scholarly journals IN VITRO PHARMACOLOGICAL SCREENING METHODS FOR ANTI-INFLAMMATORY AGENTS

2018 ◽  
Vol 11 ◽  
Author(s):  
Jayakumari S ◽  
Jijith Us
Keyword(s):  
Leukocyte Adhesion ◽  
Induced Response ◽  
Screening Methods ◽  
Adhesion Assay ◽  
Polymorphonuclear Cells ◽  
In Vitro Methods ◽  
Anti Inflammatory ◽  
Pharmacological Screening ◽  
New Compounds

Context: The development of in vitro methods is important in drug discovery process due to the restriction of animal use in the pharmacological screening process.Objective: The objective of the review was to understand the in vitro pharmacological screening methods for anti-inflammatory agents.Methods: The present review details various in vitro methods available for the screening of activity of therapeutic agents against inflammation.Results: Inhibition and measurement of nitric oxide production, mast cell degranulation, leukocyte adhesion assay, platelet-neutrophil adhesion assay, lipopolysaccharide-induced response assay, N-formyl-methionyl-leucyl-phenylalanine-induced O2 generation by polymorphonuclear cells, and cyclooxygenase assays are discussed in this review.Conclusions: These methods help to understand the real mechanism of inflammation and mediators involved in this process and help toidentify new compounds possessing the anti-inflammatory activity.

scholarly journals Evaluation of in-vitro methods to select effective streptomycetes against toxigenic fusaria

PeerJ ◽  
2019 ◽  
Vol 7 ◽  
pp. e6905 ◽  
Author(s):  
Elena Maria Colombo ◽  
Cristina Pizzatti ◽  
Andrea Kunova ◽  
Claudio Gardana ◽  
Marco Saracchi ◽  
...  
Keyword(s):  
Plant Pathogens ◽  
Culture Media ◽  
Screening Methods ◽  
Dual Culture ◽  
In Planta ◽  
In Vitro Method ◽  
In Vitro Methods ◽  
Strain Diversity ◽  
Fungal Plant Pathogens

Biocontrol microorganisms are emerging as an effective alternative to pesticides. Ideally, biocontrol agents (BCAs) for the control of fungal plant pathogens should be selected by an in vitro method that is high-throughput and is predictive of in planta efficacy, possibly considering environmental factors, and the natural diversity of the pathogen. The purpose of our study was (1) to assess the effects ofFusariumstrain diversity (N= 5) and culture media (N= 6) on the identification of biological control activity ofStreptomycesstrains (N= 20) againstFusariumpathogens of wheat in vitro and (2) to verify the ability of our in vitro screening methods to simulate the activity in planta. Our results indicate that culture media,Fusariumstrain diversity, and their interactions affect the results of an in vitro selection by dual culture assay. The results obtained on the wheat-based culture media resulted in the highest correlation score (r= 0.5) with the in planta root rot (RR) inhibition, suggesting that this in vitro method was the best predictor of in planta performance of streptomycetes against Fusarium RR of wheat assessed as extension of the necrosis on the root. Contrarily, none of the in vitro plate assays using the media tested could appropriately predict the activity of the streptomycetes against Fusarium foot rot symptoms estimated as the necrosis at the crown level. Considering overall data of correlation, the activity in planta cannot be effectively predicted by dual culture plate studies, therefore improved in vitro methods are needed to better mimic the activity of biocontrol strains in natural conditions. This work contributes to setting up laboratory standards for preliminary screening assays ofStreptomycesBCAs against fungal pathogens.

