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从根部分离得到的次级代谢产物对人胰腺癌细胞系 PANC-1 的抗应激活性。

Antiausterity Activity of Secondary Metabolites from the Roots of against the PANC-1 Human Pancreatic Cancer Cell Line.

机构信息

Institute of Pharmacy/Pharmacognosy, Center for Molecular Biosciences Innsbruck, University of Innsbruck, Innrain 80/82, Innsbruck 6020, Austria.

Daniel-Swarovski Research Laboratory, Department of Visceral, Transplant and Thoracic Surgery, Innsbruck Medical University, Innrain 66, A-6020 Innsbruck, Austria.

出版信息

J Nat Prod. 2020 Apr 24;83(4):1099-1106. doi: 10.1021/acs.jnatprod.9b01109. Epub 2020 Mar 12.

Abstract

Human pancreatic cancer is one of the most aggressive types of cancer, with a high mortality rate. Due to the high tolerance of such cancer cells to nutrient starvation conditions, they can survive in a hypovascular tumor microenvironment. In this study, the dichloromethane extract of the roots of showed potent preferential cytotoxic activity with a PC value of 0.78 μg/mL. Phytochemical investigation of this extract led to the isolation of 18 compounds, including one new sesquiterpenoid () and one new monoterpenoid (). All isolated compounds were evaluated for their preferential cytotoxicity against PANC-1 human pancreatic cancer cells by employing an antiausterity strategy. Among them, ferutinin () was identified as the most active compound, with a PC value of 0.72 μM. In addition, the real-time effect of ferutinin () and compound against PANC-1 cells, exposed to a nutrient-deprived medium (NDM), showed cell shrinkage, leading to cancer cell death within a short period of exposure. Compounds and also inhibited colony formation of PANC-1 cells. The present study indicates that the dichloromethane extract of the roots of is a rich source of bioactive compounds for targeting PANC-1 cells.

摘要

人胰腺癌细胞是最具侵袭性的癌症类型之一,死亡率很高。由于此类癌细胞对营养饥饿条件具有很高的耐受性,它们可以在低血管肿瘤微环境中存活。在这项研究中,显示出强烈的优先细胞毒性活性,PC 值为 0.78 μg/mL。对该提取物的植物化学研究导致分离出 18 种化合物,包括一种新的倍半萜()和一种新的单萜()。所有分离出的化合物都通过采用节细胞营养策略来评估其对 PANC-1 人胰腺癌细胞的优先细胞毒性。其中, ferutinin ()被鉴定为最活跃的化合物,PC 值为 0.72 μM。此外, ferutinin ()和化合物对暴露于营养缺乏培养基(NDM)的 PANC-1 细胞的实时作用显示细胞收缩,导致癌细胞在短时间暴露后死亡。化合物和也抑制了 PANC-1 细胞的集落形成。本研究表明, 的根的二氯甲烷提取物是针对 PANC-1 细胞的生物活性化合物的丰富来源。

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