JOURNAL OF COLLOID AND INTERFACE SCIENCE
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2026
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IF 9.7
Yehui Kang,Yahui Zhang,Weijiao Fan,Liya Yu,Mengdie Yu,Yuejia Ding,Yu Cai,Aihong Jiao,Jiajie Xu
Head and neck squamous cell carcinoma (HNSCC) remains a clinically challenging malignancy due to limited therapeutic options and considerable treatment-related toxicity. In this study, we present an innovative nanotherapeutic platform—monocarboxylate transporter 1 (MCT1) antibody-targeted nanoparticles co-loaded with a second near-infrared window (NIR-II, 1000–1700 nm) absorbing conjugated polymer (PDTP-TBZ-OD, denoted as PTO) and emodin (MCT@PTO-Em NPs) —that synergistically integrates emodin-induced pyroptosis with NIR-II mediated mild photothermal therapy (MPTT) to address critical limitations of current HNSCC treatments strategies. The synthesized NIR-II-absorbing conjugated polymer PTO exhibits strong absorption at 1064 nm and a high photothermal conversion efficiency (39 %), enabling deeptissue penetration and precise hyperthermia control. Accordingly, MCT@PTO-Em NPs implement a dual-modal therapeutic strategy that triggers pyroptosis through NLRP3 inflammasome activation while simultaneously enhancing tumor cell death via mild hyperthermia. Moreover, emodin encapsulated within the nanoparticles (NPs) inhibits heat-shock protein 70 (HSP70), thereby disrupting cellular thermoresistance mechanisms and sensitizing cancer cells to MPTT. Additionally, surface functionalization of the nanoparticles with MCT1-targeting antibodies enhances tumor-specific delivery and intracellular accumulation, thereby minimizing off-target effects. Both in vitro and in vivo studies demonstrate that MCT@PTO-Em NPs achieve superior tumor suppression through the synergistic interplay between pyroptosis and MPTT, while exhibiting excellent biocompatibility. This work presents a precision nanomedicine strategy that integrates molecular targeting, pyroptosis-mediated immune activation, and MPTT, offering a transformative therapeutic paradigm for HNSCC and other solid tumors.
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MICROCHEMICAL JOURNAL
·
2026
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IF 5.2
Xuesong Ma,Yuxin Zheng,Kamile Arkin,Yuting Xu,Xue Jiang,Kexin Li,Yuxin Yang,Qingkun Shang
It is urgent to develop safe and effective new antibiotics to reduce the increasingly serious threat of antibiotic resistance to human health. This study proposes a novel strategy for synthesizing antibacterial CDs (CDs) using active components from Chinese herbal medicine. Employing medicinal emodin as the carbon source and urea as the nitrogen source, a hydrothermal method was utilized to prepare water-soluble nitrogen-doped CDs (EUCDs). Under 523 nm excitation, its emission wavelength reached 600 nm with a fluorescence lifetime of 1.79 ns. Results demonstrate that EUCDs exhibit s not only superior environmental stability and biocompatibility but also effectively kills Escherichia coli ( E. coli ) and Staphylococcus aureus ( S. aureus ). The minimum inhibitory concentration (MIC) of EUCDs was determined to be 14 μg/mL. Research has revealed that EUCDs exhibit distinct red fluorescence on the membranes of L929 tumor cells. Through transmission electron microscopy combined with cell staining and imaging techniques, the antibacterial mechanism of EUCDs is identified as disrupting bacterial cell membranes, leading to the leakage of intracellular substances and effectively killing E. coli and S. aureus . This study successfully developed a carbon dot based high-efficiency antibacterial agent that also has imaging function. This is of great significance for expanding the research and application fields of traditional Chinese medicine and CDs.
