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Author correction to‘3-O-Acetyl-11-keto-bboswellic acid ameliorated aberrant metabolic landscape and inhibited autophagy in glioblastoma’[Acta Pharm Sin B 10(2020)301-312]

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Acta Pharmaceutica Sinica B 2024年第8期14卷 3783-3784页

作者： Wan Li Liwen Ren Xiangjin Zheng Jinyi Liu Jinhua Wang Tengfei Ji Guanhua Du The State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Science and Peking Union Medical CollegeBeijing 100050China Laboratory of Drug Target Research and Drug Screen Institute of Materia MedicaChinese Academy of Medical Science and Peking Union Medical CollegeBeijing 100050China

The authors apologize for two inadvertent mistakes in Fig.5:the image of immunofluorescence of LC3B in the Vehicle group(Fig.5c)and the image of transmission electron microscope in the AKBA 10 mmol/L group(Fig.5f)were provided *** corrected Fig.5 is shown *** original data of these figures have been provided to the Editorial Office,and the corresponding authors or the Editorial Office can be contacted for original data access.

关键词： correction Office image

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An Update on the Clinical Pipelines of New Antibacterial Drugs Developed in China

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Engineering 2024年第7期38卷 52-68页

作者： Xinyi Yang Congran Li Xiukun Wang Zhonghui Zheng Peiyi Sun Chunjie Xu Luni Chen Jiandong Jiang Staffan Normark Birgitta Henriques-Normark Xuefu You Beijing Key Laboratory of Antimicrobial Agents/Laboratory of Pharmacology Institute of Medicinal BiotechnologyChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China Division for Medicinal Microorganism-Related Strains CAMS Collection Center of Pathogenic MicroorganismsChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China State Key Laboratory of Bioactive Substances and Functions of Natural Medicines Institute of Medicinal BiotechnologyChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China Shandong Xinhua Pharmaceutical Co. Ltd.Zibo 255005China Department of Microbiology Tumor and Cell BiologyKarolinska InstitutetStockholm SE-17177Sweden State Key Laboratory of Bioactive Substances and Function of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China Institute of Medicinal Biotechnology Chinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China Clinical Microbiology Karolinska University HospitalBioclinicumStockholm SE-17176Sweden

Antibacterial resistance is a global health threat that requires further concrete action on the part of all *** this context,one of the biggest concerns is whether enough new antibacterial drugs are being discovered and *** several high-quality reviews on clinical antibacterial drug pipelines from a global perspective were published recently,none provides comprehensive information on original antibacterial drugs at clinical stages in *** this review,we summarize the latest progress of novel antibacterial drugs approved for marketing and under clinical evaluation in China since *** was obtained by consulting official websites,searching commercial databases,retrieving literature,asking personnel from institutions or companies,and other means,and a considerable part of the data covered here has not been included in other *** of June 30,2023,a total of 20 antibacterial projects from 17 Chinese pharmaceutical companies or developers were identified and *** them,two new antibacterial drugs that belong to traditional antibiotic classes were approved by the National Medical Products Administration(NMPA)in China in 2019 and 2021,respectively,and 18 antibacterial agents are in clinical development,with one under regulatory evaluation,five in phase-3,six in phase-2,and six in *** of the clinical candidates are new analogs or monocomponents of traditional antibacterial pharmacophore types,including two dual-acting hybrid antibiotics and a recombinant antibacterial ***,despite there being 17 antibacterial clinical candidates,our analysis indicates that there are still relatively few clinically differentiated antibacterial agents in stages of clinical development in ***,Chinese pharmaceutical companies and institutions will develop more innovative and clinically differentiated candidates with good market potential in the future research and development(R&D)of original antibacterial drugs.

