Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, Italy.
Molecules. 2024 Feb 20;29(5):929. doi: 10.3390/molecules29050929.
Diabetes mellitus (DM) is a metabolic disease characterized by hyperglycemia caused by abnormalities in insulin secretion and/or action. In patients with diabetes, complications such as blindness, delayed wound healing, erectile dysfunction, renal failure, heart disease, etc., are generally related to an increase in ROS levels which, when activated, trigger hyperglycemia-induced lesions, inflammation and insulin resistance. In fact, extensive cell damage and death occurs mainly due to the effect that ROS exerts at the level of cellular constituents, causing the deterioration of DNA and peroxidation of proteins and lipids. Furthermore, elevated levels of reactive oxygen species (ROS) and an imbalance of redox levels in diabetic patients produce insulin resistance. These destructive effects can be controlled by the defense network of antioxidants of natural origin such as phloretin and gallic acid. For this reason, the objective of this work was to create a nanocarrier (hydrogel) based on gallic acid containing phloretin to increase the antioxidant effect of the two substances which function as fundamental for reducing the mechanisms linked to oxidative stress in patients suffering from chronic diabetes. Furthermore, since the bioavailability problems of phloretin at the intestinal level are known, this carrier could facilitate its release and absorption. The obtained hydrogel was characterized using Fourier transform infrared spectroscopy (FT-IR). Its degree of swelling (a%) and phloretin release were tested under pH conditions simulating the gastric and intestinal environment (1.2, 6.8 and 7.4). The antioxidant activity, inhibiting lipid peroxidation in rat liver microsomal membranes induced in vitro by a free radical source, was evaluated for four hours. All results showed that gallate hydrogel could be applied for releasing intestinal phloretin and reducing the ROS levels.
糖尿病(DM)是一种代谢疾病,其特征是由于胰岛素分泌和/或作用异常导致的高血糖。在糖尿病患者中,失明、伤口愈合延迟、勃起功能障碍、肾衰竭、心脏病等并发症通常与 ROS 水平升高有关,ROS 被激活后会引发高血糖引起的损伤、炎症和胰岛素抵抗。事实上,广泛的细胞损伤和死亡主要是由于 ROS 在细胞成分水平上产生的影响,导致 DNA 恶化和蛋白质及脂质的过氧化。此外,糖尿病患者中活性氧(ROS)水平升高和氧化还原水平失衡会导致胰岛素抵抗。这些破坏性影响可以通过天然抗氧化剂如根皮素和没食子酸的抗氧化防御网络来控制。出于这个原因,这项工作的目的是创建一种基于含有根皮素的没食子酸的纳米载体(水凝胶),以增加这两种物质的抗氧化作用,这两种物质是减少慢性糖尿病患者与氧化应激相关机制的基础。此外,由于已知根皮素在肠道水平的生物利用度问题,这种载体可以促进其释放和吸收。使用傅里叶变换红外光谱(FT-IR)对所得水凝胶进行了表征。在模拟胃和肠道环境的 pH 条件下(1.2、6.8 和 7.4),测试了水凝胶的溶胀度(a%)和根皮素释放情况。评估了水凝胶在体外由自由基源诱导的大鼠肝微粒体膜中抑制脂质过氧化的抗氧化活性,持续四个小时。所有结果表明,没食子酸水凝胶可用于释放肠道中的根皮素并降低 ROS 水平。