JOURNAL OF ETHNOPHARMACOLOGY
·
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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DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR LIQUIDS
·
2026
·
IF 5.2
Conghuan Lin,Yan Ren,Liwei Zhang,Huizhi Du
One of the typical pathological features in Alzheimer's disease (AD) is Tau protein hyperphosphorylation. Here, by network pharmacology, 11 potential compounds of Forsythia suspensa (Thunb.) Vahl (FSTV) intervening AD was screened and AKT1, a critical enzyme involved in the Tau phosphorylation, was identified as a target of AD. Among, luteolin, phillyrin, and bicuculline, like the AKT1 agonist SC79, promoted AKT1 activity by binding to PH domain of AKT1, which was demonstrated by molecular docking. Even more, due to the slightly higher binding energy, three compounds bound to AKT1 better than the agonist, mainly through hydrogen bonding, etc. Spectral analysis showed that three compounds all bound with AKT1 to form complexes, and thus quenched the fluorescence of AKT1, with the more significant effects of luteolin and bicuculline on TYR residues of AKT1. Molecular dynamics simulations further indicated that the binding of these compounds to AKT1 occurred near the SER-473 active center of AKT1 and three complexes had relatively stable conformation. In a word, luteolin, phillyrin, and bicuculline from FSTV promoted AKT1 activity to reduce Tau protein hyperphosphorylation, and ultimately improved AD, with luteolin of the best performance.
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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
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中药学
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高分子化学
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DOI
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
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药理学
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天然产物研究
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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
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药理学
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DOI
高影响因子
PHYTOMEDICINE
·
2026
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IF 11.3
Guoguo Zhi,Haiyu Shen,Zihao Li,Manju Che,Lin Cheng,Zhirui Du,Xueqiao Yan,Shaoyang Zhang,Ruichen Yang,Xiuying Ma,Huijuan Liu,Funeng Geng,Baojie Li
Background Cutaneous wound repair is a complex biological process that restores the integrity of the skin. Forsythia suspensa (LQ) is a traditional Chinese medicinal herb known for its anti-inflammatory and antimicrobial properties; however, its role and molecular mechanisms in promoting cutaneous tissue regeneration remain unclear. Objective This study aimed to evaluate the pharmacological efficacy of LQ and its bioactive compounds in treating acute skin injuries and to elucidate the underlying molecular mechanisms. Method Two distinct animal models, a full-thickness thermal injury wound (complex inflammatory damage) and a full-thickness excisional wound (mechanical trauma), were established to evaluate the therapeutic potential of LQ. Therapeutic effects were assessed by histopathological examination and immunofluorescence analysis of skin lesions. RNA sequencing and pathway-specific inhibitors were used to investigate and validate the molecular mechanisms involved. Active compounds were identified by UPLC-MS/MS, and their mechanisms of action were explored using molecular docking, molecular dynamics simulation, and experimental validation. Results LQ significantly accelerates cutaneous wound healing in both models. Mechanistically, LQ promotes tissue regeneration by suppressing neutrophil extracellular trap (NET) formation and activating Wnt/β-catenin signaling to drive epidermal cell proliferation, and these effects are reversed by the NET inhibitor GSK484 and the Wnt pathway inhibitor IWP2. Forsythoside A, an active component of LQ, similarly enhances wound closure, re-epithelialization, and cell proliferation, indicating that it is likely the key mediator. We further show that inhibition of NETs increases Wnt ligand production and β-catenin signaling, linking inflammatory responses to regenerative signaling. Conclusion LQ and forsythoside A promote skin wound healing by coordinately regulating NET-mediated inflammation and Wnt/β-catenin signaling–mediated cell proliferation, thereby highlighting their potential as therapeutic agents in regenerative medicine.