关键词： Antimicrobial resistance New antibiotics Clinical pipelines WHO priority pathogens National Mega-Project for Innovative Drugs

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Simple and versatile in situ thermo-sensitive hydrogel for rectal administration of SZ-A to alleviate inflammation and repair mucosal barrier in ulcerative colitis

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Chinese Chemical Letters 2024年第6期35卷 462-468页

作者： Yu Yan Jiawei Song Dongdong Liu Zihan Liu Jialing Cheng Zhiyang Chen Yanfang Yang Weizhe Jiang Hongliang Wang Jun Ye Yuling Liu State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China College of Pharmacy Guangxi Medical UniversityNanning 530021China Beijing Key Laboratory of Drug Delivery Technology and Novel Formulation Institute of Materia MedicaChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China

Ulcerative colitis(UC)is a chronic inflammatory bowel disease characterized by persistent inflammation of the colon and disrupted intestinal *** mori(Sangzhi)alkaloids(SZ-A),derived from twigs of mulberry,were approved by the National Medical Products Administration in 2020 for treating type 2 diabetes *** evidence has confirmed that SZ-A also alleviates non-alcoholic fatty liver disease and ameliorates inflammation,indicating its potential to address inflammation in ***,the treatment of UC faces challenges due to low drug delivery efficiency and short retention *** overcome these challenges,an injectable and adherent in-situ thermo-sensitive hydrogel containing SZ-A was developed for rectal drug delivery,utilizing the thermo-sensitive polymers Poloxamer 407and *** thermo-sensitive hydrogel system was designed with a moderate gelation temperature of 32±0.5℃,a short gelation time of 64 s,a p H range of 7-10,high moisturizing capability exceeding 90%,and moderate mechanical strength of 4-5 *** a rat model with UC,the in situ thermo-sensitive hydrogel significantly extended the retention time at the colonic site and enabled sustained release after rectal *** of UC were markedly reduced following rectal administration of SZ-A thermosensitive ***,the release of inflammatory factors,such as interleukin-1β(IL-1β),IL-6,IL-18,tumor necrosis factor-α(TNF-α),and transforming growth factor-β1(TGF-β1),significantly decreased in the SZ-A thermo-sensitive hydrogel *** integrity of the colonic mucosal barrier was significantly enhanced following the application of SZ-A thermo-sensitive *** conclusion,rectal administration of SZ-A in situ thermo-sensitive hydrogel effectively alleviated UC symptoms,inhibited the secretion of inflammatory factors,and promoted the repair of the colonic mucosal *** approach holds promise as a potential treatment for UC.

关键词： Ulcerative colitis SZ-A Thermo-sensitive hydrogel Rectal administration Alleviation of inflammation Mucosal barrier repair

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An unexpected stereochemical effect of thio-substituted Asp in native chemical ligation

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Chinese Chemical Letters 2024年第8期35卷 278-281页

作者： Min Fu Pan He Sen Zhou Wenqiang Liu Bo Ma Shiying Shang Yaohao Li Ruihan Wang Zhongping Tan State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100050China Center of Pharmaceutical Technology School of Pharmaceutical SciencesTsinghua UniversityBeijing 100084China Chemical Engineering College Hebei Normal University of Science and TechnologyQinhuangdao 066600China

This study presents an unexpected finding that the cis isomer of β-thio-Asp exhibits higher ligation ac-tivity than the trans *** discovery sheds light on the intricate nature of native chemical ligation and highligh... 详细信息

关键词： Native chemical ligation Stereochemistry Ligation activity β-Thio-Asp Intramolecular hydrogen bond

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Identification of multi-target anti-cancer agents from TCM formula by in silico prediction and in vitro validation

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Chinese Journal of natural medicines 2022年第5期20卷 332-351页

作者： ZHANG Bao-Yue ZHENG Yi-Fu ZHAO Jun KANG De WANG Zhe XU Lv-Jie LIU Ai-Lin DU Guan-Hua State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100050China School of Life Sciences Tsinghua UniversityBeijing 100084China

