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邻脂苯芥实验室编号为AT-581,是一个新的氮芥化合物,化学名为:邻双(2-氯乙基)氨甲基-苯丙氨酸二盐酸盐.本工作进一步研究了该药对家免Brown-Pearce癌的疗效和对细胞核分裂及一般形态的影响.获得的结果如下:(1)以Brown-Pearce癌组织匀浆或瘤块接种于家兔眼前房,3天后开始以AT-581治疗.静脉注射0.7毫克/公斤时,肿瘤重量抑制率为48-78％,疗效非常显著.眼内注射0.015,0.03和0.06毫克/每眼时,肿瘤重量抑制率分别为57,61和63％,与对照组比较,差异非常显著。(2)用AT-581 0.7毫克/公斤/天静脉注射3和7天,能使癌细胞核分裂指数减低,对分裂象各期也有抑制作用.其中以注射7天组的作用最明显.癌细胞一般形态的改变包括细胞排列紊乱和体积缩小,核固缩、破裂和出现癌组织的大批坏死.(3)一次静脉注射AT-581,小剂量时先呈现刺激细胞生长的作用,继之出现强烈的抑制效能.大剂量时一开始就出现核分裂抑制,各期分裂象明显下降和细胞体积缩小.
Ophthalmic laboratory is AT-581, a new nitrogen mustard compound with the chemical name: o-bis (2-chloroethyl) aminomethyl-phenylalanine dihydrochloride. This work was further studied The efficacy of the drug on Brown-Pearce cancer-free and its effect on the mitosis and general morphology of the patients were studied.The results are as follows: (1) Brown-Pearce cancer tissue homogenate or tumor mass was inoculated into the anterior chamber of rabbits, Began to AT-581 treatment.Intravenous injection of 0.7 mg / kg, the tumor weight inhibition rate of 48-78%, the effect is very significant intraocular injection of 0.015,0.03 and 0.06 mg / eye, the tumor weight inhibition rates were 57 , 61 and 63%, respectively, compared with the control group, the difference was significant. (2) The AT-581 0.7 mg / kg / day intravenous injection of 3 and 7 days, can reduce the mitotic index of cancer cells, the division of all stages also have an inhibitory effect in which the injection of 7 days group the most obvious role .Cancer cells General morphological changes include disarranged cells and reduced volume, nuclear pyknosis, rupture and a large number of necrosis of cancerous tissue. (3) A single intravenous injection of AT-581, the role of stimulating cell growth at low doses, followed by strong Inhibition of high-dose at the beginning of the occurrence of mitotic inhibition, schizonts significantly decreased the size and cell size decreased.