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Kufotokozera:tanshinone I ndi mtundu wa IIA human recombinant sPLA2 ndi Rabbit Recombinant cPLA2 inhibitor yokhala ndi IC50 ya 11 motsatana μ M ndi 82 μ M.

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Zolinga:IC50: 11 μM (sPLA2), 82 μM (cPLA2) [1].

Phunziro la In Vitro:tanshinone ndinaletsa mapangidwe a PGE2 ndi LPS omwe amachititsa macrophages yaiwisi (IC50 = 38 μ M) Pamene tanshinone I ndi LPS zinawonjezeredwa panthawi imodzimodziyo, chigawocho chinalepheretsa kwambiri 10-100 μ PGE2 kupanga M (IC50 = 38 μ M ）. Mukawonjezeredwa mutatha kukhazikitsidwa kwathunthu kwa COX-2, tanshinone ndinachepetsanso kupanga PGE2 (IC50 = 46) μ M) Mfundo yakuti tanshinone I imalepheretsa kupanga PGE 2 kupyolera mu pre-induced COX-2 imasonyeza kuti mankhwalawa amatha. Imalepheretsa mwachindunji ntchito ya COX-2 komanso / kapena kukhudza ntchito ya PLA2. Pamene tanshinone idalumikizidwa ndi mitundu iwiri ya phospholipase A2 (PLA2), idaletsa kwambiri sPLA2 modalira ndende (IC50 = 11) μ M). potency, tanshinone Ndinaletsanso cPLA2 (IC50 = 82) μ M) [1]

Mu Phunziro la Vivo:tanshinone Ndinawonetsa ntchito yotsutsa-kutupa mu carrageenan induced paw edema ndi adjuvant induced nyamakazi mu makoswe.Pofuna kukhazikitsa anti-kutupa ntchito ya tanshinone I, mitundu yakale ya nyama zakutupa [rat carrageenan (CGN) - induced paw edema ndi rat adjuvant induced arthritis (AIA)]] idagwiritsidwa ntchito.Pamene oral tanshinone I, anasonyeza kwambiri odana ndi kutupa ntchito CGN anachititsa paw edema (47% chopinga pa 160 mg / kg), pamene IC50 wa indomethacin anali 7.1 mg/kg.Mu AIA, tanshinone ndidapereka 27% kuletsa kutupa kwachiwiri pa tsiku la 18 pakamwa pa 50 mg / kg / tsiku, pomwe prednisolone (5 mg / kg / tsiku) idawonetsa kuletsa kothandiza (65%) [1]

Kuyesera kwa Kinase:monga gwero la PLA2, munthu recombinant sPLA2 (mtundu IIA) anayeretsedwa kuchokera CHO maselo transfected ndi PLA2 jini, ndi kalulu recombinant kupatsidwa zinthu za m`mwazi cPLA2 anapezedwa mwa mawu ake mu baculovirus.Standard anachita osakaniza (200) μ 50) Munali 100 mamilimita Tris HCl bafa (pH 9.0), 6 mM CaCl2 ndi 20 nmol wa 1-acyl - [1-14C] - arachidonyl Sn glycerol mankwala ethanolamine (2000 CPM / nmol).Kapena panalibe tanshinone I. zomwe zinayambika powonjezera 50NG purified sPLA2 kapena cPLA2.Pambuyo pa mphindi 20 pa 37 ℃, mafuta amafuta aulere omwe amapangidwa adawunikidwa.Pansi pamikhalidwe iyi, pafupifupi 10% yamafuta acids aulere amatulutsidwa kuchokera ku gawo lapansi lowonjezera la phospholipid muzomwe zimasakanikirana popanda tanshinone I [1].

Kuyesa Maselo:Ma cell aiwisi 264.7 adakulitsidwa ndi DMEM yowonjezeredwa ndi 10% FBS ndi 1% maantibayotiki pa 37 ℃ pansi pa 5% CO2.Mwachidule, maselo adabzalidwa pa mbale 96 (2) × 10 (maselo 5 / chitsime).Pokhapokha zitasonyezedwa, LPS (1ug / ml) ndi tanshinone ndinawonjezedwa ndikuyikidwa kwa maola 24.Kuphatikizika kwa PGE2 mkatikati kunayesedwa pogwiritsa ntchito zida za EIA za PGE2.Pofuna kudziwa zotsatira za tanshinone I pa PGE 2 kupanga pambuyo pa kulowetsedwa kwa COX-2, maselo adasakanizidwa ndi LPS (1 μ G / ml) kwa maola 24 ndikutsuka bwino.Kenako, tanshinone ndinawonjezedwa popanda LPS ndi maselo otukuka kwa maola ena 24.Kukhazikika kwa PGE2 kunayesedwa kuchokera pakati.Mayeso a MTT adagwiritsidwa ntchito poyesa cytotoxicity ya tanshinone I pama cell aiwisi.Tanshinone I pa 100 μ M sanasonyeze cytotoxicity [1].

Kuyesera kwa Zinyama:pofuna kuyesa ntchito yolepheretsa ya tanshinone I pa zinyama zowonongeka komanso zowonongeka, makoswe a carrageenan (CGN) - omwe amachititsa paw edema ndi adjuvant induced arthritis (AIA) anagwiritsidwa ntchito.Mwachidule, 1% CGN yosungunuka mu saline yaulere ya pyrogen (0.05 ml) inalowetsedwa kumanja kwakumbuyo kwa makoswe pofuna kuyesa paw edema.Pambuyo pa maola 5, kutupa kwa zikhadabo zochizidwa kumayesedwa pogwiritsa ntchito plethysmograph.Tanshinone I kusungunuka mu 0.5% CMC anaperekedwa pakamwa 1 ola pamaso CGN jekeseni.Pakuyezetsa kwa AIA, kutupa kwa nyamakazi kudayambika pobaya Mycobacterium lactis (0.6ml / rat) wosungunuka mumafuta amchere kumanja akumbuyo kwa makoswe.Tanshinone ndinali kuperekedwa pakamwa tsiku lililonse.Kukula kwa zikhadabo zochiritsidwa ndi zosagwiritsidwa ntchito kunayesedwa pogwiritsa ntchito plethysmograph.

Zolozera:[1] Kim SY, et al.Zotsatira za Tanshinone I wolekanitsidwa ndi Salvia miltiorrhiza bunge pa arachidonic acid metabolism komanso mu vivo inflammatory responses.Phytother Res.2002 Nov;16(7):616-20.