INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2023
·
IF 8.2
Lijuan Shi,Zhen Lin,Jiantong Hou,Wenhui Liu,Jing Xu,Yuanqiang Guo
Genistein is an isoflavone with chemopreventive and therapeutic effects on various types of cancers. Apparently, in contrast to the advantages of multi-target therapy, the poor water solubility of this molecule is a major obstacle to its clinical application. In this work, zein/chicory polysaccharide nanoparticles (G-zein-P NPs) were prepared by pH-induced antisolvent precipitation method for the encapsulation of genistein. Firstly, an acidic polysaccharide (CIP70-2) with a molecular weight of 66.7 kDa was identified from the roots of chicory ( Cichorium intybus ). This natural macromolecule was identified as a plant pectin, for which the structure included RG-I (rhamnogalacturonan I) and HG (homogalacturonan) regions. Using this polysaccharide, G-zein-P NPs were prepared, in which the water solubility of genistein was improved by encapsulation. The encapsulation efficiency and loading efficiency of genistein by composite nanoparticles reached 99.0 % and 6.96 %, respectively. In vitro tumor inhibition experiments showed that the inhibitory effect of G-zein-P NPs on HepG2 cells was twice that of unencapsulated genistein. Moreover, the significant inhibition of tumor development and metastasis by G-zein-P NPs was observed in zebrafish xenograft models. The results suggested that zein/chicory polysaccharide nanoparticles may be a promising delivery carrier for genistein application in cancer prevention and therapy.
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RSC Advances
·
2025
·Vol. 15
·期 33
·26601-26607
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IF 4.6
Yuqi Dai,Lanmei Zhang,Yuemeng Wang,Anni Fu,Lanling Chu,Lei Zhao
In this work, an integrated method based on the novel packed-fiber solid-phase extraction (PFSPE) combined with high-performance liquid chromatography-ultraviolet detector (HPLC-UV) detection system was proposed for the detection of daidzein, genistein and glycitein in human urine. To efficiently adsorb three kinds of isoflavones in biological fluid, polystyrene-based nanofibers were prepared and used as adsorbents in customized solid phase extraction devices. The composition of the nanofibers, the amount of different salt ions added, the type of eluent, and the interaction of eluent volume, the amounts of nanofibers added, and the extraction time were analyzed to find the optimal adsorption conditions, respectively. The method of optimal extraction conditions for the analysis of three soy isoflavones exhibited low limits of detection (LOD) and limits of quantitation (LOQ) of 1.68–2.74 μg L−1 and 5.09–8.3 μg L−1, respectively, and spiked recovery of 95.2–107.1%, and has been successfully applied to human urine samples. This study demonstrated the potential of PFSPE as methods for the adsorption and detection of daidzein, genistein, glycitein in biological fluid concurrently, providing a valuable tool for pharmacokinetic studies and investigations into the metabolism and bioavailability of isoflavones.
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PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
·
2025
·
IF 4
Ling Zhang,Yu Long,Long-Fei Li,Xiang-Wei Xin,Xiao-Di Chen,Xiang Zhou,Li-Wei Liu,Zhi-Bing Wu,Song Yang
The overreliance on traditional chemical fungicides, combined with the emergence of resistance, poses significant challenges for food safety. Early blight, caused by the fungal pathogen Alternaria solani ( A. solani ), is among the most significant contributors to pre- and postharvest yield losses in tomato cultivation. To address this challenge, through evaluation of the antifungal activity of 52 commercially available natural products against A. solani , we revealed for the first time that the naturally occurring compound genistein exhibited potent fungicidal activity against A. solani , with an EC 50 value of 6.53 μg/mL, surpassing that of chlorothalonil (EC 50 = 8.35 μg/mL). In vivo assays demonstrated that genistein exhibited strong protective (48.1 %) and therapeutic (42.5 %) efficacy, effectively safeguarding tomatoes from fungal infection. Mechanistic investigations, including transcriptomic analysis, scanning electron microscopy, fluorescence imaging, and measurements of malondialdehyde and ATP levels, collectively indicated that genistein disrupted energy metabolism, leading to reactive oxygen species (ROS) accumulation. This oxidative stress cascade triggered both apoptotic-like responses and membrane lipid peroxidation, ultimately inhibiting the growth of A. solani . Interestingly, genistein showed enhanced anti- A. solani activity when used in combination with either chlorothalonil or tebuconazole. Additionally, genistein displayed low phytotoxicity and favorable drug-likeness properties. Taken together, these findings elucidate the mechanisms underlying genistein's antifungal activity against A. solani , underscoring its promise as a natural antifungal agent for enhancing food safety and improving tomato yield and quality. Furthermore, this study provides valuable insights for the rational design of flavonoid-based antifungal agents.
