INDUSTRIAL CROPS AND PRODUCTS
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2020
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IF 4.244
Xinsheng Wang,Yanfang Wu,Jie Li,Aoxiang Wang,Guangyao Li,Xueli Ren,Weiping Yin
In this work, deep eutectic solvents (DESs) were synthesized using ultrasound-assisted and stirring heating methods. DES combined with ultrasonic-assisted extraction (UAE) was proposed for the efficient extraction of glycosides from Syringa pubescens Turcz. A series of DES systems were used to evaluate the extraction efficiency of glycosides in S. pubescens . The DES composed of choline chloride/glycerol extracted higher than those of conventional solvents and other DESs. The extraction procedure of DES-UAE was optimized using response surface methodology. The extraction solvent was choline chloride-glycerol formed a DES with the mole ratio of 1:2 with 20 % of water content. The optimum conditions for echinacoside (ECH) and oleuropein (OLE) were ultrasound power of 200 W, extraction temperature of 68 °C, solvent to solid ratio of 20:1 mL/g and the extraction time of 45 min. Furthermore, the DES with 30 % water content can be used as dilution solvent before HPLC analysis of DES extract. In addition, the enrichment of ECH and OLE from DES extract was achieved using HPD-450 macroporous resin, with the recoveries of 80.04 % and 86.21 %, respectively.
研究领域:
植物化学
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分析化学
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DOI
高影响因子
Chemical Biology & Drug Design
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2025
·Vol. 105
·期 4
·e70097
·
IF 3.3
Wei-fang Song,Sheng-nan Li,Rui-xin Yao,Qiu-yan Jiang,Ting Shi,Dan-dan Fan,Hai-juan Zhang,Wen-hui Zhang,Rui-jun Wang
The primary objective aims to evaluate the therapeutic efficacy of echinacoside in ameliorating hepatic steatosis and exploring its role in modulating autophagic flux through AMP-activated protein kinase (AMPK) signaling, positioning it as a potential treatment for non-alcoholic fatty liver disease (NAFLD). A well-established NAFLD rat model was employed, administering varying concentrations of echinacoside. Biochemical parameters, including triglycerides (TG), total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), alongside liver enzymes alanine aminotransferase (ALT), aspartate aminotransferase (AST), and alkaline phosphatase (ALP), were measured to assess liver function. To elucidate the molecular mechanisms, western blot analyses were performed to assess the expressions of p-AMPK, total AMPK, and key autophagy markers LC-3 I/II and Beclin-1. Echinacoside significantly improved the lipid profile by lowering plasma TG, TC, and LDL-C levels while increasing HDL-C. It also reduced serum ALT, AST, and ALP activities, demonstrating hepatoprotective effects. Notably, echinacoside reversed the p-AMPK levels in NAFLD rats in a dose-dependent manner, with the highest dosage showing the strongest effect. This was accompanied by increased expression of LC-3 I/II and Beclin-1. Echinacoside is expected to be a therapeutic drug for NAFLD by activating AMPK activity and enhancing autophagy to improve liver function. These findings suggest its clinical potential, with autophagy modulation via the AMPK pathway as a possible therapeutic mechanism for NAFLD treatment.
研究领域:
药理学
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代谢生物学
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肝脏疾病研究
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2014
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IF 3.096
Di Zhang,Hua Li,Jian-Bo Wang
Amyloid protein depositions play crucial roles in a variety of degenerative disorders composing amyloidosis . There is a great interest in developing small molecule inhibitors of amyloidogenic processes. We examined the inhibitory effects of echinacoside (ECH) with different concentrations and at different fiber-forming stages in vitro utilizing the hen egg-white lysozyme (HEWL) model system. We also evaluated the antioxidant capacity of ECH by using elimination tests for the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and hydroxyl ( HO) free radicals. We investigated the protection provided by ECH against neurotoxicity induced by β-amyloid protein (Aβ). Through spectroscopic analyses, electron microscopy , cell viability assay, and hemolysis assay, we found that ECH dose dependently inhibited HEWL aggregation, and this inhibition occurred in different fiber-forming stages. ECH could also scavenge the DPPH and OH free radicals in a concentration-dependent manner. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and 2′,7′-dichlorodihydrofluoresceindiacetate (DCFH-DA) fluorescent measurement results indicated that ECH could increase viability of rat pheochromocytoma PC12 cells injured by Aβ and suppress the increase in intracellular reactive oxygen species (ROS) triggered by Aβ. The present study findings facilitate a better understanding of the interaction between ECH and amyloid-forming proteins and also shed light on the protection of ECH against amyloid fibril-induced neuronal cell death.
