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绣球藤提取物的抗炎活性及机制
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李海山 ,杨和金 ,郑永仁 (1.云南省食品药品审核查验中心,昆明 650106;2.云南省药物研究所药理室,
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1*
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昆明 650111;3.云南中医药大学动物实验中心,昆明 650500)
中图分类号 R965;R285 文献标志码 A 文章编号 1001-0408(2024)04-0453-06
DOI 10.6039/j.issn.1001-0408.2024.04.13
摘 要 目的 探讨绣球藤提取物的抗炎活性及潜在机制。方法 使用二甲苯致耳廓肿胀建立急性炎症小鼠模型,以阿司匹林
(0.25 g/kg)为阳性对照,1.25、2.5、5 g/kg绣球藤提取物对小鼠耳肿胀度的影响。以植入棉球的方法建立慢性炎症大鼠模型,以阿
司匹林(0.17 g/kg)为阳性对照,0.88、1.75、3.5 g/kg绣球藤提取物对大鼠肉芽净重的影响。以脂多糖诱导RAW264.7细胞建立炎症
损伤细胞模型,考察12.5、25、50 μg/mL绣球藤提取物对细胞上清液中一氧化氮(NO)、前列腺素E2 (PGE2 )、肿瘤坏死因子α(TNF-α)、
白细胞介素 6(IL-6)、单核细胞趋化蛋白 1(MCP-1)含量,细胞中诱导型一氧化氮合酶(iNOS)、环氧合酶 2(COX-2)、p65、磷酸化
p65(p-p65)蛋白表达水平,以及p65蛋白核转移的影响。结果 5 g/kg的绣球藤提取物可显著降低小鼠的耳肿胀度,1.75、3.5 g/kg
的绣球藤提取物可显著降低大鼠的肉芽净重(P<0.05)。12.5、25、50 μg/mL 绣球藤提取物可显著降低细胞上清液中 NO(12.5
μg/mL 绣球藤提取物除外)、PGE2、TNF-α、IL-6、MCP-1含量,以及细胞中iNOS、COX-2蛋白的相对表达量和p-p65、p65蛋白的相
对表达量比值(P<0.05或P<0.01);25、50 μg/mL绣球藤提取物可阻断p65蛋白的核转移。结论 绣球藤提取物具有良好的抗炎
活性,其作用机制可能与抑制核因子κB信号通路激活、下调COX-2和iNOS蛋白的表达、减少炎症因子的释放有关。
关键词 绣球藤提取物;抗炎活性;巨噬细胞;核因子κB信号通路
Anti-inflammatory activity and mechanism of Clematis ranunculoides extract
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LI Haishan ,YANG Hejin ,ZHENG Yongren(1. Center for Food and Drug Inspection of Yunnan Province,
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Kunming 650106, China;2. Dept. of Pharmacology, Yunnan Institute of Materia Medica, Kunming 650111,
China;3. Animal Experiment Center, Yunnan University of Chinese Medicine, Kunming 650500, China)
ABSTRACT OBJECTIVE To investigate the anti-inflammatory activity and potential mechanism of Clematis ranunculoides
extract. METHODS The ear swelling was induced by xylene to establish an acute inflammation model of mice; using aspirin (0.25
g/kg) as a positive control, the effects of 1.25, 2.5, 5 g/kg C. ranunculoides extract on the degree of ear swelling were
investigated. The chronic inflammation model of rats was also established by implanting cotton balls; using aspirin (0.17 g/kg) as a
positive control, the effects of 0.88, 1.75, 3.5 g/kg C. ranunculoides extract on the net weight of granulomas were investigated.
Furthermore, RAW264.7 cells were induced by lipopolysaccharide to establish an inflammatory injury model; the effects of 12.5,
25, 50 μg/mL C. ranunculoides extract on the contents of nitric oxide(NO), prostaglandin E2 (PGE2 ), tumor necrosis factor-α
(TNF- α), interleukin-6(IL-6) and monocyte chemotactic protein-1(MCP-1) in the cell supernatant, the protein expressions of
inducible nitric oxide synthase(iNOS), cyclooxygenase-2(COX-2), p65 and phosphorylated p65(p-p65) in cells as well as nuclear
translocation of p65 protein were assessed. RESULTS C. ranunculoides extract with 5 g/kg significantly relieved ear swelling in
mice, and C. ranunculoides extract with 1.75, 3.5 g/kg significantly decreased the net weight of granulomas in rats (P<0.05). C.
ranunculoides extract with 12.5, 25, 50 μg/mL significantly reduced the contents of NO (except for 12.5 μg/mL C. ranunculoides
extract), PGE2, TNF-α, IL-6 and MCP-1 in the cell supernatant, as well as the relative expressions of iNOS and COX-2 protein,
and relative expression ratio of p-p65 and p65 protein (P<0.05 or P<0.01); C. ranunculoides extract with 25, 50 μg/mL
inhibited the translocation of p65 protein to the cell nucleus. CONCLUSIONS C. ranunculoides extract exhibits significant anti-
inflammatory activity, the mechanism of which may be attributed to the inhibition of the activation of nuclear factor- κB signaling
pathway, down-regulation of COX-2 and iNOS protein expression,
Δ 基金项目 云 南 省 创 新 引 导 与 科 技 型 企 业 培 育 计 划 项 目
(No.202004AR040008) and the reduction of inflammatory cytokines release.
*第一作者 副主任药师。研究方向:药理学、药品审核查验。 KEYWORDS Clematis ranunculoides extract; anti-inflammatory
E-mail:840792727@qq.com activity; macrophages; nuclear factor-κB signaling pathway
# 通信作者 高级实验师。研究方向:实验动物和药效机制。
E-mail:4047135765@qq.com
中国药房 2024年第35卷第4期 China Pharmacy 2024 Vol. 35 No. 4 · 453 ·