Microorganisms
·
2025
·Vol. 13
·期 7
·1699
·
IF 4.2
Aiguo Huang,Yanqin Wei,Jialong Huang,Songlin Luo,Tingyu Wei,Jing Guo,Fali Zhang,Yinghui Wang
Streptococcus agalactiae(SA) is a severe prevalent pathogen, resulting in high morbidity and mortality in the global tilapia industry. With increasing bacterial resistance to antibiotics, alternative strategies are urgently needed. This study aims to investigate the antibacterial activity and the underlying mechanisms of the natural product xanthohumol (XN) against SA infection in tilapia (Oreochromis niloticus). The results showed that XN could significantly reduce the bacterial loads of SA in different tissues (liver, spleen and brain) after treatment with different tested concentrations of XN (12.5, 25.0 and 50.0 mg/kg). Moreover, XN could improve the survival rate of SA-infected tilapia. 16S rRNA gene sequencing demonstrated that the alpha-diversity index (Chao1 and Shannon_e) was significantly increased in the XN-treated group (MX group) compared to the SA-infected group (CG group) (p< 0.05), and the Simpson diversity index significantly decreased. The Bray–Curtis similarity analysis of non-metric multidimensional scaling (NMDS) and principal coordinate analysis (PCA) showed that there were significant differences in microbial composition among groups. At the phylum level, the relative abundance of the phyla Actinobacteria, Proteobacteria and Bacteroidetes decreased in the MX group compared to the CG group, while the relative abundance of the phyla Fusobacteria, Firmicutes and Verrucomicrobia increased. Differences were also observed at the genus level; the relative abundance ofMycobacteriumdecreased in the MX group, but the abundance ofCetobacteriumandClostridium_sensu_stricto_1increased. Metabolomics analysis revealed that XN changed the metabolic profile of the liver and significantly enriched aspartate metabolism, glycine and serine metabolism, phosphatidylcholine biosynthesis, arginine and proline metabolism, glutamate metabolism, urea cycle, purine metabolism, methionine metabolism, betaine metabolism, and carnitine synthesis. Correlation analysis indicated an association between the intestinal microbiota and metabolites. In conclusion, XN may be a potential drug for the prevention and treatment of SA infection in tilapia, and its mechanism of action may be related to the regulation of the intestinal microbiota and liver metabolism.
研究领域:
微生物学
·
鱼类免疫学
·
代谢组学
·
水产药理学
·
肠道生态学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF FISH DISEASES
·
2023
·Vol. 46
·期 9
·977-986
·
IF 2.5
Fa-Li Zhang,Liu Yang,Wei-Hao He,Ling-Jun Xie,Fei Yang,Ying-Hui Wang,Ai-Guo Huang
Streptococcosis disease caused by Streptococcus agalactiae (Group B Streptococcus, GBS) results in a huge economic loss of tilapia culture. It is urgent to find new antimicrobial agents against streptococcosis. In this study, 20 medicinal plants were evaluated in vitro and in vivo to obtain medicinal plants and potential bioactive compounds against GBS infection. The results showed that the ethanol extracts of 20 medicinal plants had low or no antibacterial properties in vitro, with a minimal inhibitory concentration ≥256 mg/L. Interestingly, in vivo tests showed that 7 medicinal plants could significantly inhibit GBS infection in tilapia, and Sophora flavescens (SF) had the strongest anti-GBS activity in tilapia, reaching 92.68%. SF could significantly reduce the bacterial loads of GBS in different tissues (liver, spleen and brain) of tilapia after treated with different tested concentrations (12.5, 25.0, 50.0 and 100.0 mg/kg) for 24 h. Moreover, 50 mg/kg SF could significantly improve the survival rate of GBS-infected tilapia by inhibiting GBS replication. Furthermore, the expression of antioxidant gene cat , immune-related gene c-type lysozyme and anti-inflammatory cytokine il-10 in liver tissue of GBS-infected tilapia significantly increased after treated with SF for 24 h. Meanwhile, SF significantly reduced the expression of immune-related gene myd88 and pro-inflammatory cytokines il-8 and il-1β in liver tissue of GBS-infected tilapia. The negative and positive models of UPLC-QE-MS, respectively, identified 27 and 57 components of SF. The major components of SF extract in the negative model were α, α-trehalose, DL-malic acid, D- (−)-fructose and xanthohumol, while in the positive model were oxymatrine, formononetin, (−)-maackiain and xanthohumol. Interestingly, oxymatrine and xanthohumol could significantly inhibit GBS infection in tilapia. Taken together, these results suggest that SF can inhibit GBS infection in tilapia, and it has potential for the development of anti-GBS agents.
