The anti-cancer property of the Vitamin K3 (Vitk3) was again recently studied by Dr Meng-Er Huang’s team (Curie Institute, CNRS UMR3348, Paris).
By using in vitro pro-oxydative cellular models, Dr Huang and collaborators observed a cancer-selective cytotoxicity of vitk3 in Peroxyredoxin 1 (PRDX1 aka PRX1)-deficient cancer cell lines.
To further investigate the underlying molecular mechanisms, the authors used a stably PRX1-depleted HeLa cell line (PRX1-) (vs. Control (PRX1+)) under various experimental conditions. They notably treated PRX1- and PRX1+ cell lines by vitk3 and 6 other known anticancer molecules targeting different cellular events (microtubule (vinblastine & taxol); DNA (doxorubicin & daunorubicin); DNA transcription (actinomycin D) and cell cycle (5-FU)).
Montelukast is a marketed drug used for asthma treatment and to relieve symptoms of seasonal allergies. It is known to function as a leukotriene receptor antagonist.
In a recent study in which young and old rats were treated with Montelukast, Maschallinger et al. (1) could show that the drug reduces neuroinflammation, elevates hippocampal neurogenesis and improves learning and memory in old animals. They could further demonstrate that some of these findings are mediated through an inhibitory effect on the GPR17 receptor.
GPR17 is an orphan G-protein-coupled receptor that is abundant in the CNS, and has been shown to play a key role in regulating oligodendrocyte differentiation and maturation although little has been known about the exact mechanism through which GPR17 influences myelination (2).
The most important result of their study is that cognitive function of old animals could be restored by the treatment with Montelukast. This could be shown in two different behavioral tests. While young rats have not been affected by the drug treatment, Montelukast significantly improved task learning in 20-month old rats. Non-cognitive behaviours such as anxiety-like behaviour, depression-like symptoms, exploration and locomotion as well as changes in body weight have not been affected by Montelukast treatment. Furthermore the authors found that Montelukast reduced microglia reactivity and restored hippocampal neurogenesis in old rats.
These findings might open the door for new potential pharmaceutic applications for Montelukast in treating dementia.
Focus Biomolecules recently released Montelukast to facilitate GPR17 related research activities. Focus Biomolecules also offer 2 more GPR17 modulators through tebu-bio.
oligodendrocytes and facilitates further study of this important process.
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(1) J. Maschallinger et al., Structural and functional rejuvenation of the aged brain by an approved anti-asthmatic drug, Nat Commun. 6, 8466 (2015)
(2) S. Hennen et al.,Decoding signaling and function of the orphan G protein-coupled receptor GPR17 with a small-molecule agonist, Sci Signal. 6, 298 (2013)
Microbial metabolites are a source of unequalled elements for in vitro assays. Sometimes neglected, these active molecules naturally provide a large spectrum of structural diversity for Drug discovery and antibiotics development programs. In this post, 6 metabolites and their respective properties are highlighted with the hope of refreshing our minds, a little bit, of the importance of such molecules in innovative research discovery.