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首页> 外文期刊>Planta medica: Natural products and medicinal plant research >Growth inhibition and G1 cell cycle arrest mediated by 25-methoxyhispidol A, a novel triterpenoid, isolated from the fruit of Poncirus trifoliata in human hepatocellular carcinoma cells.
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Growth inhibition and G1 cell cycle arrest mediated by 25-methoxyhispidol A, a novel triterpenoid, isolated from the fruit of Poncirus trifoliata in human hepatocellular carcinoma cells.

机译：25-甲氧基hispidol A介导的生长抑制和G1细胞周期停滞，这是一种新型三萜类化合物，从人类肝癌细胞中的三叶红枣果实中分离出来。

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摘要

Poncirus trifoliata (Rutaceae) extracts have been known to possess anti-allergic, anti-inflammatory and antiviral activities. However, other biological activities, especially, the anticancer potential of extracts of P. trifoliata or its constituents, have not been fully investigated yet. In this study, we have evaluated the antiproliferative effects of a novel triterpenoid, 25-methoxyhispidol A, isolated from the fruit of P. trifoliata against SK-HEP-1 human hepatocellular carcinoma cells. Flow cytometric analysis indicated that 25-methoxyhispidol A arrests the cell cycle in the G1 phase at the earlier time and subsequently induces apoptosis of the cancer cells. Further study revealed that the cell cycle arrest in the G1 phase by 25-methoxyhispidol A correlated well with the inhibition of phosphorylation of the retinoblastoma (Rb) protein, and with the down-regulation of cyclin D1 and cyclin-dependent kinase cdk4 and the induction of cdk inhibitor p21 (WAF1/Cip1) protein. These findings suggest the potential of 25-methoxyhispidol A isolated from the fructus of P. trifoliata as an antitumor agent against human hepatocarcinoma cells by arresting the cell cycle and inducing apoptosis.
机译：众所周知，Poncirus trifoliata（芸香科）提取物具有抗过敏，抗炎和抗病毒的活性。但是，还没有充分研究其他生物活性，特别是三叶紫苏提取物或其成分的抗癌潜力。在这项研究中，我们评估了一种新的三萜类化合物25-甲氧基hispidol A的抗增殖作用，该化合物从三叶果中分离出对人肝癌细胞SK-HEP-1的抑制作用。流式细胞仪分析表明，25-甲氧基hispidol A在更早的时间将细胞周期停滞在G1期，随后诱导癌细胞凋亡。进一步的研究表明，由25-甲氧基hispidol A阻滞G1期的细胞周期与抑制视网膜母细胞瘤（Rb）蛋白的磷酸化，细胞周期蛋白D1和细胞周期蛋白依赖性激酶cdk4的下调以及诱导有关。 CDK抑制剂p21（WAF1 / Cip1）蛋白的表达。这些发现表明，通过停止细胞周期并诱导细胞凋亡，从三叶草的果实中分离出的25-甲氧基hispidol A作为抗人肝癌细胞的抗肿瘤剂的潜力。

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