Imai R, Morimoto M, Marumo H, Kobayashi T, Tsuruo T, Inaba M, Tsukagoshi S, Sakurai Y
Gan. 1981 Dec;72(6):944-9.
The antitumor activity of 7-N-(p-hydroxyphenyl)-mitomycin C (M-83) was compared with that of mitomycin C (MMC) in rodent tumor systems. M-83 exhibited more potent activity than MMC against the ascitic form of lymphocytic leukemia P388 and fibrosarcoma Meth 1, and doses of over 5 mg/kg of M-83 (1/6 LD50) resulted in some 60-day survivors. The chemotherapeutic ratio (optimal dose/MED) of M-83 was around 64 and was estimated to be approximately 5 to 8 times higher than that of MMC. Upon intravenous administration, M-83 also gave a better survival and showed a higher chemotherapeutic ratio than MMC against intravenously implanted P388. M-83 inhibited the growth of solid form of sarcoma 180 to the same extent as MMC at an equivalent dose, but showed a higher safety margin than MMC. M-83 was as effective as MMC against Lewis lung carcinoma at dose levels giving the same degree of toxicity. In vitro studies on tumor growth inhibition demonstrated that the cytotoxic effects of M-83 against leukemia P388 and fibrosarcoma Meth 1 cells were similar to and stronger than those of MMC, respectively.
在啮齿动物肿瘤系统中，对7-N-(对羟基苯基)-丝裂霉素C（M-83）和丝裂霉素C（MMC）的抗肿瘤活性进行了比较。M-83对腹水型淋巴细胞白血病P388和纤维肉瘤Meth 1的活性比MMC更强，M-83剂量超过5mg/kg（1/6 LD50）可产生约60天的存活者。M-83的化疗指数（最佳剂量/MED）约为64，估计比MMC高约5至8倍。静脉给药时，M-83对静脉内植入的P388也有更好的存活率，且化疗指数高于MMC。在等效剂量下，M-83对肉瘤180实体瘤生长的抑制程度与MMC相同，但安全系数比MMC更高。在产生相同程度毒性的剂量水平下，M-83对Lewis肺癌的疗效与MMC相当。对肿瘤生长抑制的体外研究表明，M-83对白血病P388和纤维肉瘤Meth 1细胞的细胞毒性作用分别与MMC相似且比MMC更强。
