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Study on the mechanism of action of Glyasperin A in the Treatment of Atherosclerosis Based on Network Pharmacology and Molecular Docking

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Agricultural Biotechnology 2024年第2期13卷 53-57页

作者： Na LI Xiang PU Yihui CHAI Yuqi YANG Lailai LI Guizhou University of Traditional Chinese Medicine Guiyang 550025China

[Objectives] This study was conducted to investigate the mechanism of action of glyasperin A in the treatment of atherosclerosis using a network pharmacology approach. [Methods] Targets related to atherosclerosis were searched in GeneCards database. An active ingredient-disease-target network was constructed by Cytoscape 3.7.1. A target protein interaction network was constructed by String database. Gene Ontology (GO) enrichment analysis and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analysis were performed on the DAVID database. [Results] Glyasperin A acted on 36 atherosclerosis-related targets, and the biofunctional and pathway enrichment analyses showed that it was mainly involved in response to xenobiotic stimulus, drug transport across blood-brain barrier, lipid oxidation, barrier, and lipid oxidation, etc. The results showed that glyasperin A acted on 36 atherosclerosis-related targets. The biofunctional and pathway enrichment analyses showed that it was mainly involved in response to xenobiotic stimulus, drug transport across blood-brain barrier, lipid oxidation, positive regulation of protein localization to nucleus, and hepoxilin biosynthetic process, and it played an anti-fatigue role through signal pathways such as serotonergic synapse, efferocytosis, arachidonic acid metabolism, chemical carcinogenesis-receptor activation and platelet activation. [Conclusions] Glyasperin A has multi-target and multi-pathway effects in the treatment of atherosclerosis. This study provides reference for further research on glyasperin A in the treatment of atherosclerosis.

关键词： Glyasperin A Atherosclerosis Network pharmacology mechanism of action

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Naphthalimides and analogues as antitumor agents:A review on molecular design, bioactivity and mechanism of action

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Chinese Chemical Letters 2018年第12期29卷 1741-1756页

作者： Zhuo Chen Yufang Xu Xuhong Qian State Key Laboratory of Bioreactor Engineering Shanghai Key Laboratory of Chemical BiologyShanghai Key Laboratory of New Drug DesignSchool of PharmacyEast China University of Science and Technology

In this review, we retrospect our progress in biological active naphthalimide and analogues as antitumor agents in the past 20 years. On one hand, various derivations in naphthalimide pharmacophores were developed to enhance their DNA binding affinity and antitumor property thereby. Heterocyclic fused naphthalimides, bis-naphthalimides, non-fused substituted naphthalimides and the carboxamide derivatives were synthesized. For example, thio-heterocyclic fused-naphthalimides were designed and evaluated in comparison with their oxo-heterocyclic fused analogues. Extended or created heterocyclebased skeleton were also developed as antitumor agents. On the other hand, we broaden the design strategy of naphthalimide antitumor agents besides DNA intercalation and topo II poison. We have introduced more drug design methods, such as prodrugs, multitarget drugs, computer-aided drug design,photodynamic therapy. For example, we have got naphthalimide derivatives which inhibited topo II and induced LMP by introducing long alkyl chain and polyamines. Several representative compounds were clarified of their antitumor mechanism of action. In all, our research improves the structure diversity of naphthalimide antitumor agents and distinct variances of antitumor targets and mechanism of action.

关键词： Naphthalimides Antitumor Structure activity relationship Drug design strategy mechanism of action

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Antimicrobial peptides: mechanism of action, activity and clinical potential

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Military Medical Research 2022年第2期9卷 231-258页

