MOLECULES
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2017
·Vol. 22
·期 9
·1494
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IF 2.861
Yan Du,Zhibin Wang,Libo Wang,Mingjie Gao,Liqian Wang,Chunli Gan,Chunjuan Yang
A rapid and sensitive Ultra High Performance Liquid Chromatography Electrospray Ionization Tandem Mass Spectrometry (UHPLC-ESI-MS/MS) method was developed and validated to simultaneously determine the concentration of seven phenolic acids (syringic acid, ferulic acid, caffeic acid, vanillic acid,p-coumaric acid, 3,4-dihydroxybenzoic acid and 4-hydroxybenzoic acid) in rat plasma after oral administration ofEchinacea purpureaextract. After mixing with the internal standard (IS), butylparaben, plasma samples were prepared by liquid–liquid extraction with ethyl acetate. The separation was performed using the Agilent Eclipse Plus C18column (1.8 μm, 2.1 mm × 50 mm) with a gradient system consisting of solution A (0.1% acetic acid in water) and solution B (methanol) at a flow rate of 0.3 mL/min. The detection was accomplished by a multiple reaction monitoring (MRM) mode with electrospray ionization (ESI). The method was validated in terms of linearity, precision, accuracy, extraction recovery, matrix effect and stability. This method was successfully applied to study the pharmacokinetic properties of the seven compounds after oral administration ofEchinacea purpureaextract in rats.Keywords:Echinacea purpurea;phenolic acids;UHPLC-ESI-MS/MS;pharmacokinetics
研究领域:
分析化学
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药理学
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植物化学
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DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR LIQUIDS
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2021
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IF 6.165
Helin Xu,Xueqin Li,Yanyan Hao,Xiaobin Zhao,Yun Cheng,Jinli Zhang
To achieve simple and efficient separation of acteoside (ACT), extraction ACT from crude extracts of Cistanche tubulosa via ionic liquid (IL) based aqueous two-phase system (ATPS) is investigated. The IL–ATPS comprising [C 4 mim]BF 4 and (NH 4 ) 2 SO 4 exhibits excellent extraction performance, extracting almost all ACT in the [C 4 mim]BF 4 -rich phase. The high polarity of [C 4 mim]BF 4 having multi-hydrogen bond receptors is conducive for extracting ACT in the IL-rich phase, and (NH 4 ) 2 SO 4 not only provides a weak acidic microenvironment for increasing ACT stability in the IL-rich phase but also reduces the solubility of ACT in the salt-rich phase via the salting-out effect. In addition, molecular simulation results show that ACT is extracted in the [C 4 mim]BF 4 -rich phase via multi-interactions, including hydrogen bonding, van der Waals forces, and π–π stacking. This study is expected to provide a valuable reference for the separation of bioactive constituents from natural products.
研究领域:
植物化学
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天然产物分离
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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
Frontiers in Chemistry
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2020
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IF 3.693
Zhao Xiaobin,Cheng Yun,Xu Helin,Hao Yanyan,Lv Yin,Li Xueqin
Acteoside (ACT) belongs to a type of phenylethanoid glycosides (PhGs), and it is worthy of obtaining high-purity due to its significant medicinal functions. In this study, a novel class of MIMs was designed and synthesized with PVDF membranes as the base membrane for high selective separation and enrichment of ACT. The effects of the different functional monomers, the amounts of functional monomers, crosslinking agents, and initiators on the separation properties of MIMs were investigated. Furthermore, adsorption ability, permeation capacity, and reusability of MIMs were discussed for ACT. It indicated that MIM7 was the optimal performance of MIMs. The adsorption ability of MIM7 for ACT was 62.83 mg/g, and the selectivity factor (α) of MIM7 was up to 2.74 and its permeability factor (β) was greater than 2.66. Moreover, the adsorption amount of MIM7 was still more than 88.57% of the initial value after five cycles. As an ACT imprinted layer of MIMs only had recognition sites for ACT molecules, which recombined with the recognition sites in the membrane permeation experiment, ACT molecules penetration was hindered. However, the analogs of ECH successfully passed MIMs. It indicated that the selective MIMs for ACT followed the mechanism of delayed permeation. This work provides an important reference for the high permselective separation of natural products.
