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Combined inhibition of HDAC and DNMT1 induces p85α/MEKmediated cell cycle arrest by dual target inhibitor 208 in U937 cells

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Chinese Chemical Letters 2019年第6期30卷 1233-1236页

作者： Yue Ren Qinsheng Sun Zigao Yuan Yuyang Jiang Department of Chemistry Tsinghua University Beijing 100084 China state key laboratory of Chemical Oncogenomics Key Laboratory of Chemical Biology the Graduate School at Shenzhen Tsinghua University Shenzhen 518055 China National & Local United Engineering lab for Personalized Anti-tumor drugs Shenzhen Kivita Innovative Drug Discovery Institute the Graduate School at Shenzhen Tsinghua University Shenzhen 518055 China School of Life Science Tsinghua University Beijing 100084 China School of pharmaceutical Sciences Tsinghua University Beijing 100084 China

Multiple histone deacetylase inhibitors (HDACi) and DNA methyltransferase inhibitors (DNMTi) have been developed for cancer therapy. However, the research on their mechanisms of action is not sophisticated enough. In this study, we reported a dual HDAC and DNMT inhibitor 208 and found it induced G1 cell cycle arrest and apoptosis in U937 cells. Proteome and bioinformatic analyses revealed that the combined inhibition of DNMT1 and HDAC by 208 affected the expression of a series of proteins involved in many biological processes. We observed that several proteins associated with G1 cell cycle arrest and apoptosis were down regulated after 208 treatment, including p85α, MEK, and CDK4, suggesting that 208 induces cell cycle arrest and apoptosis through the p85α/MEK-mediated pathway in U937 cells. Moreover, biological function analysis showed that the combined epigenetic inhibition influenced various processes, including the synthesis and processing of RNA, translation, protein transport, and DNA repair. These findings provide novel insight into the potential mechanisms of multifunctional epigenetic inhibitors, which supports their further improvement and development.

关键词： Proteomics Epigenetic inhibitor HDAC DNMT1 Cell cycle arrest

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Determination of co-administrated opioids and benzodiazepines in urine using column-switching solid-phase extraction and liquid chromatography-tandem mass spectrometry

Determination of co-administrated opioids and benzodiazepine...

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2016年广东省药师周大会

作者： Lingjuan Xiong Rong Wang Chen Liang Xiaomei Teng Fengli Jiang Libo Zeng Haiying Ye Chunfang Ni Xiaoliang Yuan Yulan Rao Yurong Zhang Shanghai key laboratory of Crime Scene Evidence Shanghai Institute of Forensic Science state key laboratory of new drug and pharmaceutical process Shanghai Institute of Pharmaceutical Industry Pharmacy Department of Guangdong General Hospital Guangdong Academy of Medical Sciences Department of Forensic Medicine School of Basic Medical SciencesFudan University

Co-administration of opioids with benzodiazepines is very common around the world.A semi-automated method was developed for the determination of four opioids and two benzodiazepines as well as their metabolites(including glucuronide metabolites) in human urine,based on on-line column-switching-solid-phase extraction(CS-SPE) and liquid chromatography-tandem mass spectrometry(LC-MS/MS).The CS-SPE was performed by loading 200 μL of urine sample to an Oasis HLB *** was achieved using a LC-MS/MS system equipped with an electrospray ionization source(ESI).For unequivocal identification and confirmation,two selected reaction monitoring transitions were registered for each compound,and no co-elution of interferences was observed at the expected retention *** ion suppressions were observed for most analytes during chromatographic runs,but isotope-labeled internal standards(ISs) were used and found to be useful to compensate for the determination error caused by the matrix *** assay’s linearity ranged from 1-20 ng/m L to 800-1000 ng/m L for 23 compounds,except for lorazepam(LOR),whose linearity was in the range of 1-100 ng/m *** method showed to be precise and *** relative standard deviation(RSD) % values of within-run precision,between-run precision and total precision were not greater than 10.4%(n = 3),12.9%(n = 5) and 15.1%(n = 15),*** values were in the range of 87.5-110%.Limits of detection(LODs) ranged from 0.2 ng/m L to 5 ng/m L,and limits of quantification(LOQs) ranged from 1 ng/m L to 20 ng/m *** method was applied to the assay of 12 samples from forensic cases,which exemplified the co-administration of benzodiazepines(BZDs) by some heroin *** method was of high sensitivity,selectivity and reliability,minimum sample manipulation,semi-automation,and fairly high throughput(analysis time per sample was 20 min).The method developed will be useful for the detection of co-administrated drugs and t

关键词： opioids benzodiazepines co-administration glucuronide metabolites column-switching solid-phase extraction urine

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Automated and integrated ultrahigh throughput screening for industrial strain enabled by acoustic-droplet-ejection mass spectrometry