作者： Qi-Yu Zhang Zhi-Bin Yan Yue-Ming Meng Xiang-Yu Hong Gang Shao Jun-Jie Ma Xu-Rui Cheng Jun Liu Jian Kang Cai-Yun Fu Zhejiang Provincial Key Laboratory of Silkworm Bioreactor and Biomedicine College of Life Sciences and MedicineZhejiang Sci-Tech UniversityNo.928Street 2Xiasha Higher Education ZoneHangzhou 310018China Department of Oncology The 903rd Hospital of PLAHangzhou 310013China Department of Pharmaceutical Chemistry and the Cardiovascular Research Institute University of California San Francisco555 Mission Bay Blvd.SouthSan FranciscoCA 94158USA Oncogenic Signaling and Growth Control Program Peter MacCallum Cancer Centre305 Grattan StreetMelbourneVIC 3000Australia Sir Peter MacCallum Department of Oncology University of MelbourneParkvilleVIC 3010Australia

The management of bacterial infections is becoming a major clinical challenge due to the rapid evolution of antibiotic resistant *** an excellent candidate to overcome antibiotic resistance,antimicrobial peptides(AMPs)that are produced from the synthetic and natural sources demonstrate a broad-spectrum antimicrobial activity with the high specificity and low *** peptides possess distinctive structures and functions by employing sophisticated mechanisms of *** comprehensive review provides a broad overview of AMPs from the origin,structural characteristics,mechanisms of action,biological activities to clinical *** finally discuss the strategies to optimize and develop AMP-based treatment as the potential antimicrobial and anticancer therapeutics.

关键词： Antimicrobial peptides Antimicrobial resistance mechanism of action Biological activity Clinical application

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A Lindqvist-type [W_(6)O_(19)]^(2-) organic–inorganic compound: synthesis, characterization, antibacterial activity and preliminary studies on the mechanism of action

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Tungsten 2022年第2期4卷 121-129页

作者： Meng Zhao Xi-Yu Zhu Yan-Zhen Li Jiang-Nan Chang Ming-Xue Li Li-Hua Ma Xiao-Yuan Guo Henan Key Laboratory of Polyoxometalate Chemistry Institute of Molecular and Crystal EngineeringSchool of Chemistry and Chemical EngineeringHenan UniversityKaifeng475004China Agricultural Products’Quality and Safety Testing Center of Kaifeng Kaifeng Agriculture and Rural BureauHenan475004China

In this paper,a new organic–inorganic hybrid compound[Co(L)_(2)]2[W_(6)O_(19)](1)(HL=2-acetylpyridine thiosemicarbazone)was prepared and *** compound 1 exhibits remarkable antibacterial activity by determination of minimum inhibitory concentration(MIC)against Staphylococcus aureus(***,0.06μg·mL^(−1))and Escherichia coli(***,0.24μg·mL^(−1)),***,the potential mechanism of compound 1 was studied in *** potential causes of bacteria death were cell wall/membrane disruption,inhibition of intracellular respiratory chain dehydrogenases(RCD)activity,destruction of reactive oxygen species(ROS)and depletion of glutathione(GSH).

关键词： Isopolytungstate Thiosemicarbazone Bioactivity mechanism of action

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Research Progress on mechanism of action of Radix Astragalus in the Treatment of Heart Failure

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Chinese Journal of Integrative Medicine 2012年第3期18卷 235-240页

作者：杨庆有陈可冀陆曙孙慧茹 Department of Cardiovascular Diseases Wuxi Municipal Hospital of Traditional Chinese Medicien Xiyuan Hospital China Academy of Chinese Medical Sciences

This paper reviewed the retrieved literature published in the last 10 years,regarding the mechanism of Radix Astragalus in treating heart failure,in aspects of myocardial contraction improvement, cardiac muscle cell protection,neuro-endocrinal system regulation,relative cytokine regulation,and left ventricular remodeling inhibition,etc.

关键词： Radix Astragalus heart failure mechanism of action review

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Naturally derived anti-hepatitis B virus agents and their mechanism of action

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World Journal of Gastroenterology 2016年第1期22卷 188-204页

作者： Yi-Hang Wu Zhejiang Provincial Key Laboratory of Biometrology and Inspection and Quarantine Department of PharmacyCollege of Life SciencesChina Jiliang University Department of Medicinal Chemistry and Molecular Pharmacology College of PharmacyPurdue University

