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Design and synthesis of PEG curcumin monomer for the comb-like polymer prodrug

机译:梳状聚合物前药PEG姜黄素单体的设计与合成

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Curcumin is a kind of compound with various biological activities. However, curcumin suffers from low aqueous solubility, instability and poor bioavailability in vivo, which restrained it from clinical application. In this paper, novel water soluble curcumin prodrug monomer was synthesized by reacting curcumin with methacryloyl polyethylene glycol (MA-PEG), and succinic anhydride. IR, MS and 1H NMR spectroscopy were carried out to verify the products. We studied and modified the reaction conditions. The drug load rate of the monomer was 26.9%, which was 2-4-fold than previous report, and the solubility of it could be increased to 1.17g/L, which was about 150 times higher than previous report. The monomer is used to prepare comb-like polymer prodrugs.
机译:姜黄素是一种具有各种生物活性的化合物。然而,姜黄素在体内含水溶解度,不稳定性和生物利用度差,这限制了临床应用。本文通过将姜黄素与甲基丙烯酰基聚乙二醇(MA-PEG)与琥珀酸酐反应合成新的水溶性姜黄素前药单体。进行IR,MS和1H NMR光谱,以验证产品。我们研究并修饰了反应条件。单体的药物载荷率为26.9%,比上一份报告为2-4倍,并且它的溶解度可以增加至1.17g / l,比上述报告高约150倍。单体用于制备梳状聚合物前药。

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