Cancer is a complex disease associated with multiple gene mutations and malignant phenotypes,and multi-target drugs provide a promising therapy idea for the treatment of *** products with abundant chemical structure types and rich pharmacological characteristics could be ideal sources for screening multi-target antineoplastic *** this paper,50 tumor-related targets were collected by searching the Therapeutic Target Database and Thomson Reuters Integrity database,and a multi-target anti-cancer prediction system based on mt-QSAR models was constructed by using naïve Bayesian and recursive partitioning algorithm for the first *** the multi-target anti-cancer prediction system,some dominant fragments that act on multiple tumor-related targets were analyzed,which could be helpful in designing multi-target anti-cancer ***-cancer traditional Chinese medicine(TCM)and its natural products were collected to form a TCM formula-based natural products library,and the potential targets of the natural products in the library were predicted by multi-target anti-cancer prediction *** a result,alkaloids,flavonoids and terpenoids were predicted to act on multiple tumor-related *** predicted targets of some representative compounds were verified according to literature review and most of the selected natural compounds were found to exert certain anti-cancer activity in vitro biological *** conclusion,the multi-target anti-cancer prediction system is very effective and reliable,and it could be further used for elucidating the functional mechanism of anti-cancer TCM formula and screening for multi-target anti-cancer *** anti-cancer natural compounds found in this paper will lay important information for further study.

关键词： Cancer Multi-target mt-QSAR model Nave Bayesian Recursive partitioning TCM formulae

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Rg1 exerts protective effect in CPZ-induced demyelination mouse model via inhibiting CXCL10-mediated glial response

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中国药理学报（英文版） 2022年第3期43卷 563-576页

作者： Yi-xiao Dong Shi-feng Chu Sha-sha Wang Ya-juan Tian Wen-bin He Yu-sheng Du Zhen-zhen Wang Xu Yan Zhao Zhang Nai-hong Chen State Key Laboratory of Bioactive Substances and Functions of Natural Medicines Institute of Materia Medica&Neuroscience CenterChinese Academy of Medical SciencesPeking Union Medical CollegeBeijing 100050China Tianjin University of Traditional Chinese Medicine Tianjin 301617China State Key Laboratory of Bioactive Substances and Functions of Natural Medicines Institute of Materia Medica&Neuroscience CenterChinese Academy of Medical SciencesPeking Union Medical CollegeBeijing 100050China State Key Laboratory of Bioactive Substances and Functions of Natural Medicines Institute of Materia Medica&Neuroscience CenterChinese Academy of Medical SciencesPeking Union Medical CollegeBeijing 100050China Shanxi Key Laboratory of Chinese Medicine Encephalopathy Shanxi University of Chinese MedicineJinzhong 030619China Shanxi Key Laboratory of Chinese Medicine Encephalopathy Shanxi University of Chinese MedicineJinzhong 030619China State Key Laboratory of Bioactive Substances and Functions of Natural Medicines Institute of Materia Medica&Neuroscience CenterChinese Academy of Medical SciencesPeking Union Medical CollegeBeijing 100050China Tianjin University of Traditional Chinese Medicine Tianjin 301617China Shanxi Key Laboratory of Chinese Medicine Encephalopathy Shanxi University of Chinese MedicineJinzhong 030619China

Myelin damage and abnormal remyelination processes lead to central nervous system *** activation-induced microenvironment changes are characteristic features of the diseases with myelin *** previously showed that ginsenoside Rg1,a main component of ginseng,ameliorated MPTP-mediated myelin damage in mice,but the underlying mechanisms are *** this study we investigated the effects of Rg1 and mechanisms in cuprizone(CPZ)-induced demyelination mouse *** were treated with CPZ solution(300mg·kg-1·d-1,ig)for 5 weeks;from week 2,the mice received Rg1(5,10,and 20 mg·kg-1·d-1,ig)for 4 *** showed that Rg1 administration dose-dependently alleviated bradykinesia and improved CPZ-disrupted motor coordination ability in CPZ-treated ***,Rg1 administration significantly decreased demyelination and axonal injury in pathological *** further revealed that the neuroprotective effects of Rg1 were associated with inhibiting CXCL10-mediated modulation of glial response,which was mediated by NF-KB nuclear translocation and CXCL10 promoter *** microglial cell line BV-2,we demonstrated that the effects of Rg1 on pro-inflammatory and migratory phenotypes of microglia were related to CXCL10,while Rg1-induced phagocytosis of microglia was not directly related to *** CPZ-induced demyelination mouse model,injection of AAV-CXCL10 shRNA into mouse lateral ventricles 3 weeks prior CPZ treatment occluded the beneficial effects of Rg1 administration in behavioral and pathological *** conclusion,CXCL10 mediates the protective role of Rg1 in CPZ-induced demyelination mouse *** study provides new insight into potential disease-modifying therapies for myelin abnormalities.

