滇产两面针中抗肿瘤活性生物碱成分研究

Study on the alkaloids and their anticancer activity from Zanthoxylum nitidum

从滇产两面针的干燥根中分离得到12个化合物,通过其一维或二维核磁共振谱、质谱和理化性质的解析并结合文献鉴定了它们的结构,分别为9-去甲氧基两面针碱(1)、8-dehydroxyl-buesgenine(2)、6β-hydroxymenthyldihydronitidine(3)、花椒木精(4)、rhoifoline B(5)、两面针碱(6)、白屈菜红碱(7)、博落回碱(8)、白鲜碱(9)、γ-崖椒碱(10)、茵芋碱(11)和鹅掌楸碱(12)。其中,化合物1和2为新结构化合物。通过MTT法,首次评价了化合物1~12对黑色素瘤细胞WM9增殖的抑制活性,并发现化合物3和6对WM9细胞的增殖表现出较强的活性,半数抑制浓度(IC50)值分别为1.936μM和0.880μM,研究结果为抗肿瘤药物候选药物分子的发现提供了科学依据。

There are twelve compounds isolated from the ethanol extraction part of Zanthoxylum nitidum,which was traditional Chinese medicine,and the structure of these compounds were characterized through 1D,2D NMR spectrometry,mass spectrometry,as well as physicochemical properties research experiment.They were 9-demethoxynitidine(1),8-dehydroxyl-buesgenine(2),6β-hydroxymenthyldihydronitidine(3),zanthoxyline(4),rhoifoline B(5),nitidine(6),chelerythrine(7),bocconoline(8),dictamnine(9),γ-fagarine(10),skimmianine(11),liriodenine(12).Among them,compound 1 and compound 2 were found from Zanthoxylum nitidum for the first time and never been reported.The proliferation inhibition activity of compounds 1-12 against melanoma cells WM9 was evaluated for the first time by MTT method.The results showed that compound 3(IC50=1.936μM)and compound 6(IC50=0.880μM)have potent anti-proliferation activity of WM9 cells.This research has provided promising candidate molecules for the discovery of anticancer drugs.