COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
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2026
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IF 5.4
Yaning Wang,Zihui Cai,Quan Zhou,Anquan Yang,Min Xie,Yangruili Niu,Litao Wang,Yujie Fu
The growing demand for sustainable technologies has inspired interest in green extraction and delivery systems for plant-derived natural products. This study developed a hydrophobic deep eutectic solvent (HDES)-based nanoemulsion for efficient extraction and delivery of lignans from Schisandra chinensis . Through systematic screening, a HDES composed of menthol and octanoic acid (Men:C 8 ) was selected for extraction and subsequent preparation. After optimizing extraction parameters (solid-liquid ratio 40 mg/mL, extraction temperature 60°C, extraction time 40 min), the HDES demonstrated superior extraction efficiency (6.497 ± 0.008 mg/mL), representing a 1.12–2.08 fold improvement compared to water or conventional organic solvents. The extract-containing HDES was formulated into a nanoemulsion (HDES-NE) that exhibited excellent stability under various environmental conditions (pH, temperature, centrifugal force, storage time). The preparation conditions were optimized to establish optimal process parameters (oil-water ratio 2:17, homogenization time 3 min, ultrasonic power 360 W). The resulting nanoemulsion exhibited nanoscale characteristics (average particle size 115.78 nm, PDI < 0.3, and a zeta potential of −18.11 mV), with spherical morphology directly visualized by TEM, and no phase separation or precipitation. HDES-NE showed significant tyrosinase inhibition (IC 50 0.26 ± 0.04 mg/mL; 97.73% inhibition at 4 mg/mL), substantial UVB protection (SPF = 17.58 ± 0.27), and antimicrobial activity against skin pathogens, including Staphylococcus aureus and Cutibacterium acnes . This integrated approach, combining green extraction with nano-delivery, offers an environmentally friendly alternative for developing natural bioactive products.
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JOURNAL OF ETHNOPHARMACOLOGY
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2025
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IF 5.4
Xianbang Hou,Ran Chen,Juan Wu,Yujie Huang,Xueyuan Zhang,Shaobao Xu,Liwei He
Ethnopharmacological relevance Isatis tinctoria L. (Isatidis Radix) is a type of Chinese medicine used to treat various inflammations. Lignans are the main active ingredients of Isatidis Radix, which exhibit potent anti-inflammatory properties. However, the targets underlying the anti-inflammatory effects of Isatidis Radix remain unclear. Aim of the study The objective of this research was to investigate the active constituents of Isatidis Radix and the molecular mechanisms behind its anti-inflammatory properties. Materials and methods Firstly, Liquid Chromatography-Mass Spectrometry (LC-MS), network pharmacology, and molecular docking were employed to identify the active ingredients and key targets of Isatidis Radix lignans and predict their underlying anti-inflammatory mechanisms. Secondly, the enzyme-linked immunosorbent assay (ELISA) and the LPS-induced cell model were employed to verify the selective inhibitory effect of the active ingredients on the key target COX-2. Finally, the analgesic and anti-inflammatory effects were evaluated using the hot-plate test, acetic acid-induced writhing, complete Freund’s adjuvant-induced paw edema, and xylene-induced ear edema assays. Results A total of 24 compounds were found to be absorbed into the bloodstream, including 15 prototype components and 9 metabolites, as determined by LC-MS analysis. Furthermore, Network pharmacology analysis revealed that COX-2 served as the central target in the anti-inflammatory mechanism of Isatidis Radix lignans. Lariciresinol, a class of lignans derived from Isatidis Radix, selectively inhibited COX-2 and reduced inflammatory marker production in vitro and in vivo . It significantly increased the incubation period of heat pain, reduced writhing frequency, and decreased the severity of ear and foot swelling. Moreover, lariciresinol had no obvious gastrointestinal side effects and was not toxic to cardiomyocytes. Conclusion Our study indicates that Isatidis Radix lignans exert their anti-inflammatory effect by selectively inhibiting the COX-2 enzyme and confirms lariciresinol as a natural selective COX-2 inhibitor.