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Scientific Reports
·
2025
·Vol. 15
·期 1
·40205
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IF 3.9
Tang Cheng,Zou Yangyang,Meng Hao,Xu Jin,Long Fang,Chen Xiaoli,Xiao Qingling,Su Kelei,Nan Zhang,Guo Yaoyao,Li Chaojuan
To develop excipient-free carrier-free nanoparticles (DE NPs) via self-assembly of doxorubicin (DOX) and emodin (EMO) for enhanced combination chemotherapy against non-small cell lung cancer (NSCLC). DE NPs were fabricated through non-covalent interactions between DOX and EMO using a self-assembly method. The nanoparticles were characterized for morphology, stability, encapsulation efficiency, and cellular uptake. In vitro cytotoxicity and in vivo antitumor efficacy of free drugs (EMO, DOX), DOX/EMO mixture, and DE NPs were evaluated on A549 NSCLC cells. Mechanistic studies explored the role of DE NPs in suppressing efflux pump proteins via modulation of p65 activation and nuclear translocation. DE NPs formed rod-like nanostructures with high encapsulation efficiency (> 90%) and stability. They exhibited enhanced cellular uptake and intracellular drug accumulation compared to free drugs or the mixture. In vitro studies demonstrated significantly stronger cytotoxicity in A549 cells (IC50 reduction of ~ 50%) and a synergistic antitumor effect (combination index < 0.5). In vivo studies further confirmed the superior antitumor efficacy of DE NPs over individual DOX or EMO monotherapy (72.67 ± 7.20% tumor inhibition rate). Mechanistically, DE NPs inhibited p65 activation and nuclear translocation, downregulating efflux pump protein expression and prolonging drug retention in cancer cells. The excipient-free DE NPs provide a promising carrier-free nanomedicine platform for NSCLC treatment, achieving synergistic antitumor efficacy through enhanced drug delivery and suppression of drug resistance mechanisms. This strategy highlights the potential of self-assembled dual-drug nanoparticles to improve therapeutic outcomes in combination.
研究领域:
肿瘤学
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纳米医学
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药剂学
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分子肿瘤学
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转化医学
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药物递送
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耐药机制
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PHYTOMEDICINE
·
2025
·
IF 8.3
Yongyan Chen,Xu Han,Yuxuan Hao,Xu Wang,Fupeng Wu,Sheng Tan,Huijing Ye,Yang Hong,Xiaoyan Shen
Background Vascular calcification is a major cause of death in chronic kidney disease (CKD), with osteoblastic transdifferentiation of vascular smooth muscle cells (VSMCs) considered to be the crucial pathologic process. However, there remains a significant deficiency in effective prevention and treatment strategies. Purpose In an in vitro calcification screening model, we observed an inhibitory activity of Emodin on osteoblastic transdifferentiation of VSMCs. In the present study, we therefore aimed to evaluate its efficacy in CKD-induced medial vascular calcification in vitro and in vivo, and to further explore the underlying mechanisms. Study design A7R5 and MOVAS cells were treated with sodium phosphate to induce osteogenic transdifferentiation as in vitro models, while mice were fed with adenine and a high-phosphorus diet, and additionally received an intraperitoneal injection of 10,000 IU Vitamin D3 to induce chronic kidney disease (CKD) as an in vivo model. Vitamin K2 served as a positive control. Methods Alizarin Red S staining and VON-KOSSA staining were used to evaluate the effects of Emodin on osteogenic transdifferentiation. Western blotting, RT-qPCR and Von-Kossa staining were used to detect the effects of Emodin on aortic calcification in CKD mice in vivo. Chemical biology techniques including ITC, fluorescence titration, dual fluorescein reporter genes, CETSA, and DARTS, were used to detect the binding activity of Emodin to ERα and SYVN1. Immunoprecipitation, immunostaining, etc. were used to explore the mechanisms, and small molecule inhibitors and small RNA interference were used to verify the target of Emodin. Results Emodin could effectively inhibit the osteogenic transdifferentiation of A7R5 and MOVAS cells in vitro, and alleviate aortic calcification in CKD mice in vivo. Mechanism study revealed that Emodin could act as a molecular glue that binds directly to ERα and SYVN1 and enhances their interaction, thereby accelerating the ubiquitination degradation process of ERα. The decrease in ERα diminished the inhibition of ERα on the deacetylation of HIF-1α by SIRT6, thereby inhibiting VSMC osteogenic transdifferentiation and relieving the vascular cells calcification. Conclusion Our study demonstrates that ERα has a non-genomic effect to inhibit the deacetylation of HIF-1α by SIRT6, which can be abrogated by Emodin through SYVN1-mediated ERα degradation. These results provide evidences for Emodin to serve as a candidate drug for controlling clinical vascular calcification in CKD.
