STUDY OF SPECIFIC PHARMACOLOGICAL ACTIVITY OF SODIUM SALT (4-О-Β-GLUCOPYRANOSYLOXY)-BENZOIC ACID

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. 

2016 ◽  
Vol 78 (5-6) ◽  
Author(s):  
Murashko Tatyana ◽  
Ivanov Alexey ◽  
Smirnov Ivan ◽  
Bondarev Alex ◽  
Alexey Nemtsev ◽  
...  

Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used in the world, primarily due to their high efficiency for the treatment of inflammatory induced pain syndrome. The main feature of NSAIDs is a combination of anti-inflammatory, analgesic, antipyretic, and anticoagulant properties. However, their long-term use is associated with side effects in the gastrointestinal tract including peptic ulcers and other. We developed and synthesized molecule of methyl (4-О-β-glucopyranosyloxy)-benzoic acid. The anti-inflammatory effect of methyl (4-О-β-glucopyranosyloxy)-benzoic acid evaluated using the carrageenan-induced hindpaw edema model. The study shows that the intragastrically administration of test substance to animals reduces inflammatory process.


2020 ◽  
Vol 11 (4) ◽  
pp. 557-562
Author(s):  
N. M. Seredynska ◽  
V. I. Kornienko ◽  
D. V. Kibkalo ◽  
O. S. Suvorova ◽  
O. M. Marchenko ◽  
...  

 With the interaction of drugs belonging to different pharmacotherapeutic groups – nonsteroidal anti-inflammatory and antihypertensive – against the background of comorbid arterial hypertension with rheumatoid arthritis, the activity and safety of drugs may change with their combined use. Changes in the analgesic activity of nonsteroidal anti-inflammatory drugs, different in their selectivity to the types of cyclooxygenase (diclofenac, nimesulide and celecoxib), under the conditions of their long-term combined use with amlodipine in different periods of inflammation against the background of hypertension should be studied. Using the model of adjuvant arthritis comorbid with hypertension, in experiments on nonlinear mature white rats, the threshold of pain sensitivity has been determined by means of the “tail flick” test. Hypertension was caused by salt load with 1% sodium chloride solution for drinking with free access to it. Adjuvant arthritis was induced by the introduction of complete Freund’s adjuvant into the plantar aponeurosis of the hind limb of each animal with the established arterial hypertension. Against the background of arterial hypertension and comorbid pathology, there was an increase in the threshold of pain sensitivity observed in rats, which indicated the development of hypoalgesia. When combined, amlodipine enhanced the analgesic activity of diclofenac during 60 days of observation, slightly heightened the analgesic effect of nimesulide – up to 42 days, the effect of Celecoxib – in the acute period and the period of manifestation of adjuvant arthritis against the background of hypertension. The antinociceptive effect of diclofenac with amlodipine and celecoxib with amlodipine exceeded the analgesic effect of the combined nimesulide with amlodipine use against the background of comorbid pathology. The results obtained can be taken into account under the conditions of prescribing drugs belonging to the studied pharmacotherapeutic groups. It is likely that the use of diclofenac for analgesia against the background of comorbid conditions is only appropriate in the acute period of rheumatoid arthritis. The use of nimesulide to achieve an analgesic effect in the recurrence of rheumatoid arthritis against the background of hypertension is appropriate in the acute period and in the period of the inflammatory process attenuation. A highly selective coxib group cyclooxygenase-2 inhibitor, celecoxib, can reduce pain during the acute period of arthritis and during the manifestation of an inflammatory reaction that has developed against the background of arterial hypertension.


2016 ◽  
Vol 64 (3) ◽  
pp. 312-319
Author(s):  
Juliano CAVAGNI ◽  
Francisco Wilker Mustafa Gomes MUNIZ ◽  
Cassiano Kuchenbecker RÖSING

ABSTRACT Periodontal diseases are infecto-inflammatory diseases. Literature, has tried to elucidate the infections component of gingivitis and periodontitis, for several years. In recent years, much has been discussed about the role of the host response modulators to periodontal therapeutic procedures. The aim of the present literature review was to evaluate the effect of host response modulating agents (anti-inflammatories) on the pathogenesis of gingivitis and periodontitis. A search in the main databases was performed and human and animal studies were selected. The majority of studies was performed in humans and non-steroidal anti-inflammatory drugs in different dosages were used. The results have shown a potential benefit of the non-steroidal anti-inflammatory drugs concerning the microbial challenge. However, this benefit seems not to occur in the long term, thus not supporting it as a periodontal therapeutic approach. Few studies evaluated the effect of steroidal anti-inflammatory drugs on the pathogenesis of periodontal diseases. Moreover, the results in humans and animals are controversial, pointing to a possible deleterious effect of steroidal anti-inflammatory drugs on periodontal structures.


2019 ◽  
Vol 9 (5) ◽  
pp. 311-328 ◽  
Author(s):  
Rufin Marie Kouipou Toghueo

Abstract Leishmaniases and chronic inflammatory diseases are the cause of millions of deaths in the world each year. The treatment of leishmaniasis is facing serious drawbacks particularly due to the limited number of effective medicines, the resistance, and the toxicity of available drugs. On the other hand, many drugs are used for the management of inflammatory disorders. However, the most commonly prescribed although efficient is highly toxic with multiples side effects. New leads compounds for the development of new anti-leishmanial and anti-inflammatory drugs are needed. Over the past decade, several studies on the potential of endophytes to produce bioactive metabolites have been reported. We are presenting in the present review the status of research from 2000 to 2019 on the anti-leishmanial and anti-inflammatory metabolites isolated from endophytes from diverse habitats. An emphasis was put on existing gaps in the literature to inspire and guide future investigations. We hope that this review will help accelerate the drug discovery against leishmaniases and inflammation-associated disorders. Graphic Abstract


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.


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