title: Synthesis and transmembrane anion/cation symport activity of a rigid bis(choloyl) conjugate functionalized with guanidino groups.
abstract: A rigid bis(choloyl) conjugate functionalized with guanidino groups was synthesized and fully characterized on the basis of NMR ((1)H and (13)C) and ESI MS (LR and HR) data. Its transmembrane ionophoric activity across egg-yolk l-α-phosphatidylcholine-based liposomal membranes was investigated by means of chloride ion selective electrode technique and pH discharge assay. The data indicate that under the assay conditions, this conjugate was capable of promoting the transport of anions, presumably via a cation/anion symport process. A Hill analysis reveals that two molecules of this compound are assembled into the transport-active species.
authors.affiliation: School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, PR China.
authors.forename: Li-Qun
authors.initials: LQ
authors.lastname: Deng
authors.affiliation: School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, PR China.
authors.forename: Zhi
authors.initials: Z
authors.lastname: Li
authors.affiliation: School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, PR China.
authors.forename: Yong-Ming
authors.initials: YM
authors.lastname: Lu
authors.affiliation: School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, PR China.
authors.forename: Jin-Xiang
authors.initials: JX
authors.lastname: Chen
authors.affiliation: School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, PR China.
authors.forename: Chun-Qiong
authors.initials: CQ
authors.lastname: Zhou
authors.affiliation: School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275, PR China.
authors.forename: Bo
authors.initials: B
authors.lastname: Wang
authors.affiliation: School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, PR China. Electronic address: whchen@smu.edu.cn.
authors.forename: Wen-Hua
authors.initials: WH
authors.lastname: Chen
mesh_terms: D002412:Cations / Q000737:chemistry; D002712:Chlorides / Q000737:chemistry; D002793:Cholic Acids / Q000737:chemistry* / Q000494:pharmacology*; D019791:Guanidine / Q000737:chemistry* / Q000494:pharmacology*; D006863:Hydrogen-Ion Concentration; D017136:Ion Transport / Q000187:drug effects; D007476:Ionophores / Q000737:chemistry* / Q000494:pharmacology*; D008081:Liposomes / Q000737:chemistry; D010713:Phosphatidylcholines / Q000737:chemistry
chemical_list: D002412:Cations; D002712:Chlorides; D002793:Cholic Acids; D007476:Ionophores; D008081:Liposomes; D010713:Phosphatidylcholines; D019791:Guanidine
keywords: Anionophore; Anionophoric activity; Cholic acid; Guanidino group; Ion selectivity