Elderberry Flavonoids Bind to and Prevent H1N1 Infection in-vitro

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Phytochemistry (Impact Factor: 2.55). 09/2009; 70(10):1255-61. DOI: 10.1016/j.phytochem.2009.06.003
Source: PubMed


A ionization technique in mass spectrometry called Direct Analysis in Real Time Mass Spectrometry (DART TOF-MS) coupled with a Direct Binding Assay was used to identify and characterize anti-viral components of an elderberry fruit (Sambucus nigra L.) extract without either derivatization or separation by standard chromatographic techniques. The elderberry extract inhibited Human Influenza A (H1N1) infection in vitro with an IC(50) value of 252+/-34 microg/mL. The Direct Binding Assay established that flavonoids from the elderberry extract bind to H1N1 virions and, when bound, block the ability of the viruses to infect host cells. Two compounds were identified, 5,7,3',4'-tetra-O-methylquercetin (1) and 5,7-dihydroxy-4-oxo-2-(3,4,5-trihydroxyphenyl)chroman-3-yl-3,4,5-trihydroxycyclohexanecarboxylate (2), as H1N1-bound chemical species. Compound 1 and dihydromyricetin (3), the corresponding 3-hydroxyflavonone of 2, were synthesized and shown to inhibit H1N1 infection in vitro by binding to H1N1 virions, blocking host cell entry and/or recognition. Compound 1 gave an IC(50) of 0.13 microg/mL (0.36 microM) for H1N1 infection inhibition, while dihydromyricetin (3) achieved an IC(50) of 2.8 microg/mL (8.7 microM). The H1N1 inhibition activities of the elderberry flavonoids compare favorably to the known anti-influenza activities of Oseltamivir (Tamiflu; 0.32 microM) and Amantadine (27 microM).

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    • "Researchers have linked elderberry products to anti-influenza (Roschek et al., 2009), antioxidant , anti-carcinogenic, anti-viral, and antibacterial activities (Werlein et al., 2005; Milbury et al., 2002; Tarascou et al., 2011). Elderberry products are also suggested to manifest an array of health promoting benefits such as oxidative stress protection, antiinflammatory effects and inhibition of some human tumor cells (Rodrigo et al., 2011; Kong et al., 2003; Elisia et al., 2007; Bagchi et al., 2006; Dreiseitel et al., 2008). "

    Full-text · Article · Jan 2015 · Acta horticulturae
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    • "1.5 g of N. sativa seeds (Frontier Natural Products Co-op, Norway, IA) was homogenized in 10 ml of 85% ethanol and incubated for 7 d at room temperature [46,47]. 32.0 g of S. nigra fruit (San Francisco Herb Company, San Francisco, CA) was homogenized in 40 ml of 80% ethanol and incubated for 4 d at room temperature [48]. Following these incubations, extract solutions were centrifuged at 1900 × g for 5 min at room temperature to remove debris and the remaining supernatant was syringe filtered through a 0.22 μm polyvinylidene fluoride membrane (Fisher Scientific Company, Fair Lawn, NJ). "
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    ABSTRACT: Infectious bronchitis virus (IBV) is a pathogenic chicken coronavirus. Currently, vaccination against IBV is only partially protective; therefore, better preventions and treatments are needed. Plants produce antimicrobial secondary compounds, which may be a source for novel anti-viral drugs. Non-cytotoxic, crude ethanol extracts of Rhodiola rosea roots, Nigella sativa seeds, and Sambucus nigra fruit were tested for anti-IBV activity, since these safe, widely used plant tissues contain polyphenol derivatives that inhibit other viruses. Dose-response cytotoxicity curves on Vero cells using trypan blue staining determined the highest non-cytotoxic concentrations of each plant extract. To screen for IBV inhibition, cells and virus were pretreated with extracts, followed by infection in the presence of extract. Viral cytopathic effect was assessed visually following an additional 24 h incubation with extract. Cells and supernatants were harvested separately and virus titers were quantified by plaque assay. Variations of this screening protocol determined the effects of a number of shortened S. nigra extract treatments. Finally, S. nigra extract-treated virions were visualized by transmission electron microscopy with negative staining.Virus titers from infected cells treated with R. rosea and N. sativa extracts were not substantially different from infected cells treated with solvent alone. However, treatment with S. nigra extracts reduced virus titers by four orders of magnitude at a multiplicity of infection (MOI) of 1 in a dose-responsive manner. Infection at a low MOI reduced viral titers by six orders of magnitude and pretreatment of virus was necessary, but not sufficient, for full virus inhibition. Electron microscopy of virions treated with S. nigra extract showed compromised envelopes and the presence of membrane vesicles, which suggested a mechanism of action. These results demonstrate that S. nigra extract can inhibit IBV at an early point in infection, probably by rendering the virus non-infectious. They also suggest that future studies using S. nigra extract to treat or prevent IBV or other coronaviruses are warranted.
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    • "It is difficult to gauge U.S. commercial interest in S. canadensis fruit, although elderberry dietary supplements are top selling products in Europe and North America [2] [9]. European and American elderberries have purported health benefits, including anti-inflammatory, antibacterial and antiviral properties [1] [17] [24], and the pigments offer use as food colorants [5]. In elderberry, anthocyanins are derivatives of cyanidin-glycosides [10] [13] [22] [23]. "
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    ABSTRACT: BACKGROUND: Elderberry (Sambucus spp.) fruit are used for food and dietary supplements in Europe and North America, and contain large amounts of cyanidin-based anthocyanins and other phenolics that may benefit human health. OBJECTIVES: Information on the effect of both genotype and production environment on elderberry juice characteristics is needed in order to optimize production of quality food and dietary supplements. METHODS: The characteristics of elderberry fruits relative to genetic and production environment were evaluated from 12 American elderberry genotypes at three U.S. sites (two in Missouri and one in Oregon) over three growing seasons. Additional genotypes of American and European elderberry were studied at the Oregon site. RESULTS: Location, genotype, and growing season influenced pH, soluble solids, titratable acidity, total phenolics, and total anthocyanins. Elderberries grown in Oregon were consistently higher in acidity than those grown in Missouri. Differences in acidity and anthocyanin with environment were dependent on genotype. Non-acylated anthocyanins and flavonol-glycosides were more influenced by location than by genotype. CONCLUSION: 'Bob Gordon' and 'Adams 2' genotypes, which are good producers in diverse environments, were significantly higher in total phenolic and total anthocyanin contents in all locations, and may be good selections for producing juices, wines, or health products.
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