Naproxen (naprosyn) and ketoprofen (orudis)

1974 ◽  
Vol 12 (7) ◽  
pp. 25-27
Keyword(s):  
Prostaglandin Synthesis ◽  
New Drugs ◽  
Inflammatory Activity ◽  
Inhibit Prostaglandin Synthesis ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Low Incidence ◽  
Gastric Irritation

Naproxen (Naprosyn - Syntex) and ketoprofen (Orudis - M & B) are new drugs for treating various forms of arthropathy. For both drugs the manufacturers claim good anti-inflammatory activity with a low incidence of unwanted effects, particularly gastric irritation, in comparison with other non-steroidal anti-inflammatory drugs. If these claims can be substantiated these preparations would be valuable. Like aspirin and other non-steroidal anti-inflammatory drugs they both inhibit prostaglandin synthesis. Both are chemically related to other such drugs, for example ibuprofen (Brufen - Boots).

scholarly journals Phytochemical research and anti-inflammatory activity of the dry extracts from northern highbush blueberry leaves

2021 ◽  
pp. 40-48
Author(s):  
Oleksandr Stremoukhov ◽  
Oleh Koshovyi ◽  
Mykola Komisarenko ◽  
Igor Kireyev ◽  
Andriy Gudzenko ◽  
...  
Keyword(s):  
Amino Acids ◽  
Phenolic Compounds ◽  
Side Effects ◽  
New Drugs ◽  
Inflammatory Activity ◽  
Highbush Blueberry ◽  
Northern Highbush Blueberry ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Blueberry Leaves

All over the world, non-steroidal anti-inflammatory drugs (NSAIDs) are taken annually by about three hundred million people and this figure is constantly increasing. At the same time, NSAIDs are also one of the most common causes of side effects of drug therapy. The development and implementation of new anti-inflammatory drugs, including those of plant origin, with minimal side effects is an urgent task of modern pharmaceutical science. Vaccinium corymbosum L. (family Ericaceae), which is gaining more and more popularity among berry crops and is successfully cultivated in Ukraine, is promising in this direction for research. The aim: phytochemical analysis of dry extracts from blueberry leaves to establish the possibility of creating new drugs with anti-inflammatory activity. Materials and methods. The objects of the study were dry extracts of northern highbush blueberry leaves. The content of amino acids and phenolic compounds was determined by HPLC and spectrophotometry. The prototypal activity was studied in vivo and in vitro. Research results. 4 dry extracts were obtained from northern highbush blueberry leaves. In the extracts obtained by HPLC, 7 amino acids were identified, including 3 essential ones: arginine, histidine, and phenylalanine. As a result of the HPLC study, 7 phenolic compounds were identified in extracts from the leaves of northern highbush blueberry: 5 flavonoids - rutin, quercetin-3-O-glucoside, kaempferol-3-O-glucoside, quercetin and kaempferol and 2 hydroxycinnamic acids, chlorogenic and caffeic acid. For the first time, the anti-inflammatory effect of extracts from blueberry leaves was investigated. It was revealed that extract 1 at a dose of 50 mg/kg and extract 4 modified with arginine at a dose of 25 mg/kg have the highest anti-inflammatory activity. Conclusions. The results of the conducted studies indicate that extracts from the leaves of northern highbush blueberry in terms of the content of biologically active substances are promising sources for the creation of new drugs and dietary supplements with anti-inflammatory activity

scholarly journals Thiophene-Based Compounds with Potential Anti-Inflammatory Activity

2021 ◽  
Vol 14 (7) ◽  
pp. 692
Author(s):  
Ryldene Marques Duarte da Cruz ◽  
Francisco Jaime Bezerra Mendonça-Junior ◽  
Natália Barbosa de Mélo ◽  
Luciana Scotti ◽  
Rodrigo Santos Aquino de Araújo ◽  
...  
Keyword(s):  
Inflammatory Diseases ◽  
Structural Characteristics ◽  
Tiaprofenic Acid ◽  
Inflammatory Activity ◽  
Drug Candidates ◽  
Biological Target ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Privileged Structures

