Iohara Daisuke
Faculty of Pharmaceutical Sciences, Sojo University.
Yakugaku Zasshi. 2019;139(12):1539-1546. doi: 10.1248/yakushi.19-00172.
Fullerenes, large spherical molecules composed solely of carbon atoms, have gathered much attention for practical applications that take advantage of their unique spherical structure, physical properties, and biological activities. For example, fullerene C can function as a photosensitizer, an antioxidant, a bioimaging agent, and as a gene or drug carrier. However, the practical use of C for these potential biomedical applications has been hampered by the fact that it is only sparingly soluble in water. In this review, we focus on the development of hydrophilic C nanoparticles, the surface of which is covered by cyclodextrin (CD), and then evaluate its biological activities. C/CD nanoparticles were stable under physiological conditions, and even under much harsher conditions. The nanoparticles generate reactive oxygen species (ROS) under visible light irradiation. Efficient photodynamic therapy against tumor growth was achieved by the intravenous injection of C/CD nanoparticles to tumor bearing mice, followed by photoirradiation. In addition, C(OH), which is regarded as a potential candidate for use in scavenging ROS, was also prepared in the form of water soluble nanoparticles. C(OH)/CD nanoparticles protect the liver from injury by the suppression of oxidative stress occurring in the mitochondria, for example, by scavenging ROS such as superoxide anion radicals (O), nitric oxide (NO) and peroxynitrite (ONOO), which act as critical mediators in liver injuries. C-based nanoparticles represent a potentially promising material for use in the treatment of cancer and oxidative stress-related diseases, and are promising as well in terms of extensive biological applications.
富勒烯是仅由碳原子组成的大型球形分子,因其独特的球形结构、物理性质和生物活性在实际应用中备受关注。例如,富勒烯C可作为光敏剂、抗氧化剂、生物成像剂以及基因或药物载体。然而,C在这些潜在生物医学应用中的实际应用受到其在水中溶解度极低这一事实的阻碍。在本综述中,我们聚焦于亲水性C纳米颗粒的研发,其表面被环糊精(CD)覆盖,然后评估其生物活性。C/CD纳米颗粒在生理条件下甚至在更严苛的条件下都很稳定。这些纳米颗粒在可见光照射下产生活性氧(ROS)。通过向荷瘤小鼠静脉注射C/CD纳米颗粒,随后进行光照射,实现了对肿瘤生长的高效光动力治疗。此外,被视为清除ROS潜在候选物的C(OH)也被制备成水溶性纳米颗粒的形式。例如,C(OH)/CD纳米颗粒通过清除诸如超氧阴离子自由基(O)、一氧化氮(NO)和过氧亚硝酸盐(ONOO)等作为肝损伤关键介质的ROS,抑制线粒体中发生的氧化应激,从而保护肝脏免受损伤。基于C的纳米颗粒是用于治疗癌症和氧化应激相关疾病的潜在有前景的材料,在广泛的生物应用方面也很有前景。