Heparin and proteoglycans as anti-inflammatory drugs

1996 ◽  
Vol 16 (01) ◽  
pp. 56-59
Author(s):  
D. J. Tyrrell ◽  
C. P. Page

SummaryEvidence continues to accumulate that the pleiotropic nature of heparin (beyond its anticoagulant potency) includes anti-inflammatory activities at a number of levels. It is clear that drugs exploiting these anti-inflammatory activities of heparin may offer exciting new therapeutic applications to the treatment of a wide range of inflammatory diseases.

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 ◽  
...  

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.


2021 ◽  
Vol 28 ◽  
Author(s):  
Josiane Viana Cruz ◽  
Joaquín María Campos Rosa ◽  
Njogu Mark Kimani ◽  
Silvana Giuliatti ◽  
Cleydson Breno Rodrigues dos Santos

: This article presents a simplified view of celecoxib as a potential inhibitor in the treatment of inflammatory diseases. The enzyme cyclooxygenase (COX) has, predominantly, two isoforms called cyclooxygenase 1 (COX-1) and cyclooxygenase 2 (COX-2). The former plays a constitutive role that is related to homeostatic effects in renal and platelets, while the latter is mainly responsible for induction of inflammatory effects. Since COX-2 plays an important role in the pathogenesis of inflammatory diseases, it has been signaled as a target for the planning of anti-inflammatory intermediates. Many inhibitors developed and planned for COX-2 inhibition have presented side effects to humans, mainly in the gastrointestinal and/or cardiovascular tract. Therefore, it is necessary to design new potential COX-2 inhibitors, which are relatively safe and without side effects. To this end, of the generation of non-steroidal anti-inflammatory drugs from “coxibs”, celecoxib is the only potent selective COX-2 inhibitor that is still commercially available. Thus, the compound celecoxib became a commercial prototype inhibitor for the development of anti-inflammatory agents for COX-2 enzyme. In this review, we provide highlights where such inhibition should provide a structural basis for the design of promising new non-steroidal anti-inflammatory drugs (NSAIDs) which act as COX-2 inhibitors with lesser side effects on the human body.


2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Sara Mahdiabadi ◽  
Sara Momtazmanesh ◽  
George Perry ◽  
Nima Rezaei

Abstract Alzheimer’s disease (AD), the most common cause of dementia, is characterized by progressive cognitive and memory impairment ensued from neuronal dysfunction and eventual death. Intraneuronal deposition of tau proteins and extracellular senile amyloid-β plaques have ruled as the supreme postulations of AD for a relatively long time, and accordingly, a wide range of therapeutics, especially immunotherapies have been implemented. However, none of them resulted in significant positive cognitive outcomes. Especially, the repetitive failure of anti-amyloid therapies proves the inefficiency of the amyloid cascade hypothesis, suggesting that it is time to reconsider this hypothesis. Thus, for the time being, the focus is being shifted to neuroinflammation as a third core pathology in AD. Neuroinflammation was previously considered a result of the two aforementioned phenomena, but new studies suggest that it might play a causal role in the pathogenesis of AD. Neuroinflammation can act as a double-edged sword in the pathogenesis of AD, and the activation of glial cells is indispensable for mediating such attenuating or detrimental effects. The association of immune-related genes polymorphisms with the clinical phenotype of AD as well as the protective effect of anti-inflammatory drugs like nonsteroidal anti-inflammatory drugs supports the possible causal role of neuroinflammation in AD. Here, we comprehensively review immune-based therapeutic approaches toward AD, including monoclonal antibodies and vaccines. We also discuss their efficacy and underlying reasons for shortcomings. Lastly, we highlight the capacity of modulating the neuroimmune interactions and targeting neuroinflammation as a promising opportunity for finding optimal treatments for AD.


Author(s):  
M. L. Maksimov ◽  
N. M. Kiseleva ◽  
D. G. Semenikhin ◽  
B. K. Romanov

Non-steroidal anti-inflammatory drugs (NSAIDs) are included in a pharmacological group of drugs with different chemical structures providing anti-inflammatory, analgesic and antipyretic actions, as well as antiplatelet action to a certain degree. Unfortunately, NSAIDs can cause a wide range of adverse reactions (AR) posing a serious risk to the health and life of patients. Therefore, the rational use of NSAIDs should include methods for effective prevention of drug complications. Many NSAIDs have a pronounced therapeutic effect, simultaneously causing many undesirable effects, so the drug shall be chosen considering the development of predicted side effects and modern algorithms. According to clinical recommendations, risk factors and administration of safer NSAIDs shall be considered as the main prevention method. Besides, it is possible to protect the patient from the upper gastrointestinal tract complications using proton pump inhibitors. It should be noted that there are no effective medication methods for kidney and liver protection to reduce the risk of NSAID-associated complications.


2016 ◽  
Vol 29 (4) ◽  
pp. 562-571 ◽  
Author(s):  
Chethan Gejjalagere Honnappa ◽  
Unnikrishnan Mazhuvancherry Kesavan

Inflammatory diseases are complex, multi-factorial outcomes of evolutionarily conserved tissue repair processes. For decades, non-steroidal anti-inflammatory drugs and cyclooxygenase inhibitors, the primary drugs of choice for the management of inflammatory diseases, addressed individual targets in the arachidonic acid pathway. Unsatisfactory safety and efficacy profiles of the above have necessitated the development of multi-target agents to treat complex inflammatory diseases. Current anti-inflammatory therapies still fall short of clinical needs and the clinical trial results of multi-target therapeutics are anticipated. Additionally, new drug targets are emerging with improved understanding of molecular mechanisms controlling the pathophysiology of inflammation. This review presents an outline of small molecules and drug targets in anti-inflammatory therapeutics with a summary of a newly identified target AMP-activated protein kinase, which constitutes a novel therapeutic pathway in inflammatory pathology.


