Bioengineered
·
2022
·
IF 6.832
Kenan Zheng,Baojiang Lv,Lulu Wu,Chen Wang,Haoyou Xu,Xiaojun Li,Zhibing Wu,Yuanqi Zhao,Zequan Zheng
Experimental autoimmune encephalomyelitis (EAE) is characterized by demyelination of the central nervous system. Emodin is an anthraquinone derivative with comprehensive anti-inflammatory, anti-cancer, and immunomodulatory effects and is widely used in the treatment of inflammatory, tumor, and immune system diseases. However, none of the clinical or experimental studies have explored the therapeutic efficacy of emodin in EAE/multiple sclerosis (MS). Thus, we evaluated the protective effect of emodin on EAE mediated via inhibition of microglia activation and inflammation. Wild-type mice were randomly divided into the normal control, EAE, low-dose emodin, and high-dose emodin groups. Clinical scores and pathological changes were assessed 21 days after immunization. The network pharmacology approach was used to elucidate the underlying mechanisms by using an online database. Molecular docking, polymerase-chain reaction tests, western blotting, and immunofluorescence were performed to verify the network pharmacology results. An in vivo experiment showed that high-dose emodin ameliorated clinical symptoms, inflammatory cell infiltration, and myelination. Pharmacological network analysis showed AKT1 was the main target and that emodin played a key role in MS treatment mainly via the PI3K–Akt pathway. Molecular docking showed that emodin bound well with PI3K, AKT1, and NFKB1. Emodin decreased the expression of phosphorylated(p)-PI3K, p-Akt, NF-κB, and myeloid differentiation factor 88 and the levels of markers (CD86 and CD206) in M1- and M2-phenotype microglia in EAE. Thus, the emodin inhibited microglial activation and exhibited anti-inflammatory and neuroprotective effects against EAE via the Myd88/PI3K/Akt/NF-κB signalling pathway. In conclusion, emodin has a promising role in EAE/MS treatment, warranting further detailed studies.
研究领域:
神经科学
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免疫学
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药理学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2018
·Vol. 8
·期 33
·18266-18271
·
IF 2.936
Jing Zhang,Xuan Wei,Yuanhang Wang,Bo Ren,Litao Zhao,Zhaoyan Wang,Qiaosheng Pu
Change in cation concentration, including that of potassium and sodium, is characteristic of apoptosis, therefore it is significant to detect cation concentration changes. In this work a rapid, sensitive, and practical method was developed for the determination of Na+ and K+ concentration in HeLa cells during emodin induced apoptosis by a low-cost capillary electrophoresis device with capacitively coupled contactless conductivity detection (CE-C4D). Under the optimized conditions, both ions were baseline separated in 4 min with 40 mM MES/40 mM His containing 1 mM 18-crown-6 as the separation buffer at pH 6.0. The limit of detections (LODs) and limit of quantifications (LOQs) were 0.47–1.15 μM and 1.58–3.86 μM, respectively. The precision for migration times and peak areas was below 0.56% and 3.74%, respectively. The data proved that the concentration of cations in cells can be accurately quantified. It was found that the K+ concentration decreased from 82.2 μM to 52.7 μM, and the Na+ concentration increased from 62.4 μM to 127.2 μM during the process of apoptosis when the cell density was 1 × 105 cells per mL. The low-cost CE-C4D provides a convenient way to decipher the interaction of Na+ and K+ in the regulation of cell apoptosis.
