Efferth T, Rücker G, Falkenberg M, Manns D, Olbrich A, Fabry U, Osieka R
Medizinische Klinik IV, Rheinisch-Westfälische Technische Hochschule Aachen, Germany.
Arzneimittelforschung. 1996 Feb;46(2):196-200.
Four investigational drugs, p-benzoquinone, primine, miconidine acetate, and artesunate (dihydroqinghaosusuccinate), with growth inhibitory activity against flagellatae (e.g. trypanosoma, leptomonas, plasmodium) were investigated for their capability to induce programmed cell death (apoptosis) in human KG-1a leukemic cells. The results were compared with those of three well established cytostatic agents (cisplatin, daunorubicin, cytosine-arabinoside) and ionizing radiation. The antitumor activity of the drugs was validated by a cellular growth inhibition assay. The depletion of glutathione by these four investigational drugs favours the hypothesis that formation of free radicals and subsequent DNA strand breaks may be critical mechanisms of action and that the glutathione redox cycle is involved in detoxification of these reactive molecules.
研究了四种具有抗鞭毛虫（如锥虫、利什曼原虫、疟原虫）生长抑制活性的试验性药物，对苯醌、伯胺、醋酸咪康唑和青蒿琥酯（二氢青蒿素琥珀酸酯）诱导人KG-1a白血病细胞程序性细胞死亡（凋亡）的能力。将结果与三种成熟的细胞抑制剂（顺铂、柔红霉素、阿糖胞苷）和电离辐射的结果进行了比较。通过细胞生长抑制试验验证了这些药物的抗肿瘤活性。这四种试验性药物对谷胱甘肽的消耗支持了以下假设：自由基的形成和随后的DNA链断裂可能是关键的作用机制，并且谷胱甘肽氧化还原循环参与了这些反应性分子的解毒过程。
