新型抗肿瘤药槐定碱  

Sophoridine is a new antitumor medicine with new molecular structure

作　　者：李雪梅[1] 吴运光[1] 潘达鑫[1] 吴联奎[2] 余月华[1] 张爱华[2] 陈绍励[1] 管忠震[3] 杨秀玉[4] 

机构地区：[1]江西中医学院基础医学部,南昌330006 [2]江西省药物研究所,南昌330029 [3]中山大学肿瘤医院国家抗肿瘤药物临床试验研究中心,广州510060 [4]北京协和医院,北京100730

出　　处：《中国新药杂志》2006年第8期654-657,共4页Chinese Journal of New Drugs

基　　金："九五"国家科技攻关计划"新药研究与产业化开发"(1035工程)项目(96-901-01-48)

摘　　要：目的:槐定碱是从苦豆子中提取的单体生物碱。纯度高达99．50%以上。研究表明,其对动物移植瘤S-180等有30％～60％稳定的抑癌率;对癌细胞有一定直接杀伤作用;能影响癌细胞周期的G1和G2期,减少其增殖,并引起癌细胞凋亡;对癌细胞TOPO异构酶Ⅰ有抑制作用。体内过程符合二房室模型,分布广泛迅速,消除迅速,以原型经肾脏排泄。临床对恶性滋养细胞肿瘤有显著疗效,对恶性淋巴瘤和消化道肿瘤也有一定疗效,且毒性较低。Sophoridine extracted from the Sophora alopecuroides with the purity of 99.5% take effect of antitumor in those mice bearing Lewis Lung Carcinoma （LLC）,S180, U14 and ECA etc, the rates of inhibition between 30 -60% in vivo. It can kill the cancer cell directly and disturb the G1 stage and G2 stage of the proliferation cycle. It also has influence on apoptosis and can inhibit the activities of TOPO Ⅰ enzyme. Sophoridine is well absorpted quickly and distributed, excreted unchanged by glomerular filtration. It exhibits kinetic patterns that is consistent with two compartment model. The notable effect of Sophoridine in human gestational trophoblastic disease （GTD） , and moderate effect of it in lymphosorcoma and gastrointestinal tumor were approved by clinical research from the hospitals. Enough evidence showed that Sophoridine is lower in toxicity and no marked effect on main organs and born marrow of rats and patient were noticed. Beside, hematogenic function of born marrow work properly. The side effect mainly involves the nervous system.

关 键 词：槐定碱 抗肿瘤药 喹诺里西啶生物碱 

分 类 号：R979.1[医药卫生—药品] R282.71[医药卫生—药学]