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, 昆明 650111
3.云南中医药大学动物实验中心,昆明 650500
Received:22 August 2023,
Revised:2024-01-10,
Accepted:15 January 2024,
Published:29 February 2024
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李海山,杨和金,郑永仁.绣球藤提取物的抗炎活性及机制[J].中国药房,2024,35(04):453-458.
LI Haishan,YANG Hejin,ZHENG Yongren.Anti-inflammatory activity and mechanism of Clematis ranunculoides extract[J].ZHONGGUO YAOFANG,2024,35(04):453-458.
李海山,杨和金,郑永仁.绣球藤提取物的抗炎活性及机制[J].中国药房,2024,35(04):453-458. DOI: 10.6039/j.issn.1001-0408.2024.04.13.
LI Haishan,YANG Hejin,ZHENG Yongren.Anti-inflammatory activity and mechanism of Clematis ranunculoides extract[J].ZHONGGUO YAOFANG,2024,35(04):453-458. DOI: 10.6039/j.issn.1001-0408.2024.04.13.
目的
2
探讨绣球藤提取物的抗炎活性及潜在机制。
方法
2
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E
2
(PGE
2
)、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
2
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)、PGE
2
、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
2
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。
OBJECTIVE
2
To investigate the anti-inflammatory activity and potential mechanism of
Clematis ranunculoides
extract.
METHODS
2
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 E
2
(PGE
2
), 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
2
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), PGE
2
, 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
2
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, and the reduction of inflammatory cytokines release.
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