Department of Biological Sciences, Birla Institute of Technology and Science, Pilani, K.K. Birla Goa Campus, NH-17B, Zuarinagar, Goa 403726, India.
ICMR-National Institute of Traditional Medicine, Nehru Nagar, Belagavi, 590010, Karnataka, India.
Biomed Pharmacother. 2020 Aug;128:110243. doi: 10.1016/j.biopha.2020.110243. Epub 2020 May 27.
Piperlongumine (PL), a herbal drug extracted from long pepper (Piper longum L), is known for its anti-inflammatory and anti-cancer properties. Although, its anti-cancer potential has been evaluated in cancer models like breast, pancreatic, gastric, hepatocellular and lung carcinoma, there is no report on its bio-activity evaluation in intestinal cancers. Here, we report the anti-neoplastic potential of PL against human intestinal carcinoma in-vitro and its possible mechanisms of action. Cytotoxicity studies demonstrate that PL inhibits cell proliferation of INT-407 and HCT-116 cells in a concentration and time-dependent manner. Also, PL elevated the levels of intracellular reactive oxygen species, which may lead to lethal oxidative stress, mitochondrial dysfunction, and nuclear fragmentation. Remarkably, P53, P21, BAX, and SMAD4 were significantly upregulated after PL treatment whereas; BCL2 and SURVIVIN were down-regulated. Moreover, the combination study also shows the synergistic effect of PL with the current chemotherapeutic drug paclitaxel. These findings suggest that PL possesses anti-neoplastic properties in intestinal cancer cells.
荜茇酰胺（PL）是从荜茇（Piper longum L）中提取的一种草药药物，具有抗炎和抗癌特性。尽管其在乳腺癌、胰腺癌、胃癌、肝癌和肺癌等癌症模型中的抗癌潜力已得到评估，但在肠道癌症中尚未有关于其生物活性评估的报道。在这里，我们报告了 PL 对人肠道癌细胞的体外抗肿瘤潜力及其可能的作用机制。细胞毒性研究表明，PL 以浓度和时间依赖性方式抑制 INT-407 和 HCT-116 细胞的增殖。此外，PL 还增加了细胞内活性氧的水平，这可能导致致命的氧化应激、线粒体功能障碍和核碎片。值得注意的是，PL 处理后 P53、P21、BAX 和 SMAD4 显著上调，而 BCL2 和 SURVIVIN 下调。此外，联合研究还表明 PL 与当前化疗药物紫杉醇具有协同作用。这些发现表明 PL 具有在肠道癌细胞中抗肿瘤的特性。
