目的 研究矮紫杉Taxus cuspidata cv.Nana中紫杉烷类化合物成分及其抗肿瘤活性，以期发现红豆杉资源的替代品种。方法 采用高通量测序技术进行转录组测序，并采用分子对接的方式初步预测矮紫杉具有产生紫杉烷类化合物的能力。采用硅胶、Sephadex LH-20和HPLC等色谱方法进行分离纯化，并根据理化性质及波谱学数据鉴定结构。采用噻唑蓝（MTT）法、流式细胞术、Western blotting等方式，以肺癌NCI-H1299细胞、乳腺癌耐药株MCF-7/ADR、胃癌AGS细胞以及肝癌HepG 2细胞为模型，对所分离鉴定的部分化合物进行体外抗肿瘤活性评价。结果 从分子层面上验证矮紫杉具有代谢产生紫杉烷类化合物的能力，在此基础上从矮紫杉中分离得到6个紫杉烷类化合物，分别鉴定为紫杉醇（taxol，1）、三尖杉宁碱（cephalomannine，2）、巴卡亭III（baccatin III，3）、2-去乙酰氧基紫杉宁J（2-deacetoxytaxinine J，4）、2-去乙酰氧基-13-去乙酰去桂皮酰-紫杉宁J（2-deacetyloxy-13-deacetyldecinnamyl-taxinine J，5）、2-去乙酰氧-5α-羟基紫杉宁J（2-deacetoxy-5α-hydroxytaxinine J，6）。化合物1 ～3 对目标细胞株均具有良好的抗肿瘤活性。结论 栽培品种矮紫杉具有代谢产生紫杉烷类化合物的能力，可以在一定程度上作为红豆杉替代资源使用。

Objective To study the anti-tumor activity of taxanes isolated from Taxus cuspidata var and its anti-tumor activities, with a view to discovering alternative varieties of Taxus. Methods High-throughput sequencing technology is used for transcriptome sequencing, and molecular docking was used to preliminarily predict that the Taxus cuspidata var has the ability to produce taxanes. The chemical constituents were isolated from the total alkaloids of the twigs and leaves of G. multiflora by using silica gel, Sephadex LH-20, and HPLC chromatographic methods Furthermore, the cytotoxicity of some compounds against NCI-H1299 (human lung cancer cell line), MCF-7/ADR (human breast cancer drug-resistant cell line),AGS (human gastric cancer cell line), and HepG2(human liver cancer cell line) were tested by MTT, Flow Cytometry and Western blot methods. Results At the molecular level, it was verified that the Taxus cuspidata var has the ability to metabolize and produce taxanes, and on this basis. Six taxanes were isolated from the Taxus cuspidata var, and they were identified as taxol (1), cephalomannine (2), baccatin III (3), 2-deacetoxytaxinine J (4), 2-deacetyloxy-13-deacetyldecinnamyl-taxinine J (5), and 2-deacetoxy-5α-hydroxytaxinine J (6). Conclusion The cultivar Taxus cuspidata has the ability to metabolize and produce taxanes, which can be used as an alternative resource for Taxus to a certain extent.

R284.1

辽宁省“百千万人才工程”择优资助项目