药物共晶(HTHB)_4·(SiW_(12)O_(40))合成、表征及抗肿瘤活性研究  

Study on synthesis, characterization and antitumor activity of pharmaceutical cocrystal of(HTHB)_4·(SiW_(12)O_(40))

作　　者：张羽男[1] 张大俊[1] 张宇[1] 殷和美 刘立新[1] 张向宇[1] 冯艳茹[1] 沙靖全[1] 张云杰[1] 王朝兴[1] 沈宇[1] 匡海学[2] 

机构地区：[1]佳木斯大学黑龙江省药学研究所,黑龙江佳木斯154007 [2]黑龙江中医药大学中药学教育部重点实验室,哈尔滨150040

出　　处：《东北农业大学学报》2016年第8期75-81,共7页Journal of Northeast Agricultural University

基　　金：中国博士后科学基金资助项目(2014M561382);佳木斯大学青年基金项目(Lq2012-49)

摘　　要：利用溶剂热法探索合成一种未见报道的四氢小檗碱与硅钨酸药物共晶(HTHB)_4·(Si W_(12)O_(40)),通过X-射线单晶衍射、IR、XRPD和TGA等方法确定结构。X-射线单晶衍射数据分析结果表明,该化合物属四方晶系,P4/n空间群,晶胞参数:a=23.7874(15)?,b=17.2595(16)?,c=23.7874(15)?,V=9 766.1(13)?3,F(000)=7 496,Z=4。体外抗肿瘤活性试验结果表明,相同药物浓度下药物共晶(HTHB)_4·(Si W_(12)O_(40))抗肿瘤活性优于四氢小檗碱和硅钨酸抗肿瘤活性。A new pharmaceutical cocrystal of the tetrahydroberberine（THB） with the silicotungstic acid,（HTHB）4·（SiW12O40）, had been explored and synthesized by solvothermal method, and its structure had been characterized by X- ray single- crystal diffraction, IR, XRPD and TGA. X- ray single- crystal diffraction analysis revealed it belonged to the tetragonal system, space group P4/n, with a=23.7874（15）A, b=17.2595（16） A, c=23.7874（15） A, V=9 766.1（13） A3, F（000）=7 496, Z=4. Additionally, in vitro experimental study of the antitumor activity of the title compound had been investigated. The results demonstrated that the title compound exhibited more remarkable activity than parent compounds against human hepatoma Hep G2 cells at the same concentration.

关 键 词：四氢小檗碱 硅钨酸 药物共晶 抗肿瘤活性 

分 类 号：R284[医药卫生—中药学]