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蒽醌类化合物对致病原生动物、细菌和真菌的抑制活性及其与结构的关系。

The Inhibitory Activity of Anthraquinones against Pathogenic Protozoa, Bacteria, and Fungi and the Relationship to Structure.

机构信息

Healthy Processed Foods Research Unit, Agricultural Research Service, United States Department of Agriculture, Albany, CA 94710, USA.

Department of Biological Sciences, University of the Pacific, Stockton, CA 95211, USA.

出版信息

Molecules. 2020 Jul 7;25(13):3101. doi: 10.3390/molecules25133101.

DOI:10.3390/molecules25133101
PMID:32646028
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7411742/
Abstract

Plant-derived anthraquinones were evaluated in cell assays for their inhibitory activities against the parasitic protozoa human strain G3 that causes the sexually transmitted disease trichomoniasis in women, bovine strain D1 that causes sexually transmitted diseases in farm animals (bulls, cows, and pigs), -like strain C1 that causes diarrhea in domestic animals (cats and dogs), and bacteria and fungi. The anthraquinones assessed for their inhibitory activity were anthraquinone, aloe-emodin (1,8-dihydroxy-3-hydroxymethylanthraquinone), anthrarufin (1,5-dihydroxyanthraquinone), chrysazin (1,8-dihydroxyanthraquinone), emodin (1,3,8-trihydroxy-6-methylanthraquinone), purpurin (1,2,4-trihydroxyanthraquinone), and rhein (1,8-dihydroxy-3-carboxyanthraquinone). Their activities were determined in terms of IC values, defined as the concentration that inhibits 50% of the cells under the test conditions and calculated from linear dose response plots for the parasitic protozoa, and zone of inhibition for bacteria and fungi, respectively. The results show that the different substituents on the anthraquinone ring seem to influence the relative potency. Analysis of the structure-activity relationships in protozoa indicates that the aloe-emodin and chrysazin with the highest biological activities merit further study for their potential to help treat the diseases in women and domestic and farm animals. Emodin also exhibited antifungal activity against . The suggested mechanism of action and the additional reported beneficial biological properties of anthraquinones suggest that they have the potential to ameliorate a broad spectrum of human diseases.

摘要

植物来源的蒽醌类化合物在细胞实验中评估了其对寄生原生动物的抑制活性,这些原生动物包括引起女性性传播疾病滴虫病的人类株 G3、引起农场动物(公牛、母牛和猪)性传播疾病的牛株 D1、引起家畜(猫和狗)腹泻的类似株 C1,以及细菌和真菌。评估其抑制活性的蒽醌类化合物包括蒽醌、芦荟大黄素(1,8-二羟基-3-羟甲基蒽醌)、蒽蒽酮(1,5-二羟基蒽醌)、 Chrysazin(1,8-二羟基蒽醌)、大黄素(1,3,8-三羟基-6-甲基蒽醌)、大黄素(1,2,4-三羟基蒽醌)和大黄素(1,8-二羟基-3-羧基蒽醌)。它们的活性是根据 IC 值来确定的,IC 值定义为在测试条件下抑制 50%细胞的浓度,并根据寄生原生动物的线性剂量反应图以及细菌和真菌的抑制区来计算。结果表明,蒽醌环上的不同取代基似乎会影响相对效力。对原生动物的结构-活性关系进行分析表明,具有最高生物活性的芦荟大黄素和 Chrysazin 值得进一步研究,以评估它们在治疗女性和家庭及农场动物疾病方面的潜力。大黄素也表现出对 的抗真菌活性。作用机制的建议和蒽醌类化合物的其他报道的有益的生物学特性表明,它们有可能改善广泛的人类疾病。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fe1/7411742/2a9cf10522db/molecules-25-03101-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fe1/7411742/2a9cf10522db/molecules-25-03101-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fe1/7411742/2a9cf10522db/molecules-25-03101-g001.jpg

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