JOURNAL OF ETHNOPHARMACOLOGY
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2024
·
IF 4.8
Junjie Li,Yixu Wang,Jiawei Li,Sihan Xu,Shou Wang,Wenjuan Liu,Li Fu,Min Jiang,Gang Bai
Ethnopharmacological relevance Lian Qiao (LQ), the dried fruit of Forsythia suspensa (Thunb.) Vahl, is a well-documented traditional Chinese medicine known for its detoxifying and heat-clearing properties. Clinically, compounds containing LQ are widely used to treat thrombotic diseases, indicating that it may have antithrombotic effects. However, its exact mechanism of action remains unknown. Aim of the study This study aimed to verify the antithrombotic effect of LQ and further explore the material basis and target mechanism of its antithrombotic effect using various biological methods. Materials and methods An epinephrine-collagen-thrombin-induced mouse model of acute pulmonary embolism (APE) was established to study the effects of LQ on thrombus development. A UPLC/Q/TOF-MS screening and identification system based on the inhibition of platelet aggregation and Ca 2+ antagonism was established to determine the pharmacodynamic components of LQ that inhibit platelet activation. The inhibitory effect of active ingredients on platelet activation, and the determination of the target of their inhibitory effect on platelet activation have been studied using chemical proteomics. Furthermore, based on the structure and function of the target protein, a multidisciplinary approach was adopted to analyze the molecular mechanism of active ingredient binding to target proteins and to evaluate the effects of active ingredients on the downstream signaling pathways of target proteins. Results LQ showed significant anticoagulant effects in APE model mice. Phillyrin and phillygenin were the antiplatelet-activating components of LQ. PLCβ3 was identified as a target for inhibiting platelet activation by phillyrin and its metabolites. The mechanism underlying the effect involves phillyrin and its metabolites inhibiting PLCβ3 activity by blocking the binding of PLCβ3 to Gαq through non-covalently targeting the ASN260 of PLCβ3, thus inhibiting the downstream Gαq-PLCβ3-Ca 2+ signaling pathway, effectively hindering platelet activation and therefore playing an anticoagulant role. Conclusion This study not only proposes and validates the antithrombotic effect of LQ for the first time but also finds that phillyrin and phillygenin are the main pharmacological substances through which LQ exerts antithrombotic activity and reveals a novel mechanism by which they exert antiplatelet activity by directly targeting and inhibiting PLCβ3 activity. These findings significantly contribute to our understanding of the therapeutic potential of phillyrin and provide important clues for the discovery and development of new antiplatelet drugs.
研究领域:
药理学
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传统中药
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分子生物学
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生物化学
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血栓研究
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF FOOD SAFETY
·
2021
·Vol. 41
·期 4
·e12907
·
IF 1.953
Qin Zhang,Zhe Dong,Huizhi Du
Forsythoside A is used as the main chemical marker for quality control of Forsythia suspensa (Thunb.) Vahl ( F. suspensa , Lianqiao in Chinese) fruits and leaves. The hydrolysis of forsythoside A at high temperature and effects of deep eutectic solvents (DESs) on stability of forsythoside A were studied in the article. Forsythoside A, I, and H may be directly converted into each other at high temperature. With more heating time, they are gradually decomposed into smaller molecular compounds. High temperature, alkaline conditions, high humidity, the oxidant, and light drastically destroyed stability of forsythoside A, while acidic conditions and the antioxidant protected it. Compared with water and alcohol solvents, DESs improved effectively stability of forsythoside A due to the formation of hydrogen bonds between DESs and forsythoside A. Our research preliminarily uncovered the converting mechanism of forsythoside A and confirmed that DES improved the stability of forsythoside A.
