Molecular Docking and Panicolytic Effect of 8-Prenylnaringenin in the Elevated T-Maze

Bagatin, Mariane Cristovão; Tozatti, Camila Santos Suniga; Abiko, Layara Akemi; Yamazaki, Diego Alberto dos Santos; Silva, Priscila Rebeca Alves; Perego, Leonardo Martins; Audi, Elisabeth Aparecida; Seixas, Flávio Augusto Vicente; Basso, Ernani A.; Gauze, Gisele F.

doi:10.1248/cpb.c14-00569

Cited by 5 publications

(5 citation statements)

References 43 publications

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“…The positive control substance fluoxetine acted similarly. A subsequent docking study revealed that the R configuration of 8-PN had greater affinity to the transporters for serotonin, noradrenaline, and dopamine than does the S enantiomer, suggesting that the ( R )-8-PN is the active form [ 179 ].…”

Section: Other Beneficial and Adverse Effects Of 8-pnmentioning

confidence: 99%

The Potent Phytoestrogen 8-Prenylnaringenin: A Friend or a Foe?

Pohjanvirta

Nasri

2022

IJMS

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8-prenylnaringenin (8-PN) is a prenylated flavonoid, occurring, in particular, in hop, but also in other plants. It has proven to be one of the most potent phytoestrogens in vitro known to date, and in the past 20 years, research has unveiled new effects triggered by it in biological systems. These findings have aroused the hopes, expectations, and enthusiasm of a “wonder-drug” for a host of human diseases. However, the majority of 8-PN effects require such high concentrations that they cannot be reached by normal dietary exposure, only pharmacologically; thus, adverse impacts may also emerge. Here, we provide a comprehensive and up-to-date review on this fascinating compound, with special reference to the range of beneficial and untoward health consequences that may ensue from exposure to it.

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Section: Other Beneficial and Adverse Effects Of 8-pnmentioning

confidence: 99%

The Potent Phytoestrogen 8-Prenylnaringenin: A Friend or a Foe?

Pohjanvirta

Nasri

2022

IJMS

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“…[ 363 ]: neurodifferentiating potential of the product. Bagatin et al [ 364 ]: panicolytic effects in rats with generalized anxiety and panic disorders. Oberbauer et al [ 365 ]: promote neuronal differentiation and neurite outgrowth and are neuroprotective.…”

Section: Resultsmentioning

confidence: 99%

Endocrine disruptors also function as nervous disruptors and can be renamed endocrine and nervous disruptors (ENDs)

Séralini

Jungers

2021

Toxicology Reports

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“…Toll-like receptor 4; NF-kB signaling IL-1b; IL-6; IL-8; TNF expression humulone, lupulone, XN 1 , tetrahydro-iso-α-acids, bitter acids [15,[20][21][22][23] Antioxidant ROS; RNS; lipid peroxidation crude extract, bitter acids [24][25][26] Sedative and neuroprotective GABA A receptors; b-amyloid phagocytosis; dopamine levels; vagal activation; noradrenaline levels 2-methyl-3-buten-2-ol, bitter acids, 8-PN 3 , 6-PN 4 , IX 2 , iso-α-acids, matured hop bitter acids [1,6,20,[27][28][29][30][31][32][33][34][35][36][37][38] Anticancerogenic ERK1/2, AP-1, NF-kB, prostaglandin E2, NK cells, NKp44 receptor, JNK, ROS levels, cytochrome P450 enzymes, Akt, MAPK/ERK, CD44v6, aromatase expression, Keap1-Nrf2…”

Section: Anti-inflammatorymentioning

confidence: 99%

“…From a stereochemical point of view, this compound has a single chiral carbon centre in its structure, leading to two enantiomers, with enantiospecific bioactive properties that may significantly influence the pharmacological, toxicological, and pharmacokinetic profile of 8-PN [119]. Bagatin et al (2014) investigated the effectiveness of a long-term administration (21 d) of a racemic mixture of 8-PN to rats submitted to the elevated T-maze (ETM) model of generalized anxiety and panic disorders. The pharmacological trials demonstrated no effects following an 8-PN acute treatment (10 mg/kg), confirming the existence of a latency period until the onset of the therapeutic action.…”

Section: Sedative and Neuroprotective Activitiesmentioning

confidence: 99%

“…The pharmacological trials demonstrated no effects following an 8-PN acute treatment (10 mg/kg), confirming the existence of a latency period until the onset of the therapeutic action. Moreover, using docking simulations, the authors found that between the two enantiomers, (R)-8-PN had a greater affinity (lower inhibition constant) for all transporters tested (serotonin, norepinephrine, and dopamine ones) than enantiomer (S)-8-PN, indicating that the panicolytic effect observed in the animal model can be due mainly to the R enantiomer of the racemic mixture used [31].…”

Section: Sedative and Neuroprotective Activitiesmentioning

confidence: 99%

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An Updated Review of the Genus Humulus: A Valuable Source of Bioactive Compounds for Health and Disease Prevention

Carbone

Gervasi

2022

Plants

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The medicinal potential of hop (Humulus lupulus L.) is widely cited in ancient literature and is also allowed in several official pharmacopoeias for the treatment of a variety of ailments, mainly related to anxiety states. This is due to the plethora of phytoconstituents (e.g., bitter acids, polyphenols, prenyl flavonoids) present in the female inflorescences, commonly known as cones or strobili, endowed with anti-inflammatory, antioxidant, antimicrobial, and phytoestrogen activities. Hop has recently attracted the interest of the scientific community due to the presence of xanthohumol, whose strong anti-cancer activity against various types of cancer cells has been well documented, and for the presence of 8-prenyl naringenin, the most potent known phytoestrogen. Studies in the literature have also shown that hop compounds can hinder numerous signalling pathways, including ERK1/2 phosphorylation, regulation of AP-1 activity, PI3K-Akt, and nuclear factor NF-κB, which are the main targets of the antiproliferative action of bitter acids and prenylflavonoids. In light of these considerations, the aim of this review was to provide an up-to-date overview of the main biologically active compounds found in hops, as well as their in vitro and in vivo applications for human health and disease prevention. To this end, a quantitative literature analysis approach was used, using VOSviewer software to extract and process Scopus bibliometric data. In addition, data on the pharmacokinetics of bioactive hop compounds and clinical studies in the literature were analysed. To make the information more complete, studies on the beneficial properties of the other two species belonging to the genus Humulus, H. japonicus and H. yunnanensis, were also reviewed for the first time.

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Molecular Docking and Panicolytic Effect of 8-Prenylnaringenin in the Elevated T-Maze

Abstract: The purpose of this study was to investigate the effects of the chronic administration of a racemic mixture of 8-prenylnaringenin (

Cited by 5 publications

References 43 publications

The Potent Phytoestrogen 8-Prenylnaringenin: A Friend or a Foe?

The Potent Phytoestrogen 8-Prenylnaringenin: A Friend or a Foe?

Endocrine disruptors also function as nervous disruptors and can be renamed endocrine and nervous disruptors (ENDs)

An Updated Review of the Genus Humulus: A Valuable Source of Bioactive Compounds for Health and Disease Prevention

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