Literature DB >> 24706535

Development and thermodynamic evaluation of novel lipid raft stationary phase chromatography for screening potential antitumor agents.

Shanshan Tong1, Chaonan Sun, Xia Cao, Qianfeng Zheng, Huiyun Zhang, Caleb Kesse Firempong, Yingshu Feng, Yan Yang, Jiangnan Yu, Ximing Xu.   

Abstract

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.

Entities:  

Keywords:  Albizziae Cortex; antitumor activity; lipid raft stationary phase chromatography; optimum chromatographic condition; thermodynamic studies

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Year:  2014        PMID: 24706535     DOI: 10.1002/bmc.3189

Source DB:  PubMed          Journal:  Biomed Chromatogr        ISSN: 0269-3879            Impact factor:   1.902


  2 in total

Review 1.  Targeting Anti-Cancer Active Compounds: Affinity-Based Chromatographic Assays.

Authors:  Marcela Cristina de Moraes; Carmen Lucia Cardoso; Cláudia Seidl; Ruin Moaddel; Quezia Bezerra Cass
Journal:  Curr Pharm Des       Date:  2016       Impact factor: 3.116

2.  Octreotide-periplocymarin conjugate prodrug for improving targetability and anti-tumor efficiency: synthesis, in vitro and in vivo evaluation.

Authors:  Hui-Yun Zhang; Wen-Qian Xu; Yuan-Yuan Zheng; Emmanuel Omari-Siaw; Yuan Zhu; Xia Cao; Shan-Shan Tong; Jiang-Nan Yu; Xi-Ming Xu
Journal:  Oncotarget       Date:  2016-12-27
  2 in total

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