研究领域:
水产养殖
·
药理学
·
微生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2024
·Vol. 14
·期 25
·17824-17831
·
IF 3.9
Lingfeng Xu,Xinya Liu,Jingyi Zhao,Xinmin Deng,Hui Peng
Viscosity is a typical physical parameter and plays an important role in nutrient transferring, diffusion process regulating and safety warning. Aberrant mitochondrial viscosity is closely associated with an imbalance in a liquid system. Nevertheless, there is currently a lack of convenient and efficient tools for the mutation of viscosity detection at the molecular level. Herein, a natural product xanthohumol (XTH) was extracted from Humulus lupulus and used to measure the microenvironmental viscosity. Due to the existence of carbonyl and phenolic hydroxyl groups, a typical twisted intramolecular charge transfer (TICT) was formed. The conjugated single and double bonds can be employed as the rotatable site. Consequently, a turn-on method based on viscosity response is developed. High sensitivity (x = 0.56) with a remarkable enhancement (55-fold) toward viscosity and a visualized fluorescent signal can be found. In addition, it displays a single selectivity with excellent photostability and pH stability in the complex liquid system. Using the extracted XTH, a typical application toward the liquid spoilage process was performed and a positive correlation was noted. Given the comprehensive properties of XTH, liquid safety inspection at a molecular level with natural source-extracted products can be obtained.
研究领域:
化学
·
材料科学
·
生物技术
·
食品科学
✓ 已验证
DOI
PubMed
高影响因子
Heliyon
·
2023
·
IF 4
Weichao Sun,Jiaji Yue,Tianhao Xu,Yinxing Cui,Dixi Huang,Houyin Shi,Jianyi Xiong,Wei Sun,Qian Yi
Osteoarthritis (OA) is a prevalent chronic degenerative joint disease worldwide. Obesity has been linked to OA, and increased free fatty acid levels (e.g., palmitate) contribute to inflammatory responses and cartilage degradation. Xanthohumol (Xn), a bioactive prenylated chalcone, was shown to exhibit antioxidative, anti-inflammatory, and anti-obesity capacities in multiple diseases. However, a clear description of the preventive effects of Xn on obesity-associated OA is unavailable. This study aimed to assess the chondroprotective function of Xn on obesity-related OA. The in vitro levels of inflammatory and ECM matrix markers in human chondrocytes were assessed after the chondrocytes were treated with PA and Xn. Additionally, in vivo cartilage degeneration was assessed following oral administration of HFD and Xn. This study found that Xn treatment completely reduces the inflammation and extracellular matrix degradation caused by PA. The proposed mechanism involves AMPK signaling pathway activation by Xn, which increases mitochondrial biogenesis, attenuates mitochondrial dysfunction, and inhibits NLRP3 inflammasome and the NF-κB signaling pathway induced by PA. In summary, this study highlights that Xn could decrease inflammation reactions and the degradation of the cartilage matrix induced by PA by inhibiting the NLRP3 inflammasome and attenuating mitochondria dysfunction in human chondrocytes.
