Kim R A, Lukacs J, Tanaka R D, MacInnis A J
J Parasitol. 1981 Feb;67(1):20-3.
The effects of hycanthone and praziquantel on the activities of monoamine oxidases and cholinesterases were studied in the 600-g supernatant from homogenates of Schistosoma mansoni and mouse liver or brain. Hycanthone was shown to be a very potent inhibitor of monoamine oxidases from worms and mouse liver. Hycanthone also inhibited the specific and nonspecific cholinesterases of S. mansoni, but cholinesterase from mouse brain was not affected significantly by this drug. Praziquantel showed no effect on monoamine oxidase from mouse liver or the parasite; however, it was slightly inhibitory to S. mansoni cholinesterases at very high concentrations. Mouse brain cholinesterase required an even higher concentration of praziquantel to observe inhibition. The inhibition of monoamine oxidase in S. mansoni by hycanthone adds a new mode of action to our knowledge of this compound, and suggests another possibility for the development of future anthelminthics.
在曼氏血吸虫、小鼠肝脏或脑匀浆的600g上清液中,研究了羟氨喹和吡喹酮对单胺氧化酶及胆碱酯酶活性的影响。结果表明,羟氨喹是蠕虫和小鼠肝脏单胺氧化酶的强效抑制剂。羟氨喹还抑制曼氏血吸虫的特异性和非特异性胆碱酯酶,但该药物对小鼠脑胆碱酯酶无显著影响。吡喹酮对小鼠肝脏或寄生虫的单胺氧化酶无作用;然而,在非常高的浓度下,它对曼氏血吸虫胆碱酯酶有轻微抑制作用。小鼠脑胆碱酯酶需要更高浓度的吡喹酮才能观察到抑制作用。羟氨喹对曼氏血吸虫单胺氧化酶的抑制作用为我们对该化合物的认识增添了一种新的作用方式,并为未来抗蠕虫药的开发提出了另一种可能性。