In vivo study of four preparative extracts of Clematis terniflora DC. for antinociceptive activity and anti-inflammatory activity in rat model of carrageenan-induced chronic non-bacterial prostatitis

2011 ◽  
Vol 134 (3) ◽  
pp. 1018-1023 ◽  
Author(s):  
R.Z. Chen ◽  
L. Cui ◽  
Y.J. Guo ◽  
Y.M. Rong ◽  
X.H. Lu ◽  
...  
Keyword(s):  
Rat Model ◽  
Inflammatory Activity ◽  
Antinociceptive Activity ◽  
In Vivo Study ◽  
Bacterial Prostatitis ◽  
Anti Inflammatory

scholarly journals The Anti-Inflammatory Activity of a Novel Fused-Cyclopentenone Phosphonate and Its Potential in the Local Treatment of Experimental Colitis

2015 ◽  
Vol 2015 ◽  
pp. 1-10
Author(s):  
Dorit Moradov ◽  
Helena Shifrin ◽  
Efrat Harel ◽  
Mirela Nadler-Milbauer ◽  
Marta Weinstock ◽  
...  
Keyword(s):  
Rat Model ◽  
Local Treatment ◽  
Experimental Colitis ◽  
Inflammatory Activity ◽  
Mucosal Inflammation ◽  
Activated Macrophages ◽  
Aminosalicylic Acid ◽  
Anti Inflammatory

A novel fused-cyclopentenone phosphonate compound, namely, diethyl 3-nonyl-5-oxo-3,5,6,6a-tetrahydro-1H-cyclopenta[c]furan-4-ylphosphonate (P-5), was prepared and testedin vitro(LPS-activated macrophages) for its cytotoxicity and anti-inflammatory activity andin vivo(DNBS induced rat model) for its potential to ameliorate induced colitis. Specifically, the competence of P-5 to reduce TNFα, IL-6, INFγ, MCP-1, IL-1α, MIP-1α, and RANTES in LPS-activated macrophages was measured. Experimental colitis was quantified in the rat model, macroscopically and by measuring the activity of tissue MPO and iNOS and levels of TNFαand IL-1β. It was found that P-5 decreased the levels of TNFαand the tested proinflammatory cytokines and chemokines in LPS-activated macrophages. In the colitis-induced rat model, P-5 was effective locally in reducing mucosal inflammation. This activity was equal to the activity of local treatment with 5-aminosalicylic acid. It is speculated that P-5 may be used for the local treatment of IBD (e.g., with the aid of colon-specific drug platforms). Its mode of action involves inhibition of the phosphorylation of MAPK ERK but not of p38 and had no effect on IκBα.

scholarly journals In-Vivo assessment of glucocorticoid loaded tea tree oil nanoemulsion gel

2019 ◽  
Vol 9 (1) ◽  
pp. 108-113
Author(s):  
Md. Sarfaraz Alam ◽  
Rohit Saraswat ◽  
Pankaj Sharma ◽  
Md. Salahuddin Ansari
Keyword(s):  
Aqueous Phase ◽  
Clobetasol Propionate ◽  
Inflammatory Activity ◽  
In Vivo Study ◽  
Nucleoside Triphosphate ◽  
Tea Tree Oil ◽  
Tea Tree ◽  
Nanoemulsion Gel ◽  
Anti Inflammatory

Optimized formulations were subjected to various in vivo studies like anti-inflammatory activity, Nickel induced dermatitis, irritation study and Acute and repeated dose dermal toxicity studies. Clobetasol propionate (CP) has anti-inflammatory, immunomodulatory, and antiproliferative activity. The aim of the present work was to test the hypothesis that the addition CP in nanoemulsions would result in enhancement CP delivery and leading to better antipsoriatic activity. Nanoemulsions were prepared by aqueous phase titration method, using Tea Tree oil, Tween 20, Transcutol P, and distilled water as the oil phase, surfactant, co-surfactant and aqueous phase, respectively.We developed a topical O/W nanoemulsion in which drug is incorporated in disperse phase of oil and evaluated its efficacy against different types of in vivostudies. It was also found that the significantly increased their anti-inflammatory activity. It was reported that CP-loaded nanoemulsion significantly increased NTPDase (Nucleoside triphosphate diphosphohydrolases) activity in lymphocytes. This membrane protein is responsible for the hydrolysis of extracellular ATP (Adenosine triphosphate) which is responsible for cell proliferation, differentiation and inflammatory processes. In vivoirritation studies did not show any irritation in spite of having high amount of surfactant. Group treated with CP loaded nanoemulsion gel showed no evident toxicity even on repeated exposure. On the basis of above in vivo study we conclude that developed nanoemulsion is safe for human. Keywords: Clobetasol propionate, In-vivo study, Nanoemulsion, Anti-inflammatory study, Toxicity study

Formulation and Evaluation of Atorvastatin Calcium-Poly-ε-Caprolactone Nanoparticles Loaded Ocular Inserts for Sustained Release and Antiinflammatory Efficacy

2020 ◽  
Vol 21 (15) ◽  
pp. 1688-1698
Author(s):  
Germeen N.S. Girgis
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Pluronic F127 ◽  
In Vivo Study ◽  
Average Weight ◽  
Drug Release Profile ◽  
Atorvastatin Calcium ◽  
Anti Inflammatory

