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从弯曲矢车菊地上部分分离得到的阿盖林B和一种新的罕见去甲愈创木烷型内酯的抗增殖活性。

Anti-proliferative activity of aguerin B and a new rare nor-guaianolide lactone isolated from the aerial parts of Centaurea deflexa.

作者信息

Chicca Andrea, Tebano Marianna, Adinolfi Barbara, Ertugrul Kuddisi, Flamini Guido, Nieri Paola

机构信息

Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, via Bonanno 6, 56126 Pisa, Italy.

出版信息

Eur J Med Chem. 2011 Jul;46(7):3066-70. doi: 10.1016/j.ejmech.2011.03.011. Epub 2011 Mar 15.

Abstract

The phytochemical investigation of the aerial parts of Centaurea deflexa led to the identification of 21 compounds, among which three phenolic acids, one sterol, ten flavonoids, one phenylpropanoid derivative, two lignans and four sesquiterpene lactones. One of the latter compounds was a new, rare active principle (1) having an uncommon 15-nor-guaianolide skeleton. The biological investigation was carried out through a bio-guided assay fractionation of C. deflexa extracts and highlighted an anti-proliferative activity of two sesquiterpene lactones, aguerin B and the newly identified 15-nor-guaianolide (1) against human pancreatic and colonic cancer cells. Of the two compounds, only aguerin B showed to induce apoptotic cell death, confirming the role as pro-apoptotic moiety of the α-methylene-γ-lactone ring present in aguerin B but not in 1.

摘要

对弯曲矢车菊地上部分进行的植物化学研究,鉴定出了21种化合物,其中包括三种酚酸、一种甾醇、十种黄酮类化合物、一种苯丙素衍生物、两种木脂素和四种倍半萜内酯。后一类化合物中的一种是一种新的、罕见的活性成分(1),具有不常见的15-去甲愈创木烷型内酯骨架。通过对弯曲矢车菊提取物进行生物导向的分析分离来开展生物学研究,结果突出显示了两种倍半萜内酯,即阿盖林B和新鉴定出的15-去甲愈创木烷型内酯(1)对人胰腺癌细胞和结肠癌细胞具有抗增殖活性。在这两种化合物中,只有阿盖林B显示出能诱导凋亡性细胞死亡,这证实了阿盖林B中存在但1中不存在的α-亚甲基-γ-内酯环作为促凋亡部分的作用。

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