cov khoom siv

7,8-Dihydroxyflavone hmoov

7,8-Dihydroxyflavone, tseem hu ua tropoflavin, yog ib qho tshwm sim flavone nyob rau hauv Godmania aesculifolia, Tridax procumbens, thiab primula ntoo nplooj.[2][3][4] Nws tau raug pom los ua lub zog thiab xaiv me me-molecule agonist ntawm tropomyosin receptor kinase B (TrkB) (Kd ≈ 320 nM), lub ntsiab lus tseem ceeb ntawm cov neurotrophin hlwb-derived neurotrophic factor (BDNF). Tropoflavin yog ob qho tib si ntawm qhov ncauj bioavailable thiab muaj peev xwm nkag mus rau cov ntshav-hlwb barrier. Ib tug prodrug ntawm tropoflavin nrog zoo heev txhim kho potency thiab pharmacokinetics, R13 (thiab, yav tas los, R7), tab tom txhim kho rau kev kho mob ntawm Alzheimer's kab mob.

Wisepowder muaj peev xwm tsim tau thiab muab khoom ntau. Txhua qhov kev tsim khoom raws li cGMP thiab kev tswj hwm nruj, tag nrho cov ntaub ntawv xeem thiab cov qauv muaj.

7,8-Dihydroxyflavone hmoov Cov ntaub ntawv tshuaj lom neeg

lub npe 7,8-DIHYDROXYFLAVONE
CAS 38183-03-8
purity 98%
Tshuaj lub npe 7,8-Dihydroxy-2-phenyl-4H-1-benzopyran-4-one
Synonyms 7,8-DHF; 7,8-DIHYDROXYFLAVONE;7,8-dihydroxy-2-phenyl-4-benzopyrone; DIHYDROXYFLAVONE, 7,8-(RG); 7,8-Dihydroxyflavone hydrate; 7,8-dihydroxy-2-phenyl-1-benzopyran-4-one; 8-Dihydroxyflavone; 7,8-DIHYDROXYFLAVONE 7,8-DIHYDROXYFLAVONE; 7,8-dihydroxy-2-phenyl-4h-1-benzopyran-4-on
molecular Formula C15H10O4
molecular Nyhav 254.24
Boling Point 494.4 ° C ntawm 760 mmHg
InChI Qhov Tseem Ceeb COCYGNDDCWFKTMF-UHFFFAOYSA-N
daim ntawv khoom
tsos Cov hmoov daj
Ib Sim Neej /
solubility DMSO: ≥ 100 mg / mL (393.33 mM)

Soluble hauv DMSO, ethanol, thiab methanol.

cia mob chav sov
Daim ntawv thov 7,8-Dihydroxyflavone yog TrkB agonist uas inhibits glutamate-triggered apoptosis
Kuaj Cov Ntaub Ntawv Qhov

 

7,8-Dihydroxyflavone hmoov General Description

7,8-Dihydroxyflavone (7,8-DHF) yog monophenolic flavone nrog ntau yam teebmeem. Nws ua raws li agonist ntawm neurotrophic tyrosine kinase receptor TrkB (Kd = 320 nM), tiv thaiv neurons uas qhia TrkB los ntawm apoptosis.1 7,8-DHF yog neuroprotective nyob rau hauv tus tsiaj qauv ntawm Parkinson tus kab mob.1 Nws txhawb kev kawm kev xav hauv nas. thiab thim rov qab nco tsis txaus hauv tus qauv nas ntawm Alzheimer's disease.2,3 Nws kuj tseem txhim kho lub cev muaj zog thiab ua kom muaj sia nyob hauv tus qauv tsiaj ntawm Huntington tus kab mob.4 7,8-DHF inhibits cytochrome P450 aromatase (IC50 = 10 µM) thiab, nyob rau hauv no txoj kev, alters estrogen metabolism.5 Nws kuj muaj antioxidant kev ua uas ua rau kom intracellular glutathione synthesis thiab scavenges reactive oxygen hom.

