JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
·
2018
·
IF 2.831
Hongyu Ji,Yu Liu,Fang He,Ran An,Zhimin Du
Hyperlipidemia has been highlighted to be one of the most prominent and global chronic condition nowadays. Daming capsule (DMC), a traditional Chinese medicine (TCM) preparation, has treated hyperlipidemia on clinic in China for decades. Our recent study showed that aloe-emodin (AE) is one of the main bioactive components in DMC. Therefore, the present study aims to further investigate the lipid-lowering effect by serum biochemistry and histopathological examination, and reveal the underlying mechanisms by urinary metabolomics approach. After oral administration of AE for 6 weeks, the total cholesterol (TC) and low-density lipoprotein-cholesterol (LDL-c) levels in 50 and 100 mg/kg AE groups were both decreased significantly ( P < 0.05 and P < 0.001). An ultra-performance liquid chromatography/electrospray ionization quadruple time-of-flight mass spectrometry (UPLC-ESI-QTOF-MS) followed by principal components analysis (PCA), partial least squares- discriminant analysis (PLS-DA), orthogonal partial least squares-discriminant analysis (OPLS-DA), correlation analysis, heat map, and KEGG pathways was employed to identify 26 potential biomarkers. Twenty three among them were restored by AE including L-citrulline, 6-methylaminopurine, imidazoleacetic acid riboside, N-acetylhistamine, 3-methyladenine, 1-methyladenosine, dopamine, N1-methyl-4-pyridone-3-carboxamide, formylanthranilic acid, 4-pyridoxate, cAMP, salsolinol, isethionate, d -ribonic acid, 3-sulfolactic acid, vitamin C, mesaconic acid, sulfosalicylic acid, salicyluric acid, N-acetylanthranilic acid, 4,6- Dihydroxyquinoline, sebacic acid and hyocholic Acid. The related metabolic pathways include TCA cycle, the metabolism of amino acids, taurine, B vitamins, purines and pyrimidines. The results indicate that AE has a favorable therapeutic effect on HFD-induced hyperlipidemia by adjusting the metabolic disorders. Notably, urinary metabolomics combined with pattern recognition analysis provides a powerful and reliable approach into the research and development of TCM and phytochemicals.
研究领域:
药理学
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代谢组学
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中药
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色谱法
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质谱分析
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脂质代谢
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DOI
PubMed
高影响因子
PHYTOMEDICINE
·
2020
·
IF 4.268
Dan Wang,Minghui Sun,Ying Zhang,Zehong Chen,Shuya Zang,Genyun Li,Gao Li,Andrew R. Clark,Jiangeng Huang,Luqin Si
Background Ulcerative colitis (UC) is an intricate enteric disease with a rising incidence that is closely related to mucosa-barrier destruction, gut dysbacteriosis, and immune disorders. Emodin (1,3,8-trihydroxy-6-methyl-9,10-anthraquinone, EMO) is a natural anthraquinone derivative that occurs in many Polygonaceae plants. Its multiple pharmacological effects, including antioxidant, immune-suppressive, and anti-bacteria activities, make it a promising treatment option for UC. However, its poor solubility, extensive absorption, and metabolism in the upper gastrointestinal tract may compromise its anti-colitis effects. Purpose EMO was loaded in a colon-targeted delivery system using multifunctional biomedical materials and the enhanced anti-colitis effect involving mucosa reconstruction was investigated in this study. Methods EMO-loaded Poly (DL-lactide-co-glycolide)/Eudragit Ⓡ S100/montmorillonite nanoparticles (EMO/PSM NPs) were prepared by a versatile single-step assembly approach. The colon-specific release behavior was characterized in vitro and in vivo , and the anti-colitis effect was evaluated in dextran sulfate sodium (DSS)-induced acute colitis in mice by weight loss, disease activity index (DAI) score, colon length, histological changes, and colitis biomarkers. The integrity of the intestinal mucosal barrier was evaluated