Rouse Jillian G, Yang Jianzhong, Barron Andrew R, Monteiro-Riviere Nancy A
Center for Chemical Toxicology Research and Pharmacokinetics, North Carolina State University, 4700 Hillsborough Street, Raleigh, NC 27606, USA.
Toxicol In Vitro. 2006 Dec;20(8):1313-20. doi: 10.1016/j.tiv.2006.04.004. Epub 2006 May 3.
The functionalization of C(60) with such complexes as amino acids has the potential to provide greater interaction between the fullerene and the biological environment yielding potential new medical and pharmacological applications. Although scientific research in the past decade has revealed much about the chemical and physical properties of C(60), the biological activities of this compound and its derivatives are still relatively unclear. In an attempt to understand the biological activity of functionalized C(60), human epidermal keratinocytes (HEK) were exposed to fullerene-based amino acid (Baa) solutions ranging in concentrations of 0.4-0.00004 mg/mL in a humidified 5% CO(2) atmosphere at 37 degrees C. MTT cell viability after 48 h significantly decreased (p<0.05) for concentrations of 0.4 and 0.04 mg/mL. In an additional study, human cytokines IL-6, IL-8, TNF-alpha, IL-1beta, and IL-10 were assessed for concentrations ranging from 0.4-0.004 mg/mL. Media was harvested at 1, 4, 8, 12, 24 and 48 h for cytokine analysis. IL-8 concentrations for the 0.04 mg/mL treatment were significantly greater (p<0.05) than all other concentrations at 8, 12, 24, and 48 h. IL-6 and IL-1beta activities were greater at the 24h and 48 h for 0.4 and 0.04 mg/mL. No significant TNF-alpha or IL-10 activity existed at any time points for any of the concentrations. These results indicate that concentrations lower than 0.04 mg/mL initiate less cytokine activity and maintain cell viability. In HEK, Baa concentrations of 0.4 and 0.04 mg/mL decrease cell viability and initiate a pro-inflammatory response.
用氨基酸等复合物对C(60)进行功能化处理，有可能增强富勒烯与生物环境之间的相互作用，从而产生潜在的新医学和药理学应用。尽管过去十年的科学研究已经揭示了许多关于C(60)的化学和物理性质，但这种化合物及其衍生物的生物活性仍然相对不清楚。为了了解功能化C(60)的生物活性，将人表皮角质形成细胞（HEK）置于37摄氏度、湿度为5% CO(2)的气氛中，暴露于浓度范围为0.4 - 0.00004 mg/mL的基于富勒烯的氨基酸（Baa）溶液中。48小时后，浓度为0.4和0.04 mg/mL时，MTT细胞活力显著下降（p<0.05）。在另一项研究中，评估了浓度范围为0.4 - 0.004 mg/mL的人细胞因子IL-6、IL-8、TNF-α、IL-1β和IL-10。在1、4、8、12、24和48小时收集培养基用于细胞因子分析。在8、12、24和48小时，0.04 mg/mL处理组的IL-8浓度显著高于所有其他浓度（p<0.05）。在24小时和48小时，0.4和0.04 mg/mL组的IL-6和IL-1β活性更高。在任何浓度下的任何时间点，均未观察到显著的TNF-α或IL-10活性。这些结果表明，低于0.04 mg/mL的浓度引发的细胞因子活性较低并维持细胞活力。在HEK中，0.4和0.04 mg/mL的Baa浓度会降低细胞活力并引发促炎反应。
