Anti-influenza virus activity of biflavonoids

Miki, Kazuhiko; Nagai, Takayuki; Suzuki, Kazushige; Tsujimura, Ryo; Koyama, Kiyotaka; Kinoshita, Kaoru; Furuhata, Kimio; Yamada, Hideaki; Takahashi, Kunio

doi:10.1016/j.bmcl.2006.10.075

Cited by 97 publications

(53 citation statements)

References 12 publications

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“…Amentoflavone stimulates mitochondrial dysfunction and induces apoptotic cell death in yeast (Hwang et al 2012). The biflavonoid ginkgetin is cytotoxic to human ovarian adenocarcinoma and is also effective against the flu virus ( Kim et al 2008;Miki et al 2007). We review below the potent anti-oxidant, anti-inflammatory, anti-acetylcholinesterase, "-secretase inhibiting, and anti-amyloidogenic properties of biflavonoids that have been reported to contribute to their beneficial effects in AD.…”

Section: Beneficial Roles Of Biflavonoids In Alzheimer's Diseasementioning

confidence: 96%

Biflavonoids as Potential Small Molecule Therapeutics for Alzheimer’s Disease

Thapa

2015

Advances in Experimental Medicine and Biology

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Flavonoids are naturally occurring phytochemicals found in a variety of fruits and vegetables and offer color, flavor, aroma, nutritional and health benefits. Flavonoids have been found to play a neuroprotective role by inhibiting and/or modifying the self-assembly of the amyloid-β (Aβ) peptide into oligomers and fibrils, which are linked to the pathogenesis of Alzheimer's disease. The neuroprotective efficacy of flavonoids has been found to strongly depend on their structure and functional groups. Flavonoids may exist in monomeric, as well as di-, tri-, tetra- or polymeric form through C-C or C-O-C linkages. It has been shown that flavonoids containing two or more units, e.g., biflavonoids, exert greater biological activity than their respective monoflavonoids. For instance, biflavonoids have the ability to distinctly alter Aβ aggregation and more effectively reduce the toxicity of Aβ oligomers compared to the monoflavonoid moieties. Although the molecular mechanisms remain to be elucidated, flavonoids have been shown to alter the Aβ aggregation pathway to yield non-toxic, unstructured Aβ aggregates, as well as directly exerting a neuroprotective effect to cells. In this chapter, we review biflavonoid-mediated Aβ aggregation and toxicity, and highlight the beneficial roles biflavonoids can potentially play in the prevention and treatment of Alzheimer's disease.

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Section: Beneficial Roles Of Biflavonoids In Alzheimer's Diseasementioning

confidence: 96%

Biflavonoids as Potential Small Molecule Therapeutics for Alzheimer’s Disease

Thapa

2015

Advances in Experimental Medicine and Biology

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“…Biflavonoids are flavonoid dimers that have been attached to each other by either C-C or C-O-C bonds representing a variety of chemical structures [2]. Several biological activities such as antioxidant [3,4], antiviral [5], hypolipidemic [6], antidiabetic [7], anti-tumoral [8], antituberculosis [9], antimalarial [10], antibacterial [11], antifungal [12], and anti-inflammatory [13] effects have been reported for biflavonoids.…”

Section: Introductionmentioning

confidence: 99%

Molecular docking and quantum mechanical studies on biflavonoid structures as BACE-1 inhibitors

et al. 2014

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Beta-site amyloid precursor protein cleaving enzyme (BACE-1) is a well-known therapeutic target for Alzheimer disease (AD) due to its characteristic role in the pathogenesis of AD. Numerous researches have been focused on the design and development of potent peptidic and nonpeptidic BACE-1 inhibitors. In the present contribution, a series of experimentally validated biflavonoid BACE-1 inhibitors (1-21) were subjected to our structure-based molecular modeling studies. Binding modes were elucidated through molecular docking in the active site of the enzyme. Relatively good correlations between the theoretical and experimental binding affinities could be achieved (R 2 = 0.61). Analysis of intermolecular binding energy components was performed via functional B3LYP in association with splitvalence basis set using polarization functions (Def2-SVP), and structure-binding relationships were further elucidated through ligand-residue binding energies. Since little studies have been performed on the modeling and structure activity/binding relationships of biflavonoid structures as BACE-1 inhibitors, the results of this study may be useful in further extending the scope of biflavonoid structures as potential anti-Alzheimer scaffolds.

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“…Many reports in the literature describe neuraminidase inhibitor assays relying on the cumbersome use of the influenza virus preparations 1,[8][9][10][11][12] . This procedure is risky, costly and inconvenient for the set-up of a screening assay.…”

Section: Research Articlementioning

confidence: 99%