Pauferrol A, a novel chalcone trimer with a cyclobutane ring from Caesalpinia ferrea mart exhibiting DNA topoisomerase II inhibition and apoptosis-inducing activity

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• 作者：Hiroshi Nozaki ; Ken-ichiro Hayashi ; Masahiro Kido ; Kazuyuki Kakumoto ; Shogo Ikeda ; Nobuyasu Matsuura ; Hiroyuki Tani ; Daisuke Takaoka ; Munekazu Iinuma ; Yukihiro Akao
• 关键词：Caesalpinia ferrea ; Leguminosae ; Chalcone ; Topoisomerase ; Pauferrol A ; Inhibitor ; Apoptosis
• 刊名：Tetrahedron Letters
• 出版年：2007
• 期刊代码：109_00404039
• 类别：ch
• 出版时间：19 November 2007
• 卷：48
• 期：47
• 页码：8290-8292
• 文件大小：119 K

摘要

Pauferrol A (1), a unique chalcone derivative was isolated from the stems of Caesalpinia ferrea Mart, and the structure was determined on the basis of 2D-NMR spectroscopy to be a chalcone trimer fused by a cyclobutane ring. This new chalcone trimer showed potent inhibitory activity against human topoisomerase II, with an IC₅₀ value of 2.1 μM, and cell proliferation inhibitory activity through the induction of apoptosis in human leukemia HL60 cells, with an IC₅₀ value of 5.2 μM. To our knowledge, this is the first report of the isolation and structure of this chalcone trimer and its biological activity.