研究领域:
风湿病学
·
药理学
·
细胞生物学
·
分子生物学
✓ 已验证
DOI
PubMed
高影响因子
Frontiers in Pharmacology
·
2024
·
IF 4.4
Liu Wei,Chen Xiao,Zhao Jing,Yang Chen,Huang Guanqin,Zhang Zhen,Liu Jianjun
Alzheimer’s disease (AD) has an increasing prevalence, complicated pathogenesis and no effective cure. Emerging evidences show that flavonoid compounds such as xanthohumol (Xn) could play an important role as a dietary supplement or traditional Chinese herbal medicine in the management of diseases such as AD. This study aims to analyze the target molecules of Xn in the prevention and treatment of AD, and its potential mechanism from the perspective of metabolites. APP/PS1 mice 2- and 6-months old were treated with Xn for 3 months, respectively, the younger animals to test for AD-like brain disease prevention and the older animals to address therapeutic effects on the disease. Memantine (Mem) was selected as positive control. Behavioral tests were performed to assess the course of cognitive function. Urine samples were collected and analyzed by high-performance liquid chromatography (HPLC) with tandem mass spectrometry (MS/MS) coupled with online Compound Discoverer software. Morris Water Maze (MWM) tests showed that Xn, like Mem, had a therapeutic but not a preventive effect on cognitive impairment. The expression levels of urinary metabolites appeared to show an opposite trend at different stages of Xn treatment, downregulated in the prevention phase while upregulated in the therapy phase. In addition, the metabolic mechanisms of Xn during preventive treatment were also different from that during therapeutic treatment. The signaling pathways metabolites nordiazepam and genistein were specifically regulated by Xn but not by Mem in the disease prevention stage. The signaling pathway metabolite ascorbic acid was specifically regulated by Xn in the therapeutic stage. In conclusion, dietary treatment with Xn altered the urinary metabolite profile at different stages of administration in APP/PS1 mice. The identified potential endogenous metabolic biomarkers and signal pathways open new avenues to investigate the pathogenesis and treatment of AD.
研究领域:
神经科学
·
药理学
·
代谢组学
·
疾病预防与治疗
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
·
2025
·
IF 5.4
Wushi Chen,Yunqin Shen,Hongyun Jia,Shanshan Hou,Lingjie Li,Lixia Huang,Jiyi Cai,Yuhan Xing,Yanqiu Chen,Yan Yang
Ethnopharmacological relevance Humulus lupulus L. , an herb traditionally employed in medicinal practices across North America, Egypt, India, and China, demonstrates broad therapeutic properties, including anti-inflammatory, antioxidant, hepatoprotective, and diuretic effects. Xanthohumol (XN), a prenylated flavonoid derived from Humulus lupulus L., retains these anti-inflammatory and antioxidant activities. However, its potential efficacy in allergic asthma remains largely unexplored. Aim of the study This study aimed to investigate the protective properties of XN against allergic asthma and to elucidate the underlying mechanisms, particularly the role of Absent in Melanoma 2 (AIM2), an innate immune sensor, in allergic asthma and its modulation by XN. Materials and methods The OVA-induced murine model of allergic asthma with XN administration in different dosages was constructed to evaluate the regulatory effects of XN on allergic asthma, particularly during the period of acute attack. Pathological alterations, T-cell polarization, inflammatory cytokine profiles, and oxidative stress markers were systematically assessed. Bioinformatic analysis, clinical case-control, and molecular docking combined with cellular thermal shift assay (CETSA) were applied to identify the specific target of XN to execute its effects. Human bronchial epithelial (16HBE) cell models with various stimulations and treatments were used in this study to verify the mechanistic exploration. Results In allergic asthmatic mice, the results demonstrated that XN dose-dependently attenuated airway inflammation and immune balance, characterized by reduced inflammatory cell infiltration, cytokine production, IgE secretion, and Th2 immune response. AIM2 was recognized as a critical binding target