7,4'-Dihydroxyflavone
(Synonyms: 7,4'-二羟基黄酮) 目录号 : GC35185
7,4'-Dihydroxyflavone是一种从甘草(Glycyrrhiza uralensis)中分离得到的口服活性黄酮类化合物,可作为嗜酸性粒细胞趋化因子/CCL11和羰基还原酶1(CBR1)的抑制剂。
Cas No.:2196-14-7
Sample solution is provided at 25 µL, 10mM.
7,4'-Dihydroxyflavone ,an orally active flavonoid isolated from Glycyrrhiza uralensis (licorice), functions as an inhibitor of eotaxin/CCL11 and carbonyl reductase 1 (CBR1) [1]. It persistently suppresses eotaxin production and prevents the rebound effect of dexamethasone (Dex) on eotaxin generation [2]. Furthermore,7,4'-Dihydroxyflavone inhibits MUC5AC gene expression, mucus production, and secretion by modulating the NF-κB, STAT6, and HDAC2 signaling pathways[3].
In human lung fibroblast-1 cells, 7,4'-Dihydroxyflavone (10μM; 24-72h) inhibited the enhancement of p-STAT6 in Dex LT culture and suppressed the expression of HDAC2. [2]. In NCI-H292 cells, 10µM of 7,4'-Dihydroxyflavone significantly inhibited PMA-induced MUC5AC production [3].
In an ovalbumin-sensitized/challenged mouse model, 7,4'-dihydroxyflavone inhibited MUC5AC secretion in vivo. Treatment with 6µg/mL of 7,4'-dihydroxyflavone for 4 weeks significantly reduced the levels of MUC5AC protein in the bronchoalveolar lavage fluid (BAL) of ovalbumin-sensitized/challenged mice [3].
References:
[1]. Liu C, Yang N, Robalino R P, et al. 7, 4'-Dihydroxyflavone isolated from Glycyrrhiza uralensis a constituent of ASHMITM prevents dexamethasone enhancement of Eotaxin-1 secretion by human lung fibroblasts[J]. Journal of Allergy and Clinical Immunology, 2014, 133(2): AB142.
[2]. Liu ChangDa L C D, Yang Nan Y N, Chen XiaoKe C X K, et al. The flavonoid 7, 4′-dihydroxyflavone prevents dexamethasone paradoxical adverse effect on eotaxin production by human fibroblasts[J]. 2017.
[3]. Liu C, Weir D, Chakrapani S, et al. The Flavonoid 7, 4'-Dihydroxyflavone Inhibits Human Airway Epithelial Cells MUC5AC Mucin Production Via Regulation of NF-êb, STAT6 and HDAC2[J]. Journal
7,4'-Dihydroxyflavone是一种从甘草(Glycyrrhiza uralensis)中分离得到的口服活性黄酮类化合物,可作为嗜酸性粒细胞趋化因子/CCL11和羰基还原酶1(CBR1)的抑制剂[1]。7,4'-Dihydroxyflavone可以持续抑制嗜酸性粒细胞趋化因子的产生,并阻止地塞米松(Dex)对嗜酸性粒细胞趋化因子产生的反弹效应[2]。此外,7,4'-Dihydroxyflavone通过调节NF-κB、STAT6和HDAC2信号通路,抑制MUC5AC基因表达、黏液生成和分泌[3]。
在人肺成纤维细胞-1细胞中,7,4'-Dihydroxyflavone(10μM;24-72h)抑制了地塞米松培养中p-STAT6的升高,并抑制了HDAC2的表达[2]。在NCI-H292细胞中,10μM的7,4'-Dihydroxyflavone显著抑制了PMA诱导的MUC5AC产生[3]。
在卵清蛋白致敏/激发的小鼠模型中,7,4'-二羟基黄酮可抑制体内MUC5AC的分泌。用6µg/mL的7,4'-Dihydroxyflavone治疗4周后,卵清蛋白致敏/激发小鼠支气管肺泡灌洗液(BAL)中MUC5AC蛋白的水平显著降低[]。
| Cell experiment [1]: | |
Cell lines | NCI-H292 cells |
Preparation Method | 100µL of NCI-H292 cells at a concentration of 2x10⁵ cells/mL were added to a 96-well tissue culture plate and allowed to adhere. After 24 hours, the cells were washed three times with 200µL of PBS, and then treated as follows: no treatment, treatment with 10ng/mL PMA alone, or treatment with 10ng/mL PMA plus different concentrations of 7,4'-Dihydroxyflavone in serum-free RPMI medium. |
Reaction Conditions | 10-50μM; 24h |
Applications | 10µM of 7,4'-Dihydroxyflavone significantly inhibited PMA-induced MUC5AC production in H292 cells. |
| Animal experiment [1]: | |
Animal models | OVA sensitization/challenge and 7,4'-Dihydroxyflavone treatment in murine model |
Preparation Method | To establish an allergic asthma model, female BALB/c mice were sensitized by weekly intraperitoneal injection of 200mg OVA and 2mg alum (adsorbed in 0.4mL phosphate-buffered saline) for two weeks. After the last sensitization, five intratracheal (i.t.) challenges were performed on days 14, 21, 28, 45, and 46, each time injecting 100mg OVA dissolved in 0.05mL phosphate-buffered saline. Three mice, starting 24 hours after the first intratracheal challenge, were orally administered 6µg of 7,4'-Dihydroxyflavone dissolved in 1mL of 0.1% DMSO aqueous solution twice daily for one month. |
Dosage form | 6µg/mL; po; bid; 1 month |
Applications | 7,4'-Dihydroxyflavone inhibits MUC5AC secretion in vivo. After treatment with 6µg/mL of 7,4'-Dihydroxyflavone for 4 weeks, the MUC5AC protein levels in the bronchoalveolar lavage fluid (BAL) of OVA-sensitized/challenged mice were significantly reduced. |
References: | |
| Cas No. | 2196-14-7 | SDF | |
| 别名 | 7,4'-二羟基黄酮 | ||
| Canonical SMILES | O=C1C=C(C2=CC=C(O)C=C2)OC3=CC(O)=CC=C13 | ||
| 分子式 | C15H10O4 | 分子量 | 254.24 |
| 溶解度 | DMSO: ≥ 250 mg/mL (983.32 mM) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.9333 mL | 19.6665 mL | 39.3329 mL |
| 5 mM | 786.7 μL | 3.9333 mL | 7.8666 mL |
| 10 mM | 393.3 μL | 1.9666 mL | 3.9333 mL |
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