Izumoto S, Arita N, Ushio Y, Hayakawa T, Ohnishi T, Taki T, Yamamoto H, Oku Y, Mogami H, Komeshima N
Dept. of Neurosurgery, Osaka University Medical School.
Gan To Kagaku Ryoho. 1988 May;15(5):1765-9.
MX-2, a new morpholino anthracycline derivative, showed broad anti-neoplastic activity against experimental tumors. Molecular weight of MX-2 is 622.07, and it can cross blood-brain barrier because of its high lipid solubility. In this report, we described its in vitro and in vivo effects on brain tumors. The growth of rat 9L and human KNS-42 glioma cells were markedly inhibited by the medium containing more than 1 ng/ml of MX-2. The inhibitory concentration of MX-2 for 50% cell kill was 1.8 ng/ml for 9L cell and 18 ng/ml for KNS-42, respectively. These values were the almost same as those reported with P388 leukemia. In rats with meningeal carcinomatosis induced by intracisternal inoculation of Walker 256 carcinosarcoma cells, the median survival time was significantly prolonged. The increased life span was 40, 40, 40 (p less than 0.01), and 20% (p less than 0.05) in the animals given intravenous MX-2 of 1.5, 1.0, 0.75, and 0.375 mg/kg on day 1, 5, and 9 after tumor inoculation respectively. These results indicate that MX-2 may be a promising new antineoplastic agent for the treatment of malignant brain tumor.
MX - 2是一种新型吗啉代蒽环类衍生物，对实验性肿瘤显示出广泛的抗肿瘤活性。MX - 2的分子量为622.07，因其高脂质溶解性可穿过血脑屏障。在本报告中，我们描述了其对脑肿瘤的体外和体内作用。含有超过1 ng/ml MX - 2的培养基可显著抑制大鼠9L和人KNS - 42胶质瘤细胞的生长。MX - 2对9L细胞和KNS - 42细胞50%细胞杀伤的抑制浓度分别为1.8 ng/ml和18 ng/ml。这些数值与P388白血病报道的数值几乎相同。在通过脑池内接种Walker 256癌肉瘤细胞诱导脑膜癌病的大鼠中，中位生存时间显著延长。在肿瘤接种后第1、5和9天分别给予静脉注射1.5、1.0、0.75和0.375 mg/kg MX - 2的动物中，寿命延长分别为40%、40%、40%（p<0.01）和20%（p<0.05）。这些结果表明，MX - 2可能是一种有前途的治疗恶性脑肿瘤的新型抗肿瘤药物。
