Dihydrotanshinone I (DHTS) is a natural compound extracted from Salvia miltiorrhiza Bunge used for treating of cardiovascular diseases.

DHT (10 nM) 在脂多糖 (LPS) 刺激的人脐静脉内皮细胞 (HUVECs) 中，降低了类讲夹蛋白型氧化低密度脂蛋白受体-1 (LOX-1) 和 NADPH 氧化酶 4 (NOX4) 的表达，减少了活性氧 (ROS) 的产生、NF-κB 核转移、氧化低密度脂蛋白的内吞作用以及单核细胞的黏附[1]。Dihydrotanshinone I 诱导 HCT116 细胞中的caspase依赖性凋亡。Dihydrotanshinone I 的凋亡诱导作用随浓度和 ROS 的增加而增强。Z-VAD-fmk 完全阻止了Dihydrotanshinone I 诱导的凋亡。Z-LEHD-fmk 的预处理显著抑制了Dihydrotanshinone I 诱导的凋亡，但 Z-IETD-fmk 只能部分抑制。caspase-2 的基因敲低显著增加了Dihydrotanshinone I 诱导的凋亡[3]。

在ApoE-/-小鼠中，接受高脂饮食的同时，DHT (10 和 25 mg kg-1) 显著减缓动脉粥样硬化斑块形成，改善血清脂质谱，降低氧化应激，并缩小坏死核心区域。DHT 显著抑制主动脉中LOX-1、NOX4 和 NF-κB 的表达增强[1]。Dihydrotanshinone I（1, 2, 4 mg/kg）治疗能改善心脏功能，减小梗塞面积，缓解心肌酶谱和组织病理学紊乱，降低20-HETE生成，并调控心肌缺血-再灌注大鼠中与凋亡相关的蛋白表达[2]。

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.