250
secretion and cyclic AMP level, plays a role in smooth-muscle relaxation and vasodilation and is the prime inducer of peptic ulcer. H3R possesses central nervous
system regulatory potential and H4R has a role in asthma and allergic reactions. The
two important histamine receptors of pharmacological significance are HR1 and
HR2. H1R–histamine complex provokes type 1 hypersensitive conditions like rhinitis and asthma. Antihistamines are the best medicines suggested for allergic rhinitis.
These drugs act by binding to the histamine receptors on target cells and thus prevent the binding of histamine. The H1 receptors could be blocked by the classical
antihistamines and the H2 receptors by a newer class of antihistamines.
10.4.3 Leukotriene in Pathogenesis
The undesirable production and activation of leukotrienes LTB4 and CysLTs have
been implicated in a wide variety of inflammatory disorders. CysLTs are more frequently implicated in the pathogenesis of asthma and allergic rhinitis (Hedqvist
et al. 1985). Macrophages are the major source of LTB4. The accumulation of macrophages at atherosclerotic sites is a classic hallmark of this condition, thus accelerating LTB4 production and proinflammatory activities in cardiovascular diseases.
10.4.4 Cytokines in Pathogenesis
Plasma levels of various cytokines are found to be elevated in a number of inflammatory and autoimmune disorders. Thus they are best exploited for diagnostic and
prognosis assessment of many diseases, including RA. TNF-α production is found
altered in obese individuals; as a result macrophage population in adipose tissue
would be increased. Moreover, the development of many chronic inflammatory diseases is associated with the increased production of proinflammatory cytokines.
Proinflammatory cytokines such as TNF-α impair insulin action and contribute
directly to insulin resistance, and IL-6 regulates insulin sensitivity. Elevation of
IL-1β, IL-6, IL-8, and TNF-α have been found in patients with uncontrolled diabetes. Altered levels of TNF-α and IL-6 have been associated with arthritic diseases
such as gouty, rheumatoid, and psoriatic arthritis. Elevated levels of proinflammatory cytokines cause osteoporosis. Adverse effects of cytokines have been linked to
many disease conditions ranging from depression to cancer.
10.5 Anti-inflammatory Agents Modulating Immune
Response
The purpose of inflammation is to protect the body from harmful invaders and
stressful endogenous and exogenous signals via mediators of the immune system.
Inhibiting major clinically relevant inflammatory targets like cytokine, leukotriene,
and complements may reduce or augment immune response depending on their
B.C. Bhavya and M. Haridas
secretion and cyclic AMP level, plays a role in smooth-muscle relaxation and vasodilation and is the prime inducer of peptic ulcer. H3R possesses central nervous
system regulatory potential and H4R has a role in asthma and allergic reactions. The
two important histamine receptors of pharmacological significance are HR1 and
HR2. H1R–histamine complex provokes type 1 hypersensitive conditions like rhinitis and asthma. Antihistamines are the best medicines suggested for allergic rhinitis.
These drugs act by binding to the histamine receptors on target cells and thus prevent the binding of histamine. The H1 receptors could be blocked by the classical
antihistamines and the H2 receptors by a newer class of antihistamines.
10.4.3 Leukotriene in Pathogenesis
The undesirable production and activation of leukotrienes LTB4 and CysLTs have
been implicated in a wide variety of inflammatory disorders. CysLTs are more frequently implicated in the pathogenesis of asthma and allergic rhinitis (Hedqvist
et al. 1985). Macrophages are the major source of LTB4. The accumulation of macrophages at atherosclerotic sites is a classic hallmark of this condition, thus accelerating LTB4 production and proinflammatory activities in cardiovascular diseases.
10.4.4 Cytokines in Pathogenesis
Plasma levels of various cytokines are found to be elevated in a number of inflammatory and autoimmune disorders. Thus they are best exploited for diagnostic and
prognosis assessment of many diseases, including RA. TNF-α production is found
altered in obese individuals; as a result macrophage population in adipose tissue
would be increased. Moreover, the development of many chronic inflammatory diseases is associated with the increased production of proinflammatory cytokines.
Proinflammatory cytokines such as TNF-α impair insulin action and contribute
directly to insulin resistance, and IL-6 regulates insulin sensitivity. Elevation of
IL-1β, IL-6, IL-8, and TNF-α have been found in patients with uncontrolled diabetes. Altered levels of TNF-α and IL-6 have been associated with arthritic diseases
such as gouty, rheumatoid, and psoriatic arthritis. Elevated levels of proinflammatory cytokines cause osteoporosis. Adverse effects of cytokines have been linked to
many disease conditions ranging from depression to cancer.
10.5 Anti-inflammatory Agents Modulating Immune
Response
The purpose of inflammation is to protect the body from harmful invaders and
stressful endogenous and exogenous signals via mediators of the immune system.
Inhibiting major clinically relevant inflammatory targets like cytokine, leukotriene,
and complements may reduce or augment immune response depending on their
B.C. Bhavya and M. Haridas