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Journal of pharmaceutical Analysis 2024年第9期14卷 1390-1392页

作者： Zhidan Zhang Chao Zhang Xu Zhang Jiuzhou Chen Ningyun Cai Shasha Zhong Zhibo Han Yan Zhu Ping Zheng Jibin Sun Changxiao Liu School of Pharmacy Shenyang Pharmaceutical UniversityShenyang117004China key laboratory of Engineering Biology for Low-Carbon Manufacturing Systems Biology CentreTechnical Support Core FacilitiesTianjin Institute of Industrial BiotechnologyChinese Academy of SciencesTianjin300308China Institute of Traditional Chinese Medicine University of Traditional Chinese MedicineTianjin301617China College of Biotechnology Tianjin University of Science and TechnologyTianjin300457China state key laboratory of drug Delivery and Pharmacokinetics Tianjin Institute of Pharmaceutical ResearchTianjin300301China

Synthetic biology provides unprecedented opportunities to tackle critical issues including climate change and sustainable development by constructing microbial cell factories to produce industrially valuable biochemicals,biofuels,and biomaterials using renewable biomass resources[1],where strain screening for specific metabolic traits is a critical ***,accurate,and simultaneous quantification of multiple metabolites is critical for multi-perspective strain performance evaluation and strain screening,and a generalized method or platform will also reduce method development time to speed up the screening process.

关键词： strain critical screening

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Super-sensitive bifunctional nanoprobe: Self-assembly of peptide-driven nanoparticles demonstrating tumor fluorescence imaging and therapy

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Acta Pharmaceutica Sinica B 2022年第3期12卷 1473-1486页

作者： Han Xiao Rui Zhang Xiaobo Fan Xinglu Jiang Mingyuan Zou Xuejiao Yan Haiping Hao Guoqiu Wu Medical School Southeast UniversityNanjing 210009China Department of Clinical laboratory the Fifth Affiliated Hospital of Sun Yat-sen UniversityNanjing 210009China Department of Cardiology the Affiliated Changzhou No.2 People’s Hospital of Nanjing Medical UniversityNanjing 210009China state key laboratory of Natural Medicines Key Lab of Drug Metabolism and PharmacokineticsChina Pharmaceutical UniversityZhuhai 519000China Center of Clinical laboratory Medicine Zhongda HospitalSoutheast UniversityNanjing 21009China Jiangsu Provincial key laboratory of Critical Care Medicine Southeast UniversityChangzhou 213000China

The development of nanomedicine has recently achieved several breakthroughs in the field of cancer treatment;however,biocompatibility and targeted penetration of these nanomaterials remain as limitations,which lead to serious side effects and significantly narrow the scope of their *** self-assembly of intermediate filaments with arginine-glycine-aspartate(RGD)peptide(RGDIFP)was triggered by the hydrophobic cationic molecule 7-amino actinomycin D(7-AAD)to synthesize a bifunctional nanoparticle that could serve as a fluorescent imaging probe to visualize tumor *** designed RGD-IFP peptide possessed the ability to encapsulate 7-AAD molecules through the formation of hydrogen bonds and hydrophobic interactions by a one-step *** fluorescent nanoprobe with RGD peptide could be targeted for delivery into tumor cells and released in acidic environments such as endosomes/lysosomes,ultimately inducing cytotoxicity by arresting tumor cell cycling with inserted *** is noteworthy that the RGD-IFP/7-AAD nanoprobe tail-vein injection approach demonstrated not only high tumor-targeted imaging potential,but also potent antitumor therapeutic effects in *** proposed strategy may be used in peptide-driven bifunctional nanoparticles for precise imaging and cancer therapy.

关键词： Nanoprobe 7-Amino actinomycin D Intermediate filament protein Tumor image Antitumor therapy Integrin avβ3

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Site-Selective Palladium-Catalyzed 1,1-Arylamination of Terminal Alkenes

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CCS Chemistry 2022年第2期4卷 616-624页

作者： Chunhua Han Libo Cai Dongquan Zhang Rui Pan Qiuyu Li Aijun Lin Hequan Yao state key laboratory of Natural Medicines(SKLNM) Department of Medicinal ChemistrySchool of PharmacyChina Pharmaceutical UniversityNanjing 210009

Many of the commonly used pharmaceuticals and biologically active natural products are nitrogencontaining ***,the transitionmetal-catalyzed or the radical-mediated 1,2-carboamination of alkenes has been well explored to access amine ***,synthetic strategies toward the 1,1-carboamination of alkenes are severely ***,we describe a method to achieve the 1,1-arylamination using readily available building blocks enabled by palladium *** sequential three step-Heck arylation,metal migration,followed by aza-1,6-Micheal addition process exhibits excellent chemo-and *** showcase the potential as a method for diversity-oriented drug discovery,the modification of numerous structurally complex bioactive molecules was also successfully performed.