Design and characterization of a cleavage-resistant Annexin A1 mutant to control inflammation in the microvasculature

Blood ◽  
2010 ◽  
Vol 116 (20) ◽  
pp. 4288-4296 ◽  
Author(s):  
Magali Pederzoli-Ribeil ◽  
Francesco Maione ◽  
Dianne Cooper ◽  
Adam Al-Kashi ◽  
Jesmond Dalli ◽  
...  
Keyword(s):  
Polymorphonuclear Leukocytes ◽  
Early Stage ◽  
Leukocyte Adhesion ◽  
Formyl Peptide Receptor ◽  
Annexin A1 ◽  
Formyl Peptide ◽  
Anti Inflammatory ◽  
Human Polymorphonuclear Leukocytes

Abstract Human polymorphonuclear leukocytes adhesion to endothelial cells during the early stage of inflammation leads to cell surface externalization of Annexin A1 (AnxA1), an effector of endogenous anti-inflammation. The antiadhesive properties of AnxA1 become operative to finely tune polymorphonuclear leukocytes transmigration to the site of inflammation. Membrane bound proteinase 3 (PR3) plays a key role in this microenvironment by cleaving the N terminus bioactive domain of AnxA1. In the present study, we generated a PR3-resistant human recombinant AnxA1—named superAnxA1 (SAnxA1)—and tested its in vitro and in vivo properties in comparison to the parental protein. SAnxA1 bound and activated formyl peptide receptor 2 in a similar way as the parental protein, while showing a resistance to cleavage by recombinant PR3. SAnxA1 retained anti-inflammatory activities in the murine inflamed microcirculation (leukocyte adhesion being the readout) and in skin trafficking model. When longer-lasting models of inflammation were applied, SAnxA1 displayed stronger anti-inflammatory effect over time compared with the parental protein. Together these results indicate that AnxA1 cleavage is an important process during neutrophilic inflammation and that controlling the balance between AnxA1/PR3 activities might represent a promising avenue for the discovery of novel therapeutic approaches.

The anti-inflammatory vasostatin-2 attenuates atherosclerosis in ApoE-/- mice and inhibits monocyte/macrophage recruitment

2017 ◽  
Vol 117 (02) ◽  
pp. 401-414 ◽  
Author(s):  
Weixin Xiong ◽  
Xiaoqun Wang ◽  
Daopeng Dai ◽  
Bao Zhang ◽  
Lin Lu ◽  
...  
Keyword(s):  
Chromogranin A ◽  
Mesenteric Arteries ◽  
Adhesion Assay ◽  
Aortic Sinus ◽  
Necrosis Factor Alpha ◽  
Macrophage Recruitment ◽  
Inflammatory Monocytes ◽  
Anti Inflammatory

SummaryWe showed previously that reduced level of vasostatin-2 (VS-2) correlates to the presence and severity of coronary artery disease. In this study, we aimed to figure out the role of chromogranin A (CGA) derived VS-2 in the development of atherosclerosis and monocyte/macrophage recruitment. Apolipoprotein E-deficient (ApoE-/-) mice fed a high-fat diet exhibited attenuated lesion size by 65 % and 41 % in En face and aortic root Oil red O staining, MOMA-2 positive area by 64 %, respectively, in VS-2 treatment group compared with PBS group. Proinflammatory cytokines tumour necrosis factor-alpha (TNF-α), monocyte chemoattractant protein-1 (MCP-1) and vascular cell adhesion molecule-1 (VCAM-1) were all remarkably reduced in aortic tissues after VS-2 treatment. Mechanistically, in adhesion assay using intravital microscopy in vivo, VS-2 suppressed the number of leukocytes adhering to the wall of apoE-/- mice mesenteric arteries. In chemotactic assay, flow cytometry analysis of peritoneal lavage exudate from C57BL/6 mice showed VS-2 significantly decreased the recruiment number of inflammatory monocytes/macrophages in a thioglycollate-induced peritonitis model. Furthermore, fewer fluorescent latex beads labelled Ly-6Chi monocytes accumulated in aortic sinus lesions of apoE-/- mice after VS-2 treatment. In addition, according to the microarray of human monocyte/macrophage, we found VS-2 stimulation caused a dose-dependent decrease of Rac1 expression and inactivation of Pak1 in mice primary monocytes as well as THP-1 cells and inhibited MCP-1/CCL-5 induced transmigration in vitro. In conclusion, the Chromogranin A-derived VS-2 attenuates atherosclerosis in apoE-/- mice and, in addition to its anti-inflammatory property, also acts as an inhibitor in monocyte/macrophage recruitment.Supplementary Material to this article is available online at www.thrombosis-online.com.

