Kaur Puneet, Gao Jin, Wang Zhenjia
Department of Pharmaceutical Sciences, College of Pharmacy and Pharmaceutical Sciences, Washington State University, Spokane, WA 99210, USA.
Pharmaceutics. 2022 Feb 26;14(3):520. doi: 10.3390/pharmaceutics14030520.
Dietary omega 3 polyunsaturated fatty acids (PUFAs), including docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA), have been reported to be beneficial for cardiovascular diseases and cancer. Such diseases share a common pathophysiological feature of inflammation responses, such as unbalanced oxidative stress and increased cytokine release. PUFAs show anti-inflammatory effects, and thus, they are potential therapeutics to treat inflammatory disorders. Here, we proposed a novel liposomal formulation of EPA (EPA-liposomes), and the liposome was PEGylated to increase their stability. In the study, we measured the physicochemical characteristics of EPA-liposomes and their anti-inflammatory effects in neutrophil-like cells (HL 60 cells). The results showed that EPA-liposomes dramatically decreased the production of NO, ROS, and cytokines compared to EPA alone, and the molecular mechanism is associated with biosynthesis of RvE1 from EPA, and RvE1 binds to GPCRs to mediate the anti-inflammatory effects.
饮食中的ω-3多不饱和脂肪酸(PUFA),包括二十二碳六烯酸(DHA)和二十碳五烯酸(EPA),据报道对心血管疾病和癌症有益。此类疾病具有炎症反应的共同病理生理特征,如氧化应激失衡和细胞因子释放增加。PUFA具有抗炎作用,因此,它们是治疗炎症性疾病的潜在疗法。在此,我们提出了一种新型的EPA脂质体制剂(EPA-脂质体),并对脂质体进行了聚乙二醇化处理以提高其稳定性。在该研究中,我们测量了EPA-脂质体的理化特性及其在中性粒细胞样细胞(HL 60细胞)中的抗炎作用。结果表明,与单独的EPA相比,EPA-脂质体显著降低了NO、ROS和细胞因子的产生,其分子机制与从EPA生物合成RvE1有关,并且RvE1与GPCR结合以介导抗炎作用。