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PubMed
高影响因子
JOURNAL OF SEPARATION SCIENCE
·
2026
·Vol. 49
·期 1
·e70344
·
IF 2.8
Yongli Liu,Chang Gao,Shiyu Li,Jie Gao,Nan Wang
Respiratory syncytial virus (RSV) imposes a substantial health burden, particularly among pediatric and elderly populations. The RSV fusion (F) protein, a critical mediator of viral entry and syncytium formation, represents a promising and rational target for antiviral drug development. Forsythia suspensa (Lianqiao in Chinese), a traditional Chinese medicinal herb, has been empirically employed for decades in the prevention of viral infections; however, its pharmacologically active constituents remain poorly characterized. The present investigation developed a high-expression F protein cell membrane chromatography system, and integrated with UHPLC-MS, to screen pharmacological substances from FS and verified the anti-viral potential against RSV in vivo. Our study pinpointed Forsythoside A, Forsythoside B, Phillygenin, and Phillyrin as potential anti-RSV compounds in FS. The research findings suggest that Forsythoside A, Forsythoside B, and Phillygenin exhibit considerable suppressive effects on cell fusion induced by RSV, concurrently effectively diminishing the expression level of the F protein gene. In contrast, the inhibitory impact of Phillyrin seems relatively less potent. In conclusion, our findings provide a convenient, fast, and accurate method to screen potential anti-RSV ingredients in natural herbal medicines. These results may facilitate the development of RSV treatment.
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PubMed
高影响因子
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
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DOI
PubMed
高影响因子
MICROCHEMICAL JOURNAL
·
2024
·
IF 4.9
Defeng Liu,Hongxiu Liu,Xiaomin Fu,Shujing Guo,Shengci Fan,Xinsheng Fang
Deep eutectic solvents (DESs) are showing broad application prospects in separation of bioactive components from natural products because of their eco-friendly advantages. In this study, a green method for effective extraction and reThe ultrasound-assisted extraction is optimized using Box-Behnken designcovery of three bioactive lignans from the leaves of Forsythia suspensa was developed for the first time using ultrasound-assisted deep eutectic solvents extraction (UAE-DES) and macroporous resin enrichment. Choline chloride-ethylene glycol (molar ratio of 1:3) with 20 % (v/v)water was confirmed as the optimal solvent. The optimized conditions were obtained by response surface methodology: liquid to solid ratio of 30 mL/g, extraction temperature of 30℃, ultrasound power of 200 W and extraction time of 30 min. The extraction yields of phillyrin, pinoresinol and phylligenin were 6.70, 9.65 and 45.77 mg/g, respectively, which were significantly higher than those of conventional organic solvents. Furthermore, the target compounds were recovered and purified from DES extracts using macroporous resin of HPD100. The recovery efficiency of phillyrin, pinoresinol and phylligenin was 87.9 %, 95.0 % and 91.7 %, respectively. After purification by the resin the content of phillyrin, pinoresinol and phylligenin in the recovered dry extract was 10.6 %, 12.8 %, and 64.8 %, respectively. This study provided an efficient and green approach for extraction and preparative separation of active lignans from natural products.
研究领域:
植物化学
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天然产物化学
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分离科学
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环境科学
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DOI
高影响因子
FITOTERAPIA
·
2022
·
IF 3.204
Fengtang Jing,Lei Wang,Min Yang,Chao Wu,Jian Li,Lei Shi,Shuai Feng,Feng Li
As a traditional Chinese medicine , Forsythia suspensa (F. suspensa) has attracted much attention due to its significant pharmacological activity . Revealing the spatial distribution of metabolites during F. suspensa development is important for understanding its biosynthesis rules and improving the quality of medicinal materials. However, there is currently a lack of information on the spatial distribution of F. suspensa metabolites. In this work, the spatial distribution and growth metabolism patterns of important metabolites of F. suspensa were studied for the first time using matrix-assisted laser desorption/ionization mass spectrometry imaging (MALDI-MSI). Using 2,5-dimethylnaphthalene (DAN) as the matrix and detecting in negative ion mode, the spatial distribution and growth patterns of 11 metabolites obtained from longitudinal sections of F. suspensa included pinoresinol , phillygenin, forsythoside A, forsythoside E, rutin , caffeic acid , malic acid , citric acid, stearic acid , oleic acid , and linoleic acid . These results showed the mesocarp and endosperm tissues of F. suspensa were important for storing important functional metabolites. Changes in mesocarp and endosperm growth and development tissues caused large changes in the content of important functional metabolites in F. suspensa . These results provide a basis for understanding the spatial distribution of metabolites in F. suspensa tissues and the significant changes that occur during growth and development, exploring the mechanism of important synthesis of metabolites, regulating the harvest of F. suspensa , and improving the quality of medicinal herbs.