研究领域:
药学化学
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分析化学
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天然产物
✓ 已验证
产品关联
DOI
高影响因子
Foods
·
2016
·Vol. 5
·期 4
·73
·
IF 0
Na Guo,Qing-Yan Gai,Jiao Jiao,Wei Wang,Yuan-Gang Zu,Yu-Jie Fu
Fructus forsythiaessential oil (FEO) with excellent antibacterial activity was rarely reported. The objective of the present study was to investigate the antibacterial activity and the antibacterial mechanism of FEO against two food-borne pathogenic bacteria,Escherichia coli(E. coli) andStaphylococcus aureus(S. aureus) in vitro. When treated FEO, the zones of inhibition (ZOI) ofE. coli(20.5 ± 0.25 mm) andS. aureus(24.3 ± 0.21 mm) were much larger than control (p< 0.05). The minimum inhibitory concentrations (MICs) of FEO were 3.13 mg/mL and 1.56 mg/mL forE. coliandS. aureus, respectively. The antibacterial mechanism of FEO againstE. coilwas due to the changes in permeability and integrity of cell membrane leading to the leakage of nucleic acids and proteins. With the superior antibacterial activity of FEO, the nano-encapsulation method has been applied in FEO. When compared to FEO and blank chitosan nanoparticles, FEO-loaded nanoparticles (chitosan to FEO of 1:1) can effectively inhibit the growth ofE. coilabove 90% at room temperature. It is necessary to consider that FEO and FEO-loaded nanoparticles will become promising antibacterial additives for food preservative, cosmetic, and pharmaceutical applications.Keywords:Forsythia suspense;Fructus forsythiaessential oil;chitosan nanoparticles;antibacterial activity;antibacterial mechanism
研究领域:
食品科学
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微生物学
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植物化学
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产品关联
DOI
PubMed
MOLECULES
·
2025
·Vol. 30
·期 17
·3528
·
IF 4.6
Teng Wang,Zexi Zhang,Jiayu Wang,Yuanyuan Fu,Xiaolin Zou,Wei Li,Zhaolun Zhang,Youting Liu,Zhaojun Jia,Zhenguo Wen,Yong Chen
In this study, a green and efficient extraction methodology was developed by leveraging the unique properties of chitosan—namely its non-toxicity, biocompatibility, and adhesive nature—to enhance the recovery of bioactive ingredients fromForsythia suspensaleaves. The core mechanism involves the formation of complexes between chitosan and the target bioactive ingredients, which significantly boosts their extraction efficiency. To substantiate this mechanism, comprehensive characterization was performed using Powder X-ray Diffraction (PXRD), Fourier Transform Infrared Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM), and molecular docking analyses. The results provided robust evidence of a strong interaction between chitosan and the bioactive ingredients, leading to a marked enhancement in both the stability and aqueous solubility of the target compounds. For process optimization, a multi-objective approach was implemented using the Non-dominated Sorting Genetic Algorithm II (NSGA-II) to simultaneously maximize the extraction yields of phillyrin and forsythoside A. The algorithm identified the optimal parameters as a leaf-to-chitosan mass ratio of 10:11.75, a solid-to-liquid ratio of 1:52 g/mL, a temperature of 80 °C, and a duration of 120 min. Under these optimized conditions, the corresponding extraction yields for phillyrin and forsythoside A were 1.68 ± 0.16% and 3.23 ± 0.27%, respectively. These findings collectively indicate that chitosan-assisted extraction represents a highly promising and advanced technology for the sustainable and effective extraction of bioactive ingredients from botanical sources.
研究领域:
植物学
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分析化学
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药用植物学
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绿色提取技术
✓ 已验证
产品关联
DOI
PubMed
高影响因子
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
·
2024
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IF 3.1
Duan Qiong,Li Ruochen,Wang Mingxiao,Cui Zhenting,Zhu Xia,Chen Fanghong,Han Feng,Ma Jianxin
Phillyrin (PHN), derived from the dried fruit of Forsythia suspensa (Thunb.) Vahl, is a kind of Chinese herbal medicine with the effect of clearing heat, and has been used in China for thousands of years in treating various tumors. However, the mechanism of its main components on non-small cell lung cancer (NSCLC) remains unclear. PHN is a distinct component extracted from Forsythia suspensa with promising anti-cancer activity against various tumor types. This study sought to elucidate the promising effects of PHN on NSCLC. Based on network pharmacology results, we identified potential PHN targets and pathways for NSCLC treatment. CCK-8 assay, wound healing assay, apoptosis assay, western blot, and in vivo experiments verified the inhibitory effect of PHN on NSCLC. Network pharmacology identified 160 potential PHN targets, 955 NSCLC-related targets, and 54 common targets, along with 132 pathways and 2 core genes. Biological experiments demonstrated that PHN significantly inhibited the growth and migration of A549 and LLC cells while promoting their apoptosis. Western blot analysis revealed down-regulation of AKT, HSP90AA1, and CDC37 expression, suggesting that PHN inhibits A549 and LLC cell proliferation by down-regulating the HSP90-AKT pathway. In vivo experiments confirmed that PHN significantly inhibited NSCLC growth with low toxicity. This study, using network pharmacology and biological experiments, verified the effectiveness of PHN against NSCLC through the HSP90-AKT pathway. These findings provide a foundation for further research and analysis.