through transwell co-culture model in vitro and serum zonulin-related tight junctions and mucin2 (MUC2) in vivo . Results EMO/PSM NPs with a desirable hydrodynamic diameter (~ 235 nm) and negative zeta potential (~ -31 mV) could prevent the premature drug release (< 4% in the first 6 h in vitro ) in the upper gastrointestinal tract (GIT) and boost retention in the lower GIT and inflamed colon mucosa in vivo . Compared to free EMO-treatment of different doses in UC mice, the NPs could enhance the remedial efficacy of EMO in DAI decline, histological remission, and regulation of colitis indicators, such as myeloperoxidase (MPO), nitric oxide (NO), and glutathione (GSH). The inflammatory factors including induced nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), TNF-α, and IL-1β were suppressed by EMO/PSM NPs at both mRNA and protein levels. The obtained NPs could also promote the regeneration of the mucosal barrier via reduced fluorescein isothiocyanate (FITC)-dextran leakage in the transwell co-culture model and decreased serum zonulin levels, which was demonstrated to be associated with the upregulated tight junctions (TJs)-related proteins (claudin-2, occludin, and zo-1) and MUC2 at mRNA level. Moreover, the NPs could contribute to attenuating the liver injury caused by free EMO under excessive immune inflammation. Conclusion Our results demonstrated that EMO/PSM NPs could specifically release EMO in the diseased colon, and effectively enhance the anti-colitis effects of EMO related to intestinal barrier improvement. It can be considered as a novel potential alternative for oral colon-targeted UC therapy by increasing therapeutic efficacy and reducing side-effects.
研究领域:
药学
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纳米技术
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胃肠病学
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免疫学
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材料科学
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DOI
PubMed
高影响因子
Frontiers in Pharmacology
·
2022
·
IF 5.988
Pei Xie,Li-Jun Yan,Hong-Ling Zhou,Hui-Hui Cao,Yuan-Ru Zheng,Zi-Bin Lu,Hua-Yi Yang,Jia-Mei Ma,Yu-Yao Chen,Chuying Huo,Chunyang Tian,Jun-Shan Liu,Lin-Zhong Yu
Background: Acute lung injury (ALI) is a serious inflammatory disease with clinical manifestations of hypoxemia and respiratory failure. Presently, there is no effective treatment of ALI. Although emodin from Rheum palmatum L. exerts anti-ALI properties, the underlying mechanisms have not been fully explored.
Purpose: This study aimed to investigate the therapeutic effect and mechanism of emodin on LPS-induced ALI in mice.
Methods: RAW264.7 cells and zebrafish larvae were stimulated by LPS to establish inflammatory models. The anti-inflammatory effect of emodin was assessed by ELISA, flow cytometric analysis, and survival analysis. In vitro mechanisms were explored by using Western blotting, luciferase assay, electrophoretic mobility shift assay (EMSA), and small interfering RNA (siRNA) approach. The acute lung injury model in mice was established by the intratracheal administration of LPS, and the underlying mechanisms were assessed by detecting changes in histopathological and inflammatory markers and Western blotting in lung tissues.
Results: Emodin inhibited the inflammatory factor production and oxidative stress in RAW264.7 cells, and prolonged the survival of zebrafish larvae after LPS stimulation. Emodin suppressed the expression levels of phosphorylated JNK at Thr183/tyr182 and phosphorylated Nur77 at Ser351 and c-Jun, and increased the expression level of Nur77 in LPS-stimulated RAW264.7 cells, while these regulatory effects of emodin on Nur77/c-Jun were counteracted by JNK activators. The overexpression of JNK dampened the emodin-mediated increase in Nur77 luciferase activity and Nur77 expression. Moreover, the inhibitory effect of emodin on c-Jun can be attenuated by Nur77 siRNA. Furthermore, emodin alleviated LPS-induced ALI in mice through the regulation of the JNK/Nur77/c-Jun pathway.