Author(s):  
Mohd. I. Yatoo ◽  
Arumugam Gopalakrishnan ◽  
Archana Saxena ◽  
Oveas R. Parray ◽  
Noore A. Tufani ◽  
...  

2021 ◽  
Vol 12 ◽  
Author(s):  
Fernanda O. Novais ◽  
Camila Farias Amorim ◽  
Phillip Scott

Cutaneous leishmaniasis exhibits a wide spectrum of clinical presentations from self-resolving infections to severe chronic disease. Anti-parasitic drugs are often ineffective in the most severe forms of the disease, and in some cases the magnitude of the disease can result from an uncontrolled inflammatory response rather than unrestrained parasite replication. In these patients, host-directed therapies offer a novel approach to improve clinical outcome. Importantly, there are many anti-inflammatory drugs with known safety and efficacy profiles that are currently used for other inflammatory diseases and are readily available to be used for leishmaniasis. However, since leishmaniasis consists of a wide range of clinical entities, mediated by a diverse group of leishmanial species, host-directed therapies will need to be tailored for specific types of leishmaniasis. There is now substantial evidence that host-directed therapies are likely to be beneficial beyond autoimmune diseases and cancer and thus should be an important component in the armamentarium to modulate the severity of cutaneous leishmaniasis.


2021 ◽  
Vol 6 (5) ◽  
pp. 38-44
Author(s):  
O. D. Saliuk ◽  
◽  
P. H. Gerasimchuk ◽  
L. O. Zaitsev ◽  
I. I. Samoilenko ◽  
...  

In this article the review of foreign and domestic literary sources, which are devoted to the actual problem of modern dentistry – the treatment of inflammatory diseases of periodontal tissues: gingivitis and periodontitis are presented. The complex approach to their treatment involves the appointment of a significant amount of pharmacotherapeutic drugs. Therapeutic failures and iatrogenic complications have led to the fact that today the interests of doctors and population to medicinal products significantly increased. The purpose of the study is to analyze the data of scientific literature on the use of plant-based medicinal products for the treatment of periodontal inflammatory diseases over the past 10 years. Materials and methods. Comprehensive and systematic analysis of literature. Review and discussion. The analysis of information sources on the use of plant-based medicinal products in dentistry both independently and in the composition of medical and prophylactic means has established that the modern assortment of plant-based preparations in the pharmaceutical market of Ukraine to a certain extent is limited. The emergence of new plant-based species that have been tested in conditions of experimental pathology and require an evidence-based clinical base is noted. The composition of plant-based preparations used for the treatment of inflammatory periodontal diseases include vitamins, biologically active substances, glycosides, alkaloids, in connection with a wide range of action: antiseptic, anti-inflammatory, regenerating, hemostatic, antioxidative. The data on plant-based preparations that are most often used such as chamomile extracts, calendula, hypericum, plantain, kalanchoe, aloe, eucalyptus, milfoil, nettle, calamus and plant-based species are summarized. The medicinal agents considered are mainly recommended for local treatment of periodontal diseases in the form of dental care means, mouth rinse, gel, chewing gum, herbal liquer. It is known that the complex treatment of periodontal diseases includes a general influence on the body. The properties of green tea with its wide range of actions are investigated. With antioxidant properties, it can be a healthy alternative for controlling destructive changes in periodontal diseases. Attention is drawn to the proposed unique natural complex “Resverazin” due to a wide range of pharmacological action, low toxicity and relative safety. The drug produces antioxidant, anti-inflammatory, immune stimulating, vasodilative, neuroprotective action. Conclusion. Based on the literature analysis, it can be concluded that the accumulated experimental and clinical data on the therapeutic properties of plants prove perspective of their use in the complex treatment of inflammatory periodontal diseases. Future studies are mandatory for further confirmation of the effectiveness of these medicinal plants


1991 ◽  
Vol 62 (1) ◽  
pp. 35-38 ◽  
Author(s):  
G. E. Swan

A large number of non-steroidal anti-inflammatory drugs, of different chemical groups are available for veterinary use. These drugs act mainly by inhibiting the. formation of endoperoxides (prostaglandins and thromboxanes) through the inhibition of cyclo-oxygenase in the eicosanoid pathway. A wide range of pharmacological effects, including analgesic, antipyretic and anti-inflammatory effects occur as a result of this inhibition. The classification, mechanism of action and pharmacological effects of these drugs are reviewed.


2016 ◽  
Vol 78 (6-8) ◽  
Author(s):  
Smirnov Ivan ◽  
Murashko Tatyana ◽  
Ivanov Alex ◽  
Bondarev Alex ◽  
Udut Vladimir

Chronic inflammatory diseases of various genesis are prevalent today. Non-steroidal anti-inflammatory drugs (NSAIDs) are commonly used to treat pain and inflammation, but their long-term use is associated with complications in the gastrointestinal tract, including peptic ulcers. We synthesized a molecule of sodium salt (4-О-β-glucopyranosyloxy)-benzoic acid. This substance has diuretic and anti-inflammatory activities. It should be noted that most of NSAIDs has analgesic effect. In this connection, the aim of this study was to evaluate the analgesic activity of sodium salt (4-О-β-glucopyranosyloxy)-benzoic acid. We studied analgesic effect in the test “acetic writhing”. Sodium salt (4-О-β-glucopyranosyloxy)-benzoic acid significantly reduces the number of writhing by 14 units during the experiment, as an alternative criterion percent of animals with analgesia was 42.6%. Thus, in the test "acetic writhing" revealed the presence of the analgesic activity have developed drug average severity. 


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