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Food Bioscience
·
2026
·
IF 5.9
Kai Cheng,Gang Wang,Jianhua Xie,Zhibing Huang
Penicillium polysaccharides exhibit immunomodulatory activity, different polysaccharides produced by Penicillium EF-2 during fermentation were altered by adding different concentrations of genistein as an exogenous additive to change the fermentation environment. Structural characterization of the polysaccharides was performed and their activities were evaluated, and it was found that the Penicillium polysaccharides became more porous and their molecular weight decreased after the addition of genistein, thereby increasing their biological activity. Combined cell-based and animal studies demonstrated that genistein addition enhances the bioactivity of extracellular polysaccharides produced by Penicillium fermentation. However, for polysaccharide yield in Penicillium fermentation, polysaccharide content decreased at 3 d in both 0.5 g/L genistein (G_0.5E) and 1.5 g/L genistein (G_1.5E) treatments. Furthermore, it was concluded that polysaccharides may influence T cell differentiation by regulating energy metabolism, thereby exerting an immunosuppressive regulatory effect.
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JOURNAL OF NUTRITIONAL BIOCHEMISTRY
·
2022
·
IF 6.117
Huawu Gao,Xin Lei,Shu Ye,Ting Ye,Rupeng Hua,Guoquan Wang,Hang Song,Peng Zhou,Yan Wang,Biao Cai
Genistein (GS), an isoflavone compound found in soybean, plays a neuroprotective role in Alzheimer's disease (AD). However, the mechanism of its action remains unclear. Herein, binding ability between GS and GRP78 was predicted by molecular docking , and the effect of GS in vivo and vitro were further studied. In this study, the effects of GS on learning and memory ability, changes of hippocampal neurons and ultrastructure of hippocampal CA3 region in AD rats were investigated. Besides, the protein or mRNA levels of the related proteins were detected. The results showed GS could effectively improve the learning and the memory ability, reduce the damage of hippocampal neurons, and decrease the protein or mRNA expression levels of GRP78, CHOP, Caspase-12, Cle-Caspase-9, Cle-Caspase-3, PERK, and p-PERK. Taken together, our data reveal GS has a neuroprotective effect by inhibiting the ERS-mediated apoptotic pathway, which may be a new therapeutic target for the treatment of AD .
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2026
·
IF 8.7
Kaihan Li,Can Zhao,Kunshan Wang,Hongyu Liang,Suzhen Zhou,Jinbo Fan
β-Lg can simultaneously load and protect the three flavonoid compounds, namely Isl, Gen, and Bai. • In terms of stability, the β-Lg-multilinked compound shows a better protective effect against the three types of flavonoids. • A spectroscopic approach was adopted to elucidate the binding mechanisms of three flavonoids with β-Lg. • The conformational characteristics of the complexes were investigated through molecular docking and dynamics simulations. This study elucidates the interaction mechanisms of Isoliquiritigenin (Isl), Genistein (Gen) and Baicalein (Bai) with β-lactoglobulin (β-Lg), with a focus on the protein's capacity for the co-encapsulation and stabilization of these flavonoids. The binding mechanisms were characterized using fluorescence spectroscopy, high-performance liquid chromatography, non-radiative energy transfer analysis, molecular simulations. The results demonstrated that the binding affinity ( K a ) followed the order Bai > Gen > Isl. Accordingly, the calculated binding distances for Isl, Gen and Bai were 5.36 nm, 4.49 nm, and 4.20 nm, respectively. β-Lg is capable of co-encapsulating two or three flavonoids simultaneously. The most stable ternary complex (β-Lg-Isl-Gen-Bai) formed when the flavonoids were added in the sequence of Bai, Isl, and then Gen. The β-Lg multi-ligand complex provided superior protection for Isl, Gen, and Bai compared to their respective single-ligand complexes across all tested parameters: stability, antioxidant capacity, and α-amylase inhibition. For Isl, the retention rate improvement under storage stability is the largest, reaching 73.86 ± 1.04%; for Gen, the retention rate improvement under light stability is the largest, reaching 75.22 ± 0.77%; and for Bai, the retention rate improvement under thermal stability is the largest, reaching 71.90 ± 1.02%. β-Lg simultaneously encapsulates and stabilizes three flavonoids Isl, Gen, Bai, serves as a natural and potent protein carrier for these bioactive compounds, and offers theoretical support for their protection against degradation.
