海藻中抗污损活性物质研究

Algal secondary metabolites not only novel structure, and broad-spectrum biological activity, has an irreplaceable position in the field of marine natural products. Especially seaweed in the evolutionary process, the formation of unique chemical defense mechanism, maintain a clean surface, not to be defiled, can be synthesized in the body and release with antifouling activity of metabolites. Discovery of natural non-toxic antifouling active substances from algae, become the new hot spot for marine antifouling material research. After a screening of antifouling activity experiments, the research group found that collected from Zhanjiang sea seaweed ethanol extract has significant inhibition of barnacle larvae attachment activity. Antifouling compounds from 4 genera and 6 species of algae will be isolated and identified with barnacles and Bugula neritina larvae model, to safety and pollution prevention index as evaluation objective. Compounds with strong activities will be synthetized and modified. Estimating active compound to the bacterium community effect (QS) suppression activeness based on the colibacillus Escherichia coli pS401- odor pseudomonas putida IsoF. Study on the structure-activity relationship of antifouling activity and summarize the effective group. Antifouling activity will be evaluate d in outdoor to compounds with the use of field antifouling activity model. This research is expected to find new marine antifouling agent or to lay an important foundation and provide a new molecular model for further research.

海藻次级代谢产物不仅结构新颖独特，而且生物活性广谱高效，在海洋天然产物研究领域具有不可取代的位置。特别是海藻在进化过程中，形成独特的化学防御机制，体表保持洁净，不被污损，能够在体内合成并释放具有抗污损活性的代谢产物，从海藻中发现天然无毒抗污损活性物质，成为寻找海洋抗污损物质研究的新热点。经过抗污损活性实验筛选，课题组发现采自湛江海域海藻乙醇浸提物具有显著抑制藤壶幼虫附着活性。本项目在此基础上采用藤壶和草苔虫幼虫模型，以安全防污指数为评价目标，追踪分离鉴定4属6种海藻中抗污损活性化合物，对活性较好的化合物进行化学合成及结构修饰，获得大量抗污活性单体。采用大肠杆菌-恶臭假单胞菌模型评价活性化合物对细菌群体效应（QS）的抑制活性，探讨构效关系，利用野外抗污损活性模型评价活性化合物的室外抗污活性情况。该研究有望直接发现新型海洋防污剂或为之奠定重要基础，为进一步深入研究提供新的模型分子。

海藻、海绵及其微生物等海洋生物中含有大量的抗污损、抗肿瘤、抗菌等生物活性化合物，从中发现活性先导化合物已成为世界范围内共同关心的热点。 本项目采用了硅胶柱层析、反相ODS柱层析、Sephadex LH-20凝胶柱层析和高效液相等色谱分离技术对采集中国南海5种海藻、2种海绵及2种微生物等9种海洋生物中的抗污损、抗肿瘤、抗菌等生物活性成分进行提取、分离、纯化；通过核磁共振、质谱、紫外光谱和红外光谱等谱学手段对分离纯化的单体化合物进行平面结构确定，运用圆二色谱、X-ray单晶衍射及计算化学的方法确定这些单体化合物的结构（含立体结构）。 从5种海藻、2种海绵及2株海洋微生物等9种海洋生物中提取、分离、纯化、鉴定326个单体化合物，其中新的化合物76个，新颖骨架化合物5个。对单体化合物进行抗污损、抗肿瘤、抗菌等生物活性测试，发现活性单体化合物76个，较强活性化合物8个。对从海藻中发现的抗污损活性较强的蕨藻红素caulerpin进行全合成及结构改造。发表SCI收录论文21篇，包括A1论文5篇，1区论文1篇，获批授权专利6件。