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Comparative chemical characters of Ziziphi Spinosae Semen from geographical origins of China

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Science of Traditional Chinese Medicine 2024年第1期2卷 37-47页

作者： Pengwang Wang Miao Sha Weimei Zhang Hongyue Tian Xu Liang Wei Tian Bo Xu Guanglu Chang Xia Li Wenyuan Gao tianjin key laboratory for modern drug delivery&high-efficiency School of Pharmaceutical Science and TechnologyTianjin UniversityTianjinChina Institute of Chinese Materia Medica of Kenong ShijiangzhuangChina tianjin Tasly modern Chinese Medicine Resources Co. Ltd.TianjinChina

Background:Ziziphi Spinosae Semen(ZSS)contains a wide range of active *** existingmethods cannot fully evaluate these components,a new quantitative method needs to be established for component ***:Ziziphi Spinosae Semen has gained increasing attention in recent years,primarily as a medicinal and edible *** content determination of ZSS is not specified in the Chinese Pharmacopeia(2020 edition).Environmental conditions in different production areas can influence the quality of *** study aims to identify ZSS collected from various geographical origins in *** and methods:high-performance liquid chromatography(HPLC)fingerprints were established using optimized HPLCphoto-diode array ***,similarity analysis and quantification of ZSS from different sources were *** of ZSS were identified and evaluated using the UHPLC-Q Exactive HF Orbitrap MS *** component analysis,hierarchical cluster analysis,and orthogonal partial least squares discriminant analysis were performed based on all peak ***:In this study,the components of ZSS against insomnia were screened through network *** revealed by the results of protein-protein interaction network analysis,Gene Ontology analysis,and Kyoto Encyclopedia of Genes and Genomes pathway analysis,14 core components,10 core targets,and 25 pathways were ***-four batches of ZSS fingerprints were established through the HPLC method,which identified 12 characteristic peaks,with 6 being qualitatively *** identification method for assessing differences in the chemical composition of ZSS from different origins was developed by using UHPLC-Q Exactive HF Orbitrap *** markers from various origins were screened and *** multiple analyses such as principal component analysis and orthogonal partial least squares discriminant analysis,it was concluded that there were differences i

关键词： Ziziphi Spinosae Semen Network pharmacology HPLC fingerprint Metabolites UHPLC-Q Exactive HF Orbitrap MS system

(S)-3-aminopiperidine-2,6-dione is a biosynthetic intermediate of microbial blue pigment indigoidine

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mLife 2022年第2期1卷 146-155页

作者： Zhilong Zhang Pengwei Li Min Wang Yan Zhang Bian Wu Yong Tao Guohui Pan Yihua Chen State key laboratory of Microbial Resources Institute of MicrobiologyChinese Academy of SciencesBeijingChina University of Chinese Academy of Sciences BeijingChina tianjin key laboratory for modern drug delivery and high-efficiency School of Pharmaceutical Science and TechnologyTianjin UniversityTianjinChina

The biosynthetic investigations of microbial natural products continuously provide powerful biocatalysts for the preparation of valuable *** methods for preparing(S)-3-aminopiperidine-2,6-dione(2),the pharmacophore of thalidomide(1)and its analog drugs,are highly *** develop a biocatalyst for producing(S)-2,we dissected the domain functions of IdgS,which is responsible for the biosynthesis of indigoidine(3),a microbial blue pigment that consists of two 2-like *** data supported that the L-glutamine tethered to the indigoidine assembly line is first offloaded and cyclized by the thioesterase domain to form(S)-2,which is then dehydrogenated by the oxidation(Ox)domain and finally dimerized to yield *** on this,we developed an IdgS-derived enzyme biocatalyst,IdgS-Ox^(*)R539A,for preparing enantiomerically pure(S)-*** a proof of concept,one-pot chemoenzymatic synthesis of 1 was achieved by combining the biocatalytic and chemical approaches.

关键词： (S)-3-aminopiperidine-2,6-dione biocatalyst blue pigment indigoidine thalidomide

Chemical composition,pharmacological activity and development strategies of Rubus chingii:A review

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Chinese Herbal Medicines 2024年第3期16卷 313-326页

作者： Xiangmei Xiong Zheng Liu Xiance Che Xuemin Zhang Xia Li Wenyuan Gao tianjin University of Traditional Chinese Medicine Tianjin 301600China tianjin key laboratory for modern drug delivery&high-efficiency School of Pharmaceutical Science and TechnologyFaculty of MedicineTianjin UniversityTianjin 300110China key laboratory of Advanced Chinese Medicine Resources Research Enterprises Tianjin 300402China

Raspberries are used for both food and medicine,but it has not yet attracted widespread *** this paper,the chemical constituen of the original plant *** is one of the new“Zhe Bawei”medicinal materials selected in 2017.“Zhe Bawei”refers to eight kinds of genuine medicinal materials in Zhejiang *** chemical constituents,pharmacological effects,processing,and application of Rubus chingii Hu were reviewed to provide a reference for its further *** literature in recent years was collected in databases such as China Knowledge Network,Web of Science,Elsevier,PubMed,and X-Mol,using“raspberry”,“Rubus chingii”,“traditional use”,“chemical composition”,“pharmacology”,*** keywords individually or in *** summary of pharmacological activities shows that the relationship between the pharmacological activities of raspberry is still not deep *** in-depth research should be carried out in this direction to explore the mechanism of action of its active ingredients and provide effective reference for the further development of the raspberry *** the future,with the participation of more researchers,it is expected to develop innovative drugs based on raspberry for the treatment of diseases.