研究领域:
肿瘤学
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药理学
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分子生物学
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中药学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Medicina-Lithuania
·
2022
·Vol. 58
·期 12
·1749
·
IF 2.948
Aoqi Song,Zhenghua Wu,Wenjuan Zhao,Wenqing Shi,Ru Cheng,Jingjing Jiang,Zhuojun Ni,Han Qu,Xijier Qiaolongbatu,Guorong Fan,Yuefen Lou
Background and Objectives:Hypericum perforatum(HP) is widely used for depressive therapy. Nevertheless, the antidepressant effect and potential mechanism of hyperoside (Hyp), the main active component of HP, have not been determined. Materials and Methods: We performed ultra-performance liquid chromatography–quadrupole-time-of-flight–tandem mass spectrometry (UPLC-Q-TOF-MS/MS) technology to analyze the components in HP. Using data mining and network pharmacology methods, combined with Cytoscape v3.7.1 and other software, the active components, drug-disease targets, and key pathways of HP in the treatment of depression were evaluated. Finally, the antidepressant effects of Hyp and the mechanism involved were verified in chronic-stress-induced mice. Results: We identified 12 compounds from HP. Hyp, isoquercetin, and quercetin are the main active components of HP. The Traditional Chinese Medicine Systems Pharmacology Database (TCMSP), the Analysis Platform, DrugBank, and other databases were analyzed using data mining, and the results show that the active components of HP and depression are linked to targets such as TNF-, IL-2, TLR4, and so on. A potential signaling pathway that was most relevant to the antidepressant effects of Hyp is the C-type lectin receptor signaling pathway. Furthermore, the antidepressant effects of Hyp were examined, and it is verified for the first time that Hyp significantly alleviated depressive-like behaviors in chronic-stress-induced mice, which may be mediated by inhibiting the NLRP1 inflammasome through the CXCL1/CXCR2/BDNF signaling pathway. Conclusion: Hyp is one of the main active components of HP, and Hyp has antidepressant effects through the NLRP1 inflammasome, which may be connected with the CXCL1/CXCR2/BDNF signaling pathway.Keywords:depression;NLRP1 inflammasome;Hypericum perforatum;hyperoside;CXCL1/CXCR2;BDNF
研究领域:
药理学
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神经科学
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分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
AMERICAN JOURNAL OF CHINESE MEDICINE
·
2025
·Vol. 53
·期 02
·543-566
·
IF 5.5
Jia-Yuan He,Fu-Lan Xiao,Qin-Yue Zheng,Chang-Hong Wang,Yi-Yue Tang,Jun-Xuan Fu,Jia-Yi Huang,Lian-Di Zhou,Qi-Hui Zhang
The intestinal absorption of active herbal constituents plays an important role in the biomedical efficacy of Traditional Chinese Medicine (TCM) formulations after oral administration. TCM compounds with low oral bioavailability can reach the distal intestine and then interact with intestinal flora, influencing the botanical pharmacological effects. In this study, in vitro digestion and an ex vivo Ussing chamber model were utilized to evaluate the intestinal absorption behavior of Forsythiae Fructus - Lonicerae Japonicae Flos -containing Yinqiao Jiedu Granule (YQJDG). It was found that the jejunum exhibited active absorption effects for some components of the formula, while the oral bioavailability of other herbal ingredients was low. Through further research using a combined UPLC-MS/MS and 16S rDNA sequencing technique, we studied the existence of the reciprocal interactions between YQJDG and gut microbiome. The in vitro fecal fermentation results showed that YQJDG significantly impacted the microbial community composition. The YQJDG markedly increased the abundance of beneficial microorganisms, such as Parabacteroides distasonis and Streptococcus gallolyticus subsp. Macedonicus, and suppressed the abundance of conditional pathogens including Prevotella steorerea, Haemophilus parainfluenzae , and Bacteroides . These effects may potentially contribute to the body’s immune functions and anti-inflammatory capacities. UPLC-MS/MS analysis suggested that the fecal microbiota chemically transformed constituents with low bioavailability to more readily absorbed potentially active metabolites. These findings provided valuable insights into the absorption characteristics of YQJDG and its interaction with the gut microbiome, further facilitating our understanding of precise pharmacological mechanisms of action of this Chinese herbal formulation.
