Cryptotanshinone was originally isolated from the dried roots of Salvia militorrhiza, an herb that is used extensively in Asian medicine and that is known to exert beneficial effects on the circulatory system.Cryptotanshinone rapidly inhibited STAT3 Tyr705 phosphorylation in DU145 prostate cancer cells and the growth of the cells through 96 hours of the treatment.Cryptotanshinone significantly attenuated atherosclerotic plaque formation and enhanced plaque stability in ApoE-/- mice by inhibiting lectin-like oxLDL receptor-1 (LOX-1) and matrix metalloproteinase-9 (MMP-9) expression, as well as inhibiting reactive oxygen species (ROS) generation and nuclear factor- kappa B (NF-κB) activation.In vitro,Cryptotanshinone decreased oxLDL-induced LOX-1 mRNA and protein expression, and thereby, inhibited LOX-1-mediated monocytes adhesion to HUVECs through reducing the expression of adhesion molecules (ICAM-1 and VCAM-1).Cryptotanshinone inhibited NADPH oxidase subunit 4 (NOX4)-mediated ROS generation and consequent activation of NF-κB in HUVECs.
|Cell lines||KATO III, DU145, PC3, LNCaP, MDA-MB-231, MDA-MB-468, MDA-MB-453, MCF-7, MCF-10A, HeLa and HCT-116|
|Preparation method||Exposing cells to Cryptotanshinone for 24 or 48 hours. For the determination of cell proliferation, adding the cell proliferation reagent WST-1 and using an ELISA reader to measure WST-1 formazan quantitatively at 450 nm.|
|Concentrations||Dissolved in DMSO, final concentrations ~50 μM|
|Incubation time||24 or 48 hours|
|Animal models||Zucker Diabetic Fatty (ZDF) (male) type 2 diabetic rat, ob/ob mice (C57BL/6J-Lepob), db/db mice (C57BL/KsJ-Leprdb) and male C57BL/6J mice with high-fat diet-induced obesity|
|Formulation||Dissolved in 0.1% solution of sodium lauryl sulfate|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Cryptotanshinone, an orally bioactive herbal compound from Danshen, attenuates atherosclerosis in Apolipoprotein E-Deficient Mice: role of LOX-1.
Liu Z, et al. Br J Pharmacol. 2015 Jan 9. PMID: 25572313.
Cryptotanshinone inhibits constitutive signal transducer and activator of transcription 3 function through blocking the dimerization in DU145 prostate cancer cells.
Shin DS, et al. Cancer Res. 2009 Jan 1;69(1):193-202. PMID: 19118003.
Antidiabetes and antiobesity effect of cryptotanshinone via activation of AMP-activated protein kinase.
Kim EJ, et al. Mol Pharmacol. 2007 Jul;72(1):62-72. PMID: 17429005.
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