Feng Ya-Li, Li Hao, Liu Juan, Ruan Zheng, Zhai Guang-Yu
School of Pharmacy and Chemical Engineering, Zhengzhou University of Industrial Technology Zhengzhou 451100, China.
Zhongguo Zhong Yao Za Zhi. 2021 Oct;46(20):5185-5193. doi: 10.19540/j.cnki.cjcmm.20210524.602.
Quercetin is a naturally occurring phytochemical with good bioactivity, which mainly exists in the form of glycoside in vegetables, fruits, tea, and wine and exhibits beneficial health effects. Quercetin is a dietary polyphenol that exerts the protective effects through diet or use as a food supplement. Compared with chemical agents, quercetin is widely available and safe. Quercetin has been extensively studied for its anti-diabetic, anti-hypertensive, anti-Alzheimer's disease, anti-arthritic, anti-influenza virus, anti-microbial infection, anti-aging, autophagy-regulating, and cardiovascular protective effects. Studies on its activities against different can-cer cell lines have also been reported recently. However, the poor water solubility, rapid in vivo metabolism, and short half-life of quercetin have led to its low bioavailability, thus limiting its application in the field of medicine. Quercetin nanoparticles and nanoparticle drug delivery system have been effectively utilized for enhancing its bioavailability. This paper reviewed the therapeutic potential of quercetin from both preclinical and clinical aspects and proposed solutions to improve its bioavailability, so as to provide a reference for the therapeutic application of natural compounds in the field of medicine.
槲皮素是一种具有良好生物活性的天然植物化学物质,主要以糖苷形式存在于蔬菜、水果、茶和葡萄酒中,并具有有益的健康作用。槲皮素是一种膳食多酚,可通过饮食或用作食品补充剂发挥保护作用。与化学药剂相比,槲皮素广泛可得且安全。槲皮素因其抗糖尿病、抗高血压、抗阿尔茨海默病、抗关节炎、抗流感病毒、抗微生物感染、抗衰老、自噬调节和心血管保护作用而受到广泛研究。最近也有关于其对不同癌细胞系活性的研究报道。然而,槲皮素的水溶性差、体内代谢快和半衰期短导致其生物利用度低,从而限制了其在医学领域的应用。槲皮素纳米颗粒和纳米颗粒药物递送系统已被有效地用于提高其生物利用度。本文从临床前和临床两个方面综述了槲皮素的治疗潜力,并提出了提高其生物利用度的解决方案,以期为天然化合物在医学领域的治疗应用提供参考。