Rheumatoid arthritis, arthrosis and gout, among other chronic inflammatory diseases are public health problems and represent major therapeutic challenges. Non-steroidal anti-inflammatory drugs (NSAIDs) are the most prescribed clinical treatments, despite their severe side effects and their exclusive action in improving symptoms, without effectively promoting the cure. However, recent advances in the fields of pharmacology, medicinal chemistry, and chemoinformatics have provided valuable information and opportunities for development of new anti-inflammatory drug candidates. For drug design and discovery, thiophene derivatives are privileged structures. Thiophene-based compounds, like the commercial drugs Tinoridine and Tiaprofenic acid, are known for their anti-inflammatory properties. The present review provides an update on the role of thiophene-based derivatives in inflammation. Studies on mechanisms of action, interactions with receptors (especially against cyclooxygenase (COX) and lipoxygenase (LOX)), and structure-activity relationships are also presented and discussed. The results demonstrate the importance of thiophene-based compounds as privileged structures for the design and discovery of novel anti-inflammatory agents. The studies reveal important structural characteristics. The presence of carboxylic acids, esters, amines, and amides, as well as methyl and methoxy groups, has been frequently described, and highlights the importance of these groups for anti-inflammatory activity and biological target recognition, especially for inhibition of COX and LOX enzymes.

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.

Gastric ulceration induced by nonsteroidal anti-inflammatory drugs is a neutrophil-dependent process

1990 ◽  
Vol 259 (3) ◽  
pp. G462-G467 ◽  
Author(s):  
J. L. Wallace ◽  
C. M. Keenan ◽  
D. N. Granger
Keyword(s):  
Platelet Activating Factor ◽  
Gastric Ulceration ◽  
Gastric Damage ◽  
Blue Staining ◽  
Vascular Endothelial ◽  
Cyclooxygenase Activity ◽  
Inhibit Prostaglandin Synthesis ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Endothelial Integrity

The hypothesis that neutrophils play an important role in the pathogenesis of gastric ulceration induced by nonsteroidal anti-inflammatory drugs (NSAIDs) was tested in rats. Rats made neutropenic by prior treatment with an antibody to rat neutrophils raised in goat were found to be significantly more resistant to the gastric-damaging actions of indomethacin or naproxen than were control rats or rats pretreated with normal goat serum. The reduction of damage in neutropenic rats was not due to effects of the antineutrophil serum on either gastric acid secretion or the ability of indomethacin or naproxen to inhibit prostaglandin synthesis. Gastric cyclooxygenase activity was inhibited by greater than 95% in both normal and neutropenic rats that received indomethacin or naproxen. Reduction of circulating neutrophil numbers by treating rats with methotrexate also resulted in a significant reduction in the susceptibility to gastric damage induced by indomethacin. Since activation of circulating neutrophils appeared to be important in the development of gastric erosions after administration of indomethacin, and in the significant changes in vascular endothelial integrity (Monastral Blue staining) observed within 15 min of indomethacin administration, we investigated the possibility that leukotrienes (LTs) and platelet-activating factor (PAF) might be involved in the pathogenesis of indomethacin-induced ulceration. Changes in gastric LTB4 synthesis were not observed after indomethacin administration. Pretreatment with either an LTD4 antagonist or a PAF antagonist was without significant effect on the extent of gastric damage induced by indomethacin. These results suggest an important role for neutrophils in the pathogenesis of NSAID-induced gastric ulceration. Neutrophils may be important in the vascular injury that occurs early after administration of these compounds.

scholarly journals SYNTHESIS NEW POTENTIAL ANTI-INFLAMMATORY AGENT SODIUM SALT OF PENTAGAMAVUNON-0

2010 ◽  
Vol 4 (3) ◽  
pp. 180-185
Author(s):  
Enade Perdana Istyastono ◽  
Rr. Sri Untari Siwi S.M.P ◽  
Andreas Asdi Utama ◽  
Supardjan A.M
Keyword(s):  
Inflammatory Activity ◽  
Physiological Changes ◽  
Solubility In Water ◽  
Curcumin Analogues ◽  
Inflammatory Agent ◽  
Curcumin Derivatives ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Living Tissues ◽  
Anti Inflammation

Inflammation is the response of living tissues to injury. The process affects physiological changes such as erythema, edema, asthma and fever. Non-steroid Anti-inflammatory Drugs (NSAIDs) have been developed since they could inhibit inflammation process because of its ability to inhibit biosynthesis of prostaglandin, one of inflammation mediators, through inhibition of cyclooxigenase (COX) enzymes. Molecules, which have been reported having anti-inflammatory activity, for example, are curcumin, some curcumin derivatives and curcumin analogues. One of curcumin analogues that has been  developed is pentagamavunon-0 (PGV-0) whose IUPAC name is 2,5-bis(4'-hidroxy-3'-methoxy-benzylidene)cyclo-pentanone. But PGV-0, which is like curcumin, practically insoluble in water, so it causes problems in the development. The aim of this research is to synthesize a derivative of PGV-0, a natrium salt of PGV-0 (natrium pentagamavunonate-0/Na-pentagamavunonate-0), which is hoped to have a better anti-inflammatory activity and solubility in water than PGV-0. PGV-0 was synthesized by reacting vanillin and cyclopentanone catalized by acid. Na-pentagamavunonate-0 was synthesized with PGV-0 as a starting material using an appropriate method. This research was able to synthesize new compound that was estimated as a natrium salt of PGV-0 (natrium pentagamavunonate-0/Na-pentagamavunonate-0).   Keywords: Curcumin, PGV-0, Na-pentagamavunonate-0, anti-inflammation

