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Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents, Vol. 3, No. 3, 2004

 

Contents

 

Nitric Oxide

Guest Editor: Bahar Tunētan

 

Antioxidant Properties of Nitric Oxide in Cellular Physiological and Pathophysiological Mechanisms. The Implications of Biological Balance between ·NO and Oxidative Stress Pp. 181-188

Lisa A. Ridnour, Douglas D. Thomas, Daniele Mancardi, Sonia Donzelli, Nazerrano Paolocci, Pasquale Pagliaro, Katrina M. Miranda, Murali Krishna, John Fukuto, Matthew B. Grisham, James B. Mitchell, Michael G. Espey and David A. Wink

[Abstract]

 

The Physiology of Nitric Oxide: Control and Consequences Pp. 189-205

Ingrid Fleming and Rudi Busse

[Abstract]

 

Pathophysiological Roles of Nitric Oxide: In the Heart and the Coronary Vasculature Pp. 207-216

C. Dessy and O. Feron

[Abstract]

 

Nitric Oxide and Inflammation Pp. 217-222

C.C. Wu

[Abstract]

 

The Role of Nitric Oxide in Autoimmune Diseases Pp. 223-238

Klaus-Dietrich Kroncke

[Abstract]

 

Inhibitors of Nitrogen Oxide Species Production in Animal Models of Inflammation and Future Directions for Therapy in Inflammatory Disorders Pp. 239-259

Francois Feihl, Mauro Oddo, Bernard Waeber and Lucas Liaudet

[Abstract]

 

Effect of Inhibitors of Nitric Oxide in Animal Models and Future Directions for Therapy in Inflammatory Disorders Pp. 261-270

Salvatore Cuzzocrea

[Abstract]

 

The Use of Nitric Oxide Synthase Inhibitors in Inflammatory Diseases: A Novel Class of Anti-Inflammatory Agents Pp. 271-301

Bahar Tunētan and Sedat Altug

[Abstract]

 

Abstracts 

 

[Back to top] Antioxidant Properties of Nitric Oxide in Cellular Physiological and Pathophysiological Mechanisms. The Implications of Biological Balance between ·NO and Oxidative Stress

Lisa A. Ridnour, Douglas D. Thomas, Daniele Mancardi, Sonia Donzelli, Nazerrano Paolocci, Pasquale Pagliaro, Katrina M. Miranda, Murali Krishna, John Fukuto, Matthew B. Grisham, James B. Mitchell, Michael G. Espey and David A. Wink

 

The function of nitric oxide (·NO) in pathophysiology remains confounding as both protective and cytotoxic effects of ·NO have been demonstrated in many disease processes. Nitric oxide chemistry culminating in the generation of oxidative as well as itrosative intermediates have generally been proposed as mediators of pathophysiology and have overshadowed the antioxidant capabilities of ·NO. However, the counteracting role of ·NO in providing a balance under conditions of oxidative and nitrosative stress has been underappreciated. The purpose of this review is the discussion of the role of ·NO as an antioxidant and interceptor of more potent reactive intermediates in normal physiology and disease.

 

[Back to top] The Physiology of Nitric Oxide: Control and Consequences

Ingrid Fleming and Rudi Busse

 

Since its recognition as an endothelium-derived relaxing factor, the control and consequences of nitric oxide (NO) production has been investigated intensely. NO is not simply a vasodilator or regulator of smooth muscle tone but is a potent anti-platelet agent, neuromodulator and regulator of gene expression. This article reviews the mechanisms (intracellular Ca2+, phosphorylation and protein-protein interaction) that regulate the activity of each of the NO synthase isoforms and describes the physiology of NO in the circulation, kidney, skeletal muscle as well as in endocrine, immune and nervous systems.

 

[Back to top] Pathophysiological Roles of Nitric Oxide: In the Heart and the Coronary Vasculature

C. Dessy and O. Feron

 

Nitric oxide is a key player among the numerous mediators of endothelial homeostasis and cardiac contractility and is thereby involved in the pathogenic processes leading to vascular and myocardial dysfunctions. Although none of the current paradigms would elevate the influence of NO on cardiac contraction to the level of that of e.g., catecholamines or increased calcium, this unusual signaling molecule can modulate virtually all the regulatory steps of excitationcontraction coupling and influence the course of cardiac decompensation. Not only alterations in spatial confinement or post-translational modifications but also changes in the abundance of one of the three NOS isoforms may result in profound cellular disturbancies that participate in the endothelial and contractile dysfunctions leading to cardiovascular diseases.

