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LUMINESCENCE · 2014 ·Vol. 30 ·期 1 ·60-66 · IF 1.675

Molecular spectroscopic studies on the interactions of rhein and emodin with thioglycolic acid-capped core/shell CdTe/CdS quantum dots and their analytical applications

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 · 材料科学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES · 2022 ·Vol. 23 ·期 22 ·13738 · IF 6.208

Cell Metabolomics Reveals the Potential Mechanism of Aloe Emodin and Emodin Inhibiting Breast Cancer Metastasis

Guorong Cheng,Zhiqiang Liu,Zhong Zheng,Fengrui Song,Xiaoyu Zhuang,Shu Liu

Metastasis is one of the main obstacles for the treatment and prognosis of breast cancer. In this study, the effects and possible mechanisms of aloe emodin (AE) and emodin (EMD) for inhibiting breast cancer metastasis were investigated via cell metabolomics. First, a co-culture model of MCF-7 and HUVEC cells was established and compared with a traditional single culture of MCF-7 cells. The results showed that HUVEC cells could promote the development of cancer cells to a malignant phenotype. Moreover, AE and EMD could inhibit adhesion, invasion, and angiogenesis and induce anoikis of MCF-7 cells in co-culture model. Then, the potential mechanisms behind AE and EMD inhibition of MCF-7 cell metastasis were explored using a metabolomics method based on UPLC-Q-TOF/MS multivariate statistical analysis. Consequently, 27 and 13 biomarkers were identified in AE and EMD groups, respectively, including polyamine metabolism, methionine cycle, TCA cycle, glutathione metabolism, purine metabolism, and aspartate synthesis. The typical metabolites were quantitatively analyzed, and the results showed that the inhibitory effect of AE was significantly better than EMD. All results confirmed that AE and EMD could inhibit metastasis of breast cancer cells through different pathways. Our study provides an overall view of the underlying mechanisms of AE and EMD against breast cancer metastasis.Keywords:aloe emodin (AE);emodin (EMD);cell metabolomics;breast cancer;metastasis

研究领域: 肿瘤学 · 药理学 · 代谢组学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Foods · 2022 ·Vol. 11 ·期 3 ·386 · IF 5.561

Ultrasonic Solvent Extraction Followed by Dispersive Solid Phase Extraction (d-SPE) Cleanup for the Simultaneous Determination of Five Anthraquinones in Polygonum multiflorum by UHPLC-PDA

Ying Xu,Xuan Yu,Jiaqi Gui,Yiqun Wan,Jinping Chen,Ting Tan,Fan Liu,Lan Guo

A rapid and effective ultra-high performance liquid chromatography (UHPLC) method was developed for the determination of five anthraquinones (emodin, physcion, aloe-emodin, rhein, and chrysophanol) inPolygonum multiflorum. The target compounds were ultrasonically extracted with 70% methanol, followed by dispersive solid-phase extraction (d-SPE) with HC-C18 and desorption with acetonitrile. The five anthraquinones were separated on an ACQUITY UPLC®HSS T3 column (2.1 × 100 mm, 1.8 μm) and detected by a photodiode array detector (PDA) at 254 nm. Under the optimized conditions, linear relationships were achieved in the range of 0.3~100 mg/L for emodin, 0.3~40 mg/L for physcion, 0.1~20 mg/L for aloe-emodin, and 0.05~20 mg/L for rhein and chrysophanol. The limits of detection of the five analytes ranged from 0.01 to 0.08 mg/L, and the recoveries were within the range of 82.8~118.4% with an RSD (n= 6) of 1.0~10.3%. The intra-day and inter-day precision (n= 5) of the five targets were in the range of 1.0~1.8% and 3.0~3.1%, respectively. Furthermore, this method was applied to analyses ofPolygonum multiflorumsamples collected from different regions in China with satisfactory results. All the results indicated that this method is suitable for the detection of five anthraquinones inPolygonum multiflorum.Keywords:anthraquinones;Polygonum multiflorum;d-SPE;UHPLC

研究领域: 分析化学 · 中药学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BIOCHEMICAL PHARMACOLOGY · 2024 · IF 5.3

