Department of Chemistry and Biochemistry, Faculty of Agronomy, Mendel University in Brno, Brno, Czech Republic.
Electrophoresis. 2012 Jun;33(11):1545-9. doi: 10.1002/elps.201200056.
Ellipticine (5,11-dimethyl-6H-pyrido[4,3-b]carbazole), an alkaloid isolated from Apocynaceae plants, exhibits an antitumor activity, which is exceptionally high against several specific types of tumors. Ellipticine is also interesting as an anticancer drug as it has limited side effects and lacks of hematological toxicity. Various methods to study intercalating activity of this drug have been developed. However, to our best knowledge, capillary electrophoresis (CE) as a technique combining high separation resolution with various detection options has never been used for these purposes. In this study, a novel separation method based on CE with laser-induced fluorescence (CE-LIF) detection has been developed for the determination of ellipticine and for the monitoring of ellipticine-DNA interaction. Sodium acetate (50 mM, pH 4.5) was used as a background electrolyte and LIF detection at λ(ex) = 488 nm. The limit of detection for ellipticine was determined to be 5 × 10⁻⁸ M. A total of 20% dimethyl sulfoxide was found optimal as sample solvent. Additionally, intercalation of ellipticine into the double-stranded DNA was investigated. Signal corresponding to ellipticine was decreasing and a new peak appeared and was growing. It can be concluded that CE-LIF is a method applicable to in vitro studies of ellipticine-DNA complexes.
椭圆啶（5,11-二甲基-6H-吡啶并[4,3-b]咔唑），一种从夹竹桃科植物中分离出来的生物碱，具有抗肿瘤活性，对几种特定类型的肿瘤具有极高的活性。椭圆啶作为一种抗癌药物也很有趣，因为它的副作用有限，没有血液毒性。已经开发了各种研究该药物插入活性的方法。然而，据我们所知，毛细管电泳（CE）作为一种结合高分离分辨率和多种检测选择的技术，从未用于这些目的。在这项研究中，开发了一种基于 CE 与激光诱导荧光（CE-LIF）检测的新型分离方法，用于测定椭圆啶和监测椭圆啶-DNA 相互作用。使用乙酸钠（50 mM，pH 4.5）作为背景电解质和 λ（ex）= 488nm 的 LIF 检测。确定椭圆啶的检测限为 5×10⁻⁸M。发现 20%的二甲基亚砜作为样品溶剂最佳。此外，还研究了椭圆啶嵌入双链 DNA 中的情况。与椭圆啶相对应的信号减少，出现并增加了一个新的峰。可以得出结论，CE-LIF 是一种适用于椭圆啶-DNA 复合物的体外研究的方法。
