Chen Bo, Xu Junyan, Fu Qing, Dong Xuefang, Guo Zhimou, Jin Yu, Liang Xinmiao
School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, China.
Analyst. 2015 Jul 7;140(13):4676-86. doi: 10.1039/c5an00271k.
Peptides from scorpion venom represent one of the most promising drug sources for drug discovery for some specific diseases. Current challenges in their separation include high complexity, high homologies and the huge range of peptides. In this paper, a modified strong cation exchange material, named MEX, was utilised for the two-dimensional separation of peptides from complex scorpion venom. The silica-based MEX column was bonded with two functional groups; benzenesulfonic acid and cyanopropyl. To better understand its separation mechanisms, seven standard peptides with different properties were employed in an evaluation study, the results of which showed that two interactions were involved in the MEX column: electrostatic interactions based on benzenesulfonic acid groups dominated the separation of peptides; weak hydrophobic interactions introduced by cyanopropyl groups increased the column's selectivity for peptides with the same charge. This characteristic allowed the MEX column to overcome some of the drawbacks of traditional strong cation exchange (SCX) columns. Furthermore, the study showed the great effects of the acetonitrile (ACN) content, the sodium perchlorate (NaClO4) concentration and the buffer pH in the mobile phase on the peptides' retention and separation selectivity on the MEX column. Subsequently, the MEX column was combined with a C18 column to establish an off-line 2D-MEX × C18 system to separate peptides from scorpion Buthus martensi Karsch (BmK) venom. Due to complementary separation mechanisms in each dimension, a high orthogonality of 47.62% was achieved. Moreover, a good loading capacity, excellent stability and repeatability were exhibited by the MEX column, which are beneficial for its use in future preparation experiments. Therefore, the MEX column could be an alternative to the traditional SCX columns for the separation of peptides from scorpion venom.
来自蝎毒的肽类是针对某些特定疾病进行药物研发最具前景的药物来源之一。目前其分离面临的挑战包括高复杂性、高度同源性以及肽段种类繁多。本文采用一种名为MEX的改性强阳离子交换材料对复杂蝎毒中的肽段进行二维分离。基于硅胶的MEX柱键合了苯磺酸和氰丙基两个官能团。为更好地理解其分离机制,在一项评估研究中使用了七种性质不同的标准肽,结果表明MEX柱涉及两种相互作用:基于苯磺酸基团的静电相互作用主导肽段的分离;氰丙基引入的弱疏水相互作用增加了柱子对相同电荷肽段的选择性。这一特性使MEX柱克服了传统强阳离子交换(SCX)柱的一些缺点。此外,研究表明流动相中乙腈(ACN)含量、高氯酸钠(NaClO4)浓度和缓冲液pH值对肽段在MEX柱上的保留和分离选择性有很大影响。随后,将MEX柱与C18柱联用,建立离线二维MEX×C18系统来分离东亚钳蝎(BmK)毒液中的肽段。由于各维度分离机制互补,实现了47.62%的高正交性。此外,MEX柱表现出良好的负载能力、出色的稳定性和重复性,有利于其在未来制备实验中的应用。因此,MEX柱可作为传统SCX柱的替代品用于分离蝎毒中的肽段。