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
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
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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
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药物筛选
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神经科学
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生物物理学
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DOI
PubMed
高影响因子
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
·
2025
·
IF 3.1
Liqing Wang,Menghan Chen,Hanxue Wang,Qihui Sun,Sujuan Zheng,Xiaoyun Liu,Yong Yang,Rong Rong
Clinical studies have demonstrated that many traditional Chinese medicines (TCM) exhibit not only antiviral effects but also efficacy in alleviating clinical symptoms of Coronavirus Disease 2019 (COVID-19). However, the pharmacologically active constituents responsible for their anti-COVID-19 efficacy remain unclear. This study aimed to establish a novel strategy for identifying active ingredients from herbs clinically used for COVID-19. An integrated approach combining data mining with Affinity Ultrafiltration (AUF) was developed. Initially, using a data mining strategy, high-frequency herbs were selected from the herbs clinically used in COVID-19. Furthermore, AUF technology was used to screen for potential bioactive components from the high-frequency herbs. The anti-COVID-19 potential of active compounds was assessed through enzyme activity assays and molecular docking, followed by validation in cellular and animal models. Data mining revealed that Glycyrrhiza uralensis Fisch., Lonicera japonica Thunb. and Forsythia suspensa (Thunb.) Vahl were the high-frequency herbs used in COVID-19. Five potential 3-Chymotrypsin-like protease (3CL pro ) inhibitors were screened from three herbs via AUF and identified using high-resolution mass spectrometry. Further enzymatic and cellular assays demonstrated that Licochalcone C (LCC) and Forsythiaside A (FTA) inhibited Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) replication at micromolar concentrations. Notably, FTA treatment significantly suppressed the elevation of pulmonary parameters and inflammatory mediators induced by SARS-CoV-2 nucleocapsid protein in mice. In summary, this study proposes a novel strategy integrating data mining with AUF to discover active compounds from TCM. Two components, LCC and FTA, were identified as dose-dependent inhibitors of SARS-CoV-2 Omicron strain replication in vitro.
研究领域:
药理学
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病毒学
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药物化学
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生物信息学
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植物学
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产品关联
DOI
PubMed
高影响因子
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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产品关联
DOI
PubMed
高影响因子
MOLECULES
·
2025
·Vol. 30
·期 5
·1187
·
IF 4.6
Sisi Pu,Yangyang Pan,Zuoyang Wang,Huimin Liu,Jianhui Zhang,Qian Zhang,Meng Wang
Overdose intake of acetaminophen (APAP) causes liver injury involving hepatic drug metabolism and activation of oxidative stress pathways, and forsythiaside A (FA) has hepatoprotective pharmacological activity, but knowledge of the mechanism of FA treatment for APAP liver injury is still lacking the literature. In this study, we investigated the effects of FA on the pregnane X receptor (PXR) by molecular docking and reporter gene assays. In addition, we explored the effects of FA on oxidative stress, endoplasmic reticulum stress (ERS), apoptosis, and hepatic pathology by interfering withPXRin ex vivo and in vivo models. The results showed that FA decreased thePXRprotein expression level and effectively reduced the oxidative stress level in the APAP model. In addition, FA reduced the expression of ERS pathway ProteinkinaseR-likeERkinase (PERK)-translation initiation factor 2 (eIF-2α)-activating transcription factor 4 (ATF4) by inhibitingPXR, and at the same time, decreased the expression of apoptotic proteins C/EBP homologous protein (CHOP), Bax, Caspase 3, and Caspase 7, and elevated the expression of apoptosis-suppressing protein Bcl-2, which ultimately treated the hepatic pathology injury of APAP in mice. The present study confirmed that FA improved APAP metabolism by inhibitingPXR-mediated CYP1A2 and CYP3A11 and alleviated APAP-induced hepatic impairment by inhibiting hepatic oxidative stress, ERS, and apoptosis.
研究领域:
药理学
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毒理学
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分子生物学
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肝病学
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产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACOLOGY
·
2017
·
IF 2.896
Xiaojuan Yan,Tinggui Chen,Liwei Zhang,Huizhi Du
Increasing the acetylcholine level and fighting the neuroinflammation has always been taken as a treatment strategy for Alzheimer's disease (AD). Forsythoside A is a major component in Forsythia suspensa (Thunb.) Vahl (F. suspensa, Lianqiao in Chinese) that has been traditionally used as Chinese herbal medicine to treat the inflammation in China. This study examined the inhibitory acetylcholinesterase activities of Forsythoside A at chemical and biological level. Forsythoside A inhibited acetylcholinesterase in a mixed type of inhibition, with Ki of 47.68 μM. Docking analysis strongly supported these findings. In PC12 cells Forsythoside A increased cell viability and suppressed acetylcholinesterase increased by Aβ 25-35 , thus alleviated the corresponding apoptosis . Taken together, these results suggest that Forsythoside A has the protective effects on Aβ 25-35 -induced apoptosis in PC12 cells by downregulating acetylcholinesterase, making it a potential functional food ingredient or drug candidate for the treatment of AD.
