具有抗癌活性的桦木醇新型聚合物衍生物。
Novel polymeric derivatives of betulin with anticancer activity.
作者信息
Niewolik Daria, Krukiewicz Katarzyna, Bednarczyk-Cwynar Barbara, Ruszkowski Piotr, Jaszcz Katarzyna
机构信息
Department of Physical Chemistry and Technology of Polymers, Silesian University of Technology UL M Strzody 9 44-100 Gliwice Poland
Centre for Research in Medical Devices, National University of Ireland Galway Ireland.
出版信息
RSC Adv. 2019 Jul 4;9(36):20892-20900. doi: 10.1039/c9ra03326b. eCollection 2019 Jul 1.
In order to provide novel polymeric biomaterials for chemotherapeutic purposes, in this paper we described the synthesis and the characterization of the physicochemical properties of a betulin-based polyanhydride exhibiting anti-cancer effects. The polyanhydride was obtained by a melt polycondensation of a disuccinate betulin (3,28-di--succinyl betulin), and was thoroughly characterized through H NMR and C NMR spectroscopies, correlation spectroscopy, heteronuclear single quantum correlation, size exclusion chromatography, differential scanning calorimetry and FT-IR spectroscopy. It was confirmed, that the obtained polyanhydride undergoes hydrolytic degradation, releasing disuccinate betulin as a degradation product. Polyanhydride of a disuccinate betulin was tested for cytostatic activity against a wide range of cancer cell lines (HeLa, MCF-7, A-549, U-87MG, KB and HepG2), proving its efficiency in inhibiting the growth of selected cancer cells. To realize the concept of an easily administrated drug release system, polyanhydride was fabricated in a form of micro- (1-30 μm) and nanospheres (∼400 nm) by using an emulsion solvent evaporation method. The micro- and nanospheres were characterized by SEM.
为了提供用于化疗目的的新型聚合物生物材料，在本文中我们描述了一种具有抗癌作用的桦木醇基聚酐的合成及其物理化学性质的表征。该聚酐通过二琥珀酸桦木醇（3,28 - 二 - 琥珀酰桦木醇）的熔融缩聚反应制得，并通过氢核磁共振（¹H NMR）、碳核磁共振（¹³C NMR）光谱、相关光谱、异核单量子相关、尺寸排阻色谱、差示扫描量热法和傅里叶变换红外光谱（FT - IR）进行了全面表征。已证实，所得到的聚酐会发生水解降解，释放出二琥珀酸桦木醇作为降解产物。对二琥珀酸桦木醇聚酐针对多种癌细胞系（HeLa、MCF - 7、A - 549、U - 87MG、KB和HepG2）的细胞生长抑制活性进行了测试，证明其在抑制所选癌细胞生长方面的有效性。为了实现易于给药的药物释放系统的概念，通过乳液溶剂蒸发法将聚酐制成微米级（1 - 30μm）和纳米级（约400nm）的微球和纳米球。通过扫描电子显微镜（SEM）对微球和纳米球进行了表征。
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