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载有欧米伽-3 多不饱和脂肪酸的基于白藜芦醇的固体脂质纳米粒:体外对人结直肠癌细胞的理化性质和抗肿瘤活性。

Omega-3 PUFA Loaded in Resveratrol-Based Solid Lipid Nanoparticles: Physicochemical Properties and Antineoplastic Activities in Human Colorectal Cancer Cells In Vitro.

机构信息

Institute of General Pathology, School of Medicine, Università Cattolica del Sacro Cuore, Largo F. Vito, 1, 00168 Roma, Italy.

Department of Pharmacy, Health and Nutritional Sciences, Università della Calabria, Via Pietro Bucci, 87036 Arcavacata di Rende, Cosenza, Italy.

出版信息

Int J Mol Sci. 2018 Feb 16;19(2):586. doi: 10.3390/ijms19020586.

Abstract

New strategies are being investigated to ameliorate the efficacy and reduce the toxicity of the drugs currently used in colorectal cancer (CRC), one of the most common malignancies in the Western world. Data have been accumulated demonstrating that the antineoplastic therapies with either conventional or single-targeted drugs could take advantage from a combined treatment with omega-3 polyunsaturated fatty acids (omega-3 PUFA). These nutrients, shown to be safe at the dosage generally used in human trials, are able to modulate molecules involved in colon cancer cell growth and survival. They have also the potential to act against inflammation, which plays a critical role in CRC development, and to increase the anti-cancer immune response. In the present study, omega-3 PUFA were encapsulated in solid lipid nanoparticles (SLN) having a lipid matrix containing resveratrol esterified to stearic acid. Our aim was to increase the efficiency of the incorporation of these fatty acids into the cells and prevent their peroxidation and degradation. The Resveratrol-based SLN were characterized and investigated for their antioxidant activity. It was observed that the encapsulation of omega-3 PUFA into the SLN enhanced significantly their incorporation in human HT-29 CRC cells in vitro, and their growth inhibitory effects in these cancer cells, mainly by reducing cell proliferation.

摘要

新策略正在被研究以提高目前用于结直肠癌(CRC)治疗的药物的疗效并降低其毒性,CRC 是西方世界最常见的恶性肿瘤之一。已经积累了大量数据表明,无论是常规药物还是单一靶向药物的抗肿瘤治疗都可以从与ω-3 多不饱和脂肪酸(ω-3 PUFA)联合治疗中获益。这些营养素在人体试验中通常使用的剂量下被证明是安全的,能够调节参与结肠癌细胞生长和存活的分子。它们还具有对抗炎症的潜力,炎症在 CRC 的发展中起着关键作用,并能增强抗癌免疫反应。在本研究中,ω-3 PUFA 被包封在固体脂质纳米粒(SLN)中,其脂质基质含有酯化到硬脂酸的白藜芦醇。我们的目的是提高这些脂肪酸进入细胞的效率并防止其过氧化和降解。对基于白藜芦醇的 SLN 进行了表征并研究了其抗氧化活性。结果观察到,将 ω-3 PUFA 包封到 SLN 中显著提高了它们在人 HT-29 CRC 细胞中的体外摄取率,并增强了它们在这些癌细胞中的生长抑制作用,主要通过降低细胞增殖来实现。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3158/5855808/44c79f8f427e/ijms-19-00586-sch001.jpg

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