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粗茎鳞毛蕨根茎中间苯三酚类化合物的抗甲型流感病毒（H5N1）活性筛选

Anti-Influenza Virus (H5N1) Activity Screening on the Phloroglucinols from Rhizomes of Dryopteris crassirhizoma.

作者信息

Wang Juan, Yan Yan-Tao, Fu Shen-Zhen, Peng Bing, Bao Lin-Lin, Zhang Yan-Ling, Hu Jing-Hong, Zeng Zu-Ping, Geng Dong-Hao, Gao Zeng-Ping

机构信息

School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.

Beijing Institute of Traditional Chinese Medicine, Beijing Hospital of Traditional Chinese Medicine Affiliated to Capital Medical University, Beijing 100000, China.

出版信息

Molecules. 2017 Mar 8;22(3):431. doi: 10.3390/molecules22030431.

DOI:10.3390/molecules22030431
PMID:28282885
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6155227/
Abstract

For screening the active phloroglucinols on influenza virus (H5N1) from NaKai, a database was established including twenty-three phloroglucinols that had been isolated from . Their inhibitory effect on the neuraminidase (NA) of influenza virus H5N1 was screened by molecular docking. As a result, three candidates were selected. The rhizomes of were subjected to isolation and purification processes to obtain the inhibitor candidates. Thirteen phloroglucinols were obtained, including three selected candidates and two new phloroglucinols. The five phloroglucinols were investigated for their inhibitory activity on NA in vitro. The results showed that dryocrassin ABBA and filixic acid ABA exhibited inhibitory effects on NA with IC as 18.59 ± 4.53 and 29.57 ± 2.48 μM, respectively, and the other three phloroglucinols showed moderate inhibitory activity. Moreover, the anti-influenza virus (H5N1) activity and cytotoxicity of dryocrassin ABBA and filixic acid ABA were tested on Madin-Darby canine kidney (MDCK) cells with the cell counting kit-8 (CCK8) method. The results confirmed that dryocrassin ABBA exhibited an inhibitory activity with low cytotoxicity (TC > 400 μM) against influenza virus (H5N1) which will have to be investigated in further detail. In conclusion, phloroglucinols from were shown to have anti-influenza virus activity, and especially dryocrassin ABBA, one of the phloroglucinols, may have the potential to control influenza virus (H5N1) infection.

摘要

为了从NaKai中筛选对流感病毒（H5N1）有活性的间苯三酚，建立了一个数据库，其中包含从……分离出的23种间苯三酚。通过分子对接筛选它们对流感病毒H5N1神经氨酸酶（NA）的抑制作用。结果，选出了3个候选物。对……的根茎进行分离和纯化以获得候选抑制剂。得到了13种间苯三酚，包括3个选定的候选物和2种新的间苯三酚。研究了这5种间苯三酚在体外对NA的抑制活性。结果表明，绵马酸ABBA和绵马酸ABA对NA有抑制作用，IC分别为18.59±4.53和29.57±2.48μM，其他3种间苯三酚显示出中等抑制活性。此外，采用细胞计数试剂盒-8（CCK8）法在Madin-Darby犬肾（MDCK）细胞上测试了绵马酸ABBA和绵马酸ABA的抗流感病毒（H5N1）活性和细胞毒性。结果证实，绵马酸ABBA对流感病毒（H5N1）具有低细胞毒性（TC>400μM）的抑制活性，有待进一步详细研究。总之，来自……的间苯三酚显示出具有抗流感病毒活性，尤其是其中一种间苯三酚绵马酸ABBA，可能具有控制流感病毒（H5N1）感染的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/aa2fcce51e65/molecules-22-00431-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/908bc46512d0/molecules-22-00431-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/4a0ac465a397/molecules-22-00431-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/15e569178d51/molecules-22-00431-g003a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/96905696e6bf/molecules-22-00431-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/ce0acbc8e271/molecules-22-00431-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/0ba0e055e52d/molecules-22-00431-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/fe6b2be479ed/molecules-22-00431-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/e2d4a4a70637/molecules-22-00431-g006a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/860a6298b8c9/molecules-22-00431-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/aa2fcce51e65/molecules-22-00431-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/908bc46512d0/molecules-22-00431-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/4a0ac465a397/molecules-22-00431-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/15e569178d51/molecules-22-00431-g003a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/96905696e6bf/molecules-22-00431-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/ce0acbc8e271/molecules-22-00431-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/0ba0e055e52d/molecules-22-00431-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/fe6b2be479ed/molecules-22-00431-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/e2d4a4a70637/molecules-22-00431-g006a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/860a6298b8c9/molecules-22-00431-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fb2/6155227/aa2fcce51e65/molecules-22-00431-g008.jpg

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