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槲皮素作为一种有前景的抗2型糖尿病治疗药物的潜力。

Potential of Quercetin as a Promising Therapeutic Agent Against Type 2 Diabetes.

作者信息

Niziński Przemysław, Hawrył Anna, Polak Paweł, Kondracka Adrianna, Oniszczuk Tomasz, Soja Jakub, Hawrył Mirosław, Oniszczuk Anna

机构信息

Department of Pharmacology, Medical University of Lublin, Radziwiłłowska 11, 20-080 Lublin, Poland.

Department of Inorganic Chemistry, Medical University of Lublin, Chodźki 4a, 20-093 Lublin, Poland.

出版信息

Molecules. 2025 Jul 24;30(15):3096. doi: 10.3390/molecules30153096.

Abstract

Quercetin (QE) is a naturally occurring flavonoid found in many fruits, vegetables, and other plant-based foods. It is recognized for its diverse pharmacological activities. Among its many therapeutic potentials, its antidiabetic properties are of particular interest due to the growing worldwide prevalence of diabetes mellitus. QE improves glycemic control by enhancing insulin sensitivity, stimulating glucose uptake, and preserving pancreatic beta cell function. These effects are mediated by the modulation of key molecular pathways, including AMPK, PI3K/Akt, and Nrf2/ARE, as well as by the suppression of oxidative stress and pro-inflammatory cytokines, such as TNF-α and IL-6. Furthermore, QE mitigates the progression of diabetic complications such as nephropathy, retinopathy, and vascular dysfunction, reducing lipid peroxidation and protecting endothelial function. However, the clinical application of quercetin is limited by its low water solubility, poor bioavailability, and extensive phase II metabolism. Advances in formulation strategies, including the use of nanocarriers, co-crystals, and phospholipid complexes, have shown promise in improving its pharmacokinetics. This review elucidates the mechanistic basis of QE quercetin antidiabetic action and discusses strategies to enhance its therapeutic potential in clinical settings.

摘要

槲皮素(QE)是一种天然存在的类黄酮,存在于许多水果、蔬菜和其他植物性食物中。它因其多样的药理活性而被认可。在其众多治疗潜力中,由于全球糖尿病患病率不断上升,其抗糖尿病特性尤其受到关注。QE通过增强胰岛素敏感性、刺激葡萄糖摄取和维持胰腺β细胞功能来改善血糖控制。这些作用是通过调节关键分子途径介导的,包括AMPK、PI3K/Akt和Nrf2/ARE,以及通过抑制氧化应激和促炎细胞因子,如TNF-α和IL-6。此外,QE减轻糖尿病并发症如肾病、视网膜病变和血管功能障碍的进展,减少脂质过氧化并保护内皮功能。然而,槲皮素的临床应用受到其低水溶性、低生物利用度和广泛的II期代谢的限制。制剂策略的进展,包括使用纳米载体、共晶体和磷脂复合物,已显示出改善其药代动力学的前景。本综述阐明了QE槲皮素抗糖尿病作用的机制基础,并讨论了在临床环境中增强其治疗潜力的策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b7cd/12348926/fa984457bc26/molecules-30-03096-g001.jpg

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