In this study, blood- and cardio-toxicity of Rh2–treated graphene oxide (GO-Rh2), lysine-treated graphene oxide (GO-Lys), arginine-treated GO (GO-Arg), Rh2–treated GO-Lys (GO-Lys-Rh2) and Rh2–treated GO-Arg (GO-Arg-Rh2) were evaluated. Two concentrations of each nanostructures (200 and 1000 µg/ml) was injected to rats. After 2 weeks, the effects of agents were evaluated on heart tissue by histopathological assays. Cytotoxicity of all designed nanostructures was investigated on blood cancer cells (K562) by MTT assay. Toxicity of designed nanostructures was also investigated on Red Blood Cells (RBCs), Prothrombin Time (PT) and Partial Thromboplastin Time (PTT). The results demonstrated increase of anticancer activity for GO-Arg-Rh2 and GO-Lys-Rh2 in comparison with free Rh2 and GO. GO, GO-Rh2, GO-Lys, GO-Arg, GO-Lys-Rh2, and GO-Arg-Rh2 had 50% hemolysis at concentrations 250, 360, 420, 435, 500, and 575 µg/ml, respectively. GO led to RBCs aggregation and morphological change at 5–100 µg/ml, but other functionalized nanostructures did not show these changes. All nanostructures had slight effect on intrinsic and extrinsic coagulation system, especially on PTT. GO-Arg-Rh2 and GO-Lys-Rh2 had lower effect on blood coagulation system in comparison with other examined nanosystems. Besides, GO-Rh2, GO-Arg-Rh2, and GO-Lys-Rh2 had lowest toxicity on heart tissue than other synthesized nanostructures. Functionalization of GO with Arg, Lys, and especially, Rh2 led to decrease the destruction of heart tissue. So, modified GO with Rh2 and basic amino acids may be a potential and promising strategy to enhance the therapeutic index for GO because of the reduction of side effects on normal cells.

在这项研究中，Rh2处理过的氧化石墨烯（GO-Rh2），赖氨酸处理过的氧化石墨烯（GO-Lys），精氨酸处理过的GO（GO-Arg），Rh2处理过的GO-Lys（对GO-Lys-Rh2）和经Rh2处理的GO-Arg（GO-Arg-Rh2）进行了评估。将两种浓度的每种纳米结构（200和1000 µg / ml）注射到大鼠中。2周后，通过组织病理学分析评估药剂对心脏组织的作用。通过MTT测定法研究了所有设计的纳米结构对血液癌细胞（K562）的细胞毒性。还对红细胞（RBC），凝血酶原时间（PT）和部分凝血活酶时间（PTT）的设计纳米结构的毒性进行了研究。结果证明与游离Rh2和GO相比，GO-Arg-Rh2和GO-Lys-Rh2的抗癌活性增加。GO，GO-Rh2，GO-Lys，GO-Arg，GO-Lys-Rh2，和GO-Arg-Rh2在浓度分别为250、360、420、435、500和575 µg / ml时有50％的溶血作用。GO导致RBC聚集和5-100 µg / ml的形态变化，但其他功能化的纳米结构未显示出这些变化。所有的纳米结构对内在和外在的凝结系统都有轻微的影响，特别是对PTT。与其他检查的纳米系统相比，GO-Arg-Rh2和GO-Lys-Rh2对凝血系统的影响较小。此外，GO-Rh2，GO-Arg-Rh2和GO-Lys-Rh2对心脏组织的毒性比其他合成的纳米结构最低。GO与Arg，Lys，尤其是Rh2的功能化可减少心脏组织的破坏。所以，