scholarly journals Phytochemical composition and biological screening of two Lophophytum species

2021 ◽  
Vol 20 (6) ◽  
pp. 598-610
Author(s):  
Carola A. Torres ◽  
◽  
Cristina M. Perez Zamora ◽  
Hector A. Sato ◽  
Maria B. Nuñez ◽  
...  
Keyword(s):  
Chemical Composition ◽  
In Vivo Studies ◽  
Tree Roots ◽  
In Vitro Methods ◽  
Phytochemical Composition ◽  
First Results ◽  
Anti Inflammatory ◽  
Β Carotene

Lophophytum species are holoparasites that grow on tree roots. The objectives of the work were to explore the chemical composition of the tubers of two Lophophytum species and to analyze the antioxidant, anti-inflammatory and antilithiatic activity of their extracts using in vitro methods. The chemical composition was determined by histochemical, phytochemical and TLC tests. In addition, the profile of phenolic compounds was determined by HPLC-MS. The presence of secondary metabolites of recognized activity was demonstrated. The results of the HPLC-MS/MS allowed the tentative identification of catechin, luteolin and glycosides of eriodictyol, naringenin and luteolin in the extract of Lophophytum leandri and eriodictyol, naringenin, luteolin and their glycosylated derivatives in Lophophytum mirabile. The extracts showed promising antioxidant (DPPH, ABTS and β-carotene-linoleic acid), anti-inflammatory (inhibition of 5-LOX) and anti-urolytic (by bioautographic TLC) activity. It is noteworthy that these are the first results of the phytochemical composition and biological activity of L. mirabile. However, in vivo studies are required to corroborate these activities.

scholarly journals Design, Synthesis and Characterization of Some Novel benzamide derivatives and it's Pharmacological Screening

2020 ◽  
pp. 68-74 ◽  
Author(s):  
Akshay R. Yadav ◽  
Shrinivas K. Mohite
Keyword(s):  
Chemical Structure ◽  
Design Synthesis ◽  
Different Types ◽  
Anti Inflammatory ◽  
Benzoyl Isothiocyanate ◽  
Pharmacological Screening ◽  
Benzamide Derivatives

The new series of substituted N-(phenylcarbamothioyl)benzamide derivatives (2a-2f) was designed, development and synthesized by using conventional and microwave method. In present work 6 different N-(phenylcarbamothioyl)benzamide were synthesized. Substituted benzoyl chloride is converted into benzoyl isothiocyanate by esterification. Benzoyl isothiocyanate is converted into Substituted (phenylcarbamothioyl)benzamide by treating with different types of substituted aniline. Confirmation of the chemical structure of the synthesized was substantiated by TLC, IR, 1H NMR, MS spectroscopy.Novel synthesized compounds screened for their in vivo and in-vitro anti-inflammatory studies and compound 2f shows promising anti-inflammatory activity.

scholarly journals Bioadhesive Polymeric Films Based on Red Onion Skins Extract for Wound Treatment: An Innovative and Eco-Friendly Formulation

Molecules ◽  
2020 ◽  
Vol 25 (2) ◽  
pp. 318 ◽  
Author(s):  
Cinzia Pagano ◽  
Maura Marinozzi ◽  
Claudio Baiocchi ◽  
Tommaso Beccari ◽  
Paola Calarco ◽  
...  
Keyword(s):  
Sustained Release ◽  
Extraction Method ◽  
Radical Scavenging ◽  
Human Keratinocytes ◽  
Polymeric Films ◽  
Wound Treatment ◽  
In Vitro Methods ◽  
Anti Inflammatory ◽  
Dermal Application

The onion non-edible outside layers represent a widely available waste material deriving from its processing and consumption. As onion is a vegetable showing many beneficial properties for human health, a study aiming to evaluate the use of extract deriving from the non-edible outside layers was planned. An eco-friendly extraction method was optimized using a hydroalcoholic solution as solvent. The obtained extract was deeply characterized by in vitro methods and then formulated in autoadhesive, biocompatible and pain-free hydrogel polymeric films. The extract, very soluble in water, showed antioxidant, radical scavenging, antibacterial and anti-inflammatory activities, suggesting a potential dermal application for wounds treatment. In vitro studies showed a sustained release of the extract from the hydrogel polymeric film suitable to reach concentrations necessary for both antibacterial and anti-inflammatory activities. Test performed on human keratinocytes showed that the formulation is safe suggesting that the projected formulation could be a valuable tool for wound treatment.