ACSL4 promotes malignant progression of Hepatocellular carcinoma by targeting PAK2 transcription

Dandan Wu,Zongchao Zuo,Xinning Sun,Xin Li,Fangzhou Yin,Wu Yin

Long-chain fatty acyl-Coa ligase 4 (ACSL4) is an important enzyme that converts fatty acids to fatty acyl-Coa esters, there is increasing evidence for its role in carcinogenesis. However, the precise role of ACLS4 in hepatocellular carcinoma (HCC) is not clearly understood. In the present study, we provide evidence that ACSL4 expression was specifically elevated in HCC and is associated with poor clinical outcomes. ACSL4 significantly promotes the growth and metastasis of HCC both in vitro and in vivo . RNA sequencing and functional experiments showed that the effect of ACSL4 on HCC development was heavily dependent on PAK2. ACSL4 expression is well correlated with PAK2 in HCC, and ACSL4 even transcriptionally increased PAK2 gene expression mediated by Sp1. In addition, emodin, a naturally occurring anthraquinone derivative, inhibited HCC cell growth and tumor progression by targeting ACSL4. In summary, ACSL4 plays a novel oncogene in HCC development by regulating PAK2 transcription. Targeting ACSL4 could be useful in drug development and therapy for HCC.

CAS / MDL: 67-68-5
研究领域: 肿瘤学 · 分子生物学 · 癌症研究
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Revista Brasileira de Farmacognosia-Brazilian Journal of Pharmacognosy · 2020 ·Vol. 30 ·期 1 ·28-33 · IF 1.407

1H NMR Quantification of Polydatin and Emodin in Huganning, a Chinese Patent Herbal Medicine

Wang Cong,Zhang Pengpeng,Zhang Xiuli,Yu Mingming,Lv Zhihua

Huganning, a Chinese patent medicine, has been used in clinical practice for the treatment of hepatitis in China for more than 20 years, and its main physiologically active components are polydatin and emodin. In this study, a rapid and accurate proton nuclear magnetic resonance method for the quantification of these constituents was developed. 4-Nitrochlorobenzene was selected as an internal standard, and the signals for polydatin at δ 6.44 ppm and emodin at δ 7.54 ppm were chosen for the quantification. Validation of the method was performed in terms of specificity, precision, and stability. The results indicated that the method was precise and in line with the China Food and Drug Administration guidance. The method has been successfully applied to characterize tablets and capsules obtained from six pharmaceutical companies. This study indicated that the rapid 1 H NMR method is more suitable for the quality control of Huganning than the high-performance liquid chromatography method. Graphical Abstract

研究领域: 药学 · 中药学
✓ 已验证 DOI 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Natural gelatin / chitosan oligosaccharides / emodin eutectogels with multiple antibacterial effects for accelerated infected wound healing

Jia Wan,Meifang Yin,Feng Wang,Guangtao Huang,Ilaria Dal Pra,Yongzhi Liang,Jun Wu

Bacterial infections following skin injuries can lead to chronic, hard-healing wounds, and the overuse of antibiotics has made infection control a significant clinical challenge. Nature provides numerous antimicrobial agents, inspiring the design of novel antibacterial wound dressings; however, their solubility often presents additional hurdles. Herein, we leverage highly water-soluble chitosan oligosaccharide molecules dispersed within a gelatin-based gel network to overcome the poor solubility of chitosan, a known antibacterial agent. Notably, we first discovered that chitosan oligosaccharides can promote the solubility of poorly water-soluble antibacterial molecules like emodin through Schiff base reactions, thereby enabling synergistic antibacterial effects. The resulting eutectogel exhibits excellent antibacterial activity against both Staphylococcus aureus and Escherichia coli. Additionally, the gel demonstrates superior tensile strength, fracture strain, resistance to desiccation, and biocompatibility, with its outstanding overall performance laying a foundation for wound dressing applications. In animal models of infected wounds, the gel effectively accelerates wound healing, achieving wound closure rates of 166.9 % and 136.9 % of the control group on days 4 and 7, respectively. Mechanistic studies further reveal that the dressing promotes cellular proliferation, migration, and the regeneration of blood vessels and collagen, contributing to the wound healing process.

