安吖啶的抗癌效价

THE EXPERIMENTAL ANTITUMOR ACTIVITY OF AMSACRINE

体外实验中观察了本院合成的安吖啶对3株肿瘤细胞的抗癌作用.结果表明,安吖啶对L_(1210)细胞及2株人肿瘤细胞HEP及HCE均具有较强的抗癌效果.对L_(1210)细胞的杀伤效果最强,杀死1或2个log(即杀死90%和99%)瘤细胞的浓度依次为0.08及0.25μg/ml,对HCE和HEP细胞杀死1个log细胞的浓度分别为0.98及1.25μg/ml.体内实验证明本药对小鼠实体瘤S_(180)及腹水瘤L_(1210)均具有较好疗效.1～3mg/kg每天腹腔注射1次连续6天,可使荷腹水型L_(1210)瘤小鼠的活存时间较对照组延长193～214%,对S_(180)实体瘤生长的抑制率可达47～85%.与美国国立肿瘤研究所赠送的标准品NSC-249992作了比较,证明二者的抗癌效价相似.

The in vitro antitumor activity of amsacrine synthesized in our academy was investigated in three tumor cell lines.The data obtained showed that amsacrine possessed significant antitumor activity against L1210 cells and two human tumor cell lines,HEP and HCE.In the experiments of L1210 cells amsacrine showed particularly strong cytotoxicity,the concentrations for 1 or 2 log cell kills were 0.08 and 0.25μg/ml respectively.For HEP and HCE cells,the concentrations for 1 log cell kill were 0.98 and 1.25μg/ml respectively.In tumor-bearing mice amsacrine also showed significant antitumor activity.Giving ip it was quite effective in treating L1210 ascitic tumor with the median survival time increased 193 -214% as compared with the control.Amsacrine also significantly inhibited S180,the tumor growth was inhibited by 47-85%,as compared with the control animals.The above data indicated that this compound possessed the same antitumor activity as NSC-249992 （am sacrine synthesized in National Cancer Institute of the United States）.