洋金花果皮中生物碱成分及抗肿瘤活性研究

摘要

Objective:To study the alkaloids from pericarps of Datura metel L.and screen the antitumor activities of the isolated compounds.Methods:The separation and purification were taken by silica gel column chromatography,Sephadex-LH20 and semi-preparative HPLC,and the structural identification was based on physicochemical property,1H-NMR and 13 C-NMR as well as HR-MS data.The isolated compounds were evaluated according to antitumor activities of HepG-2,A549 and SGC-7901 by MTT method.Results:Ten alkaloids were obtained from the ethyl acetate of 70％ ethanol extract of pericarps of D.metel L.and the structures were identified as cyclo (PheTyr) (1),9-hydroxycanthin-6-one (2),(2,5-dioxo-4-imid-azolidinyl)-carbamic acid (3),1-ribityl-2,3-diketo-1,2,3,4-tetrahydro-6,7-dimethyl-quinoxa-line (4),grossamide (5),cannabisin F (6),hyoscyamine (7),Trans-N-p-coumaroyl tyramine (8),N-trans-feruloyloctopamine(9) and (2S,E)-N-[2-hydroxy-2-(4-hydroxyphenyl) ethyl] ferulamide (10),respectively.All isolated possessed the potential anti-tumor activity in vitro.Conclusion:Compounds 1-4 are isolated from the plants of Solanaceae for the first time,and compounds 1,2,5,6 and 8 exhibit a strongly antitumor activity.%目的:研究洋金花果皮中生物碱成分及抗肿瘤活性.方法:采用硅胶、Sephadex-LH20及HPLC等色谱方法对化合物进行分离和纯化,并利用1 H-NMR、13C-NMR及MS波谱方法鉴定化合物的结构,以肝癌HepG-2、肺癌A549及胃癌SGC-7901肿瘤细胞为受试细胞,采用MTT法评价化合物的抗肿瘤活性.结果:该研究从洋金花果皮70％乙醇回流提取物的乙酸乙酯部位中共分离得到10个生物碱类化合物,分别鉴定为cyclo (PheTyr)(1)、9-hydroxycanthin-6-one(2)、(2,5-dioxo-4-imidazo-lidinyl)-carbamic acid(3)、1-ribityl-2,3-diketo-1,2,3,4-tetrahydro-6,7-dimethyl-quinoxaline(4)、grossamide(5)、cannabisin F (6)、hyoscyamine(7)、trans-N-p-coumaroyl tyramine(8)、N-trans-feruloyloctopamine(9)和(2S,E)-N-[2-hydroxy-2-(4-hydroxyphenyl)ethyl] ferulamide(10);体外抗肿瘤实验表明,1 ～10号化合物均具有潜在肿瘤细胞抑制活性.结论:化合物1～4首次从茄科植物中分离得到,且化合物1、2、5、6和8表现为较强的抗肿瘤活性.