Mezencev R, Mojzis J, Pilatova M, Kutschy P
United Nations Monitoring, Verification and Inspection Commission, Room S-3027K, New York, NY 10017 USA.
Neoplasma. 2003;50(4):239-45.
Phytoalexins are produced by plants after exposure to physical, biological or chemical stress and a specific group of these metabolites represent indole phytoalexins produced by important plants of the family Cruciferae. With respect to the epidemiologically proven cancer chemopreventive properties of brassica vegetables, antiproliferative and anticarcinogenic activities of indole phytoalexins have been studied. Several indole phytoalexins (i.e. brassinin, spirobrassinin, brassilexin, camalexin, 1-methoxyspirobrassinin, 1-methoxyspirobrassinol and methoxyspirobrassinol methyl ether) have been found to possess significant antiproliferative activity against various cancer cells and this activity is supposed to be associated with the modulation of activity of transcription factors regulating cell cycle, differentiation and apoptosis. Indole phytoalexins (i.e. cyclobrassinin, spirobrassinin, brassinin) also exhibited cancer chemopreventive activity in models of mammary and skin carcinogenesis. Understanding the molecular and cellular mechanism of action of such drugs and their structure-activity relationships is necessary for development new derivatives with more favourable profile of antiproliferative and chemopreventive activities.
植物抗毒素是植物在受到物理、生物或化学胁迫后产生的，其中一类特定的代谢产物是十字花科重要植物产生的吲哚类植物抗毒素。鉴于芸苔属蔬菜在流行病学上已被证实具有癌症化学预防特性，人们对吲哚类植物抗毒素的抗增殖和抗癌活性进行了研究。已发现几种吲哚类植物抗毒素（即芸苔宁、螺旋芸苔宁、芸苔毒素、camalexin、1-甲氧基螺旋芸苔宁、1-甲氧基螺旋芸苔醇和甲氧基螺旋芸苔醇甲醚）对各种癌细胞具有显著的抗增殖活性，并且这种活性被认为与调节细胞周期、分化和凋亡的转录因子活性的调节有关。吲哚类植物抗毒素（即环芸苔宁、螺旋芸苔宁、芸苔宁）在乳腺癌和皮肤癌发生模型中也表现出癌症化学预防活性。了解此类药物的分子和细胞作用机制及其构效关系对于开发具有更有利抗增殖和化学预防活性的新衍生物是必要的。
