Simon O, Bohley P, Bergner H, Münchmeyer R
Arch Tierernahr. 1984 May-Jun;34(5-6):341-51. doi: 10.1080/17450398409425178.
Chymostatin is an effective inhibitor of intracellular proteinases in vitro. In the present experiment male rats were injected intraperitonealy during a 3 days period twice daily with a solution containing 0,9 mg Chymostatin per 100 g live weight. Reference animals received a control injection containing the same solvents but no chymostatin. During this period a daily nitrogen balance was made and metabolic faecal nitrogen and true digestibility of nitrogen were estimated using 15N-labelled animals. Furthermore, apparent biological half lives of proteins in liver and intestinal tissues were determined following the decay curves for radioactivity in proteins 48 hours after injection of L-[5-3H]-arginine und L-[guanido-14C]-arginine. The fractional rate of protein synthesis in tissues was measured by a 6 hours continuous infusion technique with L-[U-14C]-tyrosine and L-[U-14C]-leucine. Among the parameters estimated only the apparent biological half lives of proteins in liver and intestinal tissues were influenced by chymostatin. However, the prolonged half lives seemed to be rather an effect of an increased reutilisation of amino acids resulting from the intracellular protein breakdown than a decreased rate of protein degradation. The in vivo effect of the proteinase inhibitor was by far inferior compared with the action in vitro. Factors like distribution, degradation and excretion of the inhibitor could be responsible for the moderate in vivo action of chymostatin.
抑肽酶在体外是一种有效的细胞内蛋白酶抑制剂。在本实验中,雄性大鼠在3天内每天腹腔注射两次,每次注射含每100克体重0.9毫克抑肽酶的溶液。对照动物注射含有相同溶剂但不含抑肽酶的溶液。在此期间,每天进行氮平衡测定,并使用15N标记的动物估计代谢粪氮和氮的真消化率。此外,在注射L-[5-3H]-精氨酸和L-[胍基-14C]-精氨酸48小时后,根据蛋白质中放射性的衰减曲线测定肝脏和肠道组织中蛋白质的表观生物半衰期。通过用L-[U-14C]-酪氨酸和L-[U-14C]-亮氨酸进行6小时连续输注技术来测量组织中蛋白质合成的分数率。在所估计的参数中,只有肝脏和肠道组织中蛋白质的表观生物半衰期受抑肽酶影响。然而,半衰期延长似乎更多是由于细胞内蛋白质分解导致氨基酸再利用增加的结果,而不是蛋白质降解速率降低。与体外作用相比,蛋白酶抑制剂的体内作用要差得多。抑制剂的分布、降解和排泄等因素可能是抑肽酶体内作用适度的原因。