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阿糖腺苷与N6-苄基腺苷抗增殖活性之间的协同作用。

Synergism between the antiproliferative activities of arabinosyladenine and N6-benzyladenosine.

作者信息

Tritsch G L, Nechaev A, Mittelman A

出版信息

Cancer Biochem Biophys. 1977;2(2):87-90.

PMID:567524
Abstract

N6-Benzyladenosine is a competitive inhibitor of adenosine deaminase from L-1210 cells in axenic culture as well as a potent antiproliferative agent in vitro and in vivo. Potentiation of the growth inhibitory activity of 9-beta-D-arabinosyladenine (ara-A) was observed in the L-1210 system with maximum synergism with a mixture of 16 micron ara-A and 10 micron benzyladenosine. Kinetic studies with L-1210 cell lysates showed values for Km of 0.25 mM ara-A and Ki of 0.23 mM benzyladenosine. It is suggested that ara-A and benzyladenosine in suitable combination may be expected to demonstrate enhanced clinical chemotherapeutic effectiveness.

摘要

N6-苄基腺苷是无菌培养的L-1210细胞中腺苷脱氨酶的竞争性抑制剂,也是一种在体内外均有效的抗增殖剂。在L-1210系统中观察到9-β-D-阿拉伯糖基腺嘌呤(ara-A)的生长抑制活性增强,与16微摩尔ara-A和10微摩尔苄基腺苷的混合物具有最大协同作用。对L-1210细胞裂解物的动力学研究表明,ara-A的Km值为0.25毫摩尔,苄基腺苷的Ki值为0.23毫摩尔。有人提出,ara-A和苄基腺苷以适当组合可能有望显示出增强的临床化疗效果。

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