CANADIAN JOURNAL OF PHYSIOLOGY AND PHARMACOLOGY
·
2012
·Vol. 90
·期 4
·
IF 1.953
ChenDapeng,XiongYongjian,WangLi,LvBochao,LinYuan
Emodin is traditionally used as a laxative and is found to increase or decrease the contractility of intestinal smooth muscle in low doses and high doses, respectively. In this study, we propose that bidirectional regulation (BR) on the contractility of jejunal smooth muscle (CJSM) is inducible by emodin in the absence of control by the central nervous system. The results indicated that emodin-induced BR had the following characteristics. A stimulatory effect on CJSM was induced by emodin at 7 low contractile states, and an inhibitory effect was induced on CJSM at 7 high contractile states. Emodin-induced BR on myosin phosphorylation was also observed. BR was not observed in the presence of tetrodotoxin, suggesting that enteric nervous system is required for producing BR. The stimulatory effect of emodin on CJSM was abolished by atropine and diphenhydramine, respectively, suggesting that BR was correlated with cholinergic and histamine system while jejunal smooth muscle was at low contractile state. The inhibitory effect of emodin on CJSM was abolished by phentolamine, propranolol, and L-NG-nitroarginine (L-NNA), respectively, suggesting that BR was related to adrenergic hyperactivity and with a nitric oxide relaxing mechanism while jejunal smooth muscle was in a high contractile state. The exact mechanism, however, needs further investigation.
研究领域:
药理学
·
生理学
·
胃肠病学
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DOI
PubMed
高影响因子
MOLECULAR DIVERSITY
·
2026
·
IF 4.3
Yang Yangyang,Sun Dezhong,Jia Qingyun,Zhu Bing,Lv Huaiqing,Che Fengyuan
Excitotoxicity is a core pathological mechanism underlying various neurological disorders, including depression. It is primarily driven by the overactivation of NMDA receptors and disruption of calcium homeostasis. However, effective therapeutic interventions targeting this process remain limited. In this study, aloe-emodin was shown to reverse NMDA-induced reduction in cell viability, apoptosis, and calcium overload in a dose-dependent manner, while also attenuating NMDA-induced autophosphorylation of CaMKII. In a chronic unpredictable mild stress (CUMS) model, aloe-emodin significantly ameliorated depression-like behaviors, suppressed inflammatory responses and oxidative stress, and downregulated the expression of cleaved-PARP. By conducting biotin pull-down coupled with liquid chromatography-tandem mass spectrometry (LC–MS/MS) analysis, cellular thermal shift assay (CETSA), drug affinity responsive target stability (DARTS) analysis, and surface plasmon resonance (SPR) analysis, RANBP9 was identified as a direct molecular target of aloe-emodin, with a binding affinity (KD) of 716 nM. Molecular docking and molecular dynamics simulations revealed that aloe-emodin selectively binds to the His332 residue of RANBP9. Aloe-emodin promoted the degradation of RANBP9 via the ubiquitin–proteasome pathway by facilitating the interaction between RANBP9 and the E3 ligase CHIP. After RANBP9 was knocked down, the protective effects of aloe-emodin on cell viability and apoptosis were significantly weakened, confirming that the anti-excitotoxic activity of aloe-emodin is RANBP9-dependent. These findings collectively demonstrate that aloe-emodin is a novel and potent RANBP9-targeting compound with antidepressant activity and suggest that RANBP9 may serve as a promising target for developing antidepressant drugs. Graphical abstract
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高影响因子
JOURNAL OF ELECTROANALYTICAL CHEMISTRY
·
2021
·
IF 4.464
Lijie Hou,Chao Kong,Zhongai Hu,Yanxia Han,Bowan Wu
Emodin is a natural anthraquinone derivative and contains abundant hydroxyl and carbonyl groups, which has high redox activity. As guest molecules, Emodin molecules were anchored on graphene sheet (GNS) by simple one-step reflux method. In the three-electrode system, the optimal composite electrode material (E@GNS) obtained the high specific capacitance of 338.9 F g −1 at 5 mV s −1 and excellent rate capability in 1 mol L −1 H 2 SO 4 . Finally, an asymmetric supercapacitor (ASC) was fabricated by using E@GNS as negative electrode and Caffeic acid non-covalently modified graphene hydrogel (GH-CFA) as positive electrode, respectively. The device achieved the energy density of 32.8 Wh kg −1 along with power density of 0.8 kW kg −1 , and a light-emitting diode (LED) could be light up by two ASCs in series. To compare with the performance of ASC, we also assembled symmetric supercapacitor based on E@GNS, proving that the good matching of positive and negative electrode materials could make the supercapacitor exhibit the best capacitive performance.
