scholarly journals Phenanthrenes in Chinese Yam Peel Exhibit Anti-inflammatory Activity, as Shown by Strong in Vitro Cyclooxygenase Enzyme Inhibition

2016 ◽  
Vol 11 (9) ◽  
pp. 1934578X1601100 ◽  
Author(s):  
Qian Li ◽  
Chuan-Rui Zhang ◽  
Amila A. Dissanayake ◽  
Qun-yu Gao ◽  
Muraleedharan G. Nair
Keyword(s):  
Food Item ◽  
Inflammatory Activity ◽  
Spectroscopic Methods ◽  
Over The Counter ◽  
Chinese Yam ◽  
Inflammatory Drugs ◽  
In Vitro Bioassays ◽  
Anti Inflammatory ◽  
Cox 1

Chinese yam ( Dioscorea opposita), peeled or whole, is a popular food item that is considered to be healthy. Often, the yam is peeled before cooking. However, it is also consumed with peel. Therefore, in this study, the peel of this yam was extracted sequentially with n-hexane, ethyl acetate and methanol, and studied for its health-benefits, using in vitro bioassays. Bioactivity-guided purifications of extracts of the peel afforded phenanthrenes (1-4), as characterized by spectroscopic methods. Phenanthrene 1 is a novel analogue. The extracts and isolates were tested for anti-inflammatory activity using cyclooxygenase enzyme (COX-1 and -2) inhibitory assays. All phenanthrenes isolated from the yam peel showed higher inhibition of COX enzymes than the over-the-counter nonsteroidal anti-inflammatory drugs (NSAIDs) aspirin, ibuprofen and naproxen.

scholarly journals A REVIEW ON IN VIVO AND IN VITRO EXPERIMENTAL MODELS TO INVESTIGATE THE ANTI-INFLAMMATORY ACTIVITY OF HERBAL EXTRACTS

2018 ◽  
Vol 11 (11) ◽  
pp. 29
Author(s):  
Inayat Kabir ◽  
Imtiyaz Ansari
Keyword(s):  
Reference Model ◽  
Experimental Models ◽  
Inflammatory Activity ◽  
Herbal Extracts ◽  
Double Positive ◽  
Arthritis Models ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

The article emphasizes the anti-inflammatory effects of herbal extracts on different experimental models that are repeatedly used to test the in vivo anti-inflammatory activity of herbal components. Edema, granuloma and arthritis models are used to test the anti-inflammatory activity of plant extracts whereas formalin or acetic acid-induced writhing test and hot plate methods are the most repeatedly used to evaluate anti-nociceptive potentials of the herbal extracts. Although adjuvant-induced and collagen-induced arthritis models are also quite efficient, they have been used seldom to evaluate anti-inflammatory tendencies of the herbs. Here, we suggest a double positive reference model using both steroid and nonsteroidal anti-inflammatory drugs at the same time, instead of using only one of them either.

scholarly journals Synthesis, Anti-Inflammatory Activity and Molecular Docking Studies of 1,4,5,6-Tetrahydropyrimidine-2-Carboxamides

