title: Protein binding characteristics of 2'-benzoyloxycinnamaldehyde.
abstract: The protein binding characteristic of 2'-Benzoyloxycinnamaldehyde (BCA) was investigated, which has demonstrated a potent antitumor effect against several human solid tumor cell lines and in human tumor xenograft nude mice. Protein binding of BCA in human serum was 86 +/- 0.91% and the predominant binding protein of BCA was fatty-acid-free human serum albumin (HSA) (81 +/- 0.91%). The binding of BCA to HSA was outlined by one class, and Ka and n of BCA were 1.65 x 10(5) M(- 1) and 0.374, respectively. Displacement studies with fluorescence probes suggested that BCA mainly binds to site I on HSA, and BCA-induced enhancement in site II binding. The limited drug-drug interaction experiments suggested that BCA influences both site I and site II drug-HSA bindings via different mechanisms; a competitive displacement and a probable allosteric conformational change in HSA, respectively.
authors.affiliation: College of Pharmacy, Pusan National University, Pusan, Korea.
authors.forename: Ren
authors.initials: R
authors.lastname: Shan
authors.forename: Kyoung-Jin
authors.initials: KJ
authors.lastname: Lee
authors.forename: Byoung-Mog
authors.initials: BM
authors.lastname: Kwon
authors.forename: Chi-Ho
authors.initials: CH
authors.lastname: Lee
mesh_terms: D000171:Acrolein / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology; D000925:Anticoagulants / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000378:metabolism; D001565:Benzoates / Q000737:chemistry / Q000378:metabolism*; D003975:Diazepam / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D018757:GABA Modulators / Q000494:pharmacology; D006801:Humans; D007074:Immunoglobulin G / Q000097:blood / Q000378:metabolism; D007700:Kinetics; D009961:Orosomucoid / Q000378:metabolism; D010653:Phenylbutazone / Q000494:pharmacology; D011485:Protein Binding / Q000187:drug effects; D012709:Serum Albumin / Q000378:metabolism*; D013696:Temperature; D014859:Warfarin / Q000494:pharmacology
chemical_list: C484327:2'-benzoyloxycinnamaldehyde; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000925:Anticoagulants; D000970:Antineoplastic Agents; D001565:Benzoates; D018757:GABA Modulators; D007074:Immunoglobulin G; D009961:Orosomucoid; D012709:Serum Albumin; D014859:Warfarin; D000171:Acrolein; D010653:Phenylbutazone; D003975:Diazepam; C012843:cinnamaldehyde