School of Functional Food and Wine, Shenyang Pharmaceutical University, Shenyang 110016, China.
Molecules. 2022 Aug 19;27(16):5298. doi: 10.3390/molecules27165298.
Myocardial fibrosis (MF) is a common pathological feature of many heart diseases and seriously threatens the normal activity of the heart. Jiaogulan () tea is a functional food that is commercially available worldwide. Gypensapogenin I (Gyp I), which is a novel dammarane-type saponin, was obtained from the hydrolysates of total gypenosides. It has been reported to exert a beneficial anti-inflammatory effect. In our study, we attempted to investigate the efficiency and possible molecular mechanism of Gyp I in cardiac injury treatment induced by ISO. In vitro, Gyp I was found to increase the survival rate of H9c2 cells and inhibit apoptosis. Combined with molecular docking and Western blot analysis, Gyp I was confirmed to regulate the TLR4/NF-κB/NLRP3 signaling pathway. In vivo, C57BL6 mice were subcutaneously injected with 10 mg/kg ISO to induce heart failure. Mice were given a gavage of Gyp I (10, 20, or 40 mg/kg/d for three weeks). Pathological alterations, fibrosis-, inflammation-, and apoptosis-related molecules were examined. By means of cardiac function detection, biochemical index analysis, QRT-PCR monitoring, histopathological staining, immunohistochemistry, and Western blot analysis, it was elucidated that Gyp I could improve cardiac dysfunction, alleviate collagen deposition, and reduce myocardial fibrosis (MF). In summary, we reported for the first time that Gyp I showed good myocardial protective activity in vitro and in vivo, and its mechanism was related to the TLR4/NF-κB/NLRP3 signaling pathway.
心肌纤维化 (MF) 是许多心脏病的常见病理特征，严重威胁着心脏的正常活动。绞股蓝（）茶是一种在全球商业上可获得的功能性食品。吉潘萨苷元 I（Gyp I）是一种新型达玛烷型皂苷，从总皂苷的水解产物中获得。据报道，它具有有益的抗炎作用。在我们的研究中，我们试图研究 Gyp I 在 ISO 诱导的心肌损伤治疗中的效率和可能的分子机制。在体外，发现 Gyp I 可提高 H9c2 细胞的存活率并抑制细胞凋亡。结合分子对接和 Western blot 分析，证实 Gyp I 可调节 TLR4/NF-κB/NLRP3 信号通路。在体内，C57BL6 小鼠皮下注射 10 mg/kg ISO 诱导心力衰竭。给予 Gyp I（10、20 或 40 mg/kg/d，连续 3 周）灌胃。检查病理改变、纤维化、炎症和凋亡相关分子。通过心脏功能检测、生化指标分析、QRT-PCR 监测、组织病理学染色、免疫组化和 Western blot 分析，阐明 Gyp I 可改善心脏功能障碍、减轻胶原沉积和减少心肌纤维化 (MF)。总之，我们首次报道 Gyp I 在体外和体内均显示出良好的心肌保护活性，其机制与 TLR4/NF-κB/NLRP3 信号通路有关。