关键词： alkene 1,1-arylamination palladium-catalyzed site-selective nitrogen-containing molecules

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Structure based release kinetics analysis of doxazosin mesylate sustained-release tablets using micro-computed tomography

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ASIAN JOURNAL OF pharmaceutical SCIENCES 2024年第6期19卷 100966页

作者： Liu, Qian Zan, Mengqing Huang, Hanhan Su, Hai Zhang, Wenjing Ma, Lingyun Zhang, Guangchao Zhang, Zunjian Zhang, Jiwen Niu, Jianzhao Xu, Mingdi Natl Inst Food & drug Control NMPA Key Lab Qual Res & Evaluat Chem Drugs Beijing 100050 Peoples R China China Pharmaceut Univ Nanjing 210009 Peoples R China Natl Inst Food & drug Control NMPA Key Lab Qual Res & Evaluat Pharmaceut Excipie Beijing 100050 Peoples R China Chinese Acad Sci Ctr Drug Delivery Syst Shanghai Inst Mat Med Shanghai 201203 Peoples R China

The structures of solid dosage forms determine their release behaviors and are critical attributes for the design and evaluation of the solid dosage forms. Here, the 3D structures of doxazosin mesylate sustained-release tablets were parallelly assessed by micro- computed tomography (micro-CT). There were no significant differences observed in the release profiles between the RLD and the generic formulation in the conventional dissolution, but the generic preparation released slightly faster in media with ethanol during an alcohol-induced dose-dumping test. With their 3D structures obtained via micro-CT determination, the unique release behaviors of both RLD and the generic were investigated to reveal the effects of internal fine structure on the release kinetics. The structural parameters for both preparations were similar in conventional dissolution test, while the dissolutions in ethanol media showed some distinctions between RLD and generic preparations due to their static and dynamic structures. Furthermore, the findings revealed that the presence of ethanol accelerated dissolution and induced changes in internal structure of both RLD and generic preparations. Moreover, structure parameters like volume and area of outer contour, remaining solid volume and cavity volume were not equivalent between the two formulations in 40 % ethanol. In conclusion, the structure data obtained from this study provided valuable insights into the diverse release behaviors observed in various modified-release formulations in drug development and quality control. (c) 2024 Shenyang pharmaceutical University. Published by Elsevier B.V. This is an open access article under the CC BY license (http://***/licenses/by/4.0/)

关键词： Doxazosin mesylate sustained-release tablets Osmotic pump tablets Micro-computed tomography Three-dimensional structures Ethanol

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Gut liver brain axis in diseases:the implications for therapeutic interventions

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Signal Transduction and Targeted Therapy 2024年第1期9卷 79-104页

作者： Mengyao Yan Shuli Man Benyue Sun Long Ma Lanping Guo Luqi Huang Wenyuan Gao state key laboratory of Food Nutrition and Safety Key Laboratory of Industrial MicrobiologyMinistry of EducationTianjin Key Laboratory of Industry MicrobiologyNational and Local United Engineering Lab of Metabolic Control Fermentation TechnologyChina International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal ChemistryCollege of BiotechnologyTianjin University of Science&Technology300457 TianjinChina National Resource Center for Chinese Materia Medica China Academy of Chinese Medical Sciences100700 BeijingChina Tianjin key laboratory for Modern drug Delivery&High-Efficiency School of Pharmaceutical Science and TechnologyTianjin UniversityWeijin Road300072 TianjinChina

Gut-liver-brain axis is a three-way highway of information interaction system among the gastrointestinal tract,liver,and nervous *** the past few decades,breakthrough progress has been made in the gut liver brain axis,mainly through understanding its formation mechanism and increasing treatment *** this review,we discuss various complex networks including barrier permeability,gut hormones,gut microbial metabolites,vagus nerve,neurotransmitters,immunity,brain toxic metabolites,β-amyloid(Aβ)metabolism,and epigenetic regulation in the gut-liver-brain *** therapies containing antibiotics,probiotics,prebiotics,synbiotics,fecal microbiota transplantation(FMT),polyphenols,low FODMAP diet and nanotechnology application regulate the gut liver brain ***,some special treatments targeting gut-liver axis include farnesoid X receptor(FXR)agonists,takeda G protein-coupled receptor 5(TGR5)agonists,glucagon-like peptide-1(GLP-1)receptor antagonists and fibroblast growth factor 19(FGF19)*** gut-brain axis embraces cognitive behavioral therapy(CBT),antidepressants and tryptophan metabolism-related *** liver-brain axis contains epigenetic regulation and Aβmetabolism-related *** the future,a better understanding of gut-liver-brain axis interactions will promote the development of novel preventative strategies and the discovery of precise therapeutic targets in multiple diseases.

