Drug Design Development and Therapy
·
2022
·
IF 4.319
Nianxiu Tian,Yanbin Gao,Xiaolei Wang,Xiaoming Wu,Dawei Zou,Zhiyao Zhu,ZheJi Han,Tao Wang,Yimin Shi
Background Endoplasmic reticulum stress is associated with podocyte apoptosis in the pathogenesis of diabetic nephropathy (DN). A previous study has demonstrated that emodin has a protective effect in the kidney by suppressing proliferation of mesangial cells and inhibiting the renal tubular epithelial-to-mesenchymal transition. However, the effects of emodin on the podocyte apoptosis in DN and its mechanisms are unknown.Aim This study aimed to explore the effect of emodin on DN model KK-Ay mice and high glucose induced podocytes apoptosis via the PERK–eIF2α pathway.Methods KK-Ay mice model of DN were treated with emodin at dose of 40 and 80 mg/kg/day for 8 weeks. Urine albumin, serum creatinine, blood urea nitrogen levels and the renal histopathology in mice were performed. In vitro, conditionally immortalized mouse podocytes exposed to HG (30mM) were incubated with emodin. Cell viability was measured by CCK-8 assay. Additionally, we performed RNA interference and measured the apoptosis in cultured podocytes treated with emodin. Immunohistochemistry, immunofluorescence, western blot, and real-time PCR were used to detect gene and protein expression both in vivo and in vitro.Results The results showed that emodin treatment ameliorated urine albumin, serum creatinine, and blood urea nitrogen of DN mice. The pathological damage of kidney tissue was also improved after treatment with emodin. Moreover, emodin increased nephrin expression. Podocytes apoptosis and endoplasmic reticulum stress markers (GRP78) were significantly reduced upon emodin treatment. Furthermore, emodin treatment decreased the expression of phosphorylated protein kinase RNA-like endoplasmic reticulum kinase (P-PERK), phosphorylated P-eIF2α, ATF4, and CHOP. In vitro, emodin treatment was further found to decrease the GRP78 level induced by high glucose or tunicamycin (TM). Besides, emodin and PERK knockdown inhibited the apoptosis of podocytes cultured in high glucose by counteracting the upregulation of phosphorylated PERK, phosphorylated eIF2α, ATF4, and CHOP.Conclusion Overall, the findings indicate that emodin mitigates podocytes apoptosis by inhibiting the PERK-eIF2α signaling pathway in vivo and in vitro, and, therefore, exerts a protective action on podocytes in DN.
研究领域:
药理学
·
肾病学
·
分子生物学
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Applied Polymer Materials
·
2023
·
IF 5
Yiwen Pan,Shaoqing Chen,Yanyan Meng,Mu He,Chun Liu,Cheli Wang,Xinye Ni
The treatment of bone defects caused by diseases, trauma, or tumor has always been a great clinical challenge. Implantation of bone biomaterials into bone defect areas is an effective method for bone injury repair. In this study, we used three-dimensional (3D) printing technology to prepare nano-hydroxyapatite (nHA)/sodium alginate (SA)/gelatin (Gel) hydrogel scaffolds loaded with different ratios (0, 0.13, 0.26, 0.39, 0.53, and 0.79‰) of emodin (EM) (EM/nHA/SA/Gel). Scanning electron microscopy showed that the scaffolds had a smooth surface without fracture and nHA was evenly distributed on the surface. The cell proliferation and migration results showed that the 0.39‰ EM group, in particular, could significantly promote the proliferation and migration of mouse embryonic osteoblast precursor (MC3T3-E1) cells and significantly increase the mRNA expression of osteogenic differentiation-related genes (bone morphogenetic protein/BMP-2, BMP-9, osteocalcin). In addition, the 0.39‰ EM group exhibited the best effect on osteogenic differentiation-related proteins (alkaline phosphatase, Runx 2, OSX). The expression of M2 polarization-related genes (arginase-1, CD206) also significantly increased after the treatment with the 0.39‰ EM group. Micro-CT showed that in the rat skull defect model, the EM/nHA/SA/Gel scaffold group significantly promoted bone regeneration after being implanted into the skull for 30 days. Our results indicate that the EM/nHA/SA/Gel hydrogel scaffolds can not only directly promote the proliferation and differentiation of osteoblasts but also indirectly promote osteogenic differentiation by supporting M2 polarization of macrophages. EM/nHA/SA/Gel hydrogel scaffolds are potential bone tissue engineering materials for bone regeneration.
