Tangeretin is a naturally polymethoxylated flavone compound extracted from the citrus peel and acts as a Notch-1 inhibitor[1]. Tangeretin exhibits antitumor properties in several types of cancerous cell lines[2] and targets some hallmarks of cancer, such as antiproliferative, apoptotic, anti-inflammatory, anti-metastatic, anti-angiogenic, antioxidant, regulatory expression of tumor-suppressor genes, and epigenetic modulation[3].
Tangeretin (20μM; 24h) inhibits ROS generation and GSH depletion induced by t-BHP in HepG2 cells[4]. Tangeretin (45μM; 48h) treatment increases G2/M arrest and apoptosis by modulating PTEN and cell-cycle regulated genes such as cyclin-D mRNA and protein expressions[5].
Tangeretin (100mg/kg) pre-treatment significantly alleviated liver damage, inhibited cisplatin-induced lipid profile aberrations (total cholesterol and triglycerides) and diminished histopathologic structural damage in rat liver tissues[6]. Tangeretin (100mg/kg; 3d; i.g.) inhibits human respiratory syncytial virus (RSV) replication and RSV-induced lung inflammation in mouse[7].
References:
[1]. Liu LL, Li FH, Zhang Y, et al. Tangeretin has anti-asthmatic effects via regulating PI3K and Notch signaling and modulating Th1/Th2/Th17 cytokine balance in neonatal asthmatic mice. Braz J Med Biol Res. 2017 Jul 20;50(8):e5991. doi: 10.1590/1414-431X20175991. PMID: 28746467; PMCID: PMC5520220.
[2]. Arafa EA, Shurrab NT, Buabeid MA. Therapeutic Implications of a Polymethoxylated Flavone, Tangeretin, in the Management of Cancer via Modulation of Different Molecular Pathways. Adv Pharmacol Pharm Sci. 2021 Mar 5;2021:4709818. doi: 10.1155/2021/4709818. PMID: 33748757; PMCID: PMC7954633.
[3]. de Luna FCF, Ferreira WAS, Casseb SMM, de Oliveira EHC. Anticancer Potential of Flavonoids: An Overview with an Emphasis on Tangeretin. Pharmaceuticals (Basel). 2023 Aug 30;16(9):1229. doi: 10.3390/ph16091229. PMID: 37765037; PMCID: PMC10537037.
[4]. Liang F, Fang Y, Cao W, et al. Attenuation of tert-Butyl Hydroperoxide (t-BHP)-Induced Oxidative Damage in HepG2 Cells by Tangeretin: Relevance of the Nrf2-ARE and MAPK Signaling Pathways. J Agric Food Chem. 2018 Jun 27;66(25):6317-6325. doi: 10.1021/acs.jafc.8b01875. Epub 2018 Jun 14. PMID: 29871486.
[5]. Ma LL, Wang DW, Yu XD, et al. Tangeretin induces cell cycle arrest and apoptosis through upregulation of PTEN expression in glioma cells. Biomed Pharmacother. 2016 Jul;81:491-496. doi: 10.1016/j.biopha.2016.04.006. PMID: 27261630.
[6]. Omar HA, Mohamed WR, Arab HH, et al. Tangeretin Alleviates Cisplatin-Induced Acute Hepatic Injury in Rats: Targeting MAPKs and Apoptosis. PLoS One. 2016 Mar 31;11(3):e0151649. doi: 10.1371/journal.pone.0151649. PMID: 27031695; PMCID: PMC4816535.
[7]. Xu JJ, Liu Z, Tang W, et al. Tangeretin from Citrus reticulate Inhibits Respiratory Syncytial Virus Replication and Associated Inflammation in Vivo. J Agric Food Chem. 2015 Nov 4;63(43):9520-7. doi: 10.1021/acs.jafc.5b03482. Epub 2015 Oct 26. PMID: 26468759.
Tangeretin是一种从柑橘皮中提取的天然多甲氧基黄酮化合物，是Notch-1的抑制剂[1]。Tangeretin在多种癌细胞系中表现出抗肿瘤特性[2]，并针对癌症的多个特征发挥作用，例如抗增殖、促凋亡、抗炎、抗转移、抗血管生成、抗氧化、调控抑癌基因表达以及表观遗传调控等[3]。
Tangeretin（20μM；24小时）在HepG2细胞中可以抑制由t-BHP诱导的ROS生成和GSH耗竭[4]。Tangeretin（45μM; 48h）通过调控PTEN和细胞周期相关基因，比如cyclin-D的mRNA和蛋白质的表达来增加G2/M期阻滞和凋亡[5]。
Tangeretin（100mg/kg）预处理可以显著减轻了肝损伤，抑制顺铂诱导的脂质谱异常（总胆固醇和甘油三酯），并减少大鼠肝组织的组织病理学结构损伤[6]。Tangeretin（100mg/kg; 3d; i.g.）可以抑制人类呼吸道合胞病毒（RSV）的复制和RSV引起的小鼠肺部炎症[7]。