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Tsanangudzo:tanshinone I imhando IIA yemunhu recombinant sPLA2 uye Rabbit Recombinant cPLA2 inhibitor ine IC50 ye11 zvakateerana μ M uye 82 μ M.

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

In Vitro Chidzidzo:tanshinone Ndakadzivisa kuumbwa kwePGE2 neLPS yakakonzera macrophages yakasvibirira (IC50 = 38 μ M). ）。 Kana yakawedzerwa mushure mekugadzirwa kwakakwana kweCOX-2, tanshinone ndakaderedzawo kugadzirwa kwePGE2 (IC50 = 46) μ M) . Ichokwadi kuti tanshinone I inhibits PGE 2 kugadzirwa kuburikidza nepre-induced COX-2 inonyatsoratidza kuti chidimbu chinogona. inhibisa zvakananga COX-2 chiitiko uye / kana kukanganisa PLA2 Chiitiko. Apo tanshinone ndakaiswa nemhando mbiri dzakasiyana dzephospholipase A2 (PLA2), yakanyanya kuvharidzira sPLA2 nenzira yekutsamira (IC50 = 11) μ M). potency, tanshinone Ini zvakare inhibited cPLA2 (IC50 = 82) μ M) [1]

MuVivo Chidzidzo:tanshinone Ndakaratidza basa rinopesana nekuputika mu carrageenan induced paw edema uye adjuvant induced arthritis mumakonzo.Kuti amise basa rinopesana nekuputika kwetanshinone I, mhando dzemhando dzemhuka dzeacute uye dzisingaperi kuzvimba [rat carrageenan (CGN) - induced paw edema uye rat adjuvant induced arthritis (AIA)] yakashandiswa.Kana oral tanshinone I, yakaratidza basa rakakosha rinopesana nekuzvimba kurwisa CGN yakakonzera paw edema (47% inhibition pa160 mg / kg), nepo IC50 yeindomethacin yaive 7.1 mg / kg.MuAIA, tanshinone ndakapa 27% inhibition yekuzvimba kwechipiri pazuva 18 pamuromo we50 mg / kg / zuva, nepo prednisolone (5 mg / kg / zuva) yakaratidza inhibition inoshanda (65%) [1]

Kinase Kuedza:sechitubu chePLA2, recombinant yemunhu sPLA2 (rudzi IIA) yakacheneswa kubva kuCHO masero akatapurirwa nePLA2 gene, uye tsuro recombinant platelet cPLA2 yakawanikwa kuburikidza nekutaura kwayo mu baculovirus.Standard reaction musanganiswa (200) μ 50) Yaiva 100 mm Tris HCl buffer (pH 9.0), 6 mM CaCl2 uye 20 nmol of 1-acyl - [1-14C] - arachidonyl Sn glycerol phosphate ethanolamine (2000 CPM / nmol).Kana kuti pakanga pasina tanshinone I. maitiro akatangwa nekuwedzera 50NG yakachena sPLA2 kana cPLA2.Mushure memaminitsi makumi maviri pa37 ℃, iwo emahara mafuta acids akagadzirwa akaongororwa.Pasi pemamiriro aya akajairwa, anenge gumi muzana emahara emafuta acids anoburitswa kubva kune yakawedzera phospholipid substrate mumusanganiswa wekuita pasina tanshinone I [1].

Cell Experiment:masero 264.7 mbishi akagadzirwa neDMEM yakawedzerwa ne10% FBS uye 1% mishonga inorwisa mabhakitiriya pa37 ℃ pasi pe5% CO2.Muchidimbu, masero akadyarwa pamahwendefa makumi mapfumbamwe nematanhatu (2) × 10 (5 masero / tsime).Kunze kwekunge zvaratidzwa neimwe nzira, LPS (1ug / ml) uye tanshinone ini ndakawedzerwa uye ndakaiswa kwemaawa makumi maviri nemana.Iyo PGE2 yepakati mukati yakayerwa uchishandisa EIA kit yePGE2.Kuti uone kushanda kwetanshinone I paPGE 2 kugadzirwa mushure meCOX-2 induction, masero akasanganiswa neLPS (1 μ G / ml) kwemaawa makumi maviri nemana uye akashambidzwa zvakakwana.Ipapo, tanshinone ini ndakawedzerwa ndisina LPS uye maseru akagadzirwa kwemamwe maawa makumi maviri nemana.PGE2 concentration yakayerwa kubva pakati.MTT assay yakashandiswa kuongorora cytotoxicity ye tanshinone I pamasero mambishi.Tanshinone I pa100 μ M haina kuratidza chero cytotoxicity [1].

Kuedza kwemhuka:kuitira kuti uongorore inhibitory basa re tanshinone I pamhando dzakanyanya uye dzisingagumi dzinopisa mhuka, rat carrageenan (CGN) - induced paw edema uye adjuvant induced arthritis (AIA) mienzaniso yakashandiswa.Muchidimbu, 1% CGN yakanyungudutswa mu pyrogen isina saline (0.05 ml) yakaiswa mukati mekurudyi kumashure paw yemakonzo paw edema test.Mushure memaawa mashanu, kuzvimba kwemazino akarapwa akayerwa uchishandisa plethysmograph.Tanshinone I yakanyungudika mu 0.5% CMC yaiitwa nemuromo 1 awa isati yasvika CGN jekiseni.Kuyedzo yeAIA, kuzvimba kweArthritic kwakakonzerwa nekujova Mycobacterium lactis (0.6ml / rat) yakanyungudutswa mumafuta emaminerari mukati mekurudyi kweshure kwemakonzo.Tanshinone ndaipihwa nemuromo mazuva ese.Kuwedzerwa kwemakwenzi akarapwa uye asina kurapwa akayerwa uchishandisa plethysmograph.

References:[1] Kim SY, et al.Mhedzisiro yeTanshinone I yakasarudzika kubva kuSalvia miltiorrhiza bunge pane arachidonic acid metabolism uye muvivo kuzvimba mhinduro.Phytother Res.2002 Nov;16(7):616-20.