研究领域:
药学
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分离科学与技术
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PubMed
高影响因子
CHEMICAL ENGINEERING RESEARCH & DESIGN
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2022
·
IF 4.119
Chunying Li,Fang Nie,Changyin Feng,Mengfei Tian,Meiting Yu,Chunjian Zhao,Yujie Fu
A creative dual-template molecularly imprinted polymer (Fe 3 O 4 @MCM-41-MIPs) with good magnetic properties and specific recognition of echinacoside and acteoside was prepared by surface imprinting. Echinacoside and acteoside served as dual templates, 4-vinylpyridine (4-VP) was used as a functional monomer , the cross-linker was ethylene glycol dimethacrylate (EGDMA), and the selected initiator was azobisisobutyronitrile (AIBN). The prepared Fe 3 O 4 @MCM-41-MIPs were applied to the selective separation and enrichment of echinacoside and acteoside from Cistanche deserticola Y. C. Ma ( C. deserticola ). The resulting Fe 3 O 4 @MCM-41-MIPs were characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier transform infrared spectroscopy (FT-IR), laser particle size scanning and vibration sample magnetometry (VSM). The results of the isotherm adsorption experiment showed that the maximum adsorption capacities of Fe 3 O 4 @MCM-41-MIPs for echinacoside and acteoside were 6.02 and 1.63 mg·g -1 , respectively, at 298 K. The pseudo-second-order reaction mechanism showed that the equilibrium adsorption capacities of Fe 3 O 4 @MCM-41-MIPs for echinacoside and acteoside were 4.81 and 0.93 mg·g -1 , respectively. The characterization of Fe 3 O 4 @MCM-41-MIPs showed that the imprinted layer with dual-template molecules was wrapped on the outside of the carrier, and the obtained Fe 3 O 4 @MCM-41-MIPs showed good saturation magnetization , desirable capacity for echinacoside and acteoside adsorption, and satisfactory reuse (echinacoside and acteoside maintained relative adsorption rates of 97.5% and 95.8% after five cycles). After separation, the purities of echinacoside and acteoside were 33.50% and 27.00%, respectively. In addition, in the selective adsorption experiment, the synthesized Fe 3 O 4 @MCM-41-MIPs showed better selectivity for echinacoside and acteoside than their structural analogs. Therefore, this method proved to be sustainable, rapid and highly efficient for the separation and enrichment of echinacoside and acteoside.
研究领域:
中药化学
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分离科学
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DOI
高影响因子
TECHNOLOGY AND HEALTH CARE
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2024
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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
INTERNATIONAL IMMUNOPHARMACOLOGY
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2024
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IF 4.8
Ye Zhao,Xu Luo,Jinyuan Hu,Mogellah John Panga,Clara Appiah,Zhanxiang Du,Lin Zhu,Vladimir Retyunskiy,Xing Gao,Bo Ma,Qi Zhang
Syringin (SRG) is a bioactive principle possessing extensive activities including scavenging of free radicals, inhibition of apoptosis, and anti-inflammatory properties. However, its effects on spermatogenic defects and testicular injury as well as the underlying mechanisms are still unclear. This study aims to investigate the protective effect of SRG on testis damage in zebrafish and explore its potential molecular events. Zebrafish testicular injury was induced by exposure to bisphenol A (BPA) (3000 μg/L) for two weeks. Fish were treated with intraperitoneal injection of SRG at different doses (5 and 50 mg/kg bodyweight) for two more weeks under BPA induction. Subsequently, the testis and sperm were collected for morphological, histological, biochemical and gene expression examination. It was found that the administration of SRG resulted in a significant protection from BPA-caused impact on sperm concentration, morphology, motility, fertility rate, testosterone level, spermatogenic dysfunction and resulted in increased apoptotic and reactive oxygen species’ levels. Furthermore, testicular transcriptional profiling alterations revealed that the regulation of inflammatory response and oxidative stress were generally enriched in differentially expressed genes (DEGs) after SRG treatment. Additionally, it was identified that SRG prevented BPA-induced zebrafish testis injury through upregulation of fn1a , krt17 , fabp10a , serpina1l and ctss2 . These results indicate that SRG alleviated spermatogenic defects and testicular injury by suppressing oxidative stress and inflammation in male zebrafish.
研究领域:
药理学
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毒理学
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生殖生物学
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水生毒理学
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DOI
PubMed
高影响因子
International Journal of Nanomedicine
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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
FOOD AND CHEMICAL TOXICOLOGY
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2020
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IF 4.679
Fei Zhou,Weisu Huang,Tao Xu,Lipeng Wu,Qi Chen,Jiyu Peng,Xin Liu,Baiyi Lu
Acteoside is one of the most widespread phenylethanoid glycosides with pharmacological activities , including antioxidant, neuroprotective property, etc. However, its bioavailability is poor due to the low absorption and P-gp efflux. This study aimed to select food derived P-gp inhibitors for promoting the acteoside absorption and investigate whether the inhibitors could increase the bioavailability and stability of acteoside. Results showed that EGCG and quercetin significantly decreased the BL-to-AP efflux and promoted the AP-to-BL influx of acteoside across Caco-2 monolayers with optimum concentrations of 320 μM EGCG or 240 μM quercetin adding to 320 μM acteoside. EGCG increased the bioavailability of acteoside to 1.43-fold, but quercetin had no such effect. Further study showed that EGCG and quercetin had no effects on the storage and digestion stability of acteoside. This work revealed that EGCG could improve the acteoside absorption across the Caco-2 monolayers and enhance the bioavailability of acteoside in rats.
