biochanin A OR C004541
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Both bifidobacteria and clostridia are part of the natural gut microflora and while clostridia may be responsible for severe intestinal infections, bifidobacteria are probiotic microorganisms belonging to the most important prospective bacteria in the bowel. The antimicrobial activity of biochanin A was tested in vitro against six Bifidobacterium spp., and eight Clostridium spp. using the broth microdilution method. Biochanin A showed an inhibition against all clostridia in the range of minimum inhibitory concentrations (MIC) from 64 microg/mL (for Cl. clostridioforme, strains DSM 933 and I3) to 1,024 microg/mL (for Cl. perfringens, DSM 11778). No bifidobacteria were suppressed at four-fold higher concentration (MICs > 4,096) than MIC of Cl. perfringens. These results indicate selective growth inhibition of biochanin A and its potential use in antimicrobial prevention and/or protection.
- MeSH
- antibakteriální látky farmakologie MeSH
- Bifidobacterium klasifikace účinky léků růst a vývoj MeSH
- Clostridium klasifikace účinky léků růst a vývoj MeSH
- druhová specificita MeSH
- genistein farmakologie MeSH
- lidé MeSH
- mikrobiální testy citlivosti MeSH
- střeva mikrobiologie MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
The dietary intake of flavonoids seems to be inversely related to cardiovascular mortality. The consumption of isoflavonoids is increasing in the general population, especially due to the use of food supplements and a variety of isoflavonoid-rich foods. However, detailed studies on the vascular influence of individual pure isoflavonoids are mostly missing. For this study, 16 isoflavonoids were initially screened for their vasorelaxant properties on rat aortas. The 2 most potent of them, biochanin A and glycitein, were further tested for the mechanism of action on porcine coronary arteries. They both induced an endothelium independent vascular relaxation, with EC50 below 6 and 17 µM, respectively. Biochanin A, but not glycitein, was able to block the vasoconstriction caused by KCl, CaCl2, serotonin, and U46619 in a dose-dependent manner. Another series of experiments suggested that the major mechanism of action of biochanin A was the inhibition of L-type calcium channels. Moreover, biochanin A in relatively small concentrations (2 - 4 µM) interfered with the cGMP, but not cAMP, pathway in isolated coronary arteries. These results indicate that some isoflavonoids, in particular biochanin A, are able to have vasodilatory effects in micromolar concentrations, which is of potential clinical interest for the management of cardiovascular pathologies.
- MeSH
- cévní endotel MeSH
- genistein MeSH
- isoflavony * MeSH
- koronární cévy MeSH
- krysa rodu rattus MeSH
- lidé MeSH
- prasata MeSH
- vápník MeSH
- vápníkové kanály * MeSH
- vazodilatace MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
Práce se zabývá vlivem různých růstových regulátorů při kultivaci kalusové kultury Genista tinctoria na MS médiu za různých světelných režimů na růst kultury a produkci isoflavonoidů. Z testovaných regulátorů byl největší růst kultury zjištěn při použití BAP 10 mg/l při nepřetržitém osvětlení. Při použití BAP 0,1 mg/l a za normálního světelného režimu produkce genistinu a daidzeninu byla dokonce vyšší než v intaktní rostlině. Z pěti stanovovaných isoflavonoidů byly v kalusové kultuře prokázány čtyři, a to: genistin, genistein, daidzein a formononetin. V intaktní rostlině se podařilo stanovit daidzein, genistein a biochanin A.
The paper deals with the effects of different growth regulators on the growth of the culture and production of isoflavonoids in the cultivation of the callus culture Genista tinctoria on MS medium under varying light regimens. Of the regulators tested, the highest growth of the culture was found when using BAP 10 mg/l under continuous lighting. With the use of BAP 0.1 mg/l and under normal light regimen, the production of genistine and daidzenin was even higher than in the intact plant. Of the five isoflavonoids determined, four were demonstrated in the callus culture: genistine, genistein, daidzein, and formononetin. In the intact plant the authors managed to determine daidzein, genistein, and biochanin A.
Firefly luciferase is susceptible to inhibition and stabilization by compounds under investigation for biological activity and toxicity. This can lead to false-positive results in in vitro cell-based assays. However, firefly luciferase remains one of the most commonly used reporter genes. Here, we evaluated isoflavonoids for inhibition of firefly luciferase. These natural compounds are often studied using luciferase reporter-gene assays. We used a quantitative structure-activity relationship (QSAR) model to compare the results of in silico predictions with a newly developed in vitro assay that enables concomitant detection of inhibition of firefly and Renilla luciferases. The QSAR model predicted a moderate to high likelihood of firefly luciferase inhibition for all of the 11 isoflavonoids investigated, and the in vitro assays confirmed this for seven of them: daidzein, genistein, glycitein, prunetin, biochanin A, calycosin, and formononetin. In contrast, none of the 11 isoflavonoids inhibited Renilla luciferase. Molecular docking calculations indicated that isoflavonoids interact favorably with the D-luciferin binding pocket of firefly luciferase. These data demonstrate the importance of reporter-enzyme inhibition when studying the effects of such compounds and suggest that this in vitro assay can be used to exclude false-positives due to firefly or Renilla luciferase inhibition, and to thus define the most appropriate reporter gene.
- MeSH
- isoflavony chemie metabolismus MeSH
- luciferasy renil chemie metabolismus MeSH
- reportérové geny genetika fyziologie MeSH
- sekundární struktura proteinů MeSH
- světluškovití MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
UNLABELLED: In this study, we tested 15 naturally occurring isoflavones and their metabolites for their possible antibacterial properties against nine Gram-positive and Gram-negative bacteria. The in vitro antibacterial activity was determined using the broth microdilution method, and the results were expressed as minimum inhibitory concentrations (MICs). 6,7,4'-trihydroxyisoflavone (demethyltexasin), 7,3',4'-trihydroxyisoflavone (hydroxydaidzein), 5,7-dihydroxy-4'-methoxyisoflavone (biochanin A), 7,8,4'-trihydroxyisoflavone (demethylretusin) and 5,7,4'-trihydroxyisoflavone (genistein) produced significant antibacterial activity (MICs ≥ 16 μg ml(-1)). The most effective compound, demethyltexasin, was subsequently tested for its growth-inhibitory effect against Staphylococcus aureus, and it exhibited significant antistaphylococcal effects against various standard strains and clinical isolates, including methicillin and tetracycline resistant ones with the MICs ranging from 16 to 128 μg ml(-1). SIGNIFICANCE AND IMPACT OF THE STUDY: The results of the structure-activity relationship (SAR) analysis identified ortho-dihydroxyisoflavones as a class of antibacterially effective compounds emphasizing the hydroxyl groups at C-5, 6 and 7 positions as crucial supposition for the antibacterial action of plant isoflavones and their metabolites. Demethyltexasin, an isoflavones' metabolite present in the human body through enterohepatic recycling of soya bean isoflavones (daidzein, genistein), showed the most potent antibacterial activity, especially against various strains of Staphylococcus aureus (including MDR and MRSA). The significance of this study is a deepening of the knowledge on isoflavones' SAR and identification of the antistaphylococcal activity of demethyltexasin, which suggest that metabolites of isoflavones can be even more potent antibacterial agents than their precursors.
- MeSH
- antibakteriální látky chemie farmakologie MeSH
- genistein farmakologie MeSH
- gramnegativní bakterie účinky léků MeSH
- isoflavony chemie farmakologie MeSH
- lidé MeSH
- methicilin farmakologie MeSH
- mikrobiální testy citlivosti MeSH
- rostlinné extrakty farmakologie MeSH
- Staphylococcus aureus účinky léků MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
