title: Anti-Influenza Virus (H5N1) Activity Screening on the Phloroglucinols from Rhizomes of Dryopteris crassirhizoma.
abstract: For screening the active phloroglucinols on influenza virus (H5N1) fromDryopteris crassirhizomaNaKai, a database was established including twenty-three phloroglucinols that had been isolated fromDryopteris 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 ofD. crassirhizomawere 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 IC50as 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 fromD. crassirhizomawere 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.
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China. juan_wangli@163.com.
authors.forename: Juan
authors.initials: J
authors.lastname: Wang
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China. yanyt296@163.com.
authors.forename: Yan-Tao
authors.initials: YT
authors.lastname: Yan
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China. fushenzhen1988@163.com.
authors.forename: Shen-Zhen
authors.initials: SZ
authors.lastname: Fu
authors.affiliation: Beijing Institute of Traditional Chinese Medicine, Beijing Hospital of Traditional Chinese Medicine Affiliated to Capital Medical University, Beijing 100000, China. pengbing126@126.com.
authors.forename: Bing
authors.initials: B
authors.lastname: Peng
authors.affiliation: Institute of Laboratory Animal Sciences, Chinese Academy of Medical Sciences & Peking Union Medical College (CAMS&PUMC), Beijing 100730, China. bllmsl@aliyun.com.
authors.forename: Lin-Lin
authors.initials: LL
authors.lastname: Bao
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China. collean_zhang@163.com.
authors.forename: Yan-Ling
authors.initials: YL
authors.lastname: Zhang
authors.affiliation: School of Basic Medical Science, Beijing University of Chinese Medicine, Beijing 100029, China. hujhbj@163.com.
authors.forename: Jing-Hong
authors.initials: JH
authors.lastname: Hu
authors.affiliation: Beijing Institute of Traditional Chinese Medicine, Beijing Hospital of Traditional Chinese Medicine Affiliated to Capital Medical University, Beijing 100000, China. zzp600@sohu.com.
authors.forename: Zu-Ping
authors.initials: ZP
authors.lastname: Zeng
authors.affiliation: College of Pharmacy, China Pharmaceutical University, Nanjing 211198, China. gengdonghao@163.com.
authors.forename: Dong-Hao
authors.initials: DH
authors.lastname: Geng
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China. gaozp@bucm.edu.cn.
authors.forename: Zeng-Ping
authors.initials: ZP
authors.lastname: Gao
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000737:chemistry* / Q000494:pharmacology*; D001665:Binding Sites; D020134:Catalytic Domain; D032492:Dryopteris / Q000737:chemistry*; D004789:Enzyme Activation / Q000187:drug effects; D006801:Humans; D053124:Influenza A Virus, H5N1 Subtype / Q000187:drug effects*; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D008968:Molecular Conformation; D062105:Molecular Docking Simulation; D009439:Neuraminidase / Q000037:antagonists & inhibitors / Q000737:chemistry; D010696:Phloroglucinol / Q000737:chemistry* / Q000494:pharmacology*; D011485:Protein Binding; D021281:Quantitative Structure-Activity Relationship; D027343:Rhizome / Q000737:chemistry*; D021241:Spectrometry, Mass, Electrospray Ionization; D014764:Viral Proteins / Q000037:antagonists & inhibitors / Q000737:chemistry
chemical_list: D000998:Antiviral Agents; D014764:Viral Proteins; D010696:Phloroglucinol; C487630:NA protein, influenza A virus; D009439:Neuraminidase
keywords: Dryopteris crassirhizoma; dryocrassin ABBA; influenza virus H5N1; neuraminidase; phloroglucinols