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Process analytical technologies and self-optimization algorithms in automated pharmaceutical continuous manufacturing

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Chinese chemical Letters 2024年第3期35卷 87-95页

作者： Peiwen Liu Hui Jin Yan Chen Derong Wang Haohui Yan Mingzhao Wu Fang Zhao Weiping Zhu State Key Laboratory of Bioreactor Engineering Shanghai Key Laboratory of Chemical BiologySchool of PharmacyEast China University of Science and TechnologyShanghai 200237China State Key Laboratory of chemical Engineering School of Chemical EngineeringEast China University of Science and TechnologyShanghai 200237China Engineering Research Center of pharmaceutical Process Chemistry Ministry of EducationSchool of PharmacyEast China University of Science and TechnologyShanghai 200237China

The pharmaceutical industry is now paying increased attention to continuous *** the revolution to continuous and automated manufacturing is deepening in most of the top pharma companies in the world,the advancement of automated pharmaceutical continuous manufacturing in China is relatively slow due to some key challenges including the lack of knowledge on the related technologies and shortage of qualified *** this review,emphasis is given to two of the crucial technologies in automated pharmaceutical continuous manufacturing,i.e.,process analytical technology(PAT)and self-optimizing *** work published in recent 5 years employing advanced PAT tools and self-optimization algorithms is introduced,which represents the great progress that has been made in automated pharmaceutical continuous manufacturing.

关键词： pharmaceutical continuous manufacturing Automation Process analytical technology Self-optimization algorithm

Divergent total synthesis of marine meroterpenoids(+)-dysidavarones A–C

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Chinese chemical Letters 2024年第3期35卷 234-238页

作者： Qunlong Zhang Yang Kuang Le Chang Jingyi Kang Bingjian Wang Chuanke Chong Zhaoyong Lu State Key Laboratory of Medicinal chemical biology College of PharmacyNankai UniversityTianjin 300350China

Here,we report a concise and divergent enantioselective total synthesis of marine sesquiterpene quinone meroterpenoids(+)-dysidavarones A–C(1–3)using predysidavarone 6 as a key common *** highly strained and bridged eight-membered carbocycle of predysidavarone 6 was constructed by a one-pot intermolecular alkylation and intramolecular arylation of Wieland–Miescher ketone derivative 11 and benzyl bromide *** total synthesis of(+)-dysidavarones A–C(1–3)was achieved from predysidavarone 6 in a divergent manner by a late-stage introduction of the ethoxy group,which reveals the possible source of the ethoxy group within(+)-dysidavarones A–C(1–3)and provides a late-stage modifiable route for the synthesis of dysidavarone analogs for further anti-cancer activity evaluation.

关键词： Total synthesis Natural product Dysidavarones A–C Sesquiterpene quinone Meroterpenoid

Orthogonal Combinatorial Raman Codes Enable Rapid High-Throughput-Out Library Screening of Cell-Targeting Ligands

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Research 2024年第1期2023卷 199-208页

作者： Yuchen Tang Xingxing Zheng Tingjuan Gao China Key Laboratory of Pesticide and chemical biology of Ministry of Education College of ChemistryCentral China Normal UniversityWuhan 430079China

High-throughput assays play an important role in the fields of drug discovery,genetic analysis,and clinical *** super-capacity coding strategies may facilitate labeling and detecting large numbers of targets in a single assay,practically,the constructed large-capacity codes have to be decoded with complicated procedures or are lack of survivability under the required reaction *** challenge results in either inaccurate or insufficient decoding ***,we identified chemical-resistant Raman compounds to build a combinatorial coding system for the high-throughput screening of cell-targeting ligands from a focused 8-mer cyclic peptide *** accurate in situ decoding results proved the signal,synthetic,and functional orthogonality for this Raman coding *** orthogonal Raman codes allowed for a rapid identification of 63 positive hits at one time,evidencing a high-throughput-out capability in the screening *** anticipate this orthogonal Raman coding strategy being generalized to enable efficient high-throughput-out screening of more useful ligands for cell targeting and drug discovery.