研究领域:
材料科学
·
电化学
·
能源存储
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DOI
高影响因子
Open Chemistry
·
2020
·Vol. 18
·期 1
·1207-1216
·
IF 1.216
Lishan Tan,Xiulong Deng,Xuandi Lai,Tao Zeng,Aiqing Li,Jianqiang Hu,Zuying Xiong
The aim of this study is to explore the kidney-targeting capability of mesoscale nanoparticles (MNPs)-emodin (Em-MNPs) and its potential antifibrosis in the animal model. First, MNPs and Em-MNPs were synthesized via nanoprecipitation method, and their diameters were both ∼400 nm with the uniform size. The entrapment efficiency of MNPs was 45.1% when adding emodin at the concentration of 12 mg/mL. Moreover, cytotoxicity assay showed that Em-MNPs presented excellent biocompatibility in rat proximal tubular cells. Cellular uptake assay demonstrated that Em-MNPs had high-efficiency uptake, especially in the cytoplasm. Ex vivo organ fluorescence imaging revealed that Em-MNPs possessed specific kidney-targeting ability with relative long retention time in the kidney (∼24 h). In the renal unilateral ureteral obstruction model, Em-MNPs treatment could significantly alleviate kidney tubule injury and reduce extracellular matrix deposition compared with free MNPs. Herein, Em-MNPs with specific kidney-targeting and preferable antifibrosis effects in animal model may pave an avenue for treating renal diseases.
研究领域:
药理学
·
纳米技术
·
肾病学
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产品关联
DOI
高影响因子
Biomaterials Science
·
2018
·Vol. 7
·期 3
·867-875
·
IF 5.831
Yonghong Song,Zhujun Sheng,Yunjun Xu,Liang Dong,Weiping Xu,Fangyuan Li,Jing Wang,Zeyu Wu,Yi Yang,Yang Su,Xiaolian Sun,Daishun Ling,Yang Lu
As an active natural ingredient extracted from the plant Rheum palmatum, emodin exhibits various pharmacological activities, especially the inhibition of tumor growth and migration. However, the anticancer activity of emodin is limited mainly due to its poor solubility and the lack of specific targeting. Herein, we employed liposome to load emodin into the lipid bilayer, and high-performance ferromagnetic iron oxide nanocubes were simultaneously encapsulated in the hydrophilic bilayer. The optimized magnetic liposomal emodin nanocomposite (MLE) exhibited a 24.1% increase in the efficiency of killing MCF-7 cancer cells at a low concentration of 16 μg mL−1 compared with that of the hydrophobic free emodin. A further 8.67% enhancement of the killing efficiency was obtained by magnetic targeting. Benefitting from the high ferromagnetism, the transverse relaxivity (r2) of MLE was measured to be as high as 392.9 mM−1 s−1. With guidance from the external magnetic field, the effective accumulation of this magnetic liposome in the tumor region of a 4T1 breast tumor bearing mouse was observed by both MR tracking and fluorescence imaging, which should be beneficial for decreasing the required therapeutic dose of emodin. Hemolysis, cytotoxicity and biochemistry assays confirmed the excellent biocompatibility of this magnetic liposomal carrier. The anti-tumor therapeutic effect of MLE was further investigated in vivo, and the tumor in the therapeutic group was almost eliminated, indicating that this magnetic liposomal emodin could serve as a novel magnetically guided theranostic nanoagent.
