Imikhiqizo

Incazelo:I-isoorientin iyi-COX-2 inhibitor esebenzayo enenani le-IC50 lama-39 μ M.

Izigaba ezifanele:
Inkundla yocwaningo > > umdlavuza Imikhiqizo yemvelo > > flavonoids
Inkambu yocwaningo > > ukuvuvukala / ukungatheleleki
Ithagethi: cox-2:39 μ M (IC50)

Izifundo ze-in vitro:I-Isoorientin iyi-inhibitor ekhethiwe ye-cyclooxygenase-2 (COX-2) evela ku-tuber ye-Pueraria tuberosa [1].Amaseli e-PANC-1 kanye ne-patu-8988 aphathwe nge-Isoorientin (0,20,40,80 kanye ne-160 μ M) Khula phambi kwamahora angu-24 bese wengeza isisombululo se-CCK8.Ku-20, 40, 80 kanye ne-160 μ Ekugxilweni kwe-M, ukusebenza kweseli kwehle kakhulu.I-Isoorientin (0,20,40,80 kanye ne-160) yayisetshenziselwa amaseli μ M we-PANC-1;I-0, 20, 40, 80160 kanye ne-320 μ M yasetshenziselwa isiko le-patu-8988) amahora angu-24, futhi inkulumo ye-P yahlolwa yi-Western blot - i-AMPK ne-AMPK.Ukubonakaliswa kwe-p-ampk kukhuphuke ngemuva kokwelashwa kwe-Isoorientin.Bese, eqenjini le-shRNA, 80 μ M ukugxila ukuthola umphumela we-Isoorientin.Amazinga enkulumo we-AMPK kanye ne-p-ampk eqenjini le-shRNA ayephansi kakhulu kunalawo aku-wild-type PC cell (WT) kanye neqembu elidluliselwa nge-negative control lentivirus (NC) [2].

Izifundo ze-in vivo:Izilwane eziphathwe nge-Isoorientin ngo-10 mg/kg kanye nesisindo somzimba esingu-20 mg/kg zibe nokuncipha okuphawulekayo kwezibalo ze-claw edema, nobukhulu obukhulu obungu-1.19 ± 0.05 mm no-1.08 ± 0.04 mm, ngokulandelana.Lokhu kubonise ukuthi i-Isoorientin yehlisa kakhulu i-paw edema uma iqhathaniswa neqembu lokulawula [3].

Ukuhlolwa kweseli:Amaseli e-PANC-1 kanye ne-patu-8988 ajovwe kumapuleti emithombo engama-96.Umthombo ngamunye unamaseli angu-~ 5000 namaseli angu-200 μ L medium equkethe u-10% we-FBS.Lapho amaseli emthonjeni ngamunye efinyelela ku-70% ukuhlangana, okuphakathi kwashintshwa futhi i-FBS yamahhala enokugxila okuhlukile kwe-isoorientin yengezwa.Ngemva kwamahora angu-24, amaseli ahlanjululwa kanye nge-PBS, isiko lesiko eliqukethe i-isoorientin lalahlwa, futhi i-100% yengezwa μ L FBS i-free medium kanye ne-10 μ L cell counting kit 8 (CCK8) reagent.Amaseli afakwe ku-37 ℃ amanye amahora angu-1-2, futhi ukumuncwa komthombo ngamunye kutholwe ku-490 nm kusetshenziswa isifundi se-ELISA.Ukusebenza kweseli kuvezwa njengoshintsho oluningi ekumunceni [2].

Ukuhlolwa kwezilwane:endabeni yemodeli ye-paw edema, amagundane [3] anikezwa i-isoorientin noma i-celecoxib intraperitoneally, futhi i-carrageenan yajovwa ngokuqondile esidladleni ihora elilodwa kamuva.Kumodeli ye-airbag, zonke izindlela zokwelapha zingena emgodini wesikhwama ngokuqondile ne-carrageenan.I-isoorientin yajovwa emahoreni ama-3 ngaphambi kokuthi i-carrageenan ijovwe ku-capsule.I-Isoorientin ne-celecoxib zinikezwe amagundane.Izixazululo zesitoko ze-isoorientin (100 mg / ml) ne-celecoxib (100 mg / ml) zalungiswa nge-DMSO futhi zaphinde zahlanjululwa ngesikhathi sokwelashwa.Izilwane zahlukaniswa ngamaqembu amahlanu ahlukene alandelayo: ukulawula (i-DMSO iphathwa);I-carrageenan elashiwe (0.5 ml (1.5% (w / V) carrageenan ku-brine); I-carrageenan + celecoxib (20mg / kg isisindo somzimba); I-carrageenan + isoorientin elashiwe (10 mg / kg isisindo somzimba); Yelapha i-carrageenan + isoorientin (20mg / kg isisindo somzimba).

Ireferensi:[1].Sumalatha M, et al.I-Isoorientin, i-Selective Inhibitor ye-Cyclooxygenase-2 (COX-2) evela ku-Tubers of Pueraria tuberosa.I-Nat Prod Commun.2015 Okthoba;10(10):1703-4.
[2].Ye T, et al.I-Isoorientin yenza i-apoptosis, yehlise ukuhlasela, futhi yehlise ukugcinwa kwe-VEGF ngokwenza kusebenze ukusayina kwe-AMPK kumaseli omdlavuza we-pancreatic.I-Onco Ithagethi Ther.2016 Dec 12;9:7481-7492.
[3].U-Anilkumar K, et al.Ukuhlolwa Kwezakhiwo Eziphikisana Nokuvuvukala ze-Isoorientin Ehlukanisiwe Kuma-Tubers of Pueraria tuberosa.I-Oxid Med Cell Longev.2017;2017:5498054.