关键词: Alzheimer disease Anthocyanin C3G anti-inflammatory activity C3G anti-oxidant activity C3G bioavailability Cancer Energy homeostasis Gut microbiota dysbiosis Inflammatory bowel disease Insulin resistance Lipid metabolism Liver steatosis

Mesh : Humans Anthocyanins / pharmacology therapeutic use Obesity / metabolism prevention & control Animals Glucosides / therapeutic use pharmacology Metabolic Diseases / metabolism prevention & control Lipid Metabolism / drug effects Energy Metabolism / drug effects

来  源:   DOI:10.1016/j.bbrc.2024.150344

Abstract:
Anthocyanins, found in various pigmented plants as secondary metabolites, represent a class of dietary polyphenols known for their bioactive properties, demonstrating health-promoting effects against several chronic diseases. Among these, cyanidin-3-O-glucoside (C3G) is one of the most prevalent types of anthocyanins. Upon consumption, C3G undergoes phases I and II metabolism by oral epithelial cells, absorption in the gastric epithelium, and gut transformation (phase II & microbial metabolism), with limited amounts reaching the bloodstream. Obesity, characterized by excessive body fat accumulation, is a global health concern associated with heightened risks of disability, illness, and mortality. This comprehensive review delves into the biodegradation and absorption dynamics of C3G within the gastrointestinal tract. It meticulously examines the latest research findings, drawn from in vitro and in vivo models, presenting evidence underlining C3G\'s bioactivity. Notably, C3G has demonstrated significant efficacy in combating obesity, by regulating lipid metabolism, specifically decreasing lipid synthesis, increasing fatty acid oxidation, and reducing lipid accumulation. Additionally, C3G enhances energy homeostasis by boosting energy expenditure, promoting the activity of brown adipose tissue, and stimulating mitochondrial biogenesis. Furthermore, C3G shows potential in managing various prevalent obesity-related conditions. These include cardiovascular diseases (CVD) and hypertension through the suppression of reactive oxygen species (ROS) production, enhancement of endogenous antioxidant enzyme levels, and inhibition of the nuclear factor-kappa B (NF-κB) signaling pathway and by exercising its cardioprotective and vascular effects by decreasing pulmonary artery thickness and systolic pressure which enhances vascular relaxation and angiogenesis. Type 2 diabetes mellitus (T2DM) and insulin resistance (IR) are also managed by reducing gluconeogenesis via AMPK pathway activation, promoting autophagy, protecting pancreatic β-cells from oxidative stress and enhancing glucose-stimulated insulin secretion. Additionally, C3G improves insulin sensitivity by upregulating GLUT-1 and GLUT-4 expression and regulating the PI3K/Akt pathway. C3G exhibits anti-inflammatory properties by inhibiting the NF-κB pathway, reducing pro-inflammatory cytokines, and shifting macrophage polarization from the pro-inflammatory M1 phenotype to the anti-inflammatory M2 phenotype. C3G demonstrates antioxidative effects by enhancing the expression of antioxidant enzymes, reducing ROS production, and activating the Nrf2/AMPK signaling pathway. Moreover, these mechanisms also contribute to attenuating inflammatory bowel disease and regulating gut microbiota by decreasing Firmicutes and increasing Bacteroidetes abundance, restoring colon length, and reducing levels of inflammatory cytokines. The therapeutic potential of C3G extends beyond metabolic disorders; it has also been found effective in managing specific cancer types and neurodegenerative disorders. The findings of this research can provide an important reference for future investigations that seek to improve human health through the use of naturally occurring bioactive compounds.
摘要:
花青素,在各种色素植物中作为次生代谢产物发现,代表一类以其生物活性特性而闻名的膳食多酚,证明对几种慢性疾病的健康促进作用。其中,花色素苷-3-O-葡萄糖苷(C3G)是最常见的花色素苷类型之一。消费时,C3G经历口腔上皮细胞的I期和II期代谢,在胃上皮的吸收,和肠道转化(第二阶段和微生物代谢),有限的量进入血液。肥胖,以体内脂肪积累过多为特征,是与残疾风险增加相关的全球健康问题,疾病,和死亡率。这篇全面的综述探讨了C3G在胃肠道内的生物降解和吸收动力学。它仔细检查了最新的研究结果,从体外和体内模型中提取,提供证据强调C3G的生物活性。值得注意的是,C3G在对抗肥胖方面表现出显著的功效,通过调节脂质代谢,特别是减少脂质合成,增加脂肪酸氧化,减少脂质积累。此外,C3G通过增加能量消耗来增强能量稳态,促进棕色脂肪组织的活性,并刺激线粒体生物发生。此外,C3G显示出管理各种普遍肥胖相关疾病的潜力。这些包括通过抑制活性氧(ROS)产生的心血管疾病(CVD)和高血压,增强内源性抗氧化酶水平,和抑制核因子-κB(NF-κB)信号通路,并通过降低肺动脉厚度和收缩压来行使其心脏保护和血管作用,从而增强血管舒张和血管生成。2型糖尿病(T2DM)和胰岛素抵抗(IR)也通过AMPK途径激活减少糖异生来管理,促进自噬,保护胰腺β细胞免受氧化应激和增强葡萄糖刺激的胰岛素分泌。此外,C3G通过上调GLUT-1和GLUT-4的表达和调节PI3K/Akt途径来改善胰岛素敏感性。C3G通过抑制NF-κB途径表现出抗炎特性,减少促炎细胞因子,并将巨噬细胞极化从促炎M1表型转变为抗炎M2表型。C3G通过增强抗氧化酶的表达显示抗氧化作用,减少ROS的产生,并激活Nrf2/AMPK信号通路。此外,这些机制还有助于减轻炎症性肠病和通过减少Firmicutes和增加拟杆菌丰度来调节肠道微生物群,恢复结肠长度,并降低炎症细胞因子的水平。C3G的治疗潜力超出了代谢紊乱;它也被发现在管理特定癌症类型和神经退行性疾病方面有效。这项研究的发现可以为将来寻求通过使用天然存在的生物活性化合物来改善人类健康的研究提供重要参考。
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