Mechanisms Underlying Diquertin-Mediated Regulation of Neutrophil Function in Patients with Non-Insulin-Dependent Diabetes Mellitus

Fedosova, N. F.; Alisievich, S. V.; Lyadov, K. V.; Romanova, E.P.; Rud'ko, I. A.; Kubatiev, A. A.

doi:10.1023/b:bebm.0000028124.90768.50

Cited by 6 publications

(4 citation statements)

References 9 publications

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“…As a ubiquitous constituent of foods and herbs, taxifolin is consumed regularly in the human diet and exerts a wide range of biochemical and pharmacological effects; these include antioxidant [9,10], antitumor [11] and anti-inflammatory effects [12], the prevention of Alzheimer’s disease [13], antidiabetic [14,15], antiviral [16], antimicrobial [17], hepatoprotective [18], cardioprotective [15,19], neuroprotective [20] and immunoregulatory effects [21], and xanthine oxidase inhibition [22]. Additionally, experimental data indicate that taxifolin use is safe and nontoxic [2,23].…”

Section: Introductionmentioning

confidence: 99%

Detection of 191 Taxifolin Metabolites and Their Distribution in Rats Using HPLC-ESI-IT-TOF-MSn

Yang

et al. 2016

Molecules

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Abstract:Taxifolin is a ubiquitous bioactive constituent of foods and herbs. To thoroughly explore its metabolism in vivo, an HPLC-ESI-IT-TOF-MS n method combined with specific metabolite detection strategy was used to detect and identify the metabolites of taxifolin in rats. Of the 191 metabolites tentatively identified, 154 were new metabolites, 69 were new compounds and 32 were dimers. This is the first report of the in vivo biotransformation of a single compound into more than 100 metabolites. Furthermore, acetylamination and pyroglutamic acid conjugation were identified as new metabolic reactions. Seventeen metabolites were found to have various taxifolin-related bioactivities. The potential targets of taxifolin and 63 metabolites were predicted using PharmMapper, with results showing that more than 60 metabolites have the same five targets. Metabolites with the same fragment pattern may have the same pharmacophore. Thus these metabolites may exert the same pharmacological effects as taxifolin through an additive effect on the same drug targets. This observation indicates that taxifolin is bioactive not only in the parent form, but also through its metabolites. These findings enhance understanding of the metabolism and effective forms of taxifolin and may provide further insight of the beneficial effects of taxifolin and its derivatives.

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Section: Introductionmentioning

confidence: 99%

Detection of 191 Taxifolin Metabolites and Their Distribution in Rats Using HPLC-ESI-IT-TOF-MSn

Yang

et al. 2016

Molecules

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“…Oxidative stress has a potential role in the pathogenesis of diabetes. Fedosova et al found that quercetin could reduce the oxidative function of polymorphonuclear neutrophils (PMN) in patients with non-insulin-dependent diabetes mellitus (NIDDM) [ 76 ]. Quercetin exerted its antioxidant effects by directly inhibiting the production of lipid peroxides, such as malondialdehyde (MDA) and thiobarbituric acid-reactive substances (TBARS), and indirectly promoting the production of endogenous antioxidants, such as antioxidant enzymes glutathione peroxidase (GSH-Px), superoxide dismutase (SOD), and catalase (CAT), in STZ-induced diabetic rats and db/db mice [ 55 , 75 , 77 – 85 ].…”

Section: Pharmacological Effects and Molecular Mechanisms Of Quercetin Against Three Metabolic Diseasesmentioning

confidence: 99%

The Therapeutic Effects and Mechanisms of Quercetin on Metabolic Diseases: Pharmacological Data and Clinical Evidence

Huan

Peng²,

et al. 2021

Oxidative Medicine and Cellular Longevity

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Metabolic diseases have become major public health issues worldwide. Searching for effective drugs for treating metabolic diseases from natural compounds has attracted increasing attention. Quercetin, an important natural flavonoid, is extensively present in fruits, vegetables, and medicinal plants. Due to its potentially beneficial effects on human health, quercetin has become the focus of medicinal attention. In this review, we provide a timely and comprehensive summary of the pharmacological advances and clinical data of quercetin in the treatment of three metabolic diseases, including diabetes, hyperlipidemia, and nonalcoholic fatty liver disease (NAFLD). Accumulating evidences obtained from animal experiments prove that quercetin has beneficial effects on these three diseases. It can promote insulin secretion, improve insulin resistance, lower blood lipid levels, inhibit inflammation and oxidative stress, alleviate hepatic lipid accumulation, and regulate gut microbiota disorders in animal models. However, human clinical studies on the effects of quercetin in diabetes, hyperlipidemia, and NAFLD remain scarce. More clinical trials with larger sample sizes and longer trial durations are needed to verify its true effectiveness in human subjects. Moreover, another important issue that needs to be resolved in future research is to improve the bioavailability of quercetin. This review may provide valuable information for the basic research, drug development, and clinical application of quercetin in the treatment of metabolic diseases.

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“…With highly oxidizable flavonoids (e.g., quercetin), autoxidation can take place and has been investigated in physiological conditions (pH 7.5 aqueous buffers) 25,26. The investigations also showed that the secondary products of flavonoid oxidation may have deleterious consequences in biological systems 27–35.…”

Section: Introductionmentioning

confidence: 98%

Kinetics of inhibition of peroxidase activity of myeloperoxidase by quercetin

Momić

Vujčić

Vasić

2008

Int J of Chemical Kinetics

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The inhibition of myeloperoxidase (MPO), isolated from human neutrophils, by quercetin was investigated by following peroxidase activity of the enzyme using o-dianisidine as the substrate. The inhibition parameters (IC 50 ) were obtained by graphical analysis of the inhibition curves. A reaction mechanism, which involved the enzyme inhibition by quercetin and H 2 O 2 in excess, was proposed. The rate and equilibrium constants for the proposed reaction path were calculated from experimental data. Kinetic analysis in noninhibiting H 2 O 2 concentration range in the absence and the presence of quercetin revealed that the reaction mechanism underwent Michaelis-Menten kinetics. K app,H 2 O 2 m and V app max values indicated that quercetin was a mixed inhibitor of MPO activity. The initial reaction rates were recalculated using the obtained results. Calculated curves fitted the experimental results within the range of experimental error.

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Mechanisms Underlying Diquertin-Mediated Regulation of Neutrophil Function in Patients with Non-Insulin-Dependent Diabetes Mellitus

Cited by 6 publications

References 9 publications

Detection of 191 Taxifolin Metabolites and Their Distribution in Rats Using HPLC-ESI-IT-TOF-MSn

Detection of 191 Taxifolin Metabolites and Their Distribution in Rats Using HPLC-ESI-IT-TOF-MSn

The Therapeutic Effects and Mechanisms of Quercetin on Metabolic Diseases: Pharmacological Data and Clinical Evidence

Kinetics of inhibition of peroxidase activity of myeloperoxidase by quercetin

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