2020 ◽  
Vol 27 (3) ◽  
pp. 353-365
Author(s):  
Volodymyr Ya. Horishny ◽  
Pavlo V. Zadorozhnii ◽  
Ivanna V. Horishnia ◽  
Vasyl S. Matiychuk
Keyword(s):  
Molecular Docking ◽  
Side Effects ◽  
Docking Studies ◽  
Inflammatory Activity ◽  
Cox Inhibitors ◽  
White Rats ◽  
Urgent Task ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Background: Nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most commonly used drugs in the world. The widespread use of NSAIDs is associated with a number of serious side effects and complications observed for both selective and non-selective COX inhibitors. Therefore, the search for new COX inhibitors, which along with their effectiveness will have minimal side effects, is a very important and urgent task. Methods: This work studied the synthesis of new 1,4,5,6-tetrahydropyrimidine-2-carboxamides based on the reaction of 2-morpholin-4-yl-N-(het)aryl-2-thioxoacetamides with 1,3-diaminopropane. All obtained compounds were tested for anti-inflammatory activity in vitro and in silico conditions. All synthesized 1,4,5,6-tetrahydropyrimidine-2-carboxamides were tested for influence on the course of the exudative phase of the inflammatory process based on the carrageenan model of paw edema of laboratory nonlinear heterosexual white rats weighing 220-250 g, using Diclofenac as a reference. Optimization of the geometry of the studied structures and molecular docking was carried out using the ArgusLab 4.0.1 software package. Results: The target products were obtained with yields of 71-98% and easily isolated from the reaction mixture. The best anti-inflammatory activity was found in N-(4-chlorophenyl)-1,4,5,6-tetrahydropyrimidine-2-carboxamide and in N-[4-chloro-3-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydropyrimidine-2-carboxamide, suppression of the inflammatory response was 46.7 and 46.4%, respectively. The results of molecular docking with COX-1 and COX-2 enzymes were in good agreement with the experimental data, R2 ˃ 0.92 and R2 ˃ 0.83, respectively. Conclusion: The compounds under study were shown to be promising as potential anti-inflammatory agents.

New ibuprofen derivatives as H2S and NO donors as safer anti-inflammatory agents

2019 ◽  
Vol 11 (23) ◽  
pp. 3029-3045
Author(s):  
Ghaneya S Hassan ◽  
Gehan H Hegazy ◽  
Noha M Ibrahim ◽  
Samar H Fahim
Keyword(s):  
Docking Studies ◽  
Inflammatory Activity ◽  
Ulcer Index ◽  
No Donor ◽  
No Donors ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Edema Inhibition ◽  
Cox 1 ◽  
Gastrointestinal Ulceration

Aim: Nonsteroidal anti-inflammatory drugs are expansively used worldwide. However, their prolonged administration is associated with serious side effects, especially gastrointestinal ulceration. Materials & methods: New ibuprofen derivatives hybridized with H2S- or NO-donating moieties were synthesized and evaluated for their anti-inflammatory activity and ulcerogenic effect. COX-1/COX-2 isozymes selectivity test for the most promising derivatives was performed. Molecular docking studies were performed. Results: Most of the compounds showed promising anti-inflammatory activity comparable to that of ibuprofen (% edema inhibition = 76.6 and ulcer index = 21.26) with much better gastrointestinal tract tolerance (ulcer indices ranging from 0 to 14.67), especially compound 2 -H2S donor- (% edema inhibition = 75.5 and ulcer index = 11.75) and compound 16 -NO donor- (% edema inhibition = 65.4 and ulcer index = 8.66).

scholarly journals Studies in 3,4-diaryl-1,2,5-oxadiazoles and their N-oxides: Search for better COX-2 inhibitors

2007 ◽  
Vol 57 (1) ◽  
pp. 13-30 ◽  
Author(s):  
Mange Yadav ◽  
Shrikant Shirude ◽  
Devendra Puntambekar ◽  
Pinkal Patel ◽  
Hetal Prajapati ◽  
...  
Keyword(s):  
Enzyme Inhibition ◽  
Docking Studies ◽  
Inflammatory Activity ◽  
Rat Paw Edema ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 2 Inhibitors ◽  
Cox 1

