STAT-3 Inhibitory Bisabolanes from Carthamus glaucus
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- 作者：Orazio Taglialatela-Scafati ; Federica Pollastro ; Lavinia Cicione ; Giuseppina Chianese ; Maria Luz Bellido ; Eduardo Munoz ; Hasan 脟etin 脰zen ; Zuhal Toker ; Giovanni Appendino
- 刊名：Journal of Natural Products
- 出版年：2012
- 出版时间：March 23, 2012
- 年：2012
- 卷：75
- 期：3
- 页码：453-458
- 全文大小：243K
- 年卷期：v.75,no.3(March 23, 2012)
- ISSN：1520-6025
文摘
Apart from a large amount (ca. 2.0%) of 伪-bisabolol 尾-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鈥?b>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 [(鈭?-伪-bisabolol, 1], an anti-inflammatory cosmetic ingredient in current short supply in its natural form. A comparative investigation of the activity of 伪-bisabolol (1a), the fucopyranoside 2a, and its senecioate 2b on transcription factors involved in inflammation and cancer pathways (NF-魏B and STAT-3) showed only marginal activity on NF-魏B inhibition for all compounds, while STAT-3 was inhibited potently by the fucoside 2a and, to a lesser extent, also by 伪-bisabolol. These observations qualify 2a as an easily available compound, both as an apoptotic lead structure and as a potential alternative to natural 伪-bisabolol (1) for pharmaceutical and/or cosmetic development.