Eicosanoids are a diverse group of bioactive lipid compounds that play crucial roles in various physiological and pathological processes in the human body. Derived from polyunsaturated fatty acids (PUFAs), particularly arachidonic acid, eicosanoids serve as potent signaling molecules, exerting their effects through specific receptors.
Structure and Classification of Eicosanoids
Eicosanoids are characterized by their twenty-carbon backbone. They can broadly be classified into three major subclasses based on their structural features, namely prostaglandins, leukotrienes, and thromboxanes.
- Prostaglandins. Prostaglandins are short-lived, cyclic fatty acids with a five-carbon ring. They possess a diverse range of biological activities and are involved in numerous physiological processes such as inflammation, vasodilation, and blood clotting regulation. Prostaglandins are denoted by the prefix "PG", followed by a letter indicating their specific type (e.g., PGD2, PGE2).
- Leukotrienes. Leukotrienes are linear eicosanoids characterized by three conjugated double bonds. They are primarily involved in immune responses and inflammation, particularly in allergic reactions and asthma. Leukotrienes are denoted by the prefix "LT" followed by a number (e.g., LTB4, LTC4).
- Thromboxanes. Thromboxanes are cyclic eicosanoids that play a crucial role in platelet aggregation and vasoconstriction. They are primarily synthesized by platelets and have potent effects on blood clotting and vascular tone regulation. Thromboxanes are denoted by the prefix "TX" followed by a number (e.g., TXA2, TXB2).
- Eicosanoids affect cell surface. These receptors are widely distributed throughout the body, allowing eicosanoids to modulate various physiological processes. Eicosanoids have highly diverse and context-dependent effects. The key functions of eicosanoids in different biological systems are listed below.
- The inflammatory response. Eicosanoids, particularly prostaglandins and leukotrienes, play a pivotal role in the inflammatory response. Inflammation is a complex biological process that protects the body's defense mechanism against infection and injury. Eicosanoids are synthesized and released by immune cells, such as macrophages and mast cells, in response to inflammatory stimuli. Prostaglandins promote vasodilation, edema, and recruitment of immune cells to the site of inflammation, while leukotrienes enhance vascular permeability and leukocyte chemotaxis.
- Vascular regulation. Eicosanoids also regulate vascular tone and blood flow. Prostaglandins, such as prostacyclin (PGI2), promote vasodilation and inhibit platelet aggregation, maintaining vascular homeostasis. On the other hand, thromboxane A2 (TXA2) induces vasoconstriction and platelet aggregation, contributing to hemostasis and thrombosis. Imbalances in eicosanoids production can lead to cardiovascular disorders.
- The respiratory system. Leukotrienes, particularly leukotriene B4 (LTB4) and cysteinyl leukotrienes (LTC4, LTD4, LTE4), are implicated in various respiratory conditions, including asthma and allergic rhinitis. These eicosanoids promote bronchoconstriction, mucus secretion, and recruitment of inflammatory cells in the airways. Targeting leukotriene synthesis or receptors has proven to be an effective therapeutic strategy for managing respiratory disorders.
- Reproductive system. Eicosanoids have critical roles in reproductive physiology and pathology. Prostaglandins regulate various aspects of female sexual function, including ovulation, fertilization, implantation, and labor. For instance, prostaglandin E2 (PGE2) promotes cervical ripening and uterine contractions during labor. Additionally, eicosanoids are involved in male reproductive processes such as spermatogenesis and ejaculation.
Schematics of the eicosanoids synthesis pathway (Mendoza SR, et al., 2021)
Applications of Eicosanoids
Eicosanoids' diverse functions have paved the way for their application in various fields, including medicine, pharmacology, and research. Understanding the significance of eicosanoids has led to the development of drugs targeting their synthesis or receptors, offering therapeutic options for numerous diseases.
- Anti-inflammatory drugs. Nonsteroidal anti-inflammatory drugs (NSAIDs), such as aspirin and ibuprofen, inhibit the enzyme cyclooxygenase (COX). COX converts arachidonic acid into prostaglandins. By blocking prostaglandin synthesis, NSAIDs alleviate pain, reduce inflammation, and lower fever. However, long-term NSAID use can lead to adverse effects, highlighting the need for targeted therapies.
- Antiplatelet agents. Platelet aggregation plays a central role in thrombus formation and cardiovascular events. Drugs such as aspirin inhibit COX-1, thereby preventing the synthesis of thromboxane A2 (TXA2). Inhibition of TXA2 synthesis reduces platelet aggregation and minimizes clot risk.
- Respiratory therapeutics. The development of leukotriene modifiers, including leukotriene receptor antagonists and 5-lipoxygenase inhibitors, has revolutionized asthma and allergic rhinitis management. These medications target leukotriene synthesis or receptors, attenuating their effects and improving respiratory symptoms.
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Based on the importance of eicosanoid research, we provide services for eicosanoid analysis. We use highly sensitive LC-MS/MS methods for rapid identification and quantification of eicosanoids in different sample types, which greatly meet the needs of eicosanoid research.
- Mendoza SR, et al. "Complex and Controversial Roles of Eicosanoids in Fungal Pathogenesis." Journal of Fungi. 2021; 7(4):254.
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