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Development and thermodynamic evaluation of novel lipid raft stationary phase chromatography for screening potential antitumor agents
Author(s) -
Tong Shanshan,
Sun Chaonan,
Cao Xia,
Zheng Qianfeng,
Zhang Huiyun,
Firempong Caleb Kesse,
Feng Yingshu,
Yang Yan,
Yu Jiangnan,
Xu Ximing
Publication year - 2014
Publication title -
biomedical chromatography
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.4
H-Index - 65
eISSN - 1099-0801
pISSN - 0269-3879
DOI - 10.1002/bmc.3189
Subject(s) - chemistry , chromatography , raft , hydrogen bond , hydrophilic interaction chromatography , hydrophobic effect , column chromatography , lipid raft , van der waals force , high performance liquid chromatography , organic chemistry , receptor , polymer , biochemistry , molecule , copolymer
Novel lipid raft stationary phase chromatography (LRSC), with lipid rafts that contain abundant tropomyosin‐related tyrosine kinase A receptors immobilized on the stationary phase, was developed for a high‐throughput screening of potentially active antitumor agents. Lestaurtinib was used as a model compound to determine the operational parameters of the LRSC. Of all the factors considered, the particle size of column packing, the column temperature and the flow rate were of immense importance in determining the performance of the established LRSC system. In order to profoundly comprehend the binding interaction between the model drug and the receptors on the column, thermodynamic studies were employed. The results revealed that the interaction was spontaneous and exothermic, a typical enthalpy‐driven process. Additionally, the primary forces were hydrogen bonding and van der Waals forces. In evaluating the applicability of the method, active extracts from Albizziae Cortex were screened out using the LRSC system under the optimized conditions. The bioactive components were successfully confirmed by the MTT assay. In conclusion, it could be said that the LRSC is a good model for screening potential antitumor agents because of its viability, rapid response and scalable features. Copyright © 2014 John Wiley & Sons, Ltd.