Purpose: The work was performed to investigate the feasibility of preparing ocular inserts loaded with Poly-ε-Caprolactone (PCL) nanoparticles as a sustained ocular delivery system. Methods: First, Atorvastatin Calcium-Poly-ε-Caprolactone (ATC-PCL) nanoparticles were prepared and characterized. Then, the optimized nanoparticles were loaded within inserts formulated with Methylcellulose (MC) and Polyvinyl Alcohol (PVA) by a solvent casting technique and evaluated physically, for in-vitro drug release profile. Finally, an in-vivo study was performed on the selected formulation to prove non-irritability and sustained ocular anti-inflammatory efficacy compared with free drug-loaded ocuserts. Results: The results revealed (ATC-PCL) nanoparticles prepared with 0.5% pluronic F127 were optimized with 181.72±3.6 nm particle size, 0.12±0.02 (PDI) analysis, -27.4± 0.69 mV zeta potential and 62.41%±4.7% entrapment efficiency. Nanoparticles loaded ocuserts manifested compatibility between drug and formulation polymers. Moreover, formulations complied with average weight 0.055±0.002 to 0.143±0.023 mg, and accepted pH. ATC-PCL nanoparticles loaded inserts prepared by 5% MC showed more sustained, prolonged in-vitro release over 24h. In-vivo study emphasized non-irritability, ocular anti-inflammatory effectiveness represented by smaller lid closure scores, and statistically significant lowering in PMN count after 3h. Conclusion: These findings proposed a possibly simple, new and affordable price technique to prepare promising (ATC-PCL) nanoparticles loaded inserts to achieve sustained release with prolonged antiinflammatory efficacy.

Design, Synthesis, Characterization and in silico molecular docking studies and in vivo anti-inflammatory Activity of Pyrazoline clubbed Thiazolinone Derivatives

2020 ◽  
Vol 17 ◽  
Author(s):  
Deepak Kumar Singh ◽  
Mayank Kulshreshtha ◽  
Yogesh Kumar ◽  
Pooja A Chawla ◽  
Akash Ved ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Biological Activities ◽  
Inflammatory Activity ◽  
Standard Drug ◽  
Docking Score ◽  
Chemical Structures ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

Background: The pyrazolines give the reactions of aliphatic derivatives, resembling unsaturated compounds in their behavior towards permanganate and nascent hydrogen. This nucleus has been associated with various biological activities including inflammatory. Thiazolinone is a heterocyclic compound that contains both sulfur and nitrogen atom with a carbonyl group in their structure.Thiazolinone and their derivatives have attracted continuing interest because of their various biological activities, such as anti-inflammatory, antimicrobial, anti-proliferative, antiviral, anticonvulsant etc. The aim of the research was to club pyrazoline nucleus with thiazolinone in order to have significantanti-inflammatory activity. The synthesized compounds were chemically characterized for the establishment of their chemical structures and to evaluate as anti-inflammatory agent. Method: In the present work, eight derivatives of substituted pyrazoline (PT1-PT8) were synthesized by a three step reaction.The compounds were subjected to spectral analysis by Infrared, Mass and Nuclear magnetic resonance spectroscopy and elemental analysis data. All the synthesized were evaluated for their in vivo anti-inflammatory activity. The synthesized derivatives were evaluated for their affinity towards target COX-1 and COX-2, using indomethacin as the reference compound molecular docking visualization through AutoDock Vina. Results: Compounds PT-1, PT-3, PT-4 and PT-8 exhibited significant anti-inflammatory activity at 3rd hour being 50.7%, 54.3%, 52.3% and 57% respectively closer to that of the standard drug indomethacin (61.9%).From selected anti-inflammatory targets, the synthesized derivatives exhibited better interaction with COX-1 and COX-2 receptor, where indomethacin showed docking score of -6.5 kJ/mol, compound PT-1 exhibited highest docking score of -9.1 kJ/mol for COX-1 and compound PT-8 having docking score of 9.4 kJ/mol for COX-2. Conclusion: It was concluded that synthesized derivatives have more interaction with COX-2 receptors in comparison to the COX-1 receptors because the docking score with COX-2 receptors were very good. It is concluded that the synthesized derivatives (PT-1 to PT-8) are potent COX-2 inhibitors.

scholarly journals Anti-Tumor and Anti-Inflammatory Activity In Vivo of Apodanthera congestiflora Cogn. (Cucurbitaceae)

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 743
Author(s):  
Geovana F. G. Silvestre ◽  
Renally P. Lucena ◽  
Genil D. Oliveira ◽  
Helimarcos N. Pereira ◽  
Jhonatta A. B. Dias ◽  
...  
Keyword(s):  
Inflammatory Activity ◽  
Phytochemical Investigation ◽  
Significant Toxicity ◽  
Biological Tests ◽  
Ehrlich's Carcinoma ◽  
Anti Inflammatory ◽  
Pharmacological Potential ◽  
First Time ◽  
Anti Tumor Activity

This work aimed to carry out a study of Apodanthera congestiflora by investigating its chemical composition and pharmacological potential. From the dichloromethane phase (Dic-Ac) of the A. congestiflora stems, three compounds were identified: cayaponoside C5b (Ac-1), cabenoside C (Ac-2) and fevicordin C2 glucoside (Ac-3), being last identified for the first time as a natural product. These compounds were obtained by chromatographic methods and their structures were elucidated by means of spectroscopic analysis of IR, MS and NMR. In the quantification of Dic-Ac, it was possible to observe the presence of 7% of cayaponoside C5b. Dic-Ac showed significant toxicity for in vivo tests, with macroscopic and biochemical changes. The anti-inflammatory activity of Dic-Ac was investigated using the paw edema model. A decrease in inflammatory signs was observed in the first 5 h and the most effective dose in reducing edema with was 7.5 mg kg−1 (66.6%). Anti-tumor activity of Dic-Ac was evaluated by Ehrlich’s carcinoma model, which showed inhibition rate of 78.46% at 15 mg kg−1 dosage. The phytochemical investigation, together with the biological tests carried out in this study, demonstrated that A. congestiflora is a promising species in the search for therapeutics, since it contains substances with high pharmacological potential in its composition.

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