7,8-Dihydroxyflavone (Synonyms: 7,8-DHF) |
| カタログ番号GC16853 |
7,8-ジヒドロキシフラボンは、脳由来神経栄養因子 (BDNF) の生理学的作用を模倣する、強力かつ選択的な TrkB アゴニストです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 38183-03-8
Sample solution is provided at 25 µL, 10mM.
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7,8-Dihydroxyflavone is a naturally-occurring plant-based flavone and high-affinity tyrosine kinase receptor B (TrkB) agonist with an IC50 value of 0.26μM[1,2]. TrkB is a protein tyrosine kinase receptor, and its primary ligand Brain-derived neurotrophic factor (BDNF) is expressed in neurons and skeletal muscles during the differentiation period and in the adult, promoting neuronal survival and differentiation, synaptic plasticity, and development of myoblasts and muscle fibers, as well as regulating energy metabolism and regeneration of the muscles[3]. 7,8-Dihydroxyflavone can be used as an adjunctive treatment in schizophrenia[4].
In vitro, treatment of MC3T3-E1 cells with 7,8-Dihydroxyflavone (0.5-5μM) for 24-48h resulted in a significant increase in cyclin mRNA levels in the cells, promoting cell proliferation and differentiation[5]. After 48h treatment with 7,8-Dihydroxyflavone (10-300μM) in cardiac fibroblasts (CFs) stimulated by TGF-β1, 7,8-Dihydroxyflavone significantly reduced the viability of CFs and inhibited TGF-β1-induced CFs activity in a dose-dependent manner[6].
In vivo, administration of 7,8-Dihydroxyflavone (5mg/kg/day) via intraperitoneal injection for 28days in mice fed a high-energy diet (cafeteria diet, CAF). 7,8-Dihydroxyflavone reduced body weight and downregulated the percentage indices of epididymal adipose tissue and adipocytes. The treatment also significantly decreased triglyceride, cholesterol, amylase, alanine aminotransferase (ALT), and glucose levels[7]. In 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced Parkinson's disease mice, 5-day intraperitoneal treatment with 7,8-Dihydroxyflavone (5mg/kg/day) effectively blocked the loss of tyrosine hydroxylase (TH)-positive neurons, exerted beneficial effects on motor function and neuropathology through autophagy mechanisms[8].
References:
[1] Paul R, Nath J, Paul S, et al. Suggesting 7,8-dihydroxyflavone as a promising nutraceutical against CNS disorders[J]. Neurochem Int, 2021, 148: 105068.
[2] Tasdemir D, Kaiser M, Brun R, et al. Antitrypanosomal and antileishmanial activities of flavonoids and their analogues: in vitro, in vivo, structure-activity relationship, and quantitative structure-activity relationship studies[J]. Antimicrob Agents Chemother, 2006, 50(4): 1352-64.
[3] Deng C, Chen H. Brain-derived neurotrophic factor/tropomyosin receptor kinase B signaling in spinal muscular atrophy and amyotrophic lateral sclerosis[J]. Neurobiol Dis, 2024, 190: 106377.
[4] Du X, Hill R A. 7,8-Dihydroxyflavone as a pro-neurotrophic treatment for neurodevelopmental disorders[J]. Neurochem Int, 2015, 89: 170-80.
[5] Xue F, Zhao Z, Gu Y, et al. 7,8-Dihydroxyflavone modulates bone formation and resorption and ameliorates ovariectomy-induced osteoporosis[J]. Elife, 2021, 10.
[6] Hang P Z, Liu J, Wang J P, et al. 7,8-Dihydroxyflavone alleviates cardiac fibrosis by restoring circadian signals via downregulating Bmal1/Akt pathway[J]. Eur J Pharmacol, 2023, 938: 175420.
[7] Sahin E, Saglam N, Erdem S, et al. 7,8-Dihydroxyflavone alleviates Endoplasmic Reticulum Stress in cafeteria diet-induced metabolic syndrome[J]. Life Sci, 2022, 306: 120781.
[8] Zuo L, Dai C, Yi L, et al. 7,8-dihydroxyflavone ameliorates motor deficits via regulating autophagy in MPTP-induced mouse model of Parkinson's disease[J]. Cell Death Discov, 2021, 7(1): 254.
| Cell experiment [1]: | |
Cell lines | Cardiac fibroblasts (CFs) |
Preparation Method | The cytotoxicity of 7,8-Dihydroxyflavone was evaluated by treating CFs with different concentrations of 7,8-Dihydroxyflavone (10, 30, 100, and 300μM) for 48h. The CFs were incubated with TGF-β1 (20ng/mL) for 48h with or without 7,8-Dihydroxyflavone. CFs were seeded on a 96-well plate and treated as designated, followed by the addition of CCK-8 reagent and incubated at 37◦C for 2h. Optical density was detected using a microplate reader at 450nm. |
Reaction Conditions | 10, 30, 100, and 300μM; 48h |
Applications | 7,8-Dihydroxyflavone significantly decreased the viability of CF and inhibited the viability of TGF-β1-induced CFs in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | C57BL/6 male mice |
Preparation Method | 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) groups were administrated with MPTP (30mg/kg, i.p.) once a day for 5days. 7,8-Dihydroxyflavone (5mg/kg, i.p.) and chloroquine (50mg/kg, i.p.) were injected once a day during the whole process of experiments. The control groups received the same volume of sterile saline with or without 10% ethanol. |
Dosage form | 5mg/kg/day for 5days; Intraperitoneal injection |
Applications | 7,8-Dihydroxyflavone alleviates motor deficits and reduces the loss of dopaminergic neurons in MPTP-induced mouse model of Parkinson's disease. |
References: | |
| Cas No. | 38183-03-8 | SDF | |
| 同義語 | 7,8-DHF | ||
| Chemical Name | 7,8-dihydroxy-2-phenyl-4H-chromen-4-one | ||
| Canonical SMILES | OC1=C(C2=CC=C1O)OC(C3=CC=CC=C3)=CC2=O | ||
| Formula | C15H10O4 | M.Wt | 254.24 |
| 溶解度 | ≥ 12.75mg/mL in DMSO | Storage | Store at 4°C, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.9333 mL | 19.6665 mL | 39.3329 mL |
| 5 mM | 0.7867 mL | 3.9333 mL | 7.8666 mL |
| 10 mM | 0.3933 mL | 1.9666 mL | 3.9333 mL |
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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