棉鼠丝虫动物模型应用于药物筛选

为了寻找新的口服抗丝虫药物,1972年从国外引进棉鼠、棉鼠丝虫和柏氏禽剌螨后在我所建立了棉鼠丝虫动物模型,并开展了药物筛选工作。几年来筛选已知的和新合成的化合物共150个以及中草药7个。有14个化合物对棉鼠丝虫微丝蚴和/或成虫具有明显的杀死作用。其中硝硫氰胺、氨硝喹唑啉、呋喃西林、6-对氨基苯基-2,3,5,6-四氢咪唑并(2,1-6)噻唑-盐酸盐、2-(4-蜜胺2-基苯基)-4-羟甲基-1,3-二噻砷环戊烷和5个2-2-(5-硝基呋喃-2)乙烯-1]-1,3,4-(口恶)二唑-5-酮的衍生物的作用较显著,尤其是对成虫。本文也报道了用棉鼠丝虫动物模型进行药物筛选的有关实验方法以及棉鼠体内的微丝蚴和成虫的消长。

DRUG SCREENING WITH THE COTTON-RAT MODEL OF FILARIASIS

For the purpose of screening new oral filaricides, cotton rat filaria model consisting of cotton rats (Sigrnodon hispidus) infected with Litomosoides carinii, and rat mites (Ornithonyssus bacoti) were introduced in 1972 through the courtesy of Dr. E. Friedheim. Since then, the model has been well mainteined in our Institute and fully utilized by other institutions.During the past five years, 150 known or newly synthesized compounds and 7 medicinal herbs had been screened. 14 compounds showed obvious microfilaricidal and/or macrofilaricidal effects, among them 4-isothiocyanato-4'-nitrodiphenylamine, 2, 4-diamino-6-(3,4-dichloro-benzyl) nitrosamino] quinazoline acetate, Furacilin, 2-(4-melamin-2-ylphenyl)-4-hydroxymethyl-1, 3-dithia-arsolane (syn, Melarsoprol, Arsobal, Mel B), 6-P-nitro-phenyl-2, 3, 5, 6-tetrahydroimidazol-(2, 1-b) thiazole and five derivatives of 2-2-(5-nitrofuryl-2) vinyl-1]-1, 3, 4-oxadiazole-5-one were more outstanding, especially as macrofilaricides.The experimental methods pertinent to the drug screening and the variation of microfilaria and adult worm counts in cotton rats are described.