景东山橙中生物碱类化学成分

Chemical Constituents of Alkaloids from Melodinus khasianus

目的：夹竹桃科（Apocynaceae）山橙属（Melodinus）植物在我国民间应用的历史悠久,其生物碱类化学成分具有抗肿瘤、抗菌、抗生育等生物活性。该文对夹竹桃科山橙属植物景东山橙（Melodinus khasianus）中生物碱类化学成分进行系统研究。方法：运用硅胶柱色谱、反相硅胶柱色谱及高效液相制备色谱对景东山橙中生物碱类化学成分进行分离和纯化,并通过其理化性质及波谱数据确证生物碱类化合物的结构。通过噻唑蓝（MTT）比色法,对分离得到的化合物进行前列腺癌细胞（PC-3）,肺癌细胞（A549）,胃癌细胞（HGC-27）和人白血病细胞（HL-60）的细胞增殖抑制筛选。结果：从景东山橙乙醇提取物的三氯甲烷部位分离得到12个化合物,分别鉴定为（＋）epi-16α-hydro-14,15vincamine（1）,16β,21β-epoxy-vincadine（2）,melodinines G（3）,melodinines P（4）,melodinines N（5）,16β-hydroxy-19S-vindolinine（6）,16β-hydroxy-19R-vindolinine（7）,15α-hydroxy-14,15-dihydrovindolinine（8）,melodinines T（9）,19-epimeloscandonine（10）,门洛斯坎刀尼（11）,攀援山橙碱（12）。结论：其中化合物1～10为首次从景东山橙中分离得到的生物碱。采用MTT比色法对化合物进行体外抗肿瘤活性筛选,发现化合物4,5对前列腺癌细胞（PC-3）,肺癌细胞（A549）,胃癌细胞（HGC-27）和人白血病细胞（HL-60）等肿瘤细胞具有一定的细胞增殖抑制作用。

Objective： Melodinus（ Apocynaceae） plants have been used in folks in China for a long time. Alkaloids from Melodinus genus have showed significant antitumor,antibacterial and antifertility activities.This study focuses on the chemical constituents of alkaloids from M. khasianus. Method： The compounds were isolated and purified by silica gel column chromatography, reversed-phase C18 column chromatography and preparative liquid chromatography. The compounds were screened out for prostate cancer cells（ PC-3）,lung cancer cells（ A549）,gastric cancer cells（ HGC-27） and human leukemia cells（ HL-60） by MTT method.Result： Their chemical structures were established by their physicochemical properties and spectral data. Twelve compounds were isolated and characterized from the chloroform fraction of ethanol extract in M. khasianus. Their structures were identified as（ ＋） epi-16α-hydro-14,15 vincamine（ 1）,16β, 21β-epoxy-vincadine（ 2）,melodinines G（ 3）,melodinines P（ 4）,melodinines N（ 5）,16β-hydroxy-19 S-vindolinine（ 6）,16β-hydroxy-19 R-vindolinine（ 7）,15α-hydroxy-14,15-dihydrovindolinine（ 8）,melodinines T（ 9）,19-epimeloscandonine（ 10）,meloscandonine（ 11） and scandine（ 12）. Conclusion： Compounds 1-10 were isolated from M. khasianus for the first time. The cytotoxicity of these compounds was evaluated by MTT method in vitro. Compounds 4 and 5 displayed an inhibitory effect on the proliferation of prostate cancer cells（ PC-3）,lung cancer cells（ A549）,gastric cancer cells（ HGC-27） and human leukemia cells（ HL-60）.