Estambale B B, Howells R E
Department of Medical Microbiology, College of Health Sciences, University of Nairobi, Kenya.
Zentralbl Bakteriol. 1989 Jul;271(2):249-55. doi: 10.1016/s0934-8840(89)80080-5.
An in vitro study of the antinematodal action of two groups of compounds which act on the receptor complex of the inhibitory neurotransmitter, Gamma-aminobutyric acid (GABA) in mammalian systems is described. The compounds, Ivermectin and two benzodiazepines, Diazepam and a water soluble Midazolam were tested singly or in combination against two microfilarial parasites Onchocerca lienalis (closely related to Onchocerca volvulus) and Brugia pahangi. The combination of ivermectin and diazepam at a concentration of 0.1 microgram/ml and 33 micrograms/ml respectively achieved the same effect on microfilarial motility as when ivermectin was given at 1 microgram/ml alone or diazepam at 66 micrograms/ml alone. Similarly when the combination of ivermectin at 0.1 microgram/ml and midazolam at 10 micrograms/ml was used it achieved the same effect as ivermectin at 1 microgram/ml alone or midazolam at 33 micrograms/ml alone. This showed that both benzodiazepines had a synergistic effect on the activity of ivermectin. The microfilariae of B. pahangi were insensitive to both groups of compounds at all concentrations used.
本文描述了两组作用于哺乳动物系统中抑制性神经递质γ-氨基丁酸(GABA)受体复合物的化合物的抗线虫作用的体外研究。这些化合物,伊维菌素和两种苯二氮䓬类药物,地西泮和水溶性咪达唑仑,分别单独或联合测试对两种微丝蚴寄生虫,盘尾丝虫(与盘尾丝虫密切相关)和彭亨布鲁线虫的作用。伊维菌素和地西泮分别以0.1微克/毫升和33微克/毫升的浓度组合,对微丝蚴运动的影响与单独给予1微克/毫升伊维菌素或66微克/毫升地西泮时相同。同样,当使用0.1微克/毫升伊维菌素和10微克/毫升咪达唑仑的组合时,其效果与单独使用1微克/毫升伊维菌素或33微克/毫升咪达唑仑相同。这表明两种苯二氮䓬类药物对伊维菌素的活性具有协同作用。在所有使用的浓度下,彭亨布鲁线虫的微丝蚴对这两组化合物均不敏感。