title: Rapid screening of transferrin-binders in the flowers of Bauhinia blakeana Dunn by on-line high-performance liquid chromatography-diode-array detector-electrospray ionization-ion-trap-time-of-flight-mass spectrometry-transferrin-fluorescence detection system.
abstract: Transferrin (Transferrin, TRF, TF) has drawn increasing attention in cancer therapy due to its potential applications in drug delivery. TF receptor, highly expressed in tumor cells, recognizes and transports Fe(3+)-TF into cells to release iron into cytoplasm. Thus, discovering TF-binding compounds has become an active research area and is of great importance for target therapy. In this study, an on-line analysis method was established for screening TF-binding compounds from the flowers of Bauhinia blakeana Dunn using a high-performance liquid chromatography-diode-array detector-multi-stage mass spectrometry-transferrin-fluorescence detector (HPLC-DAD-MS(n)-TF-FLD) method. As a result, 33 of 80 identified or tentatively characterized compounds in the sample were TF-binding active. Twenty-five flavonol glycosides and eight phenolic acids were identified as TF-binders. Twelve of these active compounds together with six standard compounds were used to study the dose-response effects and structure-activity relationships of flavonoids and phenolic acids. The method was validated by vitexin with a good linearity in the range of concentrations used in the study. The limit of detection for vitexin was 0.1596 nmol. Our study indicated that the established method is simple, rapid and sensitive for screening TF-binding active compounds in the extract of Bauhinia blakeana Dunn, and therefore is important for discovering potential anti-cancer ingredients from complex samples for TF related drug delivery.
authors.affiliation: School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors.forename: Meixian
authors.initials: M
authors.lastname: Liu
authors.affiliation: Shimadzu International Trading (Shanghai) Co. Limited, Beijing 100020, China.
authors.forename: Jing
authors.initials: J
authors.lastname: Dong
authors.affiliation: Department of Pharmaceutical Sciences, University of Tennessee Health Science Center, Memphis, TN 38163, United States.
authors.forename: Zongtao
authors.initials: Z
authors.lastname: Lin
authors.affiliation: School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors.forename: Yanyan
authors.initials: Y
authors.lastname: Niu
authors.affiliation: School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors.forename: Xiaotian
authors.initials: X
authors.lastname: Zhang
authors.affiliation: School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors.forename: Haixiu
authors.initials: H
authors.lastname: Jiang
authors.affiliation: School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors.forename: Ning
authors.initials: N
authors.lastname: Guo
authors.affiliation: Department of Pharmaceutical Sciences, University of Tennessee Health Science Center, Memphis, TN 38163, United States.
authors.forename: Wei
authors.initials: W
authors.lastname: Li
authors.affiliation: School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors.forename: Hong
authors.initials: H
authors.lastname: Wang
authors.affiliation: School of Pharmaceutical Sciences, Peking University, Beijing 100191, China. Electronic address: chenshizhong66@163.com.
authors.forename: Shizhong
authors.initials: S
authors.lastname: Chen
mesh_terms: D000970:Antineoplastic Agents / Q000032:analysis* / Q000378:metabolism*; D047310:Apigenin / Q000032:analysis / Q000378:metabolism; D036481:Bauhinia / Q000737:chemistry*; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D004337:Drug Carriers / Q000378:metabolism; D005419:Flavonoids / Q000032:analysis / Q000737:chemistry / Q000378:metabolism; D035264:Flowers / Q000737:chemistry*; D005453:Fluorescence; D006027:Glycosides / Q000032:analysis / Q000378:metabolism; D062385:Hydroxybenzoates / Q000032:analysis / Q000378:metabolism; D008163:Luminescent Measurements / Q000379:methods*; D062105:Molecular Docking Simulation; D010936:Plant Extracts / Q000737:chemistry; D011485:Protein Binding; D021241:Spectrometry, Mass, Electrospray Ionization / Q000379:methods*; D013329:Structure-Activity Relationship; D014168:Transferrin / Q000378:metabolism*
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D005419:Flavonoids; D006027:Glycosides; D062385:Hydroxybenzoates; D010936:Plant Extracts; D014168:Transferrin; D047310:Apigenin; C032731:vitexin; C017616:phenolic acid
keywords: Bauhinia blakeana Dunn; On-line method; Structure-activity relationship; Transferrin; Transferrin-binding activity