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Journal of Environmental Sciences 2024年第2期136卷 512-522页

作者： Xinhang Du Wenhua Tong Xinyu Zhou Jia Luo Yuqiu Liu Yabo Wang Panyu Li Yongkui Zhang Department of pharmaceutical&Biological engineering School of Chemical EngineeringSichuan UniversityChengdu 610065China

Perfluoropolyether(PFPE)lubricants are a kind of high-molecular polymer with many excellent ***,the use of PFPEs in the nuclear industry can lead to partial decomposition and carrying radionuclides,resulting in a large amount of radioactive waste PFPE lubricants ***,radioactive waste PFPE lubricants are difficult to be effectively treated due to their high stability,the risk of possible leakage of radionuclides,and hypertoxic fluorine-containing *** this study,without any precedent,a strategy of Mn O_(2)-catalyzed decomposition and Na_(2)CO_(3)-immobilized conversion was proposed for PFPE lubricant decomposition and fluorine immobilization simultaneously based on the Lewis acid-base and oxygen vacancies concept.A high fluorine conversion efficiency of 95.4%was ***,the mechanism of decomposition suggested that Mn O_(2)mainly provided Lewis acid sites and attacked the(basic)fluorine or oxygen atoms in PFPE *** decomposition of PFPE chains was proceed down and volatile fluorine-containing gas was released by partial electron transfer,intramolecular disproportionation reaction,and unzipping ***,gas by-products could be further oxidized and then immobilized into fluoride salts by carbonate solid ***,this study provides a simple,safe,and potentially practical strategy for the harmless conversion of refractory fluorinated organic wastes,especially perfluoropolymers.

关键词： Perfluoropolyether lubricants Catalyzed decomposition Fluorine-containing gas Immobilized conversion Fluoride

Pathogenic contribution of cholesteryl ester accumulation in the brain to neurodegenerative disorders

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Neural Regeneration Research 2024年第10期19卷 2099-2100页

作者： Michiko Shirane Department of Molecular biology Graduate School of Pharmaceutical SciencesNagoya City UniversityNagoyaJapan

Cholesteryl esters(CEs) have been increasingly implicated in neurodegenerative disorders such as Alzheimer's disease(AD).Alois Alzheimer noted three prominent neuropathologic features in his original analysis of the AD brain:senile plaques,neurofibrillary tangles,and lipid granule *** plaques,which are aggregates of amyloid-beta(Aβ),and neurofibrillary tangles,which are aggregates of phosphorylated tau,have been regarded as more consistent characteristics of the AD brain compared with lipid granule accumulation and thus have been studied more intensively(Foley,2010).

关键词： esters ester cholesteryl

Advancing ophthalmic delivery of flurbiprofen via synergistic chiral resolution and ion-pairing strategies

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Asian Journal of pharmaceutical Sciences 2024年第3期19卷 181-193页

作者： Zhining Ma Yuequan Wang Huiyang He Tong Liu Qikun Jiang Xiaohong Hou school of Pharmacy Shenyang Pharmaceutical University Wuya College of Innovation Shenyang Pharmaceutical University Liaoning Provincial Institute of Drug Inspection and Testing school of pharmaceutical engineering Shenyang Pharmaceutical University

Flurbiprofen （FB）,a nonsteroidal anti-inflammatory drug,is widely employed in treating ocular inflammation owing to its remarkable anti-inflammatory ***,the racemic nature of its commercially available formulation （Ocufen?） limits the full potential of its therapeutic activity,as the （S）-enantiomer is responsible for the desired antiinflammatory ***,the limited corneal permeability of FB significantly restricts its *** this study,we successfully separated the chiral isomers of FB to obtain the highly active （S）-***,utilizing ion-pairing technology,we coupled （S）-FB with various counter-ions,such as sodium,diethylamine,trimethamine（TMA）,and l-arginine,to enhance its ocular bioavailability.A comprehensive evaluation encompassed balanced solubility,octanol-water partition coefficient,corneal permeability,ocular pharmacokinetics,tissue distribution,and in vivo ocular anti-inflammatory activity of each chiral isomer *** the various formulations,S-FBTMA exhibited superior water solubility （about 1–12 mg/ml）,lipid solubility (1owpharmaceutical enterprises focused on drug development with a valuable avenue for improving therapeutic outcomes.

