Search for Novel Anti-cancer molecules from Plant Sources as Seeds of Possible Medicinal Agents.

植物含有多种成分，是新的生物活性分子的宝贵来源。本项目的目的是从高等植物中寻找新的生物活性分子，作为可能的抗癌药物的来源。研究结果如下：1.植物成分的分离与结构鉴定：所用植物的学名及分离得到的新化合物的通称如下：(1)鬼针科植物：藤黄(8个新的口山酮)、藤黄(2个新的多戊烯基二苯甲酮类化合物)、巴西胡萝卜(3个新的香豆素)、(2)豆科植物：Dalbergia cultrata、D.nigresense、D.olibari(5个新的肉桂酚和2个新的异黄酮类)、Milletia taiwaniana(5个新的异黄酮类)(3)Rutaceae植物：Glycom is arborea(3个新的Carbaoles)、Orixa Japan onica(4个新的喹诺酮类化合物)、新的和已知的植物成分的生物活性分析：(1)抑制二苯甲酮、肉桂酚、香豆素、吖啶酮、咔唑类、苯丙类、植物喹类化合物。(2)在体内两阶段致癌中对小鼠皮肤肿瘤的抑制作用：巨噬细胞、异黄酮类化合物。(3)对DPPH的自由基清除能力：二苯甲酮类化合物。(4)在小鼠RAW-AGE-264.4细胞中NO产生的抑制作用。喹啉类药物。(5)抑制白血病细胞生长：4-取代香豆素。

Plants contain many kinds of constituents and are a valuable source of new and biologically active molecules. The purpose of this project was the search of novel biologically active molecules from higher plants as a resource of possible anti-cancer agents. The summary of the results is shown below:1. Isolation and Structure Elucidation of Plants Constituents: The scientific names of plants used and general names of isolated new compounds were shown below :(1) Guttiferae Plants : Garcinia fusca (eight new xanthones), G. assigu (two new polyprenylated benzophenones), Calophyllum brasiliense (three new coumarins)(2) Leguminosae Plants : Dalbergia cultrata, D. nigrescense, D. olibari (five new cinnamylphenols and two isoflavonoids), Milletia taiwaniana (five new isoflavonoids)(3) Rutaceae Plants : Glycosm is arborea (three new carbazoles), Orixa japonica (four new quinolones), Murraya exotica (two new bicoumarins)(4) Euphorbiaceae Plant : Croton jatrophoides (two new triterpenoids)2. Biological activity assays for new and known plant constituents were carried out :(1) Inhibitory effects on EBV-EA activation induced by TPA in Raji cells : benzophenones, cinnamylphenols, coumarins, acridones, carbazoles, phenyppropanoids, phytoquinoids.(2) Inhibitory effect on mouse skin tumor promotion in an in vivo two-stage carcinogenesis : acrid on es, isoflavonids.(3) Radical scavenging ability against DPPH : benzophenones.(4) Inhibitory effect of NO production in murine macrophage-like RAW 264.4 cells : quinolones, quinolines.(5) Inhibition of leukemic cell growth : 4-substituted coumarins.