Hill H Z, Backer R, Hill G J
Biopharm Drug Dispos. 1980 Apr-Jun;1(4):211-20. doi: 10.1002/bdd.2510010409.
Oral doses of amygdalin and intraperitoneal (i.p.) doses of potassium cyanide (KCN) in the near-lethal range were administered to CD2F1 female mice. Blood cyanide levels were then measured as a function of time. The maximum cyanide level after amygdalin administration was reached at about 11/2 to 2 h and was within the range of values seen after KCN administration. Behaviour of mice correlated with the time of maximum blood cyanide level. Acute distress was observed at times when the cyanide level was highest. There was great variability in the nature and magnitude of the response in individual mice. The ability of the contents of various regions of the gastrointestinal tract and of tumour tissue to release cyanide from amygdalin was assessed. Stomach and upper intestine had little activity while the lower end and the faeces released large amounts. Again, there was a large variation between mice. These results are interpreted to mean that enteric contents are primarily responsible for the release of cyanide from ingested amygdalin. Freshly minced tumour tissue released negligible amounts of cyanide. Ten-fold higher doses of amygdalin administered i.p. produced very small increases in blood cyanide levels and no toxic behaviour. The doses used are comparable to doses which might be ingested by patients receiving oral amygdalin or Laetrile and indicate that oral amygdalin is potentially extremely dangerous.
给CD2F1雌性小鼠口服苦杏仁苷,并腹腔注射接近致死剂量的氰化钾(KCN)。然后测定血氰水平随时间的变化。口服苦杏仁苷后的最大氰化物水平在约1.5至2小时达到,且处于注射KCN后所见的值范围内。小鼠的行为与血氰水平最高的时间相关。在氰化物水平最高时观察到急性痛苦。个体小鼠的反应性质和程度存在很大差异。评估了胃肠道不同区域的内容物以及肿瘤组织从苦杏仁苷中释放氰化物的能力。胃和上肠道几乎没有活性,而下端和粪便释放大量氰化物。同样,小鼠之间也存在很大差异。这些结果被解释为意味着肠道内容物是摄入的苦杏仁苷释放氰化物的主要原因。新鲜切碎的肿瘤组织释放的氰化物量可忽略不计。腹腔注射剂量比口服剂量高10倍的苦杏仁苷只会使血氰水平略有升高,且没有出现毒性行为。所使用的剂量与接受口服苦杏仁苷或莱特瑞尔的患者可能摄入的剂量相当,表明口服苦杏仁苷具有潜在的极大危险性。