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Anti-psoriasis molecular targets and active components discovery of Optimized Yinxieling Formula via affinity-purified strategy

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Chinese Journal of Natural Medicines 2024年第2期22卷 127-136页

作者： WANG Wei LIU Lijuan YANG Zhuo LU Chuanjian TU Pengfei ZHAO Ruizhi zeng kewu State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking UniversityBeijing 100191China State Key Laboratory of Dampness Syndrome of Chinese Medicine The Second Affiliated Hospital of Guangzhou University of Chinese MedicineGuangzhou 510006China

Psoriasis,a prevalent inherited skin condition,involves an inflammatory response as a key pathogenic *** Optimized Yinxieling Formula(OYF),rooted in traditional Chinese medicine,is extensively utilized in clinical settings to treat *** previous studies have demonstrated OYF’s significant anti-inflammatory effects in psoriasis,its potential molecular targets and active components remain *** study aimed to unveil the anti-psoriasis molecular targets and active components of *** findings indicated that OYF extract markedly reduced the production of several inflammatory mediators,including IL-23,nitric oxide,TNF-α,and IL-1β,in LPS-induced RAW264.7 *** synthesized OYF extract-crosslinked beads to isolate pharmacological targets from RAW264.7 lysates using an affinity purification strategy,known as Target *** enriched target proteins were subsequently identified via LC-MS/MS,followed by bioinformatics analysis to map the psoriasis-associated pathway-gene *** identified a total of 76 potential target proteins,which were highly associated with mRNA transcription *** particular,pathway-gene network analysis revealed that the IL-23 inflammatory pathway was involved in the anti-psoriasis effect of OYF *** further utilized a target protein-based affinity capture strategy,combined with LC-MS and SPR analysis,to globally screen OYF’s active components,focusing on the mRNA transcription regulator,fused in sarcoma(FUS).This process led to the identification of umbelliferone,vanillic acid,protocatechuic acid,gentisic acid,and echinacoside as key compounds targeting FUS to inhibit IL-23 ***,we formulated a compound cocktail(CpdC),which significantly reduced psoriasis area and severity index(PASI)scores and the expressions of IL-23 and Ki67 in an imiquimod(IMQ)-induced psoriasis mouse ***,our study elucidates the primary molecular targets and active components of OYF,offeri

关键词： Psoriasis Optimized Yinxieling Formula(OYF) FUS protein Molecular targets Affinity-purified strategy

Schisandrol A protects AGEs-induced neuronal cells death by allosterically targeting ATP6V0d1 subunit of V-ATPase

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Acta Pharmaceutica Sinica B 2022年第10期12卷 3843-3860页

作者： Xiaoqing Zhou Shaoyang Zhao Tingting Liu Lu Yao Meimei Zhao Xiaoming Ye Xiaowen Zhang Qiang Guo Pengfei Tu kewu zeng State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking UniversityBeijing 100191China

Diabetes have been shown to cause progressive neuronal injury with pain and numbness via advanced glycation end-products(AGEs)-induced neuronal cell apoptosis;however, the valuable drug targets for diabetic neuropathy have been poorly reported so far. In this study, we discovered a natural small-molecule schisandrol A(SolA) with significant protective effect against AGEs-induced neuronal cell apoptosis. ATP6V0D1, a major subunit of vacuolar-type ATPase(V-ATPase) in lysosome was identified as a crucial cellular target of SolA. Moreover, SolA allosterically mediated ATP6V0D1 conformation via targeting a unique cysteine 335 residue to activate V-ATPase-dependent lysosomal ***, SolA-induced lysosome pH downregulation resulted in a mitochondrial-lysosomal crosstalk by selectively promoting mitochondrial BH3-only protein BIM degradation, thereby preserving mitochondrial homeostasis and neuronal cells survival. Collectively, our findings reveal ATP6V0D1 is a valuable pharmacological target for diabetes-associated neuronal injury via controlling lysosomal acidification, and also provide the first small-molecule template allosterically activating V-ATPase for preventing diabetic neuropathy.

关键词： Allosteric regulation Advanced glycation endproducts AGEs Lysosomal acidification Targets V-ATPase ATP6V0D1 Schisandrol A Diabetic neuropathy

Pharmacologically targeting molecular motor promotes mitochondrial fission for anti-cancer

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Acta Pharmaceutica Sinica B 2021年第7期11卷 1853-1866页

作者： Yi Qian Meimei Zhao Qinghua Han Jingkang Wang Lixi Liao Heng Yang Dan Liu Pengfei Tu Hong Liang kewu zeng State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking UniversityBeijing 100191China Proteomics Laboratory Medical and Healthy Analytical CenterPeking University Health Science CenterBeijing 100191China