研究领域:
药理学
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营养保健品
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药物递送
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2025
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IF 8.5
Linwei Yu,Xi Li,Tianyi Shi,Ning Li,Donge Zhang,Xikai Liu,Yushuo Xiao,Xinran Liu,Robert B. Petersen,Weikang Xue,Yanxun V. Yu,De-sheng Hu,Li Xu,Hong Chen,Ling Zheng,Kun Huang,Anlin Peng
Parkinson's disease (PD), a neurodegenerative disorder without cure, is characterized by the pathological aggregation of α-synuclein (α-Syn) in Lewy bodies. Classic deposition pathway and condensation pathway contribute to α-Syn aggregation, and liquid-liquid phase separation is the driving force for condensate formation, which subsequently undergo liquid-solid phase separation to form toxic fibrils. Traditional Chinese Medicine (TCM) has a long history in treating neurodegenerative disease; herein, we identified chemicals from herbs that inhibit α-Syn aggregation. We screened commonly prescribed TCMs for PD from the CNKI database and registered patents, 13 chemicals were identified in the TCMSP databases as candidate inhibitors, among which three phenols, forsythoside B (FTSB), echinacoside (ECH), and 4-hydroxyindole (C4-OH) efficiently inhibit α-Syn aggregation. Moreover, FTSB and ECH increase α-Syn fluidity within condensates, inhibit α-Syn transition into amyloid fibrils and reduce fibril-induced toxicity in SH-SY5Y cells. Importantly, they disaggregated preformed α-Syn amyloid fibrils. Notably, in an α-Syn overexpressing NL5901 C. elegans PD model, either FTSB or ECH treatment significantly extended the lifespan and improved the PD-like movement disorders, both in the preventive and therapeutic treatment approaches, by reducing toxic α-Syn inclusion formation and improving the fluidity of α-Syn. Together, we offer new therapeutic candidates targeting phase separation-associated aggregation for PD.
研究领域:
神经科学
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药理学
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分子生物学
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传统医学
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
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2018
·Vol. 19
·期 4
·1135
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IF 3.687
Maiquan Li,Tao Xu,Fei Zhou,Mengmeng Wang,Huaxin Song,Xing Xiao,Baiyi Lu
Nuclear factor erythroid 2-related factor 2 (Nrf2) is a key transcription factor against oxidative stress and neurodegenerative disorders. Phenylethanoid glycosides (PhGs; salidroside, acteoside, isoacteoside, and echinacoside) exhibit antioxidant and neuroprotective bioactivities. This study was performed to investigate the neuroprotective effect and molecular mechanism of PhGs. PhGs pretreatment significantly suppressed H2O2-induced cytotoxicity in PC12 cells by triggering the nuclear translocation of Nrf2 and reversing the downregulated protein expression of heme oxygenase 1 (HO-1), NAD(P)H quinone oxidoreductase 1 (NQO1), glutamate cysteine ligase-catalytic subunit (GCLC), and glutamate-cysteine ligase modifier subunit (GCLM). Nrf2 siRNA or HO-1 inhibitor zinc protoporphyrin (ZnPP) reduced the neuroprotective effect. PhGs showed potential interaction with the Nrf2 binding site in Kelch-like ECH-association protein 1 (Keap1). This result may support the hypothesis that PhGs are activators of Nrf2. We demonstrated the potential binding between PhGs and the Keap1-activated Nrf2/ARE pathway, and that PhGs with more glycosides had enhanced effects.Keywords:Keap1;Nrf2;Neuroprotective;PC12 cells;PhGs
研究领域:
神经科学
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药理学
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细胞生物学
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分子生物学
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DOI
PubMed
高影响因子
Frontiers in Cell and Developmental Biology
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2021
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IF 6.684
Li Ying-Qi,Chen Yi,Jiang Si-Qi,Shi Yuan-Yuan,Jiang Xiao-Li,Wu Shan-Shan,Zhou Ping,Wang Hui-Ying,Li Ping,Li Fei
Alzheimer’s disease (AD) is the most frequent type of dementia. Acteoside (ACT) is a compound isolated from Cistanche tubulosa, which possesses excellent neuroprotective properties. However, the underlying mechanism of ACT in regulating microglia polarization remains ill-defined. Therefore, a computational network model was established to identify the driving targets of ACT and predict its mechanism by integrating multiple available databases. The AlCl3-induced AD model in zebrafish larvae was successfully constituted to demonstrate the therapeutic efficacy of ACT. Subsequently, LPS-induced BV-2 cells uncovered the positive role of ACT in M1/M2 polarization. The NF-κB and AMPK pathways were further confirmed by transcriptomic analysis, metabolomics analysis, molecular biology techniques, and molecular docking. The research provided an infusive mechanism of ACT and revealed the connection between metabolism and microglia polarization from the perspective of mitochondrial function. More importantly, it provided a systematic and comprehensive approach for the discovery of drug targets, including the changes in genes, metabolites, and proteins.
研究领域:
神经科学
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药理学
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分子生物学
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生物信息学
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DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）