Mamber S W, Mitulski J D, Borondy P E, Tunac J B
J Antibiot (Tokyo). 1987 Jan;40(1):77-80. doi: 10.7164/antibiotics.40.77.
Acetomycin has antitumor activity in vitro but not in vivo. HCT-8 human colon adenocarcinoma assays in the presence of a drug metabolizing system (rat liver S9 fraction) demonstrated that liver enzymes inactivated acetomycin. The structure of acetomycin suggested that an esterase could be the key inactivating enzyme. Assays with porcine liver esterase (EC 3.1.1.1) showed that this enzyme rapidly abolishes the activity of acetomycin against HCT-8 cells. The potential utility of acetomycin as an antitumor agent thus depends on finding a means of preventing esterase inactivation.
乙酰霉素在体外具有抗肿瘤活性，但在体内没有。在存在药物代谢系统（大鼠肝脏S9组分）的情况下进行的HCT-8人结肠腺癌测定表明，肝脏酶使乙酰霉素失活。乙酰霉素的结构表明酯酶可能是关键的失活酶。用猪肝酯酶（EC 3.1.1.1）进行的测定表明，这种酶能迅速消除乙酰霉素对HCT-8细胞的活性。因此，乙酰霉素作为一种抗肿瘤药物的潜在效用取决于找到一种防止酯酶失活的方法。
