Journal of Functional Foods
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2015
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IF 3.574
Shang-Ta Wang,Ting-Fang Fang,Chen Hsu,Chia-Hao Chen,Chun-Jung Lin,Nan-Wei Su
Research has indicated the health beneficial effects of soyfoods. Genistein, one of the primary bioactive agents in soybeans, has a number of pharmacological and biological activities; however, its low water solubility and low intestinal permeability may lead to the depletion of genistein absorption from dietary intake and contribute to its poor oral bioavailability. Previous study revealed a water-soluble phosphate conjugate of genistein, genistein 7-O-phosphate (G7P), generated by biotransformation of Bacillus subtilis var. natto BCRC80517 with genistein. This study aimed to investigate the dissolution profile, intestinal permeability and oral bioavailability of genistein and G7P. G7P improved water solubility and also enhanced intestinal permeability in vitro and in situ , and greatly increased plasma exposure to genistein after oral administration in rats. The aqueous solubility of genistein is the absorption barrier to its oral bioavailability. G7P may be a promising and efficient alternative to genistein.
研究领域:
药理学
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营养学
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生物转化
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高影响因子
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.
研究领域:
微生物学
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分子生物学
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DOI
PubMed
高影响因子
GREEN CHEMISTRY
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2025
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IF 9.2
Jia Bao Zhang,Wei Chen,Yong Jun Yang,Zhen Zhen Liu
Genistein, a plant-derived isoflavone with pharmaceutical value, is conventionally obtained through ecologically detrimental extraction processes that rely on large-scale plant harvesting and hazardous solvents. Here, we report the discovery of native genistein biosynthesis in the Paenibacillus jilinensis, which inherently produces 5.7 mg L−1 genistein via the phenylalanine branch of the phenylpropanoid pathway. This pathway mirrors plant flavonoid synthesis but operates through seven bacterial enzymes (PjPAL, PjC4H, Pj4CL, PjCHS, PjCHI, PjIFS, and PjHID) with about 30% sequence homology to the corresponding protein sequences in plants, suggesting evolutionary convergence. To leverage this native capability for sustainable production, we constructed a genome-scale metabolic model (GSMM YPG26) with 1636 reactions and 717 genes to rationally optimize carbon flux. Metabolic engineering elevated genistein titers by 9.3-fold to 52.8 mg L−1 without introducing heterologous plant genes. Green-chemistry analysis further showed that P. jilinensis-ΔGLN achieves 92% less waste than soybean extraction and up to one order of magnitude better than state-of-the-art E. coli and yeast systems. It is crucial that this bacterial platform requires only a basic culture medium for sustained production, and eliminates dependence on medicinal plants. Our findings reveal P. jilinensis as a naturally gifted genistein producer and a green chassis for industrial isoflavone synthesis, aligning with green chemistry goals of waste prevention and bio-based process innovation.
研究领域:
生物化学
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微生物学
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合成生物学
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DOI
高影响因子
Journal of the Mechanical Behavior of Biomedical Materials
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2021
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IF 3.902
Shulin Luo,Pei Wang,Min Ma,Zhangyi Pan,Liangyu Lu,Feng Yin,Junfeng Cai
Poly(ether-ether-ketone) (PEEK) with good biocompatibility exhibits high mechanical strengths but bioinert. In addition, tantalum (Ta) possesses outstanding osteogenesis but high density and elastic modulus , and cost. In this study, by blending Ta nanoparticles with PEEK, Ta/PEEK composite (TP) was prepared, which was then treated by concentrated sulfuric acid to form a microporous surface containing Ta particles on TP (TPS). Moreover, genistein (GS) with antibacterial property was loaded into the microporous surface of TPS (TPSG). Compared with TP, the surface properties ( e.g., surface roughness and hydrophilicity) of TPS was obviously improved because of the microporous surface including Ta nanoparticles . Moreover, TPS showed low antibacterial properties because of presence of sulfonic group while TPSG exhibited excellent antibacterial properties due to GS loaded into the microporous surface. Furthermore, compared with TP, TPS obviously promoted attachment and proliferation of MG63 cells, while TPSG with GS remarkably inducing osteogenic differentiation of the cells compared with TPS in vitro . Moreover, in comparison with TP, TPS with optimized surface properties promoted new bone regeneration and osseointegration, while TPSG loading GS further enhanced bone regeneration as well as osseointegration in vi vo. In summary, the GS loaded into microporous surface including Ta nanoparticles of TPSG exhibited antibacterial and osteogenic activity, which would have great potential for bone tissue repair.
