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Molecules 2017, 22(3), 431; doi:10.3390/molecules22030431

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

1
School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China
2
Beijing Institute of Traditional Chinese Medicine, Beijing Hospital of Traditional Chinese Medicine Affiliated to Capital Medical University, Beijing 100000, China
3
Institute of Laboratory Animal Sciences, Chinese Academy of Medical Sciences & Peking Union Medical College (CAMS&PUMC), Beijing 100730, China
4
School of Basic Medical Science, Beijing University of Chinese Medicine, Beijing 100029, China
5
College of Pharmacy, China Pharmaceutical University, Nanjing 211198, China
*
Author to whom correspondence should be addressed.
Academic Editor: Thomas J. Schmidt
Received: 6 December 2016 / Revised: 28 February 2017 / Accepted: 2 March 2017 / Published: 8 March 2017
(This article belongs to the Section Natural Products)
View Full-Text   |   Download PDF [4866 KB, uploaded 8 March 2017]   |  

Abstract

For screening the active phloroglucinols on influenza virus (H5N1) from Dryopteris crassirhizoma NaKai, a database was established including twenty-three phloroglucinols that had been isolated from Dryopteris crassirhizoma. 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 D. crassirhizoma 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 IC50 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 (TC50 > 400 μM) against influenza virus (H5N1) which will have to be investigated in further detail. In conclusion, phloroglucinols from D. crassirhizoma 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. View Full-Text
Keywords: Dryopteris crassirhizoma; phloroglucinols; influenza virus H5N1; neuraminidase; dryocrassin ABBA Dryopteris crassirhizoma; phloroglucinols; influenza virus H5N1; neuraminidase; dryocrassin ABBA
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Wang, J.; Yan, Y.-T.; Fu, S.-Z.; Peng, B.; Bao, L.-L.; Zhang, Y.-L.; Hu, J.-H.; Zeng, Z.-P.; Geng, D.-H.; Gao, Z.-P. Anti-Influenza Virus (H5N1) Activity Screening on the Phloroglucinols from Rhizomes of Dryopteris crassirhizoma. Molecules 2017, 22, 431.

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