关键词： enable throughput allowed

Basic regulatory science behind drug substance and drug product specifications of monoclonal antibodies and other protein therapeutics

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Journal of pharmaceutical Analysis 2024年第6期14卷 785-804页

作者： Patanachai K.Limpikirati Sorrayut Mongkoltipparat Thinnaphat Denchaipradit Nathathai Siwasophonpong Wudthipong Pornnopparat Parawan Ramanandana Phumrapee Pianpaktr Songsak Tongchusak Maoxin Tim Tian Trairak Pisitkun Department of Food and pharmaceutical Chemistry Faculty of Pharmaceutical SciencesChulalongkorn UniversityPathumwanBangkok10330Thailand pharmaceutical Sciences and Technology(PST)Graduate Program Faculty of Pharmaceutical SciencesChulalongkorn UniversityPathumwanBangkok10330Thailand Center of Excellence in Systems biology(CUSB) Faculty of MedicineChulalongkorn UniversityPathumwanBangkok10330Thailand Department of pharmaceutical Chemistry Faculty of Pharmaceutical SciencesHuachiew Chalermprakiet UniversityBang PhliSamut Prakan10540Thailand Division of Research Affairs Faculty of MedicineChulalongkorn UniversityPathumwanBangkok10330Thailand

In this review,we focus on providing basics and examples for each component of the protein therapeutic specifications to interested pharmacists and biopharmaceutical scientists with a goal to strengthen understanding in regulatory science and *** specifications comprise a list of important quality attributes for testing,references to use for test procedures,and appropriate acceptance criteria for the tests,and they are set up to ensure that when a drug product is administered to a patient,its intended therapeutic benefits and safety can be rendered *** of drug substance or drug product to the specifications is achieved by testing an article according to the listed tests and analytical methods and obtaining test results that meet the acceptance *** attributes are chosen to be tested based on their quality risk,and consideration should be given to the merit of the analytical methods which are associated with the acceptance criteria of the *** criteria are set forth primarily based on efficacy and safety profiles,with an increasing attention noted for patient-centric *** in this work are related guidelines that support the biopharmaceutical specification setting,how to set the acceptance criteria,and examples of the quality attributes and the analytical methods from 60 articles and 23 pharmacopeial *** are also explored on process analytical technologies and other orthogonal tools which are on-trend in biopharmaceutical characterization and quality control.

关键词： Biopharmaceutical analysis Biopharmaceutical quality control Biopharmaceutical specifications Monoclonal antibodies Protein therapeutics Regulatory science

Inhalable nanoparticles with enhanced cuproptosis and cGAS-STING activation for synergistic lung metastasis immunotherapy

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Acta Pharmaceutica Sinica B 2024年第8期14卷 3697-3710页

作者： Chongzheng Yan Huaiyou Lv Yafei Feng Yuhan Li Zhongxi Zhao Department of Pharmaceutics Key Laboratory of Chemical Biology of Ministry of EducationSchool of Pharmaceutical SciencesCheelloo College of MedicineShandong UniversityJinan 250012China Key University Laboratory of Pharmaceutics&Drug Delivery Systems of Shandong Province School of Pharmaceutical SciencesCheeloo College of MedicineShandong UniversityJinan 250012China Department of Pharmacy Yantai Yuhuangding Hospital Affiliated to Qingdao UniversityYantai 264001China

