小叶莲抗肿瘤多药耐药药效物质基础及其机制研究

项目名称： 小叶莲抗肿瘤多药耐药药效物质基础及其机制研究

项目编号： No.31300284

项目类型： 青年科学基金项目

立项/批准年度： 2014

项目学科： 生物科学

项目作者： 孙彦君

作者单位： 河南中医学院

项目金额： 22万元

中文摘要： 肿瘤的多药耐药性是临床上制约恶性肿瘤患者化疗疗效的严重问题。由于中药具有的独特优势，从中药中筛选高效低毒的单体化合物用于应对肿瘤的多药耐药已成为当前肿瘤化疗研究的热点。项目组发现，在对小叶莲乙醇提取物各个萃取部位进行肿瘤多药耐药逆转活性的研究中发现，小叶莲乙醇提取物乙酸乙酯萃取部位(FrA3)对乳腺癌耐药细胞MCF-7/ADR不仅具有较强的逆转活性还具有较强的细胞毒活性，对乳腺癌耐药细胞MDA-231/ADR和MCF-7/ADR的IC50分别为2.83mg/mL, 4.81mg/mL，远远强于阳性对照组(indibulin)。进一步的体内移植瘤动物模型测试表明，抑制率为49%，强于阳性对照组(indubulin)。为此，本课题采用活性跟踪法对其中的抗肿瘤多药耐药活性成分进行提取、分离、纯化以及结构鉴定, 并初步探讨其抗肿瘤多药耐药机制。

中文关键词： 小叶莲；抗肿瘤；多药耐药；物质基础；作用机制

英文摘要： Multidrug resistance(MDR) of chemoageuts is one major obstacle to the successful cancer chemotherapy. Prevention and reversal of MDR in cancer cells is emergent problem to be resolved in the cancer research．In the chemotherapy of tumor，proper administration of traditional Chinese Medicine can reverse MDR, increase efficacy and reduce toxicity, which drew the extensive attention of scholars at home and abroad．In our investigation, FrA3 displayed cytotoxicity against MDA-231/ADR and MCF-7/ADR cell lines and was more cytotoxic than indibulin. In comparision with the control, FrA3 could inhibit tumorous growth in tumor-bearing nude mice. In order to search for new natural active products and novel lead compounds, our research was focused on extraction, isolation, purification, structure identification and preliminary anti-multidrug resistance mechanism by bioactivity guiding method. It can provide the necessary theoretical foundation and effective technical support for the development and utilization of antitumor multidrug resistance drugs.

英文关键词： Sinopodophyllum emodi；antitumor；multiple drug resistance；constituent；mechnism