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

水稻层倾斜度测试用于检测黄铜固醇活性。根据标准生物测定系统，用各种浓度的化合物处理水稻品种后，使用半圆形量角器测量了叶和鞘之间诱导的角度的大小。用不同浓度的化合物处理后诱导的角度绘制了浓度。在每项评估中，两种用溶液（DMSO）和高浓度的脑核酸（10^<-6> m）的处理分别为阴性和阳性对照。从每个浓度响应曲线中，确定每种化合物的50％有效浓度EC_ <50>（M），并将EC_ <50>的相互对数用作活性指数。使用此方法，我们分别评估了Brassinolide，Castasterone和Epibrassinolide的可再现EC_ <50>分别为9.14、8.08和8.28。黄铜固醇活性的顺序是一致的，这是先前报道的结果。采用浓度响应曲线来估计50％有效浓度的评估系统的优点是，1）平均值的标准误差很小，2）能够确定恒定的活动，无论实验条件如何，3）弱化合物的活性在该弱化合物中的活性超过标准角度（通常是140度），以评估该范围的范围。借助这种生物测定系统，昆虫摩他的激动剂，例如ecdysone和dibenzoylhydrazines，诸如二乙基甲状腺脱甲醇和糖皮质激素等哺乳动物恐怖，以及其他新合成的化合物，例如甲基苯甲酸酯和苯基苯基乙醚化合物，尽管没有筛选出综合测试。构建了20-羟基环酮和铜氨基醇的三维（3-D）结构，并在它们之间进行了比较，它们在C-17位置和类固醇Skelton的D环之间的扭转角不同。较少的