研究领域:
药理学
·
肿瘤学
·
纳米医学
·
生物材料
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产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACOLOGY
·
2022
·
IF 5.195
Chujun Chen,Zhenming Lin,Wenbin Liu,Qiong Hu,Jie Wang,Xiaoyan Zhuang,Sujuan Guan,Xiaoting Wu,Tingting Hu,Shijian Quan,Xiaobao Jin,Juan Shen
Diabetic wound healing, characterized by chronic inflammation , remains a medical challenge. The failure of prompt conversion from pro-inflammatory M1-like macrophage to pro-healing M2-like macrophage is the main obstacle to diabetic wounds. Emodin , an anthraquinone derivative , has multiple bioactivities, including antibacterial, anticancer, and anti-inflammatory. Recently, emodin has shown potential in promoting wound healing. However, the underlying molecular mechanism remains unclear. In this study, we examined the effects of emodin on wound healing in db/db diabetic mice using a full-thickness excision model. Our results showed that emodin can remarkably accelerate healing by enhancing extracellular matrix (ECM) synthesis and granulation tissue formation. We identified 32 potential targets of emodin by network pharmacology analysis, and our transcriptome analysis highlighted the down-regulation of the NF-κB signaling pathway mediated by emodin. Mechanistically, emodin was shown to inhibit the p65-NF-κB complex and promote the proportion of M2 (anti-inflammatory)-like phenotype macrophages both in vitro and vivo. Then, bone-marrow-derived macrophages were co-cultured with fibroblasts (mouse dermal fibroblasts cells). Treatment of emodin significantly increased the proportion of M2-polarized macrophages and the expression level of TGF-β, a typical ECM formation-related cytokine secreted by the M2 macrophages in the co-cultured supernatant. We further revealed that emodin improved the proliferation of mouse dermal fibroblasts (MDFs) cells and upregulated the expression levels of collagen III, fibronectin and α-SMA in MDFs cells in emodin-treated co-culture systems. 1D11, a neutralizing antibody for all three major TGF-β isoforms, diminished the biological effects of emodin on proliferation and ECM formation in MDFs cells. Taken together, our study suggests emodin may serve as an effective therapeutic agent for diabetic wounds.
研究领域:
药理学
·
免疫学
·
伤口愈合
·
糖尿病
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产品关联
DOI
PubMed
高影响因子
RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY
·
2024
·Vol. 50
·期 4
·1466-1475
·
IF 1.1
Lu Liushen,Qin Ting,Chen Kai,Xie Jun,Pan Liangkun,Xi Bingwen
Abstract Objective: Resveratrol, a natural product found in plants, is a polyphenolic compound with strong antioxidant activity. In order to enhance the antioxidant activity of resveratrol, we have used a natural product emodin, which has multiple hydroxyl group structure similar to resveratrol. Methods: In this study, we investigated the antioxidant activities of resveratrol and emodin in vitro respectively, including their abilities to scavenge 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radicals, hydroxyl radicals, and superoxide radicals. Results and Discussion: our results demonstrated that the combination of resveratrol and emodin significantly enhances antioxidant activity. And the process of their DPPH radical scavenging follows a first-order reaction kinetics equation. Finally, a possible mechanism for the scavenging of DPPH free radicals by resveratrol and emodin was proposed. Conclusions: We found that emodin combined with resveratrol can increase antioxidant activity. This study provides a new sight to enhance antioxidant activity.
