Nā huahana

wehewehe:ʻO tanshinone I kahi ʻano IIA kanaka recombinant sPLA2 a me Rabbit Recombinant cPLA2 inhibitor me IC50 o 11 mau μM a me 82 μM.

Māhele pili:nā ala hōʻailona > > metabolic enzymes /
protease > > phospholipids
Kahua noiʻi > > maʻi naʻau
Nā Huahana Kūlohelohe > > Quinones

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

Haʻawina In Vitro:tanshinone I keakea i ka hookumuia ana o PGE2 e LPS i hoʻokomo 'ia maka macrophages (IC50 = 38 μ M）。 I ka tanshinone I a me LPS i hoʻohui 'ia i ka manawa like, ka pūhui i hoʻopale nui 10-100 μ PGE2 hana o M (IC50 = 38 μ M. ）。 Ke hoʻohui ʻia ma hope o ka hoʻokomo piha ʻana o COX-2, ua hoʻemi pū ʻo tanshinone I ka hana ʻana o PGE2 (IC50 = 46) μ M）。 ʻO ka ʻoiaʻiʻo o ka tanshinone I keakea i ka hana PGE 2 ma o ka COX-2 i hoʻokomo mua ʻia e hōʻike ikaika ana e hiki i ka hui. pale pololei i ka hana COX-2 a / a pili paha i ka hana PLA2. I ka wā i hoʻokomo ʻia ai au me nā ʻano like ʻole o phospholipase A2 (PLA2) i ka tanshinone. ka ikaika, tanshinone I hoʻopaʻa pū i ka cPLA2 (IC50 = 82) μ M） [1]

Ma ke aʻo ʻana ma Vivo:tanshinone Ua hōʻike au i ka hana anti-inflammatory ma ka carrageenan i hoʻokomo ʻia i ka paw edema a me ka adjuvant induced arthritis i nā ʻiole.No ka hoʻokumu ʻana i ka hana anti-inflammatory o tanshinone I, ua hoʻohana ʻia nā ʻano holoholona maʻamau o ka maʻi ʻeha a me ka maʻi mau [rat carrageenan (CGN) - induced paw edema a me rat adjuvant induced arthritis (AIA)].I ka waha o ka tanshinone I, ua hōʻike i ka hana anti-inflammatory koʻikoʻi e kū'ē i ka CGN i hoʻokomo ʻia i ka paw edema (47% inhibition ma 160 mg / kg), ʻoiai ʻo ka IC50 o indomethacin he 7.1 mg / kg.I ka AIA, tanshinone au i hāʻawi i 27% inhibition o ka lua o ka mumū i ka lā 18 ma ka waha waha o 50 mg / kg / lā, aʻo prednisolone (5 mg / kg / lā) hōʻike i ka inhibition maikaʻi (65%) [1]

Hoʻokolohua Kinase:e like me ke kumu o PLA2, kanaka recombinant sPLA2 (type IIA) ua hoʻomaʻemaʻeʻia mai CHO pūnaewele transfected me PLA2 gene, a rabbit recombinant platelet cPLA2 i loaʻa ma o kona hoike ana i ka baculovirus.ʻO ka hui ʻana o ka hopena maʻamau (200) μ 50) Loaʻa iā 100 mm Tris HCl buffer (pH 9.0), 6 mM CaCl2 a me 20 nmol o 1-acyl - [1-14C] - arachidonyl Sn glycerol phosphate ethanolamine (2000 CPM / nmol).A i ʻole ʻaʻohe tanshinone I. ua hoʻomaka ʻia ka pane ma ka hoʻohui ʻana i ka 50NG hoʻomaʻemaʻe sPLA2 a i ʻole cPLA2.Ma hope o 20 mau minuke ma 37 ℃, ua kālailai ʻia nā ʻakika momona manuahi.Ma lalo o kēia mau kūlana maʻamau, ma kahi o 10% o nā ʻakika momona manuahi e hoʻokuʻu ʻia mai ka substrate phospholipid i hoʻohui ʻia i ka hui ʻana me ka tanshinone I [1].

ʻO ka hoʻokolohua kelepona:264.7 mau pūnaewele maka i hoʻoulu ʻia me DMEM i hoʻohui ʻia me 10% FBS a me 1% mau lāʻau antibiotic ma 37 ℃ ma lalo o 5% CO2.I ka pōkole, ua kanu ʻia nā cell ma 96 mau papa punawai (2) × 10 (5 cell / well).Inā ʻaʻole i hōʻike ʻia, ua hoʻohui ʻia ʻo LPS (1ug / ml) a me tanshinone I a hoʻokomo ʻia no 24 mau hola.Ua ana ʻia ka manaʻo PGE2 i loko o ke kikowaena me ka hoʻohana ʻana i ka pahu EIA no PGE2.I mea e hoʻoholo ai i ka hopena o ka tanshinone I ma ka hana PGE 2 ma hope o ka hoʻokomo ʻana o COX-2, ua hui pū ʻia nā cell me LPS (1 μG / ml) no 24 mau hola a holoi pono.A laila, hoʻohui ʻia ʻo tanshinone me ka ʻole o LPS a ua hoʻomaʻamaʻa ʻia nā cell no nā hola 24 ʻē aʻe.Ua ana ʻia ka manaʻo PGE2 mai ka waena.Ua hoʻohana ʻia ka MTT assay no ka nānā ʻana i ka cytotoxicity o tanshinone I ma nā cell maka.ʻAʻole hōʻike ʻo Tanshinone I ma 100 μM i kekahi cytotoxicity [1].

Hoʻokolohua holoholona:no ka loiloi ʻana i ka hana hoʻopaʻa ʻana o tanshinone I ma nā ʻano holoholona inflammatory acute a me ka maʻi, ua hoʻohana ʻia nā ʻano hoʻohālike ʻo carrageenan (CGN) - induced paw edema a me adjuvant induced arthritis (AIA).I ka pōkole, 1% CGN i hoʻoheheʻe ʻia i ka pyrogen free saline (0.05 ml) ua hoʻokomo ʻia i ka wāwae hope ʻākau o nā ʻiole no ka hoʻāʻo ʻana i ka edema paw.Ma hope o 5 mau hola, ua ana ʻia ka pehu o nā maiuu i mālama ʻia me ka plethysmograph.ʻO Tanshinone aʻu i hoʻoheheʻe ʻia i ka 0.5% CMC i lawelawe waha ʻia 1 hola ma mua o ka hoʻokomo ʻana iā CGN.No ka ho'āʻo AIA, ua hoʻoulu ʻia ka ʻāʻana o ka maʻi ʻāʻī ma ka hoʻokomo ʻana i ka Mycobacterium lactis (0.6ml / ʻiole) i hoʻoheheʻe ʻia i loko o ka ʻaila mineral i loko o ka wāwae hope ʻākau o nā ʻiole.Hāʻawi waha ʻia au i ka Tanshinone i kēlā me kēia lā.Ua ana ʻia ka hoʻonui ʻana o nā maiuu i mālama ʻia a mālama ʻole ʻia me ka plethysmograph.

Kuhikuhi:[1] Kim SY, et al.Nā hopena o Tanshinone I hoʻokaʻawale ʻia mai Salvia miltiorrhiza bunge ma ka arachidonic acid metabolism a me nā pane inflammatory vivo.ʻO Phytother Res.2002 Nov;16(7):616-20.