Miltirone

Miltirone is a tanshinone that has been found in S. miltiorrhiza and has diverse biological activities.^1,2,3,4,5 It protects lard from thermal oxidation when used at a concentration of 0.02%.¹ Miltirone is a partial agonist of the benzodiazepine receptor (IC₅₀ = 0.3 µM).² It inhibits carboxylesterase 2 (CES2; K_i = 0.04 µM) as well as severe acute respiratory syndrome coronavirus (SARS-CoV) main protease (M^pro), also known as 3C-like protease (3CL^pro), and papain-like protease (PL^pro; IC₅₀s = 21.1 and 30 µM, respectively).^3,4 Miltirone is cytotoxic to HCT116 colon cancer cells (IC₅₀ = 4.27 µM) and induces mitochondrial dysfunction and the production of reactive oxygen species (ROS) in the same cells.⁵ In vivo, miltirone (10-60 mg/kg) increases the number of punished crossings in the four-plate test, indicating tranquilizing activity, in mice.²

WARNING This product is not for human or veterinary use.

1. Houlihan, C.M., Ho, C.-T., and Chang, S.S. The structure of rosmariquinone - A new antioxidant isolated from Rosmarinus officinalis L. JAOCS 62(1), 96-98 (1985).

2. Lee, C.-M., Wong, H.N.C., Chui, K.-Y., et al. Miltirone, a central benzodiazepine receptor partial agonist from a Chinese medicinal herb Salvia miltiorrhiza. Neurosci. Lett. 127(2), 237-241 (1991).

3. Hatfield, J.M., Tsurkan, L.G., Hyatt, J.L., et al. Modulation of esterified drug metabolism by tanshinones from Salvia miltiorrhiza ("Danshen"). J. Nat. Prod. 76(1), 36-44 (2012).

4. Park, J.-Y., Kim, J.H., Kim, Y.M., et al. Tanshinones as selective and slow-binding inhibitors for SARS-CoV cysteine proteases. Bioorg. Med. Chem. 20(19), 5928-5935 (2012).

5. Wang, L., Hu, T., Shen, J., et al. Miltirone induced mitochondrial dysfunction and ROS-dependent apoptosis in colon cancer cells. Life Sci. 151, 224-234 (2016).