侗药血藤果的化学成分及雌激素样作用研究

选择性雌激素受体调节剂是一类重要临床药物，根据其组织选择性及内在活性的不同，既可用于围绝经期综合征、绝经后骨质疏松的治疗；也可用于乳腺癌、子宫内膜癌等疾病的治疗。植物雌激素成分作为选择性雌激素受体调节剂的重要来源，是新药开发的热点领域之一。侗药血藤果在侗区用于妇女围绝经期综合征，产后出血，女性不孕不育等症的治疗，但其药效物质基础尚未明确。我们前期动物及细胞实验显示：血藤果能促进小鼠子宫增重及影响MCF-7细胞增殖，提示其含有植物雌激素成分。本项目拟利用天然药物化学的各种技术分离、纯化、鉴定血藤果中的植物雌激素成分，并对活性化合物的作用机制展开研究，以期为雌激素受体调节剂的开发提供新的先导化合物。本项目无论对于侗医药的传承与发展还是对于雌激素受体调节剂的开发都具有重要意义。

Selective estrogen receptor modulators (SERMs) are kinds of clinical drugs that exert different biological effects on estrogen receptor in different tissues and can be used in the treatment of perimenopausal syndrome, postmenopausal osteoporosis, breast cancer, endometrial cancer and other ailments. Phytoestrogens are considered to be the important sources of SERMs, and have become one of active fields in new drug development. The mature fruit of Kadsura coccinea (Schisandraceae) is widely used folk medicine in Dong ethnic minority regions for the treatment of perimenopausal syndrome, postpartum hemorrhage, and female infertility. However, there are no representative studies to provide us with more facts about its material foundation of efficacy. Our preliminary experiments, which have shown that the mature fruit of Kadsura coccinea can increase the uterus weight of mice, and inhibit the proliferation of MCF-7 cell lines, suggest the exist of phytoestrogens. In order to discover more lead compounds for SERMs. In this project, we are planning to investigate the chemical structures of phytoestrogens deprived from the mature fruit of Kadsura coccinea, and evaluate their potential estrogenic activities by developing an estrogen receptor -GAL4-UAS reporter gene assay and MTT assay. Additionally, certain biochemical methods, such as western-blot analysis, will be used to explore the underlying mechanisms of active ingredients. The significance of this project is to help Dong medicine to be inherited and developed, and promote the drug development of SERMs.