研究领域:
分析化学
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生物化学
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细胞生物学
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药理学
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2026
·Vol. 27
·期 10
·4411
·
IF 5.6
Rui Mao,Yuxia Guo,Haiyan Zhang,Ruiqi Wang,Yangang Cheng,Huifeng Li,Yan Wang,Yingli Wang
Emodin exhibits promising hepatomodulatory potential, yet its precise actions remain poorly characterized across distinct hepatic pathological states. Dose-dependent effects of emodin (40, 80, and 120 mg/kg) were investigated in mice with metabolic dysfunction-associated steatotic liver disease (MASLD), as well as healthy control mice, through integrated histopathological, biochemical, metabolomic, and gut microbiota profiling. The 80 mg/kg dose tended to yield the most favorable hepatoprotective outcomes in MASLD mice, whereas the 120 mg/kg dose was accompanied by apparent adverse hepatic alterations in normal mice. Correlative analyses further suggested that such divergent hepatic responses may be potentially linked to the gut microbiota–short-chain fatty acid (SCFA) axis, as well as the modulation of BAX/Bcl-2 balance and ESR1 expression. The hepatic effects of emodin are state- and dose-dependent. The dose of 80 mg/kg may represent a plausible candidate therapeutic range for MASLD, and the gut–liver axis is proposed as a likely underlying regulatory pathway.
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DOI
PubMed
高影响因子
LUMINESCENCE
·
2014
·Vol. 30
·期 1
·60-66
·
IF 1.675
Dan Li,Shaopu Liu,Yizhong Shen,Jidong Yang,Youqiu He
Water-soluble thioglycolic acid (TGA)-capped core/shell CdTe/CdS quantum dots (QDs) were synthesized. The interactions of rhein and emodin with TGA-CdTe/CdS QDs were evaluated by fluorescence and ultraviolet-visible absorption spectroscopy. Experimental results showed that the high fluorescence intensity of TGA-CdTe/CdS QDs could be effectively quenched in the presence of rhein (or emodin) at 570 nm, which may have resulted from an electron transfer process from excited TGA-CdTe/CdS QDs to rhein (or emodin). The quenching intensity was in proportion to the concentration of both rhein and emodin in a certain range. Under optimized conditions, the linear ranges of TGA-CdTe/CdS QDs fluorescence intensity versus the concentration of rhein and emodin were 0.09650–60 µg/mL and 0.1175–70 µg/mL with a correlation coefficient of 0.9984 and 0.9965, respectively. The corresponding detection limits (3σ/S) of rhein and emodin were 28.9 and 35.2 ng/mL, respectively. This proposed method was applied to determine rhein and emodin in human urine samples successfully with remarkable advantages such as high sensitivity, short analysis time, low cost and easy operation. Based on this, a simple, rapid and highly sensitive method to determine rhein (or emodin) was proposed. Copyright © 2014 John Wiley & Sons, Ltd.
研究领域:
分析化学
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材料科学
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药理学
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产品关联
DOI
PubMed
高影响因子
CHEMISTRY & BIODIVERSITY
·
2022
·Vol. 19
·期 4
·e202100928
·
IF 2.745
Yuan Zhong,Yuling Ding,Dandan Xiao,Donghua Hu,Yong Li
To integrate the active advantages of 18 β -glycyrrhetinic acid (18 β -GA) and emodin, improve bioavailability, increase efficiency, and reduce toxicity, a one-step innovative synthetic route was set up for the first time: 4-dimethylaminopyridine (DMAP) was used as catalyst, 1-ethyl-(3-dimethylaminopropyl)carboimide hydrochloride (EDCI) as condensation agent, dry dichloromethane (DCM) as solvent at 25 °C for 12 h, the three target products were obtained and purified by high performance liquid chromatography (HPLC), the chemical structures of them were characterized by nuclear magnetic resonance (NMR) technique and high resolution electron ionization mass spectrometry (HREI-MS), namely, 18 β -glycyrrhetinic acid-3-emodin ester ( 1 , yield 78.83 %, known), di-18 β -glycyrrhetinic acid-1-emodin ester ( 2 , yield 6.49 %, new), and di-18 β -glycyrrhetinic acid-8-emodin ester ( 3 , yield 1.81 %, new). To estimate their effects of the products on toxicity in zebrafish embryos and juvenile fishes, the two precursors and three target products were assayed involving in hatching rate, survival rate, morphology, heart rate, and apoptosis of cardiomyocytes. The results showed that the target products enhanced the hatching and survival rate of zebrafish embryos, decreased the malformation rate and the apoptosis of cardiomyocytes. It should be suggested that the one-step synthesis route with high yield makes the industrial application of the target products possible due to significantly reduced toxicity. The two new by-products provide potential candidates for the applications of pharmaceutical industry in the future.
