Isoorientin;Homoorientin CAS No. 4261-42-1
Ulwazi oluBalulekileyo
Igama lesiTshayina: isolysine
Igama lesiNgesi: isoorientin
Igama lesiNgesi: homoorientin;(1S) -1,5-anhydro-1-[2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-4-oxo-4H-chromen-6-yl]-D-glucitol
Inombolo yeCAS: 4261-42-1
Ifomula yemolekyuli: C21H20O11
Ubunzima beMolekyuli: 448.3769
IiPropati zePhysicochemical
Ubunyulu: ngaphezu kwe-99%, indlela yokufumanisa: HPLC.
Ubuninzi: 1.759g/cm3
Indawo yokuBilisa: 856.7 ° C kwi-760 mmHg
Indawo edanyazayo: 303.2 ° C
Uxinzelelo lomphunga: 2.9e-31mmhg ku-25 ° C
Umsebenzi webhayoloji we-Isoorientin
Inkcazo:I-isoorientin yi-COX-2 inhibitor esebenzayo enexabiso le-IC50 le-39 μ M.
Iindidi ezifanelekileyo:
Indawo yophando > umhlaza Iimveliso zeNdalo > > flavonoids
Inkalo yophando > > ukudumba / ukunganyangeki
Ithagethi: cox-2:39 μ M (IC50)
Izifundo ze-in vitro:I-Isoorientin i-inhibitor ekhethiweyo ye-cyclooxygenase-2 (COX-2) evela kwi-tuber yePueraria tuberosa [1].I-PANC-1 kunye neeseli ze-patu-8988 zaphathwa nge-Isoorientin (0,20,40,80 kunye ne-160 μ M) Ukukhula phambi kweeyure ezingama-24 kwaye ungeze isisombululo seCCK8.Kwi-20, 40, 80 kunye ne-160 μ Kwi-concentration ye-M, ukusebenza kweeseli kwehle kakhulu.I-Isoorientin (0,20,40,80 kunye ne-160) yayisetyenziselwa iiseli μ M ye-PANC-1;I-0, i-20, i-40, i-80160 kunye ne-320 μ M yayisetyenziselwa i-patu-8988) inkcubeko yeeyure ze-24, kwaye ukubonakaliswa kwe-P kwavavanywa yi-Western blot - i-AMPK kunye ne-AMPK.Ukubonakaliswa kwe-p-ampk kwanda emva konyango lwe-Isoorientin.Emva koko, kwiqela le-shRNA, i-80 μ M yoxinaniso ukufumana umphumo we-Isoorientin.Amanqanaba okuvakalisa e-AMPK kunye ne-p-ampk kwiqela le-shRNA ayephantsi kakhulu kunalawo akwiiseli zePC zohlobo lwasendle (WT) kunye neqela elosulelwe ngolawulo olubi lwe-lentivirus (NC) [2].
Izifundo ze-vivo:Izilwanyana ezinyangwa nge-Isoorientin nge-10 mg / kg kunye ne-20 mg / kg ubunzima bomzimba ziye zancitshiswa ngokuphawulekayo kwi-claw edema, kunye nobukhulu obuphakathi kwe-1.19 ± 0.05 mm kunye ne-1.08 ± 0.04 mm, ngokulandelanayo.Oku kubonise ukuba i-Isoorientin yanciphisa kakhulu i-paw edema xa kuthelekiswa neqela lokulawula [3].
Umfuniselo weseli:I-PANC-1 kunye neeseli ze-patu-8988 zifakwe kwiiplate ze-96 zequla.Iqula ngalinye liqulethe ~ 5000 iiseli kunye 200 iiseli μ L medium equlathe 10% FBS.Xa iiseli kwiqula ngalinye zifikelele kwi-70% yokudibanisa, i-medium yatshintshwa kwaye i-FBS yamahhala ephakathi kunye neentlobo ezahlukeneyo ze-isoorientin zongezwa.Emva kweeyure ze-24, iiseli zahlanjwa kanye nge-PBS, i-culture medium equkethe i-isoorientin yalahlwa, kwaye i-100% yongezwa μ L FBS i-free medium kunye ne-10 μ L ikiti yokubala i-cell 8 (CCK8) reagent.Iiseli zifakwe kwi-37 ℃ enye i-1-2 iiyure, kwaye ukufunxa kwequla ngalinye kufunyenwe kwi-490 nm usebenzisa umfundi we-ELISA.Ukusebenza kweseli kuchazwa njengotshintsho oluphindaphindiweyo kwi-absorption [2].
Umfuniselo wezilwanyana:kwimeko ye-paw edema imodeli, iigundane [3] zanikwa i-isoorientin okanye i-celecoxib intraperitoneally, kwaye i-carrageenan yafakwa ngokuthe ngqo kwi-paw kwiyure enye kamva.Kwimodeli ye-airbag, lonke unyango lungena kwi-bag cavity ngqo kunye ne-carrageenan.I-isoorientin ifakwe kwiiyure ze-3 ngaphambi kokuba i-carrageenan ifakwe kwi-capsule.I-Isoorientin kunye ne-celecoxib zalawulwa kwiimpuku.Izisombululo zesitokhwe se-isoorientin (100 mg / ml) kunye ne-celecoxib (100 mg / ml) zalungiswa kwi-DMSO kwaye zahlanjululwa ngakumbi ngexesha lonyango.Izilwanyana zahlulwa zibe ngamaqela amahlanu ahlukeneyo alandelayo: ukulawula (i-DMSO iphathwe);I-carrageenan enyangwayo (0.5 ml (1.5% (w / V) carrageenan in brine); I-carrageenan enyangwayo + i-celecoxib (20mg / kg ubunzima bomzimba); I-carrageenan enyangwayo + isoorientin (10 mg / kg ubunzima bomzimba); Nyanga i-carrageenan + isoorientin (20mg / kg ubunzima bomzimba).
Isalathiso:[1].Sumalatha M, et al.I-Isoorientin, i-Selective Inhibitor ye-Cyclooxygenase-2 (COX-2) evela kwiiTubers zePueraria tuberosa.Nat Prod Commun.2015 Okt;10(10):1703-4.
[2].Ewe T, et al.I-Isoorientin yenza i-apoptosis, iyancipha ukuhlasela, kwaye iyancipha ukukhutshwa kwe-VEGF ngokuvula umqondiso we-AMPK kwiiseli zomhlaza we-pancreatic.I-Onco ijolise kuyo.2016 Dec 12; 9: 7481-7492.
[3].UAnilkumar K, et al.Uvavanyo lweePropati ezichasayo ze-Isoorientin Ezahluliweyo kwiiTubers zePueraria tuberosa.Oxid Med Iseli Longev.2017;2017:5498054.