Zhang Ji-Zhong, Chen Xiao-Yi, Wu You-Jiao, Li Li-Min, Huang Li, Yin Qiao-Zhi, Luo Pei, Liu Yuan
Institute of Ethnic Medicine, Southwest Minzu University, Chengdu, China.
Sichuan Provincial Qiang-Yi Medicinal Resources Protection and Utilization Technology and Engineering Laboratory, Chengdu, China.
Front Pharmacol. 2020 Nov 9;11:568585. doi: 10.3389/fphar.2020.568585. eCollection 2020.
The Yi nationality herbal formula is used in China as a folk medicine to treat arthritis and related diseases. Despite its widespread use, the active ingredients, and pharmacological mechanisms are not performed. This is the first time to identify the active compounds from with the aim at providing the potential effect of and exploring its underlying anti-inflammatory mechanism in monosodium urate crystals (MSU)-induced arthritis rats. In this study, anti-hyperuricemia effect was assessed by reducing the serum uric acid levels and increasing uric acid excretion in the urine for the hyperuricemia rat model. significantly suppressed the degree of joint swelling and improved the symptoms of inflammation induced by MSU crystals. The inhibition of IL-2, IL-1β, IFN-γ, and IL-6 secretion and IL-10 increase in the serum were also observed. This study also focuses on the screening of the main compounds from against cyclooxygenase for anti-inflammatory properties using molecular docking. The result showed 3-O-[α-L-pyran rhamnose(1-3)-β-D-pyran glucuronic acid]- oleanolic acid, 3-O-(β-D-pyran glucuronic acid)-oleanolic acid-28-O-β-D-pyran glucoside, and 3-O-[α-L-pyran rhamnose(1-3)-β-D-pyran glucuronic acid]-oleanolic acid-28-O-β-D-pyran glucoside with a higher binding affinity for COX-2 than COX-1 which indicated relatively higher interaction than COX-1. The preferential selectivity toward inhibiting COX-2 enzyme over COX-1 of three compounds from were evaluated using cyclooxygenases 1 and 2 (COX-1/2) inhibition assays. Meanwhile, the down-regulated protein expression of COX-2 and VCAM-1 in synovial tissue sections from ankle joints of experiments rats were confirmed by immunohistochemistry analysis after the treatment. In conclusion, three oleanolic acid glycosides were implied as mainly efficient compounds in Yi nationality herbal formula for arthritis therapy via selectively influencing COX-2 and VCAM-1 signaling.
彝族草药配方在中国被用作治疗关节炎及相关疾病的民间药物。尽管其使用广泛，但其活性成分和药理机制尚未明确。这是首次从[具体草药名称未给出]中鉴定出活性化合物，旨在提供[具体草药名称未给出]的潜在作用，并探索其在尿酸钠晶体（MSU）诱导的关节炎大鼠中的潜在抗炎机制。在本研究中，通过降低高尿酸血症大鼠模型的血清尿酸水平和增加尿酸尿排泄来评估抗高尿酸血症作用。[具体草药名称未给出]显著抑制了关节肿胀程度，并改善了MSU晶体诱导的炎症症状。还观察到血清中IL-2、IL-1β、IFN-γ和IL-6分泌的抑制以及IL-10的增加。本研究还通过分子对接重点筛选了[具体草药名称未给出]中针对环氧化酶具有抗炎特性的主要化合物。结果表明，3-O-[α-L-吡喃鼠李糖(1-3)-β-D-吡喃葡萄糖醛酸]-齐墩果酸、3-O-(β-D-吡喃葡萄糖醛酸)-齐墩果酸-28-O-β-D-吡喃葡萄糖苷和3-O-[α-L-吡喃鼠李糖(1-3)-β-D-吡喃葡萄糖醛酸]-齐墩果酸-28-O-β-D-吡喃葡萄糖苷对COX-2的结合亲和力高于COX-1，这表明它们与COX-2的相互作用相对较高。使用环氧化酶1和2（COX-1/2）抑制试验评估了[具体草药名称未给出]中三种化合物对COX-2酶的抑制优先选择性高于COX-1。同时，在[具体草药名称未给出]处理后，通过免疫组织化学分析证实了实验大鼠踝关节滑膜组织切片中COX-2和VCAM-1的蛋白表达下调。总之，三种齐墩果酸糖苷被认为是彝族草药配方中治疗关节炎的主要有效化合物，通过选择性影响COX-2和VCAM-1信号通路发挥作用。
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