7,8-dihydroxy flavone is also a kind of flavone. Flavonoids are a class of naturally occurring substances which abundantly exist in fruits and vegetables and have a variety of biological effects. Recent studies have shown that the flavonoid derivative---7,8-DHF, as a high-affinity tropomyosin-associated kinase receptor B (TrkB) agonist, induces dimerization and autophosphorylation of receptors and activation of downstream signaling in vivo.
This compound has been shown to have a high level of neuroprotection against a variety of diseases, such as Alzheimer's disease, Parkinson's disease, Rett syndrome and Huntington's disease. It can easily penetrate the blood-brain barrier and can be taken orally. We have known that 7,8-DHF plays a role in protecting retinal ganglion cells from excitatory toxicity and oxidative stress-mediated degeneration. TrkB is a receptor tyrosine kinase that is well expressed in the retina and important for the development of retinal networks. 7,8-DHF activates TrkB receptors several times and induces a cascade of downstream pro-survival signals, such as activation of Akt and MAPK/Erk pathways. Although several studies have suggested that the neuroprotective effects of 7,8-DHF are mediated by TrkB receptors, a thorough understanding of the molecular basis of 7,8-DHF function is not known. 7,8-DHF is known to bind to cysteine cluster 2 (CC2) and the TrkB extracellular domain of the leucine-rich region (LRR).
The VEGF receptor belongs to the family of tyrosine kinase receptors, which also plays a key role in the retina. In addition to participate in the formation of new blood vessels associated with a variety of hyperplastic disease, abnormal expression of VEGF is involved in a variety of eye diseases, such as the macular edema associated with diabetic retinopathy, age-related macular degeneration (AMD) related choroid neovascularization formed, neovascular glaucoma and fibrosis complications such as glaucoma filtration surgery. VEGFR2 is well expressed in the retina and is believed to primarily modulate the cellular role of VEGF. Flavonoids have been reported to play a role in inhibition of VEGFR2, thereby inhibiting angiogenesis and proliferation of vascular endothelial cells. Therefore, VEGFR2 is an important target for studying the biological effects of 7,8-DHF and other similar flavonoids.
Interaction and binding mode of 7,8-dihydroxyflavone (7,8-DHF) with TrkB and VEGFR2.
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