Despite that some approved drugs and genetically engineered vaccines against hepatitis B virus(HBV)are available for HBV patients,HBV infection is still a severe public health problem in the *** the approved therapeutic drugs(including interferonalpha and nucleoside analogues)have their *** drugs or therapeutic methods can cure hepatitis B so ***,it is urgently needed to discover and develop new anti-HBV drugs,especially nonnucleoside *** originated compounds with enormous molecular complexity and diversity offer a great opportunity to find novel anti-HBV lead compounds with specific antiviral *** this review,the natural products against HBV are discussed according to their chemical classes such as terpenes,lignans,phenolic acids,polyphenols,lactones,alkaloids and ***,novel mode of action or new targets of some representative anti-HBV natural products are also *** aim of this review is to report new discoveries and updates pertaining to anti-HBV natural products in the last 20years,especially novel skeletons and mode of *** many natural products with various skeletons have been reported to exhibit potent anti-HBV effects to date,scarcely any of them are found in the list of conventional anti-HBV drugs ***,in anti-HBV mechanism of action,only a few references reported new targets or novel mode of action of antiHBV natural products.

关键词： Natural product Hepatitis B virus Structure mechanism of action Drug target

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Molecular basis and mechanism of action of Albizia julibrissin in depression treatment and clinical application of its formulae

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Chinese Herbal Medicines 2023年第2期15卷 201-213页

作者： Bishan Huang Yingyao Wu Chan Li Qingfa Tang Yuanwei Zhang School of Life Sciences Guangzhou UniversityGuangzhou 510006China School of Traditional Chinese Medicine Southern Medical UniversityGuangzhou 510515China

Albizzia julibrissin is empirically used as an antidepressant in clinical *** studies have indicated that its total extracts or bioactive constituents exerted antidepressant-like responses in animal models,providing the molecular basis to reveal its underlying mechanism of *** attempts have been made to understand the antidepressant effect of ***,many fundamental questions regarding its mechanism of action remain to be addressed at the molecular and systems *** this review,we conclusively discussed the mechanism of action of *** and *** formulae by reviewing recent preclinical and clinical studies conducted by using depressive animal models and depressive *** representative bioactive constituents and formulae were highlighted as examples,and their mechanisms of action were *** addition,some representative *** formulae that have been shown to be compatible with conventional antidepressants in clinical practice were also ***,we discussed the future research directions to reveal the underlying mechanism of *** at the molecular and systems levels in depression *** integrated study using both the molecular and systematic approaches is required not only for improving our understanding of its molecular basis and mechanisms of action,but also for providing a way to discover novel agents or approaches for the effective and systematic treatment of depression.

关键词： Albizia julibrissin Durazz. antidepressants depression mechanism of action clinical application

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Review on plant-derived bioactive peptides:biological activities,mechanism of action and utilizations in food development

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Journal of Future Foods 2022年第2期2卷 143-159页

作者： Hongxiu Fan Hongcheng Liu Yanrong Zhang Shanshan Zhang Tingting Liu Dawei Wang School of Food Science and Engineering Jilin Agricultural UniversityChangchun 130118China ScientifiResearch Base of Edible Mushroom Processing Technology Integration of Ministry of Agriculture and Rural Affairs Changchun 130118China Engineering Research Center of Grain Deep-processing and High-efficiency Utilization of Jilin Province Changchun 130118China Key Laboratory of Technological Innovations for Grain Deep-processing and High-efficiency Utilization of By-products of Jilin Province Changchun 130118China

Plant proteins are good alternative to animal sources in bioactive peptide production due to their safety,low-cost,rich resources and easy for large scale *** bioactivities of the peptides derived from plant proteins including antihypertensive,hypocholesterolemic,immunomodulatory,antioxidant,antimicrobial,anti-diabetic,opiate and hepatoprotective effect are being increasingly recognized with regards to health promoting and disease *** addition to bioactivities,the plant-derived bioactive peptides possess various functional properties including emulsifying and foaming properties,and water and oil retention capacities owning to the hydrophilic/lipophilic property,conformational flexibility and chain length of ***,the plant-derived bioactive peptides are promising ingredients for the development of health-care and functional *** review provides the research progress on the biological activities and functional properties of plant derived *** mechanism of action and structure-activity relationships of the bioactive peptide were also described,when ***,recent developments,major challenges and prospect in the application of the plant-derive bioactive peptides in the development of functional products are discussed and *** objective of this review is to improve the understanding of plant-derive bioactive peptides,and provide some constructive inspirations for further research and industrial application in the food and medicine industry.

