BOPIM-dma作为BSA Site Ⅰ特异性探针的研究及其应用  

BOPIM-dma as BSA Site Ⅰ Specific Probe for Drug Binding Study

作　　者：高青云[1] 刘含[1] 丁琼洁[1] 杨威[1] 刘春琳[1] 杨昌英[1] 

机构地区：[1]三峡大学生物与制药学院,湖北宜昌443002

出　　处：《三峡大学学报（自然科学版）》2016年第6期108-112,共5页Journal of China Three Gorges University：Natural Sciences

基　　金：国家自然科学基金(21473101)资助

摘　　要：本文选取具有扭转的分子内电荷转移（TICT）特性BOPIM-dma作为BSAsiteⅠ特异性探针，研究了9种药物与BSA结合性质．溶剂化荧光猝灭的BOPIM—dma在结合到BSA的结合点位SiteⅠ后在500nm处发射出强绿色荧光．选取两类作用于BSA SiteⅠ的药物，包括黄酮类药物：槲皮素（Quercetin）、山奈酚（Kaempeferol）、黄芩素（Baicalein）、柚皮素（Naringenin）、芹菜素（Apigenin）、木犀草素（Iuteolin）；抗炎药：舒林酸（Sulindac）、吲哚美辛（Indomethacin）、托美丁钠（Tolmetin Sodium Saltdihydrate）．实验结果与文献对照，仅槲皮素、山奈酚因为本身-500nm处有荧光而出现偏差，其他活性顺序与文献是一致的．并且BOPIM—dma／BSA体系发绿光，增强了实验的可视性．这也表明：BOPIM—dma作为BSA siteⅠ特异性探针研究作用于该位点的药物与BSA之间的相互作用性质是可靠的．BOPIM-dma with twisted intramolecular charge transfer （TICT） character was used to act as BSA Site I fluorescence specific probe for studying of the interaction between BSA and drugs. BOPIM-dma emits strong green fluorescence in BSA （- 500 nm）. The binding of drug to BSA quenched the fluorescence of BOPIM-dma because of dissociation of BOPIM-dma from hydrophobic pocket of BSA Site I . Two kinds of drugs, including {lavonoids：quercetin, kaempeferol, baicalein, naringenin, apigenin, iuteolin, and anti-in- flammatory.sulindac, indomethacin and tolmetin sodium salt dehydrate were selected for the binding investi-gation. It is shown that the binding constant of studied drugs to BSA obtained from our results are consistent with the data have been reported. Thus, BOPIM-dma is suitable for the specific probe for BSA Site I to study the interaction between drugs and BSA, except of drugs which emit fluorescence at - 500 nm themselves.

关 键 词：荧光探针 BOPIM-dma 牛血清蛋白(BSA) 结合位点Ⅰ 药物 结合常数 

分 类 号：O657.34[理学—分析化学]