一种来自绒毛瓜馥木的抗有丝分裂和细胞毒性查耳酮。

An antimitotic and cytotoxic chalcone from Fissistigma lanuginosum.

作者信息

Alias Y, Awang K, Hadi A H, Thoison O, Sévenet T, Païs M

机构信息

Department of Chemistry, University of Malaya, Kuala Lumpur.

出版信息

J Nat Prod. 1995 Aug;58(8):1160-6. doi: 10.1021/np50122a002.

DOI:10.1021/np50122a002

PMID:7595585

Abstract

Bioassay-guided fractionation of an ethyl acetate extract of Fissistigma lanuginosum led to the isolation of the known chalcone pedicin [1], which inhibited tubulin assembly into microtubules (IC50 value of 300 microM). From the same EtOAc fraction, two new condensed chalcones, fissistin [2] and isofissistin [3], which showed cytotoxicity against KB cells, were also obtained, together with the inactive dihydropedicin [4] and 6,7-dimethoxy-5,8-dihydroxyflavone [5]. In addition, the aminoquinones 6, 8, and 9 were isolated from the alkaloid extract. These compounds were artifacts, prepared by treatment of 1, 4, and 2, respectively, with NH4OH. The structures of the new compounds were elucidated by spectral methods, especially 2D nmr.

摘要

对毛叶瓜馥木乙酸乙酯提取物进行生物测定导向的分级分离，得到了已知的查耳酮pedicin [1]，它能抑制微管蛋白组装成微管（IC50值为300 microM）。从同一乙酸乙酯级分中，还获得了两种对KB细胞具有细胞毒性的新缩合查耳酮，即瓜馥木素[2]和异瓜馥木素[3]，以及无活性的二氢pedicin [4]和6,7-二甲氧基-5,8-二羟基黄酮[5]。此外，从生物碱提取物中分离出了氨基醌6、8和9。这些化合物是分别用NH4OH处理1、4和2制备的人工产物。通过光谱方法，特别是二维核磁共振，阐明了新化合物的结构。