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Leukotrienes

  • These three groups are collectively called eicosanoids, derived from arachidonic acid via the cyclooxygenase (COX) or lipoxygenase pathways.

  • Leukotrienes are eicosanoids derived from arachidonic acid via the lipoxygenase (LOX) pathway.

  • They are primarily involved in immune and inflammatory responses.

Major Leukotrienes:

LTB4 (Leukotriene B4):

  • Functions: Acts as a potent chemotactic agent, attracting neutrophils to sites of inflammation.

LTC4, LTD4, LTE4 (Cysteinyl Leukotrienes):

  • Functions: Induce bronchoconstriction, increase vascular permeability, and contribute to inflammatory responses.

Synthesis:

  • Immune Cells Activation: Upon stimulation, cells like mast cells, eosinophils, and macrophages release arachidonic acid.

  • LOX Pathway: 5-LOX converts arachidonic acid into leukotriene A4 (LTA4), which is further transformed into LTB4 or conjugated with glutathione to form LTC4, LTD4, and LTE4.

Arachidonic acid → (5-lipoxygenase) → Leukotriene A4 → LTB4, LTC4, LTD4, LTE4.





Synthesis of Leukotrienes
Synthesis of Leukotrienes

Physiological and Pathological Roles:

  • Asthma and Allergies: Cysteinyl leukotrienes mediate bronchoconstriction and increased mucus production.

  • Inflammation: LTB4 recruits and activates leukocytes, amplifying the inflammatory response.

  • Autoimmune Diseases: Involved in the pathogenesis of conditions like rheumatoid arthritis.

Pharmacological Effects:

  • Bronchoconstriction: Cause tightening of airway muscles, contributing to asthma and allergic reactions.

  • Increased Vascular Permeability: Promote leakage of fluids into tissues, leading to edema.

  • Chemotaxis: Attract immune cells like neutrophils to sites of inflammation.

  • Mucus Secretion: Stimulate mucus production in the respiratory tract.

  • Pain Sensitization: Enhance pain perception during inflammatory responses.

Drug targets:

  • 5-lipoxygenase inhibitor: Zileuton (used in asthma).

  • Leukotriene receptor antagonists: Montelukast, Zafirlukast (for asthma prophylaxis).


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