JOURNAL OF FISH DISEASES
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2021
·Vol. 45
·期 1
·59-68
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IF 2.767
Li-Peng Shan,Xu Zhang,Yang Hu,Lei Liu,Jiong Chen
White spot syndrome virus (WSSV) is a pathogenic and threatening virus in shrimp culture for which there is no effective control strategy. Finding antiviral lead compounds for the development of anti-WSSV drugs is urgent and necessary; in this study, esculin from 12 monomeric compounds exhibited an excellent anti-WSSV activity. The results showed that esculin increased the survival rate of WSSV-infected shrimps by 59% and reduced the virus copy number in vivo over 90% at 100 μM. In the pre-treatment and post-treatment experiments, esculin could prevent and treat WSSV infection. Compared with the control group, the virus copy number decreased by 30% after 6 h of esculin pre-incubation with WSSV particles and inhibited horizontal transmission of WSSV to a certain extent. Considering that the antiviral activity of esculin was stable in the aquacultural water for 2 days, we evaluated the dosing pattern of continuous medication changes. Obviously, the survival rate of WSSV-infected shrimps was 0% at 108 h when no esculin exchange was made, while at 120 h the survival rate was over 40% at continuous medicine changes. In addition, esculin significantly increased the expression of antimicrobial peptides and thus improved the ability of shrimp to resist WSSV. Overall, our findings suggest that esculin has the potential to be developed into an anti-WSSV medicine.
研究领域:
水产养殖
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病毒学
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海洋生物学
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PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2023
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IF 5.4
Yong-Yu Yang,Jing-Jing Qi,Si-Yi Jiang,Ling Ye
Ethnopharmacological relevance Cortex fraxini (also known as qinpi)—the bark of Fraxinus rhynchophylla Hance (Oleaceae)—is widely used as a Chinese traditional medicinal for its anti-inflammatory and anti-hyperuricemic activities. Aim of the study Obesity-induced insulin resistance (IR) is driving the rising incidence of type 2 diabetes mellitus and is related to pathological adipose tissue remodeling. Esculin, a major active component of Cortex fraxini , has anti-diabetic effects. However, whether esculin improves obesity-induced IR by regulating adipose tissue remodeling is unclear. The aims of the present study were to assess the effects of esculin on obesity-induced IR and to explore the underlying mechanisms. Materials and methods Obese IR C57BL/6J mice were treated with esculin (40 or 80 mg/kg/day) for 4 weeks. Oral glucose tolerance tests were used to assess insulin sensitivity. Histological analyses were performed to analyze the number and size distribution of adipocytes. Glucose uptake was assessed using 2-NBDG. Results Esculin had no effect on body weight gain but reduced fasting blood glucose, improved oral glucose tolerance, and increased insulin sensitivity. Esculin reduced adipocyte size and the expression levels of collagen 4A1 and tumor necrosis factor α and increased the number of adipocytes and the expression of vascular endothelial growth factor A. Esculin promoted the differentiation of 3T3-L1 cells and upregulated the mRNA expression of CCAAT/enhancer-binding protein α and peroxisome proliferator-activated receptor-γ, activated the insulin receptor substrate 1 (IRS1)/phosphatidylinositol 3-kinase (PI3K)/protein kinase B (AKT) signaling pathway, and enhanced the translocation of glucose transporter type 4 (GLUT4) and glucose uptake in adipocytes treated with palmitic acid. Conclusions These data suggest that esculin increases insulin sensitivity by improving adipose tissue remodeling and activating the IRS1/PI3K/AKT/GLUT4 pathway.
研究领域:
药理学
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内分泌学
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代谢
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中药
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DOI
PubMed
高影响因子
FOOD CHEMISTRY
·
2025
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IF 9.8
Le Zhang,Ruiyang Ma,Shuangju Song,Weihua Liu,Qiuhua Wu,Zhi Wang
A green and hydroxyl functionalized hypercrosslinked polymer (Esc/BCMBP 1:2 -HCP) was synthesized for solid-phase extraction (SPE) of diamide insecticides by using natural esculin as monomer for the first time. It exhibited an excellent adsorption performance for the diamides. The major SPE influencing parameters were investigated, and then, a new analytical approach coupling the Esc/BCMBP 1:2 -HCP based SPE with HPLC-DAD detection was developed for the analysis of the diamide insecticides. Under optimal conditions, a good linearity was achieved in the analytes concentration range of 0.2–100.0 ng mL −1 , 3.0–500.0 ng g −1 , and 3.0–500.0 ng g −1 for water, rice and soil samples, respectively, with the coefficients of determination>0.9936. The limits of detection were in the range of 0.06–0.30 ng mL −1 , 0.90–1.60 ng g −1 and 0.80–1.80 ng g −1 , respectively. The method recoveries for the spiked samples were from 87.0 % to 111 %, with the relative standard deviations < 7.5 %.