研究领域:
生物医学工程
·
组织工程
·
骨科
·
材料科学
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2023
·
IF 5.8
Wendi Liang,Yingzhen Fan,Yinghui Liu,Ting Fang,Jian Zhang,Yuyi Xu,Ji Li,Dongkai Wang
The high level of reactive oxygen species (ROS) at the tumor site has been widely used in the tumor targeted delivery. However, the ROS stimulus-responsive vector itself is also a ROS consumer, and the consumption of endogenous ROS may not be sufficient to maintain sustained drug release. In this study, we designed and synthesized ROS/pH dual-sensitive polymer micelles for the co-delivery of emodin (EMD) and chlorambucil (CLB). The release of quinone methides (QM) can consume GSH, on the one hand, it can enhance the chemotoxicity of phenylbutyrate nitrogen mustard, on the other hand, emodin can induce oxidative damage of tumor cells and maintain the sustained targeted release of drugs.
研究领域:
药学
·
癌症研究
·
纳米技术
·
药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2026
·
IF 8.7
Zhenhua Li,Fengjie Liu,Fansu Meng,Mulazim Hussain Asim,Huan Wang,Honghui Gu,Qi Li,Lina Yang,Zhenjiang Yang,Tiange Cai,Yu Cai
Emodin is a natural anthraquinone derivative with a variety of pharmacological effects such as anti-inflammatory and anti-cancer. However, its clinical application is hindered by poor water solubility and low bioavailability. To address these limitations, we developed carboxymethyl chitosan and poly(acrylic acid)/poly(allylamine hydrochloride)-modified hollow mesoporous manganese dioxide nanoparticles (CPPMNP) for emodin loading (ECPPMNP). The zeta potential of ECPPMNP was −26.4 ± 0.5 mV, the average particle size was (67.2 ± 4.7) nm, and the drug loading and encapsulation efficiency were (23.90 ± 0.29) % and (62.80 ± 0.99) %, respectively. In vitro studies, cell experiments confirmed that ECPPMNP were efficiently internalized by MDA-MB-231 triple-negative breast cancer cells, facilitating emodin release and significantly suppressing intracellular reactive oxygen species production, thereby inhibiting tumor cell proliferation. Due to the introduction of amide bonds on the surface of the nanoparticles, the nanoparticles have pH/redox dual-responsiveness, which allows them to effectively achieve controlled release of emodin at tumor sites that are more acidic and abundantly expressed glutathione. In vivo anti-tumor experiments showed that ECPPMNP significantly aggregated at the tumor site and inhibited the growth of subcutaneous tumors in nude mice, and the final tumor inhibition rate reached 81.9%. This nanocarrier system has good biocompatibility and is expected to be an effective therapeutic strategy in the field of triple negative breast cancer treatment in the future. Download: Download high-res image (133KB) Download: Download full-size image
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Drug Delivery and Translational Research
·
2021
·Vol. 12
·期 3
·603-614
·
IF 4.617
Shi Feng,Chen Lin,Wang Yaping,Liu Jing,Adu-Frimpong Michael,Ji Hao,Toreniyazov Elmurat,Wang Qilong,Yu Jiangnan,Xu Ximing
The objective of this study was to fabricate a novel drug delivery system using Soluplus® (polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol graft copolymer) and glycyrrhizic acid to improve solubility, bioavailability, and anti-hyperuricemic activity of aloe emodin (AE). The AE-loaded mixed micelles (AE-M) were prepared by thin-film hydration method. The optimal AE-M contained small-sized (30.13 ± 1.34 nm) particles with high encapsulation efficiency (m/m, %) of 90.3 ± 1.08%. The release rate of AE increased in the micellar formulation than that of free AE in the four media (DDW, pH 7.0; phosphate buffer solution, pH 7.4; phosphate buffer solution, pH 6.8; and hydrochloric acid aqueous solution, pH 1.2). In comparison to free AE, the pharmacokinetic study of AE-M showed that its relative oral bioavailability increased by 3.09 times, indicating that mixed micelles may promote gastrointestinal absorption. More importantly, AE-M effectively reduced uric acid level by inhibiting xanthine oxidase (XOD) activity in model rats. The degree of ankle swelling, serum levels of interleukin (IL)-1, and IL-6-related inflammatory factors levels all decreased in the gouty arthritis model established via monosodium urate (MSU) crystals. Taken together, the AE-M demonstrated the potential to improve the bioavailability, anti-hyperuricemic activity, and anti-inflammation of AE. Graphical abstract