研究领域:
药理学
·
生物化学
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产品关联
DOI
高影响因子
INTERNATIONAL IMMUNOPHARMACOLOGY
·
2018
·
IF 3.118
Shuang Luo,Xiangliang Deng,Qi Liu,Zengfeng Pan,Zhongxiang Zhao,Lian Zhou,Xia Luo
Emodin is an anthraquinone compound derived from Rheum officinale Baill . Several reports showed that emodin had efficacy on acute pancreatitis , keratitis , myocarditis , and rheumatoid arthritis . However, the potency of emodin on ulcerative colitis(UC) remains unclear. In this study, we investigated the effect of emodin on dextran sodium sulfate (DSS)-induced ulcerative colitis in mice. Our results showed that emodin significantly alleviated the symptoms of DSS-induced UC in mice, involving prevented the loss of body weight and colon shortening, decreased the disease activity index (DAI), intestinal damages and the count of white blood cells (WBC) in peripheral blood. In addition, emodin treatment decreased the level of anti-flagellin antibody in serum and significantly down-regulated the expression of TLR5 and NF-κB p65 in colon of the UC mice. Further study in vitro showed that emodin down-regulated the expression of TLR5 and MyD88 , up-regulated the expression of IκB, inhibited the nuclear translocation of NF-κB p65 and decreased the release of IL-8 in flagellin-stimulated HT-29 cells. These results, for the first time, demonstrated that emodin had the therapeutic potential to ameliorate UC symptoms possibly via regulating the flagellin-TLR5 signaling pathway . Emodin may be a potential candidate ingredient for ulcerative colitis.
研究领域:
药理学
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免疫学
·
胃肠病学
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产品关联
DOI
PubMed
高影响因子
TOXICOLOGY AND APPLIED PHARMACOLOGY
·
2018
·
IF 3.616
Lili Wu,Yulian Chen,Han Liu,Zhikun Zhan,Zhi Liang,Tao Zhang,Zheng Cai,Ling Ye,Menghua Liu,Jie Zhao,Shuwen Liu,Lan Tang
Aggravating effect of probenecid (a traditional anti-gout agent) on emodin-induced hepatotoxicity was evaluated in this study. 33.3% rats died in combination group, while no death was observed in rats treated with emodin alone or probenecid alone, indicating that emodin-induced (150 mg/kg) hepatotoxicity was exacerbated by probenecid (100 mg/kg). In toxicokinetics-toxicodynamics (TK-TD) study, aspartate aminotransferase (AST) and systemic exposure (area under the serum concentration-time curve, AUC ) of emodin and its glucuronide were significantly increased in rats after co-administrated with emodin and probenecid for 28 consecutive days. Results showed that the increased AUC (increased by 85.9%) of emodin was mainly caused by the decreased enzyme activity of UDP-glucuronosyltransferases (UGTs, decreased by 11.8%–58.1%). In addition, AUC of emodin glucuronide was increased 5-fold, which was attributed to the decrease of multidrug-resistant-protein 2 (MRP2) protein levels (decreased by 54.4%). Similarly, in vitro experiments proved that probenecid reduced the cell viability of emodin-treated HepG2 cells through inhibiting UGT1A9, UGT2B7 and MRP2. Our findings demonstrated that emodin-induced hepatoxicity was exacerbated by probenecid through inhibition of UGTs and MRP2 in vivo and in vitro , indicating that gout patients should avoid taking emodin-containing preparations in combination with probenecid for a long time.
研究领域:
药理学
·
毒理学
·
药学
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DOI
PubMed
高影响因子
ADSORPTION-JOURNAL OF THE INTERNATIONAL ADSORPTION SOCIETY
·
2016
·Vol. 22
·期 7
·871-878
·
IF 1.87
Ge Li,Huang Hao,Qin Yanshu,Xia Fan,Yang Kedi
Ionic liquids (ILs)-bonded silica adsorbents were prepared by chemical modification of the silica surface using N -alkylimidazolium-based ILs with Cl − , BF 4
− , PF 6
− or NO 3
− anion, and applied to selective separation of the model mixture of luteolin and aloe-emodin. Among the investigated ILs-bonded silica materials, the silica grafted with N -octyllimidazolium hexafluorophosphate ([C 8 mim]PF 6 @SiO 2 ) exhibited higher adsorption capacity and selectivity of luteolin from the model mixed solution of luteolin and aloe-emodin. The isotherm data of luteolin on [C 8 mim]PF 6 @SiO 2 correlated better to the Freundlich model than the Langmuir model, and the calculated thermodynamic parameters indicated that the adsorption of luteolin was spontaneous and exothermic. The dynamic adsorption and elution experiments demonstrated that the high adsorption capacity and good desorption efficiency of luteolin on fixed bed packed with the [C 8 mim]PF 6 @SiO 2 . Moreover, the results from batch adsorption and dynamic adsorption showed well selective separation towards the model mixture of luteolin and aloe-emodin.