研究领域:
中药学
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分子生物学
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药理学
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JOURNAL OF FOOD COMPOSITION AND ANALYSIS
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2024
·
IF 4
Wenrui Li,Guojuan Yang,Yike Dang,Qinyuan Wang,Fan Li,Ruihong Wang,Yongning Wu,Guoliang Li
Lignans from Schisandra chinensis have strong anti-hepatotoxic, antioxidant, and anti-tumor properties. Herein, a multivariate metal-organic framework (MTV-MOF) was synthesized with biphenyl dicarboxylic acid, 3,5-diaminobenzoic acid (DABA), and aluminum-based metal salts, introduced 1,8-dihydroxynaphthalene (AM) as a porous coating, constructed a new magnetic material (Fe 3 O 4 @DUT-5-DABA@AM) and utilized in magnetic solid-phase extraction (MSPE) as potent adsorbents to adsorb Schizandrol A, Schizandrol B, Schisantherin A, Schisandrin A, and Schizandrin B, five lignans. Prepared materials were characterized using FT-IR, XRD, TEM, SEM, VSM, zeta and nitrogen adsorption-desorption analyses. At the same time, their adsorption kinetics and isothermal adsorption lines were also evaluated. Due to electrostatic interactions, π stacking interactions, and hydrogen bonding, the composite exhibited excellent extraction capability for lignans. In conjunction with HPLC-MS, the MSPE approach demonstrated promising linearity (R 2 ≥ 0.9992) and low detection limits (0.024–0.2 μg·kg −1 ) for lignans under optimal circumstances. The approach efficaciously quantified lignans in S. chinensis extract, attaining recoveries of 93.4–116.6 % with relative standard deviations ≤ 6.3 %. Compared with traditional methods, the magnetic separation method proposed in this study is simple, economical, and practical with low solvent consumption, which has unique advantages in the analysis of natural active ingredients.
研究领域:
植物化学
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分析化学
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药物学
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JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
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2021
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IF 3.205
Yuan Zhou,Mengying Wei,Meiling Fan,Zhongying Liu,Aimin Wang,Yuanyuan Liu,Lihui Men,Zifeng Pi,Zhiqiang Liu,Fengrui Song
Lignans from Schisandra chinensis (Turcz.) Baill (LFS) has been proved to improve impaired cognitive ability thereby show potential in treating Alzheimer’s disease (AD). In this study, UHPLC-Q-TOF-MS and UHPLC-QQQ-MS were adopted cooperatively to establish a method synchronously detecting 10 kinds of LFS monomers in rat plasma samples. And this method was further applied for pharmacokinetic study to compare the metabolism of LFS in normal and AD rats. The results indicated that AD rats showed an observably better absorption of LFS compared to normal rats. Based on time-varying plasma concentration of LFS, metabolomics was used to establish a plasma concentration–time-endogenous metabolite connection. In total 54 time-varying endogenous metabolites were screened and most of which were closely associated with AD. And LFS exerted a concentration dependent regulating effect to most of these metabolites. Through biomarker related pathways and biological function analysis, LFS might treat AD through neuroprotection, antioxidant damage and regulating the metabolism of unsaturated fatty acids. This is the first study connecting LFS absorbtion and endogenous metabolite changes with the time lapse. The pharmacokinetics and metabolic profile differences between normal and AD rats were firstly investigated as well. This study provides a novel perspective in exploring the effect and mechanism of LFS in treating AD.
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JOURNAL OF SEPARATION SCIENCE
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2023
·Vol. 46
·期 5
·2200719
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IF 3.1
Yu Qin,Run-Qin Wang,Rong-Rong Xing,Li Yang,Xuan Chen,Shuang Hu
A supramolecular solvent-based dispersive liquid-liquid microextraction was proposed for the extraction and determination of lignans in Forsythiae Fructus combined with high-performance liquid chromatography. The supramolecular solvent, consisting of tetrabutylammonium bromide and n -hexanol, was mixed with the sample solution to extract the analytes by a vortex. After accomplishing the extraction, the extraction phase was separated by centrifugation and collected for high-performance liquid chromatography analysis. In this work, the important extraction variables such as the type and amount of extraction solvent, pH and salt amount in the sample phase, and extraction time were optimized. The synthesis of supramolecular solvent was studied and its microstructure was characterized by transmission electron microscopy. Under the optimal conditions, the analytes’ enrichment factors were between 6 and 170 for the proposed procedure. Satisfactory linear ranges ( r ≥ 0.99), detection limits (0.025–0.4 ng/ml), precisions (< 9.2%), and accuracies (recoveries: 96.5%–104.8%) were obtained. The method has been successfully applied to the preconcentration of lignans in Forsythiae Fructus with simple and rapid operation, low cost, and environmental friendliness.