研究领域:
中药学
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植物代谢组学
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DOI
PubMed
高影响因子
JOURNAL OF FOOD BIOCHEMISTRY
·
2022
·Vol. 46
·期 12
·e14460
·
IF 3.654
Jing Guo,Jian-Kai Tang,Bai-Fang Wang,Wen-Rui Yan,Ting Li,Xue-Jian Guo,Lei Zhang,Tao Wang,Qian-Yun Sun,Li-Wei Zhang
Forsythia suspensa (Thunb.) Vahl (Oleaceae) leaves are valuable sources of phillygenin. This study aimed to isolate phillygenin from F. suspensa leaves and examine its analgesic and anti-inflammatory effects. Phillygenin was successfully extracted and isolated from F. suspensa leaves after fermentation. Phillygenin significantly reduced the number of writhing induced by acetic acid, prolonged the latency period in the hot plate test, and inhibited the xylene-induced ear edema and carrageenan-induced paw edema in mice. IL-6, TNF-α, IL-1β, NO, and PGE 2 levels in the carrageenan-induced paw edema were notably reduced after pretreatment with phillygenin. Phillygenin significantly decreased the iNOS and COX-2 protein expressions and the IκB-α and NF-κB p65 phosphorylation. This study demonstrated that phillygenin is a potential therapeutic candidate for managing pain and inflammation-mediated disorders. The study contributes to the comprehensive development and utilization of F. suspensa leaves for economic and health care. Practical applications Phillygenin is one of the major active ingredients in Forsythia suspensa . But the content of phillygenin in F. suspensa is very low which limits its application. Phillygenin has potential pharmacological activity and anti-inflammatory properties. However, the potential effects of phillygenin on analgesic activity have not been clarified. Furthermore, the data on its anti-inflammatory activity in vivo are relatively limited. This study evaluated the analgesic activity for the first time and the acute anti-inflammatory effect of phillygenin from F. suspensa leaves by fermentation, which indicated phillygenin is a potential therapeutic candidate for managing pain and inflammation-mediated disorders.
研究领域:
药理学
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炎症
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疼痛管理
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天然产物
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传统中药
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产品关联
DOI
PubMed
高影响因子
Journal of Integrative Plant Biology
·
2026
·
IF 12.5
Zhiyao Wang,Naichao Zhang,Peimin Wu,Fei Chen,Ying Cao,Jing Wang,Yiming Qin,Wenhui Zheng,Yinghua Sheng,Shuai Chen,Baojing Li,Lei Wei,Junli Zhang,Yuqing Liu,Ninghua Tan,Wei Wang,Min Chen
Phillyrin, a unique antiviral lignan exclusive to Forsythia suspensa , shows potent anti-influenza activity. However, its broad pharmaceutical application is hindered by low and variable natural accumulation, underscoring the need to elucidate its biosynthetic pathway for sustainable production. In this study, we used an integrated metabolomic and transcriptomic approach to investigate tissue-specific phillyrin biosynthesis in F. suspensa . We identified two O -methyltransferases (FsE4MT01 and FsE4MT02) that catalyze the methylation of (+)-epipinoresinol to form phillygenin and a UDP-glycosyltransferase (FsP4′GT) that glucosylates phillygenin to yield phillyrin. Using recombinant proteins expressed in Escherichia coli , we validated their in vitro catalytic activities and determined their kinetic parameters. Molecular docking and site-directed mutagenesis of key residues further revealed the structural basis of their catalytic mechanisms. The in vivo functions of these enzymes were confirmed through heterologous expression in Nicotiana benthamiana and F. suspensa leaves. Importantly, by developing a transient leaf-expression system in F. suspensa , we demonstrated that overexpression of FsE4MTs and FsP4′GT substantially increased the production of phillygenin and phillyrin, respectively, whereas virus-induced gene silencing (VIGS) of these genes reduced the accumulation of the corresponding products. Notably, enhanced phillyrin production was also achieved by expressing FsE4MTs and FsP4′GT in the related species Forsythia × intermedia , highlighting the potential of these key enzymes for metabolic engineering. Our findings elucidate the terminal steps of phillyrin biosynthesis and provide a strategic foundation for engineering the sustainable production of this pharmaceutically valuable compound.
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高影响因子
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