Target intelligence / Profile preview

8-iso-prostaglandin F2α (8-isoprostane) (8-iso-PGF2α)

Target
8-iso-PGF2α
Molecular classification
Lipid, Eicosanoid, Isoprostane, Fatty acyl
01

Overview

8-iso-prostaglandin F2α, commonly known as 8-isoprostane, is a bioactive eicosanoid and a member of the isoprostane family produced by the non-enzymatic, free radical-catalyzed peroxidation of arachidonic acid [1, 3]. It is widely regarded as the 'gold standard' biomarker for assessing systemic oxidative stress and lipid peroxidation in humans due to its chemical stability and presence in biological fluids like plasma and urine [2, 13]. Unlike traditional prostaglandins synthesized by cyclooxygenase enzymes, 8-isoprostane is formed in situ within membrane phospholipids and subsequently released, serving as a reliable indicator of in vivo oxidative damage [3, 10]. Biologically, it acts as a potent vasoconstrictor in renal and pulmonary vascular beds and a bronchoconstrictor, primarily through the activation of the thromboxane A2 (TP) receptor [4, 5, 8]. Elevated levels are strongly associated with various pathological conditions characterized by oxidative stress, including cardiovascular disease, diabetes, and preeclampsia [10, 13]. While it is primarily utilized as a biomarker in clinical research to monitor the efficacy of antioxidant therapies, its physiological effects can be mitigated by TP receptor antagonists [2, 5].

Other names
8-isoprostane8-iso-prostaglandin F2α8-epi-PGF2α15-F2t-isoprostaneiPF2α-III8-epi-prostaglandin F2α8-F(2t)-isoprostane
02

Mechanism of action

8-isoprostane acts as an agonist of the Thromboxane A2 (TP) receptor, triggering G-protein coupled signaling pathways that induce smooth muscle contraction in vascular and bronchial tissues [5, 8]. It also stimulates pro-inflammatory signaling in macrophages, including the induction of IL-8 via MAPK activation [12].

03

Biological functions

VasoconstrictionBronchoconstrictionPlatelet aggregation modulationPro-inflammatory signaling
04

Disease associations

Cardiovascular diseaseInflammationDiabetes mellitusNeurodegenerative diseasePreeclampsiaAsthmaChronic obstructive pulmonary disease
05

Safety considerations

Non-specific elevation across diverse inflammatory and oxidative statesPotential interference with homeostatic thromboxane signaling when using receptor antagonistsBiological effects may promote thrombosis and endothelial dysfunction
06

Interacting drugs

Seratrodast

4 more in the full profile.

07

Biomarkers

Urinary 8-iso-prostaglandin F2αPlasma 8-iso-prostaglandin F2α

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