Development and thermodynamic evaluation of novel lipid raft stationary phase chromatography for screening potential antitumor agents.
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.
Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, People's Republic of China.
Shanshan
S
Tong
Chaonan
C
Sun
Xia
X
Cao
Qianfeng
Q
Zheng
Huiyun
H
Zhang
Caleb Kesse
CK
Firempong
Yingshu
Y
Feng
Yan
Y
Yang
Jiangnan
J
Yu
Ximing
X
Xu
D031289:Albizzia / Q000737:chemistry; D000970:Antineoplastic Agents / Q000032:analysis* / Q000737:chemistry / Q000378:metabolism*; D002227:Carbazoles / Q000032:analysis / Q000737:chemistry / Q000378:metabolism; D045744:Cell Line, Tumor; D002851:Chromatography, High Pressure Liquid / Q000295:instrumentation* / Q000379:methods*; D055808:Drug Discovery / Q000379:methods*; D005663:Furans; D006801:Humans; D021962:Membrane Microdomains / Q000737:chemistry / Q000378:metabolism*; D008956:Models, Chemical; D010316:Particle Size; D010936:Plant Extracts / Q000737:chemistry; D013816:Thermodynamics
D000970:Antineoplastic Agents; D002227:Carbazoles; D005663:Furans; D010936:Plant Extracts; C119379:lestaurtinib
Albizziae Cortex; antitumor activity; lipid raft stationary phase chromatography; optimum chromatographic condition; thermodynamic studies