Mitochondrial shape rapidly changes by dynamic balance of fusion and fission to adjust to constantly changing energy demands of cancer *** dynamics balance is exactly regulated by molecular motor consisted of myosin and actin cytoskeleton ***,targeting myosin eactin molecular motor is considered as a promising strategy for *** this study,we performed a proof-of-concept study with a natural-derived small-molecule J13 to test the feasibility of anti-cancer therapeutics via pharmacologically targeting molecular ***,we found J13 could directly target myosin-9(MYH9)eactin molecular motor to promote mitochondrial fission progression,and markedly inhibited cancer cells survival,proliferation and *** study revealed that J13 impaired MYH9 eactin interaction to inactivate molecular motor,and caused a cytoskeleton-dependent mitochondrial dynamics ***,stable isotope labeling with amino acids in cell culture(SILAC)technology-coupled with pulldown analysis identified HSPA9 as a crucial adaptor protein connecting MYH9 eactin molecular motor to mitochondrial *** together,we reported the first natural small-molecule directly targeting MYH9 eactin molecular motor for anti-cancer translational ***,our study also proved the conceptual practicability of pharmacologically disrupting mitochondrial fission/fusion dynamics in human cancer therapy.

关键词： Anti-cancer Liver hepatocellular carcinoma Mitochondrial fission Small molecule Target identification Molecular motor MYH9 HSPA9

Enhanced optical imaging and fluorescent labeling for visualizing drug molecules within living organisms

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Acta Pharmaceutica Sinica B 2024年第6期14卷 2428-2446页

作者： Ting Sun Huanxin Zhao Luyao Hu Xintian Shao Zhiyuan Lu Yuli Wang Peixue Ling Yubo Li kewu zeng Qixin Chen School of Pharmaceutical Sciences National Key Laboratory of Advanced Drug Delivery SystemMedical Science and Technology Innovation CenterShandong First Medical University&Shandong Academy of Medical SciencesJinan 250062China Departments of Diagnostic Radiology SurgeryChemical and Biomolecular Engineeringand Biomedical EngineeringYong Loo Lin School of Medicine and College of Design and EngineeringNational University of SingaporeSingapore 119074Singapore Institute of Biochemical and Biotechnological Drugs School of Pharmaceutical SciencesCheeloo College of MedicineShandong UniversityJinan 250012China Key Laboratory of Biopharmaceuticals Postdoctoral Scientific Research WorkstationShandong Academy of Pharmaceutical ScienceJinan 250098China State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking UniversityBeijing 100191China School of Life Sciences Science and Technology Innovation CenterShandong First Medical University&Shandong Academy of Medical SciencesJinan 250062China School of Chinese Materia Medica Tianjin University of Traditional Chinese MedicineTianjin 301617China Tianjin Pharmaceutical DA REN TANG Group Corporation Limited Traditional Chinese Pharmacy Research Institute Tianjin 300457China Key Laboratory of Systems Bioengineering(Ministry of Education) School of Chemistry Engineering and TechnologyTianjin UniversityTianjin 300072China

The visualization of drugs in living systems has become key techniques in modern *** advancements in optical imaging technologies and molecular design strategies have revolutionized drug *** the subcellular level,super-resolution microscopy has allowed exploration of the molecular landscape within individual cells and the cellular response to *** beyond subcellular imaging,researchers have integrated multiple modes,like optical near-infrared II imaging,to study the complex spatiotemporal interactions between drugs and their *** combining these visualization approaches,researchers gain supplementary information on physiological parameters,metabolic activity,and tissue composition,leading to a comprehensive understanding of drug *** review focuses on cutting-edge technologies in drug visualization,particularly fluorescence imaging,and the main types of fluorescent molecules ***,we discuss current challenges and prospects in targeted drug research,emphasizing the importance of multidisciplinary cooperation in advancing drug *** the integration of advanced imaging technology and molecular design,drug visualization has the potential to redefine our understanding of pharmacology,enabling the analysis of drug micro-dynamics in subcellular environments from new perspectives and deepening pharmacological research to the levels of the cell and organelles.

关键词： Optical imaging Drug visualization Fluorophore labeling Therapeutics

Allosteric regulation of protein 14-3-3ζ scaffold by small-molecule editing modulates histone H3 post-translational modifications

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Allosteric regulation of protein 14-3-3ζ scaffold by small-...

Natural Product Bufalin Blocks Hepatocellular Carcinoma Proliferation and Migration by Targeting Membrane Proteoglycan Syndecan-4

第十一届全国化学生物学学术会议

作者： Liu Yang zeng kewu Tu Pengfei State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking University

Histone post-translational modifications(PTMs) act in various biological processes such as transcriptional activation,chromosome packaging and DNA *** this study,we identified a natural small-molecule protosappanin A(PTA) with a specific binding capacity for 14-3-3ζ.Mechanism study reveals 14-3-3ζ dimerization is a key pre-requirement for histone H3 PTMs,which can be dynamically induced via an allosteric effect,resulting in a selective inhibition of 14-3-3ζ dimer with histone *** effect modulates histone H3 PTMs by exposing specific modification sites including acetylation,trimethylation,and phosphorylation,and reprograms gene transcription profiles for autophagy-lysosome function and endoplasmic reticulum stress.

