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Kufotokozera:isoorientin ndi COX-2 inhibitor yogwira mtima yokhala ndi mtengo wa IC50 wa 39 μ M.

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Cholinga: cox-2:39 μ M (IC50)

Maphunziro a in vitro:Isoorientin ndi inhibitor yosankha ya cyclooxygenase-2 (COX-2) kuchokera ku tuber ya Pueraria tuberosa [1].Maselo a PANC-1 ndi patu-8988 amathandizidwa ndi Isoorientin (0,20,40,80 ndi 160 μ M) Kukula pamaso pa maola 24 ndikuwonjezera yankho la CCK8.Pa 20, 40, 80 ndi 160 μ Pa ndende ya M, mphamvu ya maselo inachepa kwambiri.Isoorientin (0,20,40,80 ndi 160) inagwiritsidwa ntchito kwa maselo μ M kwa PANC-1;0, 20, 40, 80160 ndi 320 μ M idagwiritsidwa ntchito pa patu-8988) chikhalidwe kwa maola 24, ndipo mawu a P adayesedwa ndi Western blot - AMPK ndi AMPK.Mawu a p-ampk adawonjezeka pambuyo pa chithandizo cha Isoorientin.Kenako, mu gulu la shRNA, 80 μ M ndende kuti azindikire zotsatira za Isoorientin.Masewu a AMPK ndi p-ampk mu gulu la shRNA anali otsika kwambiri kuposa omwe ali m'maselo akutchire a PC (WT) ndipo gululo linapatsirana ndi lentivirus yoyipa (NC) [2].

Maphunziro mu vivo:Nyama zothandizidwa ndi Isoorientin pa 10 mg / kg ndi 20 mg / kg kulemera kwa thupi zinali ndi kuchepa kwakukulu kwa edema ya claw, ndi makulidwe apamwamba a 1.19 ± 0.05 mm ndi 1.08 ± 0.04 mm, motsatana.Izi zinasonyeza kuti Isoorientin inachepetsa kwambiri paw edema poyerekeza ndi gulu lolamulira [3].

Kuyesera kwa ma cell:Ma cell a PANC-1 ndi patu-8988 adayikidwa pa mbale 96 zachitsime.Chitsime chilichonse chimakhala ndi ~ maselo 5000 ndi ma cell 200 μ L sing'anga yokhala ndi 10% FBS.Maselo a chitsime chilichonse akafika pa 70% confluence, sing'angayo idasinthidwa ndipo sing'anga yaulere ya FBS yokhala ndi mitundu yosiyanasiyana ya isoorientin idawonjezedwa.Pambuyo pa maola a 24, maselowo adatsukidwa kamodzi ndi PBS, chikhalidwe cha chikhalidwe chomwe chili ndi isoorientin chinatayidwa, ndipo 100% chinawonjezeredwa μ L FBS free medium ndi 10 μ L cell counting kit 8 (CCK8) reagent.Maselo adayikidwa pa 37 ℃ kwa maola ena a 1-2, ndipo kuyamwa kwa chitsime chilichonse kunadziwika pa 490 nm pogwiritsa ntchito owerenga ELISA.Kuthekera kwa ma cell kumawonetsedwa ngati kusintha kangapo pakuyamwa [2].

Kuyesera kwa zinyama:pa nkhani ya paw edema model, mbewa [3] anapatsidwa isoorientin kapena celecoxib intraperitoneally, ndipo carrageenan anabayidwa mwachindunji mu paw ola limodzi pambuyo pake.Muchitsanzo cha airbag, mankhwala onse amalowa m'thumba la thumba mwachindunji ndi carrageenan.isoorientin anabayidwa 3 maola carrageenan jekeseni mu kapisozi.Isoorientin ndi celecoxib zidaperekedwa kwa mbewa.Mayankho a Stock a isoorientin (100 mg / ml) ndi celecoxib (100 mg / ml) adakonzedwa mu DMSO ndikusinthidwanso panthawi ya chithandizo.Nyamazo zinagawidwa m'magulu asanu otsatirawa: kulamulira (DMSO ankachitira);Mankhwala a carrageenan (0.5 ml (1.5% (w / V) carrageenan mu brine); Mankhwala a carrageenan + celecoxib (20mg / kg kulemera kwa thupi); Carrageenan + isoorientin (10 mg / kg kulemera kwa thupi); Chithandizo cha carrageenan + isoorientin (20mg / kg kulemera kwa thupi).

Zolozera:[1].Sumalatha M, et al.Isoorientin, Selective Inhibitor ya Cyclooxygenase-2 (COX-2) kuchokera ku Tubers of Pueraria tuberosa.Nat Prod Commun.2015 Oct;10(10):1703-4.
[2].Ye T, et al.Isoorientin imapangitsa apoptosis, imachepetsa kuwononga, ndipo imachepetsa kutulutsa kwa VEGF mwa kuyambitsa chizindikiro cha AMPK m'maselo a khansa ya pancreatic.Onco Target Ther.2016 Dec 12; 9:7481-7492.
[3].Anilkumar K, et al.Kuunika kwa Anti-Inflammatory Properties of Isoorientin Isolated from Tubers of Pueraria tuberosa.Oxid Med Cell Longev.2017;2017:5498054.