Anti-inflammatory sesquiterpene lactones from Onopordum illyricum L. (Asteraceae), an Italian medicinal plant

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• 作者：Carmen Formisano^a ; Cinzia Sanna^b ; Mauro Ballero^b ; Giuseppina Chianese^a ; Carmina Sirignano^a ; Daniela Rigano^a ; ^{drigano@unina.it} ; Estrella Millá ; n^c ; Eduardo Muñ ; oz^c ; Orazio Taglialatela-Scafati^a
• 关键词：Onopordum illyricum ; Sesquiterpenes ; Anti-inflammatory ; Cysteamine assay
• 刊名：Fitoterapia
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：116
• 期：Complete
• 页码：61-65
• 全文大小：414 K
• 卷排序：116

文摘

Onopordum illyricum L. is a medicinal plant used in the Mediterranean area as antipyretic for the treatment of respiratory and urinary inflammations and to treat skin ulcers. Repeated chromatographic purification of O. illyricum aerial parts led to the isolation of six known sesquiterpenes, which were evaluated for the inhibition of the pro-inflammatory transcription factors NF-κB and STAT3 and for the activation of the transcription factor Nrf2, which regulates the cellular antioxidant response. Structure–activity relationships were interpreted by the NMR-based cysteamine assay. The sesquiterpene lactone vernomelitensin significantly inhibited NF-κB and STAT3, showing also a significant Nrf2 activation. Accordingly, the cysteamine assay selected vernomelitensin as the most reactive of the isolated sesquiterpenes, identifying the α,β-unsaturated aldehyde moiety as responsible for the higher (re)activity.