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伪石蒜硷是从石蒜科植物水仙及石蒜中提得的生物硷。其游离硷及盐酸盐在动物耐受剂量下,对大鼠W-256的生长有明显的抑制作用,抑制率在49～76％之间,统计学上差异非常显著。对小鼠肝癌、艾氏腹水癌皮下型、S-180的抑制作用不明显。已测得伪石蒜硷对大鼠一次腹腔注射的LD_(50)为110(92.4～131)mg/kg。对猫静脉滴注可致缓慢血压下降,滴注致死要求很大剂量(平均881mg/kg)。根据推算现在的病人试用剂量(～1mg/kg/日)是安全的。狗的亚急性毒性试验表明,此药可引起恶心、呕吐、厌食,但对骨髓无明显抑制作用。用药后曾见血中非蛋白氮值上升,考虑为肾前因素引起。病理解剖心、肝、脾、肺、肾、肠各脏器均未见明显病变。药物正开始进行Ⅰ期临床试用中。
Pseudo-Lycoris alkaloids from the Amaryllidaceae Narcissus and Lycoris extracted alkaloids. The free base and hydrochloride showed a significant inhibitory effect on the growth of rat W-256 at animal tolerant doses, with a significant inhibition rate of 49-76%. On mouse liver cancer, Ehrlich ascites carcinoma subcutaneous, S-180 inhibition was not obvious. The LD_ (50) of pseudo-Lycorine in rats once peritoneal injection has been measured to be 110 (92.4 ~ 131) mg / kg. Intravenous drip can cause slow blood pressure drops, intravenous infusion requires a very large dose (average 881mg / kg). It is safe to base the current patient trial dose (~ 1 mg / kg / day). Subacute toxicity test dogs show that this medicine can cause nausea, vomiting, anorexia, but no significant inhibitory effect on the bone marrow. Have seen blood after treatment of non-protein nitrogen increased, consider the cause of prerenal factors. Pathological anatomy heart, liver, spleen, lung, kidney, intestine of the organs were no obvious lesions. Drugs are beginning Phase I clinical trials.