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Bayani:tanshinone I shine nau'in IIA ɗan adam recombinant sPLA2 da Rabbit Recombinant cPLA2 inhibitor tare da IC50 na 11 bi da bi μ M da 82 μM.

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Samfuran Halitta >> Quinones

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

A cikin Nazarin Vitro:tanshinone I hana samuwar PGE2 ta LPS ta haifar da raw macrophages (IC50 = 38 μ M) Lokacin da aka kara tanshinone I da LPS a lokaci guda, fili ya hana 10-100 μ PGE2 samar da M (IC50 = 38 μM). Lokacin da aka ƙara bayan ƙaddamar da COX-2 cikakke, tanshinone na kuma rage yawan samar da PGE2 (IC50 = 46) μM). kai tsaye yana hana COX-2 ayyukan da / ko shafar Ayyukan PLA2. Lokacin da tanshinone an haɗa ni da nau'ikan nau'ikan phospholipase A2 (PLA2) daban-daban, yana hana sPLA2 sosai ta hanyar dogaro da hankali (IC50 = 11) μ M). iyawa, tanshinone na kuma hana cPLA2 (IC50 = 82) μ M）[1]

A cikin Nazarin Vivo:tanshinone Na nuna aikin anti-mai kumburi a cikin carrageenan induced paw edema da adjuvant induced arthritis a cikin berayen.Don kafa aikin anti-mai kumburi na tanshinone I, an yi amfani da nau'ikan dabbobi na gargajiya na m da kumburi mai tsanani [rat carrageenan (CGN) - haifar da paw edema da bera adjuvant amosanin gabbai (AIA)].Lokacin da tanshinone na baka na baka, ya nuna gagarumin aikin anti-mai kumburi a kan CGN da ke haifar da paw edema (hani 47% a 160 mg / kg), yayin da IC50 na indomethacin ya kasance 7.1 mg / kg.A cikin AIA, tanshinone na ba da 27% hana kumburi na sakandare a rana ta 18 a kashi na baki na 50 mg / kg / day, yayin da prednisolone (5 mg / kg / day) ya nuna ingantaccen hanawa (65%) [1]

Gwajin Kinase:a matsayin tushen PLA2, ɗan adam recombinant sPLA2 (nau'in IIA) an tsarkake shi daga ƙwayoyin CHO da aka canza tare da kwayoyin PLA2, kuma an samu zomo recombinant platelet cPLA2 ta hanyar bayyanarsa a cikin baculovirus.Daidaitaccen haɗin kai (200) μ 50) Ya ƙunshi 100 mm Tris HCl buffer (pH 9.0), 6 mM CaCl2 da 20 nmol na 1-acyl - [1-14C] - arachidonyl Sn glycerol phosphate ethanolamine (2000 CPM / nmol).Ko kuma babu tanshinone I. An fara amsa ta hanyar ƙara 50NG mai tsaftataccen spLA2 ko cPLA2.Bayan mintuna 20 a 37 ℃, an bincika fatty acid ɗin da aka samar.A ƙarƙashin waɗannan daidaitattun yanayi, kusan 10% na fatty acids ana fitar da su daga ƙarar phospholipid substrate a cikin cakuda amsa ba tare da tanshinone I [1].

Gwajin Kwayoyin Halitta:raw 264.7 Kwayoyin an al'ada tare da DMEM supplemented da 10% FBS da 1% maganin rigakafi a 37 ℃ karkashin 5% CO2.A takaice, an shuka sel akan faranti 96 (2) × 10 (sel 5 / rijiyar).Sai dai in an nuna in ba haka ba, LPS (1ug / ml) da tanshinone an ƙara ni kuma an shirya ni na awanni 24.An auna maida hankali na PGE2 a cikin matsakaici ta amfani da kit ɗin EIA don PGE2.Domin sanin tasirin tanshinone I akan samar da PGE 2 bayan shigar da COX-2, an haxa sel tare da LPS (1 μ G / ml) na sa'o'i 24 kuma an wanke su sosai.Sa'an nan, tanshinone an ƙara ni ba tare da LPS ba kuma an haɓaka sel na wasu sa'o'i 24.An auna maida hankali na PGE2 daga matsakaici.An yi amfani da gwajin MTT don bincika cytotoxicity na tanshinone I akan danyen sel.Tanshinone I a 100 μM bai nuna wani cytotoxicity ba [1].

Gwajin Dabbobi:don kimanta ayyukan hanawa na tanshinone I akan nau'ikan dabbobi masu mahimmanci da na yau da kullun, rat carrageenan (CGN) - haifar da paw edema da adjuvant induced arthritis (AIA) an yi amfani da su.A takaice, 1% CGN da aka narkar da shi a cikin salin kyauta na pyrogen (0.05 ml) an allura a cikin hannun dama na berayen don gwajin edema.Bayan sa'o'i 5, an auna kumburin farawar da aka yi amfani da su ta hanyar amfani da plethysmograph.Tanshinone na narkar da a cikin 0.5% CMC an gudanar da shi ta baki 1 hour kafin allurar CGN.Don gwajin AIA, kumburin jijiyoyi ya haifar da allurar Mycobacterium lactis (0.6ml / bera) wanda aka narkar da shi a cikin man ma'adinai a cikin hannun dama na berayen.Tanshinone ana gudanar da ni ta baki kowace rana.An auna faɗaɗa farawar da aka yi da magani da ba a kula da su ta amfani da plethysmograph.

Magana:[1] Kim SY, et al.Tasirin Tanshinone I ware daga Salvia miltiorrhiza bunge a kan arachidonic acid metabolism da kuma a cikin vivo mai kumburi martani.Phytother Res.2002 Nuwamba;16 (7): 616-20.