scholarly journals THE ANTI-INFLAMMATORY ACTIVITY OF ESSENTIAL OIL OF CLOVE (Syzygium aromaticum) IN ABSORPTION BASE OINTMENT WITH ADDITION OF OLEIC ACID AND PROPYLENE GLYCOL AS ENHANCER

2019 ◽  
pp. 106-109
Author(s):  
NINING SUGIHARTINI ◽  
RANI PRABANDARI ◽  
TEDJO YUWONO ◽  
DESTY RESTIA RAHMAWATI
Keyword(s):  
Oleic Acid ◽  
Essential Oil ◽  
Propylene Glycol ◽  
Inflammatory Cells ◽  
Optimal Concentration ◽  
Inflammatory Activity ◽  
Syzygium Aromaticum ◽  
Epidermal Thickness ◽  
Cox 2 ◽  
Anti Inflammatory

Background : The optimal concentration of essential oil of clove in absorption base ointment as anti-inflammatory has been studied. The developmentof formulations can be done by adding oleic acid and propylene glycol as enhancers. The purpose of this study was to determine the anti-inflammatoryactivity of the essential oil of clove in absorption base ointment formula by adding a mixture of oleic acid and propylene glycol as enhancers.Methods: In this study, the composition of oleic acid and propylene glycol was 100% oleic acid (FI), 50% oleic acid and propylene glycol (FII), and100% propylene glycol (FIII). The profile of the anti-inflammatory activity essential oil of clove was carried out using male of mice Balb/C strain whichwas induced inflammatory with croton oil on back of skin. After treatment, it was sacrificed and then was taken the back of skin to get histopathologicalpreparation. After that, the epidermal thickness, number of inflammatory cells, and cyclooxygenase (COX)-2 expression can be measured.Results : Based on the results of the test, it shows that FIII has the smallest of the amount of COX-2 expression, the number of inflammatory cells, andthe epidermal thickness so the addition of the composition enhancer provides good anti-inflammatory activity.Conclusion: The increasing concentration of propylene glycol caused the raising activity of essential oil of clove as anti-inflammatory.

scholarly journals The Profile of Anti-inflammatory Activity of Syzigium Aromaticum Volatile Oil in Lotion with Variation Composition of Oleic Acid and Propylene Glycol as Enhancer

2017 ◽  
Vol 22 (2) ◽  
pp. 111 ◽  
Author(s):  
Fitriah Ardiawijianti Iriani ◽  
Nining Sugihartini ◽  
Tedjo Yuwono
Keyword(s):  
Oleic Acid ◽  
Essential Oil ◽  
Propylene Glycol ◽  
Mouse Strain ◽  
Inflammatory Cells ◽  
Volatile Oil ◽  
Inflammatory Activity ◽  
Syzygium Aromaticum ◽  
Cox 2 ◽  
Anti Inflammatory

Essential oil of clove (Syzygium aromaticum) containing eugenol has an anti-inflammatory activity. The study was aimed to develop the formulation of lotion by adding of oleic acid and propylene glycol as penetration enhancer. The effect of enhancer composition was also studied. Lotion was prepared with the composition of oleic acid (AO) and propylene glycol (PG) as follow: 1:0 (FI), 0,5:0,5 (FII), 0:1 (FIII). Capacity an anti-inflammatory of formulation based on parameters of the amount of cells with COX-2 expression, the number of inflammatory cells and the epidermis thickness was evaluated using male mouse strain BALb/C induced by crotton oil as inflammatory agents. The results showed that the increasing composition propylene glycol caused the decreasing of the amount of cells with COX-2 expression (p <0.05), the inflammatory cells (P <0.05) and the epidermis thickness (p <0.05)

scholarly journals Anti-inflammatory Activity of Camellia sinensis, l. Extract Cream Combined with Vitamin C as Antioxidant on Croton Oil-induced Inflamation in Male Mice Strain BALB/C

2017 ◽  
Vol 22 (2) ◽  
pp. 73
Author(s):  
Nining Sugihartini ◽  
Ratih Saridewi ◽  
Ulfa Ramdhani M ◽  
Fitri Rahmawanti ◽  
Sapto Yuliani ◽  
...  
Keyword(s):  
Vitamin C ◽  
Green Tea ◽  
Epigallocatechin Gallate ◽  
Inflammatory Cells ◽  
Green Tea Extract ◽  
Inflammatory Activity ◽  
Inflammatory Parameters ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Tea Extract