Anti-nociceptive and anti-inflammatory activity of synthesized novel benzoxazole derivatives

2021 ◽  
Vol 20 ◽  
Author(s):  
Mansi L. Patil ◽  
Swati S. Gaikwad ◽  
Naresh J. Gaikwad
Keyword(s):  
Cytotoxic Activity ◽  
Research Study ◽  
Ex Vivo ◽  
Immunological Response ◽  
Inflammatory Activity ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Introduction: Pain is an immunological response to any infection or inflammation and long term use of pain management therapy includes use of Nonsteroidal anti-inflammatory drugs which is associated with occurrence of toxicity as well as gastrointestinal bleeding. Therefore, the investigation of new analgesic and anti-inflammatory agents remains a major challenge. Aims: The objective of this research study is to undergo the pharmacological evaluation of newly synthesized benzoxazole derivatives. These novel derivatives were evaluated for anti-nociceptive, anti-inflammatory and cytotoxic activity using various in-vivo and ex-vivo methods. Methods: The study was carried out using swiss mice (adult male) weighing between 20gm to 30gm and were divided into groups containing (n=6) six animals in each group for treatment. The anti-nociceptive activity was performed by using 0.1ml of 0.6% v/v acetic acid as nociception inducer and evaluated by the diminished number of abdominal writhes. The anti-inflammatory activity was done using 0.1 ml of 2% w/v Carrageenan induced paw edema method was observed which was evaluated by calculating the percent maximum possible effect. Histopathological evaluation and cytotoxic activity of the compounds was carried out. Results: The results of this research study revealed that synthesized derivatives (a, b, c, d and e) showed promising anti-nociceptive and anti-inflammatory effect along significantly higher cytotoxic activity in MCF-7 cell lines. Conclusion: It can be concluded that synthesized derivatives (a, b, c, d and e) have potential anti-nociceptive and anti-inflammatory effect along with cytotoxic activity and certain modification in structure may result in potent activity.

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.

Anti-Inflammatory Activity of the Compositae Family and Its Therapeutic Potential

Planta Medica ◽  
2020 ◽  
Author(s):  
Deise Cristina Drummond Xavier Paes Lopes ◽  
Temistocles Barroso de Oliveira ◽  
Alessandra Lifsitch Viçosa ◽  
Simone Sacramento Valverde ◽  
Eduardo Ricci Júnior
Keyword(s):  
Web Of Science ◽  
Citation Index ◽  
Therapeutic Potential ◽  
Inflammatory Activity ◽  
Traditional Use ◽  
Scientific Databases ◽  
Research And Innovation ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Patent Survey

AbstractCompositae is the largest family of flowering plants, with more than 1600 genera and 22 000 species. It has many economic uses in foods, cosmetics, and pharmaceutics. The literature reports its numerous medicinal benefits and recognized anti-inflammatory activity. Thus, this study evaluated the technological trends of anti-inflammatory activity of Compositae, based on the survey of scientific databases, articles, and patents, as well as the website of the Brazilian National Health Regulatory Agency (ANVISA), which is responsible for registering and controlling of healthcare and cosmetic products in the Brazil. The survey was conducted between 2008 and 2018, in the databases Science Direct, Lilacs, PubMed, and Web of Science (main collection), as well as the SciELO Citation Index. The patent survey was carried out on the basis of the Derwent Innovations Index, an important source for worldwide patent consultation, which covers 20 y of registered patents. Despite the numerous studies involving species of the Compositae family in different models of anti-inflammatory activity, there are few records of patents or products on the market from these species for that purpose. Some species have a traditional use and are present even in the Phytotherapic Summary of the Brazilian Pharmacopeia. This review confirms the therapeutic potential of Compositae for the development of anti-inflammatory drugs and reinforces the need to develop competencies and reduce technological bottlenecks to promote research and innovation in biodiversity products.

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.

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