研究领域:
药物化学
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毒理学
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生物化学
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药理学
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产品关联
DOI
PubMed
高影响因子
Frontiers in Pharmacology
·
2025
·
IF 4.8
Zhihui Li,Yanqiu Gu,Jianbo Yang,Shaozhan Wang,Shengnan Li,Panpan Chen,Ru Yao,Fangbin Liu,Ying Wang,Rong Wang,Yongfang Yuan
Introduction Polygonum multiflorum Thunb. (PM) is a representative traditional Chinese medicine (TCM) that exerts different effects in raw and processed forms. The hepatotoxicity of PM is markedly reduced after processing, whereas its hepatoprotective effects are enhanced. Purpose This study aimed to establish a novel comprehensive two-dimensional (2D) biochromatography system based on farnesoid X receptor (FXR), which is an important target in cholestatic liver injury (CLI), to investigate the material basis and mechanisms underlying the enhanced hepatoprotection and reduced hepatotoxicity of processed PM (P-PM). Methods A comprehensive 2D FXR biochromatography system was established by immobilizing FXR on 3-mercaptopropyltrimethoxysilane (MPTS)-modified silica gel. This system was used to identify the FXR-binding components in raw PM (R-PM) and P-PM. Molecular docking, surface plasmon resonance, and frontal affinity chromatography were used to validate the interactions. The hepatoprotective effects of emodin and physcion were assessed in α-naphthylisothiocyanate (ANIT)-induced CLI mouse models, and an FXR antagonist (Z-guggulsterone) rescue experiment was performed. The expression of FXR signaling-related proteins, including FXR, small heterodimer partner (SHP), bile salt export pump (BSEP), Na+-taurocholate cotransporting polypeptide (NTCP), and inflammatory cytokines, was assessed by Western blotting, real-time quantitative reverse transcription PCR, and immunofluorescence. Results The comprehensive 2D FXR biochromatography system successfully identified emodin and physcion as key FXR-binding components, with significantly increased content in P-PM. These components may contribute to the enhanced hepatoprotection and reduced hepatotoxicity of P-PM. In vivo , emodin and physcion alleviated ANIT-induced CLI, as evidenced by improved histopathological features and decreased serum levels of liver function markers. Mechanistically, both components upregulated the expression of FXR, BSEP, SHP, and NTCP while suppressing inflammatory cytokine expression. Their hepatoprotective effects and FXR-related upregulation could be disrupted by FXR antagonist Z-guggulsterone. These results suggest that emodin and physcion are key components contributing to the hepatoprotective effects of P-PM, likely through activation of the FXR signaling pathway and suppression of inflammation. Conclusion This study established a novel, efficient, rapid, and accurate comprehensive 2D FXR biochromatography system, which is suitable for screening targeted components in TCM, and can be extended to research on other TCMs.