研究领域:
药剂学
·
药物递送系统
·
代谢疾病
✓ 已验证
产品关联
DOI
PubMed
高影响因子
NANO
·
2019
·
IF 1.293
Chao Yu,Jian Lu,Qi Zhang,Hougang Fan,Minjia Meng,Shi Zhou,Yinhua Jiang,Yongsheng Yan,Yilin Wu,Chunxiang Li
High purity emodin is in great demand with the development of medical treatment. Molecularly imprinted membranes (MIMs) have gained wide attention for selective separation of emodin due to its preferable selectivity. In this work, we describe a simple two-step method for developing emodin-imprinted TiO 2 @CA (ETMIMs) and emodin-imprinted SiO 2 @CA (ESMIMs) based on organic–inorganic nanoparticle (SiO 2 /TiO 2 ) modified cellulose acetate membranes at room temperature. SiO 2 /TiO 2 is used to improve the structural stability and roughness of membranes, and dopamine is used as the functional monomer and crosslinker. Importantly, the as-prepared membranes not only exhibited enhanced rebinding capacity ( ETMIMs = 3 0 . 7 3 mg g − 1 and ESMIMs = 4 6 . 0 4 mg g − 1 ) but also possessed superior rebinding selectivity (2.76 and 2.99 for physcion and 2.42 and 3.30 for aloe emodin onto ETMIMs and ESMIMs) as well as permselectivity (7.59 and 6.69 for physcion and 5.94 and 5.78 for aloe emodin onto ETMIMs and ESMIMs). The regeneration ability of ETMIMs and ESMIMs still maintained 90.4% and 89.2% of the original rebinding capacity after 10 cycling steps, respectively. The ETMIMs and ESMIMs obtained in this work show potential applications for selective separation and purification of emodin from analogs.
研究领域:
材料科学
·
生物医学工程
·
药物化学
✓ 已验证
产品关联
DOI
高影响因子
Bioengineered
·
2021
·
IF 3.269
Jinfeng Liu,Liang Ning
We aimed to explore the effects of emodin on the energy metabolism of myocardial cells in rats with post-myocardial infarction (MI) heart failure (HF) and the extracellular signal-regulated kinase (ERK) pathway. The model of MI was established by ligation of the left anterior descending branch. After 4 weeks, the rats with left ventricular ejection fraction (LVEF) of ≤45% were used aspost-MI HF model animals and randomly divided into model, low-dose, middle-dose, high-dose and control groups (n=10). Low-, middle- and high-dose groups were gavaged with 20 mg/kg, 40 mg/kg and 60 mg/kg emodin daily, respectively. After administration for 14 d, the changes in LVEF, left ventricular end-systolic diameter (LVESD), left ventricular end-diastolic diameter (LVEDD) and interventricular septum thickness (IVS) were analyzed. The apoptosis rate of myocardial cells was detected by TUNEL staining. The levels of serum cardiac troponin I (cTnI) and peroxisome proliferator-activated receptor-γ coactivator-1 (PGC-1) were determined using ELISA, and the expressions of mitochondrial respiratory chain complex I protein and phosphorylated-ERK (p-ERK) in myocardial tissues were determined by Western blotting. Compared with model group, LVEDD, LVESD, apoptosis rate of myocardial cells, levels of serum cTnI and PGC-1, and expressions of complex I and p-ERK in myocardial tissues significantly decreased, while LVEF and IVS increased in low-dose, middle-dose, high-dose and control groups (P<0.05). The changes in the above indices were significantly dependent on the dose of emodin (P<0.05).Emodin can significantly relieve post-MI HF, reduce the apoptosis rate of myocardial tissues, and ameliorate the cardiac function of rats.