Studies in 3,4-diaryl-1,2,5-oxadiazoles and theirN-oxides: Search for better COX-2 inhibitorsA series of 3,4-diaryl-1,2,5-oxadiazoles and 3,4-diaryl-1,2,5-oxadiazoleN-oxides were prepared and evaluated for COX-2 and COX-1 binding affinityin vitroand for anti-inflammatory activity by the rat paw edema method.p-Methoxy (p-OMe) substituted compounds 9, 21, 34, 41, 42 showed COX-2 enzyme inhibition higher than that showed by compounds with other substituents. 3,4-Di(4-methoxyphenyl)-1,2,5-oxadiazoleN-oxide (42) showed COX-2 enzyme inhibition of 54% at 22 μmol L-1and COX-1 enzyme inhibition of 44% at 88 μmol L-1concentrations, but showed very lowin vivoanti-inflammatory activity. Its deoxygenated derivative (21) showed lower COX-2 enzyme inhibition (26% at 22 μmol L-1) and higher COX-1 enzyme inhibition (53% at 88 μmol L-1) but, markedin vivoanti-inflammatory activity (71% at 25 mg kg-1)vs.celecoxib (48% at 12.5 mg kg-1). Molecular modeling (docking) studies showed that the methoxy group is positioned in the vicinity of COX-2 secondary pocket and it also participates in hydrogen bonding interactions in the COX-2 active site. These preliminary studies suggest thatp-methoxy (p-OMe) group in one of benzene rings may give potentially active leads in this series of oxadiazole/N-oxides.

scholarly journals Nonsteroidal Anti-Inflammatory Drugs and Prostatic Diseases

2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Hitoshi Ishiguro ◽  
Takashi Kawahara
Keyword(s):  
Antinociceptive Effects ◽  
Inflammatory Processes ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Prostatic Diseases ◽  
The Relationship ◽  
Increased Activity ◽  
Cox 1

Prostatic diseases are characterized by increased activity of cytokines, growth factors, and cyclooxygenases- (COX-) 1 and 2. Activation of COX-1 and COX-2 results in increased levels of prostaglandins and the induction of angiogenic, antiapoptotic and inflammatory processes. Inhibition of COX enzymes by members of the widely used nonsteroidal anti-inflammatory drug (NSAID) class of drugs decreases prostaglandin production, and exerts a variety of anti-inflammatory, antipyretic, and antinociceptive effects. While numerousin vitro,in vivo, and clinical studies have shown that NSAIDs inhibit the risk and progression of prostatic diseases, the relationship between NSAIDs and such diseases remains controversial. Here we review the literature in this area, critically analyzing the benefits and caveats associated with the use of NSAIDs in the treatment of prostatic diseases.

scholarly journals Design, Synthesis and Biological Screening of Novel 1,5-Diphenyl-3-(4-(trifluoromethyl)phenyl)-2-pyrazoline Derivatives

2020 ◽  
Vol 67 (4) ◽  
pp. 1139-1147
Author(s):  
Fatih Tok ◽  
Bedia Koçyiğit-Kaymakçıoğlu
Keyword(s):  
Inflammatory Activity ◽  
Antidiabetic Activity ◽  
Spectroscopic Methods ◽  
Design Synthesis ◽  
Reference Drug ◽  
Ic50 Values ◽  
Adme Properties ◽  
Anti Inflammatory ◽  
In Vitro Antioxidant Activity

1-Phenyl-5-substituted-3-(4-(trifluoromethyl)phenyl)-4,5-dihydro-1H-pyrazole derivatives were synthesized from chalcone derivatives. The structures of compounds were characterized by IR, 1H NMR spectroscopic methods and elemental analysis. All compounds were evaluated for their in vitro antioxidant activity using DPPH and ABTS methods, anti-inflammatory activity using lipoxygenase inhibitory method and antidiabetic activity using the α-glucosidase inhibitory method. Especially, pyrazoline derivatives exhibited stronger anti-inflammatory activity than the reference drug indomethacin (IC50: 50.45 μM) and their IC50 values were in the range of 0.68 and 4.45 μM. In addition, the ADME properties of all chalcone and pyrazoline derivatives were calculated by Lipinski’s and Veber’s rules.

scholarly journals Anti-inflammatory activity of nutmeg oleoresin mediated silver nanoparticles- An In- vitro study