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PHYTOTHERAPY RESEARCH
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2023
·Vol. 37
·期 4
·1422-1434
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IF 7.2
Yanfei Ban,Yang Wang,Liming Qiao,Chengzhong Zhang,Hongrui Wang,Xuhui He,Dan Jia,Chengjian Zheng
The seeds of Vitex negundo have been used for inflammation-related disease treatment in traditional medicine. This study focused on the anti-osteoarthritis (OA) effects of the total lignans of V. negundo seeds (TOV) in monosodium iodoacetate-induced osteoarthritis rats and its pharmacokinetic properties, as well as the effects and potential mechanism of its main components VN1 (6-hydroxy-4-(4-hydroxy-3-methoxy-phenyl)-3-hydro-xymethyl-7-methoxy-3,4-dihydro-2-naphthaldehydeb) and VN2 (vitedoin A) on receptor activator of NF-κB ligand (RANKL)-induced osteoclast differentiation in bone marrow macrophages (BMMs). TOV significantly attenuated osteoarthritis, leading to an increase in pain thresholds, improvement of knee articular cartilages and chondrocytes loss, and decreased total joint scores and serum levels of TNF-α, interleukin-1β (IL-1β), and prostaglandin E2 (PGE2) in osteoarthritis rats. The half-time (T 1/2 ) was 2.82 h and 1.33 h, and the bioavailability was 15.34%–21.89% and 16.29%–22.11%, for VN1 and VN2, respectively. VN2, rather than VN1, remarkably inhibited tartrate-resistant acid phosphatase (TRAP) activity, reduced the number of TRAP-positive multinuclear cells, diminished the formation of actin ring, and decreased mRNA levels of cathepsin K (CTSK), TRAP, nuclear factor of activated T cell 1 (NFATc1), and osteoclast-associated receptor, as well as downregulated protein levels of p-ERK (phosphorylated extracellular signal-regulated kinase), TRAP, CTSK and NFATc1 in BMMs. These findings suggest TOV has promising therapeutic potential for OA treatment and VN2, in particular, attenuates osteoclast differentiation by suppressing ERK/NFATc1 signaling and actin ring, mainly accounting for the anti-OA efficacy of TOV.
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Frontiers in Pharmacology
·
2022
·
IF 5.988
Jie Du,Xiaodong Chen,Yongshun Zhao,Tingting Zhao,Dalong Wang,Zujia Chen,Changyuan Wang,Qiang Meng,Jialin Yao,Huijun Sun,Kexin Liu,Jingjing Wu
CYP46A1 is a brain-specific enzyme responsible for cholesterol homeostasis. Inhibition of CYP46A1 activity serves as a therapeutic target for excitatory neurotoxicity. Sesame is a common medicine and food resource; its component lignans possess various pharmacological activities. In this study, the inhibitory effects of sesame lignans on CYP46A1 activity were investigated. Inhibition kinetics analyses revealed that sesamin and sesamolin produce mixed partial competitive inhibition of CYP46A1, while sesamol produces non-competitive inhibition. Notably, molecular simulations revealed that the sesame lignans have excellent orientations within the active cavity of CYP46A1. Importantly, the sesame lignans had high permeability coefficients and low efflux ratios. Furthermore, sesamin significantly reduced the levels of 24S-hydroxycholesterol in rat plasma and brain tissues, and down-regulated the protein expressions of CYP46A1, NMDAR2A, NMDAR2B, and HMGCR. Collectively, sesame lignans exhibit significant inhibitory effects on CYP46A1 activity, highlighting their potential therapeutic role in treating excitatory neurotoxicity.
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Frontiers in Pharmacology
·
2024
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IF 4.4
Zhang Jinpeng,Cui Xinyuan,Zhao Shuo,Chang Zenghui,Zhang Junshuo,Chen Yufeng,Liu Jiale,Sun Guohao,Wang Yiyuan,Liu Yuanyuan
Objective: Our previous studies substantiated that the biological activity of Schisandra chinensis lignans during the treatment of Alzheimer’s disease (AD) was mediated by neurotransmitter levels, and 15 of its active components were identified. However, the pharmacokinetic and pharmacodynamic relationship of Schisandra chinensis lignans has been less studied. The objective of this study was to investigate the relationship between the pharmacokinetics and pharmacodynamics of Schisandra chinensis lignans in the treatment of AD, and to establish a pharmacokinetic-pharmacodynamic (PK-PD) model.Methods and Results: Herein, we established a microdialysis-ultra performance liquid chromatography-triple quadruple mass spectrometry (MD-LC-TQ-MS) technique that could simultaneously and continuously collect and quantitatively analyze the active compounds and neurotransmitters related to the therapeutic effects of Schisandra chinensis in awake AD rats. Eight lignans were detected in the hippocampus, and a PK-PD model was established. The fitted curves highlighted a temporal lag between the maximum drug concentration and the peak drug effect. Following treatment, the levels of four neurotransmitters tended to converge with those observed in the sham operation group.Conclusion: By establishing a comprehensive concentration-time-effect relationship for Schisandra chinensis lignans in AD treatment, our study provides novel insights into the in vivo effects of these lignans in AD rats.
