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albicans[2]",{"key":245,"value":246},"体外研究","Damnacanthal对p56ck对丝氨酸\u002F苏氨酸激酶、蛋白激酶A和蛋白激酶C的选择性大于100倍,对p56ck对四受体酪氨酸激酶的选择性大于40倍。Damnacanthal也显示了p60src和p59fyn同源酶p60src对p56lck的选择性(7-20倍),但具有高度的统计学意义[1]。达姆纳坎塔尔(0.1-100μM；1-4天；HCT-116和SW480细胞)治疗导致细胞增殖显著降低,且呈浓度和时间依赖性[2]。达那坎塔尔(1-50μM；72小时；HCT-116细胞)处理导致浓度为50μM时S\u002FG1和G2\u002FG1期细胞数量显著增加[2]。达那坎塔尔(10μM；24小时；HCT-116细胞)处理显著提高caspase 3\u002F7活性。达那坎塔尔诱导细胞凋亡[2]。Damnacanthal(0.1-10μM；24小时；HCT-116细胞)诱导HCT-116细胞NAG-1表达。细胞周期蛋白D1的表达在10μM达纳坎塔尔时减少,而p21和p53不改变其表达。10μM Damnacanthal治疗仅在HCT-116细胞中见到PARP卵裂,其中NAG-1被诱导[2 ]。达那坎塔尔治疗2周后,HCT-116细胞的集落数明显减少,且呈浓度依赖性。达纳坎塔尔处理的细胞显示出对克隆形成能力的显著抑制。达那坎塔尔处理(1-50μM；48小时)的细胞以浓度依赖的方式显著抑制HCT-116细胞的迁移[2]。细胞增殖实验[2]细胞株：HCT-116和SW480细胞浓度：0.1μM、1μM、10μM、100μM培养时间：1、2和4天结果：细胞增殖明显降低,呈浓度和时间依赖性。细胞周期分析[2]细胞系：HCT-116细胞浓度：1μM,10μM和50μM孵育时间：72小时。结果：50μM浓度下,S\u002FG1期和G2\u002FG1期细胞数量显著增加。凋亡分析[2]细胞系：HCT-116细胞浓度：10μM孵育时间：24小时。结果：caspase 3\u002F7活性显著增加。Western Blot分析[2]细胞株：HCT-116细胞浓度：0.1μM,1μM,10μM孵育时间：24小时结果：NAG-1在HCT-116细胞中呈剂量和时间依赖性诱导。细胞周期蛋白D1在10μM时表达降低。",{"key":248,"value":249},"体内研究","达那坎塔尔(10-100 mg\u002Fkg；口服；10-300分钟；雄性ddY小鼠)在福尔马林试验中以剂量依赖的方式显示出显著的抗伤害作用。达那坎塔尔(100mg\u002Fkg)对组胺诱导的足肿胀有明显的抑制作用[4]。动物模型：雄性Dy小鼠(5-6周)注射福尔马林或组胺[4 ]剂量：10 mg\u002Fkg、30 mg\u002Fkg和100 mg\u002Fkg给药：口服10分钟、30分钟、60分钟或300分钟：结果显著降低了人肺肿瘤的生长,无急性毒性。",{"key":251,"value":252},"参考文献","[1].\nFaltynek CR, et al. Damnacanthal is a highly potent, selective inhibitor of p56lck tyrosine kinase activity. Biochemistry. 1995 Sep 26;34(38):12404-10.\n[2].\nNualsanit T, et al. Damnacanthal, a noni component, exhibits antitumorigenic activity in human colorectal cancer cells. J Nutr Biochem. 2012 Aug;23(8):915-23.\n[3].\nAziz MY, et al. Damnacanthal is a potent inducer of apoptosis with anticancer activity by stimulating p53 and p21 genes in MCF-7 breast cancer cells. Oncol Lett. 2014 May;7(5):1479-1484.\n[4].\nOkusada K, et al. The antinociceptive and anti-inflammatory action of the CHCl3-soluble phase and its main active component, damnacanthal, isolated from the root of Morinda citrifolia. 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