Tanshinone I is an inhibitor of type IIA human recombinantsPLA₂(IC₅₀=11 μM) and rabbit recombinantcPLA₂(IC₅₀=82 μM).

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

Tanshinone I inhibits PGE₂formation 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 PLA₂activity. 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].

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 IC₅₀of 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].

276.29

Solid

C₁₈H₁₂O₃

568-73-0

丹参酮 I

• Terpenoids
• Diterpenoids

• Plants
• Compositae
• Hemistepta lyrata

• Plants
• Labiatae

Room temperature in continental US; may vary elsewhere.

DMSO : 2 mg/mL(7.24 mM;Need ultrasonic)

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