Tanshinone IIA

Tanshinone IIA (Tan IIA) is one of the main compositions in the root of Salvia miltiorrhiza Bunge. Tanshinone IIA may suppress angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2. IC50 & Target:VEGF/VEGFR2^[1] In Vitro: The anti-tumor effect of Tanshinone IIA includes inhibiting tumor cell proliferation, disturbing tumor cell cycle, promoting tumor cell apoptosis, and inhibiting tumor cell invasion and transfer. Tanshinone IIA has anti-proliferative effects on A549 cells: the IC₅₀ of Tanshinone IIA after 24, 48 and 72 h are 145.3, 30.95 and 11.49 μM, respectively. The CCK-8 assay is used to evaluate the proliferative activity of A549 cells treated with Tanshinone IIA (2.5-80 μM) for 24, 48 and 72 h, respectively. The CCK-8 results show that Tanshinone IIA can significantly inhibit A549 cell proliferation in a dose- and time-dependent manner. Obvious apoptosis and cell growth inhibition of A549 cells are observed after drug treatment for 48 h (concentrations used are approximately IC₅₀ values: Tanshinone IIA 31 μM on A549). Western blotting finds that 48 h exposures to Tanshinone IIA (31 μM) in A549 cells, downregulates expression of VEGF and VEGFR2 protein in both drug treatment groups vs. vehicle^[1].
Tanshinone IIA, one of the most abundant constituents of the root of Salvia miltiorrhiza, protects rat myocardium-derived H9C2 cells against apoptosis. Treatment of H9C2 cells with Tanshinone IIA inhibits angiotensin II-induced apoptosis by downregulating the expression of PTEN (phosphatase and tensin homolog), a tumor suppressor that plays a critical role in apoptosis. Tanshinone IIA inhibits angiotensin II (AngII)-induced apoptosis by downregulating the expression of phosphatase and tensin homolog (PTEN)^[2].
Tanshinone IIA decreases the protein expression of EGFR, and IGFR blocking the PI3K/Akt/mTOR pathway in gastric carcinoma AGS cells^[3]. In Vivo: Tanshinone IIA (10 or 20 mg/kg; p.o) significantly reverses scopolamine-induced cognitive impairments^[1].
Tanshinone IIA (2, 4, 8 mg/kg; i.p.) mediated protective effects on the STZ-induced diabetic nephropathy may be associates with the reduced endoplasmic reticulum stress via attenuating PERK signaling activities^[2].
Tanshinone IIA (3 and 12 mg/kg; i.p.) significantly inhibits the growth of ectopic endometrium^[3].
Tanshinone IIA has been used interchangeably with Tanshinone IIA sulfonate sodium (HY-N1370) in some studies, but there are differences in water solubility, chemical structure, pharmacological activity and pharmacokinetics. When administering to animals, please prepare a solid dispersion or choose to use the sulfonate form of Tanshinone IIA sulfonate sodium (HY-N1370) with better water solubility^[4].