ANTICANCER PLANT PRINCIPLES

抗癌植物原理

• 批准号: 3165254
• 负责人: Geoffrey A Cordell
• 金额: $ 15.1万
• 依托单位: UNIVERSITY OF ILLINOIS AT CHICAGO
• 依托单位国家: 美国
• 财政年份: 1979
• 资助国家: 美国
• 起止时间: 1979-04-01 至 1989-04-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3165254
• 关键词: antineoplastics; bioassay; chemical structure function; circular dichroism; drug design /synthesis /production; drug screening /evaluation; medicinal plants; nuclear magnetic resonance spectroscopy; plant extracts

The major objectives of this work is to isolate, purify and determine the structure of the anticancer compounds present in Catharanthus roseus, Catharanthus trichophyllus, Rhazya stricta, and Gnidia kraussiana. Although Catharanthus roseus is a well established source of antitumor agents of the dimeric indole alkaloid class, several highly active fractions remain to be studied for their active constituents. The crude alkaloid mixtures will be separated initially by pH gradient techniques and subsequently by column chroamtography; monitoring each step with an appropriate biological assay technique. A number of active bisindole alkaloids have been isolated and must be characterized. Isolated compounds will be identified by their mp, mass, UV and IR spectra, optical rotation CD and PMR and CMR spectra. Structure elucidation will be carried out by interpretation of these data, chemical correlation with known compounds and in particularly difficult cases by single crystal X-ray crystallography. The alkaloid fraction of the closely related plant Catharanthus trichophyllus also displays very good in vivo antitumor activity and it is proposed to isolate additional in vivo active compounds from this fraction by techniques similar to those described above for Catharanthus roseus. The Asian plant Rhazya stricta has afforded some in vitro active compounds but further isolation studies are needed on active fractions and some structural studies are still required. Rhazya orientalis will be grown for biological testing. Gnidia kraussiana has afforded a number of exceptionally cytotoxic fractions which have been obtained and it is proposed to isolate the compounds responsible for this activity. These are suspected to be tigliane or daphnane esters.

这项工作的主要目标是分离、纯化和确定 长春花中抗癌化合物的结构， 长春花属、狭叶林蛙和格氏草属植物。 虽然长春花属植物是一种公认的抗肿瘤来源 二聚吲哚生物碱类的试剂，几种高活性的 各组分的活性成分仍有待研究。原始人 生物碱混合物最初将通过pH梯度技术和 随后通过柱层析法；使用 适宜的生物检测技术。几种活性双吲哚 生物碱已被分离出来，必须加以鉴定。分离出的化合物 将通过它们的熔点、质量、UV和IR光谱、旋光度来鉴定 CD、PMR和CMR光谱。将通过以下方式进行结构说明 对这些数据的解释，与已知化合物的化学关联以及 在特别困难的情况下，通过单晶X射线结晶学。 近缘植物长春花中的生物碱成分 毛霉菌在体内也表现出很好的抗肿瘤活性，它是 建议从该组分中分离出额外的体内活性化合物 采用与上述长春花属植物相似的技术。 亚洲植物龙须菜在体外提供了一些活性化合物。 但还需要对活性组份和一些 仍然需要进行结构研究。东方林蛙将被种植用于 生物测试。Krussiana已经提供了一些 已经获得的特殊的细胞毒性部分，它是 建议分离出对这种活性负责的化合物。这些是 怀疑是三七烷酯或瑞香烷酯。