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MOLECULES
·
2019
·Vol. 24
·期 15
·2770
·
IF 3.06
Yunchang Fan,Zeyu Niu,Chen Xu,Lei Yang,Tuojie Yang
Rheum palmatumL. (R. palmatumL.) is a traditional Chinese herb and food, in which rhein and emodin are the main bioactive components. The extraction of the two compounds fromR. palmatumL. is, thus, of great importance. In this work, protic ionic liquids (PILs) were applied in the microwave-assisted extraction (MAE) of rhein and emodin fromR. palmatumL., which avoids the toxicity of organic solvents. The results of the present study indicate that PILs possessing higher polarity exhibit higher extraction ability due to their stronger absorption ability for microwave irradiation. Compared with conventional solvents, such as methanol, trichloromethane, and deep eutectic solvents (DESs), the PIL, 1-butyl-3-himidazolium methanesulfonate ([BHim]MeSO3) reported herein is more efficient. The selected extraction conditions of liquid–solid ratio, microwave irradiation time, microwave irradiation power, and PIL concentration were 40 g·g−1, 50 s, 280 W, and 80%, respectively. Under the selected conditions, the extraction yields of rhein and emodin were 7.8 and 4.0 mg·g−1, respectively. These results suggest that PILs are efficient extraction solvents for the separation of active components from natural products.Keywords:microwave-assisted extraction;protic ionic liquids (PILs);polarity;Rheum palmatumL.
研究领域:
中药学
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分析化学
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Drug Design Development and Therapy
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2022
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IF 4.319
Zhenming Gao,Jidong Sui,Rong Fan,Weikun Qu,Xuepeng Dong,Deguang Sun
Aim Lung injury is a common complication of acute pancreatitis (AP), which leads to the development of acute respiratory distress syndrome and causes high mortality. In the present study, we investigated the therapeutic effect of emodin on AP-induced lung injury and explored the molecular mechanisms involved.Materials and Methods Thirty male Sprague-Dawley rats were randomly divided into AP (n=24) and normal (n=6) groups. Rats in the AP group received a retrograde injection of 5% sodium taurocholate into the biliary-pancreatic duct and then randomly assigned to untreated, emodin, combined emodin and ML385, and dexamethasone (DEX) groups. Pancreatic and pulmonary injury was assessed using H&E staining. In in vitro study, rat alveolar epithelial cell line L2 cells were exposed to lipopolysaccharide and treated with emodin. Nrf2 siRNA pool was applied for the knockdown of Nrf2. The contents of the pro-inflammatory cytokines in the bronchoalveolar lavage fluid and lung were determined using enzyme-linked immunosorbent assay. The expressions of related mRNAs and proteins in the lung or L2 cells were detected using real-time polymerase chain reaction, Western blot, immunohistochemistry and immunofluorescence.Key Findings Emodin administration alleviated pancreatic and pulmonary injury of rats with AP. Emodin administration suppressed the production of proinflammatory cytokines, downregulated NLRP3, ASC and caspase-1 expressions and inhibited NF-κB nuclear accumulation in the lung. In addition, Emodin increased Nrf2 nuclear translocation and upregulated HO-1 expression. Moreover, the anti-inflammatory effect of emodin was blocked by Nrf2 inhibitor ML385.Conclusion Emodin effectively protects rats against AP-associated lung injury by inhibiting NLRP3 inflammasome activation via Nrf2/HO-1 signaling.
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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Evidence-based Complementary and Alternative Medicine
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2022
·
IF 2.65
Huijie Gao,Yan Ren,Chao Liu
Background. This study was designed to assess the impact of aloe-emodin (AE) on oxidative stress and inflammation in a murine model of LPS-induced sepsis. In addition, the mechanistic basis for anti-inflammatory and antioxidant activity was assessed. Methods. Male ICR mice received an intraperitoneal injection of LPS (10 mg/kg), and the preventive properties of AE (80 or 150 mg/kg) on these mice were assessed by monitoring spleen index, and levels of inflammatory and oxidative stress-related factors. Peripheral blood TNF-α and IL-6 levels were assessed via ELISA kits, while changes in hepatic SOD and GSH-Px levels were assessed using appropriate biochemical kits. Splenic PI3K, AKT, and mTOR levels were assessed via qPCR and western blotting. Results. Relative to animals in the LPS model group, those in the AE treatment groups exhibited reduced spleen index, decreased inflammatory cytokine levels, and improved SOD and GSH-Px activity in liver tissues. Splenic PI3K, Akt, and mTOR levels were also reduced in response to AE treatment. Conclusions. These findings indicated that AE can alleviate sepsis-related tissue damage, inflammation, and oxidative stress, at least in part by suppressing the PI3K/Akt/mTOR signaling pathway. These results offer a clinical basis for the use of AE to treat sepsis and associated diseases.
