markers associated with the amyloid , protein (A,) deposits in the brain. Experimental data strongly suggests that A, aggregates can incite an inflammatory response, but there are also data suggesting that inflammation can promote A, production and deposition. Thus, antiinflammatory drugs may have some role in AD therapy. This idea is supported by epidemiologic data, which shows that long-term use of nonsteroidal antiinflammatory drugs (NSAIDs) confers protection from the development of AD. Significantly, oral salicylates have not been consistently shown to confer protection. Such studies have raised questions regarding the target or targets of NSAIDs that account for their apparent protection from AD. We have recently found that some NSAIDs have a novel mechanism of action, namely, selective lowering of the pathogenic A,42 peptide, that could contribute to their efficacy in AD. Further study will be needed to determine if the classic antiinflammatory properties of NSAIDs, the A,42-lowering property, another known or unknown property, or a combination of these contributes to NSAIDs apparent ability to protect individuals from the development of AD. Drug Dev. Res. 56:415,420, 2002. © Wiley-Liss, Inc. [source]

The molecular mechanism of human group IIA phospholipase A2 inactivation by bolinaquinone

JOURNAL OF MOLECULAR RECOGNITION, Issue 6 2009
Maria Chiara Monti
Abstract The molecular basis of the human group IIA secretory phospholipase A2 inactivation by bolinaquinone (BLQ), a hydroxyquinone marine terpenoid, has been investigated for the comprehension of its relevant antiinflammatory properties, through the combination of spectroscopic techniques, biosensors analysis, mass spectrometry (MS) and molecular docking. Indeed, sPLA2s are well known to be implicated in the pathogenesis of inflammation such as rheumatoid arthritis, septic shock, psoriasis and asthma. Our results suggest a mechanism of competitive inhibition guided by a non-covalent molecular recognition event, disclosing the key role of the BLQ hydroxyl-quinone moiety in the chelation of the catalytic Ca2+ ion inside the enzyme active site. The understanding of the sPLA2 -IIA inactivation mechanism by BLQ could be useful for the development of a new chemical class of PLA2 inhibitors, able to specifically target the enzyme active site. Copyright © 2009 John Wiley & Sons, Ltd. [source]

Pharmacodynamic interaction of recombinant human interleukin-10 and prednisolone using in vitro whole blood lymphocyte proliferation

JOURNAL OF PHARMACEUTICAL SCIENCES, Issue 5 2002
Abhijit Chakraborty
Abstract Prednisolone, a commonly used synthetic corticosteroid, and IL-10, a cytokine under investigation for strong antiinflammatory properties, are being contemplated as a potential joint therapeutic regimen in immune disorders. Their pharmacodynamic interactions were examined in blood from healthy adult male and female volunteers using an in vitro phytohemagglutinin (PHA)-stimulated whole,blood lymphocyte proliferation technique. Isobolograms along with parametric competitive and noncompetitive interaction models were used to determine the nature and intensity of interactions. Single drug effects show prednisolone more efficacious in inhibiting lymphocyte proliferation with an IC50 of 3.3 ng/mL and Imax value of 1, signifying complete suppression. Analogous parameters for IL-10 were 16.2 ng/mL for IC50 and 0.89 for Imax. There were no significant differences in the single drug immunosuppressive effects among genders. Their joint effects showed additive interaction based on isobolographic analysis. Parametric analysis using the competitive interaction model described their interaction as slightly synergistic, while the noncompetitive interaction modeling indicate a small degree of antagonism. Also, the joint effects in females tend to be more antagonistic than males. Concomitant use of prednisolone and IL-10 should thus reflect the net additive responses to concentrations of each agent. © 2002 Wiley-Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 91:1334,1342, 2002 [source]

Inhibition of UVB-mediated Oxidative Stress and Markers of Photoaging in Immortalized HaCaT Keratinocytes by Pomegranate Polyphenol Extract POMx