研究领域:
生物化学
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神经科学
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药理学
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DOI
PubMed
高影响因子
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
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2025
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IF 2.2
Yang Han,Junyong Fan,Wei Xia,Xiao Dong,Ying Ye
Primary liver cancer remains a major contributor to global cancer-related mortality. Echinacoside, a bioactive phenylethanoid glycoside isolated from traditional Chinese medicinal herbs, has shown potent anti-tumor effects. In this study, poly (lactic-co-glycolic acid) (PLGA) nanoparticles encapsulating echinacoside (E@PLGA and E@PLGA-FA) were synthesized via the double emulsification method. Their physicochemical properties, drug release kinetics, and anti-cancer efficacy were systematically evaluated through in vitro and in vivo models. Transmission electron microscopy (TEM) and dynamic light scattering (DLS) analyses revealed that the particle sizes of E@PLGA and E@PLGA-FA were approximately 91 nm and 100 nm, respectively, with zeta potentials of -22.50 mV and -31.89 mV. The polydispersity index (PDI) of E@PLGA and E@PLGA-FA was determined to be 0.16±0.01 and 0.19±0.01, respectively. The encapsulation efficiency and drug-loading capacity of echinacoside in E@PLGA-FA were 28.78% and 12.05%, respectively, slightly lower than those in E@PLGA nanoparticles (40.34% and 16.12%), likely due to folic acid modification altering PLGA solubility during formulation. In vitro release profiles demonstrated pH-dependent drug release: 22% at physiological pH (7.4) versus 67% under acidic conditions (pH 5.5) over 12 h, indicating tumor microenvironment-responsive behavior. Furthermore, E@PLGA-FA significantly inhibited the proliferation of HepG2 cells, induced apoptosis, caused cell cycle arrest at the G0/G1 phase, and suppressed cell mobility. Meanwhile, the protein levels of MMP2, MMP9 and Bax were increased after exposure to E@PLGA and E@PLGA-FA, whereas the protein levels of COL-Ⅰ, COL-Ⅱ, Bcl-2, Cyclin D1, and PCNA were decreased. In vivo, E@PLGA-FA effectively inhibited tumor growth, induced tumor cell apoptosis, and exhibited tumor-specific accumulation confirmed by fluorescence imaging. In addition, The E@PLGA-FA nanoparticle intervention did not induce pathological damage or inflammatory responses in murine liver and kidney tissues, suggesting a favorable safety profile for this compound. In conclusion, we engineered a novel tumor-targeted PLGA-based nanoparticle system for echinacoside delivery, which synergizes pH-responsive drug release, multi-mechanistic anti-cancer effects, and biosafety, offering a promising therapeutic platform for hepatocellular carcinoma.
研究领域:
药剂学
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肿瘤学
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DOI
PubMed
高影响因子
Scientific Reports
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2018
·Vol. 8
·期 1
·1-11
·
IF 4.122
Jiang Zhihui,Zhou Bo,Li Xinping,Kirby Gordon M.,Zhang Xiaoying
Male infertility is a major health issue with an estimated prevalence of 4.2% of male infertility worldwide. Our early work demonstrated that Cistanche extracts protect against sperm damage in mice and that echinacoside (ECH) is one of the major active components. Here we report an essential role for ECH, a natural product that reverses or protects against oligoasthenospermia in rats. ECH was assayed by HPLC, the quantity and quality of sperm was evaluated and hormone levels were determined by radioimmunosorbent assay. ECH reduced levels of androgen receptor (AR) and key steroidogenic-related genes as determined by Western blot and qPCR analysis. The interaction between ECH and AR were evaluated by indirect ELISA and molecular docking. The results show that ECH combined with hypothalamic AR in the pocket of Met-894 and Val-713 to inhibit transfer of AR from the cytoplasm to nuclei in the hypothalamus. While negative feedback of sex hormone regulation was inhibited, positive feedback was stimulated to increase the secretion of luteinizing hormone and testosterone subsequently enhancing the quantity of sperm. Taken together, these data demonstrate that ECH blocks AR activity in the hypothalamus to increase the quantity of sperm and protect against oligoasthenospermia in rats.
