6-F硫色烯并[4,3-c]吡唑啉的体内抗肿瘤活性  

Antitumor Activity of 6-Fluoro-thiochromene[4,3-c]pyrazoline in Vivo

作　　者：贾苗辉[1] 杨更亮[1] 杨春柳[1] 刘智勤[1] 马正月[1] 郭兰弟[1] 

机构地区：[1]河北大学药学院,河北省药物质量分析控制重点实验室,河北保定071002

出　　处：《河北大学学报（自然科学版）》2009年第5期507-510,共4页Journal of Hebei University(Natural Science Edition)

基　　金：河北省科技攻关项目(06276479B,07276407D)

摘　　要：用小鼠移植性肿瘤法对6-F硫色烯并[4,3-c]吡唑啉(Ja)进行体内抗肿瘤活性研究.通过检测其对小鼠H22肝癌细胞、S180肿瘤细胞的体内抑瘤作用,计算肿瘤抑制率和生命延长率,并与阳性药顺铂做比较.结果表明,该化合物可抑制H22肝癌细胞皮下移植瘤的生长,在剂量为1,2,4 mg/(kg.d)时,腹腔注射给药抑瘤率分别为13.93%,37.49%,47.45%;而以剂量为5,10,20 mg/(kg.d)灌胃给药时,抑瘤率分别为31.53%,43.77%,50.73%;另外,该化合物可明显延长S180腹水瘤小鼠存活时间,以剂量为5,10,20 mg/(kg.d)灌胃给药时实验测得生命延长率分别为30.4%,64.7%,88.2%.该化合物有较强的体内抗肿瘤活性,对其抗癌作用机制值得进行深入研究.The antitumor effect of 6-fluoro-thiochromene[4,3-c]pyrazoline（Ja）in vivo was studied in mice with subcutaneous inoculation of the tumor cells.Through observing the inhibitory effects in vivo of Ja on H22 and S180 tumors,tumor growth inhibition rates and the rates of survival prolongation were calculated,and contrasting with positive control drug DDP.The results showed the compound inhibited the growth of implanted solid tumor H22 and prolonged live time implanted ascitic tumor S180 of mice in a dose-dependent manner.At the dose of 1,2,and 4 mg/（kg·d）（i.p.） and 5,10,and 20 mg/（kg·d）（i.g.）,the inhibition rates of Ja on H22 tumor in 3 repeated experiments were 13.93%,37.49%,47.45% and 31.53%,43.77%,50.73% respectively,and the rates of survival prolongation of the tumor-bearing mice were 30.4%,64.7% and 88.2% at the dose of 5,10,and 20 mg/（kg·d）（i.g.）,respectively.The compound which possesses obvious antitumor activity in vivo deserves further research on its antitumor-mechanism.

关 键 词：6-F硫色烯并[4 3-c]吡唑啉 鼠肝癌H22移植瘤 S180腹水瘤 顺铂 

分 类 号：R979.1[医药卫生—药品]