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Antiausterity Activity of Secondary Metabolites from the Roots of Ferula hezarlalehzarica against the PANC-1 Human Pancreatic Cancer Cell Line.
Journal of Natural Products ( IF 5.1 ) Pub Date : 2020-03-12 , DOI: 10.1021/acs.jnatprod.9b01109
Mostafa Alilou 1, 2 , Dya Fita Dibwe 3 , Stefan Schwaiger 1 , Mojtaba Khodami 4 , Jakob Troppmair 2 , Suresh Awale 3 , Hermann Stuppner 1
Affiliation  

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 Ferula hezarlalehzarica showed potent preferential cytotoxic activity with a PC50 value of 0.78 μg/mL. Phytochemical investigation of this extract led to the isolation of 18 compounds, including one new sesquiterpenoid (6) and one new monoterpenoid (18). All isolated compounds were evaluated for their preferential cytotoxicity against PANC-1 human pancreatic cancer cells by employing an antiausterity strategy. Among them, ferutinin (2) was identified as the most active compound, with a PC50 value of 0.72 μM. In addition, the real-time effect of ferutinin (2) and compound 6 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 2 and 6 also inhibited colony formation of PANC-1 cells. The present study indicates that the dichloromethane extract of the roots of F. hezarlalehzarica is a rich source of bioactive compounds for targeting PANC-1 cells.

中文翻译:

阿魏根部次生代谢产物对PANC-1人胰腺癌细胞系的抗紧缩活性。

人胰腺癌是最具有侵略性的癌症之一,死亡率很高。由于此类癌细胞对营养缺乏条件的高度耐受性,因此它们可以在血管不足的肿瘤微环境中生存。在这项研究中,阿魏根的二氯甲烷提取物显示出强大的优先细胞毒性活性,PC50值为0.78μg/ mL。对这种提取物的植物化学研究导致分离出18种化合物,其中包括一种新的倍半萜(6)和一种新的单萜(18)。通过采用抗紧缩策略,评估了所有分离的化合物对PANC-1人胰腺癌细胞的优先细胞毒性。其中,铁白蛋白(2)被鉴定为活性最高的化合物,PC50值为0.72μM。此外,Ferutinin(2)和化合物6对暴露于营养剥夺培养基(NDM)中的PANC-1细胞的实时作用显示细胞收缩,导致癌细胞在短时间内暴露死亡。化合物2和6也抑制PANC-1细胞的集落形成。目前的研究表明,F。hezarlalehzarica根的二氯甲烷提取物是靶向PANC-1细胞的丰富生物活性化合物的来源。
更新日期:2020-03-12
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