PHOTOCHEMISTRY & PHOTOBIOLOGY, Issue 4 2007
Mohammad Abu Zaid
In recent years there has been an increase in use of botanicals with antioxidant properties as skin photoprotective agents. Pomegranate (Punica granatum L.) fruit possesses strong antioxidant and antiinflammatory properties. Recently, we have shown that pomegranate-derived products rich in anthocyanidins and ellagitannins inhibit UVB-mediated activation of nuclear factor kappa B and modulate UVA-mediated cell proliferation pathways in normal human epidermal keratinocytes. In this study, we evaluated the effect of polyphenol-rich pomegranate fruit extract (POMx) on UVB-induced oxidative stress and photoaging in human immortalized HaCaT keratinocytes. Our data show that pretreatment of HaCaT cells with POMx (10,40 ,g mL,1) inhibited UVB (15,30 mJ cm,2)-mediated (1) decrease in cell viability, (2) decrease in intracellular glutathione content and (3) increase in lipid peroxidation. Employing immunoblot analysis we found that pretreatment of HaCaT cells with POMx inhibited UVB-induced (1) upregulation of MMP-1, -2, -7 and -9, (2) decrease in TIMP-1, (3) phosphorylation of MAPKs and (iv) phosphorylation of c-jun, whereas no effect was observed on UVB-induced c-fos protein levels. These results suggest that POMx protects HaCaT cells against UVB-induced oxidative stress and markers of photoaging and could be a useful supplement in skin care products. [source]

Estimation of the relative antiinflammatory efficacies of six commercial preparations of Harpagophytum procumbens (Devil's Claw)

PHYTOTHERAPY RESEARCH, Issue 3 2010
Nassima Abdelouahab Ouitas
Abstract The current work compared the relative efficacies of six commercial formulations of H. procumbens. Each formulation was assayed for the content of harpagoside (1), harpagide (2), verbascoside (3) and 8- O-p -coumaroyl harpagide (4) and, based on the recommended dosages, the total daily amounts were determined and used to establish anti-/proinflammatory (A/P) factors. The formulations were compared using ex vivo porcine skin for their activities towards COX-2 by Western blotting. The results showed great variation in the amounts of compounds 1,4 within the six formulations examined. The relative proportions of 1,4 also varied widely between the products and this inconsistency was reflected in the A/P factors, which correlated with the COX-2 expression (R2 = 0.9496). Although the data support the beneficial antiinflammatory effects from the use of some of the brands tested, others would appear potentially to exacerbate inflammation. To conclude, a ratio based upon the amount and relative proportions of anti- and proinflammatory compounds can be used to predict relative antiinflammatory properties. Also, with access to a diversity of ostensibly similar commercial products, the patient may experience varying therapeutic responses. Finally, current pharmacopoeia monographs, which are generally concerned with a minimum harpagoside content, are inadequate for ensuring the quality of products based on H. procumbens. Copyright © 2009 John Wiley & Sons, Ltd. [source]

Effects of a herbal gel containing carvacrol and chalcones on alveolar bone resorption in rats on experimental periodontitis

PHYTOTHERAPY RESEARCH, Issue 4 2008
Marco Antonio Botelho
Abstract Carvacrol and dimeric chalcones are the respective bioactive components of Lippia sidoides and Myracrodruon urundeuva, popular medicinal plants of Northeastern Brazil with proven antimicrobial and antiinflammatory properties. Periodontal disease is associated with inflammation and microbiological proliferation, thus the study aimed to investigate the effect of a topical gel based on carvacrol and chalcones in the experimental periodontal disease (EPD) in rats. Animals were treated with carvacrol and/or chalcones gel, immediately after EPD induction, three times a day for 11 days. Appropriate controls were included in the study. Animals were weighed daily. They were killed on day 11, the mandibles dissected and alveolar bone loss was measured. The periodontium were examined at histopathology and the neutrophil influx into the gingiva was assayed using myeloperoxidase activity. The bacterial flora were assessed through culture of the gingival tissue. Alveolar bone loss was significantly (p < 0.05) inhibited by combined carvacrol and chalcones gel, compared with the vehicle and non-treated groups. The treatment with the combined gel reduced tissue lesion at histopathology, decreased myeloperoxidase activity in gingival tissue and inhibited the growth of oral microorganisms as well as the weight loss. Carvacrol and chalcones combination gel has a beneficial effect upon EPD in this model. Copyright © 2008 John Wiley & Sons, Ltd. [source]

Fatty acids profile and antiinflammatory activity of Nonea setosa R. et S.