 

[Back to top] Nitric Oxide and Inflammation

C.C. Wu

 

Nitric oxide (NO) is a very labile molecule of ubiquitous significance in biological systems in general. During the past two decades, NO has been recognized as one of the most versatile players in immune function. This diatomic molecule is normally produced by constitutive NO synthase and plays an important role in physiological regulation of nerve transmission and cardiovascular function. In contrast, an enormous and uncontrollable amount of NO, is synthesized by inducible NO synthase in activated immune cells during inflammation. Although the production of NO in inflammation has been described in numerous studies, the equivocal role for NO in vs. during an inflammatory response is not clearly defined. For example, when produced in excess, NO or its metabolites may not only be cytotoxic to host cells but also mediate local host defense mechanisms. As a result, NO has been nicknamed both “murderer” and “mediator”. This article reviews these two apparently opposing aspects of NO action during infection in the human system. This review deviates from post-1990 authoritative reviews in attempting to highlight important differences in the reaction of NO with oxygen or superoxide when fluxes of NO are dramatically enhanced reactions, which may predominate during active inflammation. This article proposes that in humans, the physiological chemistry of NO and its metabolites allow one to identify which of the many NO-dependent reactions contribute to the modulation of inflammatory response, and may help scientists in the design of new therapeutic agents for the treatment of inflammatory diseases.

 

[Back to top] The Role of Nitric Oxide in Autoimmune Diseases

Klaus-Dietrich Kroncke

 

Comprising multiple organ-specific to systemic disorders and symptoms, autoimmune diseases include type 1 diabetes, rheumatoid arthritis, multiple sclerosis, systemic lupus erythematosus, scleroderma, thyroiditis, and others. There are also implications of autoimmune pathology in common health problems such as arteriosclerosis, inflammatory bowel diseases, psoriasis, schizophrenia, and certain types of infertility. Protein expression of the inducible nitric oxide synthase (iNOS) has been found in the majority of the above mentioned human autoimmune diseases or in animal models of these diseases, mostly in inflammatory cell infiltrates like activated macrophages, but also in organ-specific epithelial cells or in parenchymal cells. The role of NO in inflammation is very complex. On the one hand, NO mediates important direct cytotoxic effects and on the other hand it modulates immunological functions, which in the setting of autoimmune diseases may be beneficial. Current knowledge regarding the role of iNOS-derived NO in various human autoimmune diseases as well as in the respective animals models is reviewed here.

 

[Back to top] Inhibitors of Nitrogen Oxide Species Production in Animal Models of Inflammation and Future Directions for Therapy in Inflammatory Disorders

Francois Feihl, Mauro Oddo, Bernard Waeber and Lucas Liaudet

 

Nitric oxide (NO) and inflammation interact at many levels. First, NO produced in low, physiological levels by vascular endothelial cells under the control of the constitutive endothelial nitric oxide synthase (eNOS) tends to inhibit endothelial-leucocyte interactions. Thus, pharmacologic interventions, which block eNOS are counterproductive in inflammatory diseases. Second, inflammation is characteristically associated with the stimulated expression of the inducible isoform of nitric oxide synthase (iNOS), leading to production of large amounts of NO for extended period of time in many cell types. These large amounts of NO potentially contribute to tissue damage through the generation of toxic reactive nitrogen species such as higher nitrogen oxides and peroxynitrite. Therefore, it could be of therapeutic value to selectively inhibit iNOS, while leaving intact the

activity of eNOS. In recent years, considerable progress has occurred in the molecular design of highly potent and highly selective inhibitors of iNOS. However, effects of these agents in specific disease conditions is not readily predictable, because the interactions of NO and inflammation are considerably more intricate than just indicated. For example, the activation of nuclear factor kappa B (NF-kB), an essential pathway for induction of an inflammatory cellular phenotype, may either by enhanced or inhibited by NO, depending on particular conditions. In addition, NO has a complex influence on the production of inflammatory prostanoids. NO is also a player in acquired immunity, for example by tilting the Th1/Th2 balance in favour of Th2 responses. Finally, NO is an important effector in the defense against at least some invading pathogens. Here we provide a detailed review of efforts made at characterizing the effects of disrupting the function of iNOS, by either genetic or pharmacologic means, in three classes of experimental paradigms: 1) models of arthritis, 2) models of inflammatory bowel disease, and 3) models of generalized inflammation induced by endotoxemia or bacterial sepsis. The accrued evidence in each of these cases suggests that the contribution of NO to pathophysiology of inflammatory diseases is highly heterogeneous, and therefore difficult to target therapeutically by the presently available means.

