Phenolic Derivatives from <i>Ruprechtia polystachya</i> and Their Inhibitory Activities on the Glucose‐6‐phosphatase System

Abreu, M. Bruzual De; Temraz, Abeer; Malafronte, Nicola; González-Mujica, Freddy; Duqué, Sandra; Braca, Alessandra

doi:10.1002/cbdv.201000334

Cited by 16 publications

(2 citation statements)

References 29 publications

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“…Chemistry: Compounds 4, 10, [34] 12, [35] 19, [36] 22, [37] 24, [38] and 25 [39] were isolated from various plant extracts, as previously reported. Quercetin 8 was obtained from Sigma-Aldrich.…”

Section: Methodsmentioning

confidence: 99%

Targeting Different Transthyretin Binding Sites with Unusual Natural Compounds

et al. 2016

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Misfolding and aggregation of the transthyretin (TTR) protein leads to certain forms of amyloidosis. Some nutraceuticals, such as flavonoids and natural polyphenols, have recently been investigated as modulators of the self-assembly process of TTR, but they generally suffer from limited bioavailability. To discover innovative and more bioavailable natural compounds able to inhibit TTR amyloid formation, a docking study was performed using the crystallographic structure of TTR. This computational strategy was projected as an adhoc inspection of the possible relationship between binding site location and modulation of the assembly process; interactions with the as-yet-unexplored epigallocatechin gallate (EGCG) sites and with the thyroxine (T4) pocket were simultaneously analyzed. All the compounds studied seem to prefer the traditional T4 binding site, but some interesting results emerged from the screening of an in-house database, used for validating the computational protocol, and of the Herbal Ingredients Targets (HIT) catalogue available on the ZINC database

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Section: Methodsmentioning

confidence: 99%

Targeting Different Transthyretin Binding Sites with Unusual Natural Compounds

et al. 2016

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“…The known G6Pase inhibitors can be placed into two categories: catalytic protein inhibitors and inhibitors of T 1 -, T 2 - and T 3 -translocase. Among these inhibitors, some natural products such as chlorogenic acid 85 exhibited high inhibitory affinities to the translocase sites, and is a secondary metabolite of many plants, phloretin and phlorizin, 86 which are the principal phenolic components of apple trees, flavonoids from Bauhinia megalandra leaves, 87 as well as many products of fungi or bacteria, 88 including kodaistatin, anthraquinones, mumbaistatin and thielavins. In addition, it is reported that extracts of some plants also inhibit the transcriptional expression or activity of G6Pase, and include mulberry branch bark extract, 89 aqueous extract of Clitocybe nuda 90 and methanolic extract of Ventilago maderaspatana .…”

Section: Hepatic Production In Normal and Metabolically Disturbed Stamentioning

confidence: 99%

Natural products, an important resource for discovery of <br />multitarget drugs and functional food for regulation of hepatic glucose metabolism

Li¹,

Yu²,

Wang³

et al. 2018

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Imbalanced hepatic glucose homeostasis is one of the critical pathologic events in the development of metabolic syndromes (MSs). Therefore, regulation of imbalanced hepatic glucose homeostasis is important in drug development for MS treatment. In this review, we discuss the major targets that regulate hepatic glucose homeostasis in human physiologic and pathophysiologic processes, involving hepatic glucose uptake, glycolysis and glycogen synthesis, and summarize their changes in MSs. Recent literature suggests the necessity of multitarget drugs in the management of MS disorder for regulation of imbalanced glucose homeostasis in both experimental models and MS patients. Here, we highlight the potential bioactive compounds from natural products with medicinal or health care values, and focus on polypharmacologic and multitarget natural products with effects on various signaling pathways in hepatic glucose metabolism. This review shows the advantage and feasibility of discovering multicompound–multitarget drugs from natural products, and providing a new perspective of ways on drug and functional food development for MSs.

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Red wine consumption may affect sperm biology: The effects of different concentrations of the phytoestrogen Myricetin on human male gamete function

Aquila

Santoro

Amicis

et al. 2013

Molecular Reproduction Devel

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Myricetin is a natural flavonoid, particularly enriched in red wines, whose occurrence is widespread among plants. Despite extensive research, the beneficial effects of Myricetin on human health are still controversial. Here, we tested the estrogen-like effect of the phytoestrogen Myricetin on human ejaculated sperm biology. To this aim, human normozoospermic samples were exposed to increasing concentrations (10 nM, 100 nM, and 1 µM) of Myricetin. Motility, viability, capacitation-associated biochemical changes (i.e., cholesterol efflux and tyrosine phosphorylation), acrosin activity, as well as glucose utilization and fatty-acid oxidation (i.e., glucose and lipid metabolism) were all significantly increased by low doses of Myricetin. Importantly, both estrogen receptors α and β (ERs) and phosphatidylinositol-3-OH kinase (PI3K)/AKT signaling are activated in the presence of Myricetin since these were both abrogated by specific inhibitors of each pathway. Our results show how Myricetin, through ERs and PI3K/AKT signalings, potentiates sperm function. This effect is dose-dependent at low concentrations of Myricetin (up to 100 nM), whereas higher amounts do not seem to improve any further sperm motility, viability, or other tested features, and, in some cases, they reduced or even abrogated the efficacy exerted by lower doses. Further studies are needed to elucidate if high levels of Myricetin, which could be attained even with moderate wine consumption, could synergize with endogenous estrogens in the female reproductive tract, interfering with the physiological sperm fertilization process.

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Phenolic Derivatives from Ruprechtia polystachya and Their Inhibitory Activities on the Glucose‐6‐phosphatase System

Cited by 16 publications

References 29 publications

Targeting Different Transthyretin Binding Sites with Unusual Natural Compounds

Targeting Different Transthyretin Binding Sites with Unusual Natural Compounds

Natural products, an important resource for discovery of <br />multitarget drugs and functional food for regulation of hepatic glucose metabolism

Red wine consumption may affect sperm biology: The effects of different concentrations of the phytoestrogen Myricetin on human male gamete function

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