研究领域:
心脏病学
·
药理学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
LWT-FOOD SCIENCE AND TECHNOLOGY
·
2023
·
IF 6
Peiyuan Li,Fangzhou Wen,Hongjun Yan,Qiuting Xu,Wei Su
In order to promote the application of natural photosensitizer, the photodynamic antibacterial effect of emodin combined with visible light on Escherichia coli and Staphylococcus aureus were studied in this work. The results showed that emodin mediated photodynamic antibacterial activity was dependent on concentration, light time and pH. Confocal microscopy and scanning electron microscopy confirmed that emodin can produce reactive oxygen species to kill bacteria under visible light irradiation. After treatment with emodin and visible intermittent radiation, S. aureus inoculated on the surface of fresh-cut apples was significantly reduced to 1.5 Log CFU/mL during 5 days of storage, and the storage method had no significant effect on the weight and appearance of apples. The results indicate that photodynamic inactivation of foodborne pathogens by combining emodin with visible light is a potential food safety technology.
研究领域:
微生物学
·
食品科学
·
光化学
✓ 已验证
产品关联
DOI
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2026
·
IF 12.5
Liangwei Wang,Zhongpan Li,Zhilang Xie,Xianghan Hou,Rongzhu Li,Yulin Xiang,Xiaohui Chen,Fulan Zhao,Jiaqi Wu,Guoyou Wang,Rui Huang
Injectable nanohydrogel enabled localized and sustained intra-articular delivery. • GLP hydrogel prolonged joint retention and enabled sustained local drug exposure. • GLP hydrogel alleviated synovial inflammation and cartilage damage in CIA rats. • GLP hydrogel suppressed NF-κB/NLRP3-driven pyroptosis with good in vivo safety. Rheumatoid arthritis (RA) is a chronic autoimmune disease characterized by persistent synovial inflammation. To overcome the limitations of conventional therapies, including poor bioavailability, insufficient target specificity, and cumulative systemic toxicity, this investigation delineates the design and fabrication of an enzymatically cross-linked hydrogel scaffold derived from a gelatin-gallic acid (GGA) graft copolymer, designated as GGA@Lipo@EMO (GLP), for the encapsulation of emodin (EMO)-loaded liposomal nanoparticles. This advanced delivery platform facilitates localized sustained release and precise intra-articular drug delivery. Rheological analysis, scanning electron microscopy (SEM), and proton nuclear magnetic resonance ( 1 H NMR) confirmed its injectability, interconnected porous structure, and controlled release behavior. The Network pharmacology analyses, in vitro cellular experiments, and in vivo studies using collagen-induced arthritis (CIA) rat models collectively demonstrate that the GLP hydrogel effectively inhibits the nuclear factor-κB (NF-κB) signaling pathway and NOD-like receptor protein 3 (NLRP3) inflammasome activation, thereby blocking cysteine–aspartic acid protease-1 (caspase-1)/gasdermin D (GSDMD)-mediated pyroptosis. This results in significant downregulation of key inflammatory cytokines such as tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), and interleukin-18 (IL-18), thereby mitigating inflammatory cell infiltration and cartilage degradation. The GLP hydrogel exhibits substantial therapeutic efficacy and favorable biosafety, offering a new approach for localized therapy of RA. Download: Download high-res image (211KB) Download: Download full-size image
✓ 已验证
产品关联
DOI
高影响因子
Autophagy
·
2026
·
IF 18.6
Xu Zhang,Li-Peng Shan,Lei Liu,Jiong Chen
White spot syndrome virus (WSSV) devastates shrimp aquaculture, yet safe antivirals remain scarce. Here we identify a druggable host-directed pathway centered on hemocyanin (HMC). This pathway coordinates endoplasmic reticulum (ER)-mitochondrial crosstalk to promote WSSV replication, which could be counteracted by the natural anthraquinone emodin. In Litopenaeus vannamei, emodin suppressed viral replication with a half maximal inhibitory concentration (IC50) of 1.174 μM, improved survival in both therapeutic and prophylactic regimens, remained effective after per os administration, and retained antiviral activity in water for up to 4 d. Target fishing, orthogonal biophysics, and docking analyses show that emodin binds HMC (Kd = 4.49 μM) and interferes with HMC-HSPA5/BiP (heat shock protein family A (Hsp70) member 5) association. Mechanistically, emodin weakens the ITPR/IP3R (inositol 1,4,5-trisphosphate receptor)-VDAC (voltage dependent anion channel)-MCU (mitochondrial calcium uniporter) conduit at ER-mitochondrial contact sites, thereby limiting Ca2+ transfer, restoring mitochondrial membrane potential and organelle spacing, and attenuating ER stress. Untargeted metabolomics revealed that WSSV induced phosphoinositide and amino acid dysregulation, whereas emodin selectively normalizes phosphatidylinositol (PtdIns) and phosphatidylinositol 1,4,5-trisphosphate (PtdIns[1,4,5]P3) signaling and rebalances amino acid, tricarboxylic acid (TCA) intermediates. Correspondingly, emodin inhibited phosphoinositide 3-kinase (PI3K)-AKT/protein kinase B-MTOR (mechanistic target of rapamycin kinase) complex 1 (MTORC1) signaling and restored lysosome-dependent macroautophagy/autophagy. HMC RNAi or ITPR and MCU inhibition phenocopied emodin, whereas exogenous HMC or ER stress activation exacerbated infection and was mitigated by emodin or MCU blockade. These findings establish HMC-anchored ER-mitochondrial contact as a central proviral vulnerability and position emodin as a practical scaffold for next-generation antivirals in aquaculture.
