Umezawa H
Int J Clin Pharmacol Ther Toxicol. 1982 Jan;20(1):19-23.
A screening method to identify microbial products that bind to surfaces of cells involved in immunity has been established. By means of this method, several small molecular weight compounds, bestatin, amastatin, forphenicine, and esterastin, inhibiting enzymes located on the cell surface, aminopeptidase B and leucine aminopeptidase, aminopeptidase A, alkaline phosphatase, and esterase, were discovered. These small molecular weight microbial products showed immunity-modifying activity. Among these, bestatin, which has an extremely low toxicity, was studied in detail. The clinical study indicated that bestatin enhances the cellular immunity in cancer patients. The use of small molecular weight immunomodifiers to annihilate minimal residual tumors in the lung is discussed.
已建立一种筛选方法,用于鉴定与免疫相关细胞表面结合的微生物产物。通过该方法,发现了几种抑制位于细胞表面的酶(氨基肽酶B和亮氨酸氨基肽酶、氨基肽酶A、碱性磷酸酶和酯酶)的小分子化合物,即抑氨肽酶素、氨肽菌素、甲磺酸酚妥拉明和酯抑素。这些小分子微生物产物具有免疫调节活性。其中,毒性极低的抑氨肽酶素得到了详细研究。临床研究表明,抑氨肽酶素可增强癌症患者的细胞免疫。本文还讨论了使用小分子免疫调节剂消灭肺部微小残留肿瘤的问题。