控制释放是缓解植物源抗肿瘤药物毒副作用的有效途径。申请者前期研究发现，通过杨木预水解提取的天然两亲性木质素-碳水化合物复合体（LCC），经定向修饰可获得具有自乳化能力的理想纳米微球，显示优良的药物包裹控释作用。但对预水解LCC的形成机制及其定向修饰后分子结构与包裹控释行为的关系等关键科学问题尚不清楚。本项目将采用β-O-4´型、5-5´型和β-5´型三种木质素模型物，分别与碳水化合物混合预水解，解析预水解LCC的形成途径。通过引入长链脂肪族化合物和调控木质素/碳水化合物比例，对木质纤维预水解LCC进行分子修饰，实现预水解LCC组成和结构的定向调控。自乳化形成稳定的LCC纳米微球，包裹植物源抗肿瘤药物，构建LCC组成、结构及其微球微观构象与控释效率的三维构效关系。上述研究将为LCC新的丰富来源和新的应用领域提供理论基础。

Controlled release technology is an effective approach to alleviate the toxic side effects of plant-derived anticancer drugs. In the early-stage study, the amphipathic lignin-carbohydrate compound (LCC) was extracted from poplar prehydrolysis liquor. Directional modification of LCC made the natural product a great potential candidate for preparing nanospheres, which could encapsulate paclitaxel and show controlled-release effect, by means of a simple self-emulsifying method. However, the formation mechanism of prehydrolysis LCC was still to be solved, and the relationship between modified structures and controlled-release behaviors still remained unclear. In this project, β-O-4´, 5-5´ and β-5´ lignin models will be synthesized and utilized to reveal the formation path of prehydrolysis LCC. By introducing hydrophobic aliphatic compound and reducing hydrophilic carbohydrate group, the LCC from lignocellulose prehydrolysis liquor will be modified so as to realize the regulation of composition and structure. Stable LCC nanospheres will be prepared through self-emulsification, and encapsulate plant-derived anticancer drugs to form a novel drug carrier. Controlled release efficiency will be studied for elucidating the 3D structure-activity relationship with LCC composition, structure and its microsphere conformation. The above research will provide references to the development of controlled-release materials, and give a new way for the use of LCC.