抗白血病药物安吖啶的肽衍生物ALGA的细胞毒性作用及对细胞周期的影响
Cytotoxic action and cell cycle effects of ALGA, a peptidic derivative of the antileukemic drug amsacrine.
作者信息
Collyn-d'Hooghe M, Bernier J L, Henichart J P
机构信息
Unité 124 INSERM, Institut de Recherches sur le Cancer de Lille, France.
出版信息
Cancer Biochem Biophys. 1987 Sep;9(3):257-64.
4'-(9-acridinylamino) methanesulfon-m-anisidide (amsacrine or AMSA), an antitumor drug which has been tested in clinical trials, is known to bind to DNA by the intercalation of its 9-amino acridine moiety between DNA base pairs. Like AMSA, a peptidic derivative of 4-(9-acridinylamino) aniline, 4-(9-acridinylamino)-N-(lysylglycyl) aniline (ALGA) binds to DNA by intercalation and its affinity for the target was found to be higher than the parent drug. The antitumor effect of AMSA and ALGA has been monitored by drug exposure assays on EMT 6 cells. AMSA showed a slightly higher cytotoxic activity. The cell cycle effects of both drugs were studied using flow cytofluorimetry; an accumulation of cells in the S phase followed by a cycle arrest in the G2 phase, characteristic of intercalating drugs, was observed.
4'-(9-吖啶基氨基)甲磺酰基间茴香胺（安吖啶或AMSA）是一种已在临床试验中进行测试的抗肿瘤药物，已知它通过其9-氨基吖啶部分插入DNA碱基对之间而与DNA结合。与AMSA一样，4-(9-吖啶基氨基)苯胺的肽衍生物4-(9-吖啶基氨基)-N-(赖氨酰甘氨酰)苯胺（ALGA）也通过插入作用与DNA结合，并且发现它对靶标的亲和力高于母体药物。通过对EMT 6细胞进行药物暴露试验监测了AMSA和ALGA的抗肿瘤作用。AMSA显示出略高的细胞毒性活性。使用流式细胞荧光测定法研究了两种药物对细胞周期的影响；观察到细胞在S期积累，随后在G2期发生周期停滞，这是嵌入药物的特征。
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