Conclusions: Emodin protects against LPS-induced ALI through regulation on JNK/Nur77/c-Jun signaling. Our results indicate the potential of emodin in the treatment of ALI.Keywords: acute lung injury, inflammation, lipopolysaccharide, emodin, JNK/Nur77/c-Jun
研究领域:
药理学
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免疫学
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分子生物学
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DOI
PubMed
高影响因子
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
·
2026
·
IF 5.4
Hang Zhu,Haiyang He,Peilun Shen,Dianwen Liu,Guohui Wang,Haoxiang Wang,Yongchao Miao
Emodin (EM) was innovatively employed as a selective depressant for the flotation separation of chalcopyrite from talc. • EM exhibited significantly stronger adsorption on talc than on chalcopyrite. • EM selectively hindered PAX adsorption on talc while scarcely affecting chalcopyrite. • EM formed stronger Mg–O interactions on talc than Fe–O interactions on chalcopyrite. Talc and chalcopyrite both exhibit inherently high floatability, making their selective flotation separation particularly challenging. Therefore, the development of environmentally friendly depressants with high selectivity is essential for the efficient utilization of copper resources. In this study, the natural product emodin (EM) was employed as a novel green depressant for the flotation separation of chalcopyrite from talc. Under the optimum flotation conditions, EM effectively depressed talc flotation while exerting only limited influence on chalcopyrite, resulting in a recovery difference of 85.01 %age points between the two minerals. Artificial mixed-mineral flotation further confirmed the excellent separation performance, achieving a chalcopyrite recovery of 98.14% and a copper separation efficiency of 94.49%. Contact angle and zeta potential analyses demonstrated that EM effectively depressed talc flotation while exerting a limited influence on chalcopyrite flotation under potassium amyl xanthate (PAX) conditions. Microcalorimetry, XPS, and density functional theory (DFT) calculations further revealed that EM exhibited a much stronger affinity toward talc, preferentially forming stable Mg–O interactions with Mg active sites, whereas only relatively weaker Fe–O interactions were established on chalcopyrite. Collectively, these findings elucidate the molecular-level selective depression mechanism of EM toward talc, providing a theoretical basis for the efficient flotation separation of chalcopyrite from talc and the development of environmentally friendly flotation depressants. Download: Download high-res image (206KB) Download: Download full-size image
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DOI
高影响因子
RSC Advances
·
2020
·Vol. 10
·期 35
·20862-20871
·
IF 3.119
Guoyan Ren,He Sun,Gen Li,Jinling Fan,Lin Du,Guoting Cui
The molecular mechanism of interaction between aloe-emodin (AE) and trypsin was investigated, exhibiting remarkable outcomes. To detect the interaction mechanism, the binding of AE with trypsin was examined by a multi-spectroscopy and molecular docking method. Results showed that the binding of AE and trypsin would lead to static quenching and their binding forces were van der Waals forces and hydrogen bonding. The results of simultaneous and three-dimensional fluorescence spectroscopy showed that the combination of AE and trypsin caused changes in the microenvironment around the trypsin fluorophore, which might change the spatial structure of trypsin. FT-IR spectroscopy showed that the contents of α-helix and β-turn in trypsin were decreased and the contents of β-sheet, random coil and antiparallel β-sheet were increased. Moreover, all these experimental results were verified and reasonably explained by molecular docking results. We also investigated the enzyme activity of trypsin and the antioxidant activity of AE. The results showed that both the enzyme activity of trypsin and the antioxidant activity of AE were decreased after interaction between AE and trypsin. The findings outlined in this study should elucidate the molecular mechanisms of interaction between AE and trypsin and contribute to making full use of AE in the food industry.