研究领域:
环境科学
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高分子化学
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分析化学
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农药残留分析
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PubMed
高影响因子
INTERNATIONAL IMMUNOPHARMACOLOGY
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2023
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IF 5.6
Jiangwei Ni,Ge Li,Ningfeng Dai,Zijiao Quan,Haibin Tong,Yu Liu
Objectives Acute lung injury (ALI) poses a serious threat to human health globally, particularly with the Coronavirus 2019 (COVID-19) pandemic. Excessive recruitment and infiltration of neutrophils is the major etiopathogenesis of ALI. Esculin, also known as 6,7-dihydroxycoumarin, is a remarkable compound derived from traditional Chinese medicine Cortex fraxini . Accumulated evidence indicates that esculin has potent anti-inflammatory effects, but its pharmaceutical effect against ALI and potential mechanisms are still unclear. Methods This study evaluated the protective effect of esculin against ALI by histopathological observation and biochemical analysis of lung tissues and bronchoalveolar lavage fluid (BALF) in lipopolysaccharide (LPS)-challenged ALI mice in vivo . The effects of esculin on N-formyl-met-leu-phe (fMLP)-induced neutrophil migration and chemotaxis were quantitatively assessed using a Transwell assay and an automated cell imaging system equipped with a Zigmond chamber, respectively. The drug affinity responsive target stability (DARTS) assay, in vitro protein binding assay and molecular docking were performed to identify the potential therapeutic target of esculin and the potential binding sites and pattern. Results Esculin significantly attenuated LPS-induced lung pathological injury, reduced the levels of pro-inflammatory cytokines in both BALF and lung, and suppressed the activation of NF-κB signaling. Esculin also significantly reduced the number of total cells and neutrophils as well as myeloperoxidase (MPO) activity in the BALF. Esculin impaired neutrophil migration and chemotaxis as evidenced by the reduced migration distance and velocity. Furthermore, esculin remarkably inhibited Vav1 phosphorylation, suppressed Rac1 activation and the PAK1/LIMK1/cofilin signaling axis. Mechanistically, esculin could interact with β 2 integrin and then diminish its ligand affinity with intercellular adhesion molecule-1 (ICAM-1). Conclusions Esculin inhibits β 2 integrin-dependent neutrophil migration and chemotaxis, blocks the cytoskeletal remodeling process required for neutrophil recruitment, thereby contributing to its protective effect against ALI. This study demonstrates the new therapeutic potential of esculin as a novel lead compound.
研究领域:
药理学
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免疫学
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病理生理学
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分子生物学
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DOI
PubMed
高影响因子
Food Bioscience
·
2024
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IF 4.8
Dianhui Wu,Ziqiang Chen,Yongxuan Lv,Lixia Yang,Hua Liu,Ran Qiu,Hengde Xu,Jianbo Li,Jian Lu,Guolin Cai
The utilization of mixed cultures of Saccharomyces and non -Saccharomyces cerevisiae strains to improve the quality and aroma complexity of wines has garnered considerable attention as of late. In this study, three non -S. cerevisiae strains exhibiting a strong β-glucosidase production capacity were screened from the yeasts preserved in the laboratory. Subsequently, the physiological characteristics of the strains were evaluated through growth curve analysis as well as alcohol and osmotic pressure tolerance experiments. Finally, the non -S. cerevisiae strain S14 ( Torulaspora delbrueckii ) was selected and applied to ferment Yuan'an yellow tea beer combined with S. cerevisiae S189. The results showed that the optimal fermentation performance was achieved when S14 was inoculated first, followed by the addition of S189 after 12 h of fermentation, with an S14:S189 ratio of 10:1. Mixed fermentation resulted in a significant increase in the concentration of volatile flavor compounds in beer, particularly terpenes, alcohols, esters, and acids, which exhibited levels of 520.98 μg/L, 5534.28 μg/L, and 1631.80 μg/L, respectively; these values were 299.25%, 32.45%, and 56.57% higher compared to purebred fermentation. Furthermore, mixed fermentation demonstrated an improvement in the antioxidant activity of beer, as evidenced by the increase in the comprehensive evaluation score (CES) from 1.86 to 2.89. Overall, these findings indicated the notable advantage of non -S. cerevisiae strain S14 in fermenting Yuan'an yellow tea beer.