PHYTOTHERAPY RESEARCH, Issue 5 2006
Massimo Curini
Abstract In order to verify the antiinflammatory properties of Nonea setosa R. et S. (Fam. Boraginaceae) and to identify the relevant active principles, aerial parts of this plant were extracted with increasing polarity solvents. The antiinflammatory activity was investigated by a bioassay-oriented fractionation using the inhibition of the croton oil-induced ear oedema in mice as an experimental model of inflammation. GC-MS analysis of the most active fraction revealed the presence of high amounts of polyunsaturated fatty acids. Copyright © 2006 John Wiley & Sons, Ltd. [source]

A water soluble extract from Uncaria tomentosa (Cat's Claw) is a potent enhancer of DNA repair in primary organ cultures of human skin

PHYTOTHERAPY RESEARCH, Issue 3 2006
Thomas Mammone
Abstract Cat's Claw (Uncaria tomentosa) water extracts, essentially free of oxindole alkaloids, have been shown to possess a broad spectrum of biological activity including DNA repair enhancement and antiinflammatory properties. These two biological mechanisms are key molecular targets to develop treatments that protect skin exposed to ultraviolet light from the sun. Because C-Med-100, a Cat's Claw water extract, is the only documented natural source of components that can up-regulate simultaneously both DNA repair and antiinflammation, its ability to modulate DNA repair in human skin organ cultures was undertaken. For this purpose skin cultures were treated with or without 5 mg/mL C-Med-100, irradiated with 0,100 mJ/cm2 UVB, and microscopically analysed for necrosis as well as the level of pyrimidine dimers using immunofluorescent TT-dimer antibody staining. The data clearly demonstrated that co-incubation with C-Med-100 reduced skin cell death from UV exposure, and this protection was accounted for by a concomitant increase in DNA repair. Based on these results, it was concluded that C-Med-100 was a natural plant extract worthy of further consideration as a sunscreen product. Copyright © 2006 John Wiley & Sons, Ltd. [source]

Assessment of a bioactive compound for its potential antiinflammatory property by tight junction permeability

PHYTOTHERAPY RESEARCH, Issue 12 2005
Young Hoon Bai
Abstract Lactobacillus probiotic strains are proving to be abundant sources of bioactive components, including antiinflammatory components. Lifree was made of fruits fermented by Lactobacillus paracasei, Lactobacillus reuterrii and Saccharomyces cerevisiae. This study was designed to test these compounds in cell assays measuring epithelial barrier function and proliferation in the first instance. Cell proliferation was measured in mouse fibroblasts cells (3T3NIH) and rat intestinal epithelial cells (IEC-6), and tight junction activity in the kidney epithelial cell line (MDCK). Tight junction permeability was assessed by measuring transepithelial electrical resistance (TER) across confluent monolayers, following the addition of Lifree with or without a challenge with EGTA. Lifree promoted tight junction formation and recovery following loss of TER from challenge with EGTA. On the other hand, Lifree did not stimulate cell growth in either 3T3NIH and IEC-6 cells. Lifree stimulates tight junction maintenance and formation, suggesting it may have potential antiinflammatory properties. Copyright © 2005 John Wiley & Sons, Ltd. [source]

Analgesic and antiinflammatory properties of Sideritis lotsyi var. Mascaensis

PHYTOTHERAPY RESEARCH, Issue 3 2002
Margarita Hernández-Pérez
Abstract The antiinflammatory, analgesic and antimicrobial activities of crude ethanol extracts of Sideritis lotsyi var. mascaensis (Lamiaceae), and chloroform and aqueous fractions were evaluated in mice using paw and ear oedema induced by carrageenan and 12-o-tetradecanoyl-phorbol-acetate (TPA), respectively, as inflammation models, the writhing test induced by acetic acid for evaluating analgesic activity and the disk-diffusion method for testing antimicrobial actions. The results obtained demonstrated significant topical antiinflammatory and analgesic activities for the ethanol extract and chloroform fraction, but no relevant antimicrobial activity against the microorganisms tested. Copyright © 2002 John Wiley & Sons, Ltd. [source]