研究领域:
生物化学
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食品科学
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药理学
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产品关联
DOI
PubMed
高影响因子
Cancer Cell International
·
2021
·Vol. 21
·期 1
·1-12
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IF 5.722
Jiang Dongxiao,Ding Shufei,Mao Zhujun,You Liyan,Ruan Yeping
Background Colon cancer is a malignant gastrointestinal tumour with high incidence, mortality and metastasis rates worldwide. Aloe-emodin is a monomer compound derived from hydroxyanthraquinone. Aloe-emodin produces a wide range of antitumour effects and is produced by rhubarb, aloe and other herbs. However, the mechanism by which aloe-emodin influences colon cancer is still unclear. We hope these findings will lead to the development of a new therapeutic strategy for the treatment of colon cancer in the clinic.Methods We identified the overlapping targets of aloe-emodin and colon cancer and performed protein–protein interaction (PPI), Gene Ontology (GO), and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analyses. In addition, we selected apoptosis pathways for experimental verification with cell viability, cell proliferation, caspase-3 activity, DAPI staining, cell cycle and western blotting analyses to evaluate the apoptotic effect of aloe-emodin on colon cancer cells.Results The MTT assay and cell colony formation assay showed that aloe-emodin inhibited cell proliferation. DAPI staining confirmed that aloe-emodin induced apoptosis. Aloe-emodin upregulated the protein level of Bax and decreased the expression of Bcl-2, which activates caspase-3 and caspase-9. Furthermore, the protein expression level of cytochrome C increased in a time-dependent manner in the cytoplasm but decreased in a time-dependent manner in the mitochondria.Conclusion These results indicate that aloe-emodin may induce the apoptosis of human colon cancer cells through mitochondria-related pathways.
研究领域:
肿瘤学
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药理学
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分子生物学
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细胞生物学
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DOI
PubMed
高影响因子
PHOTOCHEMICAL & PHOTOBIOLOGICAL SCIENCES
·
2020
·Vol. 19
·期 4
·485-494
·
IF 2.831
Ma Wenpeng,Liu Chengcheng,Li Jiao,Hao Ming,Ji Yanhong,Zeng Xiaoyan
The extensive and repetitive use of antifungal drugs has led to the development of drug-resistant Candida albicans . Antimicrobial photodynamic therapy (aPDT) has received considerable attention as an emerging and promising approach to combat drug-resistant microbes. This study evaluated the photodynamic effects mediated by aloe emodin (AE), a natural compound isolated from Aloe vera and Rheum palmatum, on azole-sensitive and azole-resistant C. albicans in vitro . AE exhibited no significant dark toxicity, but in the presence of light, effectively inactivated C. albicans cells in a concentration-dependent manner. The uptake of AE by fungal cells was investigated by confocal laser scanning microscopy (CLSM), and the results showed that AE possessed stronger ability to enter into C. albicans cells following light irradiation. Transmission electron microscopy analysis suggested that AE-mediated aPDT could induce damage to the cell wall, cytoplasm, and nucleus. Damage to the surface of C. albicans was observed by scanning electron microscopy. These results suggest that AE is a potential PS for use in aPDT of drug-resistant C. albicans strains, and AE-mediated aPDT shows promise as an antifungal treatment.
研究领域:
微生物学
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药理学
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抗菌治疗
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真菌病理学
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DOI
PubMed
高影响因子
ACS Omega
·
2021
·
IF 3.512
Guodong Zheng,Jiahui Zheng,Le Xiao,Tongyi Shang,Yanjun Cai,Yuwei Li,Yiming Xu,Xiaoming Chen,Yun Liu,Bin Yang
In this study, a pH-responsive nano-prodrug was fabricated by conjugating emodin to the PEGylated polyethyleneimine (mPEG-PEI) with acid-sensitive boronate ester bonds. 1H NMR spectra results showed that emodin was effectively bonded to mPEG-PEI, and acid-sensitive assay further confirmed the formation of boronate ester bonds. The size and morphology of the nano-prodrug were ascertained through transmission electron microscopy (TEM) and dynamic light scattering (DLS), which showed that the prodrug has a sphere-like shape with hydrodynamic size around 102 nm at pH 7.4. Subsequently, a drug-release behavior assay was carried out to carefully investigate the acid-sensitive drug-delivery property of the prodrug. Moreover, in vitro cell viability assay confirmed the superior cytotoxic effect of the nano-prodrug against HeLa cells compared to free emodin. Furthermore, the antibacterial study showed that the nano-prodrug could inhibit the bacterial (both Gram-positive and Gram-negative) growth more effectively than free emodin. Overall, this study provides a promising paradigm of the multifunctional nano-prodrug for pH-responsive tumor therapy and antibacterial activity.
