SAAD Centre for Pharmacy and Diabetes, School of Pharmacy and Pharmaceutical Science, Ulster University, Coleraine, County Londonderry, BT52 1SA, UK.
School of Biomedical Sciences, University of Ulster, Coleraine, Northern Ireland, BT52 1SA, UK.
Drug Deliv Transl Res. 2019 Feb;9(1):14-24. doi: 10.1007/s13346-018-00597-9.
Hypoxia inducible factor and nuclear factor-kappa beta pathways have been proposed as therapeutic targets for several inflammatory diseases. Caffeic acid phenethyl ester (CAPE) and piceatannol (PIC) are natural anti-inflammatory compounds; however, poor bioavailability and limited understanding of biomolecular mechanistic limits its clinical use. The aims of this study are to enhance bioavailability and investigate their impact on nuclear p65 and HIF-1α for the first time in experimental colitis.Dextran sulphate sodium was used to induce colitis in mice and effect of either free CAPE/PIC or CAPE/PIC loaded albumin nanoparticles treatment was observed on disease development and levels of cellular p65 and HIF-1α.Our results indicate that albumin nano-encapsulation of CAPE/PIC not only enhances its anti-inflammatory potential but also potentiates its ability to effectively modulate inflammation related biomolecular pathways. Hence, combining nanotechnology with natural compounds could result in development of new therapeutic options for IBD.
缺氧诱导因子和核因子-κB 途径已被提议作为几种炎症性疾病的治疗靶点。咖啡酸苯乙酯 (CAPE) 和白皮杉醇 (PIC) 是天然的抗炎化合物；然而，较差的生物利用度和对生物分子机制的有限理解限制了其临床应用。本研究的目的是提高生物利用度，并首次研究其对核 p65 和 HIF-1α 的影响，以观察实验性结肠炎。葡聚糖硫酸钠用于诱导小鼠结肠炎，并观察游离 CAPE/PIC 或 CAPE/PIC 负载白蛋白纳米颗粒治疗对疾病发展和细胞 p65 和 HIF-1α 水平的影响。我们的结果表明，白蛋白纳米囊封 CAPE/PIC 不仅增强了其抗炎潜力，还增强了其有效调节炎症相关生物分子途径的能力。因此，将纳米技术与天然化合物相结合可能为 IBD 开发新的治疗选择。
