School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, China.
Department of Pharmaceutics, School of Pharmacy, Fudan University & Key Laboratory of Smart Drug Delivery, Ministry of Education, Shanghai, 201203, China.
BMC Complement Med Ther. 2021 May 25;21(1):149. doi: 10.1186/s12906-021-03302-5.
Rheumatoid arthritis (RA) is an autoimmune disease which causes disability and threatens the health of humans. Therefore, it is of great significance to seek novel effective drugs for RA. It has been reported that various ginsenoside monomers are able to treat RA. However, it is still unclear which ginsenoside is the most effective and has the potential to be developed into an anti-RA drug.
The ginsenosides, including Rg1, Rg3, Rg5, Rb1, Rh2 and CK, were evaluated and compared for their therapeutic effect on RA. In in vitro cell studies, methotrexate (MTX) and 0.05% dimethyl sulfoxide (DMSO) was set as a positive control group and a negative control group, respectively. LPS-induced RAW264.7 cells and TNF-α-induced HUVEC cells were cultured with MTX, DMSO and six ginsenosides, respectively. Cell proliferation was analyzed by MTT assay and cell apoptosis was carried out by flow cytometry. CIA mice model was developed to evaluate the therapeutic efficacy of ginsenosides. The analysis of histology, immunohistochemistry, flow cytometry and cytokine detections of the joint tissues were performed to elucidate the action mechanisms of ginsenosides.
All six ginsenosides showed good therapeutic effect on acute arthritis compared with the negative control group, Ginsenoside CK provided the most effective treatment ability. It could significantly inhibit the proliferation and promote the apoptosis of RAW 264.7 and HUVEC cells, and substantially reduce the swelling, redness, functional impairment of joints and the pathological changes of CIA mice. Meanwhile, CK could increase CD8 + T cell to down-regulate the immune response, decrease the number of activated CD4 + T cell and proinflammatory M1-macrophages, thus resulting in the inhibition of the secretion of proinflammatory cytokine such as TNF-α and IL-6.
Ginsenoside CK was proved to be a most potential candidate among the tested ginsenosides for the treatment of RA, with a strong anti-inflammation and immune modulating capabilities.
类风湿性关节炎（RA）是一种自身免疫性疾病，可导致残疾并威胁人类健康。因此，寻找新型有效的 RA 治疗药物具有重要意义。据报道，各种人参皂苷单体均可治疗 RA。然而，哪种人参皂苷最有效，并有潜力开发成抗 RA 药物仍不清楚。
评估并比较 Rg1、Rg3、Rg5、Rb1、Rh2 和 CK 等人参皂苷对 RA 的治疗作用。在体外细胞研究中，甲氨蝶呤（MTX）和 0.05%二甲基亚砜（DMSO）分别设为阳性对照组和阴性对照组。分别用 MTX、DMSO 和 6 个人参皂苷培养 LPS 诱导的 RAW264.7 细胞和 TNF-α 诱导的 HUVEC 细胞。用 MTT 法分析细胞增殖，用流式细胞术分析细胞凋亡。建立 CIA 小鼠模型评价人参皂苷的治疗效果。对关节组织进行组织学、免疫组织化学、流式细胞术和细胞因子检测分析，阐明人参皂苷的作用机制。
与阴性对照组相比，6 个人参皂苷对急性关节炎均有较好的治疗作用，其中人参皂苷 CK 治疗效果最佳。它能显著抑制 RAW264.7 和 HUVEC 细胞的增殖，促进其凋亡，明显减轻 CIA 小鼠关节肿胀、红肿、功能障碍及病理改变。同时，CK 可增加 CD8+T 细胞，下调免疫反应，减少活化的 CD4+T 细胞和促炎 M1 巨噬细胞数量，从而抑制 TNF-α和 IL-6 等促炎细胞因子的分泌。
在测试的人参皂苷中，人参皂苷 CK 被证明是治疗 RA 的最有潜力的候选药物，具有较强的抗炎和免疫调节作用。
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