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槲皮素 5--酰基衍生物的合成、抗增殖活性和自由基清除能力。

Synthesis, Antiproliferative Activity and Radical Scavenging Ability of 5--Acyl Derivatives of Quercetin.

机构信息

School of Chemical Sciences, University of Auckland, 23 Symonds Street, Auckland 1010, New Zealand.

Auckland Cancer Society Research Centre, University of Auckland, Auckland 1023, New Zealand.

出版信息

Molecules. 2021 Mar 14;26(6):1608. doi: 10.3390/molecules26061608.

DOI:10.3390/molecules26061608
PMID:33799363
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7999741/
Abstract

Quercetin is a flavonoid that is found in many plant materials, including commonly eaten fruits and vegetables. The compound is well known for its wide range of biological activities. In this study, 5--acyl derivatives of quercetin were synthesised and assessed for their antiproliferative activity against the HCT116 colon cancer and MDA-MB-231 breast cancer cell lines; and their radical scavenging activity against the 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cation and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical species. Four derivatives were found to have improved the antiproliferative activity compared to quercetin whilst retaining radical scavenging activity.

摘要

槲皮素是一种类黄酮,存在于许多植物材料中,包括常见的食用水果和蔬菜。该化合物以其广泛的生物活性而闻名。在这项研究中,合成了槲皮素的 5-酰基衍生物,并评估了它们对 HCT116 结肠癌细胞和 MDA-MB-231 乳腺癌细胞系的增殖活性;以及它们对 2,2'-联氮双(3-乙基苯并噻唑啉-6-磺酸)(ABTS)自由基阳离子和 2,2-二苯基-1-苦基肼(DPPH)自由基的清除活性。发现四种衍生物在保持自由基清除活性的同时,提高了对槲皮素的增殖活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cffd/7999741/991c266cbd09/molecules-26-01608-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cffd/7999741/ddebb3911310/molecules-26-01608-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cffd/7999741/148ae1af1c9f/molecules-26-01608-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cffd/7999741/05f482a0a464/molecules-26-01608-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cffd/7999741/991c266cbd09/molecules-26-01608-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cffd/7999741/ddebb3911310/molecules-26-01608-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cffd/7999741/148ae1af1c9f/molecules-26-01608-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cffd/7999741/05f482a0a464/molecules-26-01608-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cffd/7999741/991c266cbd09/molecules-26-01608-g003.jpg

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