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(IC50)\nPKA:0.17 mM (IC50)\nTPK:0.1 mM (IC50)",{"key":266,"value":267},"体外研究","白屈菜红碱抑制BclXL-Bak BH3肽结合,IC50为1.5μM,并取代BclXL中含有BH3的蛋白质Bax。用白屈菜红碱处理的哺乳动物细胞经历细胞凋亡,其特征在于线粒体途径的参与[1]。白屈菜红碱处理通过选择性抑制p38丝裂原活化蛋白激酶(MAPK)和细胞外信号调节蛋白激酶1和2(ERK1\u002F2)激活,抑制LPS诱导的小鼠腹腔巨噬细胞中LPS诱导的TNF-α水平和NO产生。此外,白屈菜红碱对NO和细胞因子TNF-α产生的影响可能可以通过p38 MAPK和ERK1\u002F2在调节炎症介质表达中的作用来解释[2]。白屈菜红碱对人单核细胞白血病细胞具有细胞毒作用,LD50值为3.46μM。 LPS刺激后2小时,受血根碱和白屈菜红碱影响的细胞使CCL-2表达显着下降3.5和1.9 [3]。白屈菜红碱以剂量依赖性方式显着增强ERK1\u002F2的磷酸化。此外,白屈菜红碱抑制p38的磷酸化[4]。",{"key":269,"value":270},"体内研究","白屈菜红碱通过抑制LPS诱导的肿瘤坏死因子-α(TNF-α)水平和血清中一氧化氮(NO)的产生,在体内实验诱导的小鼠内毒素休克模型中显示出显着的抗炎作用[2]。白屈菜红碱氯化物(5mg\u002Fkg \u002F天,ip)诱导RCC细胞凋亡而对小鼠没有显着毒性。白屈菜红碱治疗导致p53的剂量依赖性积累[4]。",{"key":272,"value":273},"细胞实验","通过MTT测定评估细胞活力。将100μL培养基中的细胞（2×103 HEK-293细胞\u002F孔和3×103 SW-839细胞\u002F孔）接种到96孔板中，并孵育12小时。接下来，用含有各种浓度的白屈菜红碱的培养基替换每个孔中的培养基，并将细胞在37℃下再培养24和48小时。随后，向每个孔中加入20μLMTT（5mg \u002F mL）。在37℃下另外温育4小时后，除去上清液，并向每个孔中加入100μLDMSO。使用iMark™微孔板吸光度读数器测定吸光度值（在540nm处读数）。使用Microplate Manager软件（版本6.3; 1689520）分析数据。",{"key":275,"value":276},"动物实验","将总共5×106个SW-839细胞与Matrigel®混合，并皮下注射到14只5周龄雄性BALB \u002F c裸鼠的侧腹中。将小鼠保持在18×30-cm笼中，每笼3只小鼠，温度为22℃，使用12小时光照\u002F黑暗循环。食物和水随意提供。小鼠随机分为两组（n = 7）。如前所述，通过腹膜内注射给小鼠施用剂量为5mg \u002F kg \u002F天的白屈菜红碱氯化物5周，在注射SW-839细胞后第一次注射白屈菜红碱24小时。对照小鼠施用相同体积的含有1％DMSO的PBS。每周测量一次小鼠肿瘤的体积和重量。在切除肿瘤后，在接种癌细胞后36天处死所有小鼠。",{"key":278,"value":279},"参考文献","[1].\nChan, et al. Identification of chelerythrine as an inhibitor of BclXL function. J Biol Chem. 2003 Jun 6;278(23):20453-6.\n[2].\nLi W, et al. Effect of Chelerythrine Against Endotoxic Shock in Mice and Its Modulation of Inflammatory Mediators in Peritoneal Macrophages Through the Modulation of Mitogen-Activated Protein Kinase (MAPK) Pathway. Inflammation. 2012 Jul 24.\n[3].\nPencikova K, et al. Investigation of sanguinarine and chelerythrine effects on LPS-induced inflammatory gene expression in THP-1 cell line. Phytomedicine. 2012 Jul 15;19(10):890-5. Epub 2012 May 14.\n[4].\nChen XM, et al. Chelerythrine chloride induces apoptosis in renal cancer HEK-293 and SW-839 cell lines. Oncol Lett. 2016 Jun;11(6):3917-3924\n[5].\nHerbert JM, et al. Chelerythrine is a potent and specific inhibitor of protein kinase C. 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