Tanshinone I (Tanshinone A), an active principle isolated from the herbal medicine Salvia miltiorrhiza, displays cytotoxicity against tumor cells.

PLA2:11 μM

Tanshinone I在大鼠肉胶原（CGN）诱导的爪肿胀和大鼠佐剂诱导性关节炎（AIA）模型中展示了抗炎活性，这些模型是研究急性和慢性炎症的经典动物模型。口服Tanshinone I对CGN诱导的爪肿胀表现出显著的抗炎活性（160 mg/kg时，抑制率为47%），而indomethacin的IC50为7.1 mg/kg。在AIA模型中，Tanshinone I以每日口服50 mg/kg的剂量，在第18天抑制二次炎炎症27%，而prednisolone（每日5 mg/kg）展现出更强的抑制效果（65%）[1]。

As sources of PLA2, human recombinant sPLA2 (type IIA) is purified from CHO cells transfected with the PLA2 gene and rabbit recombinant platelet cPLA2 is obtained through its expression in baculovirus. The standard reaction mixture (200 μL) contained 100 mM Tris-HCl buffer (pH 9.0) with 6 mM CaCl2 and 20 nmol 1-acyl-[1-14C]-arachidonyl-sn-glycerophosphoethanolamine (2000 cpm/nmol) in the presence or absence of Tanshinone I. The reaction is started by adding 50 ng purified sPLA2 or cPLA2. After 20 min at 37°C, the free fatty acid generated is analysed. Under these standard conditions, the reaction mixture in the absence of Tanshinone I released approximately 10% of free fatty acid from the phospholipid substrate added[1].

RAW 264.7 cells are cultured with DMEM supplemented with 10% FBS and 1% antibiotics under 5% CO2 at 37°C. Briefly, cells are plated in 96-well plates (2×105 cells/well). LPS (1 ug/mL) and Tanshinone I are simultaneously added and incubated for 24 h, unless otherwise specified. The PGE2 concentration in the medium is measured using an EIA kit for PGE2. In order to determine the effects of Tanshinone I on PGE2 production after induction of COX-2, cells are incubated with LPS (1 ug/mL) for 24 h and thoroughly washed. Then, Tanshinone I is added without LPS and the cells are incubated for another 24 h. From the medium, PGE2 concentrations are measured. The cytotoxicity of Tanshinone I to RAW cells is checked using the MTT assay. Tanshinone I does not show any cytotoxicity up to 100 uM[1].