基于模拟胃液消化转化作用的三叶木通功效活性成分发掘研究

Akebia trifoliata is a plant of traditional Chinese medicine with wide and important pharmacological effects. But the main bioactive constituents of this plant related to its specific pharmacological effects are presently not clear. Our recent pre-study showed that some chemical constituents of A. trifoliata extract significantly transformed by simulated gastirc juice (SGJ) digestion, and the SGJ treated extract showed enhanced biological activity than untreated control, which indicates these new components transformed by SGJ possessing strong biological activities. However, the detatils of these structures, their bioactivities and their parental natural products of the new components generated by SGJ digestion still need further investigation. Based on our preliminary study and technique foundation, this project we are planning to systematically analyze and identify the newly generated components transformed by SGJ in treated A. trifoliata extract and manage to identify their corresponding parental natural compounds, as well as exploring the important bioactive activities and structure correlations between new transformed compounds and their parent chemicals. In this project, we would identify potentially new, highly-valued and bioactive transformed compounds from pre-treated extract of A. trifoliata by SGJ, which will promote a more effective development and utilization of this medicinal plant. It is predictable that this project will provide a demonstration and technical support for investigating potentially bioactive ingredients of Chinese herbal medicinal plant based on SGJ digestion.

三叶木通为我国传统重要的中药材植物，具有多方面重要药理功效，但其具体发挥药理功效的主要活性成分尚不明确。我们前期研究发现，模拟胃液消化转化处理能明显改变三叶木通提取物的化学成分构成，且经处理后的提取物相对处理前样品具有显著提高的生物活性，这提示经模拟消化转化后新产生的成分为具强生物活性的化合物。但这些新产生成分的结构与生物活性及其是由哪些天然产物经结构转化而生成的等问题均有待研究揭示。本项目基于前期研究和技术基础，拟对三叶木通提取物经模拟消化转化作用后新产生的成分及其潜在对应的原天然产物进行分离纯化和结构鉴定，并就新产生成分的重要生物活性及其与原天然产物间于化学结构上的相关性进行系统分析研究。本项目将能自经相关处理的三叶木通提取物中发掘出经结构转化新生成的高生物活性成分从而积极推进该植物功效成分的定位和更有效开发利用，并可望为中药材植物基于模拟消化转化的潜在活性成分研发提供示范和技术支持。

三叶木通为具多方面重要药理功效的传统中药材植物，但其具体发挥药理功效的活性成分却不甚明确。前期研究已显示模拟胃液消化作用能明显改变三叶木通提取物的化学成分构成进而显著提升其相关生物活性，但相应提取物原既有天然产物与发生转化成分的结构与具体活性及其结构转化过程等问题均有待揭示。基于上述背景和前期研究基础,本项目具体对三叶木通经模拟消化处理前后的提取物所含化学成分进行了系统的分离纯化和结构鉴定,总体从三叶木通植物相应提取物中共系统分离鉴定出了结构类型多样的五十八个成分，其中有十七个为新化合物；进而对分离所获化合物开展了多方面重要生物活性的分析检测，已揭示部分成分具有较显著的抑制糖苷酶、抑制肿瘤细胞生长、抗人体病原菌等重要生物活性；并通过结构与活性的对比分析研究，揭示经模拟消化作用转化生成的成分在结构特征和呈现重要生物活性方面与原天然产物间潜在具有紧密的相关关系。本项目研究实现了对三叶木通相应提取物潜在活性成分的较系统解析，积极推进了该植物相关主要功效成分的分析定位，并提示胃环境的消解转化作用促使三叶木通部分成分的结构转化（特别是三萜皂苷类成分的转化）在该植物发挥药理功效的过程中具有至关重要的作用。项目研究结果不仅将促进三叶木通植物功效相关成分的更有效开发利用，并在促进中药材植物基于消化转化作用的潜在活性成分研发方面具有一定示范意义。