Komuro T, Kakimoto N, Katayama T, Hazato T
Biotechnol Appl Biochem. 1986 Oct;8(5):379-86.
Twenty-eight species of carboxyethyl germanium sesquioxide (Ge-132) derivatives were examined for their inhibitory effects on enkephalin-degrading enzymes that were purified from monkey brain, the longitudinal muscle layer of bovine small intestine, and human cerebrospinal fluid (CSF). A series of the sulfurized Ge-132 derivatives showed strong inhibition of these purified enzymes. The most effective ones were Ge-014 and Ge-107, which showed IC50 values of 60 and 100 micrograms/ml, respectively, for dipeptidylcarboxypeptidase from the longitudinal muscle layer. They also exhibited inhibitory activity against aminopeptidase from human CSF, the IC50 values being 450 and 440 micrograms/ml, respectively. Furthermore, these compounds showed inhibition of dipeptidylaminopeptidase from monkey brain and the longitudinal muscle layer of bovine small intestine. These compounds are expected to have analgesic effects due to their inhibition of the degradation of endogenous opioid peptides.
对28种羧乙基锗倍半氧化物（Ge-132）衍生物进行了研究，考察它们对从猴脑、牛小肠纵肌层及人脑脊液（CSF）中纯化得到的脑啡肽降解酶的抑制作用。一系列硫化Ge-132衍生物对这些纯化酶表现出强烈抑制作用。其中最有效的是Ge-014和Ge-107，它们对牛小肠纵肌层的二肽基羧肽酶的IC50值分别为60和100微克/毫升。它们对人脑脊液中的氨肽酶也表现出抑制活性，IC50值分别为450和440微克/毫升。此外，这些化合物对猴脑和牛小肠纵肌层的二肽基氨肽酶也有抑制作用。由于这些化合物抑制内源性阿片肽的降解，预计它们具有镇痛作用。