Biomedicine ◽  
2020 ◽  
Vol 39 (2) ◽  
pp. 234-238
Author(s):  
Shivani Narendra ◽  
Anitha Roy ◽  
Rajeshkumar Shanmugam ◽  
Lakshmi Thangavelu
Keyword(s):  
Silver Nanoparticles ◽  
In Vitro Study ◽  
Inflammatory Activity ◽  
Synthesis Of Nanoparticles ◽  
Natural Substances ◽  
Therapeutic Uses ◽  
Vis Spectroscopy ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Introduction and Aim: The most emerging area of research in nanotechnology deals with the synthesis of nanoparticles which are of great importance due to its use in various biological fields. Myristica fragrans is commonly known as “nutmeg”. It is popular as a spice and also possesses various therapeutic properties. It has a characteristic pleasant fragrance and a slightly warm taste. It has various therapeutic uses and is widely used. The aim is to assess the anti-inflammatory activity of nutmeg oleoresin mediated silver nanoparticles. Materials and Methods: The nutmeg oleoresin mediated silver nanoparticles were synthesized and was confirmed by UV Vis spectroscopy. The anti-inflammatory property of the prepared nutmeg oleoresin mediated silver nanoparticles was assessed using albumin denaturation inhibitory assay technique. Results: The nutmeg oleoresin mediated silver nanoparticles showed good anti-inflammatory activity with increasing concentration of the nanoparticles. Conclusion: Although a variety of steroidal and non-steroidal anti-inflammatory drugs have been developed, researchers are focusing on natural substances to develop new anti-inflammatory agents. Nutmeg mediated silver nanoparticles showed a good range of inhibition and can be used against inflammation. The myristicin present in the nutmeg maybe responsible for its anti-inflammatory action. Increased albumin denaturation is reported in conditions like in rheumatoid arthritis, diabetes and cancer. Hence this may pay way to manage such conditions.  

Expression of VEGF-A And COX-2 mRNA in non-steroidal anti-inflammatory drugs treated rat primary colonic fibroblast

2020 ◽  
Vol 1 (1) ◽  
Author(s):  
Andrew Limavanady ◽  
Jonathan J ◽  
Gloria Evita Thalia ◽  
Rasya Mayora ◽  
Ade Saputri ◽  
...  
Keyword(s):  
Mrna Expression ◽  
In Vitro Study ◽  
Rat Colon ◽  
Colon Anastomosis ◽  
Anastomosis Leakage ◽  
Inflammatory Drugs ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

Non-steroidal anti-inflammatory drugs (NSAIDs) is often used to shorten recovery time after surgery, including after colon anastomosis surgery. Studies showed that NSAIDs might involve in the development of colon anastomotic leakage. However, the effect of NSAIDs in colon anastomosis leakage is still a subject of controversy. Studies indicated that selectivity of COX-2 might have a role in the deleterious effect of NSAIDs in colon anastomosis. Disruption of VEGF-A by NSAIDs also suspected to be the culprit in the development of anastomosis leakage during NSAIDs treatment. This study aimed to investigate the NSAIDs effect toward VEGF-A and COX-2 mRNA in rat primary colonic fibroblast. The in vitro study was conducted using fibroblast isolated from rat colon. The isolated fibroblast was divided into 4 groups of treatment i.e.controlgroup, acetaminophen group, metamizole group, and ketorolacgroup. After 48 h of treatment, the cell was harvested and the RNA was isolated. The expression of VEGF-A and COX-2 mRNA was conducted using semi-quantitative PCR(sq-PCR). Both VEGF-A and COX-2 were not expressed in untreated rat colon fibroblast. However, VEGF-A mRNA washighly expressed in the ketorolacgroup. Interestingly, COX-2 mRNA couldbe seen in the ketorolac and metamizole groups but not in the acetaminophen group. The COX-2 mRNA expression wasthe highest in ketorolac treated rat colon fibroblast. It can be concluded that the effect of various kinds of NSAIDs towards VEGF-A and COX-2 mRNA expression of colon fibroblasts is different. This condition is duetotheir different inhibitory selectivity towards COX-1 and COX2.

Sign in / Sign up

Export Citation Format

Share Document