7,8-dihydroxyflavone (7,8-DHF): An Flavone With Remarkable Health Benefits

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7,8-Dihydroxyflavone (7,8-DHF) is a naturally-occurring flavone found in:

  • Godmania aesculifolia
  • Tridax procumbens
  • Primula tree leaves

Flavones are a class of flavonoids which are a class of plant secondary metabolites.

Natural flavones include:

  • Apigenin (4′,5,7-trihydroxyflavone)
  • Luteolin (3′,4′,5,7-tetrahydroxyflavone)
  • Tangeritin (4′,5,6,7,8-pentamethoxyflavone)
  • Chrysin (5,7-hydroxyflavone)
  • 6-hydroxyflavone
  • Baicalein (5,6,7-trihydroxyflavone)
  • Scutellarein (5,6,7,4′-tetrahydroxyflavone)
  • Wogonin (5,7-dihydroxy-8-methoxyflavone)

Synthetic flavones include:

  • Diosmin
  • Flavoxate
  • 7,8-dihydroxyflavone (7,8-DHF)

7,8-Dihydroxyflavone (7,8-DHF) has been determined and studied to be a potent and selective agonist of the TrkB receptor, which is the main signaling receptor of brain-derived neurotrophic factor (BDNF). It is able to penetrate the blood-brain-barrier after oral consumption.

7,8-DHF has been very therapeutically efficient in various central nervous system disorders including:

  • Depression [1]
  • Alzheimer’s disease [2]
  • Schizophrenia [3]
  • Parkinson’s disease [4]
  • Huntington’s disease [5]
  • Amyotrophic lateral sclerosis [6]
  • Traumatic brain injury [7]
  • Cerebral ischemia [8]

7,8-DHF has also been found to be a potent antioxidant [9] and provides neuroprotection against glutamate-induced excitotoxicity.

The authors of the study concluded that:

Our data demonstrate that 7,8-DHF protects against hydrogen peroxide and menadione-induced cell death, suggesting that 7,8-DHF has an antioxidant effect. In summary, although 7,8-DHF is considered as a selective TrkB agonist, our results demonstrate that 7,8-DHF can still confer neuroprotection against glutamate-induced toxicity in HT-22 cells via its antioxidant activity.” [10]


References:

[1] Liu X, Chan CB, Jang SW, Pradoldej S, Huang J, He K et al. (2010). “A synthetic 7,8-dihydroxyflavone derivative promotes neurogenesis and exhibits potent antidepressant effect”. J. Med. Chem. 53 (23): 8274–86. doi:10.1021/jm101206p. PMC 3150605. PMID 21073191

[2] Castello NA, Nguyen MH, Tran JD, Cheng D, Green KN, LaFerla FM (2014). “7,8-Dihydroxyflavone, a small molecule TrkB agonist, improves spatial memory and increases thin spine density in a mouse model of Alzheimer disease-like neuronal loss”. PLoS ONE 9 (3): e91453. doi:10.1371/journal.pone.0091453. PMC 3948846. PMID 24614170.

Chen C, Li XH, Zhang S, Tu Y, Wang YM, Sun HT (2014). “7,8-dihydroxyflavone ameliorates scopolamine-induced Alzheimer-like pathologic dysfunction”. Rejuvenation Res 17 (3): 249–54. doi:10.1089/rej.2013.1519. PMID 24325271.

Zhang Z, Liu X, Schroeder JP, Chan CB, Song M, Yu SP et al. (2014). “7,8-dihydroxyflavone prevents synaptic loss and memory deficits in a mouse model of Alzheimer’s disease”. Neuropsychopharmacology 39 (3): 638–50. doi:10.1038/npp.2013.243. PMID 24022672.

[3] Yang YJ, Li YK, Wang W, Wan JG, Yu B, Wang MZ et al. (2014). “Small-molecule TrkB agonist 7,8-dihydroxyflavone reverses cognitive and synaptic plasticity deficits in a rat model of schizophrenia”. Pharmacol. Biochem. Behav. 122: 30–6. doi:10.1016/j.pbb.2014.03.013. PMID 24662915.

[4] Jang SW, Liu X, Yepes M, Shepherd KR, Miller GW, Liu Y et al. (2010). “A selective TrkB agonist with potent neurotrophic activities by 7,8-dihydroxyflavone”. Proc. Natl. Acad. Sci. U.S.A. 107 (6): 2687–92. doi:10.1073/pnas.0913572107. PMC 2823863. PMID 20133810.

[5] Jiang M, Peng Q, Liu X, Jin J, Hou Z, Zhang J et al. (2013). “Small-molecule TrkB receptor agonists improve motor function and extend survival in a mouse model of Huntington’s disease”. Hum. Mol. Genet. 22 (12): 2462–70. doi:10.1093/hmg/ddt098. PMC 3658168. PMID 23446639.

[6] Korkmaz OT, Aytan N, Carreras I, Choi JK, Kowall NW, Jenkins BG et al. (2014). “7,8-Dihydroxyflavone improves motor performance and enhances lower motor neuronal survival in a mouse model of amyotrophic lateral sclerosis”. Neurosci. Lett. 566: 286–91. doi:10.1016/j.neulet.2014.02.058. PMID 24637017

[7] Wu CH, Hung TH, Chen CC, Ke CH, Lee CY, Wang PY et al. (2014). “Post-injury treatment with 7,8-dihydroxyflavone, a TrkB receptor agonist, protects against experimental traumatic brain injury via PI3K/Akt signaling”. PLoS ONE 9 (11): e113397. doi:10.1371/journal.pone.0113397. PMC 4240709. PMID 25415296.

[8] Wang B, Wu N, Liang F, Zhang S, Ni W, Cao Y et al. (2014). “7,8-dihydroxyflavone, a small-molecule tropomyosin-related kinase B (TrkB) agonist, attenuates cerebral ischemia and reperfusion injury in rats”. J. Mol. Histol. 45 (2): 129–40. doi:10.1007/s10735-013-9539-y. PMID 24045895.Uluc K, Kendigelen P, Fidan E, Zhang L, Chanana V, Kintner D et al. (2013). “TrkB receptor agonist 7, 8 dihydroxyflavone triggers profound gender- dependent neuroprotection in mice after perinatal hypoxia and ischemia”. CNS Neurol Disord Drug Targets 12 (3): 360–70. PMC 3674109. PMID 23469848.

[9] Flavonoids, Coumarins, and Cinnamic Acids as Antioxidants in a Micellar System. Structure−Activity Relationship†

[10] Antioxidant activity of 7,8-dihydroxyflavone provides neuroprotection against glutamate-induced toxicity.  

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