关键词： Plant-derived bioactive peptides Biological activities mechanism of action Industrial application

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Anticancer Activities and mechanism of action of Nagilactones, a Group of Terpenoid Lactones Isolated from Podocarpus Species

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Natural Products and Bioprospecting 2020年第6期10卷 367-375页

作者： Christian Bailly OncoWitan 59290 Lille(Wasquehal)France

Nagilactones are tetracyclic natural products isolated from various Podocarpus *** lactone-based compounds display a range of pharmacological effects,including antifungal,anti-atherosclerosis,anti-inflammatory and anticancer activities reviewed *** most active derivatives,such as nagilactones C,E and F,exhibit potent anticancer activities against different cancer cell lines and tumor models.A comprehensive analysis of their mechanism of action indicates that their anticancer activity mainly derives from three complementary action:(i)a drug-induced inhibition of cell proliferation coupled with a cell cycle perturbation and induction of apoptosis,(ii)a blockade of the epithelial to mesenchymal cell transi-tion contributing to an inhibition of cancer cell migration and invasion and(iii)a capacity to modulate the PD-L1 immune *** molecular effectors have been implicated in the antitumor activity,chiefly the AP-1 pathway blocked upon activation of the JNK/c-Jun ***-C is a potent inhibitor of protein synthesis binding to eukaryotic ribosomes and inhibition of different protein kinases,such as RIOK2 and JAK2,has been postulated with *** literature survey on nagilactones highlights the therapeutic potential of these little-known *** mechanistic analysis also provides useful information for structurally related compounds(podolactones,oidiolactones,inumakilactones)isolated from Podo-carpus plants.

关键词： Cancer Natural products mechanism of action Molecular target Terpenoids

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Hinokiflavone and Related C-O-C-Type Biflavonoids as Anti-cancer Compounds:Properties and mechanism of action

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Natural Products and Bioprospecting 2021年第4期11卷 365-377页

作者： Jean-François Goossens Laurence Goossens Christian Bailly Univ.Lille CHU LilleEA 7365-GRITA-Groupe de Recherche sur les Formes Injectables et les Technologies Associées59000 LilleFrance OncoWitan 59290 Lille(Wasquehal)France

Biflavonoids are divided in two classes:C-C type compounds represented by the dimeric compound amentoflavone and C-O-C-type compounds typified by hinokiflavone(HNK)with an ether linkage between the two connected apigenin *** later sub-group of bisflavonyl ethers includes HNK,ochnaflavone,delicaflavone and a few other dimeric compounds,found in a variety of plants,notably Selaginella species.A comprehensive review of the anticancer properties and mechanism of action of HNK is provided,to highlight the anti-proliferative and anti-metastatic activities of HNK and derivatives,and HNK-containing plant *** anticancer effects rely on the capacity of HNK to interfere with the ERK1-2/p38/NFκB signaling pathway and the regulation of the expression of the matrix metalloproteinases MMP-2 and MMP-9(with a potential direct binding to MMP-9).In addition,HNK was found to function as a potent modulator of pre-mRNA splicing,inhibit-ing the SUMO-specific protease *** such,HNK represents a rare SENP1 inhibitor of natural origin and a scaffold to design synthetic *** formulations of HNK have been elaborated to enhance its solubility,to facilitate the compound delivery and to enhance its anticancer *** review shed light on the anticancer potential of C-O-C-type biflavonoids and specifically on the pharmacological profile of *** compound deserves further attention as a regu-lator of pre-mRNA splicing,useful to treat cancers(in particular hepatocellular carcinoma)and other human pathologies.

关键词： Hinokiflavone Biflavonoid Cancer therapy mechanism of action Natural product

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