Sava G, Zorzet S, Perissin L, Pacor S, Lassiani L, Nisi C, Varnavas A
Institute of Pharmacology, Faculty of Pharmacy, University of Trieste, Italy.
Cancer Chemother Pharmacol. 1991;27(6):423-8. doi: 10.1007/BF00685155.
The antitumor and antimetastatic effects of p-(3-methyl-1-triazeno)benzoic acid potassium salt (MM-COOK) as compared with those of the parent 3,3-dimethyl derivative (DM-COOK) were examined using Lewis lung carcinoma, MCa mammary carcinoma of the CBA mouse and TLX5 lymphoma. Similarly to DM-COOK, MM-COOK reduces metastasis formation and significantly prolongs the survival of mice bearing the Lewis lung carcinoma when given at a daily dose corresponding to one-half that of DM-COOK. Unlike DM-COOK, MM-COOK exhibits significant cytotoxicity to metastatic foci and pronounced inhibition of primary tumor development. MM-COOK also causes cytotoxic effects on TLX5 lymphoma cell growing in the peritoneal cavity, even when used at low doses. The antimetastatic effects observed in mice bearing MCa mammary carcinoma are unrelated to the inhibition of primary tumor growth and are more likely due to the selection of clones endowed with lower metastatic ability. It appears that MM-COOK exhibits the same antineoplastic activity as DM-COOK, but the former does so at a lower daily dose and produces interesting cytotoxic effects other than those reflecting its antimetastatic properties. It thus seems to be a valid alternative to DM-COOK, in view of the possible introduction of newer aryltriazenes into clinical use.
使用Lewis肺癌、CBA小鼠的MCa乳腺癌和TLX5淋巴瘤,研究了对-(3-甲基-1-三氮烯)苯甲酸钾盐(MM-COOK)与母体3,3-二甲基衍生物(DM-COOK)相比的抗肿瘤和抗转移作用。与DM-COOK相似,当以相当于DM-COOK剂量一半的每日剂量给药时,MM-COOK可减少转移形成并显著延长荷Lewis肺癌小鼠的生存期。与DM-COOK不同,MM-COOK对转移灶表现出显著的细胞毒性,并对原发性肿瘤发展有明显抑制作用。即使以低剂量使用,MM-COOK对在腹腔中生长的TLX5淋巴瘤细胞也有细胞毒性作用。在荷MCa乳腺癌小鼠中观察到的抗转移作用与原发性肿瘤生长的抑制无关,更可能是由于选择了具有较低转移能力的克隆。似乎MM-COOK与DM-COOK表现出相同的抗肿瘤活性,但前者以较低的每日剂量即可做到,并且除了反映其抗转移特性的作用外,还产生了有趣的细胞毒性作用。鉴于可能将更新的芳基三氮烯引入临床应用,因此它似乎是DM-COOK的有效替代品。