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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,
                          2
                 1*
                                  3 #
          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
                   1
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          LI Haishan ,YANG Hejin ,ZHENG Yongren(1.  Center  for  Food  and  Drug  Inspection  of  Yunnan  Province,
                                 2
          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 ·
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