一种丝氨酸蛋白酶抑制性苯甲脒衍生物可抑制人结肠癌细胞的生长。
A serine protease-inhibitory benzamidine derivative inhibits the growth of human colon carcinoma cells.
作者信息
Nishimura Y, Yasui W, Yoshida K, Matsuyama T, Dohi K, Tahara E
机构信息
First Department of Pathology, Hiroshima University School of Medicine.
出版信息
Jpn J Cancer Res. 1992 Jul;83(7):723-8. doi: 10.1111/j.1349-7006.1992.tb01972.x.
The inhibitory effect of a serine protease-inhibiting tetra-benzamidine derivative, TAPP-Br, on the cell growth of 8 human colon carcinoma cell lines was examined and the mechanism of the inhibition was analyzed. TAPP-Br inhibited the cell growth of all the colon carcinoma cell lines, and this effect was irreversible. The expression of mRNAs for nuclear oncogenes such as MYC, FOS and JUN was decreased by TAPP-Br after treatment for 3 h and the effect continued for 48 h. mRNA expression of epidermal growth factor receptor, transforming growth factor-beta and type IV collagenase was suppressed at 48 h after the initiation of TAPP-Br treatment, suggesting an indirect action of TAPP-Br. TAPP-Br decreased protein kinase C activity in the particulate fraction, whereas it increased the enzyme activity in the soluble fraction. These findings overall suggest that the serine protease inhibitor, TAPP-Br, might inhibit the cell growth of colon carcinoma cell lines through suppressing the expression of genes whose promoter contains a 12-O-tetradecanoylphorbol-13-acetate-responsive element or serum-responsive element.
研究了一种丝氨酸蛋白酶抑制性四苯甲脒衍生物TAPP-Br对8种人结肠癌细胞系细胞生长的抑制作用，并分析了其抑制机制。TAPP-Br抑制了所有结肠癌细胞系的细胞生长，且这种作用是不可逆的。处理3小时后，TAPP-Br使MYC、FOS和JUN等核癌基因的mRNA表达降低，且这种作用持续48小时。TAPP-Br处理开始48小时后，表皮生长因子受体、转化生长因子-β和IV型胶原酶的mRNA表达受到抑制，提示TAPP-Br存在间接作用。TAPP-Br降低了颗粒部分的蛋白激酶C活性，而增加了可溶性部分的酶活性。这些发现总体表明，丝氨酸蛋白酶抑制剂TAPP-Br可能通过抑制启动子含有12-O-十四烷酰佛波醇-13-乙酸酯反应元件或血清反应元件的基因表达来抑制结肠癌细胞系的细胞生长。
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