Mehta R G, Liu J, Constantinou A, Hawthorne M, Pezzuto J M, Moon R C, Moriarty R M
Specialized Cancer Center, College of Medicine, University of Illinois at Chicago 60612.
Anticancer Res. 1994 May-Jun;14(3A):1209-13.
Brassinin, a phytoalexin, is found in Chinese cabbage. Previously, we showed that brassinin significantly inhibited dimethylbenz(a)anthracene (DMBA)-induced mammary lesions in organ culture. Moreover, it was an effective inhibitor against two stage skin carcinogenesis. In the present study, we synthesized several analogs of brassinin and evaluated their effectiveness in the mouse mammary gland organ culture model. Results showed that cyclobrassinin, also a naturally occurring brassinin analog, was more effective than brassinin. Spirobrassinin and N-ethyl-2,3-dihydrobrassinin also significantly inhibited mammary lesion formation. However, none of the methyl substituted analogs were effective. The effects of brassinin may, in part, be mediated by induction of phase II detoxifying enzymes such as quinone reductase.
油菜素内酯是一种植物抗毒素，存在于大白菜中。此前，我们发现油菜素内酯能显著抑制器官培养中由二甲基苯并(a)蒽（DMBA）诱导的乳腺病变。此外，它是两阶段皮肤致癌作用的有效抑制剂。在本研究中，我们合成了几种油菜素内酯类似物，并在小鼠乳腺器官培养模型中评估了它们的有效性。结果表明，环油菜素内酯也是一种天然存在的油菜素内酯类似物，其效果比油菜素内酯更好。螺环油菜素内酯和N-乙基-2,3-二氢油菜素内酯也能显著抑制乳腺病变的形成。然而，甲基取代的类似物均无效。油菜素内酯的作用可能部分是通过诱导II期解毒酶如醌还原酶来介导的。
