Tanshinone ICAS号: 568-73-0分子式: C18H12O3分子量: 276.29描述纯度储存/保存方法别名外观可溶性/溶解性In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
Tanshinone I is an inhibitor of type IIA human recombinant sPLA2 (IC50=11 μM) and rabbit recombinant cPLA2 (IC50=82 μM).
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纯度 |
>98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
丹参酮I ;Tanshinone A
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外观 |
red powder
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可溶性/溶解性 |
DMSO : 2.5 mg/mL (9.05 mM; Need ultrasonic)
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生物活性 | |
In vitro(体外研究) |
Tanshinone I inhibits PGE2 formation from LPS-induced RAW macrophages (IC50=38 μM). When Tanshinone I is added simultaneously with LPS, this compound clearly inhibits PGE2 production (IC50=38 μM) at 10-100 μM. Tanshinone I also reduces PGE2 production (IC50=46 μM) when added after COX-2 is fully induced. The fact that Tanshinone I inhibits PGE2 production by pre-induced COX-2 strongly suggests that this compound may directly inhibit COX-2 activity and/or affect PLA2 activity. When Tanshinone I is incubated with two different forms of phospholipase A2 (PLA2), it clearly inhibits sPLA2 (IC50=11 μM) in a concentration-dependent manner. Although being less potent, Tanshinone I also inhibits cPLA2 (IC50=82 μM).
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In vivo(体内研究) |
Tanshinone I shows antiinflammatory activity in rat carrageenan-induced paw oedema and adjuvant-induced arthritis. In order to establish the anti-inflammatory activity of Tanshinone I, the classical animal models of acute and chronic inflammation [rat carrageenan (CGN)-induced paw oedema and rat adjuvant-induced arthritis (AIA)] are employed. When Tanshinone I is orally administered, it shows significant anti-inflammatory activity against CGN-induced paw oedema (47% inhibition at 160 mg/kg), while the IC50 of indomethacin is 7.1 mg/kg. In AIA, Tanshinone I gives 27% inhibition of secondary inflammation at 18 day with an oral dose of 50 mg/kg/day, whereas prednisolone (5 mg/kg/day) shows potent inhibition (65%).
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分子结构图