Department of Pathophysiology, School of Basic Medicine, Health Science Center, Yangtze University, Jingzhou, 434023, China.
Laboratory of Oncology, Center for Molecular Medicine, School of Basic Medicine, Health Science Center, Yangtze University, Jingzhou, 434023, China.
Inflammopharmacology. 2024 Dec;32(6):3585-3610. doi: 10.1007/s10787-024-01566-0. Epub 2024 Sep 22.
Quercetin is a natural flavonoid that is widely found in fruits and vegetables. As an important flavonoid, it exhibits a wide range of biological activities, including antioxidant, anti-inflammatory, antiviral, immunomodulatory, and analgesic activities. Quercetin exerts powerful antioxidant activity by regulating glutathione, enzyme activity, and the production of reactive oxygen species (ROS). Quercetin exerts powerful anti-inflammatory effects by acting on the Nod-like receptor protein 3 (NLRP3) inflammasome. In diabetes, quercetin has been shown to improve insulin sensitivity and reduce high blood sugar level, while, in neurological diseases, it potentially prevents neuronal degeneration and cognitive decline by regulating neuroinflammation. In addition, in liver diseases, quercetin may improve liver inflammation and fibrosis by regulating the NLRP3 activity. In addition, quercetin may improve inflammation in other diseases based on the NLRP3 inflammasome. With this background, in this review, we have discussed the progress in the study on the mechanism of quercetin toward improving inflammation via NLRP3 inflammasome in the past decade. In addition, from the perspective of quercetin glycoside derivatives, the anti-inflammatory mechanism of hyperoside, rutin, and isoquercetin based on NLRP3 inflammasome has been discussed. Moreover, we have discussed the pharmacokinetics of quercetin and its nanoformulation application, with the aim to provide new ideas for further research on the anti-inflammatory effect of quercetin and its glycoside derivatives based on NLRP3 inflammasome, as well as in drug development and application.
槲皮素是一种广泛存在于水果和蔬菜中的天然类黄酮。作为一种重要的类黄酮，它具有广泛的生物活性，包括抗氧化、抗炎、抗病毒、免疫调节和镇痛作用。槲皮素通过调节谷胱甘肽、酶活性和活性氧（ROS）的产生来发挥强大的抗氧化活性。槲皮素通过作用于 Nod-like 受体蛋白 3（NLRP3）炎性小体发挥强大的抗炎作用。在糖尿病中，槲皮素已被证明可以提高胰岛素敏感性并降低高血糖水平，而在神经疾病中，它可以通过调节神经炎症来预防神经元变性和认知能力下降。此外，在肝脏疾病中，槲皮素可能通过调节 NLRP3 活性来改善肝脏炎症和纤维化。此外，槲皮素可能基于 NLRP3 炎性小体改善其他疾病的炎症。有鉴于此，在这篇综述中，我们讨论了过去十年中关于槲皮素通过 NLRP3 炎性小体改善炎症的机制的研究进展。此外，从槲皮素糖苷衍生物的角度，讨论了桃叶珊瑚苷、芦丁和异槲皮苷基于 NLRP3 炎性小体的抗炎机制。此外，我们还讨论了槲皮素的药代动力学及其纳米制剂的应用，以期为进一步研究基于 NLRP3 炎性小体的槲皮素及其糖苷衍生物的抗炎作用以及药物开发和应用提供新的思路。