研究领域:
药剂学
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肿瘤学
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微生物学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF PHARMACOLOGICAL SCIENCES
·
2024
·
IF 3
Zhihang Zhang,Yalan Luo,Xijing Zhuang,Haifeng Gao,Qi Yang,Hailong Chen
Acute lung injury (ALI) is closely related to high mortality in severe acute pancreatitis (SAP). This study unveils the therapeutic effect and mechanism of miR-217-5p on SAP-associated ALI. The miR-217-5p RNA expression was significantly up-regulated in lipopolysaccharide (LPS)-stimulated primary rat alveolar epithelial type II cells (AEC II) and sodium taurocholate-treated pancreas and lung in SAP rats. miR-217 inhibition protected AEC II from LPS-induced damage by inhibiting apoptosis and reducing the TNF-α, IL-6, and ROS levels. miR-217 inhibition suppressed apoptosis and alleviated mitochondrial damage through mitochondria-mediated apoptotic pathway in vitro . Sirt1 is a direct target of miR-217-5p. Dual-luciferase reporter assay confirmed the binding of miR-217-5p to Sirt1 mRNA 3′-UTR. The rescue experiment identified that the anti-apoptotic, anti-inflammatory, and anti-oxidative effects of miR-217 inhibition were mediated by Sirt1 in vitro . Emodin (EMO) protected AEC II from LPS-induced damage and alleviated pancreatic and lung tissue injuries. EMO exerted similar effects as miR-217 inhibition in vitro and in vivo . The effects of EMO were abolished by miR-217 overexpression. In conclusion, miR-217-5p inhibition exerts protective effects on SAP-ALI in vitro and in vivo by repressing apoptosis, inflammation, and oxidative stress through Sirt1 activation. EMO protects against lung injuries in SAP-associated ALI rats through miR-217-5p/Sirt1 axis.
研究领域:
药理学
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分子生物学
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病理生理学
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内科学
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产品关联
DOI
PubMed
高影响因子
AQUACULTURE
·
2025
·
IF 3.9
Yao Wang,Mengmeng Wang,Zhiyang Lin,Guangshuo Wang,Yunlong Qin,Mingzhu Liu,Fei Ling,Haifeng Jiang,Tianqiang Liu,Gaoxue Wang
Micropterus salmoides rhabdovirus (MSRV) is a highly pathogenic rhabdovirus that has caused significant economic losses in the aquaculture industry of largemouth bass. To date, there is no approved treatment for MSRV infection. In order to address this urgent need, virtual screening of the natural product monomer compound library targeting MSRV glycoprotein was conducted and the antiviral activity of 13 natural compounds identified in the screening was studied. Among these compounds, Aloe emodin (AE) exhibited high binding affinity and antiviral activity, inhibiting MSRV replication in grass carp ovary (GCO) cells with a half-maximal inhibitory concentration (IC 50 ) of 2.55 μM. Additionally, viral titers and cytopathic effects (CPE) were significantly reduced in the presence of AE. AE was demonstrated to directly destroy MSRV virions and inhibit their adsorption to GCO cells according to ultracentrifugation assay and viral binding assay. In vivo studies demonstrated that AE injection increased the survival rate of MSRV-infected largemouth bass by 63.3 %, which was 46.7 % higher than that of the virus group. RT-qPCR and pathological tissue section results demonstrated that AE treatment could significantly reduce viral loads in the liver, spleen, and kidney on days 1, 4, and 7 post-infection, and AE effectively mitigated tissue damage caused by MSRV infection. Circular dichroism (CD) spectroscopy and Isothermal titration calorimetry (ITC) showed that AE induced changes in the secondary structure of the MSRV glycoprotein and exhibited high affinity for the glycoprotein (Kd = 2.803 × 10 −5 M, ΔG = −25.99 kJ/mol). These results suggested that AE was a natural product with potent anti-MSRV activity through direct targeting of the glycoprotein.
