Prim-O-glucosylcimifugin
Aplikasi saka Prim-O-glucosylcimifugin
Prim-o-glucosylcimifugin duweni efek anti-inflamasi sing kuat.Ekspresi iNOS lan COX-2 bisa dicegah kanthi ngatur transduksi sinyal JAK2 / STAT3.
Jeneng Prim-O-glucosylcimifugin
jeneng Cina:Cimicifugin glikosida
Jeneng Inggris:(2S)-2-(2-hydroxypropan-2-yl)-4-methoxy-7-[[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan -2-yl]oxymethyl]-2,3-dihydrofuro[3,2-g]chromen-5-siji
CinaAlias:Cimicifugin
Bioaktivitas Prim-O-glucosylcimifugin
katrangan:
prim-o-glucosylcimifugin nduweni efek anti-inflamasi sing kuat.Ekspresi iNOS lan COX-2 bisa dicegah kanthi ngatur transd sinyal JAK2 / STAT3
Kategori sing relevan:
Jalur sinyal > > kekebalan lan inflamasi > > nitric oxide synthase
Bidang riset > > inflamasi/kekebalan
Produk Alami > > liyane
Target:iNOS
COX-2
Sinau In Vitro:
prim-o-glucosylglycine (POG) minangka isi paling dhuwur saka kromo lan salah siji komponen aktif utama ing Fangfeng (RS).Prim-o-glucosylglycine nduweni peran anti-inflamasi ing makrofag 264.7 mentah kanthi nyegah transduksi sinyal JAK2 / STAT3 lan nyegah ekspresi iNOS lan COX-2.Sitotoksisitas prim-o-glukosida ing LPS aktif 264.7 makrofag mentah diukur.Gunakake LPS (1 μ G / ml) lan nambah konsentrasi prim-o-glucosylglycine (15, 50 lan 100 μ G / ml) sajrone 24 jam, lan viabilitas sel dievaluasi kanthi uji CCK-8.Dibandhingake karo sel sing diobati DMSO (kontrol), 24 jam lan paparan 15-100 μ Sawise g / ml prim-o-glucoside, viabilitas sel ora kena pengaruh.Kanggo nyinaoni efek anti-inflamasi saka prim-o-glucosylglycine, apa prim-o-glucosylglycine bisa mengaruhi sintesis NO diteliti ing sel mentah 264.7 sing diaktifake LPS.Gunakake LPS (1 μ G / ml) lan macem-macem konsentrasi prim-o-glucosylglycine (15, 50 lan 100 μ G / ml) sajrone 24 jam.Konsentrasi kasebut ora diukur ing supernatan kultur kanthi reaksi Griess.Konsentrasi ora ana ing supernatan kultur mundhak sacara signifikan kanthi paparan LPS, lan prim-o-glukosida sacara signifikan nyandhet LPS ora nyebabake produksi kanthi cara sing gumantung konsentrasi [1].
Ing Vivo Study
Cairan lavage bronchoalveolar (BALF) diklumpukake 7 jam sawise administrasi lipopolysaccharide (LPS), lan tingkat sitokin ing BALF diukur kanthi ELISA.Dibandhingake karo klompok kontrol, TNF ing BALF- α , IL-1 β Lan IL-6 tingkat tambah akeh.Nanging, pretreatment karo prime-o-glucosylglycine (2,5, 5 utawa 10 mg / kg) sacara signifikan nyuda TNF-α, IL-1 β lan IL-6 kanthi cara gumantung dosis (P <0,05, P <0,05, 0,01). ) [1].
Eksperimen Sel
Cell counting Kit (CCK-8) digunakake kanggo nemtokake konsentrasi sitotoksik prim-o-glukosilglisin.Singkatnya, 264,7 sel mentah dirawat kanthi 1 saben sumur × Kapadhetan 104 sel diinokulasi ing 96 sumur lan diinkubasi sewengi.Banjur nggunakake 1 μ Sel dirangsang karo g / ml LPS lan diobati karo macem-macem konsentrasi prim-o-glucosylglycine (15, 50 lan 100 μg / mL; Medchem express, Princeton, NJ, USA) utawa perawatan DMSO.Sawise inkubasi ing 37 ℃ suwene 24 jam, solusi CCK-8 ditambahake ing saben sumur lan diinkubasi sajrone jam liyane.Penyerapan diukur ing 450 nm nggunakake pembaca microplate [1].
Eksperimen kewan
tikus [1] BALB/C tikus jantan, umur 8 minggu, boboté watara 18 nganti 20g.Tikus dipérang dadi 5 klompok kanthi acak: kelompok kontrol;klompok LPS;LPS + prime-o-glucosylglycine (2,5, 5 utawa 10mg / kg bobot awak).Prime-o-glucosylglycine diterbitake intraperitoneal.Sawise 1 jam, tikus ing grup LPS lan grup LPS + prime-o-glucosylglycine diwenehi 50 mg / L intranasal (in) (200 mg / L) μ LLPs kanggo nyebabake cedera paru-paru akut.Tikus kontrol diwenehi 50% intranasal (in) tanpa LPS μ LPBS
[1]
Referensi:
[1].Zhou J, et al.Prim-O-glucosylcimifugin Attenuates Lipopolysaccharideinduced Inflammatory Response in RAW 264.7 Makrofag.Pharmacogn Mag.2017 Jul-Sep;13(51):378-384.
[2].Chen N, et al.Prime-O-glucosylcimifugin attenuates ciloko paru-paru akut sing disebabake lipopolysaccharide ing tikus.Int Immunopharmacol.2013 Jun;16(2):139-47.
Sifat Fisikokimia Prim-O-glucosylcimifugin
Kapadhetan: 1,5 ± 0,1 g / cm3
Titik didih: 736,9 ± 60,0 ° C ing 760 mmHg
Formula Molekul: C22H28O11
Bobot molekul: 468,451
Titik nyala: 255,0 ± 26,4 ° C
Massa pas: 468.163147
PSA: 168.28000
LogP:-1.35
Tekanan Uap: 0,0 ± 2,5 mmHg ing 25 ° C
Indeks bias: 1.648
Prim-O-glucosylcimifugin informasi safety
Pranyatan Keamanan (Eropa): 24 / 25
Kode Pabean: 29389090
Alias Inggris saka Prim-O-glucosylcimifugin
5H-Furo[3,2-g][1]benzopyran-5-one,7-[(β-D-glucopyranosyloxy)metil]-2,3-dihydro-2-(1-hydroxy-1-methylethyl)- 4-methoxy-, (2S)-
HMS2196A10
[(2S)-2-(2-Hydroxypropan-2-yl)-4-metoxy-5-oxo-2,3-dihydro-5H-furo[3,2-g]chromen-7-yl]metil β- D-glucopyranoside
N1606
[(2S)-2-(2-Hydroxy-2-propanyl)-4-methoxy-5-oxo-2,3-dihydro-5H-furo[3,2-g]chromen-7-yl]metil β- D-glucopyranoside
Prim-O-glucosylcimifugin