Lihlahisoa

Tlhaloso:tanshinone I ke mofuta oa IIA human recombinant sPLA2 le Rabbit Recombinant cPLA2 inhibitor e nang le IC50 ea 11 ka ho latellana μ M le 82 μ M.

Lihlopha tse amanang:litsela tsa matšoao > > li-enzyme tsa metabolism /
liprotheine > > phospholipids
Sebaka sa lipatlisiso > > lefu la pelo
Lihlahisoa tsa Tlhaho > > Quinones

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

Thuto ea In Vitro:tanshinone Ke ile ka thibela ho thehoa ha PGE2 ka LPS e entseng macrophages e tala (IC50 = 38 μ M) Ha tanshinone I le LPS li kenngoa ka nako e le 'ngoe, motsoako o ile oa thibela haholo 10-100 μ PGE2 tlhahiso ea M (IC50 = 38 μ M ）。 Ha e kenyelletsoa ka mor'a ho kenngoa ka ho feletseng ha COX-2, tanshinone ke boetse ke fokotsa tlhahiso ea PGE2 (IC50 = 46) μ M) . Taba ea hore tanshinone ke thibela tlhahiso ea PGE 2 ka COX-2 e entsoeng pele e fana ka maikutlo a matla a hore motsoako o ka khona ho etsa joalo. Ha tanshinone ke ne ke kenngoa ka mefuta e 'meli e fapaneng ea phospholipase A2 (PLA2), e thibela sPLA2 haholo ka mokhoa o itšetlehileng ka mahloriso (IC50 = 11) μ M). potency, tanshinone Ke boetse ke thibela cPLA2 (IC50 = 82) μ M) [1]

Thutong ea Vivo:tanshinone Ke bontšitse tšebetso e khahlanong le ho ruruha ka carrageenan e bakileng paw edema le adjuvant induced ramatiki ho likhoto.E le ho theha ts'ebetso e khahlanong le ho ruruha ea tanshinone I, mefuta ea khale ea liphoofolo ea ho ruruha e matla le e sa foleng [rat carrageenan (CGN) - induced paw edema le rat adjuvant induced arthritis (AIA)]).Ha oral tanshinone I, e bontšitse ts'ebetso ea bohlokoa e khahlanong le ho ruruha khahlanong le CGN e bakileng paw edema (47% inhibition ho 160 mg / kg), ha IC50 ea indomethacin e ne e le 7.1 mg / kg.Ho AIA, tanshinone ke fane ka 27% ea thibelo ea ho ruruha ha bobeli ka letsatsi la 18 ka tekanyo ea molomo ea 50 mg / kg / letsatsi, ha prednisolone (5 mg / kg / letsatsi) e bontšitse thibelo e sebetsang (65%) [1]

Teko ea Kinase:e le mohloli oa PLA2, motho oa recombinant sPLA2 (mofuta oa IIA) o ile oa hloekisoa ho tloha liseleng tsa CHO tse fetisitsoeng ka liphatsa tsa lefutso tsa PLA2, 'me cPLA2 ea recombinant ea mmutla e ile ea fumanoa ka polelo ea eona ho baculovirus.Motsoako o tloaelehileng oa karabelo (200) μ 50) E ne e e-na le 100 mm Tris HCl buffer (pH 9.0), 6 mm CaCl2 le 20 nmol ea 1-acyl - [1-14C] - arachidonyl Sn glycerol phosphate ethanolamine (2000 CPM / nmol).Kapa ho ne ho se na tanshinone I. karabelo e qalile ka ho eketsa 50NG purified sPLA2 kapa cPLA2.Kamora metsotso e 20 ho 37 ℃, li-acid tse sa lefelloeng tsa mafura tse hlahisitsoeng li ile tsa hlahlojoa.Tlas'a maemo ana a tloaelehileng, hoo e ka bang 10% ea li-acid tse sa lefelloeng tsa mafura li lokolloa ho tsoa ho phospholipid substrate e kenyelletsoeng motsoako oa karabelo ntle le tanshinone I [1].

Teko ea Cell:lisele tse tala tsa 264.7 li ne li hlahisoa ka DMEM e tlatsitsoeng ka 10% FBS le 1% ea lithibela-mafu ho 37 ℃ tlas'a 5% CO2.Ka bokhutšoanyane, lisele li ile tsa jaloa ka lipoleiti tsa seliba tse 96 (2) × 10 (lisele tse 5 / seliba).Ntle le ha ho bonts'itsoe ka tsela e 'ngoe, LPS (1ug / ml) le tanshinone ke ile ka eketsoa mme ka kenngoa lihora tse 24.Mahloriso a PGE2 bohareng a lekantsoe ho sebelisoa EIA kit bakeng sa PGE2.E le ho fumana phello ea tanshinone I ka tlhahiso ea PGE 2 ka mor'a ho kenngoa ha COX-2, lisele li ne li kopantsoe le LPS (1 μ G / ml) bakeng sa lihora tse 24 'me li hlatsuoa hantle.Joale, tanshinone ke ile ka eketsoa ntle le LPS mme lisele li ile tsa hlahisoa ka lihora tse ling tse 24.PGE2 mahloriso a lekantsoe ho tloha bohareng.Teko ea MTT e ne e sebelisetsoa ho hlahloba cytotoxicity ea tanshinone I liseleng tse tala.Tanshinone I ka 100 μ M ha ea ka ea bontša cytotoxicity [1].

Teko ea Liphoofolo:e le ho hlahloba ts'ebetso ea inhibitory ea tanshinone I holim'a mefuta e matla le e sa foleng ea liphoofolo tse ruruhileng, rat carrageenan (CGN) - e bakoang ke paw edema le mefuta ea adjuvant induced arthritis (AIA) e sebelisitsoe.Ka bokhutšoanyane, 1% CGN e qhibilihisitsoeng ka saline ea mahala ea pyrogen (0.05 ml) e ile ea kenngoa ka lehlakoreng le letona le ka morao la likhoto bakeng sa tlhahlobo ea paw edema.Ka mor'a lihora tse 5, ho ruruha ha manala a phekoloang ho ne ho lekanyetsoa ho sebelisa plethysmograph.Tanshinone Ke qhibilihile ka 0.5% CMC e ne e tsamaisoa ka molomo hora ea 1 pele ho ente ea CGN.Bakeng sa tlhahlobo ea AIA, ho ruruha ha ramatiki ho ile ha bakoa ke ho enta Mycobacterium lactis (0.6ml / rat) e qhibilihisitsoeng ka oli ea liminerale ka har'a mooko o ka morao oa likhoto.Tanshinone Ke ne ke e fuoa ka molomo letsatsi le leng le le leng.Ho atolosoa ha manala a phekoloang le a sa alafshoang ho ile ha lekanyetsoa ho sebelisoa plethysmograph.

Litšupiso:[1] Kim SY, et al.Litlamorao tsa Tanshinone I e arohaneng le Salvia miltiorrhiza bunge mabapi le metabolism ea arachidonic acid le karabelo ea ho ruruha ea vivo.Phytother Res.2002 Nov;16(7):616-20.