scholarly journals Hydrogen Sulfide in Pharmacotherapy, Beyond the Hydrogen Sulfide-Donors

Biomolecules ◽  
2020 ◽  
Vol 10 (2) ◽  
pp. 323 ◽  
Author(s):  
Ewelina Zaorska ◽  
Lenka Tomasova ◽  
Dominik Koszelewski ◽  
Ryszard Ostaszewski ◽  
Marcin Ufnal
Keyword(s):  
Hydrogen Sulfide ◽  
Clinical Practice ◽  
Drug Metabolism ◽  
Therapeutic Effect ◽  
Clinical Studies ◽  
Chemical Structure ◽  
Anti Inflammatory

Hydrogen sulfide (H2S) is one of the important biological mediators involved in physiological and pathological processes in mammals. Recently developed H2S donors show promising effects against several pathological processes in preclinical and early clinical studies. For example, H2S donors have been found to be effective in the prevention of gastrointestinal ulcers during anti-inflammatory treatment. Notably, there are well-established medicines used for the treatment of a variety of diseases, whose chemical structure contains sulfur moieties and may release H2S. Hence, the therapeutic effect of these drugs may be partly the result of the release of H2S occurring during drug metabolism and/or the effect of these drugs on the production of endogenous hydrogen sulfide. In this work, we review data regarding sulfur drugs commonly used in clinical practice that can support the hypothesis about H2S-dependent pharmacotherapeutic effects of these drugs.

scholarly journals Synthesis, Characterization and Evaluation of In Vivo Anti-Inflammatory Activity of N-Substituted-1,3,4-Oxadiazole Derivatives

2020 ◽  
pp. 234-239
Author(s):  
Manisha Dhondising Rajput ◽  
C. S. Magdum. ◽  
S. K. Mohite ◽  
S. R. Kane
Keyword(s):  
Carboxylic Acid ◽  
1H Nmr ◽  
Clinical Studies ◽  
Chemical Structure ◽  
Ethyl Benzoate ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Oxadiazole Derivatives ◽  
Anti Inflammatory

The new series oxadiazole derivatives were prepared by reacting aromatic carboxylic acids.In the present work 10 different 5-substituted-1,3,4-oxadiazole -2-amine derivatives (3a -i) were synthesized. Substituted carboxylic acid is converted into substituted ethyl benzoate by esterification. Different ethyl benzoate is converted into different aroyl hydrazide by treating with hydrazine hydrate.The different aroyl hydrazide is converted 5-substituted-1,3,4-oxadiazole-2-amine derivatives by treating with cyanogen bromide.Confirmation of the chemical structure of the synthesized compounds was substantiated by TLC,IR,1H NMR, and MS spectroscopy.In present study,a series of 1,3,4-oxadiazole derivatives(3a- i)were evaluated for in vivo anti-inflammatory activity by carrageenan induced paw edema method. The results of anti-inflammatory evaluation revealed that compounds 3c, 3e and3i exhibited significant anti-inflammatory activity at a dose of 25 mg kg-1 compared to indomethacin used as the reference standard.The anti-inflammatory activity investigation highlights that the synthesized compound 3e could be considered for further clinical studies.

Study of Physico-chemical Characteristics and Pharmacological Effects of 1-Ethyl-Salicyldene-bis-Ethylene-Diamine and Its Complex with Mn(II)

2019 ◽  
Vol 70 (7) ◽  
pp. 2534-2537
Author(s):  
Gladiola Tantaru ◽  
Mihai Apostu ◽  
Antonia Poiata ◽  
Mihai Nichifor ◽  
Nela Bibire ◽  
...  
Keyword(s):  
Schiff Base ◽  
Chemical Structure ◽  
Antimicrobial Activities ◽  
Ethylene Diamine ◽  
Chemical Characteristics ◽  
Gram Negative Bacteria ◽  
Pharmacological Effects ◽  
Physico Chemical ◽  
Anti Inflammatory ◽  
Inflammatory Effect

The paper presents the synthesis of a new complex combination of a Bis-Schiff base with Mn(II) ions with great potential for antimicrobial and anti-inflammatory activity. A new complex of the Salen-type ligand, 1-ethyl-salicylidene-bis-ethylene diamine was synthetized using Mn(II) ions. The chemical structure was confirmed through 1H-NMR and IR spectroscopy. The antimicrobial activities of the Bis-Schiff base and its complex were tested in comparison with Ampicillin, Chloramphenicol, Tetracycline, Ofloxacin and Nystatin. Those compounds were found to be active against Gram-positive or Gram-negative bacteria, and had an anti-inflammatory effect comparable to that of Indomethacin.