of xanthohumol through database analysis, molecular docking, and CETSA. Clinically, elevated serum AIM2 levels in asthma patients correlated positively with eosinophil percentage, IgE levels, and systemic immune inflammation index (SII). Mechanistically, both in vivo and in vitro studies revealed that XN mitigated oxidative stress and mitochondrial dysfunction, thereby reducing double-stranded DNA release, a key activator of the AIM2 inflammasome. Moreover, XN dose-dependently suppressed AIM2 inflammasome activation, an effect further validated in Poly (dA:dT)-stimulated and AIM2-silenced 16HBE cells. Conclusion This study provides the first evidence implicating XN can improve OVA-induced allergic asthma by suppressing AIM2 inflammasome activation, highlighting XN as a promising therapeutic candidate for allergic asthma.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
FOOD HYDROCOLLOIDS
·
2022
·
IF 11.504
Limin Wang,Yunsen Zhang,I. Agbaka Johnpaul,Kai Hong,Hanlu Gao,Yumei Song,Chenyan Lv,Changwei Ma
Xanthohumol (XN), as an abundant chalcone in hops, has received increasing attention due to its pharmacologic effects. However, poor solubility and bioaccessibility in aqueous solutions have limited its application. This work reported a novel carrier to improve the solubility and bioaccessibility of XN by using heat-stable, serpin-like protein Z (PZ) derived from barley malt. In this study, the solubility of XN was increased by 145-fold (vs. free XN in water) using 200 μM PZ as the carrier. Fluorescence results demonstrated that XN interacted with PZ via static quenching process, with binding constant (K a ) of 5.70 × 10 4 L/mol at 298 K. PZ as a serine protease inhibitor exhibited excellent in vitro digestive stability that could inhibit trypsin with a low half inhibitory concentration (IC 50 ) of 3.90 ± 0.03 mg/L and showed only 26.54 ± 0.70% degree of hydrolysis after gastrointestinal digestion. Furthermore, the retention ratio of XN was 50.28 ± 1.80% after gastrointestinal digestion, which is 8-fold higher than XN alone, suggesting that PZ remarkably enhanced the bioaccessibility of XN. Molecular dynamics simulation analysis revealed that XN was bound within the hydrophobic pocket of PZ, near the Glu338 residue of PZ, whereas the external active loop of PZ was involved in binding with trypsin. This helped to elucidate the roles of PZ in improving the bioaccessibility of XN that PZ encapsulated XN in its hydrophobic cavity, without influencing its inhibition on trypsin. These findings suggest that PZ may be developed as carriers that protect XN or other hydrophobic bioactive molecules in the gastrointestinal tract.
研究领域:
药理学
·
食品科学
·
生物技术
·
蛋白质工程
✓ 已验证
产品关联
DOI
高影响因子
EUROPEAN JOURNAL OF NUTRITION
·
2025
·Vol. 64
·期 6
·1-17
·
IF 4.3
Chen Huihui,Lin Hongzhou,Qian Rengcheng,Tang Guoqi,Ding Yinjuan,Jiang Yalan,Guo Xiaoling,Wang Dexuan
Purpose Nephrotic syndrome (NS) is the main cause of the increasing end-stage renal disease (ESRD) patients worldwide. Podocytes are considered the crucial cells involved in the progression of NS, and their damage can directly lead to proteinuria. The objective of this study was to explore the protective effects of xanthohumol (XN) on podocyte injury. Methods Adriamycin (ADR)-induced podocyte injury in vivo and in vitro models were established to explore the effects of XN on adriamycin nephropathy (AN) by urine and serum biochemical assay, periodic acid-schiff (PAS) staining, immunohistochemistry, immunofluorescence, western blot, and real-time quantitative PCR (RT-qPCR). Results The results showed that XN could upregulate the expressions of podocyte specific marker Wilms’ tumor protein 1 (Wt1), and glomerular filtration related functional proteins such as Nephrin, Synaptopodin, Zonula occludens 1 (ZO-1), and Crumbs2 (Crb2) as well as downregulate the expression of podocyte injury marker Desmin in ADR-treated podocytes to restrain the podocyte actin cytoskeleton disruption. Conclusion Our study showed that XN treatment significantly attenuated ADR-induced podocyte injury, suggesting that XN may be a potential therapy option for patients with NS.