研究领域: 生物材料 · 伤口敷料 · 抗菌治疗 · 组织工程
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Botanical Studies · 2014 ·Vol. 55 ·期 1 ·1-8 · IF 0.809

Folium Sennae protects against hydroxyl radical-induced DNA damage via antioxidant mechanism: an in vitro study

Lin Jian,Li Xican,Han Lu,Li Fei,Lu Wenbiao,Bai Ye,Chen Dongfeng

Background In the study, Folium Sennae (FS) was firstly extracted by various solvents to obtain five FS extracts. Then, five FS extracts were evaluated for the protective effects against •OH-induced DNA damage, antioxidant abilities in vitro, and chemical contents using various methods. On this basis, the correlation graphs between the pharmacological effects and chemical contents were plotted to obtain the correlation coefficients (R values). Finally, in order to obtain biological evidence, ethyl acetate extract of FS (EAFS) was investigated for the protective effect against •OH-induced MSCs (mesenchymal stem cells) damage using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl) assay. Results The pharmacological assays indicated that five FS extracts could effectively protect against •OH-induced DNA damage. The correlation analysis suggested that the average R values of total phenolics, total anthraquinones, aloe-emodin, rhein, and emodin were respectively 0.843, 0.833, 0.753, 0.820, and 0.784, while those of total sugars and total saponins were respectively 0.103 and 0.0068. The mechanistic analysis revealed that five FS extracts could also scavenge •OH, •O 2 – , DPPH• & ABTS• + radicals, and reduce Cu 2+ to Cu + . MTT assay revealed that the viability of MSCs which were treated with •OH radicals has been effectively protected by EAFS (3 and 30 μg/mL). Conclusion On this basis, it can be concluded that: ( i ) Folium Sennae exhibits a protective effect against •OH-induced damages to DNA and MSCs; ( ii ) The effects may be attributed to phytophenols (especially aloe-emodin, rhein, and emodin), not sugars or saponins; ( iii ) They exert the protective action via hydrogen atom transfer (HAT) and/or sequential electron proton transfer (SEPT) mechanisms which make phenolic –OH moiety be oxidized to stable semi-quinone form; ( iv ) The stability of semi-quinone form can ultimately be responsible for the protective or antioxidant effect of phytophenols.

研究领域: 药理学 · 生物化学 · 细胞生物学
✓ 已验证 DOI PubMed 高影响因子
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JOURNAL OF DAIRY SCIENCE · 2021 · IF 4.034

Bactericidal and antibiofilm properties of Rumex japonicus Houtt. on multidrug-resistant Staphylococcus aureus isolated from milk

G. Kim,Y.J. Xu,A.K. Farha,Z.Q. Sui,H. Corke

ABSTRACT Multidrug-resistant (MDR) Staphylococcus aureus and its biofilm formation have been challenging to control in milk and dairy industries. Biofilms formed by Staph. aureus may result in the failure of antibacterial agents and disinfectants to penetrate the biofilm in an attempt to control contamination. Novel natural antibacterial agents are required to combat MDR bacteria and biofilms. In this study, we evaluated the bactericidal, antibiofilm, and antimotility effects of Rumex japonicus Houtt. (RJH) extract on MDR Staph. aureus isolated from milk. The RJH extract exhibited good antibacterial activity against MDR strains with minimum inhibitory concentrations (MIC) ranging from 0.78 to 6.25 mg/mL and minimum bactericidal concentrations ranging from 3.125 to 12.5 mg/mL. The extract showed strong inhibition of biofilm formation (81.9%) at sub-MIC value and eradication of biofilm at higher concentrations. The motility of Staph. aureus was effectively blocked by the extract. Major compounds emodin, chrysophanol, and physcion were identified in RJH extract using HPLC-linear trap quadrupole (LTQ)/Orbitrap-mass spectrometry. The extract was nontoxic to human epithelial cell lines such as Caco-2 and HT-29 cell lines at concentrations ranging from 0.1 to 0.5 mg/mL, and from 0.1 to 0.75 mg/mL, respectively. These findings suggest that RJH extract could be an alternative to synthetic preservatives in milk and dairy products.

