Hesperidin, a flavonoid from the peel of navel orange, inhibits lipid peroxidation with an IC50 value of 179.1μM[1]. Hesperidin possesses strong antioxidant, anti-inflammatory and neuroprotective properties and has been widely used in anti-cancer researches[2-3].
In vitro, Hesperidin treatment for 24h exhibited strong cytotoxic effects on the Caco-2, CEM/ADR5000 and CCRF-CEM cancer cell lines, with IC50 values of 195, 230 and 95µM, respectively[4]. Pretreatment of RAW 264.7 cells with 50μM Hesperidin for 24 hours significantly inhibited the production of NO and PGE2 induced by lipopolysaccharide (LPS) treatment (1μg/mL; 24h), and reduced the levels of pro-inflammatory cytokines (such as TNF-α and IL-6)[5]. Hesperidin treatment (80μM; 24h) significantly increased the expression of PinX1 protein, and inhibited cell proliferation and invasion of Lewis lung carcinoma (LLC) cells, without affecting the viability of normal lung cells[6].
In vivo, Hesperidin treatment at dose of 25mg/kg (1h; p.o.) prevented mechanical ventilation-induced lung damage and improved antioxidant defense in C57BL/6 mice[7]. Oral administration of 100mg/kg/day of Hesperidin to male C57BL/6 mice for seven consecutive days promoted the transport and excretion of bile acids from the liver to the feces, thereby alleviating bile stasis in the mice[8].
References:
[1] Cho J. Antioxidant and neuroprotective effects of hesperidin and its aglycone hesperetin[J]. Archives of pharmacal research, 2006, 29(8): 699-706.
[2] Hajialyani M, Hosein Farzaei M, Echeverría J, et al. Hesperidin as a neuroprotective agent: a review of animal and clinical evidence[J]. Molecules, 2019, 24(3): 648.
[3] Rahmani A H, Babiker A Y, Anwar S. Hesperidin, a bioflavonoid in cancer therapy: a review for a mechanism of action through the modulation of cell signaling pathways[J]. Molecules, 2023, 28(13): 5152.
[4] El-Readi M Z, Hamdan D, Farrag N, et al. Inhibition of P-glycoprotein activity by limonin and other secondary metabolites from Citrus species in human colon and leukaemia cell lines[J]. European Journal of Pharmacology, 2010, 626(2-3): 139-145.
[5] Choi S S, Lee S H, Lee K A. A comparative study of hesperetin, hesperidin and hesperidin glucoside: antioxidant, anti-inflammatory, and antibacterial activities in vitro[J]. Antioxidants, 2022, 11(8): 1618.
[6] Yao Y, Lin M, Liu Z, et al. Hesperidin inhibits lung cancer in vitro and in vivo through PinX1[J]. Frontiers in pharmacology, 2022, 13: 918665.
[7] de Souza A B F, de Matos N A, de Freitas Castro T, et al. Effects in vitro and in vivo of hesperidin administration in an experimental model of acute lung inflammation[J]. Free Radical Biology and Medicine, 2022, 180: 253-262.
[8] Zhang G, Sun X, Wen Y, et al. Hesperidin alleviates cholestasis via activation of the farnesoid X receptor in vitro and in vivo[J]. European journal of pharmacology, 2020, 885: 173498.
Hesperidin是一种从脐橙果皮中提取的黄酮类化合物，能抑制脂质过氧化，IC50值为179.1μM [1]。Hesperidin具有显著的抗氧化、抗炎及神经保护特性，被广泛应用于抗癌研究领域[2-3]。
在体外，Hesperidin处理24小时对Caco-2、CEM/ADR5000和CCRF-CEM癌细胞系表现出强细胞毒作用，IC50值分别为195μM、230μM和95μM[4]。50μM的Hesperidin预处理RAW 264.7细胞24小时可显著抑制脂多糖（LPS）（1μg/mL）诱导NO和PGE2的产生，并降低促炎细胞因子（如TNF-α和IL-6）水平[5]。80μM浓度的Hesperidin处理24小时能显著提升Lewis肺癌（LLC）细胞的PinX1蛋白表达，抑制LLC细胞的增殖与侵袭，且不影响正常肺细胞活性[6]。
在体内，口服25mg/kg剂量的Hesperidin1小时可预防机械通气诱导的C57BL/6小鼠肺损伤并增强抗氧化防御能力[7]。连续7天口服100mg/kg/day剂量的Hesperidin能促进雄性C57BL/6小鼠的胆汁酸从肝脏向粪便的转运与排泄，缓解胆汁淤积症状[8]。