研究领域:
病毒学
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水产养殖学
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药理学
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DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Jia Wan,Feng Wang,Meifang Zhong,Yongzhi Liang,Jun Wu
Conductive gels have been extensively explored in the field of wearable electronics due to their excellent flexibility and deformability. Traditional gels constructed from synthetic networks pose risks to biosecurity due to residual monomers like acrylamide, while pure biological hydrogels are plagued by inadequate mechanical performance. This study explores an innovative strategy, employing a dual-network (DN) system with purely biological components, as a superior alternative to conventional synthetic networks. By integrating gelatin and chitosan, two natural polymers with inherent biocompatibility and advantageous biomedical properties, this approach successfully avoids the toxic risk of synthetic polymers. By utilizing emodin, a natural extract from Rheum officinale , as a cross-linking agent for chitosan by Schiff base reactions, and Hofmeister effect of gelatin induced by sodium carbonate, the DN gelatin/chitosan/emodin organohydrogels achieve ultrahigh tensile strength (up to 9.45 MPa), tunable moduli (ranging from 0.07 to 3.42 MPa), excellent toughness (∼9.64 MJ/m 3 ), and high ionic conductivity (7.63 mS/cm). Remarkably, these conductive organohydrogels also exhibit high sensitivity (gauge factor up to 1.5) and ultrahigh linearity (R 2 up to 0.9995), making them promising candidates for soft human-motion sensors capable of accurately detecting and monitoring human movements in real time with high sensitivity and durability.
研究领域:
材料科学
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生物医学工程
·
化学
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DOI
PubMed
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2025
·
IF 13.2
Yuan Tian,Qing Xu,Ning Wang,Yanling Li,Wenyu Yang,Fei Huang,Qing Hao,Liping Zhao,Zhiruo Zhang,Fengchun Zhao,Fanglong Zhao
The intricate regulatory networks in filamentous fungi severely constrain the production of high-value natural products. Here, we developed an efficient CRISPR-dCas9-SunTag activation system to overcome transcriptional repression in Aspergillus nidulans . Through systematic optimization of GCN4 repeat numbers and implementation of P2A-mediated dCas9-SunTag/GCN4-VP64 tandem expression, this platform showed 20-fold higher activation efficiency compared to dCas9-VPR system. When deployed to regulate the emodin biosynthetic pathway, multiplexed sgRNA targeting enabled coordinated upregulation of three key biosynthetic genes mdpF , mdpG , and mdpH . This precise regulation approach minimized byproduct accumulation while boosting emodin titer to 101 mg/L, achieving 71 % higher production than the natural transcription factor overexpression. Furthermore, this optimized CRISPRa system demonstrated consistent stability during liquid fermentation in 1 L bioreactors (emodin 1.3 g/L) and solid-state fermentation (emodin 1.5 mg/g cell dry weight), highlighting its potential for scalable fungal metabolic engineering. This study establishes a modular and precise genetic toolkit for reprogramming fungal secondary metabolism, offering broad potential for the engineered biosynthesis of high-value compounds.
研究领域:
分子生物学
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基因工程
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合成生物学
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真菌生物技术
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天然产物生物合成
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高影响因子
危险品化学品经营许可证（带存储）