Minocycline prevents cholinergic loss in a mouse model of Down's syndrome

ANNALS OF NEUROLOGY, Issue 5 2004
Christopher L. Hunter PhD
Individuals with Down's syndrome develop Alzheimer's-like pathologies comparatively early in life, including progressive degeneration of basal forebrain cholinergic neurons (BFCNs). Cholinergic hypofunction contributes to dementia-related cognitive decline and remains a target of therapeutic intervention for Alzheimer's disease. In light of this, partial trisomy 16 (Ts65Dn) mice have been developed to provide an animal model of Down's syndrome that exhibits progressive loss of BFCNs and cognitive ability. Another feature common to both Down's syndrome and Alzheimer's disease is neuroinflammation, which may exacerbate neurodegeneration, including cholinergic loss. Minocycline is a semisynthetic tetracycline with antiinflammatory properties that has demonstrated neuroprotective properties in certain disease models. Consistent with a role for inflammatory processes in BFCN degeneration, we have shown previously that minocycline protects BFCNs and improves memory in mice with acute, immunotoxic BFCN lesions. We now report that minocycline treatment inhibits microglial activation, prevents progressive BFCN decline, and markedly improves performance of Ts65Dn mice on a working and reference memory task. Minocycline is an established antiinflammatory and neuroprotective drug and may provide a novel approach to treat specific AD-like pathologies. Ann Neurol 2004 [source]

Chondroitin sulfate increases hyaluronan production by human synoviocytes through differential regulation of hyaluronan synthases: Role of p38 and Akt

ARTHRITIS & RHEUMATISM, Issue 3 2009
Maha David-Raoudi
Objective To uncover the mechanism by which chondroitin sulfate (CS) enhances hyaluronan (HA) production by human osteoarthritic (OA) fibroblast-like synoviocytes (FLS). Methods The production of HA was investigated by exposing human OA FLS to CS in the presence or absence of interleukin-1, (IL-1,). HA levels were determined by enzyme-linked immunosorbent assay, and levels of messenger RNA (mRNA) for HA synthase 1 (HAS-1), HAS-2, and HAS-3 were determined by real-time polymerase chain reaction analysis. The effect of CS and IL-1, on signaling pathways was assessed by Western blotting. Specific inhibitors were used to determine their effects on both HA production and HAS expression. The molecular size of HA was analyzed by high-pressure liquid chromatography. Results CS increased HA production by FLS through up-regulation of the expression of HAS1 and HAS2. This was associated with activation of ERK-1/2, p38, and Akt, although to a lesser extent. Both p38 and Akt were involved in CS-induced HA accumulation. IL-1, increased HA production and levels of mRNA for HAS1, HAS2, and HAS3. CS enhanced the IL-1,,induced level of HAS2 mRNA and reduced the level of HAS3 mRNA. IL-1,,induced activation of p38 and JNK was slightly decreased by CS, whereas that of ERK-1/2 and Akt was enhanced. More high molecular weight HA was found in CS plus IL-1,,treated FLS than in FLS treated with IL-1, alone. Conclusion CS stimulates the synthesis of high molecular weight HA in OA FLS through up-regulation of HAS1 and HAS2. It reduces the IL-1,,enhanced transcription of HAS3 and increases the production of HA of large molecular sizes. These effects may be beneficial for maintaining viscosity and antiinflammatory properties in the joint. [source]

Protection of Mouse Brain from Aluminum-induced Damage by Caffeic Acid

CNS: NEUROSCIENCE AND THERAPEUTICS, Issue 1 2008
Jun-Qing Yang
The natural product caffeic acid is a specific inhibitor of 5-lipoxygenase (5-LOX); it also possesses antioxidant and antiinflammatory properties. The current study was designed to determine whether the neuroprotective properties of caffeic acid are due to inhibition of 5-LOX. Cerebral damage was induced in mice by intracerebroventricular microinjection of aluminum (5.0 ,g aluminum in 2.0 ,L, once a day, for 5 days). Caffeic acid was administered intragastrically at 30 min prior to aluminum and repeated daily for an additional 10 days. The brain injury was determined by observation of behavioral changes in mice, as well as by measuring biochemical and pathological changes in the cerebral tissue. The levels of 5-LOX proteins and 5-LOX mRNA expression were measured in brain tissue. Aluminum impaired learning and memory in mice produced neuronal death in hippocampi, elevated brain malondialdehyde levels, increased protein expression of amyloid precursor protein (APP), amyloid beta, and 5-LOX. It also increased 5-LOX mRNA expression and decreased choline acetyl transferase (ChAT) protein expression in the brain tissue of mice. Caffeic acid prevented brain damage as well as behavioral and biochemical changes caused by aluminum overload. The results of this study suggest that overexpression of 5-LOX accompanies the cerebral injury induced by aluminum overload in mice, and that selective inhibitors of 5-LOX may have potential value in the treatment of aluminum neurotoxicity and conceivably of diseases associated with neuronal injury. [source]