用于靶向抗炎治疗的甘露糖修饰人参皂苷Rb1白蛋白纳米粒

Mannose-decorated ginsenoside Rb1 albumin nanoparticles for targeted anti-inflammatory therapy.

作者信息

Fu Zhihui, Wang Xiaohui, Lu Xuan, Yang Ying, Zhao Lingling, Zhou Lin, Wang Kaikai, Fu Hanlin

机构信息

The First Affiliated Hospital of Zhengzhou University, Zhengzhou, China.

School of Pharmacy and Affiliated Hospital of Nantong University, Nantong University, Nantong, China.

出版信息

Front Bioeng Biotechnol. 2022 Aug 15;10:962380. doi: 10.3389/fbioe.2022.962380. eCollection 2022.

Ginsenoside Rb1 is a potential anti-inflammatory natural molecule, but its therapeutic efficacy was tremendously hampered by the low solubility and non-targeted delivery. In this study, we innovatively developed a mannose (Man)-modified albumin bovine serum albumin carrier (Man-BSA) to overcome the previously mentioned dilemmas of Rb1. The constructed Man-BSA@Rb1 NPs could improve the solubility and increase the cellular uptake of Rb1, finally leading to the enhanced anti-inflammatory effects. The robust therapeutics of Man-BSA@Rb1 NPs were measured in terms of nitrite, tumor necrosis factor-α (TNF-α), and interleukin-6 (IL-6) levels, which might be achieved by potently inhibiting nuclear factor-κB (NF-κB) and mitogen-activated protein kinase (MAPK) signaling pathways in lipopolysaccharide (LPS)-induced Raw264.7 cells. Moreover, the therapeutic efficacy of Man-BSA@Rb1 NPs was further confirmed in the d-Gal/LPS-induced liver injury model. The results indicated that Man-BSA may offer a promising system to improve the anti-inflammatory therapy of Rb1.

人参皂苷Rb1是一种具有潜在抗炎作用的天然分子，但其治疗效果因溶解度低和非靶向递送而受到极大阻碍。在本研究中，我们创新性地开发了一种甘露糖（Man）修饰的牛血清白蛋白载体（Man-BSA），以克服Rb1上述的困境。构建的Man-BSA@Rb1纳米粒可以提高Rb1的溶解度并增加其细胞摄取量，最终增强抗炎效果。通过检测亚硝酸盐、肿瘤坏死因子-α（TNF-α）和白细胞介素-6（IL-6）水平来衡量Man-BSA@Rb1纳米粒强大的治疗效果，这可能是通过有效抑制脂多糖（LPS）诱导的Raw264.7细胞中的核因子-κB（NF-κB）和丝裂原活化蛋白激酶（MAPK）信号通路来实现的。此外，在d-半乳糖/LPS诱导的肝损伤模型中进一步证实了Man-BSA@Rb1纳米粒的治疗效果。结果表明，Man-BSA可能为改善Rb1的抗炎治疗提供一个有前景的系统。