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从远志的中等细胞毒性部位分离鉴定两种酚类化合物。

Isolation and Identification of Two Phenolic Compounds from a Moderately Cytotoxic Fraction of Bunge.

作者信息

Sajjadi Seyed Ebrahim, Ghanadian Mustafa, Haghighi Mehrangiz

机构信息

Department of Pharmacognosy, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran.

出版信息

Adv Biomed Res. 2017 Jun 6;6:66. doi: 10.4103/2277-9175.190980. eCollection 2017.

DOI:10.4103/2277-9175.190980
PMID:28626741
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5468789/
Abstract

BACKGROUND

Little information is available about chemical components of the genus. A primary cytotoxicity screening on showed moderate cytotoxic activity against OVCAR-3 ovarian and HT-29 colon cancer cells. Therefore, the aim of this study is a phytochemical investigation to identify the compounds responsible for this bioactivity.

MATERIALS AND METHODS

Extraction was done through percolation and fractionations by reverse phase column chromatography and normal column chromatography. Using standard 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay Fr.b8 with moderate cytotoxicity was selected for identification of major components. Fr.b8 was subjected to polyamide column chromatography. More purification was done using a new modified recycle high-performance liquid chromatography (HPLC) with flow splitter.

RESULTS

Two known compounds: Apigenin (flavone) and caffeic acid (phenolic acid) were obtained from phenolic bioactive fraction for the first time from this plant.

CONCLUSIONS

Apigenin and caffeic acid with known antitumor and matrix metalloproteinase inhibitory effects seem to be the bioactive components responsible for moderate cytotoxicity of phenolic fraction. Recycle HPLC following with flow splitting is a new method useful for isolation of closely eluted compounds in HPLC chromatogram.

摘要

背景

关于该属的化学成分信息较少。对[未提及的对象]进行的初步细胞毒性筛选显示,其对OVCAR - 3卵巢癌细胞和HT - 29结肠癌细胞具有中等细胞毒性活性。因此,本研究的目的是进行植物化学研究,以鉴定具有这种生物活性的化合物。

材料与方法

通过渗漉法进行提取,并采用反相柱色谱和正相柱色谱进行分离。使用标准的3 -(4,5 - 二甲基噻唑 - 2 - 基)- 2,5 - 二苯基四氮唑溴盐法,选择具有中等细胞毒性的Fr.b8进行主要成分鉴定。将Fr.b8进行聚酰胺柱色谱分离。使用带有分流器的新型改良循环高效液相色谱(HPLC)进行进一步纯化。

结果

从该植物的酚类生物活性组分中首次获得了两种已知化合物:芹菜素(黄酮)和咖啡酸(酚酸)。

结论

具有已知抗肿瘤和基质金属蛋白酶抑制作用的芹菜素和咖啡酸似乎是酚类组分具有中等细胞毒性的生物活性成分。带有分流的循环HPLC是一种用于分离HPLC色谱图中紧密洗脱化合物的新方法。

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本文引用的文献

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Caffeic acid derivatives inhibit the growth of colon cancer: involvement of the PI3-K/Akt and AMPK signaling pathways.咖啡酸衍生物抑制结肠癌生长:PI3-K/Akt和AMPK信号通路的参与
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Fitoterapia. 2013 Dec;91:87-94. doi: 10.1016/j.fitote.2013.08.016. Epub 2013 Sep 17.
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Apigenin and its impact on gastrointestinal cancers.
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Selective matrix metalloproteinase inhibitors for cancer.选择性基质金属蛋白酶抑制剂在癌症中的应用。
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Novel and therapeutic effect of caffeic acid and caffeic acid phenyl ester on hepatocarcinoma cells: complete regression of hepatoma growth and metastasis by dual mechanism.咖啡酸和咖啡酸苯酯对肝癌细胞的新特性及治疗效果:通过双重机制使肝癌生长和转移完全消退
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Apigenin acts on the tumor cell invasion process and regulates protease production.
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