γ-氨基丁酸（GABA）和1,3-二棕榈酰-2-（4-氨基丁酰基）甘油盐酸盐（一种甘油二酯前药）杀丝虫活性的体外评估
In-vitro evaluation of filaricidal activity of GABA and 1,3-dipalmitoyl-2-(4-aminobutyryl)glycerol HCl: a diglyceride prodrug.
作者信息
Deverre J R, Loiseau P, Couvreur P, Letourneux Y, Gayral P, Benoit J P
机构信息
Laboratoire de Pharmacie Galénique et de Biopharmacie, UA CNRS, Université de Paris XI, Chatenay-Malabry, France.
出版信息
J Pharm Pharmacol. 1989 Mar;41(3):191-3. doi: 10.1111/j.2042-7158.1989.tb06428.x.
A diglyceride ester of gamma-aminobutyric acid (GABA) has been synthesized and its filaricidal activity compared with GABA, and progabide in-vitro, on infective larvae and microfilariae of Molinema dessetae, a rodent filaria. GABA induced paralysis in infective larvae but was inactive on microfilariae. There were interactions between the culture medium and GABA. The ester drug at 0.1 mmol L-1 (1,3-dipalmitoyl-2-(4-aminobutyryl)glycerol HCl) was as active as progabide on infective larvae and hundredfold more potent than GABA. Its microfilaricidal activity at 1 mmol L-1 was lower than that progabide at 0.1 mmol L-1 but a delayed effect was observed. The data confirm filariae sensitivity to GABA derivatives.
已合成γ-氨基丁酸（GABA）的甘油二酯，并将其杀丝虫活性与GABA和普罗加比进行体外比较，以研究其对啮齿动物丝虫——德氏莫林线虫的感染性幼虫和微丝蚴的作用。GABA可使感染性幼虫麻痹，但对微丝蚴无活性。培养基与GABA之间存在相互作用。酯类药物在0.1 mmol/L（1,3-二棕榈酰-2-(4-氨基丁酰)甘油盐酸盐）时对感染性幼虫的活性与普罗加比相当，且比GABA强百倍。其在1 mmol/L时的杀微丝蚴活性低于0.1 mmol/L的普罗加比，但观察到有延迟效应。数据证实丝虫对GABA衍生物敏感。
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