title: Evaluation of affinity interaction between small molecules and platelets by open tubular affinity capillary electrochromatography.
abstract: In this paper, an open tubular affinity capillary electrochromatography (OT-ACEC) was developed by physical adsorption of rabbit platelets on the inner surface of capillary. The interactions between small molecules include adenosine diphosphate (ADP) (positive control), protocatechuic acid (negative control) and seven natural products (salvianolic acid B, salvianic acid A sodium, hydroxysafflor yellow A, ferulic acid, chlorogenic acid, sinapic acid, caffeic acid) and platelets were evaluated by their retention factors and binding constants obtained based on peak-shift assay. Then, the activities of anti-platelet aggregation induced by thrombin (THR), ADP and arachidonic acid (AA) for those small molecules (except ADP) were evaluated by turbidimetric method. The results indicate that: (i) ADP, a platelet aggregation inducer, had strong interaction with platelet, while protocatechuic acid that had no inhibition on platelet aggregation behaved no specific interaction; (ii) there was a positive correlation between the anti-platelet aggregation activities of small molecules and their interactions with platelet, generally those compounds with higher binding constants with platelet exhibited higher activities. Therefore, the OT-ACEC method developed in the present study can be a potential method to evaluate affinity interactions between small molecules and platelets, so as to predict the biological activities such as anti-platelet aggregation for the small molecules.
authors.affiliation: School of Chemistry and Chemical Engineering, Chongqing University, Chongqing, P. R. China.
authors.forename: Feng-Qin
authors.initials: FQ
authors.lastname: Wang
authors.affiliation: School of Chemistry and Chemical Engineering, Chongqing University, Chongqing, P. R. China.
authors.forename: Qian
authors.initials: Q
authors.lastname: Zhang
authors.affiliation: School of Chemistry and Chemical Engineering, Chongqing University, Chongqing, P. R. China.
authors.forename: Chun-Hong
authors.initials: CH
authors.lastname: Li
authors.affiliation: School of Chemistry and Chemical Engineering, Chongqing University, Chongqing, P. R. China.
authors.forename: Yin-Zhen
authors.initials: YZ
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, P. R. China.
authors.forename: Yuan-Jia
authors.initials: YJ
authors.lastname: Hu
authors.affiliation: School of Chemistry and Chemical Engineering, Chongqing University, Chongqing, P. R. China.
authors.forename: Qi-Hui
authors.initials: QH
authors.lastname: Zhang
authors.affiliation: School of Chemistry and Chemical Engineering, Chongqing University, Chongqing, P. R. China.
authors.forename: Zhi-Ning
authors.initials: ZN
authors.lastname: Xia
authors.affiliation: School of Chemistry and Chemical Engineering, Chongqing University, Chongqing, P. R. China.
authors.forename: Feng-Qing
authors.initials: FQ
authors.lastname: Yang
mesh_terms: D000818:Animals; D001792:Blood Platelets / Q000166:cytology / Q000187:drug effects*; D053801:Capillary Electrochromatography / Q000295:instrumentation / Q000379:methods*; D002478:Cells, Cultured; D006401:Hematologic Agents / Q000494:pharmacology*; D008297:Male; D010974:Platelet Aggregation / Q000187:drug effects*; D011817:Rabbits
chemical_list: D006401:Hematologic Agents
keywords: Affinity interaction; Anti-platelet aggregation activity; Binding constant; Open tubular affinity capillary electrochromatography; Retention factor