关键词： Biomedicine general Pharmacology/Toxicology Medical Microbiology Immunology Internal Medicine Vaccine

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A kinetic resolution accompanied chirality transformation process for asymmetric synthesis of chiral phenol,oxaziridine,andα-hydroxyl cyclic ketone

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Science China Chemistry 2024年第9期67卷 2989-2997页

作者： Pengxin Wang Xiaoyong Zhang Lingqing Wang Rui Wang Dongxu Yang Key Laboratory of Preclinical Study for New Drugs of Gansu Province School of Basic Medical Sciences&Research Unit of Peptide ScienceChinese Academy of Medical SciencesLanzhou UniversityLanzhou 730000China State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100050China School of Sciences Great Bay UniversityDongguan 523000China Institute of Systems and Physical Biology Shenzhen Bay LaboratoryShenzhen 518055China

Chirality transformation is a basic,attractive,and important strategy for obtaining enantioenriched products with desired chiral *** reported chirality conversion reaction often involves the process from one type of chirality to another *** better utilize the chirality transformation strategy for obtaining two or more products with different chiral elements in a single reaction,a new method of kinetic resolution accompanied by a chirality transformation protocol is proposed and successfully realized in this *** process is used for the asymmetric oxidation of phenol compounds along with the kinetic resolution of oxaziridines.A wide scope of products,including axially chiral phenols,oxaziridines,andα-hydroxyl cyclic ketones were smoothly obtained in high levels of yields and enantioselectivities in the developed *** products can be readily used for the synthesis of various types of chiral ligands,which are potential choices for other catalytic asymmetric reactions.

关键词： chirality transformation kinetic resolution accompanied axially chiral phenols chiral oxaziridines

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Structural diversification of phenylspirodrimane lactams by employing a biosynthetic intermediate

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Chinese Chemical Letters 2023年第12期34卷 141-145页

作者： Jimei Liu Zhenfei Wang Jun Wu Yaotian Han Fei Ye Tiantai Zhang Haibo Yu Zhengshun Wen Jungui Dai State Key Laboratory of Bioactive Substance and Function of Natural Medicines CAMS Key Laboratory of Enzyme and Biocatalysis of Natural DrugsNHC Key Laboratory of Biosynthesis of Natural Productsand Beijing Key Laboratory of Non-Clinical Drug Metabolism and PK/PD StudyInstitute of Materia MedicaChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100050China Zhejiang Provincial Engineering Technology Research Center of Marine Biomedical Products School of Food Science and PharmaceuticsZhejiang Ocean UniversityZhoushan316022China

Phenylspirodrimanes are a kind of meroterpenoids with structural diversity and complexity,exhibiting a wide of biological properties,especially for the lactam derivatives consisting a y-lactam moiety and N-linked side *** compounds were derived from multi-step combination of enzymatic and non-enzymatic conversions of intermediates in their biosynthetic ***(2)with an o-phthalaldehyde unit was supposed as the high-reactivity intermediate of phenylspirodrimane lactams via nonenzymatic reaction with *** the present work,an effective and non-enzymatic diversification strategy was developed for the structural diversification of phenylspirodrimane lactams including monomers and dimers from 2 by feeding structurally various mono-and diamines in the fungus Stachybotrys chartarum *** total,24 phenylspirodrimane lactams(1,3-25)including 18 new compounds were *** them,stachybocin A(1),a bioactive phenylspirodrimane lactam dimer,was produced with the yield of 18.7 mg/g of cell dry *** structures of these compounds were elucidated by extensive spectroscopic data,single-crystal X-ray diffraction(Cu Kα),and calculated electronic circular dichroism(ECD)*** revealed that compounds 1,17,and 24 displayed significant inhibitory effect on the inactivated state of hNav 1.2 channels with IC_(50) values of 0.22,2.08,and 0.53μmol/L,*** addition,1 showed potent protein tyrosine phosphatase 1B(PTP1B)inhibitory N-methyl-b-aspartate(NMDA)receptor antagonistic,and anti-inflammatory activities.