Due to the insufficient Cu^(+)accumulation,Cu^(+)efflux mechanism,and highly immunosuppressive tumor microenvironment(TME)in lung metastasis,the cuproptosis efficacy is ***,an inhalable nanodevice(CLDCu)is constructed to successfully overcome the drawbacks of *** consists of a Cu^(2+)-chitosan shell and low molecular weight heparin-tocopherol succinate(LMWH-TOS,LT)core with disulfiram(DSF)*** prepared CLDCu can be inhaled and accumulate in large amounts in lung lesions(63.6%)with 56.5 times higher than intravenous *** tumor cells,the mild acidity triggers the co-release of DSF and Cu2+,thus generating bis(diethyldithiocarbamate)-copper(CuET)to block Cu^(+)efflux protein ATP7B and forming toxic Cu^(+),leading to enhanced ***,the released chitosan cooperates with CLDCu-induced cuproptosis to activate stimulator of interferon genes(STING)pathway,which significantly potentiates dendritic cells(DCs)maturation,as wells as evokes innate and adaptive *** lung metastatic mice model,CLDCu is found to induce cuproptosis and reverse the immunosuppressive TME by inhalation ***,CLDCu combined with anti-programmed cell death protein ligand-1 antibody(aPD-L1)provokes stronger antitumor ***,nanomedicine that combines cuproptosis with STING activation is a novel strategy for tumor immunotherapy.

关键词： Cuproptosis cGAS-STING activation Disulfiram Inhalation administration Tumor microenvironment PD-L1 checkpoint blockade Lung metastasis Immunotherapy

Synthetic Studies toward Pseudolaric Acids:Radical Cyclization to Form Bridged Scaffold

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Chinese Journal of Chemistry 2024年第15期42卷 1699-1705页

作者： Yujie Niu Minggui Lin Hao Cui Yanji Huang Yang Shen Yandong Zhang State Key Laboratoryof Physical Chemistry of Solid Surfaces Key Laboratory of Chemical Biology of Fujian ProvinceicHEMCollege of Chemistryand Chemical EngineeringXiamen UniversityXiamenFujian 361005China

Pseudolaric acids are a family of diterpenoid natural products that exhibit a broad spectrum of biological *** main structural feature of their framework is a trans-fused perhydroazulene bearing a bridged lactone positioned at the junction of the ***,we have developed a radical cyclization strategy that allows flexible tuning of the cyclization process through diverse silicon substitutions on the *** strategy can assist in constructing a series of skeletons with structural resemblance to pseudolaric acids and expedites the construction of the bridged ***,it facilitates the synthesis of the entire skeletal structure of the pseudolaric acidfamily of natural products,excludingthe B-ringfunctionalization.

关键词： Terpenoids Total synthesis Radical cyclization Bridged cycles Regioselectivity

Direct Synthesis of α-Aminophosphonates from Amines,Alcohols,and White Phosphorus

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CCS Chemistry 2024年第1期6卷 91-99页

作者： Mengpei Bai Yinwei Cao Junwei Huang Yan Liu Guo Tang Yufen Zhao Department of Chemistry and Key Laboratory for chemical biology of Fujian Province College of Chemistry and Chemical EngineeringXiamen UniversityXiamenFujian 361005

Developing practical strategies for the synthesis of organophosphorus compounds(OPCs)from white phosphorus(P_(4))without the use of Cl_(2) and PCl_(3) remains a significant *** first multicomponent oxidative α-phosphonylation of amines with P_(4) and alcohols has been *** the use of copper(Ⅱ)as the catalyst and air as the safe oxidant,structurally sophisticated α-aminophosphonates have been prepared in high ***,this method is also suitable for selective construction of P-O-P *** reaction is characterized by a complete conversion of P_(4).The activation of P_(4) with transition metals often leads to formation of complexes[M_(x)P_(y)]_(n) associated with the deactivation of transition *** breakthrough showcases the potential of transition-metal-catalyzed reactions in elemental phosphorus chemistry.

关键词： white phosphorus P-C bonds dialkyl phosphites aminophosphonates pyrophosphates

Förster resonance energy transfer reveals phillygenin and swertiamarin concurrently target AKT on different binding domains to increase the anti-inflammatory effect

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Chinese chemical Letters 2024年第5期35卷 207-212页

作者： Xiaoyao Ma Jinling Zhang Ge Fang He Gao Jie Gao Li Fu Yuanyuan Hou Gang Bai State Key Laboratory of Medicinal chemical biology College of Pharmacy and Tianjin Key Laboratory of Molecular Drug ResearchNankai UniversityTianjin 300000China College of Life Health Dalian UniversityDalian 116622China Dalian Fusheng pharmaceutical Co. Ltd.Dalian 116000China

