Naringenin chalcone functions as an anti-allergic compound that can be taken orally and has shown effectiveness in reducing human placental CYP19A1 activity with an IC50 value of 2.6μmol/L[1]. Naringenin chalcone is a flavonol biosynthesis intermediate that converts into Naringenin through spontaneous metabolism by chalcone isomerase and serves as a common research subject for anti-inflammatory studies[2].
In vitro, Naringenin chalcone treatment (100µmol/L; 48h) significantly promoted the apoptosis of U87MG human glioblastoma cells, inhibited chromatin condensation, DNA fragmentation and membrane blistering of the cells, and upregulated the expression of all PI3K-related proteins[3]. Naringenin chalcone inhibited the histamine release from rat peritoneal mast cells with IC50 value of 68μg/ml for 24h[4]. After treating 3T3-L1 cells with 100µmol/L Naringenin chalcone for 24h, the genes related to mitochondrial energy metabolism were upregulated and the metabolic function of the cells was improved[5].
In vivo, Naringenin chalcone treatment (80mg/kg/day; p.o.) for 24 days significantly inhibited tumor weight and tumor volume in xenograft tumor model of nude mice[3]. After oral administration of Naringenin chalcone (20mg/kg) to male Sprague-Dawley rats for 24 hours, the level of Naringenin chalcone 2 '-O-β -D-glucuronide in the rat serum increased, inhibiting histamine release[6]. Oral administration of Naringenin chalcone (0.8mg/kg/day) for 23 days can alleviate allergic respiratory tract inflammation in the experimental mouse model of allergic asthma[7].
References:
[1] Wang Y, Pan P, Li X, et al. Food components and environmental chemicals of inhibiting human placental aromatase[J]. Food and Chemical Toxicology, 2019, 128: 46-53.
[2] Kolot C, Rodriguez-Mateos A, Feliciano R, et al. Bioavailability of naringenin chalcone in humans after ingestion of cherry tomatoes[J]. International Journal for Vitamin and Nutrition Research, 2019.
[3] Zhang S, Jiang Z F, Pan Q, et al. Anti-cancer effect of naringenin chalcone is mediated via the induction of autophagy, apoptosis and activation of PI3K/Akt signalling pathway[J]. Bangladesh Journal of Pharmacology, 2016, 11(3): 684-690.
[4] Yamamoto T, Yoshimura M, Yamaguchi F, et al. Anti-allergic activity of naringenin chalcone from a tomato skin extract[J]. Bioscience, biotechnology, and biochemistry, 2004, 68(8): 1706-1711.
[5] Escribano-Ferrer E, Queralt Regue J, Garcia-Sala X, et al. In vivo anti-inflammatory and antiallergic activity of pure naringenin, naringenin chalcone, and quercetin in mice[J]. Journal of natural products, 2019, 82(2): 177-182.
[6] Yoshimura M, Sano A, Kamei J I, et al. Identification and quantification of metabolites of orally administered naringenin chalcone in rats[J]. Journal of agricultural and food chemistry, 2009, 57(14): 6432-6437.
[7] Iwamura C, Shinoda K, Yoshimura M, et al. Naringenin chalcone suppresses allergic asthma by inhibiting the type-2 function of CD4 T cells[J]. Allergology International, 2010, 59(1): 67-73.
Naringenin chalcone是一种口服抗过敏化合物，具有降低人胎盘CYP19A1活性的作用，IC50值为2.6μmol/L[1]。Naringenin chalcone是一种黄酮醇生物合成中间体，通过查尔酮异构酶自发代谢转化为柚皮素，是抗炎研究的常用研究对象[2]。
在体外，Naringenin chalcone处理（100µmol/L; 48h）可显著促进U87MG人胶质母细胞瘤细胞的凋亡，抑制细胞染色质凝聚、DNA断裂和膜起泡，上调所有PI3K相关蛋白的表达[3]。Naringenin chalcone处理24小时可抑制大鼠腹膜肥大细胞的组胺释放，IC50值为68μg/ml[4]。100µmol/L Naringenin chalcone处理3T3-L1细胞24小时后，细胞线粒体能量代谢相关基因上调，细胞代谢功能得到改善[5]。
在体内，Naringenin chalcone处理（80mg/kg/day; p.o.）24天后可显著抑制裸鼠异种移植瘤模型的肿瘤重量和肿瘤体积[3]。口服Naringenin chalcone（20mg/kg）24小时后，雄性SD大鼠血清中柚皮素查尔酮2'-O-β-D-葡糖苷含量升高，Naringenin chalcone可抑制组胺释放[6]。口服Naringenin chalcone（0.8mg/kg/day）23天可减轻实验性哮喘小鼠模型的过敏性呼吸道炎症[7]。