Cov khoom

Nqe lus piav qhia:tanshinone I yog hom IIA tib neeg recombinant sPLA2 thiab Rabbit Recombinant cPLA2 inhibitor nrog IC50 ntawm 11 raws li μ M thiab 82 μ M.

Pawg muaj feem:Kev taw qhia txoj hauv kev > > metabolic enzymes /
Proteases > > phospholipids
Kev tshawb fawb teb > > kab mob plawv
Khoom ntuj >> Quinones

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

Kev tshawb fawb hauv Vitro:tanshinone I inhibited qhov tsim ntawm PGE2 los ntawm LPS induced raw macrophages (IC50 = 38 μ M). ). Thaum ntxiv tom qab ua tiav induction ntawm COX-2, tanshinone kuv kuj txo cov zus tau tej cov PGE2 (IC50 = 46) μ M). ncaj qha inhibit COX-2 kev ua si thiab / lossis cuam tshuam rau PLA2 Kev Ua Si. Thaum tanshinone kuv tau tsim nrog ob hom sib txawv ntawm phospholipase A2 (PLA2), nws cuam tshuam sPLA2 nyob rau hauv ib qho kev ua kom muaj zog (IC50 = 11) μ M). potency, tanshinone kuv kuj inhibited cPLA2 (IC50 = 82) μ M) [1]

Hauv Vivo Study:tanshinone Kuv tau pom cov tshuaj tiv thaiv kab mob hauv carrageenan induced paw edema thiab adjuvant induced mob caj dab hauv nas.Txhawm rau tsim kom muaj kev tiv thaiv kev ua haujlwm ntawm tanshinone I, cov tsiaj qus qauv ntawm kev mob hnyav thiab mob ntev [rat carrageenan (CGN) - induced paw edema thiab rat adjuvant induced arthritis (AIA)] tau siv.Thaum lub qhov ncauj tanshinone kuv, nws tau pom muaj kev tiv thaiv tseem ceeb tiv thaiv CGN induced paw edema (47% inhibition ntawm 160 mg / kg), thaum IC50 ntawm indomethacin yog 7.1 mg / kg.Hauv AIA, tanshinone kuv tau muab 27% inhibition ntawm qhov mob thib ob rau hnub 18 ntawm qhov ncauj ntawm 50 mg / kg / hnub, thaum prednisolone (5 mg / kg / hnub) pom tias muaj txiaj ntsig inhibition (65%) [1]

Kev sim Kinase:Raws li lub hauv paus ntawm PLA2, tib neeg recombinant sPLA2 (hom IIA) tau ntxuav los ntawm CHO hlwb hloov nrog PLA2 noob, thiab luav recombinant platelet cPLA2 tau txais los ntawm nws cov lus qhia hauv baculovirus.Standard tshuaj sib tov (200) μ 50) Nws muaj 100 hli Tris HCl tsis (pH 9.0), 6 mM CaCl2 thiab 20 nmol ntawm 1-acyl - [1-14C] - arachidonyl Sn glycerol phosphate ethanolamine (2000 CPM).Los yog tsis muaj tanshinone I. cov tshuaj tiv thaiv tau pib los ntawm kev ntxiv 50NG purified sPLA2 los yog cPLA2.Tom qab 20 feeb ntawm 37 ℃, cov dawb fatty acids tsim tau raug tshuaj xyuas.Raws li cov qauv no, kwv yees li 10% ntawm cov roj ntsha dawb tau tso tawm los ntawm cov phospholipid substrate ntxiv hauv cov tshuaj tiv thaiv sib xyaw yam tsis muaj tanshinone I [1].

Kev sim Cell:raw 264.7 hlwb raug coj los ntawm DMEM ntxiv nrog 10% FBS thiab 1% tshuaj tua kab mob ntawm 37 ℃ qis dua 5% CO2.Nyob rau hauv luv luv, hlwb tau noob rau ntawm 96 qhov zoo daim hlau (2) × 10 (5 hlwb / qhov zoo).Tshwj tsis yog hais tias muaj lwm yam qhia, LPS (1ug / ml) thiab tanshinone kuv tau ntxiv thiab incubated rau 24 teev.PGE2 concentration hauv nruab nrab yog ntsuas siv EIA cov khoom siv rau PGE2.Txhawm rau txiav txim siab txog cov txiaj ntsig ntawm tanshinone I ntawm PGE 2 ntau lawm tom qab COX-2 induction, cov hlwb tau tov nrog LPS (1 μ G / ml) rau 24 teev thiab ntxuav kom huv si.Tom qab ntawd, tanshinone kuv tau ntxiv yam tsis muaj LPS thiab cov hlwb raug coj mus rau lwm 24 teev.PGE2 concentration tau ntsuas los ntawm qhov nruab nrab.MTT assay tau siv los tshuaj xyuas cytotoxicity ntawm tanshinone I ntawm cov hlwb nyoos.Tanshinone I ntawm 100 μ M tsis pom muaj cytotoxicity [1].

Kev sim tsiaj:Txhawm rau ntsuas qhov inhibitory kev ua haujlwm ntawm tanshinone I ntawm tus qauv mob hnyav thiab mob ntev, nas carrageenan (CGN) - induced paw edema thiab adjuvant induced arthritis (AIA) qauv tau siv.Nyob rau hauv luv luv, 1% CGN yaj nyob rau hauv pyrogen dawb saline (0.05 ml) yog txhaj rau hauv txoj cai rear paw ntawm nas rau paw edema kuaj.Tom qab 5 teev, qhov o ntawm cov claws kho tau raug ntsuas los ntawm plethysmograph.Tanshinone kuv yaj nyob rau hauv 0.5% CMC yog siv rau qhov ncauj 1 teev ua ntej txhaj tshuaj CGN.Rau qhov kev xeem AIA, mob caj dab raug mob los ntawm kev txhaj tshuaj Mycobacterium lactis (0.6ml / nas) yaj hauv cov roj ntxhia rau hauv txoj cai hind paw ntawm nas.Tanshinone kuv tau noj txhua hnub.Kev nthuav dav ntawm kev kho thiab tsis kho cov claws tau ntsuas siv plethysmograph.

Cov ntaub ntawv:[1] Kim SY, et al.Cov teebmeem ntawm Tanshinone I cais tawm ntawm Salvia miltiorrhiza bunge ntawm arachidonic acid metabolism thiab hauv vivo inflammatory teb.Phytother Res.Nov 2002;16(7):616-20.