Mileva Milka, Traikov Lubomir, Deliyska Boriana
Department of Physics and Biophysics Medical University, Faculty of Medicine, Medical University, Sofia, Bulgaria.
Med Pregl. 2007;60 Suppl 2:121-3.
Endoxan (cyclophosphamide) is a cyclic propylene phosphamide ester of nitrogen mustard. Endoxan--main advantage of chemotherapy is complete penetration of the tissues, reaching the most widely spread malignant cells. It is one of the most useful cytotoxics available today. Endoxan is a "transport form" and as such it has a selective tumour affinity. Endoxan is used for active treatment of all neoplastic diseases of the reticulo-endothelial system, e.g. lymphomas, lymphosarcomas, reticular-sarcomas, Hodgkin's disease, chronic lymphatic leukaemias, multiple myelomas. In our experiments Endoxan is equivalent with mean therapeutic the concentration used in chemotherapy in tumours, we suppose that at these levels Endoxan interact with renal cells and probably induce or inhibits new generation of superoxide free forms in the same tissue. Endoxan was tested at renal supernatant and free enzyme model systems, for superoxide-scavenging and antioxidante activity. The ability of Endoxan to interact with the superoxide radical, to influence their generation and probably to change the levels of lipid peroxidation in model systems were investigated. The ability of Endoxane to affect Fe2+-induced lipid peroxidation in a renal supernatant was studied. The results show that Endoxan in a concentration range of 10(-4); 10(-5) M has small but significant effect. The values for the control samples without Endoxan, are compared. We found a dose-dependent superoxide-scavenging effect of the drug in xanthite/xanthine oxidase system for generation of superoxide. According to obtained results lndoxan could be used in insertion in a liposomes and this could impact lndoxan tissue penetration.
环磷酰胺是氮芥的环状丙烯磷酰胺酯。环磷酰胺——化疗的主要优势在于其能完全渗透组织，抵达扩散最广的恶性细胞。它是当今最有用的细胞毒性药物之一。环磷酰胺是一种“转运形式”，因此具有选择性肿瘤亲和力。环磷酰胺用于积极治疗网状内皮系统的所有肿瘤疾病，如淋巴瘤、淋巴肉瘤、网状肉瘤、霍奇金病、慢性淋巴细胞白血病、多发性骨髓瘤。在我们的实验中，环磷酰胺在肿瘤化疗中使用的平均治疗浓度相当，我们推测在这些水平下环磷酰胺与肾细胞相互作用，并可能在同一组织中诱导或抑制新一代超氧自由基形式。在肾组织上清液和游离酶模型系统中测试了环磷酰胺的超氧清除和抗氧化活性。研究了环磷酰胺与超氧自由基相互作用、影响其生成以及可能改变模型系统中脂质过氧化水平的能力。研究了环磷酰胺对肾组织上清液中Fe2+诱导的脂质过氧化的影响。结果表明，浓度范围为10(-4)；10(-5) M的环磷酰胺具有微小但显著的作用。将不含环磷酰胺的对照样品的值进行比较。我们发现在黄嘌呤/黄嘌呤氧化酶系统中该药物具有剂量依赖性的超氧清除作用以产生超氧。根据所得结果，环磷酰胺可用于脂质体包封，这可能会影响环磷酰胺的组织渗透。