研究领域:
中药学
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微生物学
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药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Biomass Conversion and Biorefinery
·
2023
·
IF 4
Weng Di,Tian RongRong,Jin HaiXin,Zha ShengHua,Zhao QingSheng,Zhao Bing
In this study, a method to enrich forsythiaside A (FA) from the ball-milled powder of Forsythia suspensa leaves was established. Forsythiaside A was extracted by heating and stirring, and the extraction process was optimized by response surface methodology using the independent variables of extraction temperature, extraction time, liquid-to-material ratio, ethanol concentration, and pH value of the solution, respectively. Then five types of macroporous resins with different polarities were studied to explain the adsorption mechanism by static adsorption and desorption experiments. Different models were used to study the static adsorption thermodynamics and kinetic process of AB-8 resin on FA extracts, and optimal conditions of the process were optimized. Finally, the antioxidant abilities of purified FA were evaluated. The results showed that the optimum extraction conditions were 2.2 h, 53.4 °C, 45.7 mL/g, 60% ethanol, and pH 6, and the extraction efficiency of forsythiaside A could achieve 120.96 mg/g. The AB-8 macroporous resin was the most suitable resin with high adsorption and desorption rates. It was found that the Temkin model was able to calculate the adsorption parameters accurately. The adsorption kinetic process of the resin was in accordance with the pseudo-second-order kinetic model. The optimal process conditions were as follows: the optimum loading concentration of 5.83 mg/mL, the loading rate of 1 BV/h, and the loading volume of 7.51 BV; in the desorption process, deionized water was used to remove impurities first, and then, 30% ethanol was used with an elution rate of 1 BV/h. The purity of FA increased from 20.52 to 81.58%. The purified FA exhibited superior scavenging ability for DPPH radicals and ABTS radicals. Cytotoxicity experiments proved that it was safe and nontoxic and was capable of promoting cell growth. In conclusion, the present study provides a theoretical basis for industrially extracting and purifying FA on a reliable basis.
研究领域:
植物化学
·
药理学
·
天然产物研究
✓ 已验证
产品关联
DOI
高影响因子
POWDER TECHNOLOGY
·
2022
·
IF 5.64
Di Weng,Sheng-Hua Zha,Yuan Zhu,Hang Li,Shou-Bu Hou,Qing-Sheng Zhao,Bing Zhao
Four powders of Forsythia suspensa leaf were prepared by coarse grinding and subsequent ball milling . The effects of particle size on the physicochemical and antioxidant properties of the powders were evaluated. The results showed that the particle size of the powder decreased from 107.99 to 29.20 μm by ball milling for 5 h. In addition, the ball-milled powders had substantial advantages in water holding, solubility and swelling capacities. Thus, the ball-milled powders had a better dissolution of phenolic, flavonoid , and polysaccharide components (25.45, 1.99 and 44.19 mg/g of powder for 5 h of ball milling), ultimately resulting in a superior antioxidant activity (maximum reductions of 14.96% and 19.20% for DPPH and ABTS radicals, respectively). The FTIR analysis showed that the structure of the active ingredients remained intact after ball milling. In conclusion, ball milling is a promising technique for preparing Forsythia suspensa leaf powder with improved physicochemical and biological properties.
