State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, China.
College of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, China.
Pharm Biol. 2021 Dec;59(1):242-251. doi: 10.1080/13880209.2020.1870506.
Naoxintong capsule (NXT) is one of the most prevalent Traditional Chinese Medicine formulations in the treatment of coronary heart disease (CHD), yet the action of pharmacodynamic components remains unclear.
To determine the basis by which pharmacodynamic components of NXT may be effective in the treatment of CHD.
The protective effect of NXT (0.01-100 μg/mL) on 293 T and hy926 cells was determined by MTT assay for 24 h. Afterwards, to investigate the pharmacodynamic material basis of NXT in anti-inflammatory and antioxidant effects, based on previous UPLC/Q-TOF analysis, 293 T and hy926 cells were divided into control (treated with solvent), model (incubated with TNF-α, LPS or HO), intervention (treated with UPLC components) and positive groups. After 24 h of treatment, all cells were tested to verify the screening results. MOE software was applied to dock bioactive compounds with phosphoinositide 3-kinase (PI3K), then the protein expression and phosphate levels were determined by western blotting.
NXT could significantly inhibit the expression of NF-κB, MMP-9 and NO in cells with IC values of 0.1178, 0.1182 and 0.1094 μg/mL. Based on the screening results, six components of NXT were identified (calycosin, ferulic acid, salvianolic acid B, ononin, salvianolic acid E, and salvianolic acid F) which can inhibit NF-κB, MMP-9, and NO simultaneously, while exerting cytoprotective effects by inhibiting the activation of the PI3K/AKT pathway under different conditions by virtue of their advantageous interaction with PI3K.
These ingredients have outstanding therapeutic potential and may provide a scientific basis for the future application and research of NXT.
脉络宁胶囊（NXT）是治疗冠心病（CHD）最常用的中药方剂之一，但药效成分的作用尚不清楚。
确定 NXT 的药效成分在治疗 CHD 中的作用基础。
采用 MTT 法测定 NXT（0.01-100μg/mL）对 293T 和 hy926 细胞的保护作用 24h。之后，为了研究 NXT 在抗炎和抗氧化作用中的药效物质基础，基于之前的 UPLC/Q-TOF 分析，将 293T 和 hy926 细胞分为对照组（用溶剂处理）、模型组（用 TNF-α、LPS 或 HO 孵育）、干预组（用 UPLC 成分处理）和阳性组。处理 24h 后，所有细胞均进行测试以验证筛选结果。MOE 软件用于将生物活性化合物与磷酸肌醇 3-激酶（PI3K）对接，然后通过 Western blot 测定蛋白表达和磷酸化水平。
NXT 能显著抑制细胞中 NF-κB、MMP-9 和 NO 的表达，IC 值分别为 0.1178、0.1182 和 0.1094μg/mL。基于筛选结果，鉴定出 NXT 的六种成分（毛蕊异黄酮、阿魏酸、丹酚酸 B、芒柄花苷、丹酚酸 E 和丹酚酸 F），这些成分可同时抑制 NF-κB、MMP-9 和 NO，同时通过与 PI3K 的有利相互作用，在不同条件下抑制 PI3K/AKT 通路的激活，发挥细胞保护作用。
这些成分具有突出的治疗潜力，可为 NXT 的未来应用和研究提供科学依据。