关键词： applications chemical compositions processing pharmacological effects Rubus chingii Hu

Developing macromolecular therapeutics:the future drug-of-choice

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Frontiers of Chemical Science and Engineering 2010年第1期4卷 10-17页

作者： Huining HE Weibing DONG Junbo GONG Jingkang WANG Victor C.YANG tianjin key laboratory for modern drug delivery and high efficiency Tianjin UniversityTianjin 300072China State key laboratory of Chemical Engineering Tianjin UniversityTianjin 300072China School of Chemical Engineering Tianjin UniversityTianjin 300072China Department of Pharmaceutical Sciences College of PharmacyUniversity of Michigan428 Church StreetAnn ArborMI 48109-1065USA

Macromolecular drugs including peptides,proteins,antibodies,polysaccharides and nucleic acids have been widely used for therapy of major diseases such as carcinoma and AIDS as well as cardiovascular and neurodegenerative disorders among other medical *** to their unmatched properties of high selectivity and efficiency,macromolecular drugs have been recognized as the drug-of-choice of the *** worldwide progress on macromolecular therapeutics still remains in the infant stage and is therefore wide open for equalground competition,R&D related to macromolecular drugs should be considered as the main point of focus in China in setting up its strategic plans in pharmaceutical *** this article,research strategies and drug delivery approaches that should be adopted to enhance the therapeutic effects of macromolecular drugs are *** addition,comments concerning how to implement such strategies to excel from competition in this challenging research field,such as the design of innovative and highly effective delivery systems of macromolecular drugs with self-owned intellectual property rights,are provided.

关键词： macromolecular drugs drug delivery systems therapeutic efficacy

Rhizoma paridis saponins protected against liver injury in diethylnitrosamine-induced mice

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Traditional Medicine Research 2023年第2期8卷 7-12页

作者： Chen Luo Jing-Wen Yao Shu-Li Man Wen-Yuan Gao key laboratory of Industrial Microbiology Ministry of Education/Tianjin Key Laboratory of Industry Microbiology/National and Local United Engineering Lab of Metabolic Control Fermentation Technology/College of BiotechnologyTianjin University of Science&TechnologyTianjin 300457China tianjin key laboratory for modern drug delivery and high efficiency School of Pharmaceutical Science and TechnologyTianjin UniversityTianjin 300072China

Background:Diethylnitrosamine,one of food additives,possessed a strong carcinogenic effect in *** paridis saponins,as the main active components of Paris polyphylla,have a good anti-cancer effect in our previous *** verify their inhibitory effect on diethylnitrosamine-induced liver cancer,we carried out this ***:We established diethylnitrosamine-induced mouse hepatocarcinoma models to evaluate antitumor of Rhizoma paridis ***,gas chromatography-mass spectrometry was applied to analyze the metabolites in the urine and serum ***:Rhizoma paridis saponins alleviated diethylnitrosamine-induced *** the one hand,Rhizoma paridis saponins down-regulated the levels of liver function markers,such as alanine aminotransferase,aspartate transaminase and alpha *** the other hand,Rhizoma paridis saponins reduced metabolic disorders by increasing fructose and mannose metabolism,and decreasing pentose and glucuronate interconversion,inositol phosphate metabolism,and the process of saturated fatty acids transforming to unsaturated fatty acids,which based on the regulating mRNA expression of glucose transporter type 4,lactate dehydrogenase A,fatty acid synthetas,acetyl-CoA carboxylase and apolipoprotein ***:Rhizoma paridis saponins has the potential application to inhibit chemical-induced hepatocarcinogenesis in the future.

关键词： Rhizoma paridis saponins liver injury diethylnitrosamine metabolites

Recent progress in the structural study of ion channels as insecticide targets

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Insect Science 2022年第6期29卷 1522-1551页

作者： Hadiatullah Hadiatullah Yongliang Zhang Arthur Samurkas Yunxuan Xie Rajamanikandan Sundarraj Han Zuilhof Jianjun Qiao Zhiguang Yuchi tianjin key laboratory for modern drug delivery&high-efficiency Collaborative Innovation Center of Chemical Science and EngineeringSchoolof Pharmaceutical Science and TechnologyTianjin UniversityTianjinChina Department of MolecularPharmacology Tianjin Medical University Cancer Institute&HospitalNational Clinical Research Center for CancerKey Laboratory of Cancer Prevention and TherapyTianjin laboratory of Organic Chemistry Wageningen University&Research WageningenThe Netherlands Department of Environmental Science Tianjin UniversityTianjinChina key laboratory of Systems Bioengineering(Ministry of Education) Tianjin UniversityTianjinChina