Food and drugs

2002 ◽  
Vol 55 (1-2) ◽  
pp. 5-12 ◽  
Author(s):  
Kornelija Djakovic-Svajcer
Keyword(s):  
Plasma Level ◽  
Drug Metabolism ◽  
Drug Interactions ◽  
Therapeutic Effect ◽  
Significant Influence ◽  
Plasma Concentrations ◽  
Chemical Properties ◽  
Therapeutic Index ◽  
Food Composition ◽  
Drug Bioavailability

Food can exert a significant influence on the effects of certain drugs. The interactions between food and drugs can be pharmacokinetic and pharmacodynamic. Pharmacokinetic interactions most often take place on absorption and drug metabolism levels. Absorption can be either accelerated or delayed, increased or decreased, while drug metabolism can be either stimulated or inhibited. The factors which influence food-drug interactions are as follows: composition and physic-chemical properties of drugs, the interval between a meal and drug intake and food composition. Food consistency is of lesser influence on drug bioavailability than food composition (proteins, fats, carbohydrates, cereals). Important interactions can occur during application of drugs with low therapeutic index, whereby the plasma level significantly varies due to changes in resorption or metabolism (e.g. digoxin, theophyllin, cyclosporin) and drugs such as antibiotics, whose proper therapeutic effect requires precise plasma concentrations.

scholarly journals Novel Hydrogen Sulfide (H2S)-Releasing BW-HS-101 and Its Non-H2S Releasing Derivative in Modulation of Microscopic and Molecular Parameters of Gastric Mucosal Barrier

2021 ◽  
Vol 22 (10) ◽  
pp. 5211
Author(s):  
Dominik Bakalarz ◽  
Edyta Korbut ◽  
Zhengnan Yuan ◽  
Bingchen Yu ◽  
Dagmara Wójcik ◽  
...  
Keyword(s):  
Blood Flow ◽  
Hydrogen Sulfide ◽  
Gastric Mucosa ◽  
Dna Oxidation ◽  
Gastric Blood Flow ◽  
Gastric Mucosal Damage ◽  
Mucosal Barrier ◽  
Gastric Injury ◽  
Zinc Protoporphyrin ◽  
Anti Inflammatory

Hydrogen sulfide (H2S) is an endogenously produced molecule with anti-inflammatory and cytoprotective properties. We aimed to investigate for the first time if a novel, esterase-sensitive H2S-prodrug, BW-HS-101 with the ability to release H2S in a controllable manner, prevents gastric mucosa against acetylsalicylic acid-induced gastropathy on microscopic and molecular levels. Wistar rats were pretreated intragastrically with vehicle, BW-HS-101 (0.5–50 μmol/kg) or its analogue without the ability to release H2S, BW-iHS-101 prior to ASA administration (125 mg/kg, intragastrically). BW-HS-101 was administered alone or in combination with nitroarginine (L-NNA, 20 mg/kg, intraperitoneally) or zinc protoporphyrin IX (10 mg/kg, intraperitoneally). Gastroprotective effects of BW-HS-101 were additionally evaluated against necrotic damage induced by intragastrical administration of 75% ethanol. Gastric mucosal damage was assessed microscopically, and gastric blood flow was determined by laser flowmetry. Gastric mucosal DNA oxidation and PGE2 concentration were assessed by ELISA. Serum and/or gastric protein concentrations of IL-1α, IL-1β, IL-2, IL-4, IL-6, IL-10, IL-13, VEGF, GM-CSF, IFN-γ, TNF-α, and EGF were determined by a microbeads/fluorescent-based multiplex assay. Changes in gastric mucosal iNOS, HMOX-1, SOCS3, IL1-R1, IL1-R2, TNF-R2, COX-1, and COX-2 mRNA were assessed by real-time PCR. BW-HS-101 or BW-iHS-101 applied at a dose of 50 μmol/kg protected gastric mucosa against ASA-induced gastric damage and prevented a decrease in the gastric blood flow level. H2S prodrug decreased DNA oxidation, systemic and gastric mucosal inflammation with accompanied upregulation of SOCS3, and EGF and HMOX-1 expression. Pharmacological inhibition of nitric oxide (NO) synthase but not carbon monoxide (CO)/heme oxygenase (HMOX) activity by L-NNA or ZnPP, respectively, reversed the gastroprotective effect of BW-HS-101. BW-HS-101 also protected against ethanol-induced gastric injury formation. We conclude that BW-HS-101, due to its ability to release H2S in a controllable manner, prevents gastric mucosa against drugs-induced gastropathy, inflammation and DNA oxidation, and upregulate gastric microcirculation. Gastroprotective effects of this H2S prodrug involves endogenous NO but not CO activity and could be mediated by cytoprotective and anti-inflammatory SOCS3 and EGF pathways.

scholarly journals In Pursuit of an Effective Treatment: the Past, Present and Future of Clinical Trials in Inclusion Body Myositis

