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7,8-Dihydroxyflavone bubuk

7,8-Dihydroxyflavone, uga dikenal minangka tropoflavin, minangka flavon alami sing ditemokake ing Godmania aesculifolia, Tridax procumbens, lan godhong wit primula.[2][3][4] Wis ditemokake minangka agonis molekul cilik sing kuat lan selektif saka reseptor tropomiosin kinase B (TrkB) (Kd ≈ 320 nM), reseptor sinyal utama saka faktor neurotropik sing asale saka otak neurotrophin (BDNF). Tropoflavin minangka bioavailable sacara lisan lan bisa nembus sawar getih-otak. Prodrug tropoflavin kanthi potensi lan farmakokinetik sing apik banget, R13 (lan, sadurunge, R7), lagi dikembangake kanggo perawatan penyakit Alzheimer.

Wisepowder nduweni kemampuan kanggo ngasilake lan nyedhiyakake jumlah gedhe. Kabeh produksi ing kondisi cGMP lan sistem kontrol kualitas sing ketat, kabeh dokumen testing lan sampel kasedhiya.

7,8-Dihydroxyflavone bubuk Informasi Dasar Kimia

jeneng 7,8-DIHYDROXYFLAVONE
CAS 38183-03-8
Kemurnian 98%
Jeneng kimia 7,8-Dihydroxy-2-phenyl-4H-1-benzopyran-4-one
Liyane 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
Formula molekul C15H10O4
Bobot molekul 254.24
Boling Point 494.4 ° C ing 760 mmHg
InChI Key COCYGNDCWFKTMF-UHFFFAOYSA-N
Formulir Ngalangi
katon Kuning bubuk
Separuh Urip /
kelarutan DMSO: ≥ 100 mg/mL (393.33 mM)

Larut ing DMSO, etanol, lan metanol.

kawontenan Storage kamar ruangan
aplikasi 7,8-Dihydroxyflavone minangka agonis TrkB sing nyegah apoptosis sing dipicu glutamat
Dokumen Tes kasedhiya

 

7,8-Dihydroxyflavone bubuk Katrangan Umum

7,8-Dihydroxyflavone (7,8-DHF) minangka flavon monofenolik kanthi efek sing maneka warna. Tumindak minangka agonis saka neurotrophic tyrosine kinase reseptor TrkB (Kd = 320 nM), nglindhungi neuron sing nyebut TrkB saka apoptosis.1 7,8-DHF minangka neuroprotective ing model kewan saka penyakit Parkinson.1 Ndhukung sinau emosional ing tikus. lan mbalikke defisit memori ing model tikus penyakit Alzheimer.2,3 Uga nambah fungsi motor lan ngluwihi kaslametan ing model kewan penyakit Huntington.4 7,8-DHF nyegah aromatase cytochrome P450 (IC50 = 10 µM) lan, kanthi cara iki, ngowahi metabolisme estrogen.5 Uga nduweni aksi antioksidan sing ningkatake sintesis glutathione intraselular lan scavenges spesies oksigen reaktif.

 

7,8-Dihydroxyflavone bubuk Sajarah

Ing 2017, bukti diterbitake nuduhake yen tropoflavin lan macem-macem agonis TrkB molekul cilik liyane sing dilaporake bisa uga ora dadi agonis langsung saka TrkB lan bisa uga mediasi efek sing diamati kanthi cara liya.

 

7,8-Dihydroxyflavone bubuk Mechanisme Of Action

7,8-Dihydroxyflavone minangka agonis reseptor tirosin kinase selektif B (TrkB). Iki nuduhake kabeh efek terapeutik saka faktor neurotropik sing asale saka otak (BDNF) - kayata nglindhungi neuron saka apoptosis, nyegah keracunan sing disebabake dening asam kainic, nyuda volume infark ing stroke, lan neuroprotecting ing model kewan penyakit Parkinson-tanpa profil farmakokinetik miskin BDNF mbatesi potensial terapeutik.

7,8-Dihydroxyflavone (7,8-DHF) bisa digunakake kanggo mbantu ngenali lan mbedakake efek fisiologis lan jalur sinyal sel sing ditengahi dening aktivasi TrkB, kayata sing nglibatake, memori, vasorelaxation lan hipertensi. 7,8-DHF entuk proteksi ing disfungsi patologis kaya Alzheimer sing disebabake scopolamine.

 

7,8-Dihydroxyflavone bubuk Aplikasi

7,8-Dihydroxyflavone hydrate wis digunakake minangka agonis tropomiosin-reseptor-kinase B (TrkB) ing tikus lan kanggo nyegah TrkB kanggo ngawasi arus postsynaptic excitatory (eEPSCs).

 

7,8-Dihydroxyflavone bubuk Riset liyane

Ana macem-macem analog struktural cedhak tropoflavin uga ditemokake kanggo tumindak minangka agonis TrkB ing vitro, kalebu 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, lan 3,7-dihydroxyflavone.[37] Gossypetin analog sing hidroksilasi banget (3,5,7,8,3′,4′-hexahydroxyflavone), kosok balene, katon minangka antagonis TrkB in vitro.

Tropoflavin uga ditemokake kanggo ngurangi turu tikus ing fase peteng lan ngurangi tingkat hipotalamus saka orexin A nanging ora orexin B ing tikus.

 

reference

  1. Andero et al (2012) 7,8-dihydroxyflavone, agonis reseptor TrkB, ngalangi gangguan memori spasial jangka panjang sing disebabake dening stres immobilisasi ing tikus. Hippocampus 22 399
  2. Jang et al (2010) A agonis TrkB selektif kanthi aktivitas neurotropik kuat dening 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). "Assays kuantitatif Multiplex nuduhake perlu kanggo reevaluating kacarita agonis TrkB molekul cilik". Sinyal Sci.
  4. Jiang Agonis reseptor TrkB molekul cilik nambah fungsi motor lan ngluwihi kaslametan ing model tikus penyakit Huntington. Hum.Mol.Genet. 2013