龙血竭黄酮类化合物的生源途径与仿生合成研究

Natural Dragon's Blood (Resina Draconis), a precious medicinal herb, bears the problem of rare materials and low yield. As the natural formation mechanism has been the bottlenecks of its artificial development, the main component, flavonoids, becomes the key point to break through it. Based on the theories of biotransformation and bionics, this program focuses on the structure formation and its transforming relationship of flavonoids in Dragon's Blood by biosynthetic pathway, in order to construct a preparation system applicable to the exploitation and utilization of Dragon's Blood and explore a new method for researching natural products based on the combination of chemistry and biology..Flavonoids are biomimetically synthesized by the protocol based on the optimized biosynthetic pathway of flavonoids in Dragon's Blood, and then the compounds are acted on the tissue cultured Dracaena cochinchinensis (Lour.) S. C. Chen to verify the biotransformation process of flavonoids. This procedure also be applied to synthesis the compounds with potential medicinal value, such as derivatives of Dragon's Blood flavonoids and biflavonoids. Supported by the research background and basis of organic synthesis of natural products and biotransformation of Dragon's Blood, this program is of important theoretical significance and wide application prospect for constructing the preparation and transformation system of flavonoids, revealing the natural formation mechanism and realizing the sustainable development of Dragon's Blood.

名贵药材天然龙血竭原料珍稀且产量极低，其自然形成机制问题是人工开发的瓶颈，而主要组分黄酮物质成为突破的关键点。本项目以黄酮生物转化和仿生学理论为依据，依生源途径研究龙血竭中黄酮类化合物的结构形成及其转化关系。以期构建适用于龙血竭人工开发的制备体系，并探索基于生物和化学相结合研究天然产物的新方法。.通过优化龙血竭黄酮类化合物生源途径设计合成路线，仿生合成黄酮类化合物，并将合成的化合物作用于组培剑叶龙血树验证黄酮化合物生物转化过程。最后将方法应用于合成龙血竭黄酮类衍生物、双黄酮等具潜在药用价值的化合物。项目组在有机合成天然产物和龙血竭生物转化等方面具有较好的研究背景和基础。项目实施对于构建黄酮化合物制备转化体系和揭示龙血竭自然形成机制实现可持续开发利用，都具有十分重要的理论意义和广阔的应用前景。

名贵中药材龙血竭原料珍稀且产量极低，其自然形成机制和活性组分的人工合成是开发的瓶颈，具有较高的科学意义以及应用价值。本项目针对龙血竭主要物质成分黄酮类化合物形成和转化问题，优化了龙血竭黄酮类化合物生源途径，设计仿生合成路线并合成了查尔酮、黄烷、黄酮、双黄酮等关键黄酮类物质和含氧杂环化合物，实现了龙血竭关键组分龙血素a、b的克级制备和龙血素c骨架分子构建，对其中查尔酮类衍生物进行了初步镇痛、降糖生物活性和安全性评价，显现较好的结果。本项目研究对于龙血竭资源深度开发利用具有重要意义和应用价值。