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Nkọwa:tanshinone I bụ ụdị IIIA mmadụ recombinant sPLA2 na Rabbit Recombinant cPLA2 inhibitor nwere IC50 nke 11 n'otu n'otu μ M na 82 μM.

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

N'ime Vitro Ọmụmụ:tanshinone M na-egbochi nhazi nke PGE2 site na LPS na-ebute macrophages raw (IC50 = 38 μ M) . Mgbe tanshinone I na LPS agbakwunyere n'otu oge ahụ, ogige ahụ gbochiri 10-100 μ PGE2 mmepụta M (IC50 = 38 μM). Mgbe agbakwunyere mgbe ntinye nke COX-2 zuru oke, tanshinone m na-ebelata mmepụta nke PGE2 (IC50 = 46) μM). na-egbochi ọrụ COX-2 ozugbo na / ma ọ bụ na-emetụta ọrụ PLA2. Mgbe tanshinone ejiri m ụdị abụọ dị iche iche nke phospholipase A2 (PLA2), ọ na-egbochi sPLA2 n'ụzọ dabere na ntinye uche (IC50 = 11) μM). ike, tanshinone m gbochiri cPLA2 (IC50 = 82) μ M）[1]

Na Ọmụmụ Vivo:tanshinone M gosiri mgbochi mkpali ọrụ na carrageenan butere paw edema na adjuvant na-akpata ọrịa ogbu na nkwonkwo na oke.Iji guzobe ọrụ mgbochi mkpali nke tanshinone I, a na-eji ụdị anụmanụ oge ochie nke nnukwu na-adịghị ala ala mbufụt [rat carrageenan (CGN) - induced paw edema na rat adjuvant induced arthritis (AIA)].Mgbe ọnụ tanshinone I, ọ gosipụtara nnukwu mgbochi mkpali ọrụ megide CGN butere paw edema (mmechi 47% na 160 mg / kg), ebe IC50 nke indomethacin bụ 7.1 mg / kg.Na AIA, tanshinone m nyere 27% mgbochi nke mbufụt nke abụọ n'ụbọchị 18 na ọnụọgụ ọnụ nke 50 mg / kg / ụbọchị, ebe prednisolone (5 mg / kg / ụbọchị) gosipụtara mgbochi dị irè (65%) [1].

Nnwale Kinase:dị ka isi iyi nke PLA2, a sachara mmadụ recombinant sPLA2 (ụdị IIA) site na mkpụrụ ndụ CHO bufere site na PLA2 gene, na oke bekee recombinant platelet cPLA2 nwetara site na nkwupụta ya na baculovirus.Ngwakọta mmeghachi omume ọkọlọtọ (200) μ 50) Ọ nwere 100 mm Tris HCl ihe nchekwa (pH 9.0), 6 mM CaCl2 na 20 nmol nke 1-acyl - [1-14C] - arachidonyl Sn glycerol phosphate ethanolamine (2000 CPM / nmol).Ma ọ bụ enweghị tanshinone I. mmeghachi omume malitere site n'ịgbakwunye 50NG dị ọcha sPLA2 ma ọ bụ cPLA2.Mgbe nkeji 20 gachara na 37 ℃, a na-enyocha acid fatty n'efu emepụtara.N'okpuru ọnọdụ ọkọlọtọ ndị a, a na-ahapụ ihe dịka 10% nke fatty acids n'efu site na ntinye phospholipid agbakwunyere na ngwakọta mmeghachi omume na-enweghị tanshinone I [1].

Nnwale cell:Azụlitere mkpụrụ ndụ 264.7 raw na DMEM gbakwunyere na 10% FBS na 1% ọgwụ nje na 37 ℃ n'okpuru 5% CO2.Na nkenke, a na-akụ mkpụrụ ndụ mkpụrụ ndụ na efere olulu mmiri 96 (2) × 10 (sel 5 / olulu mmiri).Ọ gwụla ma egosiputara n'ụzọ ọzọ, LPS (1ug / ml) na tanshinone etinyere m wee tinye ya maka awa 24.A tụrụ ntinye uche PGE2 na ọkara site na iji ngwa EIA maka PGE2.Iji chọpụta mmetụta nke tanshinone I na mmepụta PGE 2 mgbe ntinye COX-2 gasịrị, a na-ejikọta mkpụrụ ndụ na LPS (1 μ G / ml) maka awa 24 ma saa ya nke ọma.Mgbe ahụ, agbakwunyere tanshinone m na-enweghị LPS ma mepụta mkpụrụ ndụ maka awa 24 ọzọ.A tụrụ ntinye uche PGE2 site na ọkara.Ejiri MTT nyocha iji nyochaa cytotoxicity nke tanshinone I na mkpụrụ ndụ raw.Tanshinone I na 100 μM egosighi ihe ọ bụla cytotoxicity [1].

Nnwale anụmanụ:iji nyochaa ọrụ mgbochi nke tanshinone I na ụdị anụmanụ na-egbu egbu na-adịghị ala ala, a na-eji ụdị rat carrageenan (CGN) na-akpata paw edema na adjuvant induced arthritis (AIA).Na nkenke, 1% CGN gbazere na saline free pyrogen (0.05 ml) ka agbanyere n'ime aka nri azụ nke oke maka ule edema paw.Mgbe awa 5 gachara, a na-eji plethysmograph tụọ ọzịza nke mkpịsị aka a na-agwọ.Tanshinone m gbazere na 0.5% CMC ka a na-enye ọnụ 1 hour tupu ịgbanye CGN.Maka ule AIA, mbufụt ogbu na nkwonkwo kpalitere site na ịgbanye Mycobacterium lactis (0.6ml / rat) gbazere na mmanụ ịnweta n'ime aka nri oke oke.A na-enye Tanshinone m ọnụ kwa ụbọchị.A tụrụ mgbasawanye nke nkwojiaka a na-agwọghị na nke a na-agwọghị site na iji plethysmograph.

Ntụaka:[1] Kim SY, et al.Mmetụta nke Tanshinone I dịpụrụ adịpụ na Salvia miltiorrhiza bunge na arachidonic acid metabolism na na nzaghachi mkpali vivo.Phytother Res.2002 Nov;16 (7): 616-20 .