土青木香降压成分——广玉兰碱的药理作用
PHARMACOLOGICAL STUDIES ON MAGNOFLORINE,A HYPOTENSIVE PRINCIPLE FROM TU QING MU XIANG
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摘要: 自土青木香中提出的广玉兰碱具有如下的药理作用:(1)麻醉猫静脉注射2毫克/公斤,降压达50—60%,持续90—120分钟;口服20—40毫克/公斤,也可得到与静脉注射相近的降压效果,不过作用发生较慢,而持续较久。(2)不麻醉动物:大白鼠腹腔注射20—40毫克/公斤,平均降压30%,持续达90分钟左右;口服100毫克/公斤,降压平均24%,持续时间120分钟;口服200毫克/公斤降压34.6%,持续135分钟,对肾性高血压犬,6毫克/公斤静脉注射,也有明显的降压作用,对舒张压的作用尤为明显。(3)广玉兰碱不具M-胆碱样作用,对N-胆碱反应系统尤以神经节有显著的阻断作用,但较C6为弱;有微弱的箭毒样作用;对肾上腺素反应系统没有阻断作用,所以广玉兰碱的降压作用与神经节阻断作用有密切关系。此外,对颈总动脉阻断,电刺激坐骨神经向中端的加压反应均有抑制现象。(4)小白鼠一次静脉注射的LD50为0.02克/公斤;长期口服其10倍剂量,并无明显的慢性毒性。根据家兔背部皮内试验,广玉兰碱用至10%的浓度,并无刺激现象。Abstract: Magnoflorine (Mf) a quaternary ammonium base, has been isolated from the Chinese herb Tu Qing Mu Xiang (roots of Aristolochia debilis Sieb. et Zucc.) as its hypotensive principle. The results of our pharmacological studies on this alkaloid are reported as follows: 1. In anesthetized cats intravenous injection of Mf (2mg/kg) produced a prompt and significant fall of the blood pressure, lasting about 1-2 hours. Oral administration (20, 40mg/kg) also resulted in hypotension (Fig. 1). 2. In unanesthetized rats and in a Goldblatt hypertensive dog, Mf injected either intraperitoneally or intravenously, also exhibited a hypotensive action (Fig. 2, 3). 3. Mf gave no noticeable effect on the M-cholinergic reactive system. It inhibited the N-cholinergic reactive system: its ganglionic blocking action being about half as active as that of hexamethonium (c6) (Fig. 6). Some curarelike action was also noticed (Fig. 8). On the adrenergic reactive system it showed practically no effect. The hypotensive action of Mf is, therefore, mainly associated with its ganglionic blockade. 4. The acute LD50 of Mf by intravenous injection in mice was 0.02 g/kg. Oral medication with a 10-fold dose daily for 4 weeks neither elicited any toxic symptoms nor retarded the growth.
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