研究领域:
药理学
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生殖生物学
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分子生物学
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内分泌学
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DOI
PubMed
高影响因子
SENSORS AND ACTUATORS B-CHEMICAL
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2018
·
IF 5.667
Shuo Li,Yinghao Duan,Sheng Lei,Jiantong Qiao,Gaiping Li,Baoxian Ye
In this work, a brand new nanocomplex (denoted as [email protected] ) is elaborately designed and successfully synthesized meaning the in-situ assembly of porous-morphology Zn-based MOFs (MOF-5) onto the as-prepared PDDA-rGO-Ni (PGN for short) nanocomposites. When this nanocomplex contributes to construct the electrochemical sensor ( [email protected] /GCE), it presents a highly-sensitive response towards echinacoside, and the first measurement for echinacoside by electrochemistry accordingly evolves forward. The crystallization processes are investigated by FT-IR instrument and XRD analysis, as well as micro-morphology of modified materials is visible upon SEM and TEM. Adorably, a novel ratiometric sensor was progressively fabricated by encapsulating methylene blue (MB) molecules into cubic MOF-5 framewoks (MB encased [email protected] /GCE), and apart from assisting in establishing the analysis method with extreme accuracy and favorable practicality, it dose devote a wider linear scale and a lower detection limit than that [email protected] /GCE has given out. Drawn from the developed calibration curve using differential pulse voltammetry (DPV) technique, the peak intensity ratio (I Ech /I MB ) varies linearly with increased echinacoside concentration in the range of 3.0 × 10 −8 – 1.0 × 10 −6 mol L −1 with limit of detection (LOD) reaching 1.0 × 10 −8 mol L −1 (S/N = 3). Additionally, the proposed assay method has been employed to detect echinacoside in real sample sliced cistanche with satisfactory results.
研究领域:
分析化学
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电化学
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纳米材料
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药物分析
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DOI
高影响因子
JOURNAL OF CELLULAR PHYSIOLOGY
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2018
·Vol. 234
·期 2
·1880-1888
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IF 3.923
Ying Ye,Yanan Song,Juhua Zhuang,Guoyu Wang,Jing Ni,Wei Xia
Echinacoside (ECH) is a phenylethanoid glycoside extracted from a Chinese herbal medicine, Cistanches salsa . ECH possesses many biological properties, including anti-inflammation, neural protection, liver protection, and antitumor. In the current study, we aimed to explore the effects of ECH on hepatocellular carcinoma (HCC) and the underlying mechanisms. The results showed that ECH could attenuate diethylnitrosamine (DEN)-induced HCC in mice, and exerted antiproliferative and proapoptotic functions on HepG2 HCC cell line. ECH exposure in HepG2 cells dose-dependently reduced the phosphorylation of AKT (p-AKT) and enhanced the expression of p21 (a cell cycle inhibitor) and Bax (a proapoptotic protein). Furthermore, ECH significantly suppressed insulin-like growth factor-1-induced p-AKT and cell proliferation. These data indicated that phosphoinositide 3-kinase (PI3K)/AKT signaling was involved in the anti-HCC activity of ECH. Gene set enrichment analysis results revealed a positive correlation between the PI3K pathway and triggering receptors expressed on myeloid cells 2 (TREM2) expression in HCC tissues. ECH exposure significantly decreased TREM2 protein levels in HepG2 cells and DEN-induced HCC. Furthermore, ECH-mediated proliferation inhibition and AKT signaling inactivation were notably attenuated by TREM2 overexpression. In conclusion, ECH exerted its antitumor activity via decreasing TREM2 expression and PI3K/AKT signaling.
研究领域:
肿瘤学
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药理学
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细胞生物学
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DOI
PubMed
高影响因子
Experimental and Therapeutic Medicine
·
2018
·Vol. 16
·期 2
·643-648
·
IF 1.41
Sibo Li,Haitao Jiang,Xiaohua Gu
Glucocorticoids (GCs) are widely used to treat chronic diseases. Prolonged and/or overdose administration of GCs has many side‑effects to human health including GC‑induced osteoporosis (GIOP). In this investigation, the objective was to assess the influence that echinacoside (ECH) exerts upon dexamethasone‑treated murine osteoblastic MC3T3‑E1 cells. We found that ECH (5, 10, 20 and 40 mg/l) inhibited dexamethasone (1,000 nM)‑suppressed cell viability as demonstrated by Cell Counting Kit‑8 (CCK‑8) assay. The dose of 10 mg/l was selected for the following experiments because this dose had a better effect than the dose of 5 mg/l, and the doses >10 mg/l had a similar effect as this dose. ECH (10 mg/l) or pifithrin‑α (PFT‑α) (a p53 inhibitor, 20 µM) suppressed dexamethasone‑induced MC3T3‑E1 apoptosis as illustrated by Annexin V/propidium iodide (PI) double‑labeling flow cytometry analysis. ECH or PFT‑α treatment also alleviated dexamethasone's action of inhibiting Bcl‑2 expression as well as dexamethasone's action of stimulating on the expression of p53 and Bax. Moreover, lentivirus mediated‑p53 overexpression reversed the effects of ECH in dexamethasone‑treated MC3T3‑E1 cells, suggesting that ECH induced anti‑apoptotic effects in dexamethasone‑treated osteoblasts via p53‑dependent pathway. In summary, ECH has a protective effect against osteoblastic cell apoptosis induced by dexamethasone, suggesting that ECH may have potentials for clinical application in the treatment of GIOP.