CAS / MDL: 548-62-9
研究领域: 微生物学 · 食品科学 · 药理学 · 天然产物化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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SCIENCE OF THE TOTAL ENVIRONMENT · 2018 · IF 4.61

Rapid adsorption and enhanced removal of emodin and physcion by nano zirconium carbide

Bingjie Zhang,Jiawen Ji,Xue Liu,Changsheng Li,Meng Yuan,Jingyang Yu,Yongqiang Ma

In this study, nano zirconium carbide (n-ZrC) was synthesized by preceramic polymers method, and it was used to adsorb emodin and physcion from solutions for the first time. The prepared material was characterized by various technologies . The adsorption experiment was carried out to investigate the emodin and physcion removal performance. The results indicate that the pseudo-second-order kinetic model and the Langmuir model correlated satisfactorily to the experimental data, and the thermodynamic parameters are also calculated. Especially, n-ZrC can remove >95% of emodin or physcion in a minute under the optimal conditions, it is the fastest adsorption rate compared to other commonly used adsorbents (commercial zirconium carbide, activated carbon, C18, PSA, GCB and florisil). The adsorption mechanism was discussed, which suggests that Van der Waals' forces are the primary driving power during the adsorption process. Moreover, n-ZrC is stable at different pH and it can be reused at least fifteen times.

研究领域: 环境科学 · 材料科学 · 药物化学
✓ 已验证 DOI 高影响因子
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JOURNAL OF ETHNOPHARMACOLOGY · 2022 · IF 5.195

Pharmacokinetic characteristics of emodin in polygoni Multiflori Radix Praeparata

Dongpeng Wang,Jufeng Duan,Xiao-Jing Chen,Kaiqi Liu,Yingying Guo,Run Shi,Sha Li,Ming Liu,Lijun Zhao,Bei Li,Hongtao Liu,Minglun Li,Yibin Feng,Hongliang Li,Xuanbin Wang

Ethnopharmacological relevance Polygoni Multiflori Radix Praeparata (Zhiheshouwu) has been a Wudang Taoist medicine for tonifying the liver and kidney, resolving turbidity and reducing lipid. Emodin is one of the active anthraquinones in Zhiheshouwu. Our previous studies showed that emodin (EM) and the other anthraquinones in Zhiheshouwu extract (HSWE) exerted similar inhibitory effects on liver cancer cells in vitro . However, it is still unknown if the other anthraquinones enhance pharmacokinetics (PK) of EM in HSWE in vivo . Aim of the study In this study, we compared the PK characteristics of EM alone with that in Zhiheshouwu aiming to explore which anthraquinones in HSWE contribute to the changed PK of EM in rats. Materials and methods Quality control of HSWE was determined using high performance liquid chromatography (HPLC). The ratios of emodin to other anthraquinones, physcion (PH), chrysophanol (CH), rhein (RH), aloe-emodin (AE), emodin-8-O- β -D-glycoside (EMG), physcion-1-O- β -D-glycoside (PHG) and chrysophanol-8-O- β -D-glycoside (CHG) in HSWE were determined and analyzed using UPLC combined with tandem mass spectrometry (UPLC/MS). The PK parameters and intestinal tissue concentration of EM alone, EM in HSWE, or with other anthraquinones in SD rats were analyzed using UPLC/MS. Results The quality of the Zhiheshouwu samples met the quality standard of the Chinese Pharmacopoeia (Version 2020). The PK results showed that compared with EM alone, C max (239.90 ± 146.71 vs . 898.46 ± 291.62, P  < 0.001), T max (0.26 ± 0.15 vs. 12.55 ± 1.33, P  < 0.001), AUC 0-t (1575.09 ± 570.46 vs. 12154.96 ± 5394.25, P  < 0.001), and AUC 0-∞ (4742.51 ± 1837.62 vs. 37131.34 ± 21647.39, P  < 0.001) of EM in HSWE were decreased due to PH and EMG, while the values of V d (380.75 ± 217.74 vs . 11.75 ± 7.35, P  < 0.001), T 1/2 (10.81 ± 1.99 vs . 6.65 ± 2.76, P  < 0.05) and CL (19.30 ± 7.82 vs . 2.78 ± 1.88, P  < 0.001) of EM in HSWE were increased due to PH and AE. In addition, the intestinal tissue concentration of emodin in HSWE was decreased compared with that of EM alone in 20 and 780 min (25.37 ± 5.98 vs . 43.29 ± 4.16 and 26.72 ± 4.03 vs . 43.40 ± 14.19, respectively. P  < 0.05) dominantly due to RH and PH. Conclusion In conclusion, compared with treatment of EM alone, the AUC 0-t value of EM in HSWE was decreased with different ways in rats. PH shortened T max , and increased V d and CL. While AE prolonged T 1/2 of EM. This indicated that the other anthraquinones in HSWE changed the PK of EM in rats and participated in the complex effects of EM on liver cancer. Besides the other anthraquinones, other components (e.g., 2,3,5,4′-tetrahydroxystilbene-2-O- β -D-glucoside) in Zhiheshouwu may contribute in the pharmacokinetic and pharmacodynamic interactions with EM for anti-liver cancer.

