Cancer chemotherapy by liposomal 6-[12-(dimethylamino)ethyl]aminol-3-hydroxy-7H-indeno[2,1-clquinolin-7-one dihydrochloride (TAS-103), a novel anti-cancer agent.
Cancer chemotherapy by liposomal 6-[12-(dimethylamino)ethyl]aminol-3-hydroxy-7H-indeno[2,1-clquinolin-7-one dihydrochloride (TAS-103), a novel anti-cancer agent.
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采用脂质体 6-[12-(二甲氨基)乙基]氨基醇-3-羟基-7H-茚并[2,1-氯喹啉-7-酮二盐酸盐 (TAS-103)（一种新型抗癌剂）进行癌症化疗。
DOI：
10.1248/bpb.25.1385
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发表时间：
2002
影响因子：
2
通讯作者：
N. Oku
中科院分区：
文献类型：
--
作者：
K. Shimizu;M. Takada;T. Asai;K. Kuromi;K. Baba;N. Oku
新型抗肿瘤药物6-[[2-（二甲氨基）乙基]氨基]-3-羟基-7H-茚并[2，1-c]喹啉-7-酮二盐酸盐（TAS-103）可有效抑制拓扑异构酶I和II活性。为了增强抗肿瘤疗效并减少药物的副作用，进行了TAS-103的脂质体化。TAS-103通过远程加载法有效包封在脂质体中，在4 ℃和50%血清存在下稳定。为评价TAS-103脂质体的抗肿瘤疗效，检查了其对刘易斯肺癌细胞的体外生长抑制作用和对荷实体瘤小鼠的体内治疗疗效。TAS-103脂质体对刘易斯肺癌细胞显示出较强的细胞毒作用，且呈剂量依赖性，与游离TAS-103给药小鼠相比，TAS-103脂质体可有效抑制实体瘤生长，并延长荷瘤小鼠的生存时间。这些结果表明，脂质体TAS-103可用于癌症治疗。
A novel anti-tumor agent, 6-[[2-(dimethylamino)ethyl]amino]-3-hydroxy-7H-indeno[2,1-c]quinolin-7-one dihydrochloride (TAS-103), effectively inhibits both topoisomerase I and II activities. To enhance anti-tumor efficacy and to reduce the side effects of the agent, liposomalization of TAS-103 was performed. TAS-103 was effectively entrapped in liposomes by a remote-loading method, and was stable at 4 degrees C and in the presence of 50% serum. To evaluate the anti-tumor efficacy of liposomal TAS-103, the growth inhibition against Lewis lung carcinoma cells in vitro and the therapeutic efficacy against solid tumor-bearing mice in vivo were examined. Liposomal TAS-103 showed strong cytotoxic effect against Lewis lung carcinoma cells in a dose dependent manner and effectively suppressed solid tumor growth accompanying longer survival time of tumor-bearing mice in comparison with the mice treated with free TAS-103. These results suggest that liposomal TAS-103 is useful for cancer therapy.
影响因子：
2.9
作者：
Fortune, JM;Velea, L;Osheroff, N
通讯作者：
Osheroff, N