Dihydrotanshinone I 是从丹参中分离到的一种天然产物,可抑制 MERS-CoV,可研究心血管疾病。
产品描述
Dihydrotanshinone I is a natural compound extracted from Salvia miltiorrhiza Bunge used for treating of cardiovascular diseases.
体外活性
DHT (10 nM) decreases lectin-like ox-LDL receptor-1 (LOX-1) and NADPH oxidase 4 (NOX4) expression, reactive oxygen species (ROS) production, NF-κB nuclear translocation, ox-LDL endocytosis and monocytes adhesion in lipopolysaccharide (LPS)-stimulated human umbilical vein endothelial cells (HUVECs)[1]. Dihydrotanshinone I induces caspase-dependent apoptosis induced in HCT116 cells. Dihydrotanshinone I induces concentration and ROS dependent caspase activation. Apoptosis induced by Dihydrotanshinone I is completely prevented by Z-VAD-fmk. Apoptosis induced by Dihydrotanshinone I is significantly inhibited by pretreatment of Z-LEHD-fmk but only is partially inhibited by Z-IETD-fmk. Apoptosis induced by Dihydrotanshinone I is significantly increased by caspase-2 knockdown[3].
体内活性
In ApoE-/- mice fed with an atherogenic diet, DHT (10 and 25 mg kg-1) significantly attenuated atherosclerotic plaque formation, altered serum lipid profile, decreased oxidative stress and shrunk necrotic core areas. DHT dramatically inhibits the enhanced expression of LOX-1, NOX4, and NF-κB in aorta[1]. Dihydrotanshinone I (1, 2, 4 mg/kg) treatment can improve cardiac function, reduce infarct size, ameliorate the variations in myocardial zymogram and histopathological disorders, decrease 20-HETE generation, and regulate apoptosis-related protein in myocardial ischemia-reperfusion rats[2].
激酶实验
Cells are treated with various concentrations of Dihydrotanshinone I (3.13-20 μM) for 48 h. For the activity assay, Ac-DEVD-AMC (1 μg/μL), Ac-IETD-AMC (1 μg/μL) or Ac-LEDH-AMC (1 μg/μL) and cell lysate are added into Protease Assay Buffer in 96-well plate. Reaction mixtures with lysis buffer are used as negative controls. Cells treated with DMSO (0.1%) are treated as vehicle control. The reaction mixtures are incubated for 1 h at 37°C. The AMC liberated from the substrates is measured using spectrofluorometer of Victor 2 plate reader with an excitation wavelength of 380 nm and an emission wavelength of 430 nm.
Cas No.
87205-99-0
分子式
C18H14O3
分子量
278.307
别名
二氢丹参酮I;15,16-dihydrotanshinone I;二氢丹参酮 I;DHTS
储存和溶解度
DMSO:35.9 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years