Baskova I P, Khalil S, Nikonov G I, Rabinovich S E, Nartikova V F
Biokhimiia. 1988 Sep;53(9):1467-73.
It has been shown for the first time that the salivary gland secretion of the medicinal leech (Hirudo medicinalis) contains a human blood plasma kallikrein inhibitor which is capable of blocking the amidolytic activity of the enzyme in an irreversible manner (with D-Pro-Phe-Arg-pNA as substrate) and which also suppresses the kininogenase activity of kallikrein. The inhibition of the amidolytic activity of highly purified kallikrein preparations from human blood plasma obeys the pseudo-first order kinetics. The experimental results suggest that in the salivary-gland secretion of H. medicinalis the inhibitor concentration exceeds by one order of magnitude that in whole leech homogenate extracts, which indicates that the inhibitor biosynthesis may be localized in leech salivary glands.
首次表明，药用水蛭（医蛭）的唾液腺分泌物含有一种人血浆激肽释放酶抑制剂，该抑制剂能够以不可逆的方式阻断该酶的酰胺水解活性（以D-脯氨酸-苯丙氨酸-精氨酸-对硝基苯胺为底物），并且还能抑制激肽释放酶的激肽原酶活性。对来自人血浆的高度纯化的激肽释放酶制剂的酰胺水解活性的抑制遵循假一级动力学。实验结果表明，在医蛭的唾液腺分泌物中，抑制剂浓度比整个水蛭匀浆提取物中的浓度高出一个数量级，这表明抑制剂的生物合成可能定位于水蛭的唾液腺中。
