HAWKING F, SEN A B
Br J Pharmacol Chemother. 1960 Dec;15(4):567-70. doi: 10.1111/j.1476-5381.1960.tb00283.x.
Homidium, quinapyramine, and suramin (Group II compounds) produce their trypanocidal effect in vivo only after a latent period of 24 hr. or more, during which time the trypanosomes may continue to multiply; this is in contrast to trivalent arsenical and diamidine compounds (Group I compounds), which begin to act immediately. Group II compounds also differ from Group I compounds in that (a) they have only a slight tendency to combine with trypanosomes, (b) they have little trypanocidal action in vitro, but (c) they make trypanosomes non-infective to fresh subinoculated mice. To explain these features it is postulated that homidium, quinapyramine, and suramin first combine in small amounts with some receptor on the trypanosome and then block some biochemical system which produces a hypothetical substance X which is needed for cell division of the trypanosome; the trypanosome is supposed to contain a preformed store of this substance X sufficient for several divisions to take place; and it is only when this store is exhausted that cell division is prevented and the trypanosome eventually dies.
霍米啶、喹那嘧啶和苏拉明(第II组化合物)仅在24小时或更长的潜伏期后才在体内产生杀锥虫作用,在此期间锥虫可能会继续繁殖;这与三价砷化合物和双脒化合物(第I组化合物)形成对比,后者会立即起效。第II组化合物与第I组化合物的不同之处还在于:(a)它们与锥虫结合的倾向很小;(b)它们在体外几乎没有杀锥虫作用;但(c)它们会使锥虫对新接种的小鼠失去感染性。为了解释这些特征,有人提出霍米啶、喹那嘧啶和苏拉明首先会少量结合到锥虫上的某些受体上,然后阻断某个生化系统,该系统会产生锥虫细胞分裂所需的一种假定物质X;锥虫应该含有这种物质X的预先形成的储备,足以进行几次分裂;只有当这种储备耗尽时,细胞分裂才会被阻止,锥虫最终死亡。