研究领域:
生药学
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中医药学
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分子药理学
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天然产物化学
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肝脏疾病研究
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色谱分离技术
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产品关联
DOI
PubMed
高影响因子
Chinese Journal of Natural Medicines
·
2017
·
IF 1.667
Qiong YU,Li-Long JIANG,Na LUO,Ya-Xi FAN,Jiang MA,Ping LI,Hui-Jun LI
Polygoni Multiflori Radix (PMR) has been commonly used as a tonic in China for centuries. However, PMR-associated hepatotoxicity is becoming a safety issue. In our previous in vivo study, an interaction between stilbenes and anthraquinones has been discovered and a hypothesis is proposed that the interaction between stilbene glucoside-enriching fraction and emodin may contribute to the side effects of PMR. To further support our previous in vivo results in rats, the present in vitro study was designed to evaluate the effects of 2, 3, 5, 4′-tetrahydroxystilbene-2- O-β -D-glucopyranoside (TSG) on the cellular absorption and human liver microsome metabolism of emodin. The obtained results indicated that the absorption of emodin in Caco-2 cells was enhanced and the metabolism of emodin in human liver microsomes was inhibited after TSG treatment. The effects of the transport inhibitors on the cellular emodin accumulation were also examined. Western blot assay suggested that the depressed metabolism of emodin could be attributed to the down-regulation of UDP-glucuronosyltransferases (UGTs) 1A8, 1A10, and 2B7. These findings definitively demonstrated the existence of interaction between TSG and emodin, which provide a basis for a better understanding of the underlying mechanism for PMR-induced liver injury.
研究领域:
药理学
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毒理学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
NANOTECHNOLOGY
·
2022
·Vol. 33
·期 27
·275604
·
IF 3.953
Kai Cheng,Jie Zhou,Yujie Zhao,Yu Chen,Lan Ming,Da Huang,Rui Yang,Zhenyu Lin,Daozhen Chen
Herein, an amphiphilic block copolymer CD44-targeting peptide-conjugated polyethylene glycol-block-hydroxyethyl starch-block-poly (L-lactic acid) (CD44p-conjugated PEG-b-HES-b-PLA) are synthesized, which could self-assemble into the pH-responsive and CD44-targeting polymer micelles against breast cancer cells MDA-MB-231. Emodin (Emo) is a natural anthraquino with pharmacological activities in anti-tumor effects. However, Emo suffers from poor water solubility, low biocompatibility, rapid systemic elimination, and off-target side effects, resulting in unsatisfactory treatment outcomes. Nanotechnology-based drug delivery systems have proven great potential for cancer chemotherapy. The constructed polymeric micelles Emo@CD44p-PM have exhibited an average size of 154.5 ± 0.9 nm characterized by DLS and TEM. Further, the Emo@CD44p-PM have effective Emo-loading capacity, good thermal stability, and pH responsiveness. Intracellular uptake study shows the enhanced cellular internalization of Emo@CD44p-PM due to the increased exposure of CD44p enhances the cellular internalization of Emo@CD44p-PM effectively. Furthermore, the in vitro results showed Emo@CD44p-PM has been observed good biocompatibility and anti-tumor effects. Therefore, the polymeric micelles Emo@CD44p-PM provide a promising delivery strategy of targeted therapy for breast cancer.
研究领域:
纳米技术
·
药学
·
癌症研究
·
高分子化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CHEMICO-BIOLOGICAL INTERACTIONS
·
2022
·
IF 5.168
Xu Wang,Lingwen Dong,Guode Zhao,Weiwei Li,Ying Peng,Jiang Zheng
2,3,5,4′-Tetrahydroxy stilbene-2-Ο- β -D-glucoside (TSG) and emodin (EMD) are two main components of Polygonum multiflorum Thunb. (PMT). Its root is widely used as herbal medicine and supplement. However, PMT-induced liver injury has drawn increasing attention. The purpose of this study was to investigate the interaction of TSG with EMD in the aspects of enzymology , pharmacokinetics , and hepatotoxicity. Co-administration with TSG increased internal exposure of EMD, EMD-derived hepatic protein adduction, and EMD-induced liver injury in mice. Mouse and human liver microsomal incubation study demonstrated that co-incubation with TSG decreased the formation of hydroxylation metabolites of EMD. Human recombinant cytochrome P450 enzyme incubation study showed that TSG induced time-, concentration-, NADPH-dependent and irreversible inhibition of CYP2C19 and CYP3A4 . An epoxide metabolite derived from TSG was responsible for the observed enzyme inactivations. The findings allow us to better understand the mechanisms by which herbal processing detoxifies raw PMT.
研究领域:
药理学
·
毒理学
·
酶学
·
中药学
✓ 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）