✓ 已验证
DOI
PubMed
高影响因子
Food Bioscience
·
2025
·
IF 5.9
Chunying Li,Jiahui Gong,Mengfei Tian,Hongying Ge,Xiaofei Xie,Qi Liang,Ying Yang,Chunjian Zhao,Ying Liu
The typical phytochemical emodin (ED) found in Rumex acetosa L. is extensively utilized in traditional medicine and demonstrates substantial pharmacological effects. However, Rumex acetosa L. is frequently regarded as a weed and discarded, leading to the underutilization of this valuable resource. In this work, a polydopamine molecularly imprinted resin (PDA@MIR) was successfully synthesized for the selective recognition and isolation of ED. The PDA@MIR is fabricated using macroporous resin X-5 as the carrier, dopamine as the green functional monomer, and emodin as the template molecule. The PDA@MIR displays excellent adsorption capacity (41.55 mg⋅g −1 ) for ED and adsorption affinity (IF = 3.19). Meanwhile, even after going through 10 cycles of adsorption-desorption tests, it demonstrates consistent adsorption efficacy and reusability. Moreover, the PDA@MIR can serve as the innovative column filler in solid-phase extraction (SPE) for applying to the separation of ED from Rumex acetosa L. roots extracts. The adsorption recovery rate of ED reaches 90.95%, while the effective adsorption recovery rate is 85.33%. The DFT simulation and NMR analysis reveales that the recognition mechanism of PDA@MIR is attributed to interactions involving hydrogen bonds and Van der Waals forces. Furthermore, this study provides valuable insights into the design of molecularly imprinted resin materials, which possess superior recognition capabilities and exceptional selectivity for the specific separation and recognition of phytochemicals from plant extracts.
研究领域:
药用植物学
·
材料科学
·
分析化学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF MOLECULAR LIQUIDS
·
2024
·
IF 5.3
Mohan Li,Na Gan,Dian Zhou,Yi He,Fang Geng,Wei Wang,Di Wu
Aloe dairy products have occupied a certain market share, and the interaction between the small bioactive molecules contained in aloe and milk proteins during product processing profoundly affects the performance of dairy products. In this study, two typical and potentially dangerous bioactive small molecules of aloe, aloin (AA) and aloe-emodin (AE), were selected to investigate their interaction mechanism with β -lactoglobulin ( β -La). Computer simulations showed that AA/AE had the potential to form complexes with β -La, and the β -La-AA system exhibited a stronger binding affinity than the β -La-AE system. Fluorescence analysis showed that the binding affinity values of AA to β -La at 298 K were deduced to be (4.184 ± 1.06) × 10 4 M −1 , meaning medium-strength interactions, comparatively, AE to β -La was weaker, were deduced to be (3.15 ± 1.25) × 10 3 M −1 . In addition, the thermodynamic analysis found that ΔH 0 and ΔS 0 were positive in both the β -La-AA system and the β -La-AE system, which implies that the main driving force for the combination of AA/AE and β -La to form the ground state complex is the hydrophobic force. The conformation changes in β -La brought about by binding to AA/AE may alter the properties and functions of the protein, such as surface hydrophobicity and oxidation resistance. Analysis shows that β -La is potentially present in whey as an AA/AE carrier during the production of aloe milk.
研究领域:
食品科学
·
生物化学
·
分子生物学
·
营养学
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）