关键词： Phenylspirodrimane lactams Stachbotrydial Nonenzymatic reaction hNav 1.2channels inhibitoryactivity Stachybotrys chartarum

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Concise Synthesis of Lactococcus garvieae Lipoteichoic Acids Through an Additive-Modulated Preactivation Protocol and the Immunological Studies

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CCS Chemistry 2024年第2期6卷 403-414页

作者： Tianlu Li Tong Li Yue Yang Haoru Zhuang Jianwu Lv Ning Zhou Miaomiao Zhang Fengshan Wang Yiqun Geng Richard R.Schmidt Peng Peng National Glycoengineering Research Center Shandong Key Laboratory of Carbohydrate Chemistry and GlycobiologyNMPA Key Laboratory for Quality Research and Evaluation of Carbohydrate Based MedicineShandong UniversityQingdao 266237 State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100050 Department of Chemistry University of KonstanzD-78457 Konstanz

Lipoteichoic acids(LTAs)are macroamphiphiles composed of alditol,lipid,phosphate,and carbohydrate *** to their inherent complexity,it is a severe challenge to access LTAs with structural integrity from natural sources for biological or immunological ***,we describe the first total synthesis of Lactococcus garvieae LTA(type II LTA),containing five distinct 1,2-cis gluco/galactopyranosidic linkages,via a novel additive-modulated O-glycosyl trichloroacetimidate preactivation glycosidation *** strategy features(1)high glycosidation yields and excellent 1,2-cis stereoselectivities independent of the donor anomeric configuration,(2)common and inexpensive reagents as promoters and additives,(3)application to standard glycosyl imidate donors without resorting to participating protection,and(4)general application to reactive and less reactive glycosyl ***,via the precise stereocontrolled construction of three galactopyranosidic and two glucopyranosidic bonds on a multigram scale,a series of structurally well-defined LTA molecules were successfully *** evaluation of these type II synthetic LTAs showed a structure–activity relationship in the stimulation of a proinflammatory response.

关键词： 1,2-cis glycosidation stereoselectivity lipoteichoic acid total synthesis additive-modulated trichloroacetimidate glycosidation immune response

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Monoterpene derivatives from the fruits of Illicium simonsii

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Journal of Asian natural Products Research 2025年第6期27卷 834-843页

作者： Li, Mi Su, Guo-Zhu Wang, Hai-Qiang Wang, Xiao-Jing Li, Li Li, Yu-Huan Ma, Shuang-Gang Yu, Shi-Shan State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia Medica Chinese Academy of Medical Sciences & Peking Union Medical College Beijing 100050 China Institute of Medicinal Biotechnology Chinese Academy of Medical Sciences and Peking Union Medical College Beiing 100050 China

Three previously undescribed monoterpene derivatives, illisimoncins A–C (1–3) and one undescribed 2-formylpyrrole alkaloid (4) were isolated from the fruits of Illicium simonsii together with five known monoterpenes (5-9). Structural elucidation of compounds 1-4 was elucidated through comprehensive spectroscopic analyses and their absolute configurations were determined by the dimolybdenum tetraacetate [Mo₂(AcO)₄]-induced ICD experiment and modified Mosher’s method. Compounds 2 and 7 showed antiviral activities against Coxsackievirus B3 with IC₅₀ values of 57.74 and 23.24 µM, respectively. © 2025 Informa UK Limited, trading as Taylor & Francis Group.

关键词： anti-Coxsackievirus B3 activity Illiciaceae Illicium simonsii monoterpene derivatives

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