College of Pharmacy, Keimyung University, 1095 Dalgubeol-daero, Daegu 42601, Korea.
Molecules. 2021 Apr 6;26(7):2092. doi: 10.3390/molecules26072092.
Periodontitis is a set of chronic inflammatory diseases caused by the accumulation of Gram-negative bacteria on teeth, resulting in gingivitis, pocket formation, alveolar bone loss, tissue destruction, and tooth loss. In this study, the contents of ginsenosides isolated from fruit extract were quantitatively analyzed, and the anti-inflammatory effects were evaluated in human periodontal ligament cells. The major ginsenosides, Re, Ra8, and Rf, present in ginseng fruit were simultaneously analyzed by a validated method using high-performance liquid chromatography with a diode-array detector; Re, Ra8, and Rf content per 1 g of fruit extract was 1.01 ± 0.03, 0.33 ± 0.01, and 0.55 ± 0.04 mg, respectively. Ginsenosides-Re, -Ra8, and -Rf inhibited the production of pro-inflammatory factors and the expression of important cytokines in periodontitis by inducing the expression of heme oxygenase 1 (HO-1), promoting osteoblast differentiation of periodontal ligament cells, suppressing alveolar bone loss, and promoting the expression of osteoblast-specific genes, such as , , and . An inhibitory effect of these ginsenosides on periodontitis and alveolar bone loss was observed via the regulation of HO-1 and subsequent epidermal growth factor receptor (EGFR) signaling. Silencing EGFR with EGFR siRNA confirmed that the effect of ginsenosides on HO-1 is mediated by EGFR. In conclusion, this study evaluated the contents of ginsenosides-Re, -Ra8, and -Rf isolated from fruit extract. Therefore, these results provide important basic data for future fruit component studies and suggest that ginsenosides Re, Ra8, and Rf have potential as future treatment options for periodontitis.
牙周炎是一组由牙齿上革兰氏阴性菌积累引起的慢性炎症性疾病，导致牙龈炎、袋形成、牙槽骨丧失、组织破坏和牙齿脱落。在这项研究中，定量分析了从人参果中分离的人参皂苷的含量，并在人牙周膜细胞中评价了其抗炎作用。采用高效液相色谱-二极管阵列检测器验证方法，同时分析了人参果中存在的主要人参皂苷 Re、Ra8 和 Rf；每 1 g 人参果提取物中 Re、Ra8 和 Rf 的含量分别为 1.01 ± 0.03、0.33 ± 0.01 和 0.55 ± 0.04 mg。人参皂苷 Re、Ra8 和 Rf 通过诱导血红素加氧酶 1（HO-1）的表达，抑制牙周炎中促炎因子的产生和重要细胞因子的表达，促进牙周膜细胞成骨分化，抑制牙槽骨丢失，促进成骨特异性基因如、和的表达，从而抑制牙周炎和牙槽骨丢失。通过调节 HO-1 和随后的表皮生长因子受体（EGFR）信号，观察到这些人参皂苷对牙周炎和牙槽骨丢失的抑制作用。用 EGFR siRNA 沉默 EGFR 证实了人参皂苷对 HO-1 的作用是通过 EGFR 介导的。总之，本研究评价了从人参果提取物中分离的人参皂苷 Re、Ra8 和 Rf 的含量。因此，这些结果为人参果成分的进一步研究提供了重要的基础数据，并表明人参皂苷 Re、Ra8 和 Rf 具有作为牙周炎未来治疗选择的潜力。
