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Tanshinone I 是一種IIA型人重組 sPLA2 和兔重組 cPLA2 抑制劑,IC50 分別為 11 μM 和 82 μM。
生物活性
Tanshinone I is an inhibitor of type IIA human recombinant sPLA2 (IC50=11 μM) and rabbit recombinant cPLA2 (IC50=82 μM).
IC50 & Target
IC50: 11 μM (sPLA2), 82 μM (cPLA2)[1].
體外研究(In Vitro)
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)[1].
體內(nèi)研究(In Vivo)
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%)[1].
分子量:276.29
性狀:Solid
Formula:C18H12O3
CAS 號:568-73-0
中文名稱:丹參酮 I
運輸條件:Room temperature in continental US; may vary elsewhere.
儲存方式
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 2 mg/mL (7.24 mM; Need ultrasonic)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 3.6194 mL | 18.0969 mL | 36.1939 mL |
5 mM | 0.7239 mL | 3.6194 mL | 7.2388 mL |
10 mM | --- | --- | --- |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲存時,請在 6 個月內(nèi)使用,-20°C 儲存時,請在 1 個月內(nèi)使用。
參考文獻
[1]. Kim SY, et al. Effects of Tanshinone I isolated from Salvia miltiorrhiza bunge on arachidonic acid metabolism and in vivo inflammatory responses. Phytother Res. 2002 Nov;16(7):616-20. [Content Brief]
Tanshinone I 是一種IIA型人重組 sPLA2 和兔重組 cPLA2 抑制劑,IC50 分別為 11 μM 和 82 μM。
生物活性
Tanshinone I is an inhibitor of type IIA human recombinant sPLA2 (IC50=11 μM) and rabbit recombinant cPLA2 (IC50=82 μM).
IC50 & Target
IC50: 11 μM (sPLA2), 82 μM (cPLA2)[1].
體外研究(In Vitro)
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)[1].
體內(nèi)研究(In Vivo)
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%)[1].
分子量:276.29
性狀:Solid
Formula:C18H12O3
CAS 號:568-73-0
中文名稱:丹參酮 I
運輸條件:Room temperature in continental US; may vary elsewhere.
儲存方式
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 2 mg/mL (7.24 mM; Need ultrasonic)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 3.6194 mL | 18.0969 mL | 36.1939 mL |
5 mM | 0.7239 mL | 3.6194 mL | 7.2388 mL |
10 mM | --- | --- | --- |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲存時,請在 6 個月內(nèi)使用,-20°C 儲存時,請在 1 個月內(nèi)使用。
參考文獻
[1]. Kim SY, et al. Effects of Tanshinone I isolated from Salvia miltiorrhiza bunge on arachidonic acid metabolism and in vivo inflammatory responses. Phytother Res. 2002 Nov;16(7):616-20. [Content Brief]