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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病理生理学
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Frontiers in Bioengineering and Biotechnology
·
2026
·
IF 5.8
Xinpeng Dong,Yuan Wang,Yi Li,Xin Wang,Qing Yu,Changhao Han,Jiayi Wang,Shen Liu,Jinglei Wu,Shenghe Liu
Introduction Tendon injuries are prevalent musculoskeletal conditions in clinical settings, affecting various regions such as the rotator cuff tendons, forearm flexor/extensor tendons, finger flexor tendons, and Achilles tendon. While surgery is an effective treatment, it often fails to balance intrinsic and extrinsic healing processes, leading to abnormal cell activation, proliferation, and migration, resulting in collagen deposition at the injury site. This pathological fibrosis causes severe peritendinous adhesions, posing a therapeutic challenge. Traditional nonsteroidal anti-inflammatory drugs (NSAIDs) and implantable membranes have limited long-term efficacy and come with various side effects. Literature indicates that Aloe emodin(AE) can potentially inhibit multiple known pro-inflammatory pathways, including NF-κB, MAPK, p38, and ERK, directly or indirectly reducing oxidative stress. In the field of fibrosis, Aloe emodin regulates the TGFβ/Smad signaling pathway, downregulates extracellular matrix gene transcription, inhibits collagen deposition, improves cardiac function and myocardial fibrosis. Based on these findings, we hypothesize that Aloe emodin may serve as an effective therapeutic agent for improving peritendinous adhesions. Methods This study involved grafting Aloe emodin onto polylactic acid via esterification to create a polylactic acid ‐ Aloe emodin conjugate compound. Using electrospinning technology, a novel polylactic acid-Aloe emodin conjugate electrospun nanofiber membrane (PCA) was developed and characterized, and its role in preventing peritendinous adhesions was thoroughly validated. We validated and systematically evaluated the anti-adhesive capability of the new electrospun membrane through in vitro and in vivo experiments in rats. Results Experimental results demonstrate that the electrospun membrane of polylactic acid-Aloe emodin grafted material exhibits excellent mechanical properties and hydrophilicity, and can achieve localized targeted release of damaged tissues after treatment with lipase. Compared with polylactic acid-Aloe emodin hybrid electrospun membrane (PBA), PCA exhibits superior anti-adhesion properties and maintains longer-lasting therapeutic effects. In vitro studies showed that PCA effectively reduced fibroblast activity, inhibiting their proliferation, adhesion, and PA formation. In vivo experiments confirmed that PCA could effectively wrap around surgically treated tendons and inhibit the TGFβ1/COLIII signaling pathway, significantly reducing peritendinous adhesions in rats, offering a new approach for PA treatment. Discussion In this study, we designed and manufactured a novel polylactic acid - Aloe emodin conjugate electrospun nanofiber membrane. We validated and systematically evaluated the anti-adhesive capability of the new electrospun membrane through in vitro and in vivo experiments in rats. In summary, our research proposed a new approach for the treatment of tendon adhesions.
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2015
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IF 0.476
Yaping Li,Lili Wang,Yanbei Tu,Jin Yan,Kailin Xu,Hui Li
Emodin (EM), with two p K a values (p K a 1 = 8.0 and p K a 2 = 10.9), presents low solubility and dissolution rate, which results in low bioavailability. In this report, two EM sodium salts, C 15 H 9 O 5 − · N a + (EM-1Na) and C 15 H 8 O 5 2− · 2 N a + (EM-2Na), were prepared by adding various amounts of sodium hydroxide . Salt forms were characterized by FT-IR, XRPD, 1 H NMR, DSC , and SEM, as well as solubility and dissolution rate studies in triple-deionized water, buffer at pH 1.2 and pH 6.8, respectively. The aqueous solubility of EM was notably enhanced by more than 20,000 and 50,000 times, corresponding to EM-1Na and EM-2Na. Meanwhile, the dissolution rate exhibited significant enhancement and the dissolution time was shortened. The results showed the dissolution of EM-1Na and EM-2Na was 25 and 35 times greater than EM in 60 min. The results of β-amyloid (Aβ) self-aggregation inhibition and MIC assay did not show apparent difference from those of EM, indicating that the functional groups were not broken down. Moreover, salt formation significantly enhanced the bioavailability of EM, consistent with the ABTS free radical scavenging test results. The significant decrease in IC 50 values in the range of 18,394 μg/mL to 29.07 μg/mL indicated a more effective anti-AD action.