研究领域:
药理学
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细胞生物学
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骨骼健康
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DOI
PubMed
高影响因子
International Journal of Nanomedicine
·
2024
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IF 6.6
Zemin Ou,Yun You,Hong Yi,Xiaoqian Liu,Yan Tong,Dewen Liu,Jinyu Wang
Introduction Parkinson’s disease (PD) is a common neurodegenerative disorder characterized by the degeneration of dopaminergic neurons in the substantia nigra. The precise molecular mechanisms underlying neuronal loss in PD remain unknown, and there are currently no effective treatments for PD-associated neurodegeneration. Echinacoside (ECH) is known for its neuroprotective effects, which include scavenging cellular reactive oxygen species and promoting mitochondrial fusion. However, the blood-brain barrier (BBB) limits the bioavailability of ECH in the brain, posing a significant challenge to its use in PD treatment.Methods We synthesized and characterized PEGylated ECH liposomes (ECH@Lip) and peptide angiopep-2 (ANG) modified liposomes (ECH@ANG-Lip). The density of ANG in ANG-Lip was optimized using bEnd.3 cells. The brain-targeting ability of the liposomes was assessed in vitro using a transwell BBB model and in vivo using an imaging system and LC-MS. We evaluated the enhanced neuroprotective properties of this formulation in a the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced PD model.Results The ECH@ANG-Lip demonstrated significantly higher whole-brain uptake compared to ECH@Lip and free ECH. Furthermore, ECH@ANG-Lip was more effective in mitigating MPTP-induced behavioral impairment, oxidative stress, dopamine depletion, and dopaminergic neuron death than both ECH@Lip and free ECH.Conclusion The formulation used in our study significantly enhanced the neuroprotective efficacy of ECH in the MPTP-induced PD model. Thus, ECH@ANG-Lip shows considerable potential for improving the bioavailability of ECH and providing neuroprotective effects in the brain.
研究领域:
神经科学
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药学
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生物技术
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DOI
PubMed
高影响因子
TECHNOLOGY AND HEALTH CARE
·
2024
·
IF 1.4
Wang Guoyu,Han Yang,Zhuang Juhua,Mai Zhongchao,Xia Wei,Ye Ying
BACKGROUND: Hepatocellular carcinoma (HCC) is the third leading cause of cancer-attributed mortality and the primary liver malignancy in the world. Echinacoside is a phenylethanoid glycoside derived from traditional Chinese medicinal herbs which possessed multiple health benefits on humans, including anti-tumor effects. OBJECTIVE: This study aimed to demonstrate the function of echinacoside in HCC progression and the involvement of miR-30c-5p/FOXD1/KLF12 axis. METHODS: The HepG2 cells were treated by different dose of echinacoside, miR-30c-5p mimic, miR-30c-5p inhibitor, and FOXD1 overexpression lentiviruses or siRNA individually or simultaneously. The cell invasion and migration were measured by transwell assay. RNA and protein levels were tested by RT-PCR and western blot, respectively. The regulatory function of miR-30c-5p on Forkhead box D1 (FOXD1), FOXD1 on Krüppel-like factor 12 (KLF12) was tested by luciferase reporter assay or/and ChIP assay. Meanwhile, a liver cancer lung metastasis mice model was used to examine the functions of echinacoside and miR-30c-5p on HCC metastasis in vivo. Moreover, the correlations among miR-30c-5p, FOXD1, KLF12, and HCC prognosis was analyzed using clinical sample and TCGA database. RESULTS: Based on both in vitro and in vivo investigations, we found that echinacoside could inhibit HCC cell migration, invasiveness, and tumor metastasis, and associated with the enhanced miR-30c-5p/FOXD1/KLF12 axis. Furthermore, through analyzing the interactions among intermediate molecules, we revealed that miR-30c-5p, FOXD1, and KLF12üere clinically relevant with each other in HCC patients, correlated with HCC prognosis, and regulated by echinacoside to contribute in the inhibition of HCC progression. CONCLUSIONS: These findings suggest that echinacoside could inhibit HCC progression, and the mechanism related to the enhanced miR-30c-5p/FOXD1/KLF12 axis. Moreover, the abovementioned intermediate molecules might serve as prospective biomarkers for HCC prognosis.