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FOOD CHEMISTRY
·
2020
·
IF 6.306
Wanbao Ouyang,Xin Liu,Yanling Wang,Zhibing Huang,Xiujiang Li
Monascus , which is traditionally used in various Asian industries, produces several secondary metabolites during the fermentation process, including citrinin, a toxin whose impact limits the development of the Monascus industry. We have previously found that the addition of 2.0 g/L genistein to Monascus medium reduces citrinin production by approximately 80%. Here, we explored the molecular mechanisms whereby genistein affects citrinin production. We sequenced the Monascus genome and performed transcriptome analysis on genistein-treated and -untreated groups. Comparison between the two groups showed 378 downregulated and 564 upregulated genes. Among the latter, we further examined the genes related to citrinin biosynthesis and quantified them using quantitative real-time polymerase chain reaction (qRT-PCR). Genes orf5 , pksCT , orf3 , orf1 , orf6 , and ctnE were significantly downregulated, demonstrating that genistein addition indeed affects citrinin synthesis. Our results may lay the groundwork for substantial improvements in the Monascus fermentation industry.
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POULTRY SCIENCE
·
2026
·Vol. 105
·期 4
·106548
·
IF 4.2
Dan Liu,Honglei Guo,Yaxian Yang,Xin He,Xinghua Zhao
Fatty Liver Hemorrhagic Syndrome ( FLHS ) is a metabolic disorder characterized by hepatic lipid metabolism dysfunction in poultry. This study aimed to investigate the efficacy and underlying mechanism of a solid dispersion of genistein ( SDG ) in ameliorating FLHS in laying hens. In this study, a total of 60 Lohmann gray laying hens, aged 40-week-old, were randomly divided into five groups including the control group (normal diet), MOD group (high-energy low-protein diet; HELP diet), GEN group (400 mg/kg GEN + HELP diet), SDG group (3200 mg/kg SDG + HELP diet), and physical mixture of GEN group (PMG) (3200 mg/kg PMG + HELP diet). The results demonstrated that all three treatment groups exerted therapeutic effects on FLHS, with SDG exhibiting the superior efficacy. SDG improved the production performance of laying hens, modulated hepatic function, and reduced blood lipid levels. Furthermore, SDG supplementation attenuated intestinal pathological damage and restored intestinal permeability and barrier function. Meanwhile, SDG reshaped gut microbiota structure and metabolite composition, increasing the abundance of Akkermansia, UCG-008, Elusimicrobium, Zag_111 , and phosphoglycerides ( P < 0.05), and reducing Bifidobacterium and lysophospholipids ( P < 0.05). Transcriptomic analysis showed that the pyruvate metabolism pathway was significantly enriched. SDG upregulated the expression of PCK2, PC , and ACAT2 within this pathway, while downregulating the expression of ME1 . The underlying mechanism may involve the inhibition of hepatic triglyceride synthesis, the facilitation of free cholesterol conversion into cholesterol esters, and the promotion of oxaloacetate and acetyl-CoA entry into the tricarboxylic acid cycle, thereby suppressing hepatic lipid deposition. In conclusion, our study demonstrated solid dispersion technology enhanced the effect of GEN on alleviating FLHS, and established a foundation for applying SDG to improving poultry liver health.
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JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE
·
2023
·Vol. 103
·期 13
·6440-6451
·
IF 4.1
Haiyun Yang,Zhiqing Peng,Liuming Xie,Jianhua Xie,Zhibing Huang
BACKGROUND Chinese yam fermented by Monascus , namely red mold dioscorea (RMD), has the potential of treating diseases. However, the production of citrinin limits the application of RMD. In the present study, the fermentation process of Monascus was optimized by adding genistein or luteolin to reduce citrinin yield. RESULTS The results showed that citrinin in 25 g of Huai Shan yam was reduced by 48% and 72% without affecting the pigment yield by adding 0.2 g of luteolin or genistein, respectively, to a 250-mL conical flask after fermentation for 18 days at 28 °C, whereas the addition of luteolin increased the content of yellow pigment by 1.3-fold. Under optimal conditions, citrinin in 20 g of iron bar yam decreased by 55% and 74% after adding 0.2 g of luteolin or genistein. Luteolin also increased yellow pigment content by 1.2-fold. Ultra HPLC coupled to quadrupole time-of-flight mass spectrometry was used for the preliminary analysis of Monascus fermentation products. It was found that the amino acid types in RMD are similar to those in yams, but there are fewer polysaccharides and fatty acids. CONCLUSION The results obtained in the present study showed that the addition of genistein or luteolin could reduce citrinin on the premise of increasing pigment yield, which laid a foundation for the better use of yams in Monascus fermentation. © 2023 Society of Chemical Industry.