关键词： Flurbiprofen Anti-inflammatory Ophthalmic delivery Chiral resolution Ion-pairing

Immune checkpoint inhibitors:breakthroughs in cancer treatment

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Cancer biology & Medicine 2024年第6期21卷 451-472页

作者： Xueqing Kong Jinyi Zhang Shuwei Chen Xianyang Wang Qing Xi Han Shen Rongxin Zhang Laboratory of Immunology and Inflammation School of Life Sciences and BiopharmaceuticsGuangdong Pharmaceutical UniversityGuangzhou 510006China Department of biology School of Life Sciences and BiopharmaceuticsGuangdong Pharmaceutical UniversityGuangzhou 510006China

Over the past two decades,immunotherapies have increasingly been considered as first-line treatments for most *** such treatment is immune checkpoint blockade(ICB),which has demonstrated promising results against various solid tumors in clinical *** antibodies(mAbs)are currently available as immune checkpoint inhibitors(ICIs).These ICIs target specific immune checkpoints,including cytotoxic T-lymphocyte-associated antigen-4(CTLA-4)and programmed cell death protein 1(PD-1).Clinical trial results strongly support the feasibility of this immunotherapeutic ***,a substantial proportion of patients with cancer develop resistance or tolerance to treatment,owing to tumor immune evasion mechanisms that counteract the host immune ***,substantial research focus has been aimed at identifying additional ICIs or synergistic inhibitory receptors to enhance the effectiveness of anti-PD-1,anti-programmed cell death ligand 1(anti-PD-L1),and anti-CTLA-4 ***,several immune checkpoint molecular targets have been identified,such as T cell immunoreceptor with Ig and ITIM domains(TIGIT),mucin domain containing-3(TIM-3),lymphocyte activation gene-3(LAG-3),V-domain immunoglobulin suppressor of T cell activation(VISTA),B and T lymphocyte attenuator(BTLA),and signal-regulatory proteinα(SIRPα).Functional m Abs targeting these molecules are under ***-4,PD-1/PD-L1,and other recently discovered immune checkpoint proteins with distinct structures are at the forefront of *** review discusses these structures,as well as clinical progress in m Abs targeting these immune checkpoint molecules and their potential applications.

关键词： Immunotherapy cancer ICIs PD-1 CTLA-4

Inorganic virus-like nanoparticles for biomedical applications:a minireview

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未来食品学报(英文) 2024年第1期4卷 71-82页

作者： Liying Zhao Jiahong Zhou Dawei Deng Department of pharmaceutical engineering School of EngineeringChina Pharmaceutical UniversityNanjing 211198China Department of Biomedical engineering School of EngineeringChina Pharmaceutical UniversityNanjing 211198China

Nature has the ingenious capability to design spiky topological features at the macro-and nanoscales,which exhibits fascinating interface adhesive properties by means of multivalent *** a biomimetic approach,such as nanoscale virus particles are highly infectious toward host cells,a range of organic and inorganic spiky particles(virus-like nanostructures)have been precisely engineered for diverse biomedical ***,organic virus-like particles(VLPs)derived from viral capsids(often termed as virosomes)have been extensively studied and reviewed,but concomitant concerns regarding immunogenicity and risks of mutagenesis limit clinical potential of organic *** contrast,inorganic VLPs(viral-mimicking topography)possess fascinating physicochemical characteristics,such as excellent electrical,optical,magnetic,mechanical and catalytic properties,which make them particularly suitable for biomedical ***,there is no comprehensive review related to inorganic VLPs engineered with non-viral shell for biomedical ***,in this review,we present a brief overview on inorganic VLPs,followed by summarizing the construction and properties of virus-like nanostructures,as well as the mechanisms of nano-bio interface interactions initiated by spiky ***,we focus on the recent advances of VLPs for biomedical applications(including biosensing,antibacterial therapy and cancer treatment).Finally,the future outlook and emerging challenges will be *** review aims to provide future scope of the rational design of inorganic non-viral vectors,especially with respect to gene-based therapy platforms.

关键词： Nanotopography Virus-like Spike Inorganic particles Biomedical applications

Controllable Construction of Vinyl Sulfones and β-Keto Selenosulfones via Selective Oxidative Sulfonylation of Alkenes

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Chinese Journal of Chemistry 2024年第12期42卷 1367-1372页

作者： Xiang Liu Yuan Zhang Yi Zheng Changfeng Huang Hua Cao school of Chemistry and Chemical engineering Guangdong Pharmaceutical UniversityZhongshanGuangdong 528458China

Comprehensive Summary The selective oxidative sulfonylation of alkenes with selenium sulfonate depended on the reaction *** electrochemical C—H sulfonylation proceeded smoothly to afford(E)-vinyl sulfones with good selectivity in an undivided cell without external *** aerobic trifunctionalization of alkenes occurred in the presence of KI in the air,which providesβ-keto selenosulfones via the formation of C—O,C—S,and C—Se bonds in *** control experiments,a plausible mechanism is proposed to rationalize the experimental results.