研究领域:
食品科学
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微生物学
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高影响因子
MOLECULAR NEUROBIOLOGY
·
2026
·Vol. 63
·期 1
·432
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IF 5.5
Lin Jinyu,You Bowen,Yang Xin,Li Xue,Sun Wenjuan,Xu Zhongyu,Zhang Yi,Tong Xuhui,Dong Shuying
Cerebral ischemia/reperfusion injury (CIRI) refers to the secondary brain injury that occurs when blood supply is restored to ischemic cerebral tissue, and represents one of the primary causes of adult disability and mortality. Current evidence indicates that aesculin exhibits antioxidative and anti-inflammatory activities; however, its therapeutic effects on CIRI remain to be elucidated. The objective of this study was to investigate the potential role of Esculin (ESCU) in protecting against CIRI and to elucidate its underlying mechanisms. Adult male mice were used to establish the middle cerebral artery occlusion/reperfusion (MCAO/R) model. The mice were administered varying doses of ESCU or a reference positive control drug. To evaluate the neuroprotective effects of ESCU, neurological deficit scores were assessed, and cerebral blood flow was measured. 2,3,5-triphenyltetrazolium chloride staining, H&E staining, and Nissl staining were used to determine neuronal damage. NLRP3-related markers and mitophagy-related markers were determined to investigate the mechanism of action of ESCU. ESCU afforded robust neuroprotection in mice, ameliorating functional deficits, reducing infarct size, and preserving neuronal structure. It potently alleviated oxidative stress and restored mitochondrial function (reduced ROS, improved cristae morphology, and increased mitochondrial membrane potential). Mechanistically, ESCU activated mitophagy (upregulating LC3Ⅱ, PINK1, and Parkin; downregulating p62) and inhibited the NLRP3 inflammasome (downregulating NLRP3, GSDMD-N, cleaved caspase-1, IL-1β, and IL-18). Notably, the mitophagy inhibitor Mdivi-1 abolished ESCU’s inhibition of the NLRP3 pathway, establishing a causal relationship. Thus, ESCU mitigates cerebral ischemia-reperfusion injury by coordinately enhancing mitophagy and suppressing NLRP3 inflammasome activation. Our study demonstrates that ESCU attenuates CIRI mechanistically by promoting PINK1/Parkin-mediated mitophagy, thereby suppressing NLRP3 inflammasome activation. These findings not only elucidate a novel pathway underlying ESCU’s neuroprotection but also position it as a promising therapeutic candidate for CIRI, warranting further investigation into its precise targets and clinical potential.
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PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Jinxia Liu,Xinyi Liu,Zhaoqing Song,Wenying Cao,Yue Li,Mingyu Xia,Dong Wang
Alpha-amylases typically act on starch and oligosaccharides that contain α-1,4 glycosidic linkages, while ginsenosides primarily consist of β-1,2 and β-1,6 glycosidic bonds, which cannot be hydrolyzed by α-amylases. However, for the first time, we have successfully isolated Streptococcus thermophilus 17140 (St17140), capable of converting ginsenoside Rb1 into rare ginsenosides. St17140 expresses a novel α-amylase (StAMY), which hydrolyzes ginsenoside Rb1 to produce Rd, gypenoside XVII, F 2 , and Rh 2 . With Rb 1 as the substrate, the optimal reaction temperature is 50 °C and the optimal pH is 5.5. When Rb 1 , Rd, or gypenoside XVII are used as substrates, the Km are 0.135 mM, 0.0871 mM, and 0.260 mM respectively, the Kcat are 0.621 min −1 , 0.397 min −1 , and 0.297 min −1 respectively, and the Kcat/Km are 4.59 min −1 ·mM −1 , 4.56 min −1 ·mM −1 and 1.14 min −1 ·mM −1 respectively. Utilizing molecular docking and site-directed mutagenesis techniques, the mechanism of ginsenoside hydrolysis by StAMY was further elucidated. A107, F201, A337 and A268 are key amino acid residues that anchor the saponin in the active pocket, and D234 and D331 as catalytic amino acid residues to hydrolyze ginsenosides into rare ginsenosides. It is the first time to discover a novel α-amylase with the ability to hydrolyze ginsenosides β-1,2 and β-1,6 glycosidic linkage, and the first time to discover the ability of S. thermophilus to transform rare ginsenosides. These not only enrich the resources of glycosidases and offer novel insights for the rational modification of glycosidase, also are important for further elucidating the mechanism of probiotic transformation of rare ginsenosides and developing engineering bacteria with high production of rare ginsenosides.
研究领域:
生物化学
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微生物学
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药理学
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PubMed
高影响因子
危险品化学品经营许可证（带存储）