scholarly journals Comparative Assessment of the New PDE7 Inhibitor – GRMS-55 and Lisofylline in Animal Models of Immune-Related Disorders: A PK/PD Modeling Approach

2020 ◽  
Vol 37 (2) ◽  
Author(s):  
Artur Świerczek ◽  
Krzysztof Pociecha ◽  
Marietta Ślusarczyk ◽  
Grażyna Chłoń-Rzepa ◽  
Sebastian Baś ◽  
...  
Keyword(s):  
Animal Models ◽  
Tnf Alpha ◽  
Collagen Induced Arthritis ◽  
Future Studies ◽  
Immune Mediated ◽  
Pde Inhibitors ◽  
Anti Inflammatory ◽  
New Compounds

Abstract Purpose This study aimed to assess the activity of two phosphodiesterase (PDE) inhibitors, namely GRMS-55 and racemic lisofylline ((±)-LSF)) in vitro and in animal models of immune-mediated disorders. Methods Inhibition of human recombinant (hr)PDEs and TNF-alpha release from LPS-stimulated whole rat blood by the studied compounds were assessed in vitro. LPS-induced endotoxemia, concanavalin A (ConA)-induced hepatitis, and collagen-induced arthritis (CIA) animal models were used for in vivo evaluation. The potency of the investigated compounds was evaluated using PK/PD and PK/PD/disease progression modeling. Results GRMS-55 is a potent hrPDE7A and hrPDE1B inhibitor, while (±)-LSF most strongly inhibits hrPDE3A and hrPDE4B. GRMS-55 decreased TNF-alpha levels in vivo and CIA progression with IC50 of 1.06 and 0.26 mg/L, while (±)-LSF with IC50 of 5.80 and 1.06 mg/L, respectively. Moreover, GRMS-55 significantly ameliorated symptoms of ConA-induced hepatitis. Conclusions PDE4B but not PDE4D inhibition appears to be mainly engaged in anti-inflammatory activity of the studied compounds. GRMS-55 and (±)-LSF seem to be promising candidates for future studies on the treatment of immune-related diseases. The developed PK/PD models may be used to assess the anti-inflammatory and anti-arthritic potency of new compounds for the treatment of rheumatoid arthritis and other inflammatory disorders.

IN VITRO ANTIARTHRITIC AND ANTI-INFLAMMATORY ACTIVITY OF PETETHER EXTRACT OF HYPTIS SUAVEOLENS

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (09) ◽  
pp. 60-62
Author(s):  
M. R Elayaraja Krishnan ◽  
◽  
R. Vijaya Kanth ◽  
S. Muthu Pandi
Keyword(s):  
Diclofenac Sodium ◽  
Inflammatory Activity ◽  
Ether Extract ◽  
In Vitro Methods ◽  
Whole Plant ◽  
Hyptis Suaveolens ◽  
Excellent Activity ◽  
Anti Inflammatory ◽  
The Stability

In our present study, various concentrations of pet ether extract of whole plant of Hyptis suaveolens were prepared and subjected for anti arthritic and anti-inflammatory activity by in vitro methods. The antiarthritic activity was carried out by bovine serum albumin denaturation paradigm. The results showed that the pet ether extract (44.51%) showed excellent arthritic activity when compared to the standard diclofenac sodium (31.44%) at 2000μg/mL. Meanwhile, in the anti-inflammatory paradigm, the same extract (99.10%) showed excellent activity than the standard diclofenac sodium (73.80%) at 2000μg/ mL by restoring the stability of degraded red blood corpuscles. In both the paradigms, increase in concentration of the extract increases the action potential against the methanol degradation of bovine albumin and HRBC.

Sign in / Sign up

Export Citation Format

Share Document