The invention refers to novel tocotrienol derivatives that specifically inhibit 5-lipoxygenase (5-LOX) activity and leukotrienes synthesis. Leukotrienes promote inflammation. Novel tocotrienol derivatives strongly inhibit 5-LOX activity at very low concentrations (nanomolar levels) thus preventing leukotrienes synthesis and inflammation.
A screening step has revealed many secondary metabolites isolated from Garcinia amplexicaulis and Garcinia kola as potential anti-inflammatory agents. In vitro tests highlighted 2 hits : garcinoïc acid and α-amplexichromanol. As a consequence, additional tests were realized on an atopic dermatitis Reconstructed Human Epidermis model (RHE) by SYNELVIA in Toulouse : α-amplexichromanol proved to prevent atopic dermatitis. Its anti-inflammatory activity is close to that of dexamethasone, a strong dermocorticoid with huge side-effects.
Reactive/sensitive skin and atopic dermatitis are major hurdles in the field of dermo-cosmetology and represent huge markets. Many companies are looking for innovative technologies and natural ingredients to prevent skin inflammation. Tocotrienol derivatives proved to be efficient molecules targeting inflammation. RHE in vitro tests confirmed their ability to prevent inflammation and atopic dermatitis. Moreover raw materials sourcing are clearly identified and processes are easy to scale-up.
No toxicity below 50 µm (RHE model)
SYNELVIA’s objectivization report : “effective for the treatment of atopic dermatitis” (details available on demand), anti-inflammatory activity close to that of dexamethasone, a strong dermocorticoid with huge side-effects
Dermo-cosmetic applications : skin inflammation and atopic dermatitis
Stade de développement
Laboratoire de recherche
EA 921 - SONAS
Équipe de recherche
SUBSTANCES D'ORIGINALE NATURELLE ET ANALOGUES STRUCTURAUX
Propriété intellectuelle associée
EP : EP15182827 - filed on the 08-27-2015
WO - CA,CN,EP,JP,US