Steroids with anti-inflammatory activity from Vernonia nigritiana Oliv. & Hiern.

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• 作者：Antonio Vassallo ; Nunziatina De Tommasi ; Irmgard Merfort ; Rokia Sanogo ; Lorella Severino ; Marco Pelin ; Roberto Della Loggia ; Aurelia Tubaro ; Silvio Sosa
• 关键词：Vernonia nigritiana ; Asteraceae ; Anti-inflammatory activity ; Croton oil ear test ; NF-魏B ; Steroids
• 刊名：Phytochemistry
• 出版年：December, 2013
• 年：2013
• 卷：96
• 期：Complete
• 页码：288-298
• 全文大小：745 K

文摘

The leaves of Vernonia nigritiana Oliv. & Hiern. (Asteraceae) were investigated for their in vivo topical anti-inflammatory properties, following a bioassay-oriented fractionation approach. Petroleum ether, chloroform and chloroform-methanol extracts inhibited the Croton oil-induced ear dermatitis in mice. The chloroform extract was only about half as active as the non steroidal anti-inflammatory drug indomethacin (ID₅₀ = 237 and 93 渭g/cm², respectively). Phytochemical investigation of this extract led to the isolation of nine polyhydroxylated stigmasterol glycosides and six polyhydroxylated stigmasterols. Their structures were elucidated by NMR, MS and chemical methods. Each compound exerted a significant anti-oedema activity, the most active being class="boldFont">1 (3尾-O-尾-d-glucopyranosyloxy-5伪-stigmasta-7,9(11),24(28)Z-triene-6尾,16尾,26,29-tetrol) and class="boldFont">3 (3尾-O-尾-d-glucopyranosyloxy-5伪-stigmasta-7,9(11),24(28)Z-triene-6尾,16尾,29-triolclass="boldFont">), only two and five fold less potent than the steroidal drug hydrocortisone (ID₅₀ = 0.10, 0.21 and 0.04 渭mol/cm², respectively). Compound class="boldFont">1 (50 渭M) also completely inhibited the transcription factor NF-魏B in vitro.