Green tea extract cream contains epigallocatechin gallate (EGCG) as the active ingredient for anti-inflammatory. Epigallocatechin gallate is easyly oxidized and able to reduce its effectivity as an anti-inflammatory. Therefore, an addition of antioxidants in order to increase its stability is required. The purpose of this study was to determine the effect of adding the antioxidant Vitamin C on the effectivity of green tea extract as an anti-inflammatory. This study uses 6 groups of male mice strain BALB/C which were given treatment as follows: normal control, negative control, base cream, green tea extract (0.2%), Vitamin C cream (1%) and green tea extract cream with addition of Vitamin C. The anti-inflammatory activity was evaluated based on the expression of COX-2, inflammatory cells and the thickness of the epidermis in the skin tissue of mice after given crotton oil (0.1%) on the back for the induction of inflammation. After treatment cream for 3 days, mice were sacrificed for histopathological tissue preparations made with hematoxylin eosin staining and immunohistochemistry COX-2. Data were analyzed statistically with one way Anova followed by t-test to determine differences between groups at a significance level of 0.05. The test results indicate that cream of green tea extract is higher in decreasing inflammatory parameters in comparison with cream of Vitamin C, except in the thickness of epidermal parameter. Green tea extract cream with the addition of Vitamin C is higher in reducing inflammatory parameters than cream of green tea extract or cream of Vitamin C. The decline percentage of cells that express COX-2, inflammatory cells and the thickness of the epidermis in the each of groups were cream of green tea extract:57.95%;53.75%;34.83%, cream of Vitamin C:48.76%;34.96%;34.27%, cream of green tea extract and Vitamin C:61,89%;65,54%;46.30%, respectively. Based on the results of this study, it can be concluded that anti-inflammatory activity of green tea extract cream increased due to the addition of 1% vitamin C as an antioxidant.

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 Evaluation of Anticonvulsant Activity of Dual COX-2/5-LOX Inhibitor Darbufelon and Its Novel Analogues

2021 ◽  
Vol 89 (2) ◽  
pp. 22
Author(s):  
Mariia Mishchenko ◽  
Sergiy Shtrygol’ ◽  
Andrii Lozynskyi ◽  
Semen Khomyak ◽  
Volodymyr Novikov ◽  
...  
Keyword(s):  
Drug Design ◽  
Anticonvulsant Activity ◽  
Inflammatory Activity ◽  
Significant Protection ◽  
Protection Level ◽  
Inflammatory Drugs ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Target Agent

Neuroinflammation is an integral part of epilepsy pathogenesis and other convulsive conditions, and non-steroidal anti-inflammatory drugs (NSAIDs) present a potent tool for the contemporary search and design of novel anticonvulsants. In the present paper, evaluation of the anticonvulsant activity of the potential NSAID dual COX-2/5-LOX inhibitor darbufelone methanesulfonate using an scPTZ model in mice in dose 100 mg/kg is reported. Darbufelone possesses anticonvulsant properties in the scPTZ model and presents interest for in-depth studies as a possible anticonvulsant multi-target agent with anti-inflammatory activity. The series of 4-thiazolidinone derivatives have been synthesized following the analogue-based drug design and hybrid-pharmacophore approach using a darbufelone matrix. The synthesized derivatives showed a significant protection level for animals in the scPTZ model and are promising compounds for the design of potential anticonvulsants with satisfactory drug-like parameters.

Non-acidic 1,3,4-trisubstituted-pyrazole derivatives as lonazolac analogs with promising COX-2 selectivity, anti-inflammatory activity and gastric safety profile

2018 ◽  
Vol 77 ◽  
pp. 568-578 ◽  
Author(s):  
Khaled R.A. Abdellatif ◽  
Wael A.A. Fadaly ◽  
Yaseen A.M.M. Elshaier ◽  
Waleed A.M. Ali ◽  
Gehan M. Kamel
Keyword(s):  
Safety Profile ◽  
Inflammatory Activity ◽  
Pyrazole Derivatives ◽  
Cox 2 ◽  
Anti Inflammatory

An Overview of Novel Bioactive Compounds with Potent Anti-Inflammatory Activity via Dual COX-2 and 5-LOX Enzyme Inhibition

