ANTICANCER PLANT PRINCIPLES

本工作的主要目的是分离、纯化和测定 长春花中抗癌化合物的结构， 毛叶长春花（Catharanthus trichophyllus）、Rhazya stricta和Gnidia kraussiana。 虽然长春花是一种公认的抗肿瘤来源， 二聚吲哚生物碱类药物，几种高活性 级分的活性成分仍有待研究。 粗 生物碱混合物将首先通过pH梯度技术分离， 随后通过柱色谱法; 适当的生物测定技术。 一些活性双吲哚 生物碱已被分离出来，必须加以鉴定。 分离的化合物 将通过其mp，质量，UV和IR光谱，旋光度 CD和PMR和CMR光谱。 结构解析将由 这些数据的解释、与已知化合物的化学相关性， 在特别困难的情况下，通过单晶X射线晶体学。 长春花属植物的生物碱部分 毛叶菌还显示出非常好的体内抗肿瘤活性， 建议从该级分中分离另外的体内活性化合物 通过类似于上述用于长春花的技术。 亚洲植物Rhazya stricta已经提供了一些体外活性化合物 但需要对活性组分进行进一步的分离研究， 仍需进行结构研究。 Rhazya orientalis将被种植， 生物测试 Gnidia kraussiana提供了许多 已经获得了特别具有细胞毒性的级分， 建议分离负责这种活动的化合物。 这些是 怀疑是惕各烷或瑞香烷酯。

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.