Overlack A, Scicli A G, Carretero O A
Am J Physiol. 1983 Jun;244(6):G689-94. doi: 10.1152/ajpgi.1983.244.6.G689.
We studied the possibility of intestinal absorption of glandular kallikrein in unanesthetized rats after administration of 5 mg of active or phenylmethylsulfonyl fluoride-inactivated pig pancreatic kallikrein (PPK). Immunoreactive PPK was measured in plasma and urine by radioimmunoassay using an antiserum to PPK that does not cross-react with rat glandular kallikrein. In addition, we studied the effect of intestinally administered active PPK on the intestinal blood flow distribution. Although immunoreactive PPK could not be detected (less than 10 ng/ml) in plasma after active PPK was administered, very small amounts were found in urine (20-40 ng/3 h). In the urine most of the PPK was in active form because over 75% could be bound to aprotinin-Sepharose. After inactive PPK was administered, immunoreactive PPK was detectable in the plasma of all rats, and urinary excretion was higher than after administration of active PPK. Blood flow distribution to the small intestine as a percentage of cardiac output was significantly greater 30 min after intestinal application of active PPK (5 mg) than after administration of the vehicle alone (1 ml of 0.9% saline). These results suggest that active and inactive PPK is absorbed from the gut in very small amounts. The finding of higher amounts of immunoreactive PPK in plasma and urine after inactive PPK was administered is probably due to the fact that the inactive form of the enzyme is not bound by the plasma inhibitors. These small amounts of kallikrein absorbed appear to have some effect on intestinal blood flow distribution.
我们研究了在未麻醉的大鼠中,给予5毫克活性或苯甲基磺酰氟灭活的猪胰激肽释放酶(PPK)后,其肠道吸收的可能性。使用与大鼠腺体激肽释放酶无交叉反应的抗PPK血清,通过放射免疫测定法测量血浆和尿液中的免疫反应性PPK。此外,我们研究了肠道给予活性PPK对肠道血流分布的影响。虽然给予活性PPK后血浆中未检测到免疫反应性PPK(低于10纳克/毫升),但在尿液中发现了极少量(20 - 40纳克/3小时)。尿液中的大多数PPK呈活性形式,因为超过75%可与抑肽酶 - 琼脂糖结合。给予灭活的PPK后,所有大鼠的血浆中均可检测到免疫反应性PPK,且尿排泄量高于给予活性PPK后。肠道应用活性PPK(5毫克)后30分钟,小肠血流分布占心输出量的百分比显著高于单独给予载体(1毫升0.9%盐水)后。这些结果表明,活性和灭活的PPK均以极少量从肠道吸收。给予灭活的PPK后血浆和尿液中免疫反应性PPK含量较高,这可能是由于酶的无活性形式未被血浆抑制剂结合。吸收的这些少量激肽释放酶似乎对肠道血流分布有一定影响。