Sorbonne Universités, UPMC Univ Paris 06, CNRS, Institut Parisien de Chimie Moléculaire (UMR 8232), 4 Place Jussieu, 75005 Paris, France.
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
Eur J Med Chem. 2018 Feb 25;146:194-205. doi: 10.1016/j.ejmech.2018.01.040. Epub 2018 Feb 4.
The most common fullerene member C displays many biological applications, such as, anticancer, human immunodeficiency virus and hepatitis C virus inhibitors, O uptake inhibitor and vectors for drug and DNA. Nevertheless, the innate hydrophobicity of C constrains its further development. We introduced cyclodextrins to enhance the water-solubility of C. Nine cyclodextrin-C conjugates, including seven α-cyclodextrin-C conjugates and two γ-cyclodextrin-C conjugates, were designed and synthesized. All of these conjugates did not show obvious cytotoxicity. The anti-influenza virus activity of nine conjugates was assessed. Two γ-cyclodextrin-C conjugates, which were relatively more water-soluble, exerted higher inhibition with IC values of 87.73 μM and 75.06 μM, respectively, than seven α-cyclodextrin-C conjugates.
最常见的富勒烯成员 C 表现出许多生物应用，如抗癌、人类免疫缺陷病毒和丙型肝炎病毒抑制剂、O 摄取抑制剂以及药物和 DNA 的载体。然而，C 的固有疏水性限制了它的进一步发展。我们引入了环糊精来提高 C 的水溶性。设计并合成了 9 种环糊精-C 缀合物，包括 7 种α-环糊精-C 缀合物和 2 种γ-环糊精-C 缀合物。所有这些缀合物均没有表现出明显的细胞毒性。评估了 9 种缀合物的抗流感病毒活性。两种相对水溶性更高的γ-环糊精-C 缀合物，其抑制活性分别为 87.73µM 和 75.06µM，高于 7 种α-环糊精-C 缀合物。
