埃贝内酯B通过抑制一种尿羧肽酶Y样激肽酶对麻醉大鼠的利尿和利钠作用。
Diuretic and natriuretic effect of ebelactone B in anesthetized rats by inhibition of a urinary carboxypeptidase Y-like kininase.
作者信息
Majima M, Kuribayashi Y, Ikeda Y, Adachi K, Kato H, Katori M, Aoyagi T
机构信息
Department of Pharmacology, Kitasato University School of Medicine, Kanagawa, Japan.
出版信息
Jpn J Pharmacol. 1994 May;65(1):79-82. doi: 10.1254/jjp.65.79.
Ebelactone B (EB) (10(-7)-10(-5) M) inhibited dose-dependently carboxypeptidase (CP) Y-like exopeptidase, one of the major kininases separated from rat urine, whereas it inhibited neither CPA, CPB or neutral endopeptidase (NEP). Degradation of bradykinin (BK) to BK-(1-8) in rat urine was completely inhibited by EB (10(-5) M) with the increased generation of BK-(1-7). Intraduodenal administration of EB (3 mg/kg) to anesthetized rats caused marked diuresis (by 110%) and natriuresis (130%), in parallel with the increase in urinary kinin levels (110%). Intravenous infusion of a BK antagonist, Hoe140 (3 mg/kg/hr), strongly blocked both EB-induced diuresis and natriuresis. EB may be a novel type of diuretic and natriuretic agent that acts by increasing urinary kinin levels.
埃贝内酯B（EB）（10⁻⁷ - 10⁻⁵ M）剂量依赖性地抑制羧肽酶（CP）Y样外肽酶，这是从大鼠尿液中分离出的主要激肽酶之一，而它对CPA、CPB或中性内肽酶（NEP）均无抑制作用。EB（10⁻⁵ M）完全抑制了大鼠尿液中缓激肽（BK）降解为BK - (1 - 8)，同时BK - (1 - 7)的生成增加。对麻醉大鼠十二指肠内给予EB（3 mg/kg）可引起显著的利尿（增加110%）和利钠（增加130%），同时尿激肽水平升高（增加110%）。静脉输注BK拮抗剂Hoe140（3 mg/kg/小时）可强烈阻断EB诱导的利尿和利钠作用。EB可能是一种新型的利尿和利钠剂，其作用机制是通过增加尿激肽水平。
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