关键词： Histone post-translational modifications 14-3-3ζ allosteric effect PTA

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Natural Product Bufalin Blocks Hepatocellular Carcinoma Prol...

Study on Chemical Constituents of Notopterygium incisum

第十一届全国化学生物学学术会议

作者： Heng Yang kewu zeng Pengfei Tu State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking University

Bufalin,a main components of traditional chinese medicine from toad venom,is widely used to treat a variety of cancers including hepatocellular *** the potential anti-hepatocellular carcinoma target and molecular mechanism of bufalin still remains unclear,which seriously hinders its clinical application and development. In this study,we investigate the effects and mechanisms of bufalin on inhibiting HepG2 cells migration and ***,we discover that bufalin could binding Syndecan-4 as a direct cellular target to prevent HepG2 cells proliferation,invasion and *** on quantitative proteomic with stable isotope labeling,we find that bufalin inhibited the proliferation and migration of HepG2 cells through regulating cell cycle,cell migration and expression of mitogen-activated protein kinase pathway-related ***,we reveal DDX23,a RNA helicase,as critical mediator of Syndecan-4 in regulating cell proliferation and migration signaling *** findings indicate that Syndecan-4 is a potential target for cancer treatment and provide insights into the pathogenesis of hepatocellular carcinoma.

关键词： bufalin hepatocellular carcinoma drug target Syndecan-4

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Study on Chemical Constituents of Notopterygium incisum

Developmentally Regulated Glucosylation of Bitter Triterpenoid in Cucumber by the UDP-Glucosyltransferase UGT73AM3

中国化学会第十一届全国天然有机化学学术会议

作者： Xikang Zheng kewu zeng Yong Jiang Pengfei Tu State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking University Health Science Center

＜正＞Qiang *** dried roots and rhizomes of Notopterygium incisium and Notopterygium *** used in traditional Chinese medicine for treating the common cold and inflammatory diseases such as rheumatoid arthritis and as ...

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Molecular Plant 2017年第7期10卷 1000-1003页

作者： Yang Zhong Xiaofeng Xue Zhiqiang Liu Yongshuo Ma kewu zeng Lida Han Jingjing Qi Dae-Kyun Ro Soren Bak Sanwen Huang Yuan Zhou Yi Shang Key Laboratory of Biology and Genetic Improvement of Horticultural Crops of the Ministry of Agriculture Sino-Dutch Joint Laboratory of Horticultural Genomics Institute of Vegetables and Flowers Chinese Academy of Agricultural Sciences Beijing 100081 China Agriculturat Genome Institute at Shenzhen Chinese Academy of Agricultural Science Shenzhen 518124 China Tongji School of Pharmacy Huazhong University of Science and Technology 13 Hangkong Road Wuhan 430030 China Institute of Apicuiture Research Chinese Academy of Agricultural Sciences Beijing 100093 China School of Life Science Shanxi University Taiyuan 030006 China School of Pharmaceutical Sciences Peking University Health Science Center Beijing 100191 China Biotechnology Research Institute Chinese Academy of Agricultural Sciences Beijing 100081 China College of Life Sciences Nanjing Agricultural University Nanjing 210095 China Department of Biological Sciences University of Calgary Calgary T2N 1N4 Canada Department of Plant and Environmental Sciences Copenhagen PlantScience Centre University of Copenhagen Copenhagen 1871 Denmark

Dear Editor,Plants have evolved great plasticity to adapt to external environments. A huge number of structurally diverse metabolites gener- ated through the glycosylation process is one potential mechanism that contr...

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Lignans and flavonoids from Artemisia brachyloba

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Journal of Chinese Pharmaceutical Sciences 2018年第6期27卷 429-435页

作者： Puming Zhang Chen Zhang kewu zeng Yong Jiang Pengfei Tu State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking University Health Science CenterBeijing 100191China

A phytochemical investigation on the aerial parts of Artemisia brachyloba led to the isolation of 13 compounds（1-13） for the first time, including eight lignans（1-8） and five flavonoids（9-13）. The structures of the isolated compounds were elucidated by analysis of the NMR spectroscopic data and comparison with the literature. The 1 H and 13 C NMR data of 1 were fully assigned for the first time by the 2 D NMR analysis. All the isolates were evaluated for their inhibitory effects on nitric oxide production in lipopolysaccharide-challenged BV-2 microglial cells.

关键词： Artemisia brachyloba Lignans Flavonoids NO