Genistein—Opportunities Related to an Interesting Molecule of Natural Origin

Garbiec, Ewa; Cielecka‐Piontek, Judyta; Kowalówka, Magdalena; Hołubiec, Magdalena; Zalewski, Przemysław

doi:10.3390/molecules27030815

Cited by 23 publications

(12 citation statements)

References 174 publications

(195 reference statements)

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“…It may have a positive impact on some parameters associated with increased risk of cardiovascular disease [ 11 ] and modulate genes involved in the inflammatory process, thus being potentially beneficial in the control of psoriasis [ 12 ]. GEN also has anti-inflammatory and antioxidant properties [ 13 ] and has been reported as a promising compound to prevent and treat diabetes [ 14 , 15 ].…”

Section: Introductionmentioning

confidence: 99%

Genistein Co-Amorphous Systems with Amino Acids: An Investigation into Enhanced Solubility and Biological Activity

Garbiec,

Rosiak,

Zalewski

et al. 2023

Pharmaceutics

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Genistein, an isoflavone known for its antioxidant and antidiabetic effects, suffers from the drawback of low solubility. To overcome this limitation, co-amorphous systems were synthesized by incorporating amino acids that were chosen through computational methods. The confirmation of the amorphous state of lysine and arginine-containing systems was ascertained by X-ray powder diffraction. Subsequently, the characterization of these systems was extended by employing thermo-gravimetry, differential scanning calorimetry, Fourier-transform infrared spectroscopy, and scanning electron microscopy. The investigation also included an assessment of the physical stability of the samples during storage. The apparent solubility of the systems was studied in an aqueous medium. To evaluate the in vitro permeability through the gastrointestinal tract, the parallel artificial membrane permeability assay was employed. The biological properties of the systems were assessed with regard to their antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl and cupric ion-reducing antioxidant capacity assays, as well as their ability to inhibit α-glucosidase. The systems’ glass transition temperatures were determined, and their homogeneity confirmed via differential scanning calorimetry analysis, while Fourier-transform infrared spectroscopy analysis provided data on molecular interactions. Stability was maintained for the entire 6-month storage duration. The co-amorphous system containing lysine displayed the most pronounced apparent solubility improvement, as well as a significant enhancement in antioxidant activity. Notably, both systems demonstrated superior α-glucosidase inhibition relative to acarbose, a standard drug for managing type 2 diabetes. The results indicate that co-amorphous systems with lysine and arginine have the potential to significantly enhance the solubility and biological activity of genistein.

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Section: Introductionmentioning

confidence: 99%

Genistein Co-Amorphous Systems with Amino Acids: An Investigation into Enhanced Solubility and Biological Activity

Garbiec,

Rosiak,

Zalewski

et al. 2023

Pharmaceutics

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“…Several researchers have reported the mechanisms of action of this molecule involving numerous targets in living cells, such as the growth factors and their intracellular signaling. (Cui et al 2017 ; Chae et al 2019 ; Tuli et al 2019 ; Garbiec et al 2022 ). In relation to liver disease, previous studies have revealed that genistein inhibits EGFR system and has a protective effect during the processes of acute and chronic liver disease (Rodriguez et al 2016 ; Tanjak et al 2018 ; Xin et al 2019 ; Semeniuk et al 2021 ).…”

Section: Discussionmentioning

confidence: 99%

EGF-receptor phosphorylation and downstream signaling are activated by genistein during subacute liver damage

et al. 2023

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The epidermal growth factor receptor (EGFR) plays an important role on hepatic protection in acute and chronic liver injury. The aim of this study was to investigate the role of genistein on EGFR expression, phosphorylation and signaling pathways in experimental subacute liver damage induced by carbon tetrachloride (CCl4). We used male Wistar rats that were randomly divided into four groups: (1) Control; (2) Genistein 5 mg/kg per oral; (3) Subacute liver damage induced by CCl4 4 mg/kg subcutaneously; and (4) Animals received CCl4 and genistein at the dosage indicated. The effect of genistein on EGFR expression, phosphorylation and signaling pathways were investigated by western blot and densitometric analyses. Histological changes were evaluated on slices stained with Hematoxylin-Eosin and Masson´s trichromic, as well as an immunohistochemical analysis for proliferating cell nuclear antigen (PCNA). Additionally, pro-inflammatory cytokines and liver enzymes were quantified. Our study showed that genistein increased EGFR expression, EGFR-specific tyrosine residues phosphorylation (pY1068-EGFR and pY84-EGFR), signal transducer and activator of transcription phosphorylation (pSTAT5), protein kinase B phosphorylation (pAKT) and PCNA in animals with CCl4-induced subacute liver damage. It was found a significant reduction of pro-inflammatory cytokines in serum from animals with subacute liver damage treated with genistein. Those effects were reflected in an improvement in the architecture and liver function. In conclusion, genistein can induce a transactivation of EGFR leading to downstream cell signaling pathways as early events associated with regeneration and hepatoprotection following subacute liver damage.

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“…Certain dietary strategies, such as adopting a balanced and nutrient-rich diet, regular physical activity, and weight management, have the potential to reduce the risk of developing cancer [ 68 , 80 , 81 , 82 , 83 , 84 ]. Prevention is a crucial aspect of cancer management, and dietary interventions can also play a significant role in reducing the occurrence of cancer [ 78 ].…”

Section: Discussionmentioning

confidence: 99%

Potential of Dietary HDAC2i in Breast Cancer Patients Receiving PD-1/PD-L1 Inhibitors

Wang,

Lu,

Ling

et al. 2023

Nutrients

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Breast cancer (BC) is a lethal malignancy with high morbidity and mortality but lacks effective treatments thus far. Despite the introduction of immune checkpoint inhibitors (ICIs) (including PD-1/PD-L1 inhibitors), durable and optimal clinical benefits still remain elusive for a considerable number of BC patients. To break through such a dilemma, novel ICI-based combination therapy has been explored for enhancing the therapeutic effect. Recent evidence has just pointed out that the HDAC2 inhibitor (HDAC2i), which has been proven to exhibit an anti-cancer effect, can act as a sensitizer for ICIs therapy. Simultaneously, dietary intervention, as a crucial supportive therapy, has been reported to provide ingredients containing HDAC2 inhibitory activity. Thus, the novel integration of dietary intervention with ICIs therapy may offer promising possibilities for improving treatment outcomes. In this study, we first conducted the differential expression and prognostic analyses of HDAC2 and BC patients using the GENT2 and Kaplan–Meier plotter platform. Then, we summarized the potential diet candidates for such an integrated therapeutic strategy. This article not only provides a whole new therapeutic strategy for an HDAC2i-containing diet combined with PD-1/PD-L1 inhibitors for BC treatment, but also aims to ignite enthusiasm for exploring this field.

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Genistein—Opportunities Related to an Interesting Molecule of Natural Origin

Cited by 23 publications

References 174 publications

Genistein Co-Amorphous Systems with Amino Acids: An Investigation into Enhanced Solubility and Biological Activity

Genistein Co-Amorphous Systems with Amino Acids: An Investigation into Enhanced Solubility and Biological Activity

EGF-receptor phosphorylation and downstream signaling are activated by genistein during subacute liver damage

Potential of Dietary HDAC2i in Breast Cancer Patients Receiving PD-1/PD-L1 Inhibitors

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