脂质的1-β-D-阿拉伯呋喃糖基胞嘧啶缀合物对小鼠WEHI-3B白血病的治疗活性。
Therapeutic activity of 1-beta-D-arabinofuranosylcytosine conjugates of lipids in WEHI-3B leukemia in mice.
作者信息
Berdel W E, Okamoto S, Danhauser-Riedl S, Hong C I, Winton E F, West C R, Rastetter J, Vogler W R
机构信息
Department of Medicine, Emory University School of Medicine, Atlanta, Georgia 30322.
出版信息
Exp Hematol. 1989 May;17(4):364-7.
Two new conjugates of 1-beta-D-arabinofuranosylcytosine (ara-C) and lipids were tested for therapeutic activity in myelomonocytic WEHI-3B leukemia in mice. Both conjugates were superior to equimolar mixtures of their respective parent compounds and to ara-C alone. IP treatment was found effective after either IP or IV transplantation of the leukemia. The thioether-linked lipid conjugate ara-CDP-D,L-PTBA showed considerably higher efficacy than the ester-linked lipid conjugate ara-CDP-L-dipalmitin. The optimal therapeutic regimen of ara-CDP-D,L-PTBA consisted of 60 mg/kg given IP qd 1-5 after transplantation of the WEHI-3B leukemia.
对两种新的1-β-D-阿拉伯呋喃糖基胞嘧啶（阿糖胞苷，ara-C）与脂质的缀合物进行了测试，以观察其对小鼠骨髓单核细胞性WEHI-3B白血病的治疗活性。两种缀合物均优于其各自母体化合物的等摩尔混合物以及单独的阿糖胞苷。在白血病经腹腔内（IP）或静脉内（IV）移植后，发现腹腔内给药治疗有效。硫醚连接的脂质缀合物阿糖胞苷二磷酸-D,L-硫代磷酸丁酯（ara-CDP-D,L-PTBA）显示出比酯连接的脂质缀合物阿糖胞苷二磷酸-L-二棕榈酸酯（ara-CDP-L-dipalmitin）更高的疗效。阿糖胞苷二磷酸-D,L-硫代磷酸丁酯的最佳治疗方案为在移植WEHI-3B白血病后第1 - 5天，每天腹腔内给予60 mg/kg。
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