Satoh K, Yasuda I, Nagai F, Ushiyama K, Akiyama K, Kano I
Department of Toxicology, Tokyo Metropolitan Research Laboratory of Public Health, Japan.
Yakugaku Zasshi. 1991 Feb;111(2):138-45. doi: 10.1248/yakushi1947.111.2_138.
In the folk-medicine, several kinds of crude drugs are used as diuretics. Twenty three kinds of diuretic drugs were chosen, and examined for their effects on the horse kidney (Na+ + K+)-adenosine triphosphatase (ATPase), which is an intrinsic enzyme of the plasma membrane and responsible for the active transport of Na+ and K+ across the membrane. Twenty one out of twenty three kinds of ethanol extracts of diuretic drugs inhibited the kidney (Na+ + K+)-ATPase activity. The intensity of the inhibition of these drugs was compared by estimating the amounts of their ethanol extracts which inhibited the (Na+ + K+)-ATPase activity by 50% (I50, micrograms/ml). Among these drugs, Atractylodis Lanceae Rhizoma (I50 = 12.8) Atractylodis Rhizoma (I50 = 15.2), Plantaginis Semen (I50 = 16.0), Plantaginis Herba (I50 = 16.0) and Alismatis Rhizoma (I50 = 22.0), have strong inhibitory effects on the kidney (Na+ + K+)-ATPase activity. The ethanol extracts of the rhizomes of Atractylodes lancea De Candolle and Atractylodis japonica Kitamura were examined with varying concentrations of ATP and ouabain. The mode of inhibition of these two extracts on the (Na+ + K+)-ATPase activity appeared to be uncompetitive with respect to ATP as judged from Lineweaver-Burk plot. The ethanol extract of Atractylodes japonica Kitamura decreased the I50 for ouabain from 1.6 x 10(-7) to 7.0 x 10(-9) M, while that of Atractylodes lancea De Candolle did not change the I50 for ouabain.
在民间医学中,有几种天然药物被用作利尿剂。选择了23种利尿药物,并检测它们对马肾(Na⁺ + K⁺)-腺苷三磷酸酶(ATP酶)的作用,该酶是质膜的一种固有酶,负责Na⁺和K⁺跨膜的主动转运。23种利尿药物的乙醇提取物中有21种抑制了肾(Na⁺ + K⁺)-ATP酶活性。通过估计使(Na⁺ + K⁺)-ATP酶活性抑制50%(I50,微克/毫升)的乙醇提取物的量来比较这些药物的抑制强度。在这些药物中,茅苍术根茎(I50 = 12.8)、白术根茎(I50 = 15.2)、车前子(I50 = 16.0)、车前草(I50 = 16.0)和泽泻根茎(I50 = 22.0)对肾(Na⁺ + K⁺)-ATP酶活性有很强的抑制作用。用不同浓度的ATP和哇巴因检测了茅苍术根茎和北苍术根茎的乙醇提取物。根据Lineweaver-Burk图判断,这两种提取物对(Na⁺ + K⁺)-ATP酶活性的抑制模式对ATP似乎是非竞争性的。北苍术根茎的乙醇提取物使哇巴因的I50从1.6×10⁻⁷降至7.0×10⁻⁹M,而茅苍术根茎的乙醇提取物则未改变哇巴因的I50。