The clinical benefit of combination therapy is significant,but it is not easy to define the mechanism of complexity and *** studies illustrate that phillygenin(Phi)binds in the allosteric inhibit pocket of protein kinase B(AKT),and swertiamarin(Swe)acts on the pleckstrin homology(PH)domain of ***,the combined synergistic effect of relieving the inflammatory response has yet to be *** on high sensitivity,specificity and fast-responsibility fluorescent sensors,the Förster resonance energy transfer(FRET)technique offers a route to provide clear insights into physiological and pathological *** the study,molecular docking,the fluorescent probes of Phi and Swe for FRET were designed and *** analysis shown that Swe and Phi concurrently acted on the PH domain and allosterically inhibited pocket of AKT,*** combination of Swe and Phi significantly increased the heat stability of AKT and decreased protease-induced *** lipopolysaccharides(LPS)-induced mice and cells,the combination arrested AKT activation,nuclear factor kappa-B(NF-κB)phosphorylation,and the expression of tumor necrosis factor-α(TNF-α),interleukin(IL)-6 and *** conclusion,FRET revealed Phi and Swe concurrently targeted AKT on different domains and the combination of Phi and Swe enhanced the anti-inflammatory effect.

关键词： FRET Swertiamarin Phillygenin AKT Anti-inflammation Combinatorial drug

chemical biology investigation of a triple-action,smart-decomposition antimicrobial booster based-combination therapy against“ESKAPE”pathogens

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Science China Chemistry 2024年第9期67卷 3071-3082页

作者： Min Wang Huangsheng Pu Yangfan Xu Chenxuan Wu Yuanxin Gu Qingyun Cai Guoxing Yin Peng Yin Chunhui Zhang Wing-Leung Wong Muyang Wan Yugang Bai Xinxin Feng State Key Laboratory of Chem-/Bio-Sensing and Chemometrics Hunan Provincial Key Laboratory of Biomacromolecular Chemical Biologyand School of Chemistry and Chemical EngineeringHunan UniversityChangsha 410082China College of biology Hunan UniversityChangsha 410082China College of Advanced Interdisciplinary Studies&Hunan Provincial Key Laboratory of Novel Nano Optoelectronic Information Materials and Devices National University of Defense TechnologyChangsha 410073China Nanhu Laser Laboratory National University of Defense TechnologyChangsha 410073China Key Laboratory of chemical biology and Traditional Chinese Medicine Research(Ministry of Education) College of Chemistry and Chemical EngineeringHunan Normal UniversityChangsha 410081China State Key Laboratory of chemical biology and Drug Discovery Department of Applied Biology and Chemical TechnologyThe Hong Kong Polytechnic UniversityHong Kong SAR 999077China Hunan Provincial Key Laboratory of Anti-Resistance Microbial Drugs The Third Hospital of Changsha(The Affiliated Changsha Hospital of Hunan University)Changsha 410015China

The global antibiotic resistance crisis necessitates urgent *** innovative approach involves potentiating antibiotics and non-antibiotic drugs with adjuvants or boosters.A major drawback of these membrane-active boosters is their limited biocompatibility,as they struggle to differentiate between prokaryotic and eukaryotic *** study reports the chemical biology investigation of a dual-action oligoamidine(OA1)booster with a glutathione-triggered decomposition ***1,when combined with other antimicrobial molecules,exhibits a triple-targeting mechanism including cell membrane disruption,DNA targeting,and intracellular enzyme *** multi-targeting mechanism not only enhances the in vitro and in vivo eradication of antibiotic-resistant“ESKAPE”pathogens,but also suppresses the development of bacterial ***,OA1 maintains its activity in bacterial cells by creating an oxidative environment,while it quickly decomposes in mammalian cells due to high glutathione *** mechanistic insights and design principles may provide a feasible approach to develop novel antimicrobial agents and effective anti-resistance combination therapies.

关键词： antimicrobial booster oligoamidine membrane disruption DNA targeting triggered degradation anti-resistance