新疆骆驼蓬种子抗肿瘤活性成分的研究

Studies on the antitumor activity constituents of Xinjiang Peganum Harmala Seeds

目的 :研究从新疆骆驼蓬种子中提取、分离的有效成分对肿瘤细胞的生长抑制作用 ,对比有效成分之间抗肿瘤活性大小。 方法 :采用醇提法及柱层析法得到 4种单体化合物 ,利用熔点测定法及紫外光谱、红外光谱、核磁共振、质谱鉴定结构 ;以这 4种单体化合物作为受试样品 ,分别对人胃癌细胞系 BGC82 3、人大肠癌细胞系 L O-VO、人宫颈癌细胞系 Hela以及小鼠肉瘤细胞系 S180进行生长抑制作用的实验 ,以 IC50 、细胞抑制率为指标 ,考查抗肿瘤活性大小。结果:经结构鉴定推断 4种单体化合物为生物碱 ,分别为去氢骆驼蓬碱、骆驼蓬碱、鸭嘴花碱及鸭嘴花酮碱 ;去氢骆驼蓬碱、骆驼蓬碱对上述 4种细胞系均有明显的生长抑制作用 ;而鸭嘴花碱和鸭嘴花酮碱在最大浓度 2 0 μg/ml均未见到对各细胞株的生长抑制作用。 结论:去氢骆驼蓬碱、骆驼蓬碱有明显的抗肿瘤活性 。

Objective: This experiment studied on antitumor activity constituents of Xinjiang Peganum Harmala Seeds. Methods: We used chemical methods extracted and separated activity constituents from Peganum Harmala Seeds. Isolated four monomers. Their chemical structures determined by means of MP, UV, IR,NMR,MS. Then these four Monomers were used to experiments on the human gastric carcinoma cell BGC 823, human large colon carcinoma cell LOVO, human cervical carcinoma Hela and rat sarcoma cell S 180 . Results: These four monomers were alkloids. They were named Harmine, Harmaline, Vasicine and Vasicinone. The results showed that harmine and harmaline have certain inhibition. Based on this experimental, results, it showed that harmine and harmaline can significantly inhibit these four cells growth, and they have the potent antitumor activity. The inhibition rate of harmine was 40.0%0~87.5%; the IC 50 was (8.25 ±0.61) μg/ml, (8.67±1.36) μg/ml, (7.89±0.64) μg/ml, (8.35±0.69) μg/ml; the IC 50 of harmaline was (10.21±2.22)μg/ml,(7.08±4.86)μg/ml,(9.495±1.087)μg/ml,(10.83±1.53)μg/ml.But the other alkaloids vasicine and vasicinone showed no antitumor activity. Conclusion:Hamine and Harmaline have significant anti tumor activity,but Vasicine and Vasicinone have not the anti tumor activity.