Chiou C Y
J Pharm Sci. 1977 Jun;66(6):837-41. doi: 10.1002/jps.2600660626.
The effect of bromoacetylcholine on mouse neuroblastoma C-1300 was investigated in cell culture as well as in A/J mice. In vitro, bromoacetylcholine (1 X 10(-5) M) was a potent cytolytic agent and produced an additive effect in combination with vincristine (3 X 10(-9) M). Since the choline acetyltransferase inhibitor, dimethylaminoethyl chloroacetate, does not inhibit neuroblastoma efficiently in vitro, the potent cytolytic action of bromoacetylcholine is probably not due to its choline acetyltransferase inhibitory action. Furthermore, the neuroblastoma inhibitory effect of bromoacetylcholine was not affected by atropine. Therefore, the inhibitory action is not related to the interaction of bromoacetylcholine with muscarinic receptors either. In in vivo experiments, 1, 10, or 30 mg/kg of bromoacetylcholine was injected directly into the tumors three times daily for 6 weeks. Bromoacetylcholine at 10 and 30 mg/kg gave significant protection of A/J mice from the death induced by neuroblastoma inoculation, and the lifespan was prolonged significantly with these bromoacetylcholine treatments.
在细胞培养以及A/J小鼠中研究了溴乙酰胆碱对小鼠神经母细胞瘤C-1300的作用。在体外,溴乙酰胆碱(1×10⁻⁵M)是一种强效细胞溶解剂,与长春新碱(3×10⁻⁹M)联合使用时产生相加作用。由于胆碱乙酰转移酶抑制剂氯乙酸二甲基氨基乙酯在体外不能有效抑制神经母细胞瘤,溴乙酰胆碱的强效细胞溶解作用可能不是由于其胆碱乙酰转移酶抑制作用。此外,溴乙酰胆碱对神经母细胞瘤的抑制作用不受阿托品影响。因此,该抑制作用也与溴乙酰胆碱与毒蕈碱受体的相互作用无关。在体内实验中,每天三次将1、10或30mg/kg溴乙酰胆碱直接注射到肿瘤中,持续6周。10和30mg/kg的溴乙酰胆碱能显著保护A/J小鼠免受神经母细胞瘤接种诱导的死亡,并且这些溴乙酰胆碱治疗显著延长了小鼠的寿命。