目的 研究亚乎奴Cissampelos pareira var.hirsuta的萜类和生物碱类化学成分。方法 采用硅胶、Sephadex LH-20、ODS、MCI等柱色谱和半制备液相色谱对其化学成分进行分离纯化，通过MS、NMR等波谱分析技术，结合理化性质分析，鉴定化合物结构。采用MTS法，测试化合物1、2、4、6～9、13、14对人急性早幼粒白血病HL-60细胞、人肺癌A549细胞、人肝癌SMMC-7721细胞、人乳腺癌MCF-7细胞、人结肠癌SW480细胞的细胞毒性。结果 从亚乎奴95%乙醇提取物中分离得到15个化合物，分别鉴定为羽扇豆醇（1）、白桦脂醇（2）、3β,14-二羟基-14β-孕甾-5-烯-20-酮（3）、3β-羟基-l7β-孕甾-5-烯-7,20-二酮（4）、假虎刺酮（5）、脱氢地芰普内酯（6）、黑麦草内酯（7）、(＋)-去氢催吐萝芙木醇（8）、(3S,5R,6S,7E)-3,5,6-三羟基-7-巨豆烯-9-酮（9）、(6R,7E,9S)-9-羟基-4,7-巨豆二烯-3-酮（10）、催吐萝芙木醇（11）、8,9-二氢-8,9-二羟基巨豆三烯酮（12）、橙黄胡椒酰胺乙酸酯（13）、橙黄胡椒酰胺（14）、橙黄胡椒酰胺苯甲酸酯（15）。MTS测试结果显示，化合物2对A549细胞和SMMC-7721细胞具有一定的细胞毒活性，半数抑制浓度（median inhibition concentration，IC₅₀）值分别为23.62、27.46 μmol/L。结论 所有化合物均为首次从锡生藤属植物中分离得到，包括三萜类化合物4个（1～4）、单萜类化合物8个（5～12）、生物碱类化合物3个（13～15）。羽扇豆烷型三萜可能为亚乎奴药材抗肿瘤活性的药效物质基础。

Objective To study the terpenoids and alkaloids from Cissampelos pareira var. hirsuta. Methods The compounds were isolated and purified by silica gel, Sephadex LH-20, ODS, MCI column chromatography and preparative HPLC, and their structures were identified by physicochemical properties, NMR and MS. Compounds 1, 2, 4, 6-9, 13 and 14 were tested for their cytotoxicity in human liver cancer SMMC-7721, breast cancer MCF-7, leukemia HL-60, lung cancer A549, colon cancer SW480 cell lines by MTS. Results Fifteen compounds were isolated from the 95% ethanol extract of Cissampelos pareira var.hirsuta, and their structures were identified as lupeol (1), betulin (2), 3β,14-dihydroxy-14β-pregn-5-en-20-one (3), 3β-hydroxy-l7β-pregn-5- ene-7,20-dione (4), carissone (5), dehydrololiolide (6), loliolide (7), dehydrovomifoliol (8), (3S,5R,6S,7E)-3,5,6-trihydroxy- 7-megastigmen-9-one (9), (6R,7E,9S)-9-hydroxy-4,7-megastigmadien-3-one (10), vomifoliol (11), 8,9-dihydro-8,9- dihydroxymegastigmatrienone (12), aurantiamide acetate (13), aurantiamide (14), and aurantiamide benzoate (15). Compound 2 showed the most potent cytotoxic activities against the A549 and SMMC-7721 cell lines, with IC₅₀ values of 23.62 and 27.46 µmol/L, respectively. Conclusion All compounds are isolated from Cissampelos genus for the first time, including four triterpenoids (1~4), eight monoterpenoids (5~12) and three alkaloids (13~15). Lupane triterpenoids may be antitumor constituents from Cissampelos pareira var. hirsuta.

R284.1

河南中医药大学省属高校基本科研业务专项（2014KYYWF-QN26）；河南中医药大学科技创新人才（2016XCXRC01）；河南省科技攻关（192102310438）；河南省中医药科学研究专项（20-21ZY1039）