研究领域:
肾脏病学
·
分子生物学
·
药理学
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF NUTRITION
·
2024
·Vol. 64
·期 1
·1-13
·
IF 4.1
Han Ning,Li Jie,Li Yangyang,Zhao Feiei,Wang Jun,Ye Peiyu,Zeng Zhenling
Ethnopharmacological relevance Xanthohumol (XN), an isoprenylated flavonoid natural product found only in hops, possesses a variety of biological activities such as anticancer, anti-inflammatory, hepatoprotective, and anti-obesity. Aim of the study The aim of this study was to investigate the effects and mechanisms of XN on the treatment of colitis. Materials and methods First, acute colitis was induced by using distilled water containing 3% DSS for 10 consecutive days. The therapeutic efficacy of XN was assessed by an established DSS-induced mouse colitis model. Subsequently, disease activity index (DAI) and colon length of mice were assessed. The health of the intestines was assessed by histopathological analysis. Inflammatory factors, IL-1β, IL-6, and TNF-α, were detected in colon tissues by ELISA.Finally, mouse intestinal contents were extracted and subjected to 16 S rRNA Sequencing, and the gut microbiota was analysed for Alpha-diversity and Beta-diversity. Results The results showed that XN ameliorated DSS-induced colitis. Furthermore, XN reduced pro-inflammatory cytokine levels such as IL-1β, IL-6, and TNF-α, as well as inhibited the activation of the TLR4/NF-κB pathway, all of which helped to mitigate the inflammatory response. Finally, we also found that XN alleviated intestinal dysbiosis in colitis mice. Conclusion In conclusion, our study demonstrated that XN provides protective effects against colitis, and has the potential to be further explored as a lead compound for the treatment of inflammatory bowel disease (IBD). Graphical
研究领域:
药理学
·
免疫学
·
胃肠病学
·
微生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOMATERIALS
·
2025
·
IF 12.9
Yan Gao,Zilin Song,Wenxin Gan,Xue Zou,Yaning Bai,Xiuli Zhao,Dawei Chen,Mingxi Qiao
Despite the promise of ferroptosis in cancer therapy, selectively inducing robust ferroptosis in cancer cells remains a significant challenge. In this study, manipulation of fatty acids β-oxidation (FAO) by combination of mild photodynamic therapy (PDT) and inhibition of triglycerides (TGs) synthesis was found to induce robust and iron-independent ferroptosis in cancer cells with dysregulated lipid metabolism for the first time. To achieve that, TGs synthesis inhibitor of xanthohumol (Xan) and FAO initiator of tetrakis (4-carboxyphenyl) porphyrin (TCPP) were co-delivered by a nanoplexes composed of pH-responsive amphiphilic lipopeptide C 18 -pHis 10 and DSPE-PEG 2000 . TCPP was found to rapidly increase the intracellular ROS under laser irradiation without inducing antioxidant response and apoptosis, activating the AMPK in cancer cells and accelerating mitochondrial FAO. Xan fueled the mitochondrial FAO with substrates by suppressing the conversion of fatty acids (FAs) to TGs. This also led to augmented intracellular polyunsaturated fatty acids (PUFAs) and PUFAs-phospholipids levels, increasing the intrinsic susceptibility of cancer cells to lipid peroxidization. As a result, the excessive ROS generated from the sustained mitochondrial FAO caused remarkably lipid peroxidation and ultimately ferroptosis. Collectively, our study provides a new approach to selectively induce iron-independent ferroptosis in cancer cells by taking advantage of dysregulated lipid metabolism.