 

[Back to top]  Effect of Inhibitors of Nitric Oxide in Animal Models and Future Directions for Therapy in Inflammatory Disorders

Salvatore Cuzzocrea

 

The aim of the current article is to overview the recent developments in the field of inflammation, as it relates to the roles of nitric oxide (NO) and peroxynitrite in the pathogenesis of this condition. The first part of the review focuses on the roles of NO and peroxynitrite, a reactive oxidant produced from the reaction of NO and superoxide. The second part of the review deals with the novel findings related to the recently identified regulatory roles of the inducible isoform of nitric oxide synthase (iNOS) in the expression of pro-inflammatory mediators in inflammation. Reactive oxygen species can initiate a wide range of toxic oxidative reactions. These include initiation of lipid peroxidation, direct inhibition of mitochondrial respiratory chain enzymes, inactivation of glyceraldehyde-3phosphate dehydrogenase, inhibition of membrane sodium/potassium ATP-ase activity, inactivation of membrane sodium channels, and other oxidative modifications of proteins. All these toxicities are likely to play a role in the pathophysiology of inflammation. Reactive oxygen species (e.g., superoxide, peroxynitrite, hydroxyl radical and hydrogen peroxide) are all potential reactants capable of initiating DNA single strand breakage, with subsequent activation of the nuclear enzyme poly (ADP ribose) synthetase (PARS), leading to eventual severe energy depletion of the cells, and necrotic-type cell death. Recently , it has been demonstrated that iNOS inhibitor prevents the activation of poly (ADP ribose) synthetase, and prevents the organ injury associated with inflammation. Although the severity and duration of inflammation may dictate the timing and extent of NOS expression, it is now evident that the upregulation of NOS can take place during sustained inflammation. Pharmacological inhibition of iNOS or genetic inactivation of NOS (iNOS knockout mice) attenuates the activation of the transcription factors nuclear factor kappa B (NFKB) and Signal Transducer and Activator of Transcription 3 (STAT3), and ameliorates the increases in G-CSF messenger RNA levels in the tissue. Thus, induced nitric oxide, in addition to being a "final common mediator" of inflammation, is essential for the upregulation of the inflammatory response. Furthermore, a picture of a pathway is evolving that contributes to tissue damage both directly via the formation of peroxynitrite, with its associated toxicities, and indirectly through the amplification of the inflammatory response.

 

[Back to top]  The Use of Nitric Oxide Synthase Inhibitors in Inflammatory Diseases: A Novel Class of Anti-Inflammatory Agents

Bahar Tunētan and Sedat Altug

 

Nitric oxide (NO) is produced enzymatically in numerous tissues and considered as important mediator of many physiological and pathophysiological processes. NO is synthesized from L-arginine by three isoforms of the enzyme NO synthase (NOS). Among these three established isozymes of NOS, neuronal NOS (nNOS) and endothelial NOS (eNOS) are constitutive (cNOS) and low-output enzymes whose physiological functions are signal transduction. The third form of NOS, inducible NOS (iNOS), is constitutively expressed only in certain tissues and more typically synthesized in response to inflammatory or pro-inflammatory mediators. Although considerable evidences implicate the role of NO in the pathophysiology of inflammatory processes, there are contradictory reports in the literature concerning its role as an anti-inflammatory or pro-inflammatory agent. It is likely that NO from eNOS plays a role in the early stages of inflammation whereas NO from iNOS contributes to many aspects of chronic inflammation. Therefore, the use of selective iNOS inhibitors may be beneficial for the treatment of inflammatory processes. On the other hand, development of selective iNOS inhibitors will have to address potential problems related to inhibition of NO derived from cNOS in situations in which this mediator may be beneficial. In this review, contribution of NO to the pathophysiology of inflammatory conditions and clinical use of substrate-based NOS inhibitors, including arginine analogues and amidinecontaining inhibitors as potential anti-inflammatory agents in a variety of inflammatory diseases will be discussed.