Prostaglandin f2alpha

Prostaglandins, PGs, are almost ubiquitously present in the organism and are characterized by a broad pharmacological spectrum of activity. Prostaglandins belong to the eicosanoids and act as so-called tissue hormones. They are normally not stored in the various organs and cells, but are newly synthesized and released in response to various stimuli.

Substrates of the biosynthesis of prostaglandins are polyunsaturated C20 fatty acids like arachidonic acid. The C20 fatty acids and their derivatives are also called eicosanoids (Greek "eicosi" = 20). .

The arachidonic acid is present in the cells mostly in esterified form in the membrane phospholipids. The concentration of free (cytosolic) arachidonic acid is very low. Only free arachidonic acid can serve as a substrate for cyclooxygenase or lipoxygenases. Thus, the eicosanoid biosynthesis primarily depends on the release of the C20 fatty acids from the membrane phospholipids. This is done, for example, by the activity of the membrane-bound phosopholipase A2 or phosopholipase C. The activation of the eicosanoid biosynthesis takes place by chemical, physiological, pathophysiological and pharmacological stimuli.

Prostaglandins have a broad physiological and pathophysiological spectrum of activity. They unfold their effectiveness via prostaglandin receptors. Prostaglandin receptors belong to the group of G-protein coupled membrane receptors.

Prostaglandin F2alpha (PGF2alpha) is an inflammatory arachidonic acid derivative with multiple effects.

The corpus luteum produces and secretes growth factors (fibroblast growth factor, vascular endothelial growth factor (VEGF) and the insulin-like growth factor), vasoactive factors (NO, angiotensin II and endothelin-1), steroids (progesterone), oxytocin and prostaglandins (PGF2alpha and PGE2) which are important for the development and regression of the corpus luteum to the corpus albicans.

PGF2alpha is produced by stimulation with oxytocin in utero. The PGF2alpha isoform 8-iso-PGF2alpha is significantly increased in patients with endometriosis.

The prostanoids PGF2alpha and PGF2alpha analogues such as Latanoprost, Travoprost, Bimatoprost and Tafluprost are "first-line" drugs in glaucoma and are effective in reducing ocular pressure.

In several studies, correlations between the activity of PGF2alpha and the development of cardiovascular disease were found. Helmersson-Karl et al.(2014) were able to demonstrate the association between elevated levels of inflammatory PGF2alpha and cardiovascular mortality in a 10-year study.

Several clinical studies concern the use of prostaglandin F2alpha in various diseases. forms of alopecia.

1. Choi YM et al (2015) Promising alternative clinical uses of prostaglandin F2α analogues: beyond the eyelashes. J Am Acad Dermatol 72:712-716.
2. Dams I et al. (2013)Therapeutic uses of prostaglandin F(2α) analogues in ocular disease and novel synthetic strategies. Prostaglandins Other Lipid Mediat 104-105:109-121.
3. Helmersson-Karlqvist J et al (2015) Prostaglandin F2α formation is associated with mortality in a Swedish community-based cohort of older males. Eur Heart J 36:238-243.
4. Miyamoto A et al (2010) Regulation of corpus luteum development and maintenance: specific roles of angiogenesis and action of prostaglandin F2alpha. Soc Reprod Fertil Suppl. 67:289-304.