Ibicuruzwa

Ibisobanuro:tanshinone I ni ubwoko bwa IIA recombinant sPLA2 na Rabbit Recombinant cPLA2 inhibitor hamwe na IC50 ya 11 bikurikiranye μ M na 82 μ M。

Ibyiciro bifitanye isano:inzira yerekana inzira >> enzymes za metabolike /
protease >> fosifolipide
Urwego rwubushakashatsi >> Indwara yumutima
Ibicuruzwa Kamere >> Quinone

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

Mu Kwiga Vitro:tanshinone I yabujije ishyirwaho rya PGE2 na LPS itera macrophage mbisi (IC50 = 38 μ M）。 Iyo tanshinone I na LPS byongeweho icyarimwe, uruganda rwabujije cyane umusaruro wa 10-100 μ PGE2 kubyara M (IC50 = 38 μ M . guhagarika byimazeyo ibikorwa bya COX-2 kandi / cyangwa bigira ingaruka kubikorwa bya PLA2. Iyo tanshinone ya I yashizwemo nuburyo bubiri butandukanye bwa fosifolipase A2 (PLA2), yabujije cyane sPLA2 muburyo bushingiye ku kwibanda (IC50 = 11) μ M). imbaraga, tanshinone Nanjye nabujije cPLA2 (IC50 = 82) μ M） [1]

Mu Kwiga Vivo:tanshinone Nerekanye ibikorwa byo kurwanya inflammatory muri carrageenan iterwa na paw edema hamwe na arthritis iterwa na rubagimpande mu mbeba.Mu rwego rwo gushyiraho ibikorwa byo kurwanya inflammatory ya tanshinone ya I, hakoreshejwe uburyo bw’inyamanswa za kera z’umuriro ukabije kandi udakira [imbeba carrageenan (CGN) - yatewe na paw edema na imbeba iterwa na rubagimpande (AIA)].Iyo umunwa wa tanshinone wa I, werekanye ibikorwa bikomeye byo kurwanya inflammatory kurwanya CGN yatewe na paw edema (47% yabujijwe kuri mg / kg 160), naho IC50 ya indomethacine yari 7.1 mg / kg.Muri AIA, tanshinone natanze 27% yo kubuza gutwikwa kwa kabiri kumunsi wa 18 kumunwa wa 50 mg / kg / kumunsi, mugihe prednisolone (5 mg / kg / kumunsi) yerekanaga kubuza (65%) [1]

Ubushakashatsi bwa Kinase:nkisoko ya PLA2, recombinant yumuntu sPLA2 (ubwoko bwa IIA) yasukuwe muri selile CHO yandujwe na gene ya PLA2, kandi urukwavu recombinant platelet cPLA2 rwabonetse binyuze mumagambo yayo muri baculovirus.Imvange isanzwe ivanze (200) μ 50) Yarimo mm 100 ya Tris HCl buffer (pH 9.0), 6 mM CaCl2 na 20 nmol ya 1-acyl - [1-14C] - arachidonyl Sn glycerol fosifate etanolamine (2000 CPM / nmol).Cyangwa nta tanshinone yariho I. reaction yatangijwe no kongeramo 50NG isukuye sPLA2 cyangwa cPLA2.Nyuma yiminota 20 kuri 37 ℃, aside irike yubusa yakozwe yarasesenguwe.Muri ibi bihe bisanzwe, hafi 10% ya aside irike yubusa irekurwa muri substrate ya fosifolipide munganda zivanze nta tanshinone I [1].

Ubushakashatsi bwakagari:selile 264.7 mbisi zarezwe hamwe na DMEM hiyongeraho 10% FBS na antibiotique 1% kuri 37 ℃ munsi ya 5% CO2.Muri make, selile zabibwe ku isahani 96 y'iriba (2) × 10 (selile 5 / iriba).Keretse niba byerekanwe ukundi, LPS (1ug / ml) na tanshinone nongeyeho kandi nashizwemo amasaha 24.Ubunini bwa PGE2 murwego rwapimwe hifashishijwe ibikoresho bya EIA kuri PGE2.Kugirango umenye ingaruka za tanshinone I ku musaruro wa PGE 2 nyuma yo kwinjizwa kwa COX-2, selile zavanze na LPS (1 μ G / ml) amasaha 24 hanyuma zozwa neza.Noneho, tanshinone nongeyeho nta LPS kandi selile zarakuze mumasaha 24.Ubunini bwa PGE2 bwapimwe uhereye hagati.MTT assay yakoreshejwe mugusuzuma cytotoxicity ya tanshinone I kuri selile mbisi.Tanshinone I kuri 100 μ M ntabwo yerekanye cytotoxicity [1].

Ubushakashatsi ku nyamaswa:mu rwego rwo gusuzuma ibikorwa byo guhagarika tanshinone ya I ku buryo bw’inyamanswa zikarishye kandi zidakira, imbeba carrageenan (CGN) - yatewe na paw edema yatewe na moderi ya arthritis (AIA).Muri make, 1% CGN yashonga muri salogene yubusa ya pyrogene (0,05 ml) yatewe mumaguru yinyuma yimbeba yimbeba kugirango yipimishe.Nyuma yamasaha 5, kubyimba inzara zavuwe byapimwe hakoreshejwe plethysmograf.Tanshinone I yashonga muri 0.5% CMC yatanzwe kumunwa isaha 1 mbere yo guterwa CGN.Kwipimisha AIA, gutwika arthritic byatewe no gutera Mycobacterium lactis (0,6ml / imbeba) yashonga mumavuta yubutare mumaboko yinyuma yimbeba.Tanshinone Nayobowe kumanwa buri munsi.Kwagura inzara zavuwe kandi zitavuwe zapimwe hakoreshejwe plethysmograf.

Reba:[1] Kim SY, n'abandi.Ingaruka za Tanshinone Natandukanije na Saliviya miltiorrhiza bunge kuri metabolism acide arachidonic no mubisubizo bya vivo inflammatory.Phytother Res.2002 Ugushyingo;16 (7): 616-20.