研究领域:
化学工程
·
分离科学
·
药物化学
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DOI
高影响因子
PHYTOTHERAPY RESEARCH
·
2021
·Vol. 35
·期 9
·5203-5213
·
IF 5.882
Shanshan Dai,Bozhi Ye,Longwang Chen,Guangliang Hong,Guangju Zhao,Zhongqiu Lu
Myocardial injury and cardiovascular dysfunction are serious consequences of sepsis and contribute to high mortality. Currently, the pathogenesis of myocardial injury in sepsis is still unclear, and therapeutic approaches are limited. In this study, we investigated the protective effect of emodin on septic myocardial injury and the underlying mechanism. Lipopolysaccharide (LPS)-induced C57BL/6 mice and cardiomyocytes were used as models of sepsis in vivo and in vitro, respectively. The results showed that emodin alleviated cardiac dysfunction, myocardial injury and improved survival rate in LPS-induced septic mice. Emodin attenuated the levels of inflammatory cytokines and cardiac inflammation induced by LPS. Emodin reduced NOD-like receptor protein 3 (NLRP3) and Gasdermin D (GSDMD) expression in the heart tissue of LPS-induced septic mice. In vitro, emodin alleviated LPS-induced cell injury and inflammation in cardiomyocytes by inhibiting NLRP3 inflammasome activation. In addition, an NLRP3 inhibitor was used to further confirm the function of the NLRP3 inflammasome in LPS-induced myocardial injury. Taken together, our findings suggest that emodin improves LPS-induced myocardial injury and cardiac dysfunction by alleviating the inflammatory response and cardiomyocyte pyroptosis by inhibiting NLRP3 inflammasome activation, which provides a feasible strategy for preventing and treating myocardial injury in sepsis.
研究领域:
药理学
·
免疫学
·
心脏病学
·
传染病学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF COLLOID AND INTERFACE SCIENCE
·
2025
·
IF 9.7
Zehao Li,Ying Lu,Jianbo Song,Peide Han,Huixian Shi,Xiaohong Yao,Xiangyu Zhang,Guannan Zhang
Emodin (ED), as a traditional Chinese medicine, possesses a variety of biological activities and is also one of natural sonosensitizer. Whether emodin could react with titanium dioxide to enhance the sonodynamic activity for safely treating osteomyelitis remains to be explored. Hence, an ED-conjugated Mn-doped titanium dioxide (TOM) nanorod array is designed and prepared on titanium to eliminate bacterial infections under ultrasound (US) treatment. The doping of Mn and the formation of an inorganic–organic interfacial between ED and TOM cause an imbalance in the interfacial charge and reduce the band gap of TOM, thereby increasing the production of reactive oxygen species (ROS) under US. The generated ROS effectively destroys the bacterial cell membrane, accelerating Mn ions intake and thereby inducing ferroptosis-like death of MRSA. Moreover, the hybrid coating activates cAMP and cGMP-PKG pathways to modulate M1 polarization of macrophages to display potent phagocytosis to bacteria. After eliminating the bacterial infection, the coating also can facilitate macrophage M2 polarization to promote osteogenic differentiation. Overall, the Chinese medicine enhanced sonodynamic and immunotherapy have great promise in treating bacterial-infected osteomyelitis.
研究领域:
纳米技术
·
生物医学工程
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药学
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免疫学
·
骨科
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DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）