研究领域:
生物医学工程
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材料科学
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骨组织工程
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DOI
PubMed
高影响因子
FOOD AND CHEMICAL TOXICOLOGY
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2026
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IF 3.2
Ruo Du,Qingyuan Li,Yi Cheng,Yuting Zeng,Mairewulan Abula,Wenyi Liu,Fangfang Yu,Weihua Jia,Yuhui Du,Yue Ba,Yanjie Wang,Guoyu Zhou
Zearalenone (ZEA), a mycotoxin produced by Fusarium fungi, has drawn significant attention due to its multi-organ toxicity. To explore the molecular mechanisms of ZEA-induced hepatotoxicity and identify effective intervention strategies, this study identified key targets associated with ZEA-induced hepatotoxicity by screening public databases. Further construction of a protein interaction network revealed five crucial targets: TP53 , STAT3 , HSP90AA1 , ESR1 , and PPARG . Moreover, genistein (GEN) was identified from the TCMSP database as a compound capable of simultaneously targeting these targets. Molecular docking results indicated that GEN exhibits strong binding affinity with the five targets (all binding energies <0 kcal/mol). To validate hepatotoxicity mediated by ZEA and intervention mechanisms of GEN, ZEA exposure and ZEA + GEN treated mouse models were conducted. The results exhibited that exposure to ZEA led to increased liver weight and liver coefficient as well as abnormal changes in typical hepatotoxicity indicators in mice, while GEN can alleviate the aforementioned changes. Furthermore, results from quantitative RT-PCR and Western blot indicated that hepatic Hsp90aa1 and HSP90α (the protein encoded by the Hsp90aa1 gene) expression was significantly upregulated by ZEA but significantly downregulated after GEN supplementation. In conclusion, HSP90α may be a key regulatory node in GEN treatment of hepatotoxicity caused by ZEA. Download: Download high-res image (558KB) Download: Download full-size image
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF FOOD SCIENCES AND NUTRITION
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2013
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IF 1.257
Hui Cao,Xiaohui Jing,Donghui Wu,Yujun Shi
Methylation of flavonoids appears to be a simple and effective way to improve metabolic resistance and transport of flavonoids. Serum albumins are major soluble proteins serving as transport proteins for many exogenous compounds. This work in here mainly concerns about the effect of methylation of flavonoids on the affinity for human serum albumin (HSA) and ovalbumin. One isoflavone (genistein) and one flavonol (kaempferol) and their monomethylated derivatives at position 4′ (biochanin A and kaempferide) were studied for their affinities for ovalbumin and HSA. The methylation of flavonoids significantly affects the binding process. In general, the methylation of flavonoids improved the affinities for proteins by 2–16 times. This result supports that the methylation of genistein and kaempferol enhanced the transporting ability, which leads to facilitated absorption and greatly increased bioavailability. The methylation increases the hydrophobicity of genistein and kaempferol, and the hydrophobic interaction plays an important role in binding flavonoids to HSA and ovoalbumin.
研究领域:
药理学
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生物化学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY B-BIOLOGY
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2015
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IF 2.96
Suyun Lin,Guowen Zhang,Junhui Pan,Deming Gong
Genistein (Gen), widely distributed in soybean, is proved to be important in homeostasis in the human body. Herein, the inhibitory mechanism of Gen against xanthine oxidase (XO) was studied through multispectroscopic methods and molecular simulation. The inhibition kinetics showed that Gen competitively inhibited XO with an inhibition constant of (1.39 ± 0.11) μM by competing with xanthine for binding to the active site of XO. Fluorescence titration study suggested that the fluorescence quenching mechanism of XO was static, resulting from the formation of a Gen–XO complex at one fold site. The calculated thermodynamic parameters revealed that the interaction process was driven mainly by hydrophobic interactions and hydrogen bonds with affinity of (5.24 ± 0.02) × 10 4 L mol − 1 . Conformational analyses demonstrated that the microenvironment and the secondary structure of XO were changed upon binding of Gen. The molecular docking displayed that Gen bound to the active cavity of XO by interacting with the surrounding amino acid residues (Leu648, Phe649, Glu802, Ser876, Glu879, Arg880, Phe914, Phe1009, Thr1010 and Phe1013). Thus, the inhibition may be attributed to the insertion of Gen into the active site of XO occupying the catalytic center of the enzyme to avoid entry of the substrate and inducing conformational changes of XO (more compact), which was further unfavorable for forming the active cavity and further reduced the landing and oxidation of substrate. This study may offer novel insights into the inhibition mechanism of Gen on XO.