CAS / MDL: 9004-32-4 9085-26-1
研究领域: 中药学 · 药理学 · 生物化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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PHYTOMEDICINE · 2023 · IF 7.9

Emodin attenuates cardiomyocyte pyroptosis in doxorubicin-induced cardiotoxicity by directly binding to GSDMD

Shanshan Dai,Yunxuan Chen,Xiaoxi Fan,Jibo Han,Lingfeng Zhong,Yucong Zhang,Qingran Liu,Jiahui Lin,Weijian Huang,Lan Su,Zhouqing Huang,Bozhi Ye

Background Doxorubicin (Dox), which is an anticancer drug, has significant cardiac toxicity and side effects. Pyroptosis occurs during Dox-induced cardiotoxicity (DIC), and drug inhibition of this process is one therapeutic approach for treating DIC. Previous studies have indicated that emodin can reduce pyroptosis. However, the role of emodin in DIC and its molecular targets remain unknown. Hypothesis/Purpose We aimed to clarify the protective role of emodin in mitigating DIC, as well as the mechanisms underlying this effect. Methods The model of DIC was established via the intraperitoneal administration of Dox at a dosage of 5 mg/kg per week for a span of 4 weeks. Emodin at two different doses (10 and 20 mg/kg) or a vehicle was intragastrically administered to the mice once per day throughout the Dox treatment period. Cardiac function, myocardial injury markers, pathological morphology of the heart, level of pyroptosis and mitochondrial function were assessed. Protein microarray, biolayer interferometry and pull-down assays were used to confirm the target of emodin. Moreover, GSDMD-overexpressing plasmids were transfected into GSDMD −/− mice and HL-1 cells to further verify whether emodin suppressed GSDMD activation. Results Emodin therapy markedly enhanced cardiac function and reduced cardiomyocyte pyroptosis in mice induced by Dox. Mechanistically, emodin binds to GSDMD and inhibits the activation of GSDMD by targeting the Trp415 and Leu290 residues. Moreover, emodin was able to mitigate Dox-induced cardiac dysfunction and myocardial injury in GSDMD −/− mice overexpressing GSDMD, as shown by increased EF and FS, decreased serum levels of CK-MB, LDH and IL-1β and mitigated cell death and cell morphological disorder. Additionally, emodin treatment significantly reduced GSDMD-N expression and plasma membrane disruption in HL-1 cells overexpressing GSDMD induced by Dox. In addition, emodin reduced mitochondrial damage by alleviating Dox-induced GSDMD perforation in the mitochondrial membrane. Conclusion Emodin has the potential to attenuate DIC by directly binding to GSDMD to inhibit pyroptosis. Emodin may become a promising drug for prevention and treatment of DIC.

CAS / MDL: 518-82-1
研究领域: 药理学 · 心脏病学 · 分子生物学 · 细胞生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ACS Omega · 2021 · IF 3.512

Construction of a Phenylboronic Acid-Functionalized Nano-Prodrug for pH-Responsive Emodin Delivery and Antibacterial Activity

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 · 肿瘤学 · 微生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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