Iimveliso

Inkcazo:tanshinone I luhlobo IIA yabantu recombinant sPLA2 kunye noMvundla Recombinant cPLA2 inhibitor ene-IC50 ye-11 ngokulandelelanayo μ M kunye ne-82 μ M.

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

Isifundo se-In Vitro:I-tanshinone ndathintela ukubunjwa kwe-PGE2 nge-LPS eyenza i-macrophages eluhlaza (IC50 = 38 μ M) ）. Xa yongezwa emva kokungeniswa okupheleleyo kwe-COX-2, i-tanshinone ndaye ndanciphisa ukuveliswa kwe-PGE2 (IC50 = 46) μ M) Inyaniso yokuba i-tanshinone inqanda i-PGE 2 imveliso ngokusebenzisa i-COX-2 yangaphambili iphakamisa kakhulu ukuba i-compound ingakwazi. inqanda ngokuthe ngqo umsebenzi we-COX-2 kunye / okanye ichaphazela umsebenzi we-PLA2. Xa i-tanshinone ndifakwe kwiifom ezimbini ezahlukeneyo ze-phospholipase A2 (PLA2), yayinqande kakhulu i-sPLA2 ngendlela yokuxhomekeka koxinzelelo (IC50 = 11) μ M) Nangona iphantsi kwayo. amandla, tanshinone Ndikwanqande cPLA2 (IC50 = 82) μ M）[1]

KwiSifundo seVivo:tanshinone Ndabonisa umsebenzi wokuchasana nokudumba kwi-carrageenan eyenza i-paw edema kunye ne-adjuvant induced arthritis kwiigundane.Ukuze kusekwe umsebenzi wokuchasana nokudumba kwe-tanshinone I, iimodeli zezilwanyana zakudala zokuvuvukala okubukhali kunye nokungapheliyo [i-rat carrageenan (CGN) - i-paw edema eyenziwe kunye ne-rat adjuvant induced arthritis (AIA)] yasetyenziswa.Xa i-tanshinone yomlomo I, ibonise umsebenzi ochasene nokuvuvukala kwi-CGN eyenza i-paw edema (i-47% inhibition kwi-160 mg / kg), ngelixa i-IC50 ye-indomethacin yayingu-7.1 mg / kg.Kwi-AIA, i-tanshinone ndinike i-27% inhibition yokuvuvukala kwesibini ngosuku lwe-18 kwi-dose yomlomo ye-50 mg / kg / ngosuku, ngelixa i-prednisolone (5 mg / kg / ngosuku) ibonise ukuvinjelwa okusebenzayo (65%) [1]

Uvavanyo lukaKinase:njengomthombo we-PLA2, i-sPLA2 ye-recombinant (uhlobo lwe-IIA) yahlanjululwa kwiiseli ze-CHO ezigqitywe nge-PLA2 gene, kunye ne-rabbit recombinant platelet cPLA2 yafunyanwa ngokubonakaliswa kwayo kwi-baculovirus.Standard reaction umxube (200) μ 50) Yayiqulathe 100 mm Tris HCl buffer (pH 9.0), 6 mM CaCl2 kunye 20 nmol 1-acyl - [1-14C] - arachidonyl Sn glycerol phosphate ethanolamine (2000 CPM / nmol).Okanye kwakungekho tanshinone I. impendulo yaqalwa ngokudibanisa 50NG purified sPLA2 okanye cPLA2.Emva kwemizuzu engama-20 kwi-37 ℃, iiasidi ezinamafutha asimahla avelisiweyo ahlalutywa.Ngaphantsi kwezi meko eziqhelekileyo, malunga ne-10% ye-fatty acids yamahhala ikhutshwe kwi-substrate ye-phospholipid eyongezelelweyo kumxube wokuphendula ngaphandle kwe-tanshinone I [1].

Uvavanyo lweSeli:iiseli ze-264.7 ezikrwada zakhuliswa kunye ne-DMEM eyongezwa nge-10% ye-FBS kunye ne-1% ye-antibiotics kwi-37 ℃ phantsi kwe-5% CO2.Ngamafutshane, iiseli zahlwayelwa kwiiplate ze-96 kakuhle (2) × 10 (iiseli ezi-5 / kakuhle).Ngaphandle kokuba kuboniswe ngenye indlela, i-LPS (1ug / ml) kunye ne-tanshinone ndongezwa kwaye ndifakwe kwiiyure ze-24.Ugxininiso lwe-PGE2 oluphakathi lulinganiswe kusetyenziswa ikhithi ye-EIA ye-PGE2.Ukuze unqume umphumo we-tanshinone I kwi-PGE 2 yokuveliswa emva kokungeniswa kwe-COX-2, iiseli zixutywe kunye ne-LPS (1 μ G / ml) kwiiyure ze-24 kwaye zihlanjwe kakuhle.Emva koko, i-tanshinone ndongezwa ngaphandle kwe-LPS kwaye iiseli zakhuliswa ezinye iiyure ezingama-24.Ugxininiso lwe-PGE2 lulinganiswa ukusuka phakathi.Uvavanyo lwe-MTT lwalusetyenziselwa ukuvavanya i-cytotoxicity ye-tanshinone I kwiiseli eziluhlaza.I-Tanshinone I kwi-100 μ M ayizange ibonise nayiphi na i-cytotoxicity [1].

Uvavanyo lwezilwanyana:ukwenzela ukuvavanya umsebenzi we-inhibitory we-tanshinone I kwiimodeli zezilwanyana ezivuthayo kunye ezingapheliyo, i-rat carrageenan (CGN) - i-paw edema eyenziwe nge-paw kunye ne-adjuvant induced arthritis (AIA) isetyenziswe.Ngamafutshane, i-1% ye-CGN echithwe kwi-saline yamahhala ye-pyrogen (0.05 ml) ifakwe kwi-paw yangemva yangemva yeegundane zokuvavanya i-paw edema.Emva kweeyure ze-5, ukudumba kweenzipho eziphathwayo kulinganiswa kusetyenziswa i-plethysmograph.I-Tanshinone ndachithwa kwi-0.5% ye-CMC ilawulwa ngomlomo ngeyure ye-1 ngaphambi kwe-CGN injection.Kuvavanyo lwe-AIA, ukudumba kwe-arthritic kwenziwa ngokutofa iMycobacterium lactis (0.6ml / ibuzi) inyibilikiswe kwioyile yamaminerali kwimpuku yangasemva yasekunene.ITanshinone ndandiyinikwa ngomlomo yonke imihla.Ukwandiswa kweenzipho ezinyangwayo nezinganyangwanga kwalinganiswa kusetyenziswa iplethysmograph.

IiReferensi:[1] UKim SY, et al.Iziphumo ze-Tanshinone I zahlukanisiwe kwi-Salvia miltiorrhiza bunge kwi-arachidonic acid metabolism kunye neempendulo ezivuthayo ezivuthayo.Phytother Res.2002 Nov;16(7):616-20.