 

7,8-Dihydroxyflavone hmoov Keeb kwm

Hauv xyoo 2017, cov ntaub ntawv pov thawj tau tshaj tawm qhia tias tropoflavin thiab lwm yam tshaj tawm me me-molecule TrkB agonists tej zaum yuav tsis yog cov agonists ncaj qha ntawm TrkB thiab tej zaum yuav kho tau lawv cov kev pom los ntawm lwm txoj kev.

 

7,8-Dihydroxyflavone hmoov Mechanism Of Action

7,8-Dihydroxyflavone yog ib qho kev xaiv tyrosine kinase receptor B (TrkB) receptor agonist. Nws tshwm sim tag nrho cov kev kho mob ntawm lub paj hlwb-derived neurotrophic yam (BDNF) - xws li tiv thaiv neurons los ntawm apoptosis, inhibiting kainic acid-induced toxicity, txo infarct volumes nyob rau hauv mob stroke, thiab neuroprotecting nyob rau hauv ib tug tsiaj qauv ntawm Parkinson tus kab mob - tsis muaj lub tsis zoo pharmacokinetic profile ntawm BDNF txwv nws cov peev xwm kho mob.

7,8-Dihydroxyflavone (7,8-DHF) tuaj yeem siv los pab txheeb xyuas thiab sib txawv ntawm cov teebmeem ntawm lub cev thiab cov xovtooj ntawm tes taw qhia txoj hauv kev sib kho los ntawm kev ua kom TrkB, xws li cov koom nrog, nco, vasorelaxation thiab kub siab. 7,8-DHF elicits tiv thaiv nyob rau hauv scopolamine induced Alzheimer-zoo li pathologic dysfunction.

 

7,8-Dihydroxyflavone hmoov Daim ntawv thov

7,8-Dihydroxyflavone hydrate tau siv los ua tropomyosin-receptor-kinase B (TrkB) agonist hauv cov nas thiab inhibit TrkB rau kev soj ntsuam evoked excitatory postsynaptic tam sim no (eEPSCs).

 

7,8-Dihydroxyflavone hmoov Kev tshawb fawb ntxiv

Ntau yam ntawm cov qauv zoo sib xws ntawm tropoflavin kuj tau pom los ua TrkB agonists hauv vitro, suav nrog diosmetin (5,7,3′-trihydroxy-4′-methoxyflavone), norwogonin (5,7,8-trihydroxyflavone), eutropoflavin (4'-dimethylamino-7,8-dihydroxyflavone), 7,8,3'-trihydroxyflavone, 7,3'-dihydroxyflavone, 7,8,2'-trihydroxyflavone, 3,7,8,2'-tetrahydroxyflavone, thiab 3,7-dihydroxyflavone [37] Cov hydroxylated analogue gossypetin ntau heev (3,5,7,8,3',4'-hexahydroxyflavone), hloov pauv, zoo li yog tus antagonist ntawm TrkB hauv vitro.

Tropoflavin kuj tseem pom tias txo cov nas pw tsaug zog hauv qhov tsaus ntuj thiab txo qis hypothalamus qib ntawm orexin A tab sis tsis yog orexin B hauv cov nas.

 

reference

  1. Andero et al (2012) 7,8-dihydroxyflavone, ib tug TrkB receptor agonist, thaiv lub sij hawm ntev spatial nco impairment los ntawm immobilzation kev nyuaj siab nyob rau hauv nas. Hippocampus 22 399
  2. Jang et al (2010) Ib qho kev xaiv TrkB agonist nrog cov haujlwm muaj zog neurotrophic los ntawm 7,8-dihydroxyflavone. Proc.Natl.Acad.Sci.USA 107 268
  3. Boltaev U, Meyer Y, Tolibzoda F, Jacques T, Gassaway M, Xu Q, Wagner F, Zhang YL, Palmer M, Holson E, Sames D (2017). "Multiplex quantitative assays qhia qhov xav tau rau kev rov ntsuam xyuas qhia me me-molecule TrkB agonists". Sci Signal.
  4. Jiang Me-molecule TrkB receptor agonists txhim kho lub cev muaj zog thiab ua kom muaj sia nyob hauv tus qauv nas ntawm Huntington tus kab mob. Hum.Mol.Genet. 2013