STAT-3 inhibitory bisabolanes from carthamus glaucus

Orazio Taglialatela-Scafati, Federica Pollastro, Lavinia Cicione, Giuseppina Chianese, Maria Luz Bellido, Eduardo Munoz, Hasan Çetin Özen, Zuhal Toker, Giovanni Appendino

Risultato della ricerca: Contributo su rivistaArticolo in rivistapeer review

Abstract

Apart from a large amount (ca. 2.0%) of α-bisabolol β-d-fucopyranoside (2a), the aerial parts of the Mediterranean weed Carthamus glaucus afforded an unusual triglyceride (E-2-crotonyl-1,3- distearolylglycerol, 7), two lipophilic flavonoids (6a,b), and a series of bisabolane fucopyranosides variously acylated on the sugar moiety (2b-e) or oxidized on the terpenoid core (3, 4a,b, 5a,b). The fucopyranoside 2a is more soluble in polar media and more versatile in terms of formulation than its aglycone [(-)-α-bisabolol, 1], an anti-inflammatory cosmetic ingredient in current short supply in its natural form. A comparative investigation of the activity of α-bisabolol (1a), the fucopyranoside 2a, and its senecioate 2b on transcription factors involved in inflammation and cancer pathways (NF-κB and STAT-3) showed only marginal activity on NF-κB inhibition for all compounds, while STAT-3 was inhibited potently by the fucoside 2a and, to a lesser extent, also by α-bisabolol. These observations qualify 2a as an easily available compound, both as an apoptotic lead structure and as a potential alternative to natural α-bisabolol (1) for pharmaceutical and/or cosmetic development.

Lingua originaleInglese
pagine (da-a)453-458
Numero di pagine6
RivistaJournal of Natural Products
Volume75
Numero di pubblicazione3
DOI
Stato di pubblicazionePubblicato - 23 mar 2012

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