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

Pohjanvirta, Raimo; Nasri, Atefeh

doi:10.3390/ijms23063168

Cited by 12 publications

(13 citation statements)

References 187 publications

(267 reference statements)

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“…In contrast to most other phytoestrogens that show higher binding affinity for ERβ than for ERα, 8-PN has been shown to have a higher affinity for ERα in in vitro competitive binding assays and transfected yeast cells [32,33]. This preferential binding activity of 8-PN for ERα is believed to enable its pharmacological roles, particularly in the regulation of bone and energy metabolism [14,32]. In this study, STZ treatment markedly reduced the protein expression levels of both Erα and Erβ in the pancreas, skeletal muscle, and liver (Figure 6).…”

Section: Discussionmentioning

confidence: 89%

“…Because 8-PN has been identified as a phytoestrogen that has potent ER-agonistic activity [31], the question of whether 8-PN displays its pharmacological effects in an ERdependent manner or not is an important issue for understanding its molecular mechanism. In contrast to most other phytoestrogens that show higher binding affinity for ERβ than for ERα, 8-PN has been shown to have a higher affinity for ERα in in vitro competitive binding assays and transfected yeast cells [32,33]. This preferential binding activity of 8-PN for ERα is believed to enable its pharmacological roles, particularly in the regulation of bone and energy metabolism [14,32].…”

Section: Discussionmentioning

confidence: 99%

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Naringenin and Phytoestrogen 8-Prenylnaringenin Protect against Islet Dysfunction and Inhibit Apoptotic Signaling in Insulin-Deficient Diabetic Mice

Park

Sim²,

Hwangbo

et al. 2022

Molecules

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It has been shown that citrus flavanone naringenin and its prenyl derivative 8-prenylnaringenin (8-PN) possess various pharmacological activities in in vitro and in vivo models. Interestingly, it has been proposed that prenylation can enhance biological potentials, including the estrogen-like activities of flavonoids. The objective of this study was to investigate the anti-diabetic potential and molecular mechanism of 8-PN in streptozotocin (STZ)-induced insulin-deficient diabetic mice in comparison with naringenin reported to exhibit hypoglycemic effects. The oral administration of naringenin and 8-PN ameliorated impaired glucose homeostasis and islet dysfunction induced by STZ treatment. These protective effects were associated with the suppression of pancreatic β-cell apoptosis and inflammatory responses in mice. Moreover, both naringenin and 8-PN normalized STZ-induced insulin-signaling defects in skeletal muscles and apoptotic protein expression in the liver. Importantly, 8-PN increased the protein expression levels of estrogen receptor-α (ERα) in the pancreas and liver and of fibroblast growth factor 21 in the liver, suggesting that 8-PN could act as an ERα agonist in the regulation of glucose homeostasis. This study provides novel insights into the mechanisms underlying preventive effects of naringenin and 8-PN on the impairment of glucose homeostasis in insulin-deficient diabetic mice.

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Section: Discussionmentioning

confidence: 89%

Section: Discussionmentioning

confidence: 99%

Naringenin and Phytoestrogen 8-Prenylnaringenin Protect against Islet Dysfunction and Inhibit Apoptotic Signaling in Insulin-Deficient Diabetic Mice

Park

Sim²,

Hwangbo

et al. 2022

Molecules

View full text Add to dashboard Cite

show abstract

“…The main critical issues seem to be related to the type of analytical assay used, particularly the nature of the radical employed. The authors also pointed out a dosedependent antioxidant activity of 8-PN, on average lower than that of XN [134]. Finally, Kontek et al (2021), in their recent study, fractionated the powder of the freeze-dried hop cone (cv.…”

Section: Antioxidant Activitymentioning

confidence: 96%

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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“…8PN has a high affinity for estrogen receptors (ER), with a preference for ERα over ERβ. ERα expression is prevalent in uterus, bone, adipose tissue and mammary gland, among others (Pohjanvirta and Nasri, 2022). In vivo and in vitro studies show that 8PN has a beneficial effect on osteogenesis, prevents bone loss and improves biomechanical bone properties (Hümpel et al, 2005;Sehmisch et al, 2008;Ming et al, 2013;Luo et al, 2014).…”

Section: Osteoporosis Phytoestrogens and Reproductive Organsmentioning

confidence: 99%

Analysis of Uterine Morphology in Ovariectomized Rats Treated With Alendronate and Hop Extract Using Open-Soruce Software

et al. 2022

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Free and open-source software for image analysis and morphological measurements in scientific research is rising in popularity and capabilities as new methods, plugins and macros are being actively developed. A semi-automated method for measuring rat uterus morphology using free and open-source software (Gimp and FIJI) is demonstrated in this paper. Research was performed on ovariectomized rats as a model of osteoporosis (with sham-operated control group). The animals were treated with alendronate, hop extract or the combination of the two. Whole histological slides were photographed and images were manually pre-processed in Gimp. Color masks from Gimp were loaded in FIJI and polar transformation and measurements were made using a custom macro. This analysis was supplemented by manual assessment of Ki67 proliferation marker expression by a pathologist. Our results suggest that monotherapy or combination therapy with alendronate and hop extract does not cause proliferation of the endometrium in ovariectomized rats and would be safe for use in osteoporosis treatment in this regard. The semi-automated method used in this research is more precise and unbiased than older manual methods. Furthermore, it can be easily adapted for analysis of whole-slide images of almost any round or oval organ.

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

Cited by 12 publications

References 187 publications

Naringenin and Phytoestrogen 8-Prenylnaringenin Protect against Islet Dysfunction and Inhibit Apoptotic Signaling in Insulin-Deficient Diabetic Mice

Naringenin and Phytoestrogen 8-Prenylnaringenin Protect against Islet Dysfunction and Inhibit Apoptotic Signaling in Insulin-Deficient Diabetic Mice

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

Analysis of Uterine Morphology in Ovariectomized Rats Treated With Alendronate and Hop Extract Using Open-Soruce Software

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