• Title/Summary/Keyword: Neuraminidase inhibitor

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Neuraminidase Inhibitors from the Fruiting Body of Phellinus igniarius

  • Kim, Ji-Yul;Kim, Dae-Won;Hwang, Byung Soon;Woo, E-Eum;Lee, Yoon-Ju;Jeong, Kyeong-Woon;Lee, In-Kyoung;Yun, Bong-Sik
    • Mycobiology
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    • v.44 no.2
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    • pp.117-120
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    • 2016
  • During our ongoing investigation of neuraminidase inhibitors from medicinal fungi, we found that the fruiting bodies of Phellinus igniarius exhibited significant inhibitory activity against neuraminidase from recombinant H3N2 influenza viruses. Two active compounds were isolated from the methanolic extract of P. igniarius through solvent partitioning and Sephadex LH-20 column chromatography. The active compounds were identified as phelligridins E and G on proton nuclear magnetic resonance ($^1H$ NMR) and electrospray ionization mass measurements. These compounds inhibited neuraminidases from recombinant rvH1N1, H3N2, and H5N1 influenza viruses, with $IC_{50}$ values in the range of $0.7{\sim}8.1{\mu}M$.

Identification of Suitable Natural Inhibitor against Influenza A (H1N1) Neuraminidase Protein by Molecular Docking

  • Sahoo, Maheswata;Jena, Lingaraja;Rath, Surya Narayan;Kumar, Satish
    • Genomics & Informatics
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    • v.14 no.3
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    • pp.96-103
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    • 2016
  • The influenza A (H1N1) virus, also known as swine flu is a leading cause of morbidity and mortality since 2009. There is a need to explore novel anti-viral drugs for overcoming the epidemics. Traditionally, different plant extracts of garlic, ginger, kalmegh, ajwain, green tea, turmeric, menthe, tulsi, etc. have been used as hopeful source of prevention and treatment of human influenza. The H1N1 virus contains an important glycoprotein, known as neuraminidase (NA) that is mainly responsible for initiation of viral infection and is essential for the life cycle of H1N1. It is responsible for sialic acid cleavage from glycans of the infected cell. We employed amino acid sequence of H1N1 NA to predict the tertiary structure using Phyre2 server and validated using ProCheck, ProSA, ProQ, and ERRAT server. Further, the modelled structure was docked with thirteen natural compounds of plant origin using AutoDock4.2. Most of the natural compounds showed effective inhibitory activity against H1N1 NA in binding condition. This study also highlights interaction of these natural inhibitors with amino residues of NA protein. Furthermore, among 13 natural compounds, theaflavin, found in green tea, was observed to inhibit H1N1 NA proteins strongly supported by lowest docking energy. Hence, it may be of interest to consider theaflavin for further in vitro and in vivo evaluation.

Antioxidative Effect and Neuraminidase Inhibitory Activity of Polyphenols Isolated from a New Korean Red Waxy Sorghum (Sorghum bicolor L. cv. Hwanggeumchalsusu) (황금찰수수(Sorghum bicolor L. cv. Hwanggeumchalsusu) 유래 에탄올 추출물 및 폴리페놀계 화합물의 항산화 활성 및 뉴라미니데이즈 억제 효과)

