1,721,147 research outputs found
Peptidi e Peptidomimetici: Progettazione, sintesi e caratterizzazione, applicazioni di nuove strategie sintetiche (chimica combinatoriale, microonde)
No full textThe nitric oxide related therapeutic phenomenon: a challenging task.
No full textResearch in the nitric oxide (NO) field has enormously extended in the past 20 years and maintaining an overview of NO research has become very difficult. NO biology has been extensively studied and several aspects of its role in physiology and pathology have been clarified. The final outcome of these researches is that NO is a double edge sword mediator in that it can exert beneficial or detrimental effect depending on the physiopathological context. However, the development of drugs based on these new knowledge has been strongly impaired by these double face of NO. The purpose of this review is to briefly outline the role of this almost ubiquitous mediator and give a state of the art on the development of new drugs based on the NO concept rather than summarising the large number of NO donors that have been synthesised since there are several specific review dealing with this matter. The final picture that comes out by our analysis is that it goes without any doubt that much has still to be done to develop new drugs. Thus, the development of new drugs still represents a challenging task. There has been an enormous interest on nitric oxide (NO) since its discovery and its involvement in many physiological and pathological events has been demonstrated or postulated. Drugs which acts through NO such as the organic nitrates have been used in therapy since many years and it would have been predicted that due to the enormous effort profuse in understanding the biology of NO, new drugs based on all these new findings would have been ready developed. So far this matter has resulted in a challenging task since, as it is summarised below, NO has multiple action that are linked to both beneficial and pathological effect. Thus, in some cases we want to prevent NO production while in other cases we want deliver or increase NO production. This review will briefly addresses some of the major areas of biology where NO has been involved and give an overview of what is the state of the art in developing drugs that works through NO
The application of microwave irradiation as new convenient synthetic procedure in drug discovery
No full textThe application of microwave irradiation as new convenient synthetic procedure in drug discovery
No full textA hydrogen sulfide-releasing dexamethasone derivative attenuates atopic dermatitis severity signs and the associated oxidative stress markers in mice
No full textAtopic dermatitis (AD) is a highly prevalent chronic inflammatory skin disease characterized by pruritus and eczematous skin lesions. Considering that hydrogen sulfide (H2S) is
produced in the skin and participates of several processes, such as the regulation of inflammation, pruritus, scarring, and angiogenesis (Coavoy-Sánchez, Costa, Muscará, 2019), we decided to test the effects of a H2S-releasing dexamethasone (Dexa) derivative in a murine model of AD
Hydrogen Sulfide (H2S)-Donor Molecules: Chemical, Biological, and Therapeutical Tools
Full text linkThis Special Issue aims to gather new research on hydrogen sulfide (H2S)-releasing compounds (Figure 1) as cutting-edge pharmacological tools and to advance the understanding of the critical role that H2S plays in physiological and pathological processes [...
Perfusion of rat colon with sennosides, rhein and rheinanthrone. Concentration-related histamine release
No full textGastrointestinal safety and anti-inflammatory effects of a hydrogen sulfide-releasing diclofenac derivative in the rat
No full textBACKGROUND & AIMS: Gastrointestinal damage caused by nonsteroidal
anti-inflammatory drugs (NSAIDs) remains a significant clinical problem. Hydrogen
makes an important contribution to mucosal defense, and NSAIDs can suppress its
synthesis. In this study, we evaluated the gastrointestinal safety and
anti-inflammatory effects of a novel "HS-NSAID" (ATB-337) that consists of
diclofenac linked to a hydrogen sulfide-releasing moiety.
METHODS: The gastrointestinal injury-inducing effects of single or repeated
administration of diclofenac versus ATB-337 were compared in rats, as were their
effects on prostaglandin synthesis and cyclooxygenase-1 and -2 activities. The
ability of these drugs to reduce carrageenan-induced paw edema and to elicit
leukocyte adherence to the vascular endothelium (intravital microscopy) were also
examined in rats.
RESULTS: Diclofenac (10-50 micromol/kg) dose-dependently damaged the stomach,
while ATB-337 did not. Repeated administration of diclofenac caused extensive
small intestinal damage and reduced hematocrit by 50%. ATB-337 induced >90% less
intestinal damage and had no effect on hematocrit. Diclofenac, but not ATB-337,
elevated gastric granulocyte infiltration and expression of tumor necrosis factor
alpha, lymphocyte function-associated antigen 1, and intercellular adhesion
molecule 1. ATB-337 inhibited cycloxygenase-1 and cyclooxygenase-2 activity as
effectively as diclofenac. ATB-337 did not induce leukocyte adherence, whereas
diclofenac did, and was more potent at reducing paw edema.
CONCLUSIONS: An HS-NSAID spares the gastric mucosa of injury despite markedly
suppressing prostaglandin synthesis. This effect may be related to hydrogen
sulfide-mediated inhibition of tumor necrosis factor-alpha expression and of the
leukocyte adherence to vascular endothelium normally induced by cyclooxygenase
inhibitors
- …
