Due to the unique physicochemical properties, graphene oxide has been widely applied in material chemistry, biomedical science and life science. However, here is still a great challenge to maximize the advantages of graphene oxide and overcome the deleterious effects caused by its inherent properties. For a better understanding of current status in this research field, recent progress in surface chemical modifications of graphene oxide and interaction mechanisms at the nano-bio interface has been comprehensively reviewed. First, the physicochemical properties of graphene oxide and the representative strategies of surface chemical modifications will be briefly introduced, including oxidation and reduction, carboxylation, amination, small organic molecule modification, polymer modification, peptide/protein modification, nucleic acid modification and nanoparticle modification, as well as their potential roles in mediating the graphene oxide-resulted biological effects. Following, we will present the primary interaction mechanisms of pristine and surface-modified graphene oxide at the nano-bio interface, including the formation of protein corona, cell membrane damage, membrane receptor interaction and oxidative stress. Finally, the knowledge gaps and future challenges in this research field will be detailedly discussed. Keywords graphene oxide; surface chemical modification; nano-bio interface; interaction mechanism; biological effect 1 引言 2004 年, Geim 等 [1] 首次通过机械剥离法制得单层石 墨烯. 石墨烯(graphene)是一种二维纳米材料, 具有类 似蜂巢的六元环平面网状结构, 厚度仅为 0.3354 nm [1] . 在石墨烯的纳米片层结构中, 碳原子发生了 sp 2 杂化, 每个碳原子通过键长为 142 nm 的 σ 键与其它三个碳原 子连接, 并在与片层垂直的方向形成离域大 π 键 [2,3] . 这 些结构特征赋予了石墨烯优异的机械强度、化学稳定 性、高比表面积、导电和导热性能 [4][5][6][7] . 因此, 石墨烯在 能源、材料、健康、环境等方面都展现了广阔的应用前 景.石墨烯拥有多种衍生物, 包括氧化石墨烯(graphene oxide, GO)、还原氧化石墨烯(reduced graphene oxide, rGO)、氟化石墨烯(fluorographene)等.