研究领域:
肿瘤学
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分子生物学
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药理学
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中药学
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DOI
PubMed
高影响因子
FREE RADICAL BIOLOGY AND MEDICINE
·
2026
·
IF 8
Zi Li,Zhi Li,Qiubo Li,Ronghui Miao,Yuchao Ma,Silei Wei,Junnan Mao,Xuan Wang,Xiangtao Zeng,Yi Zhou,Jingjing Ye,Weidong Xia,Cai Lin,Cong Mao
Due to complex immune and metabolic dysfunctions, diabetic wounds commonly suffer from infection, oxidative stress, impaired angiogenesis, thereby leading to chronic non-healing lesions. Since current therapies remain insufficient, increasing attention has been directed toward mitophagy, a key regulator of energy balance and stress responses, with mitochondrial dysfunction recognized as a critical driver of defective repair. In this study, we explored the therapeutic role of echinacoside (Ech), a phenylethanol glycoside from Echinacea , known for its potent antioxidant, anti-inflammatory, and pro-angiogenic properties, in promoting diabetic wound healing. Network pharmacology analysis was employed to identify the potential targets of Ech in diabetic condition. In vitro, under H 2 O 2 -induced oxidative stress, Ech mitigated the functional impairment of human umbilical vein endothelial cells (HUVECs), enhancing their proliferation, migration, angiogenesis, and antioxidant capacity. Mechanistically, Ech restored HUVECs function by activating Parkin-MFN2-mediated mitophagy through ubiquitination and concurrently upregulated USP35 expression, which mitigated excessive mitophagy. These effects were confirmed using the Parkin-dependent mitophagy inhibitor cyclosporin A (CsA) and USP35-specific siRNA (siUSP35). In a diabetic mouse full-thickness cutaneous wound model, Ech treatment significantly activated Parkin-dependent mitophagy, leading to enhanced neovascularization and collagen deposition at wound site, thereby accelerated the healing process of diabetic wounds. Collectively, these findings identify Ech as a promising therapeutic agent for diabetic wound repair and provide mechanistic insights into its regulation of mitophagy to improve antioxidant responses and angiogenesis, offering a foundation for the development of targeted treatment strategies.
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DOI
PubMed
高影响因子
JOURNAL OF MICROBIOLOGY AND BIOTECHNOLOGY
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2026
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IF 3.4
YiXi Zeng,Yanqing Ma,Shunfan Chen,Lanyue Zhang,Hui Li
We aimed to investigate the neuroprotective effect of Echinacoside (ECH) extracted from Cistanche tubulosa (Schenk) Wight in a mouse model of LPS-induced neuroinflammation and associated memory impairment, and the potential role of the microbiota-gut-brain axis (MGBA) in this process. Intraperitoneal injection of LPS in mice can induce inflammation, causing learning and memory impairment, and it can also affect the balance of the intestinal flora. The Morris water maze (MWM) experiment, immunohistochemistry, immunofluorescence chemistry, Nissl staining, and 16S rRNA gene sequencing of the mice intestinal flora were performed for the study. The results of the MWM experiment showed that mice treated with ECH were able to find the platform faster compared to the model group, with shorter distances moved than the C. tubulosa (Schenk) Wight extract (CTE) group, and they had more platform crossings. Immunofluorescence staining of brain cortex and hippocampal tissues showed that ECH could attenuate LPS-induced neuronal damage and reduce the expression levels of Ionized calcium-binding adapter molecule 1 (Iba-1) positive cells and the Tumor Necrosis Factor-alpha (TNF-α). 16S rRNA gene sequencing of mice intestinal flora revealed that ECH exerted beneficial effects by reshaping the structure of the intestinal flora. Our findings suggest that ECH may be beneficial for alleviating neuroinflammation-related cognitive impairments, providing theoretical support for a new neuro-psycho-pharmacological approach to MGBA-related diseases through restoring intestinal flora homeostasis.
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PubMed
高影响因子
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