2021 ◽  
Vol 18 ◽  
Author(s):  
Roopal Mittal ◽  
Shailesh Sharma ◽  
Ajay Singh Kushwah
Keyword(s):  
Bioactive Compounds ◽  
Enzyme Inhibitors ◽  
World Health Organisation ◽  
The Body ◽  
Inflammatory Activity ◽  
World Health ◽  
Quality Data ◽  
The World ◽  
Cox 2 ◽  
Anti Inflammatory

Background: Inflammation is the earliest body defence mechanism in which the immune system recognises and counters the antigens and aids in healing the disease. The World Health Organisation suggests that inflammation is one of the greatest causes of death in the world. Inflammation could be acute or chronic due to the release of inflammatory mediators i.e. prostaglandins, leukotrienes due to mitogens, antigens or cytokines found in the body. Methods: Bibliographic database using pub med cites for peer-reviewed research articles with titles containing dual COX-2 and 5-LOX enzyme inhibitors, heterocyclic moieties, with AND Boolean operator's terms since last ten years of literature work. The quality papers containing the natural or synthetic lead compounds were extracted; the detailed study and conceptual framework attracted its attention. Results: Out of 127 research and review articles evaluated, 54 articles were cited to provide high quality data regarding pharmacoactive molecules having anti-inflammatory activity via dual COX-2/5-LOX inhibition. In addition, highlighting their in silico and experimental wet laboratory studies in increasing order over the past decade with the best illustration of dual enzyme inhibitory activity. Conclusion: This review gathered details of isolated bioactive compounds such as pyrazole, coumaperine, indoles, phenanthrene derivatives that have been significantly reported for anti-inflammatory activities.

Anti-inflammatory activity of essential oil of an endemicThymus fontanesiiBoiss. & Reut. with chemotype carvacrol, and its healing capacity on gastric lesions

2017 ◽  
Vol 41 (3) ◽  
pp. e12359 ◽  
Author(s):  
Lilia Mouhi ◽  
Houria Moghrani ◽  
Noureddine Nasrallah ◽  
Abdeltif Amrane ◽  
Rachida Maachi
Keyword(s):  
Essential Oil ◽  
Inflammatory Activity ◽  
Gastric Lesions ◽  
Anti Inflammatory

scholarly journals IN SILICO DESIGN AND MOLECULAR DOCKING STUDIES OF SOME 1, 2-BENZISOXAZOLE DERIVATIVES FOR THEIR ANALGESIC AND ANTI-INFLAMMATORY ACTIVITY

2017 ◽  
Vol 9 (3) ◽  
pp. 133
Author(s):  
Sarath Sasi Kumar ◽  
Anjali T
Keyword(s):  
Molecular Docking ◽  
Acetylcholine Receptor ◽  
Nicotinic Acetylcholine Receptor ◽  
Analgesic Activity ◽  
In Silico ◽  
Docking Studies ◽  
Inflammatory Activity ◽  
Nicotinic Acetylcholine ◽  
Cox 2 ◽  
Anti Inflammatory

Objective: In silico design and molecular docking of 1,2-benzisoxazole derivatives for their analgesic and anti-inflammatory activity using computational methods.Methods: In silico molecular properties of 1,2-benzisoxazole derivatives were predicted using various software’s such as Chemsketch, Molinspiration, PASS and Schrodinger to select compounds having optimum drug-likeness, molecular descriptors resembling those of standard drugs and not violating the ‘Lipinski rule of 5’. Molecular docking was performed on active site of nicotinic acetylcholine receptor (PDB: 2KSR) for analgesic activity and COX-2 (PDB: 6COX) for anti-inflammatory activity using Schrodinger under maestro molecular modelling environment.Results: From the results of molecular docking studies of 1,2-benzisoxazole derivatives, all the compounds showed good binding interactions with Nicotinic acetylcholine receptor and COX-2. Compounds 4a and 4c showed highest binding scores (-7.46 and-7.21 respectively) with nicotinic acetylcholine receptor and exhibited maximum analgesic activity. Compound 4a showed highest binding score (-7.8) with COX-2 and exhibited maximum anti-inflammatory activity.Conclusion: All the derivatives of 1,2-benzisoxazole showed good analgesic and anti-inflammatory activity as predicted using molecular docking on respective receptors.

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