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DOI
高影响因子
Oncotarget
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2017
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IF 5.168
Hao Gu,Wei Wu,Beilei Yuan,Qiuqin Tang,Dan Guo,Yiqiu Chen,Yankai Xia,Lingqing Hu,Daozhen Chen,Jiahao Sha,Xinru Wang
Genistein (GEN) is one of the isoflavones that has effect on male reproduction. However, the underlying mechanism remains unknown. miRNAs are a type of small non-coding RNAs that play important roles in spermatogenesis. We measured the GEN levels and miR-17-92 cluster expression in infertile subjects and found that miR-17-92 might be involved in GEN induced abnormal spermatogenesis. To clarify, we fed adult ICR mice with different doses of GEN (0, 0.5, 5, 50 and 250 mg/kg/day) for 35 days to study the underlying mechanism. We found that sperm average path velocity, straight-line velocity and eurvilinear velocity of the mice orally with GEN at 5mg/kg/day were significantly decreased, the expression levels of miR-17 and miR-20a in mice testis were higher in corresponding group. We also found miR-20a was the only miRNA that differentially expressed both in human and mice. By applying bioinformatics methods, Limk1 was predicted to be the target gene of miR-20a that is involved in spermatogenesis. Limk1 were significantly decreased in the corresponding group. Dual-luciferase report assay also proved that miR-20a could directly target Limk1. These results implied that Limk1 might be the target gene of miR-20a that is involved in GEN induced abnormal spermatogenesis.
研究领域:
生殖生物学
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分子生物学
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基因组学
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DOI
PubMed
高影响因子
CELLULAR PHYSIOLOGY AND BIOCHEMISTRY
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2018
·Vol. 47
·期 4
·1667-1681
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IF 5.5
Lan Ying,Li Xiulian,Liu Xuebo,Hao Cui,Song Ni,Ren Sumei,Wang Wei,Feng Ningchuan,Zhang Lijuan
Background/Aims: Genistein is a natural isoflavone enriched in soybeans. It has beneficial effects for patients with mucopolysaccharidose type III through inhibiting glycosaminoglycan biosynthesis. However, other studies indicate that genistein does not always inhibit glycosaminoglycan biosynthesis. Methods: To understand the underlying molecular mechanisms, CHOK1, CHO3.1, CHO3.3, and HCT116 cells were treated with genistein and the monosaccharide compositions and quantity of all glycans from the cell lysate were measured after thorough acid hydrolysis followed by HPLC analysis. In addition, the glycosaminoglycan disaccharide compositions were obtained by stable isotope labeling coupled with LC/MS analysis. Results: Genistein treatment reduced the amount of glycans but increased the amount of glycosaminoglycans in HCT116 cells. In contrast, genistein treatment reduced both glycan and glycosaminoglycan quantities in CHOK1, CHO3.1, and CHO3.3 cells in addition to differential changes in glycosaminoglycan disaccharide compositions. Conclusion: Genistein treatment reduced overall glycan quantity but glycosaminoglycan quantities were either increased or decreased in a cell type-dependent manner
研究领域:
医学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
PHYTOMEDICINE
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2026
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IF 11.3
Jieli Pan,Jinjun Ji,Xingpan Xin,Yihong Gan,Zixin Huang,Jing Chen,Ying Li,Jie Bao,Yujun Tang,Chengping Wen,Li Xu
Background Systemic lupus erythematosus (SLE) is an autoimmune disease with marked female predominance. Lupus nephritis (LN), one of its most severe manifestations, is strongly associated with aberrant activation of signal transducer and activator of transcription 3 (STAT3). Estrogen receptor β (ERβ) has been reported to exert immunoregulatory effects, but its role in restraining STAT3 signaling in LN remains unclear. Purpose This study aimed to investigate whether genistein, a phytoestrogen with selective affinity for ERβ, can modulate the ERβ–STAT3 axis to attenuate lupus nephritis. Methods The therapeutic effects of genistein were evaluated in MRL/lpr and pristane-induced