2021 ◽  
Author(s):  
A. M. Snedden ◽  
J. B. Lilleker ◽  
H. Chinoy
Keyword(s):  
Clinical Practice ◽  
Effective Treatment ◽  
Inclusion Body ◽  
Therapeutic Effect ◽  
Outcome Measures ◽  
Inclusion Body Myositis ◽  
Cytotoxic T Cells ◽  
Treatment Options ◽  
Trial Methodology ◽  
Short Treatment

Abstract Purpose of review No clinical trial in sporadic inclusion body myositis (IBM) thus far has shown a clear and sustained therapeutic effect. We review previous trial methodology, explore why results have not translated into clinical practice, and suggest improvements for future IBM trials. Recent findings Early trials primarily assessed immunosuppressive medications, with no significant clinical responses observed. Many of these studies had methodological issues, including small participant numbers, nonspecific diagnostic criteria, short treatment and/or assessment periods and insensitive outcome measures. Most recent IBM trials have instead focused on nonimmunosuppressive therapies, but there is mounting evidence supporting a primary autoimmune aetiology, including the discovery of immunosuppression-resistant clones of cytotoxic T cells and anti-CN-1A autoantibodies which could potentially be used to stratify patients into different cohorts. The latest trials have had mixed results. For example, bimagrumab, a myostatin blocker, did not affect the 6-min timed walk distance, whereas sirolimus, a promotor of autophagy, did. Larger studies are planned to evaluate the efficacy of sirolimus and arimoclomol. Summary Thus far, no treatment for IBM has demonstrated a definite therapeutic effect, and effective treatment options in clinical practice are lacking. Trial design and ineffective therapies are likely to have contributed to these failures. Identification of potential therapeutic targets should be followed by future studies using a stratified approach and sensitive and relevant outcome measures.

Chemical structure and anti-inflammatory activity of a branched polysaccharide isolated from Phellinus baumii

2021 ◽  
pp. 118214
Author(s):  
Yuqing Sun ◽  
Jinxi Huo ◽  
Shi Zhong ◽  
Jianxun Zhu ◽  
Yougui Li ◽  
...  
Keyword(s):  
Chemical Structure ◽  
Inflammatory Activity ◽  
Phellinus Baumii ◽  
Anti Inflammatory

Hydrogen sulfide-mediated cardioprotection: mechanisms and therapeutic potential

2010 ◽  
Vol 120 (6) ◽  
pp. 219-229 ◽  
Author(s):  
Madhav Lavu ◽  
Shashi Bhushan ◽  
David J. Lefer
Keyword(s):  
Blood Pressure ◽  
Cardiovascular Disease ◽  
Hydrogen Sulfide ◽  
Therapeutic Potential ◽  
Blood Pressure Regulation ◽  
Pressure Regulation ◽  
Signalling Molecule ◽  
Anti Inflammatory ◽  
Antioxidant Effects

H2S (hydrogen sulfide), viewed with dread for more than 300 years, is rapidly becoming a ubiquitously present and physiologically relevant signalling molecule. Knowledge of the production and metabolism of H2S has spurred interest in delineating its functions both in physiology and pathophysiology of disease. Although its role in blood pressure regulation and interaction with NO is controversial, H2S, through its anti-apoptotic, anti-inflammatory and antioxidant effects, has demonstrated significant cardioprotection. As a result, a number of sulfide-donor drugs, including garlic-derived polysulfides, are currently being designed and investigated for the treatment of cardiovascular conditions, specifically myocardial ischaemic disease. However, huge gaps remain in our knowledge about this gasotransmitter. Only by additional studies will we understand more about the role of this intriguing molecule in the treatment of cardiovascular disease.

Application of Steroid in Clinical Practice

2021 ◽  
pp. 448-450
Author(s):  
Tushar N. Sonwane ◽  
Pradip D. Dhangar ◽  
Dhananjay D. Chaudhari ◽  
Rajesh D. Ahire ◽  
Ritik S. Jain
Keyword(s):  
Clinical Practice ◽  
Chronic Diseases ◽  
Corticosteroid Therapy ◽  
Physiological Effects ◽  
Oral Diseases ◽  
Life Saving ◽  
Specific Organ ◽  
Anti Inflammatory ◽  
Oral Condition ◽  
Important Indication

Corticosteroids represent important therapies for numerous acute conditions and chronic diseases based on their broad anti-inflammatory and immunosuppressant effects. They have been used extensively in managing many oral diseases, due to their excellent anti-inflammatory and immune-modulator effect. This article is present at reviewing the uses of corticosteroids in the treatment various oral condition. To study more about corticosteroids and other related concepts. It was focus on Physiological effects, Effect of anesthesia and surgery and important indication of steroid in anaesthetic practice. There are strategies that can be used to minimize these risks, but some risks are often unavoidable. Topical use of corticosteroids, including inhalation, can be used to target specific organ for treatment. Corticosteroid therapy can be life-saving in serious and serve medical conditions.

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