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POULTRY SCIENCE
·
2021
·
IF 3.352
Zhenwu Huang,Song Jin,Zengpeng Lv
ABSTRACT Genistein is abundant in the soybean products, which exerts prominent effects on immune function. Little information is available about the effect of dietary genistein on thymic transcriptome, especially when suffering from lipopolysaccharide challenge. In this study, 180 one-day-old male broilers were randomly allocated to 3 groups: nonchallenged chicks given a basal diet ( CON ), and lipopolysaccharide-challenged chicks fed a basal diet ( LPS ), or lipopolysaccharide-challenged chicks fed a basal diet supplemented with 40 mg/kg genistein ( GEN ). Lipopolysaccharide injection induced thymocyte apoptosis and inflammatory reactions in the chicks. The results showed dietary genistein significantly reduced the percentage of CD3+ T lymphocytes by 10.04% and CD4+/CD8+ T lymphocyte ratio by 21.88% in the peripheral blood induced by lipopolysaccharide injection ( P < 0.05). In addition, genistein significantly reduced the thymus index by 50% and apoptotic index by 12.34% induced by LPS challenge ( P < 0.05). Transcriptomic analysis identified 1,926 DEGs (1,014 upregulated and 912 downregulated, P < 0.05) between GEN and LPS groups, which altered the mRNA expression profile and signaling pathways (Toll-like receptor, and NOD-like receptor signaling pathway) in the thymus. Furthermore, 5 splicing (AS) isoforms of the Drosophila Disabled-2 ( DAB2 ) gene were detected, which were significantly upregulated in the GEN group compared with that in the LPS group. In summary, dietary genistein supplementation altered the RNA expression profile and AS signatures in the thymus, and alleviated immune response against lipopolysaccharide challenge.
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International Journal of Nanomedicine
·
2015
·
IF 4.383
Tianpeng Zhang,Huan Wang,Yanghuan Ye,Xingwang Zhang,Baojian Wu
Polymeric micelles receive considerable attention as drug delivery vehicles, depending on the versatility in drug solubilization and targeting therapy. However, their use invariably suffers with poor stability both in in vitro and in vivo conditions. Here, we aimed to develop a novel nanocarrier (micellar emulsions, MEs) for a systemic delivery of genistein (Gen), a poorly soluble anticancer agent. Gen-loaded MEs (Gen-MEs) were prepared from methoxy poly(ethylene glycol)-block-(ε-caprolactone) and medium-chain triglycerides (MCT) by solvent-diffusion technique. Nanocarriers were characterized by dynamic light scattering, transmission electron microscopy, and in vitro release. The resulting Gen-MEs were approximately 46 nm in particle size with a narrow distribution. Gen-MEs produced a different in vitro release profile from the counterpart of Gen-ME. The incorporation of MCT significantly enhanced the stability of nanoparticles against dilution with simulated body fluid. Pharmacokinetic study revealed that MEs could notably extend the mean retention time of Gen, 1.57- and 7.38-fold as long as that of micelles and solution formulation, respectively, following intravenous injection. Furthermore, MEs markedly increased the elimination half-life (t1/2β) of Gen, which was 2.63-fold larger than that of Gen solution. Interestingly, Gen distribution in the liver and kidney for MEs group was significantly low relative to the micelle group in the first 2 hours, indicating less perfusion in such two tissues, which well accorded with the elongated mean retention time. Our findings suggested that MEs may be promising carriers as an alternative of micelles to systemically deliver poorly soluble drugs.
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Food Chemistry-X
·
2024
·
IF 6.5
Mengmeng Zhang,Jingbo Liu,Yu Gao,Bing Zhao,Meng-Lei Xu,Ting Zhang
A Se site targeted-two circles antioxidant of polyphenols EGCG and genistein in glutathione peroxidase 4 (GPx4)–like catalytic peroxide H 2 O 2 and cumene hydroperoxide degradation was demonstrated by surface-enhanced Raman scattering (SERS). Se atom's active center is presenting a ‘low-oxidation’ and a ‘high-oxidation’ catalytic cycle. The former is oxidized to selenenic acid (SeO − ) with a Raman bond at 619/ 610 cm −1 assigned to the νO − Se by the hydroperoxide substrate at 544/ 551 cm −1 assigned to ωHSeC decreased. Under oxidative stress, the enzyme shifted to ‘high-oxidation’ catalytic cycle, in which GPx4 shuttles between R-SeO − and R-SeOO − with a Raman intensity of bond at 840/ 860 cm −1 assigned to νO Se. EGCG could act as a reducing agent both in H 2 O 2 and Cu-OOH degradation, while, genistein can only reduce Cu-OOH, because it binds more readily to the selenium site in GPx4 than EGCG with a closer proximity, therefore may affect its simultaneous binding to coenzymes.
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