  • Ra, Ji-Eun;Seo, Kyung Hye;Ko, Jee Yeon;Lee, Mi-Ja;Kang, Hyeon Jung;Kim, Sun Lim;Chung, Ill-Min;Seo, Woo Duck
    • Journal of Life Science
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    • v.25 no.7
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    • pp.786-794
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    • 2015
  • To identify nutritional and therapeutic properties of the new Korean red waxy sorghum cultivar ‘Hwanggeumchalsusu (HGC)’, we assayed the antioxidative effects and neuraminidase inhibitory activity. A methanol and 70% ethanol extract of HGC exhibited strong antioxidative effects (IC50 values of 83.2±2.7 for DPPH) and 85.6±2.4 μg/ml for ABTS) and neuraminidase (ND) inhibitory activity (IC50 values of 1.8±0.1 from extracted with methanol and 3.4±0.1 μg/ml from extracted with 70% ethanol) compared with that of the control, noncolored sorghum cultivar ‘Huinchalsusu (HC)’ (IC50> 200 μg/ml). We isolated nine polyphenols, Gallic acid (1), Protocatecuic acid (2), p-Hydroxy benzoic acid (3), Vanillic acid (4), Caffeic acid (5), Ferulic acid (6), Luteolinidin (7), Apigeninidin (8), Luteolin (9), from the HGC - methanol extract, to determine whether they were the active components Luteolinidin of one kind of polyphenols from the HGC, exhibited significant antioxidative effects (IC50 values of 10.9±0.5 μM for DPPH and 8.6 0.6 μM for ABTS) and neuraminidase (ND) inhibitory activity (IC50 values of 26.3±0.6) showed noncompetitive inhibition model. The binding affinity of the ND inhibitors in molecular docking experiments correlated with their ND inhibitory activities. These results suggest that HGC may be utilized to serve as a potential effective antioxidant and inhibitor of ND.

Purification and Characterization of a New Galactoside Specific Lectin from Trichosanthes kirilowii Root

  • Yun, Doo-Hee;Park, Eun-Ju;Park, Jong-Ok;Lee, Young-Han;Seo, Jeong-Kon;Ryu, Sung-Ho;Suh, Pann-Ghill;Kim, Hee-Sook
    • BMB Reports
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    • v.28 no.1
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    • pp.6-11
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    • 1995
  • A new lectin, named TRA, was purified from Trichosanthes kirilowii root by acid-treated Sepharose 6B, Mono-Q, and TSK-gel 3000SW column sequential chromatography. The lectin appeared homogeneous by native gel electrophoresis at pH 4.3 and gave two protein bands of Mr=31 and 28 kDa by SDS-PAGE. The N-terminal amino acid sequences of the polypeptides of TRA have not been reported in amino acid sequences of the lectins. TRA lectin formed a precipitate with asialofetuin, neuraminidase-treated fetuin. A sugar inhibition assay indicated that N-acetyl-D-galactosamine, among the monosaccharides tested, was the most potent inhibitor of TRA-induced hemagglutination. Asialofetuin showed a 260-times stronger inhibitory activity than N-acetyl-D-galactosamine. TRA lectin also showed agglutination with normal leukocytes and lymphoma cells, but not with premature hemopoietic cells. These results suggest that TRA is a novel plant lectin.

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Antiviral Activity of Plant-derived Natural Products against Influenza Viruses (식물 유래 천연물의 인플루엔자에 대한 항바이러스 활성)

  • Kim, Seonjeong;Kim, Yewon;Kim, Ju Won;Hwang, Yu-bin;Kim, Seong Hyeon;Jang, Yo Han
    • Journal of Life Science
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    • v.32 no.5
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    • pp.375-390
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    • 2022
  • Influenza viruses are zoonotic respiratory pathogens, and influenza infections have caused a substantial burden on public health systems and the livestock industry. Although currently approved seasonal influenza vaccines have shown potent protection efficacy against antigenically well-matched strains, there are considerable unmet needs for the efficient control of viral infections. Enormous efforts have been made to develop broadly protective universal influenza vaccines to tackle the huge levels of genetic diversity and variability of influenza viruses. In addition, antiviral drugs have been considered important interventions for the treatment of viral infections. The viral neuraminidase inhibitor oseltamivir is the most widely used antiviral medication to treat influenza A and influenza B viruses. However, unsatisfactory clinical outcomes resulting from side effects and the emergence of resistant variants have led to greater attention being paid to plants as a natural resource for anti-influenza drugs. In particular, the recent COVID-19 pandemic has underpinned the need for safe and effective antiviral drugs with a broad spectrum of antiviral activity to prevent the rapid spread of viruses among humans. This review outlines the results of the antiviral activities of various natural products isolated from plants against influenza viruses. Special focus is paid to the virucidal effects and the immune-enhancing effects of antiviral natural products, since the products have broad applications as inactivating agents for the preparation of inactivated vaccines and vaccine adjuvants.