具有增强载药量的阿拉伯胶-姜黄素缀合物胶束用于姜黄素向肝癌细胞的递送。
Gum arabic-curcumin conjugate micelles with enhanced loading for curcumin delivery to hepatocarcinoma cells.
机构信息
Department of Chemistry, Indian Institute of Space Science and Technology (IIST), Valiamala, Thiruvananthapuram, Kerala 695 547, India.
Tissue Culture Laboratory, Biomedical Technology Wing, Sree Chitra Tirunal Institute for Medical Sciences and Technology, Poojappura, Thiruvananthapuram, Kerala 695 012, India.
出版信息
Carbohydr Polym. 2015 Dec 10;134:167-74. doi: 10.1016/j.carbpol.2015.07.068. Epub 2015 Jul 23.
Curcumin is conjugated to gum arabic, a highly water soluble polysaccharide to enhance the solubility and stability of curcumin. Conjugation of curcumin to gum arabic is confirmed by (1)H NMR, fluorescence and UV spectroscopy studies. The conjugate self assembles to spherical nano-micelles (270 ± 5 nm) spontaneously, when dispersed in aqueous medium. Spherical morphology of the self assembled conjugate is evidenced by field emission scanning electron microscopy and transmission electron microscopy. The self assembly of the amphiphilic conjugate into micelle in aqueous medium significantly enhances the solubility (900 fold of that of free curcumin) and stability of curcumin in physiological pH. The anticancer activity of the conjugate micelles is found to be higher in human hepatocellular carcinoma (HepG2) cells than in human breast carcinoma (MCF-7) cells. The conjugate exhibits enhanced accumulation and toxicity in HepG2 cells due to the targeting efficiency of the galactose groups present in gum arabic.
姜黄素与阿拉伯胶结合，阿拉伯胶是一种高度水溶性的多糖，可提高姜黄素的溶解度和稳定性。（1）H NMR、荧光和紫外光谱研究证实了姜黄素与阿拉伯胶的结合。该共轭物在分散于水介质中时，会自发自组装成球形纳米胶束（270 ± 5nm）。场发射扫描电子显微镜和透射电子显微镜证明了自组装共轭物的球形形态。该两亲性共轭物在水介质中胶束自组装，可显著提高姜黄素的溶解度（比游离姜黄素高 900 倍）和在生理 pH 值下的稳定性。研究发现，胶束的抗癌活性在人肝癌（HepG2）细胞中高于人乳腺癌（MCF-7）细胞。由于阿拉伯胶中存在的半乳糖基团的靶向效率，该共轭物在 HepG2 细胞中表现出增强的积累和毒性。
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