Xinjiang Institute of Materia Medica, Urumqi, China.
Pharm Biol. 2013 Jan;51(1):74-83. doi: 10.3109/13880209.2012.711839. Epub 2012 Oct 4.
Dracocephalum moldavica Linn (Labiatae) is one of the ethnomedicinal drugs of Uygur in Xinjiang, China. This herb is mainly used in treating cardiovascular diseases, such as atherosclerosis. However, the mechanism of pharmacological activity of D. moldavica has been poorly studied.
To explore the pharmacological mechanism of D. moldavica in treating atherosclerosis by investigating the effects of total flavonoids from the aerial portion of D. moldavica on rat vascular smooth muscle cells (VSMCs).
The proliferation and migration of VSMCs were evaluated via a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay and transwell chamber experiment, respectively. The expression of proliferating cell nuclear antigen (PCNA), nuclear factor κB p65 (NF-κB p65), intercellular adhesion molecule-1 (ICAM-1), and vascular cell adhesion molecule-1 (VCAM-1) of VSMCs was determined using immunohistochemistry staining and quantitative real-time PCR (qRT-PCR).
Total flavonoids (IC(50) = 145.63 μg/mL) significantly inhibited tumor necrosis factor-α (TNF-α) induced VSMC proliferation at concentrations of 25, 50, and 100 μg/mL. Treatment with 50 and 100 μg/mL of total flavonoids also significantly inhibited TNF-α-induced VSMC migration, whereas 25 μg/mL of total flavonoids did not elicit any significant inhibitory effect. In addition, the effects of total flavonoids on inflammatory molecule expression of cells were tested by immunohistochemistry staining, showing that TNF-α-induced expression of PCNA, NF-κB p65, ICAM-1, and VCAM-1 in VSMCs was dose-dependently suppressed by total flavonoids. Furthermore, qRT-PCR data confirmed the inhibition of mRNA expressions of these inflammatory molecules.
These data suggest that total flavonoids from D. moldavica exhibit anti-inflammatory activities, which is probably one of the underlying mechanisms of D. moldavica for clinical treatment of atherosclerosis.
Dracocephalum moldavica Linn（唇形科）是中国新疆维吾尔族民间药物之一。该草药主要用于治疗心血管疾病，如动脉粥样硬化。然而，D. moldavica 的药理活性机制研究甚少。
通过研究 D. moldavica 地上部分总黄酮对大鼠血管平滑肌细胞（VSMCs）的作用，探讨 D. moldavica 治疗动脉粥样硬化的药理机制。
通过 3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐（MTT）测定和 Transwell 室实验分别评估 VSMCs 的增殖和迁移。采用免疫组织化学染色和实时定量 PCR（qRT-PCR）检测 VSMCs 增殖细胞核抗原（PCNA）、核因子 κB p65（NF-κB p65）、细胞间黏附分子-1（ICAM-1）和血管细胞黏附分子-1（VCAM-1）的表达。
总黄酮（IC（50）=145.63μg/ml）在 25、50 和 100μg/ml 浓度下显著抑制肿瘤坏死因子-α（TNF-α）诱导的 VSMC 增殖。50 和 100μg/ml 的总黄酮也显著抑制 TNF-α诱导的 VSMC 迁移，而 25μg/ml 的总黄酮则没有明显的抑制作用。此外，通过免疫组织化学染色测试了总黄酮对细胞内炎症分子表达的影响，结果表明，TNF-α诱导的 VSMCs 中 PCNA、NF-κB p65、ICAM-1 和 VCAM-1 的表达被总黄酮呈剂量依赖性抑制。此外，qRT-PCR 数据证实了这些炎症分子的 mRNA 表达受到抑制。
这些数据表明，D. moldavica 中的总黄酮具有抗炎活性，这可能是 D. moldavica 临床治疗动脉粥样硬化的机制之一。
