New sesquiterpene lactones, vernonilides A and B, from the seeds of Vernonia anthelmintica in Uyghur and their antiproliferative activities

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• 作者：Takuya Ito^a ; ^{itot@inm.u-toyama.ac.jp" class="auth_mail" title="E-mail the corresponding author} ; Simayijiang Aimaiti^a ; Nwet Nwet Win^a ; ^b ; Takeshi Kodama^a ; Hiroyuki Morita^a ; ^{hmorita@inm.u-toyama.ac.jp" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Vernonia anthelmintica ; Sesquiterpene lactones ; Antiproliferative activity
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 August 2016
• 年：2016
• 卷：26
• 期：15
• 页码：3608-3611
• 全文大小：498 K

文摘

A new guaianolide sesquiterpene lactone, vernonilide A (1), and a new elemanolide sesquiterpene lactone, vernonilide B (2), were isolated from the seeds of Vernonia anthelmintica, together with three known elemanolide sesquiterpene lactones (3–5). The structures of the isolated compounds were elucidated on the basis of physicochemical evidences. Compounds 1, 3, and 4 showed strong antiproliferative activities against three human cancer cell lines (A549, HeLa, and MDA-MB-231), with IC₅₀ values ranging from 0.10 to 1.00 μM. In addition, 5 exhibited significant antiproliferative activities against HeLa and MDA-MB-231 cells, with IC₅₀ values ranging from 1.90 to 2.20 μM. The antiproliferative activities of the acetyl derivatives 6 and 7 prepared from 4 and 3, respectively, against the three cell lines were 4–10-fold weaker than the original activities.