关键词： Synthetic methods Alkenes Difunctionalization Selenylation Sulfonylation

Tumor-targeted metabolic inhibitor prodrug labelled with cyanine dyes enhances immunoprevention of lung cancer

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Acta Pharmaceutica Sinica B 2024年第2期14卷 751-764页

作者： Wen Li Jiali Huang Chen Shen Weiye Jiang Xi Yang Jingxuan Huang Yueqing Gu Zhiyu Li Yi Ma Jinlei Bian State Key Laboratory of Natural Medicines China Pharmaceutical UniversityNanjing 210009China Department of Biomedical engineering School of EngineeringChina Pharmaceutical UniversityNanjing 210009China Jiangsu Key Laboratory of Drug Design and Optimization Department of Medicinal ChemistrySchool of PharmacyChina Pharmaceutical UniversityNanjing 210009China

Recent progress in targeted metabolic therapy of cancer has been limited by the considerable toxicity associated with such *** address this challenge,we developed a smart theranostic prodrug system that combines a fluorophore and an anticancer drug,specifically 6-diazo-5-oxo-L-norleucine(DON),using a thioketal linkage(TK).This system enables imaging,chemotherapy,photodynamic therapy,and on-demand drug release upon radiation *** optimized prodrug,DON-TK-BM3,incorporating cyanine dyes as the fluorophore,displayed potent reactive oxygen species release and efficient tumor cell *** the parent drug DON,DON-TK-BM3 exhibited no toxicity toward normal ***,DON-TK-BM3 demonstrated high tumor accumulation and reduced side effects,including gastrointestinal toxicity,in *** study provides a practical strategy for designing prodrugs of metabolic inhibitors with significant toxicity stemming from their lack of tissue selectivity.

关键词： Smart prodrug system Glutamineantagonists Immunotherapy Photodynamictherapy Reactive oxygen species Metabolicinhibitor Cyaninedye Non-small-cell lung cancer(NSCLC)

Thylakoid engineered M2 macrophage for sonodynamic effect promoted cell therapy of early atherosclerosis

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Nano Research 2024年第4期17卷 2919-2928页

作者： Guanghao Wu Changwen Mu Qianru Zhao Yao Lei Ran Cheng Weidong Nie Jiamin Qu Yuping Dong Ruili Yang Haiyan Xie State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesChemical Biology CenterPeking UniversityBeijing 100191China school of Materials Science and engineering Beijing Institute of TechnologyBeijing 100081China school of Life Science Beijing Institute of TechnologyBeijing 100081China school of Stomatology Peking UniversityBeijing 100081China

Atherosclerosis is the most common cause of cardiovascular diseases that contribute to the major morbidity worldwide,but still lacking of effective treatment ***,a hybrid cell is constructed for the sonodynamic effect promoted cell therapy of early atherosclerosis by fusing M2 macrophages with thylakoid(TK)*** systemic administration,the obtained TK-M2 actively accumulates in the early atherosclerotic plaques,wherein M2 macrophages relieve the cholesterol accumulation and the inflammation in the foam ***,the TK membranes decorated on the M2 macrophages exhibit both type I and type II sonodynamic effects under ultrasound(US)activation,inducing the direct apoptosis of foam *** cooperation of M2 and TK leads to significant outcome in eliminating atherosclerotic plaques without obvious side-effects,providing a new avenue for atherosclerosis treatment.

关键词： atherosclerosis thylakoid ultrasound M2 macrophage

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

Discovery of GluN2A subtype-selective N-methyl-d-aspartate(NMDA)receptor ligands

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Acta Pharmaceutica Sinica B 2024年第5期14卷 1987-2005页

作者： Liyang Jiang Na Liu Fabao Zhao Boshi Huang Dongwei Kang Peng Zhan Xinyong Liu Department of Medicinal Chemistry Key Laboratory of Chemical Biology(Ministry of Education)School of Pharmaceutical SciencesCheeloo College of MedicineShandong UniversityJinan 250012China

The N-methyl-d-aspartate(NMDA)receptors,which belong to the ionotropic Glutamate receptors,constitute a family of ligand-gated ion *** the various subtypes of NMDA receptors,the GluN1/2A subtype plays a significant role in central nervous system(CNS)*** present article aims to provide a comprehensive review of ligands targeting GluN2A-containing NMDA receptors,encompassing negative allosteric modulators(NAMs),positive allosteric modulators(PAMs)and competitive ***,the ligands’structure–activity relationships(SARs)and the binding models of representative ligands are also discussed,providing valuable insights for the clinical rational design of effective drugs targeting CNS diseases.

关键词： NMDA receptors GluN2A subtype Subtype-selective ligands SARs Protein ligand interactions