Design of nonsteroidal durassinosteroids

非甾体杜拉斯素类固醇的设计

基本信息

批准号：
09660117
负责人：
NAKAGAWA Yoshiaki
金额：
$ 2.18万
依托单位：
KYOTO UNIVERSITY
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (C)
财政年份：
1997
资助国家：
日本
起止时间：
1997 至 1998
项目状态：
已结题

项目摘要

The rice lamina inclination test was used to detect the brassinosteroid activity. After treating the rice cultivar with various concentration of compounds according to the standard bioassay system, the magnitude of the angle induced between the leaf and sheath was measured using semicircular protractor. The angles induced after treatments with various concentration of compounds were plotted against the concentrations. In each assay, both treatments with a solvent (DMSO) and a high concentration of brassinolide (10^<-6> M) were included as the negative and positive control, respectively. From each concentration-response curve, the 50% effective concentration EC_<50> (M) was determined for each compound, and the reciprocal logarithm of EC_<50> was used as the activity index. Using this method, we evaluated reproducible EC_<50> values for brassinolide, castasterone, and epibrassinolide to be 9.14, 8.08, and 8.28, respectively. The order of the activity of brassinosteroids is consistent wi … More th the previously reported results. The advantage of this evaluation system in which the concentration-response curve is adopted to estimate the 50% effective concentration is that 1) the standard error of averaged value is small, 2) the constant activity is able to be determined regardless of the experimental conditions, 3) the activity of weak compounds for which the angle exceeding the standard angle (usually 140 degree) is not observed in the measurement is able to be evaluated. With this bioassay system, insect molting hormone agonists such as ecdysone and dibenzoylhydrazines, mammalian hormones such as diethylstilbestrol and glucocorticoids, and other newly synthesized compounds such as oxime and phenyl benzyl ether compounds were screened, although none of compounds tested was not active. Three-dimensional (3-D) structures of 20-hydroxyecdysone and brassinolide were constructed and compared between them, which were different with respect to the torsion angle between alkyl chain at C- 17 position and D-ring of steroid skelton. Less

水稻叶片倾斜度测试用于检测油菜素类固醇活性。根据标准生物测定系统用不同浓度的化合物处理水稻品种后，使用半圆量角器测量叶片和鞘之间诱导的角度的大小。将用不同浓度的化合物处理后相对于浓度作图。在每个测定中，用溶剂(DMSO)和高浓度芸苔素内酯(10 1 -6 M)的处理均包括在内作为阴性。分别从每个浓度-反应曲线中确定每个化合物的50％有效浓度EC_ 50 (M)，并且使用该方法将EC_ 50 的倒数对数用作活性指数。，我们评估油菜素内酯、卡斯特酮和表油菜素内酯的可重复 EC_<50> 值为 9.14、8.08 和油菜素类固醇的活性顺序与之前报道的结果一致。采用浓度-反应曲线来估计50%有效浓度的评价系统的优点是：1）标准。平均值误差小，2）无论实验条件如何，都能测定恒定的活性，3）未观察到超过标准角度（通常为140度）的弱化合物的活性通过该生物测定系统，可以筛选昆虫蜕皮激素激动剂，例如蜕皮激素和二苯甲酰肼，哺乳动物激素，例如己烯雌酚和糖皮质激素，以及其他新合成的化合物，例如肟和苯基苄基醚化合物，但没有。 20-羟基蜕皮酮和的化合物的三维 (3-D) 结构不具有活性。构建并比较了它们之间的油菜素内酯，它们在甾体骨架的C-17位烷基链与D环之间的扭转角度上有所不同。