关键词： metabolism therapeutic immunity

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Promising natural lysine specific demethylase 1 inhibitors for cancer treatment:advances and outlooks

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Chinese Journal of Natural Medicines 2022年第4期20卷 241-257页

作者： LI Zhong-Rui GU Meng-Zhen XU Xiao ZHANG Jing-Han ZHANG Hai-Li HAN Chao Department of Medicinal Chemistry School of PharmacyNanjing Medical UniversityNanjing 211166China state key laboratory of Natural Medicines Jiangsu Key Laboratory of Bioactive Natural Product ResearchSchool of Traditional Chinese PharmacyChina Pharmaceutical UniversityNanjing 210009China

Lysine specific demethylase 1(LSD1),a transcriptional corepressor or coactivator that serves as a demethylase of histone 3 lysine 4 and 9,has become a potential therapeutic target for cancer ***1 mediates many cellular signaling pathways and regulates cancer cell proliferation,invasion,migration,and *** research has focused on the exploration of its pharmacological *** products are a major source of compounds with abundant scaffold diversity and structural complexity,which have made a major contribution to drug discovery,particularly anticancer *** this review,we briefly highlight recent advances in natural LSD1 inhibitors over the past *** present a comprehensive review on their discovery and identification process,natural plant sources,chemical structures,anticancer effects,and structure-activity relationships,and finally provide our perspective on the development of novel natural LSD1 inhibitors for cancer therapy.

关键词： Histone lysine demethylase LSD1 inhibitor Natural product Anticancer

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Design, synthesis and antitumor evaluations of nucleoside base hydroxamic acid derivatives as DNMT and HDAC dual inhibitors

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Chinese Chemical Letters 2021年第8期32卷 2479-2483页

作者： Qinsheng Sun Qiuzi Dai Cunlong Zhang Yan Chen Lei Zhao Zigao Yuan Yuyang Jiang School of Life Science Tsinghua UniversityBeijing 100084China National&Local United Engineering lab for Personalized Anti-tumor drugs The State Key Laboratory of Chemical OncogenomicsKey Laboratory of Chemical BiologyTsinghua Shenzhen International Graduate SchoolTsinghua UniversityShenzhen 518055China Institute of Biomedical Health Technology and Engineering Shenzhen Bay LaboratoryShenzhen 518055China National&Local United Engineering lab for Personalized Anti-tumor drugs Shenzhen Kivita Innovative Drug Discovery InstituteShenzhen 518110China School of pharmaceutical Sciences Tsinghua UniversityBeijing 100084China

DNA methyl transferase(DNMT) and histone deacetylase(HDAC) are well recognized epigenetic targets for discovery of antitumor *** this study,we designed and synthesized a series of nucleoside base hydroxamic acid derivatives as DNMT and HDAC dual *** assays and enzymatic inhibitory activity tests indicated that compound 204 exhibited potent DNMT1 and HDAC1/6 inhibitory potency simultaneously in enzymatic levels and at cellular levels,inducing hypomethylation of p16 and hyperacetylation of histones H_(3) K9 and H4 ***,204 remarkably inhibited proliferation against cancer cells U937 by prompting G0/G1 cell cycle *** docking models explained the functional mechanism of 204 inhibiting DNMT1 and *** studies on metabolic profiles revealed that 204 showed desirable stability in liver *** study suggested that 204 inhibiting DNMT and HDAC concurrently can be a potential lead compound for epigenetic cancer therapy.

关键词： Epigenetic DNMT HDAC Multitarget Antitumor bioactivity

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Deep proteome profiling promotes whole proteome characterization and drug discovery for esophageal squamous cell carcinoma

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Cancer Biology & Medicine 2022年第3期19卷 273-277页

作者： Wei Liu Yongping Cui Wen Liu Zhihua Liu Liyan Xu Enmin Li College of Science Heilongjiang Institute of TechnologyHarbin 150050China Guangdong Provincial key laboratory of Infectious Diseases and Molecular Immunopathology the Key Laboratory of Molecular Biology for High Cancer Incidence Coastal Chaoshan AreaShantou University Medical CollegeShantou 515041China Department of Pathology Key Laboratory of Cellular Physiology(Shanxi Medical University)Ministry of EducationTaiyuan 030001China Fujian Provincial key laboratory of Innovative drug Target Research School of Pharmaceutical SciencesXiamen UniversityXiamen 361005China state key lab of Molecular Oncology National Cancer Center/Cancer HospitalChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100021China

Proteins are key players in various cellular *** the ultimate executors of cellular processes,they play essential roles in linking genotypes to *** in protein expression and post-translational modifications(PTMs)are closely associated with the initiation and development of cancer,and they carry biological information inaccessible to genomics and *** complements genomic and transcriptomic data,thus enabling comprehensive analysis of cancer pathogenesis and accelerating biomedical research2.

关键词： esophageal linking carry

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