Screening of bioactive ingredients of Tsantan Sumtang in ameliorating H9c2 cells injury,Journal of Ethnopharmacology

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Screening of bioactive ingredients of Tsantan Sumtang in ameliorating H9c2 cells injury
Journal of Ethnopharmacology ( IF 4.8 ) Pub Date : 2021-11-19 , DOI: 10.1016/j.jep.2021.114854
Yi Zhou ₁ , Zhanqiang Li ₂ , Dejun Zhang ₁ , Benyin Zhang ₁

Affiliation

Ethnopharmacological relevance

Tsantan Sumtang (TS), a traditional Tibetan medicine, has been used in the clinic for the treatment of myocardial ischemia (MI) for ages, however, the bioactive ingredients that are responsible for improving MI remain unknown.

Aim of the study

This study investigated the chemical components of TS and their medicinal efficacies at cell levels, in order to expound the bioactive ingredients in TS.

Materials and methods

First, a response-surface methodology was employed to determine the optimum ethanol reflux extraction process of polyphenols in TS (PTS) due to their close correlation with MI improvement. Second, a serum pharmacochemistry technique was used to analyze the compounds of PTS absorbed into the blood of rats. Third, hypoxia-, H₂O₂-, and adriamycin (ADM)-induced H9c2 cell injury models were used to investigate the cardioprotective effects of these compounds in vitro. Fourth, protective effects of isovitexin, quercitrin, and isoeugenol on mitochondrial function were further tested.

Results

The optimum extraction conditions for obtaining PTS were an ethanol concentration of 78.22%, an extraction time of 67.4 min, and a material–liquid ratio of 1:72.60 mL/g. Serum pharmacochemistry analysis detected 21 compounds, of which 11 compounds were always present in the blood within 5 hours. Cytotoxicity and the protective effect of 11 compounds in hypoxia-, H₂O₂-, and ADM-induced H9c2 cell injury models shown that isovitexin, quercitrin, and isoeugenol had almost no cytotoxicity, and they could elevate the survival rate in injured H9c2 cells. Furthermore, isovitexin, quercitrin, and isoeugenol could decrease mitochondrial reactive oxygen species (ROS) releasion, inhibite mitochondrial permeability transition pore (mPTP) opening, ameliorate the change of mitochondrial membrane potential (MMP) to exert mitochondrial protection effect.

Conclusion

Isovitexin, quercitrin, and isoeugenol exhibited cardioprotective effect at cell levles, these three compounds might be the bioactive ingredients in TS. These findings elucidate the pharmacodynamic substances and mechanisms of TS, guiding its clinical use.

中文翻译：

参丹松汤改善H9c2细胞损伤的生物活性成分筛选

民族药理学相关性

藏药参丹松堂 (TS) 已在临床上用于治疗心肌缺血 (MI) 多年，然而，负责改善 MI 的生物活性成分仍然未知。

研究目的

本研究从细胞水平研究TS的化学成分及其药用功效，以阐明TS中的生物活性成分。

材料和方法

首先，采用响应面法确定 TS (PTS) 中多酚的最佳乙醇回流提取工艺，因为它们与 MI 改善密切相关。其次，使用血清药物化学技术分析吸收到大鼠血液中的PTS化合物。第三，使用缺氧、H ₂ O ₂和阿霉素 (ADM) 诱导的 H9c2 细胞损伤模型来研究这些化合物在体外的心脏保护作用。第四，进一步测试了异牡荆素、槲皮素和异丁香酚对线粒体功能的保护作用。

结果

获得PTS的最佳提取条件为乙醇浓度为78.22%、提取时间为67.4 min、料液比为1:72.60 mL/g。血清药化分析检测到21种化合物，其中11种化合物在5小时内始终存在于血液中。_{11种化合物在缺氧、H 2} O ₂中的细胞毒性及保护作用- 和 ADM 诱导的 H9c2 细胞损伤模型表明，异牡荆素、槲皮素和异丁香酚几乎没有细胞毒性，它们可以提高受损 H9c2 细胞的存活率。此外，异牡荆素、槲皮素和异丁香酚可降低线粒体活性氧（ROS）释放，抑制线粒体通透性转换孔（mPTP）开放，改善线粒体膜电位（MMP）变化，发挥线粒体保护作用。