本文選題：人參皂苷　切入點：熒光探針　出處：《有機(jī)化學(xué)》2017年08期

【摘要】：24R-奧克梯隆型皂苷元(Pyxinol),化學(xué)名稱(20S,24R)-環(huán)氧達(dá)瑪-3β,12β,25-三醇,是20(S)-原人參二醇的主要代謝產(chǎn)物,具有抗心肌缺血再灌注損傷(myocardial ischemia-reperfusion injury,MIRI)的活性.為了構(gòu)建有活性的Pyxinol熒光探針,設(shè)計應(yīng)用不同物理特性的連接臂連接Pyxinol與熒光基團(tuán)異硫氰酸熒光素(FITC,常用熒光基團(tuán)),以降低熒光大基團(tuán)對Pyxinol的空間位阻干擾.合成的熒光探針用H9C2心肌細(xì)胞進(jìn)行了體外抗MIRI活性評價.結(jié)果顯示,具有親水柔性乙氧基鏈的熒光探針保留了Pyxinol的抗MIRI活性.該活性小分子熒光探針的首次合成,為Pyxinol等人參皂苷的生物活性機(jī)制研究提供了重要的分子工具.
[Abstract]:Pyxinolus saponins of the type of 24R- Oxythyleneuron, the chemical name of which is "20Sn 24R" -Epoxy Dama -3 尾 -12 尾 -butadiol, is the main metabolite of 20 ~ (-) -protopaxadiol, and has the activity of resisting myocardial ischemia-reperfusion injuryMIRI. in order to construct the active Pyxinol fluorescent probe, a new fluorescent probe was developed for myocardial ischemia and reperfusion injury in order to construct the active Pyxinol fluorescent probe, which is the main metabolite of 20 ~ (-4) -protopanaxadiol. In order to reduce the steric interference of large fluorescent groups to Pyxinol, the Pyxinol and FITC with different physical characteristics were designed. The synthesized fluorescent probes were carried out by H9C2 cardiomyocytes. The in vitro evaluation of MIRI activity showed that, The fluorescence probe with hydrophilic flexible ethoxy chain retains the anti-#en1# activity of Pyxinol. The first synthesis of the small molecule fluorescence probe provides an important molecular tool for the study of the bioactivity mechanism of Pyxinol and other ginsenosides.
【作者單位】： 煙臺大學(xué)新型制劑與生物技術(shù)藥物研究山東省高校協(xié)同創(chuàng)新中心分子藥理和藥物評價教育部重點實驗室;
【基金】：國家自然科學(xué)基金(No.21502164) 山東省優(yōu)秀中青年科學(xué)家科研獎勵基金(No.BS2015YY039) 煙臺大學(xué)博士科研基金(No.YX14B17)資助項目~~
【分類號】：O657.3;R914;R96

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