Ion channels,many expressed in insect neural and muscular systems,have drawn huge attention as primary targets of *** the recent technical breakthroughs in structural biology,especially in cryo-electron microscopy(cryo-EM),many new high-resolution structures of ion channel targets,apo or in complex with insecticides,have been solved,shedding light on the molecular mechanism of action of the insecticides and resistance *** structures also provide accurate templates for structure-based insecticide screening and rational *** review summarizes the recent progress in the structural studies of 5 ion channel families:the ryanodine receptor(RyR),the nicotinic acetylcholine receptor(nAChR),the voltage-gated sodium channel(VGSC),the transient receptor potential(TRP)channel,and the ligand-gated chloride channel(LGCC).We address the selectivity of the channel-targeting insecticides by examining the conservation of key coordinating residues revealed by the *** possible resistance mechanisms are proposed based on the locations of the identified resistance mutations on the 3D structures of the target channels and their impacts on the binding of ***,we discuss how to develop“green”insecticides with a novel mode of action based on these high-resolution structures to overcome the resistance.

关键词： cryo-electron microscopy structure crystal structure insecticide ion chan-nel resistance

Evaluation of bioactive flavonoids in Citri Reticulatae Pericarpium from different regions and its association with antioxidant andα-glucosidase inhibitory activities

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Traditional Medicine Research 2022年第1期7卷 1-9页

作者： Na Liu Jia-Chen Sun Wen-Na Yang Di Liang Lan-Ping Guo Xia Li Wen-Yuan Gao tianjin key laboratory for modern drug delivery&high-efficiency School of Pharmaceutical Science and TechnologyTianjin UniversityTianjin 300193China School of Biotechnology and Food Science Tianjin University of CommerceTianjin 300134China National Resource Center for Chinese Materia Medica Academy of Chinese Medical SciencesBeijing 100700China

Background:To explore the differences of 14 batches of Citri Reticulatae Pericarpium from different ***:The main aim of this study was to develop a high-performance liquid chromatography method-photodiode array detection for determining the contents of five flavonoids and the chromatographic fingerprints of Citri Reticulatae Pericarpium from different ***α-glucosidase inhibitory activities and antioxidant properties of Citri Reticulatae Pericarpium,based on free-radical scavenging assays against 1,1-diphenyl-2-picrylhydrazyl,2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid),and hydroxyl radicals,were estimated and ***:Among the tested compounds,the content of hesperidin(13.386-68.235 mg/g)was the highest and that of hesperitin(0.045-0.277 mg/g)was the *** comparing different sources of Citri Reticulatae Pericarpium,the contents of narirutin in Citri Reticulatae Pericarpium from Guangdong(0.824-0.851 mg/g)and Sichuan(1.069-1.204 mg/g)provinces of China were lower than in other *** contrast,nobiletin(8.429-12.237 mg/g)and tangeretin(3.947-4.613 mg/g)were most abundant in Guangdong sources of Citri Reticulatae Pericarpium,followed by samples from Sichuan Province(nobiletin:6.761-7.658 mg/g;tangeretin:3.422-3.933 mg/g).Correlation analysis showed that nobiletin and tangeretin were the main contributors to the antioxidant capacity,and narirutin was the main active component inhibiting theα-glucosidase activity of Citri Reticulatae ***:This work revealed that the intrinsic quality of Citri Reticulatae Pericarpium was affected by different growing regions,which provides a scientific basis for controlling the quality of Citri Reticulatae Pericarpium and rationally developing and utilizing Citri Reticulatae Pericarpium.

关键词： Citri Reticulatae Pericarpium flavonoids HPLC-PDA antioxidant activity α-glucosidase inhibitory activity

Pd-Catalyzed ortho-mono functionalization of anilides under oxidative conditions

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Pd-Catalyzed ortho-mono functionalization of anilides under ...

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

中国化学会第29届学术年会

作者： Shaonan Lu Ranran Zhu Di Zhu Jianhui Huang tianjin key laboratory for modern drug delivery ＆ high-efficiency School of Pharmaceutical Science and Technology Tianjin University

The Pd-catalyzed cross-dehydrogenative coupling（CDC） reactions of C（sp2）-H bond has received much attention in recent years.1 The reactions are normally under forcing conditions with competition between mono- and di- functionalization. In the group, we are interested in the studies of selective direct C-H functionalization of arenes under mild conditions.2 Recently, we have developed a practical synthesis for the mono ortho-substituted aryl amide syntheses under oxidative conditions. As demonstrated in the Scheme below, a series of functionalities have been introduced under our *** this poster, detailed reaction scope and limitations will be described;the reaction mechanism will be discussed for the understanding of the reaction pathway.

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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