生物活性
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.
化学数据
分子量 | 296.36 |
分子式 | C19H20O3 |
CAS号 | 35825-57-1 |
纯度 | >98% |
溶解性(25°C) | DMSO 3 mg/mL |
储存和运输条件 | 固体粉末: -20°C 冷藏长期储存 常温运输及临时存放 |
实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验 |
---|
细胞系 | KATO III, DU145, PC3, LNCaP, MDA-MB-231, MDA-MB-468, MDA-MB-453, MCF-7, MCF-10A, HeLa and HCT-116 |
方法 | 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. |
浓度 | Dissolved in DMSO, final concentrations ~50 μM |
处理时间 | 24 or 48 hours |
动物实验 |
---|
动物模型 | 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 |
配制 | Dissolved in 0.1% solution of sodium lauryl sulfate |
剂量 | ~600 mg/kg/day |
给药处理 | Orally |
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 3.3743 mL | 16.8714 mL | 33.7427 mL |
5 mM | 0.6749 mL | 3.3743 mL | 6.7485 mL |
10 mM | 0.3374 mL | 1.6871 mL | 3.3743 mL |