Morise T, Okamoto S, Takasaki H, Ikeda M, Takeda R, Kiuti F, Tuda Y
Second Department of Internal Medicine, School of Medicine, Kanazawa University, Japan.
Jpn Circ J. 1988 Nov;52(11):1309-16. doi: 10.1253/jcj.52.1309.
In order to study the biological activity of endogenous digitalis-like substance (DLS) and Na-K-ATPase inhibitor (ATPI), human urine was partially purified and administered to rats, and its effects on the urinary volume, urinary Na excretion and blood pressure (BP) were determined. In addition, the effect on myocardial Na-K-ATPase activity was also measured. After the extraction of 40L of urine with a reversed phase cartridge column (S-fraction), 20 ml of chloroform was added and extraction was repeated. The chloroform layer was applied to an open silica gel column, and at a fraction with ethylacetate: methanol (60: 40, T-1 fraction), DLS and ATPI were eluted at the highest concentration. The water layer was treated with charcoal (D-1 fraction). The acute administration of K-1, T-1 fraction to rats in vivo caused significant rises in urinary volume, urinary Na excretion and BP. In chronic administration of K-1 fraction, urinary Na excretion was significantly elevated and myocardial Na-K-ATPase activity was also significantly suppressed. These results suggest that DLS and ATPI cause increase in the urinary volume and urinary Na excretion and also possess a hypertensive action; and moreover, these substance may affect the heart like cardiotonic steroids and regulate BP by increasing cardiac contractility.
为研究内源性洋地黄样物质（DLS）和钠钾ATP酶抑制剂（ATPI）的生物活性，将人尿进行部分纯化后给予大鼠，并测定其对尿量、尿钠排泄及血压（BP）的影响。此外，还测量了其对心肌钠钾ATP酶活性的影响。用反相柱（S组分）提取40L尿液后，加入20ml氯仿并重复提取。将氯仿层应用于开放硅胶柱，在乙酸乙酯：甲醇（60:40，T-1组分）的馏分中，DLS和ATPI以最高浓度洗脱。水层用活性炭处理（D-1组分）。对大鼠体内急性给予K-1、T-1组分可导致尿量、尿钠排泄及血压显著升高。慢性给予K-1组分时，尿钠排泄显著升高，心肌钠钾ATP酶活性也显著受到抑制。这些结果表明，DLS和ATPI可导致尿量和尿钠排泄增加，且具有升压作用；此外，这些物质可能像强心甾体一样影响心脏，并通过增加心肌收缩力来调节血压。
