Nahar Pragati P, Slitt Angela L, Seeram Navindra P
Bioactive Botanical Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island , Kingston, Rhode Island, USA.
J Med Food. 2015 Jul;18(7):786-92. doi: 10.1089/jmf.2014.0053. Epub 2014 Dec 9.
Inflammation and the presence of pro-inflammatory cytokines are associated with numerous chronic diseases such as type-2 diabetes mellitus, cardiovascular disease, Alzheimer's disease, and cancer. An overwhelming amount of data indicates that curcumin, a polyphenol obtained from the Indian spice turmeric, Curcuma longa, is a potential chemopreventive agent for treating certain cancers and other chronic inflammatory diseases. However, the low bioavailability of curcumin, partly due to its low solubility and stability in the digestive tract, limits its therapeutic applications. Recent studies have demonstrated increased bioavailability and health-promoting effects of a novel solid lipid particle formulation of curcumin (Curcumin SLCP, Longvida(®)). The goal of this study was to evaluate the aqueous solubility and in vitro anti-inflammatory effects of solid lipid curcumin particle (SLCP) formulations using lipopolysaccharide (LPS)-stimulated RAW 264.7 cultured murine macrophages. SLCPs treatment significantly decreased nitric oxide (NO) and prostaglandin-E2 (PGE2) levels at concentrations ranging from 10 to 50 μg/mL, and reduced interleukin-6 (IL-6) levels in a concentration-dependent manner. Transient transfection experiments using a nuclear factor-kappa B (NF-κB) reporter construct indicate that SLCPs significantly inhibit the transcriptional activity of NF-κB in macrophages. Taken together, these results show that in RAW 264.7 murine macrophages, SLCPs have improved solubility over unformulated curcumin, and significantly decrease the LPS-induced pro-inflammatory mediators NO, PGE2, and IL-6 by inhibiting the activation of NF-κB.
炎症和促炎细胞因子的存在与许多慢性疾病相关,如2型糖尿病、心血管疾病、阿尔茨海默病和癌症。大量数据表明,姜黄素是一种从印度香料姜黄(Curcuma longa)中提取的多酚,是一种潜在的化学预防剂,可用于治疗某些癌症和其他慢性炎症性疾病。然而,姜黄素的低生物利用度,部分原因是其在消化道中的低溶解度和稳定性,限制了其治疗应用。最近的研究表明,一种新型的姜黄素固体脂质颗粒制剂(Curcumin SLCP,Longvida®)具有更高的生物利用度和促进健康的作用。本研究的目的是使用脂多糖(LPS)刺激的RAW 264.7培养的小鼠巨噬细胞,评估固体脂质姜黄素颗粒(SLCP)制剂的水溶性和体外抗炎作用。SLCP处理在10至50μg/mL的浓度范围内显著降低了一氧化氮(NO)和前列腺素E2(PGE2)水平,并以浓度依赖的方式降低了白细胞介素-6(IL-6)水平。使用核因子κB(NF-κB)报告构建体的瞬时转染实验表明,SLCP显著抑制巨噬细胞中NF-κB的转录活性。综上所述,这些结果表明,在RAW 264.7小鼠巨噬细胞中,SLCP比未配制的姜黄素具有更高的溶解度,并通过抑制NF-κB的激活显著降低LPS诱导的促炎介质NO、PGE2和IL-6。