研究领域:
药剂学
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药物化学
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药物递送
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神经科学
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微生物学
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Cancer Nanotechnology
·
2021
·Vol. 12
·期 1
·1-15
·
IF 5.095
Zou Tengteng,Lan Meng,Liu Fengjie,Li Lihong,Cai Tiange,Tian Huaqin,Cai Yu
Background The role of epithelial–mesenchymal transition (EMT) involved in breast cancer metastasis and chemoresistance has been increasingly recognized. However, it is necessary to search for more effective strategies to inhibit EMT thereby increase the sensitivity of breast cancer cells to chemotherapy drugs. Emodin has a potential in overcoming tumor drug resistance and restraining the development of EMT, but the poor internalization into breast cancer cells limited the application.Results MCF-7/ADR cells have more EMT characteristics than MCF-7 cell. EMT in MCF-7/ADR cells promotes the development of drug resistance via apoptosis resistance and facilitating the expression of P-gp. The anti-cancer effect of DOX enhanced by the decreasing of drug resistance protein P-gp and apoptosis-related proteins after EMT inhibited in MCF-7/ADR cells. E-PLNs increase the cellular uptake of EMO and restore DOX sensitivity in MCF-7/ADR cells by inhibiting EMT.Conclusion E-PLNs inhibit EMT to enhance the sensitivity of breast cancer to DOX. The combination of E-PLNs and DOX can improve the efficacy of DOX in the treatment of breast cancer, which provides a new method to prevent or delay clinical drug resistance.
研究领域:
肿瘤学
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药学
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纳米技术
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细胞生物学
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高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2018
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IF 6.735
Jian Lu,Yingying Qin,Qi Zhang,Chao Yu,Yilin Wu,Yongsheng Yan,Hougang Fan,Minjia Meng,Chunxiang Li
Sponge is widely used in our daily life as a low-cost and easily available material. Its three-dimensional (3D) porous structure is particularly suitable for the application of membrane-based separation. Herein, we report an antibacterial, high-flux and 3D porous molecularly imprinted nanocomposite sponge membranes (Emodin-MIS) based on sponge for cross-flow filtration of emodin from analogues (aloe-emodin and physcion). A GO/Ag/KH570 modification strategy was implemented to (i) provide ‘active secondary platforms’, (ii) increase the antibacterial property, and (iii) facilitate the fixation of molecularly imprinted polymers. Base on formation of ‘emodin-recognition sites’, optimal selectivity of emodin/aloe-emodin (1.61) and emodin/physcion (1.70) in static adsorption, as well as aloe-emodin/emodin (7.66–3.93) and physcion/emodin (10.00–4.68) in cross-flow filtration, were achieved on Emodin-MIS with the imprinting factor of 3.28. Langmuir isothermal model and pseudo-second-order kinetic model best fitted rebinding data of Emodin-MIS. Specifically, the rebinding capacity of Emodin-MIS was still higher than 85% of initial after 10 regeneration cycles which included an interval of 15 days. This novel-designed Emodin-MIS exhibits superior results for emodin separation in cross-flow filtration and shows promising potentials for wider applications.
研究领域:
材料科学
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分离技术
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药物化学
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高影响因子
Environmental Chemistry Letters
·
2021
·Vol. 19
·期 4
·3517-3522
·
IF 9.027
Liu Hui,Qiu Xiaojun,Li Zhi,Zhu Xiaomei,Sun Bing,Zhang Xiaoxing
Dissolved organic matter (DOM) in waters, soils, sediments, and organic waste is considered to have major role in the photochemical generation of emerging organobromine contaminants, yet mechanisms are unclear. Here we fractionated soil humic acids into bound quinone-like substances and an effluent fraction, using a new emodin-imprinted polymer. We tested the effect of these fractions on the photobromination of phenol with bromide. Results show that quinone-like substances induce three times more bromophenols than the effluent fraction. Our findings reveal a new method to separate reactive compounds from DOM and imply that formation of organobromine contaminants may be controlled by the composition of organic matter.
研究领域:
环境化学
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光化学
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分析化学
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环境科学
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高影响因子
危险品化学品经营许可证（带存储）