盐酸青藤碱单晶的制备方法及其在抗肿瘤药物方面及应用.pdfVIP

盐酸青藤碱单晶的制备方法及其在抗肿瘤药物方面的应用 * 张虹，向俊锋，沈刚，杨凤敏，唐亚林 （中国科学院化学研究所，分子动态稳 态实验室，北京，100190） 摘要：目的 确定了盐酸青藤碱单晶的制备工艺，并探讨其在抗肿瘤药物方面的 应用。方法 采用酸碱滴定的方法制备出盐酸青藤碱单晶，利用X 射线衍射分析 （XRD ）进行晶体结构分析。采用四甲基偶氮唑蓝实验（MTT ）观察化合物对 胶质瘤细胞生长的抑制作用，并利用酶联免疫吸附方法评价了化合物对酪氨酸激 酶活性的抑制作用。结果 采用酸碱滴定方法制备出纯白色的盐酸青藤碱单晶， 晶体属于正交晶系，空间群为：P2(1)2(1)2(1) ，晶胞参数为：a=7.2160 ；b=14.3237 ； c=19.2357 ；α=90.000 ；β=90.000 ；γ=90.000 。通过MTT 及酶联免疫吸附方法测 定该化合物对肿瘤细胞的增殖及酪氨酸激酶的活性具有较好的抑制作用。结论 通过酸碱法滴定方法可以得到纯白色的盐酸青藤碱单晶。上述盐酸青藤碱单晶具 有很好的抗肿瘤效果，并对酪氨酸激酶的活性具有抑制作用。 关键词：盐酸青藤碱，单晶，抗肿瘤，酪氨酸激酶 The preparation method of sinomenine single crystal and its application in antitumor drug ZHANG Hong, XIANG Jun-feng, SHEN Gang, YANG Feng-min, TANG Ya-lin* (National Laboratory for Molecular Sciences, Center for Molecular Sciences, State Key Laboratory for Structural Chemistry of Unstable and Stable Species, Institute of Chemistry Chinese Academy of Sciences, Beijing 100190) ABSTRACT: OBJECTIVE The processes for preparing of sinomenine hydrochloride crystal was studied. And the application in the anti-tumor drug was discussed. METHODS The sinomenine hydrochloride crystal was analyzed by X-ray diffraction (XRD). The inhibitory effects of sinomenine on C6 cells proliferation was analyzed by MTT assay in vitro. And the Elisa method was used to evaluate the inhibitory effects of compounds on the activity of protein tyrosine kinase. RESULTS By using the acid-base titration method, the sinomenine hydrochloride crystal was prepared and the crystal belongs toorthorhombic, space group P2(1)2 (1)2 (1), unit cell parameters: a =7.2160; b=14.3237; c=19.2357; =90.000; =90.000; gamma =90.000. Moreover, sinomenine inhibited the activity of protein tyrosine kinase, and it has shown obvious anti-tumor effect on C6 tumor cells. CONCLUSION The acid-base titration