研究领域:
神经科学
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药理学
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中医药
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Linwei Yu,Xi Li,Tianyi Shi,Ning Li,Donge Zhang,Xikai Liu,Yushuo Xiao,Xinran Liu,Robert B. Petersen,Weikang Xue,Yanxun V. Yu,De-sheng Hu,Li Xu,Hong Chen,Ling Zheng,Kun Huang,Anlin Peng
Parkinson's disease (PD), a neurodegenerative disorder without cure, is characterized by the pathological aggregation of α-synuclein (α-Syn) in Lewy bodies. Classic deposition pathway and condensation pathway contribute to α-Syn aggregation, and liquid-liquid phase separation is the driving force for condensate formation, which subsequently undergo liquid-solid phase separation to form toxic fibrils. Traditional Chinese Medicine (TCM) has a long history in treating neurodegenerative disease; herein, we identified chemicals from herbs that inhibit α-Syn aggregation. We screened commonly prescribed TCMs for PD from the CNKI database and registered patents, 13 chemicals were identified in the TCMSP databases as candidate inhibitors, among which three phenols, forsythoside B (FTSB), echinacoside (ECH), and 4-hydroxyindole (C4-OH) efficiently inhibit α-Syn aggregation. Moreover, FTSB and ECH increase α-Syn fluidity within condensates, inhibit α-Syn transition into amyloid fibrils and reduce fibril-induced toxicity in SH-SY5Y cells. Importantly, they disaggregated preformed α-Syn amyloid fibrils. Notably, in an α-Syn overexpressing NL5901 C. elegans PD model, either FTSB or ECH treatment significantly extended the lifespan and improved the PD-like movement disorders, both in the preventive and therapeutic treatment approaches, by reducing toxic α-Syn inclusion formation and improving the fluidity of α-Syn. Together, we offer new therapeutic candidates targeting phase separation-associated aggregation for PD.
研究领域:
神经科学
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药理学
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分子生物学
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传统医学
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产品关联
DOI
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
·
绿色提取技术
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF MEDICINAL CHEMISTRY
·
2024
·
IF 6.8
Mengzhen Gu,Xiaoqing Xu,Xiaoping Wang,Yun Wang,Yu Zhao,Xiaoxian Hu,Lu Zhu,Zhenzhong Deng,Chao Han
Histone lysine-specific demethylase 1 (LSD1) is hyperactive in breast cancer, which is associated with the metastasis of the tumor. Current irreversible LSD1 inhibitors are all synthesized by covalently binding to the flavin adenine dinucleotide cofactor, which often have side effects due to the high affinity for a variety of targets. Here, we identified isoforsythiaside (IFA), a natural phenylpropanoid glycoside isolated from Forsythia suspensa, as a novel covalent inhibitor of LSD1. The target ligand fishing technique and LC–MS/MS analysis identified that IFA could covalently bind to the Ser817 residue of LSD1 by α,β-unsaturated ketone moiety to block the amine oxidase-like domain of LSD1. Moreover, RBMS3/Twist1/MMP2, the downstream signaling pathway of LSD1, was activated after IFA treatment to inhibit the metastasis of MDA-MB-231 cells in vitro and in vivo. This study provided novel molecular templates for development of LSD1 covalence-binding inhibitor and laid a foundation for developing agents against breast carcinoma metastasis for targeting LSD1.
研究领域:
癌症生物学
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药理学
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分子生物学
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生物化学
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产品关联
DOI
PubMed
高影响因子
Journal of Applied Spectroscopy
·
2022
·Vol. 89
·期 3
·559-566
·
IF 0.816
Gao Ch.,Du H.
Forsythoside E is one of the major secondary metabolites in Forsythia suspensa . The interactions between forsythoside E and two types of cholinesterases, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) were investigated in PBS buffer (pH 7.40) by using multispectroscopic techniques. Forsythoside E increased the fluorescence intensity of AChE but quenched the fluorescence of BChE. Synchronous fluorescence studies showed that forsythoside E mainly acts on tyrosine residues of AChE and tryptophan residues of BChE. It was also proved that the complex between the compound and cholinesterases formed spontaneously at a stoichiometric ratio of 1:1 via multispectral technology. Finally, forsythoside E inhibited the activities of cholinesterases with similar IC 50 values of 1.08 mM for AChE and 0.92 mM for BChE. The results illuminate the details of the interaction between forsythoside E and cholinesterases.
研究领域:
药理学
·
生物化学
·
分子生物学
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DOI
高影响因子
SEPARATION AND PURIFICATION TECHNOLOGY
·
2025
·
IF 9
Xin Li,Yushuai Jiang,Desheng Yang,Yun Li,Zhihui Zhao,Longyin Wan,Xiaoming Li,Weichao Chen
A biomass-derived poly (2,5-furan dicarboxylate propanediol-block-polyethylene glycol) (PTF-b-PEG) copolyester is synthesized through incorporating flexible polyethylene glycol (PEG) segments into the PTF polymer backbone and its basic properties are tested. Electrospun nanofiber membrane with PTF-b-PEG displays improved hydrophilicity, superior flexibility (elongation at break ∼287.35 %), but achieve only 86.6 % air filtration efficiency due to its large fiber diameters (1.71 μm). To address this limitation, forsythin (FT) is introduced to simultaneously modulate the fiber diameters and impart antibacterial properties. The FT-modified nanofiber membranes show narrower diameters according to the amount of FT (0.48 μm for FT 10 @PTF-b-PEG as an example) and excellent ultrafine particulate matter (PM) capture. The membrane can achieve an ultrafine particle filtration efficiency of 99.92 % at a pressure drop of 72 Pa, with a quality factor of 0.09 Pa −1 .The antibacterial activities against Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli) are 98.68 % and 99.76 %, respectively. Consequently, the FT-modified PTF-b-PEG membrane was used for the bioaerosol filtration, which not only intercepted but also killed the bacterial at the same time, thus avoiding any secondary contamination to the environment. The results indicate that the FT-modified PTF-b-PEG nanofiber membrane is a promising candidate for high-performance and antibacterial air purification.
研究领域:
材料科学
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高分子化学
·
环境工程
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纳米技术
·
生物医学工程
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产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）