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咔啉抗丝虫药:对卡里尼丝虫雌性虫体碳水化合物代谢酶的影响。

Carboline antifilarials: effects on carbohydrate metabolising enzymes in Litomosoides carinii female.

作者信息

Bose C, Agarwal S K, Chatterjee R K, Srivastava V M

机构信息

Division of Biochemistry, Central Drug Research Institute, Lucknow, India.

出版信息

Indian J Exp Biol. 1994 Jun;32(6):431-3.

PMID:7959914
Abstract

Two antifilarial compounds, viz., 90/55 (7-oxo-1-phenyl-8, 14-dihydropyrido (3,4-b) imidazo (1,2-c) quinazolo (4,5-g) and 87/639 (6-Nitro-1-phenyl-9H-pyrido (3,4-b) indole at 0.5 and 2.0 micron concentrations substantially inhibited glucose uptake and increased lactate production by L. carinii during in vitro incubation for 2 hr. The treated parasites, showed increased activities of glycogen phosphorylase, phosphofructokinase and pyruvate kinase. Hexokinase and fumarate reductase activities level in the worms were significantly lowered. Therefore it appears that both the compounds kill adult L. carinii by interfering with its carbohydrate metabolism.

摘要

两种抗丝虫化合物,即90/55(7-氧代-1-苯基-8,14-二氢吡啶并[3,4-b]咪唑并[1,2-c]喹唑啉[4,5-g])和87/639(6-硝基-1-苯基-9H-吡啶并[3,4-b]吲哚),在0.5和2.0微米浓度下,在体外孵育2小时期间,能显著抑制卡氏肺孢子虫对葡萄糖的摄取并增加乳酸生成。经处理的寄生虫,糖原磷酸化酶、磷酸果糖激酶和丙酮酸激酶的活性增加。蠕虫中的己糖激酶和延胡索酸还原酶活性水平显著降低。因此,似乎这两种化合物都是通过干扰其碳水化合物代谢来杀死成年卡氏肺孢子虫的。

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