BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
·
2025
·
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
·
肿瘤学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF SEPARATION SCIENCE
·
2016
·Vol. 39
·期 10
·1853-1862
·
IF 2.741
Xianrui Liang,Qiao Xu
A validated method based on ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry was established to separate and identify phenolic compounds in Bidens pilosa L. Mass spectrometry experiments were performed both in positive and negative ion modes. A total of 35 compounds were detected, and 26 phenolic compounds were unequivocally identified or tentatively assigned based on retention time, maximum UV absorption, molecular formula, and fragments. The ultra high performance liquid chromatography method was validated and showed good linearity ( R 2 ≧ 0.9996) over the test range. The limits of detection and quantification were above 0.072 and 0.162 μg/mL, respectively. The relative standard deviations of intraday and interday precision were below 0.3 and 1.6%, respectively.
研究领域:
植物化学
·
分析化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF SEPARATION SCIENCE
·
2016
·Vol. 39
·期 9
·1628-1637
·
IF 2.741
Chunli Gan,Lu Liu,Yan Du,Liqian Wang,Mingjie Gao,Lijun Wu,Chunjuan Yang
A rapid and sensitive assay based on ultra-high performance liquid chromatography with electrospray ionization tandem mass spectrometry was established and validated for the simultaneous determination of cichoric acid, chlorogenic acid, quinic acid, and caffeic acid in rat plasma after oral administration of Echinacea purpurea extract using butylparaben as the internal standard. Samples were pretreated by liquid–liquid extraction with ethyl acetate. The separations for analytes were performed on an ACQUITY UPLC HSS C 18 column (1.8 μm 2.1 × 100 mm) using a gradient elution program with acetonitrile/10 mM ammonium acetate (pH 5.6) at a flow rate of 0.3 mL/min. The analytes were detected in multiple reaction monitoring mode with negative electrospray ionization. The lower limit of quantification of each analyte was not higher than 10.85 ng/mL. The relative standard deviation of the intraday and interday precisions was less than 14.69%. The relative errors of accuracies were in the range of –13.80 to 14.91%. The mean recoveries for extraction recovery and matrix effect were higher than 80.79 and 89.98%, respectively. The method validation results demonstrated that the proposed method was sensitive, specific, and reliable, which was successfully applied to the pharmacokinetic study of four components after oral administration of Echinacea purpurea extract.
研究领域:
分析化学
·
药理学
·
植物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Food & Function
·
2020
·Vol. 11
·期 9
·7576-7583
·
IF 4.171
Qiu Li,Fenfang Yang,Ranran Hou,Tingting Huang,Zhihui Hao
We extracted and purified three polysaccharides from Echinacea purpurea using pectinase-assisted extraction to obtain crude preparations and optimized the method using an orthogonal analysis. We obtained three polysaccharide fractions (EPPS-1, -2 and -3) using DEAE ion exchange and gel filtration chromatography. The homogeneity of the fractions was confirmed using high performance gel permeation chromatography. EPPS-3 administered to mice in a LPS-induced septicemia model effectively counteracted the effects of LPS resulting in significantly less lung damage. This trend was also seen in the serum and lung cytokine levels where EPPS-3 significantly decreased the levels of TNF-α and IL-6 and increased IL-10. Particularly, we fully characterized the structure of the EPPS-3 polysaccharide using a series of technologies. This polysaccharide structure was mainly composed of →4)-α-Glcp-(1→, →4)-α-Galp-(1→, T-α-Araf-(1→, →3,4)-β-GalpA-(1→ glycosidic linkages at a certain proportion. In sum, EPPS-3, with a clear structure, has potent anti-inflammatory activities and is a candidate for further development as an anti-inflammatory agent for clinical development.
研究领域:
药理学
·
免疫学
·
植物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）