lupus mouse models and in LPS-stimulated macrophages. Macrophage polarization, oxidative stress, mitochondrial function, and ERβ–STAT3 signaling were assessed using flow cytometry, biochemical assays, immunoblotting, and bioinformatic analyses. Results Genistein significantly ameliorated renal injury, reduced proteinuria, and decreased serum autoantibody and IL-6 levels in lupus models. Mechanistically, genistein suppressed M1 macrophage polarization by activating ERβ and inhibiting STAT3 and NF-κB signaling. Genistein also attenuated oxidative stress by preserving mitochondrial membrane potential, reducing reactive oxygen species production, and restoring antioxidant capacity. Pharmacological blockade of ERβ markedly attenuated the anti-inflammatory effects of genistein, confirming ERβ-dependent regulation of STAT3 signaling. Conclusion This study identifies ERβ as a negative regulator of STAT3-driven inflammation and demonstrates that genistein therapeutically engages this axis to suppress macrophage-mediated renal injury, offering a promising therapeutic strategy for lupus nephritis.
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PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2026
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IF 6.7
Yi Kuang,Cailing Tan,Xianrui Tan,Jian Zhang
Isoflavones from legumes, particularly genistein, are highly valued as functional food ingredients. However, the poor water solubility and low bioavailability hinder its application, which can be improved through glycosylation. The glycosyltransferase GT2419 from Bacillus subtilis ATCC 6633 catalyzes the 7-OH and 4′–OH glycosylation of genistein, but its poor regioselectivity hampers the efficient synthesis of genistein 7-O-glucoside. Here, a semirational design strategy was employed to obtain the F231V mutant, which significantly increased the conversion rate of genistein 7-O-glucoside from 21.1% to 72.2% and improved the 7-O regioselectivity to 73.8%. Kinetic analysis revealed that the F231V mutant exhibited enhanced affinity and catalytic efficiency toward genistein. Computational analysis revealed that the F231V mutant enlarged the substrate-binding pocket and disrupted intermolecular hydrophobic interactions, thereby altering substrate orientation, and enhancing the regioselective formation of genistein 7-O-glucoside. This study provides an efficient biosynthetic method for genistein 7-O-glucoside, with promising applications in the food industry.
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DOI
PubMed
高影响因子
Food & Function
·
2021
·Vol. 13
·期 3
·1393-1407
·
IF 5.396
Liuming Xie,Zhibing Huang,Hui Meng,Zhibing Fan,Xiaoyi Shi,Jianhua Xie
Manipulating the structures, physicochemical properties, and monosaccharide compositions of exopolysaccharides (EPS) isolated from microorganisms has been reported to enhance their biological activities. Hence, the aim of this work was to examine the effects of genistein addition during fermentation on the amount, physicochemical properties, and immunomodulatory activity of EPS secreted by M. purpureus. Results showed that genistein addition significantly increased M. purpureus biomass and EPS yield to 2.42 g L−1 and 6.08 g L−1, respectively, and affected the physicochemical properties and structures of EPS. Furthermore, EPS produced by genistein-treated M. purpureus (G-EMP) improved the immunomodulatory activity of RAW264.7 macrophages by increasing the secretion of nitric oxide and cytokines. Moreover, phospho-Jun N-terminal kinase (p-JNK), phospho-extracellular regulated protein kinase (p-ERK), phospho-p38 (p-p38) mitogen-activated protein kinase (MAPK) and nuclear factor-kappa B (NF-κB) phospho-p65 (p65) proteins were remarkably upregulated by G-EMP stimulation, blocking Toll-like receptor 4 (TLR4) that dramatically reduced the pinocytic and phagocytic capacities. Overall, these findings provide potential rationales for the application of genistein in improving the EPS yield of M. purpureus.
研究领域:
微生物学
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免疫学
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生物技术
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产品关联
DOI
PubMed
高影响因子
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