研究领域:
肿瘤学
·
生物化学
·
医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BRAIN RESEARCH BULLETIN
·
2025
·
IF 3.7
Wei Liu,Xiao Chen,Chen Yang,Zequn Lin,Xinfeng Huang,Zhen Zhang,Jianjun Liu
Alzheimer's disease (AD) is a complex disease with unknown etiology and pathogenesis. We described a combined analysis of murine proteomics and microbiomics to find potential therapeutic targets of different doses of xanthohumol (Xn), with the goal of providing a biological basis for the treatment of early AD. Xn improved the spatial learning and memory ability of APP/PS1 mice; this was associated with an increased number of newborn neurons in the subgranular zone (SGZ) and dentate gyrus (DG) and a decreased inflammatory response. 108 proteins were significantly changed after 0.5 mg/kg Xn treatment while only 72 proteins changed by 5 mg/kg Xn. Eight significant microbiota were modulated by different doses of Xn at line discriminant analysis (LDA) score 3.0, but only three of which were regulated by 0.5 mg/kg Xn at LDA score 4.0. In addition, Xn treatment could significantly regulate the pathways of neurodegeneration- multiple diseases in the hippocampus and the penicillin and cephalosporin biosynthesis and atrazine degradation pathways in the gut. Interestingly, Nefl protein validated by correlation analysis was found in the common signaling pathway. 0.5 mg/kg Xn was able to reverse the correlation between hippocampal proteins and gut microbiota. Xn treatment significantly improved cognitive function in AD transgenic mice. Different doses of Xn caused significant differences in protein expression and flora composition and abundance, suggesting that the doses of Xn should be selected with caution, and low dose may be better in the prevention of AD.
研究领域:
神经生物学
·
药理学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PHYTOMEDICINE
·
2026
·
IF 8.3
Wen Yan,Ying Huang,Yanjie Zhou,Qingfang Xie,Wanbin Huang,Yuexiu Lei,Zheman Xiao
Background Migraine is a common neurological disorder characterized by repeated attacks, with central sensitization recognized as a critical mechanism underlying the pathogenesis of chronic migraine (CM). Xanthohumol (Xn), a predominant bioactive allyl flavonoid derived from hops ( Humulus lupulus L. ), demonstrates notable anti-inflammatory and antioxidant properties. However, its therapeutic potential for migraine remains poorly characterized. Purpose The study focused on investigating the protective effects of Xn on a migraine model in mice, which was triggered by repeated dural applications of inflammatory soup (IS), and aimed to identify the underlying mechanisms. Methods A migraine mouse model was established through repeated dural IS stimulation. These mice received two doses of Xn treatment. Headache behavior was assessed using tests including head scratching, the periorbital mechanical threshold, cold allodynia, and light aversive behavior. Analyses of biomarkers and key protein expression via Western blot (WB), immunofluorescence (IF), and immunohistochemistry (IHC) were conducted to evaluate central sensitization. Through network pharmacology, molecular docking, cellular thermal shift assay (CETSA), and surface plasmon resonance (SPR), peroxisome proliferator-activated receptor α (PPARα) was identified as a potential target for Xn's migraine treatment. Downstream molecular mechanisms were validated by both activating and inhibiting PPARα. Results Comprehensive behavioral analyses revealed that Xn administration significantly alleviated migraine-like symptoms in migraine model mice, including increasing the periorbital mechanical threshold, reducing cold allodynia and head scratching, and improving light aversive behaviors. Network pharmacological analyses suggested that PPARα was a potential target for Xn in the treatment of migraine. Molecular docking, CETSA, and SPR experiments confirmed direct binding between Xn and PPARα. Mechanistic investigations demonstrated that Xn exerted regulatory effects through PPARα/AMPK pathway activation coupled with cyclooxygenase-2 (COX-2) suppression and downregulation of pro-inflammatory cytokines. Conclusion This study revealed that Xn alleviated migraine-related central censitization by activating the PPARα/AMPK axis and reducing neuroinflammation, proposing Xn as a novel migraine treatment.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）