Search for Novel Anti-tumor Constituents from Plant Sources and Their Drug Development

在从植物中寻找新的抗肿瘤活性成分的过程中，从植物中分离得到了许多新的吖啶酮、咔唑、喹诺酮、喹唑啉等生物碱类化合物，以及氧杂蒽酮、香豆素、氟拉伐他汀、苯丙素类化合物，并通过光谱和合成方法确定了它们的结构。此外，还对本项目中分离的化合物进行了几种类型的生物活性测试。本项目所用植物来源科属：（1）芸香科植物：九里香属、黄皮属、甘草属、婆罗尼亚属、假黄皮属植物（2）豆科植物：降香属、鸡血藤属、鱼藤属植物（3）杜仲科植物：胡桐属、藤黄属植物（4）白骨壤科植物：白骨壤属植物2。生物活性测定（1）抗肿瘤促进作用测定：7-甲氧基香豆素类、氧杂蒽酮类、苯丙素类（2）诱导HL-60细胞分化活性测定：吖啶酮生物碱（3）对几种癌细胞系的抗增殖作用测定：吖啶酮生物碱（4）一氧化氮生成抑制作用测定：香豆素类

In the search of novel anti-tumor constituents from plant sources, many kinds of novel acridone-, carbazole-, quinolone-, and quinazoline-alkaloids, and xanthones, coumarins, fulalvonoids, and phenylpropanoids were isolated and their structures were established by spectrometric and synthetic methods. Further, several types of biological activities were also tested for the compounds isolated in this project.1. Families and genus of plant sources used in this project :(1) Plants of Rutaceae : plants of genus Murraya, Clausena, Glycosmiss, Boronia, Micromelum(2) Plants of Leguminosae : plants of genus Dalbergia, Milletia, Derris(3) Plant of Guttiferae : plants of genus Calophyllum, Garcinia(4) Plant of Avicenniaceae : plants of genus Avicennia2. Assays of Biological Activities(1) Assay of Anti-tumor Promoting Effects : 7-methoxycoumarins, xanthones, Phenylpropanoids(2) Assay of the Activity of Induction of HL-60 Cell Differentiation : acridone alkaloids(3) Assay of Anti-proliferative Effects on Several Cancer Cell Lines : acridone alkaloids(4) Assay of Inhibitory Effects of Nitric Oxide Generation : coumarins