研究领域:
药理学
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神经科学
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分析化学
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Food & Function
·
2019
·Vol. 10
·期 9
·5656-5668
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IF 3.241
Mengying Wei,Zhongying Liu,Yuanyuan Liu,Shizhe Li,Mingxin Hu,Kexin Yue,Tianshu Liu,Yang He,Zifeng Pi,Zhiqiang Liu,Fengrui Song
Schisandra chinensis (Turcz.) Baill (S. chinensis), a functional food, is used as a tonic and sedative agent in traditional Chinese medicine. Modern pharmacological research has proved that S. chinensis could prevent and treat age-related neurodegenerative diseases. The presence of bioactive lignans in S. chinensis is the main reason for its neuroprotective and cognitive enhancement effects. This study aimed to clarify the mechanism of lignans in S. chinensis in ameliorating learning and memory deficits in Alzheimer's disease (AD) animals. The step-down test and Morris water maze (MWM) test were used to verify the effects of lignans in S. chinensis on learning and memory in AD animals. Then, metabolomics approaches based on ultraperformance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) were used to clarify the mechanism of lignans in S. chinensis in treating AD. Finally, quantitative analysis of AD-related neurotransmitters in the brain was conducted after treatment with lignans in S. chinensis. In the MWM and step-down tests, lignans in S. chinensis showed a clear ability to ameliorate the impaired learning and memory of AD animals. A total of 31 endogenous metabolites were identified after treatment with lignans in S. chinensis, which were associated with lignans ameliorating learning and memory. These biomarkers were mainly associated with polyunsaturated fatty acid metabolism and amino acid and vitamin metabolism. Moreover, lignans in S. chinensis upregulated the levels of γ-aminobutyric acid (GABA), 5-hydroxytryptamine (5-HT), acetylcholine (Ach), norepinephrine (NE) and glycine (Gly) and downregulate the level of aspartic acid (Asp). Lignans in S. chinensis might alleviate the neurotoxic effects of neurological inflammation and oxidative stress, Aβ deposition, and tau phosphorylation via the regulation of multiple endogenous metabolic pathways during pathological AD. The research might provide useful support for the further study of pharmacology and new drug development of lignans in S. chinensis.
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MOLECULES
·
2019
·Vol. 24
·期 7
·1203
·
IF 3.06
Mengying Wei,Yuanyuan Liu,Zifeng Pi,Shizhe Li,Mingxin Hu,Yang He,Kexin Yue,Tianshu Liu,Zhiqiang Liu,Fengrui Song,Zhongying Liu
Lignans fromSchisandra chinensis(Turcz.) Baill can ameliorate cognitive impairment in animals with Alzheimer’s disease (AD). However, the metabolism of absorbed ingredients and the potential targets of the lignans fromS. chinensisin animals with AD have not been systematically investigated. Therefore, for the first time, we performed an in-vivo ingredient analysis and implemented a target-network pharmacology strategy to assess the effects of lignans fromS. chinensisin rats with AD. Ten absorbed prototype constituents and 39 metabolites were identified or tentatively characterized in the plasma of dosed rats with AD using ultra high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry. Based on the results of analysis of the effective constituents in vivo, the potential therapeutic mechanism of the effective constituents in the rats with AD was investigated using a target-network pharmacology approach and independent experimental validation. The results showed that the treatment effects of lignans fromS. chinensison cognitive impairment might involve the regulation of amyloid precursor protein metabolism, neurofibrillary tangles, neurotransmitter metabolism, inflammatory response, and antioxidant system. Overall, we identified the effective components of lignans inS. chinensisthat can improve the cognitive impairment induced by AD and proposed potential therapeutic metabolic pathways. The results might serve as the basis for a fundamental strategy to explore effective therapeutic drugs to treat AD.Keywords:Alzheimer’s disease;lignan;metabolite identification;Schisandra chinensis;target-network pharmacology;UHPLC–Q-TOF-MS
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