Frontiers in Pharmacology
·
2024
·
IF 4.4
Li Qing-qing,Yan Jia-hui,Zhou Zhi-e,Geng Xiang,Xiong Jian-hua
Introduction: Chlorogenic acid (CGA) has been identified to possess salient anti-inflammatory, antioxidant, and anticancer attributes. However, its application is limited by its instability and low bioavailability. Liposomes have been considered effective pharmaceutical delivery vehicles due to their ability to continuously release loaded drugs, improve drug stability, and display good biocompatibility. They can be easily modified by other small molecules to acquire additional biological functions. In this study, we developed and characterized folic acid-TPGS-modified chlorogenic acid liposome (FTCLP) and evaluated its anti-inflammatory activity.Methods: The successful encapsulation of CGA within FTCLP was confirmed through examination using electron microscopy, fourier-transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC). The in vitro release characteristics of FTCLP were evaluated using the dialysis bag membrane method. Meanwhile, a dextran sulfate sodium (DSS) -induced colitis model was employed to investigate the anti-inflammatory effect of FTCLP and its mechanism.Results: The FTCLP exhibited an encapsulation efficiency (EE) of 84.85 ± 1.20% and a drug loading (DL) of 11.67 ± 0.04%. The particle size of FTCLP was determined to be 150.63 ± 0.71 nm, with a polydispersity index (PDI) of 0.198 ± 0.02 and a zeta potential of 2.61 ± 0.38 mV. The in vitro release profile followed the Higuchi model, indicating sustained-release characteristics. The in vivo study demonstrated that FTCLP treatment was effective in improving the symptoms of DSS-induced inflammatory response, as evidenced by mitigation of weight loss, reduction in the disease activity index (DAI) score, restoration of colon length, and attenuation of colon tissue damage. Furthermore, the levels of pro-inflammatory cytokines, including interferon-gamma (INF-γ), interleukin-1 beta (IL-1β), and interleukin-6 (IL-6), were markedly diminished in both the serum and colon tissue. FTCLP was also observed to suppress the expression of INF-γ, IL-1β, IL-6, tumor necrosis factor-alpha (TNF-α), and nuclear factor kappa B (NF-κB) p65, while concomitantly upregulating the expression of Janus kinase (JAK) and signal transducer and activator of transcription 3 (STAT3). Besides, the administration of FTCLP was found to result in an increase in the abundance of Lactobacillaceae and Peptostreptococcaceae, while decreasing the abundance of Bacteroidaceae, Rikenellaceae, and Helicobacteraceae.Conclusion: Following encapsulation of CGA within liposomes, FTCLP revealed favorable stability and sustained release properties, and enhanced the anti-inflammatory effects by modulating multiple inflammation-related biomarkers. FTCLP has the potential to be a safe and effective drug for targeted therapy of colitis.
研究领域:
药学
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生物医学工程
·
炎症研究
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Ran Zhang,Lulu Xing,Xin Wang,Zuoyu Shan,Tianxin Wang,Ye Zhang,Wenjie Wang,Yuan Wang,Hao Wang
Inhibiting the activity of pancreatic lipase and reducing intestinal cholesterol absorption are potential strategies to combat obesity. This study investigated the mechanisms by which hawthorn ( Crataegus pinnatifida ) extract affects pancreatic lipase (PL) and disrupts cholesterol micelle formation. Enriched with bioactive compounds, hawthorn extract (HE) inhibited PL activity through reversible mixed inhibition, with a half-maximal inhibitory concentration (IC50) of 2.92 mg/mL. Infrared spectroscopy, circular dichroism and fluorescence quenching experiments demonstrated that HE binding to PL induces conformational changes in both tertiary and secondary structures. This interaction facilitated the transformation of β-turns to random coils and quenched the fluorescence of the protein through a static quenching mechanism. HPLC, immobilized enzymes and molecular docking studies collectively revealed that rutin, chlorogenic acid, and isoquercitrin in HE exhibited strong binding affinity with PL, serving as key components in inhibiting PL activity. Furthermore, HE increased the particle size of cholesterol micelles while decreasing their solubility, which makes it more difficult for lipases to function in the intestine. Overall, our study suggests that HE may serve as an effective pancreatic lipase inhibitor, presenting potential applications in the development of functional foods for obesity reduction and lipid-lowering.
研究领域:
营养学
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生物化学
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药理学
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产品关联
DOI
PubMed
高影响因子
NEW JOURNAL OF CHEMISTRY
·
2022
·Vol. 47
·期 2
·828-837
·
IF 3.925
Tiantian Wan,Zulei Zhang,Hailong Wang,Yiwen Yang,Hanxing Yang,Jian Zhang,Yanbo Zeng,Lei Li,Jinchun Li
Chlorogenic acid (CGA), a cis-diol-containing compound, exhibits anti-inflammatory, antiviral, antimicrobial and anti-oxidation properties. Thus, selective determination of CGA in food products is extremely necessary. In this study, a boron affinity magnetic polymer named Fe3O4@SiO2@PIL was synthesized to detect the concentration of CGA in actual fruit samples. The Fe3O4@SiO2@PIL was characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier transform infrared (FT-IR) spectroscopy, X-ray photoelectron spectroscopy (XPS) and thermogravimetric (TG) analysis. The results showed that the Fe3O4@SiO2@PIL has uniform morphology, good magnetic properties, suitable structure and high stability. The experimental assays showed that the Fe3O4@SiO2@PIL can detect the concentration of CGA within 7 min, and has a good linear relationship with CGA in the concentration range of 0.025–2 μM (R2 = 0.9989) with a detection limit of 10 nM (S/N = 3). Moreover, the Fe3O4@SiO2@PIL exhibited excellent selectivity and can be reused for at least 5 runs, indicating its good stability and reusability. Finally, the Fe3O4@SiO2@PIL was used to selectively separate CGA in real fruit samples with the recovery ranging from 93.4% to 103.0% and the relative standard deviation (RSD) between 0.7% and 5.1%. This study gives a new insight into the utilization of magnetic materials by grafting boric acid functionalized ionic liquids for specific and rapid detection of natural cis-diol-containing compounds.
研究领域:
分析化学
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食品科学
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产品关联
DOI
高影响因子
MICROCHEMICAL JOURNAL
·
2022
·
IF 5.304
Yang Cheng,Hongdi Liu,Jing Li,Lixue Kuang,Guofeng Xu
In this study, magnetic molecularly imprinted polymers (Fe 3 O 4 @MIPs) were successfully synthesized through surface molecular imprinting method with chlorogenic acid (CGA) as the template molecule. The adsorption properties of Fe 3 O 4 @MIPs for CGA were carefully evaluated through adsorption kinetics, adsorption isotherms and selectivity experiments. The obtained Fe 3 O 4 @MIPs displayed high adsorption capacity (35.84 mg/g), excellent reusability and significant selectivity for CGA, and the adsorption equilibrium could be achieved within 40 min. Finally, the resulting Fe 3 O 4 @MIPs were successfully employed as effective adsorbents combined with high-performance liquid chromatography for the detection of CGA in juice samples with excellent selectivity. A good linear relationship in the range of 0.1–100 μg/mL and the limit of detection (LOD) (0.03 µg/mL) were obtained under the optimized conditions. The satisfactory recoveries of proposed method at three spiked levels analysis were 93.5 %–101.6 % with the relative standard deviation (RSD) less than 5 %.
研究领域:
食品科学
·
分析化学
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）