Kirenol, darutoside and hesperidin contribute to the anti-inflammatory and analgesic activities of Siegesbeckia pubescens makino by inhibiting COX-2 expression and inflammatory cell infiltration
Kirenol, darutoside and hesperidin contribute to the anti-inflammatory and analgesic activities of Siegesbeckia pubescens makino by inhibiting COX-2 expression and inflammatory cell infiltration
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DOI：
10.1016/j.jep.2020.113547
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发表时间：
2021-01-15
影响因子：
5.4
通讯作者：
Tang, He-Bin
中科院分区：
文献类型：
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作者：
Li, Yu-Sang;Zhang, Jian;Tang, He-Bin
人种药理学相关性：为了阐明中药中药稀毛泽兰（Siegesbeckia pubescens Makino，SM）乙醇提取物（ethanol extract of Siegesbeckia pubescens Makino，ESM）中活性成分抗炎镇痛作用的机制，对中药稀毛泽兰乙醇提取物（ethanol extract of Siegesbeckia pubescens Makino，ESM）的抗炎镇痛作用进行了研究。采用高效液相色谱-二极管阵列检测器（HPLC-DAD）对ESM中的活性成分进行鉴定。采用二甲苯致小鼠耳肿胀、完全弗氏佐剂（CFA）致小鼠足肿胀、醋酸致小鼠扭体痛和脂多糖（LPS）致小鼠RAW264.7细胞迁移4种模型，研究ESM有效成分的抗炎镇痛作用机制。（1）在ESM中鉴定出奇壬醇、达鲁托苷和橙皮苷3种有效成分，相对含量分别为0.6%、0.2%和0.01%;橙皮苷是ESM中首次报道。(2)ESM及其有效成分均能有效减轻小鼠耳廓和足趾肿胀程度，提高热痛阈值，降低足趾受试部位皮肤组织中炎症蛋白环氧合酶-2（考克斯-2）的过度表达，减少醋酸致小鼠扭体次数。(3)结论：ESM及其有效成分能有效抑制化学性炎症诱导的炎症因子表达，阻止炎症细胞浸润，发挥良好的抗炎和镇痛作用。
Ethnopharmacological relevance: The Chinese traditional medicine of Siegesbeckia pubescens Makino (SM), which has the effect of healing rheumatism and promoting joint health, is often used to treat rheumatoid arthritis and ischemic stroke.Aim of the study: To clarify the mechanisms underlying the anti-inflammatory and analgesic influence of active components in the ethanol extract of Siegesbeckia pubescens Makino (ESM).Materials and methods: The active ingredients in the ESM were identified practicing high-performance liquid chromatography-diode array detection (HPLC-DAD). Four models including xylene-induced ear oedema, complete Freund's adjuvant (CFA)-induced hind paw oedema, acetic acid-induced pain writhing and lipopolysaccharide (LPS)-induced RAW264.7 cell migration, were used to clarify the anti-inflammatory and analgesic mechanisms of the active ingredients in the ESM.Results: (1) Three active ingredients of kirenol, darutoside and hesperidin were identified in the ESM, with relative proportion of 0.6%, 0.2% and 0.01%, respectively; hesperidin was reported for the first time in the ESM. (2) Both the ESM and its active ingredients could effectively alleviate the degree of swelling of the auricle and toes, increase the threshold of heat pain, decrease the overexpression of inflammatory protein cyclooxygenase-2 (COX-2) in the skin tissue of the tested parts of the toes, and reduce the number of writhes induced by acetic acid in mice. (3) ESM and its active ingredients also dose-dependently inhibited the migration of RAW264.7 cells.Conclusions: ESM and its active ingredients can effectively attenuate the expression of inflammatory factors induced by chemical inflammation, prevent the infiltration of inflammatory cells, and exert good antiinflammatory and antinociceptive activities.