Cryptotanshinone

Biological Activity

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.

Product Citations

• 

  Front Immunol . 2022 Feb 7;13:820685.

  The Study on the Regulation of Th Cells by Mesenchymal Stem Cells Through the JAK-STAT Signaling Pathway to Protect Naturally Aged Sepsis Model Rats
  Cryptotanshinone purchased from AbMole

• 

  Research Square. 2020 Feb 13.

  STAT3 signaling pathway could be involved in the progress of cognitive dysfunction caused by ligature-induced periodontitis
  Cryptotanshinone purchased from AbMole

• 

  Acta Pharmacol Sin. 2019 Dec 17.

  Acid sphingomyelinase downregulation alleviates vascular endothelial leptin resistance in rats.
  Cryptotanshinone purchased from AbMole

Customer Product Validations & Biological Datas

	Source	Customer experimental result (2018).
	Method	Western blot & Cell viability assay
	Cell Lines
	Concentrations	20 μmol/L
	Incubation Time	48 h
	Results	After treatment with STAT3 inhibitor cryptotanshinone (20 μmol/L) for 48 h, the expression of p-STAT3 and STAT3 was detected by Western blot. Effect on cell viability at 48 h of the STAT3 inhibitor cryptotanshinone is shown on the right.

Protocol (for reference only)

Cell Experiment
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 Experiment
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
Dosages	~600 mg/kg/day
Administration	Orally

Chemical Information

Molecular Weight	296.36
Formula	C19H20O3
CAS Number	35825-57-1
Solubility (25°C)	DMSO 3 mg/mL
Storage	Powder          -20°C   3 years ;  4°C   2 years In solvent       -80°C   6 months ;  -20°C   1 month

Conversion of different model animals based on BSA (PMID: 27057123)

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Liu Z, et al. Br J Pharmacol. Cryptotanshinone, an orally bioactive herbal compound from Danshen, attenuates atherosclerosis in Apolipoprotein E-Deficient Mice: role of LOX-1.

[2] Shin DS, et al. Cancer Res. Cryptotanshinone inhibits constitutive signal transducer and activator of transcription 3 function through blocking the dimerization in DU145 prostate cancer cells.

[3] Kim EJ, et al. Mol Pharmacol. Antidiabetes and antiobesity effect of cryptotanshinone via activation of AMP-activated protein kinase.