ANTINEOPLASTIC AGENTS FROM BLUE GREEN ALGAE

我们从两个加勒比海分离出两个系列的新天然产物 蓝绿藻Anabaina vanarioides和Microcoleus lyngbyaceus。 所有 这些次级代谢产物中的一种显示出良好的体外细胞毒性， 我们已经明确地将其指定为新的苯乙烯基色酮结构， 显示出优异的细胞毒性，ID50值在纳克范围内。 此外，后一种天然产物选择性地抑制RNA合成， 两种癌细胞系 我们随后收集的这两个 来自不同栖息地和季节的蓝绿色植物指出， 这些生命形式的极端化学变化。 这些提取物 后者的收集物具有很强的生物活性， 通过TLC分析发现与以前的系列不同的化学成分。 上述观察使我们提出了一个系统的调查， 这些和其他加勒比海蓝绿色藻类的新的细胞毒素。 我们还 探讨环境因子对蓝绿色藻的影响 通过季节性收集和实验室培养工作进行次生代谢。 我们的长期目标是发现新的化疗药物， 治疗肿瘤疾病，因此，进一步了解 细胞毒性的结构要求。

We have isolated two series of novel natural products from two Caribbean blue-green algae, Anabaina oscillarioides and Microcoleus lyngbyaceus. All of these secondary metabolites show good in vitro cytotoxicity and one, for which we have unambiguously assigned a novel styrylchromone structure, shows excellent cytotoxicity with ID50 values in the nanogram range. Further, this latter natural product selectively inhibits RNA synthesis in two cancerous cell lines. Our subsequent collections of these same two blue-greens from different habitats and seasons have pointed out the extreme chemical variability of these life forms. The extracts of these latter collections are strongly biologically active yet contain very different chemistry by TLC analysis than the previous collections. The above observations lead us to propose a systematic investigation of these and other Caribbean blue green algae for new cytotoxins. Further, we plan to explore the influence of environmental factors on blue green algal secondary metabolism by seasonal collections and labaoratory culture work. Our long term objectives are to discover new chemotherapeutic agents for treating neoplastic diseases, and hence, to further understand the structural requirements for cellular toxicity.