Andrographolide, a potential cancer therapeutic agent isolated from Andrographis paniculata.
Andrographolide, a potential cancer therapeutic agent isolated from Andrographis paniculata.
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DOI：
10.1046/j.1359-4117.2003.01090.x
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发表时间：
2003-05-01
影响因子：
--
通讯作者：
Rajagopalan, R
中科院分区：
文献类型：
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作者：
Rajagopal, Sriram;Kumar, R Ajaya;Rajagopalan, R
穿心莲植物提取物具有多种药理活性。穿心莲是提取物的主要成分，与其药理活性有关。我们研究了在人类癌症和免疫细胞中由穿心莲内酯治疗调节的细胞过程和靶点。穿心莲内酯治疗抑制不同肿瘤细胞系的体外增殖，代表各种类型的癌症。该化合物通过诱导细胞周期抑制蛋白p27和降低细胞周期蛋白依赖性激酶4（CDK 4）的表达，将细胞周期阻滞在G 0/G1期，从而对癌细胞发挥直接的抗癌活性。穿心莲内酯的免疫刺激活性通过增加淋巴细胞增殖和白细胞介素-2的产生来证明。穿心莲还增强了肿瘤坏死因子-α的产生和CD标记物的表达，导致淋巴细胞对癌细胞的细胞毒性活性增加，这可能有助于其间接抗癌活性。该化合物的体内抗癌活性针对B16 F0黑色素瘤同系和HT-29异种移植模型得到进一步证实。这些结果表明，穿心莲是一个有趣的药效团，具有抗癌和免疫调节活性，因此有潜力被开发为癌症治疗剂。
Andrographis paniculata plant extract is known to possess a variety of pharmacological activities. Andrographolide, the major constituent of the extract is implicated towards its pharmacological activity. We studied the cellular processes and targets modulated by andrographolide treatment in human cancer and immune cells. Andrographolide treatment inhibited the in vitro proliferation of different tumor cell lines, representing various types of cancers. The compound exerts direct anticancer activity on cancer cells by cell-cycle arrest at G0/G1 phase through induction of cell-cycle inhibitory protein p27 and decreased expression of cyclin-dependent kinase 4 (CDK4). Immunostimulatory activity of andrographolide is evidenced by increased proliferation of lymphocytes and production of interleukin-2. Andrographolide also enhanced the tumor necrosis factor-alpha production and CD marker expression, resulting in increased cytotoxic activity of lymphocytes against cancer cells, which may contribute for its indirect anticancer activity. The in vivo anticancer activity of the compound is further substantiated against B16F0 melanoma syngenic and HT-29 xenograft models. These results suggest that andrographolide is an interesting pharmacophore with anticancer and immunomodulatory activities and hence has the potential for being developed as a cancer therapeutic agent.