研究领域:
植物学
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食品科学
·
药理学
✓ 已验证
产品关联
DOI
高影响因子
Scientific Reports
·
2020
·Vol. 10
·期 1
·1-10
·
IF 3.998
Ma Huiyan,Chen Yu,Chen Jinhui,Zhang Yunqiu,Zhang Tian,He He
Mikania micrantha and Ipomoea cairica are two invasive plants widely distribute and seriously damage in Hainan island. In this study, the leaves extracts of two weeds were collected and determined for their allelopathic potentials on Chrysanthemum coronarium . The phytotoxicity bioassay showed that when the extract concentration was 50 and 100 mg/ml, the inhibited effects of M. micrantha on growth of C. coronarium were greater than by I. cairica . However, when the extract concertation at 400 mg/ml, the opposite inhibited effects were observed. We speculated this phenomenon was caused by different allelopathic compounds. Therefore, using gas chromatography–mass spectrometry, 19 and 23 compounds were identified respectively, benzoic acid and cinnamic acid were the main components in the two leaves extracts, which were selected to carry out the further bioassays. Subsequent bioassay results showed the effects of two allelochemicals on morphological index and chlorophyll content and POD activity were all negative to C. coronarium , whereas the content of MDA and activity of SOD, CAT represented adverse changes. Moreover, the inhibitions by cinnamic acid were generally greater than those by benzoic acid. Thus, the phenolic acids played the most crucial roles in the allelopathic effccts of M. micrantha and I. cairica leaves extracts.
研究领域:
生态学
·
植物学
·
农学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF POLYMER RESEARCH
·
2022
·Vol. 29
·期 11
·1-10
·
IF 3.061
Sui Kun,Mei Fengce,Li Xiangyao,Wang Zifan,Wang Zhongwei,Han Yuxi,Yu Qing,Cheng Guiqing
Forsythia suspensa extract (FSE) obtained from traditional Chinese herbal medicine was employed as the stabilizer for polyethylene (PE). The effects of FSE on the thermos-oxidative stability, processing stability and mechanical properties of PE have been discussed through comparison of the performance of pure PE and modified PE samples on oxidation induction time (OIT), melt flow rate (MFR) and tensile tests. With the addition of FSE, the thermal oxidation stability of samples noticeably improved even after multiple extrusions: An OIT value of ca. 65.0 and 45.5 min could be achieved with PE-FSE 0.8 -626 sample after the first and fifth extrusions, which is extremely higher than pure PE. The improved antioxidant performance could be ascribed to the attractive free radical scavenging efficiency of FSE, confirmed by 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical–scavenging experiment. MFR results showed that FSE could effectively enhance the processing stability of PE matrix, the change of MFR after five extrusions was only 0.22 g/10 min for PE-FSE 0.8 -626 sample. Moreover, the tensile strength and elongation at break increased after the addition of FSE, which also maintained through the five extrusions. In addition, the cooperation of FSE and Ultranox 626 on the stability of PE was also explored. All results reveal that forsythia suspensa extract was good and multifunctional stabilizer for PE. This study opens up novel opportunities in utilizing traditional Chinese herbal medicine as natural antioxidants for the thermal oxidation stability of polyolefin, which is benefit for the development of sustainable and environmental friendly polymers.
研究领域:
材料科学
·
中药学
·
高分子化学
✓ 已验证
DOI
高影响因子
Communications Chemistry
·
2025
·Vol. 8
·期 1
·1-12
·
IF 6.2
Bai Si-Cong,Wang Ye-Cheng,Ye Wei-Lin,Wu Sheng-Yen,Jia Lee,Hong Liu,Xie Huan-Zhang,Li Gao
Abnormal amyloid beta (Aβ) aggregation is a key factor in Alzheimer’s disease (AD) pathology. Despite efforts to develop Aβ aggregation inhibitors, efficient screening strategies remain limited. Here, we initially applied structure-based virtual screening to target Aβ fibril ends, aiming to identify compounds that could effectively combat AD neurodegeneration. Using this approach, we screened a traditional Chinese medicine library with thousands of compounds, and selected high-scoring hits likely to inhibit fibril elongation or promote fibril depolymerization. Forsythoside A emerged as the most potent inhibitor, effectively reducing Aβ 40 aggregation and disassembling pre-formed fibrils, as confirmed through biophysical assays and surface plasmon resonance analysis. Chemical kinetics further elucidated its inhibitory mechanism. In Caenorhabditis elegans , forsythoside A alleviated Aβ-induced toxicity and extended the lifespan of the AD transgenic models. Further virtual screening and experimental validation using a CNS-penetrant compound library confirmed the robustness of our strategy. Our study underscores the effectiveness of virtual screening in the identification of Aβ aggregation inhibitors and emphasizes the critical significance of targeting fibril ends.
研究领域:
结构生物学
·
药物筛选
·
神经科学
·
生物物理学
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）