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Chinese Journal of Chemistry 2024年第2期42卷 157-163页

作者： Weicai Li Lu Tan Yijun Chen Rui Liu Zhongyu Qi Shixuan Yuan Zhanwen Huang Siping Wei Xi Du Dong Yi Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province School of PharmacySouthwest Medical UniversityLuzhouSichuan 646000China Department of Chemistry School of Basic Medical ScienceSouthwest Medical UniversityLuzhouSichuan 646000China Department of pharmacy Affiliated HospitalSouthwest Medical UniversityLuzhouSichuan 646000China

Tetralin-1-carboxamides are frequently incorporated in myriad medicinally important ***,their existing synthetic routes not only suffer from some drawbacks such as tedious procedures,harsh reaction conditions,narrow substrate scope,low yields,and environmental problems,but are also based upon the elaboration of uneasily available non-linear tetralin ***,we describe a metal-and additive-free visible light-induced[4+2]annulation of two simple linear starting materials,namely acrylamides and 2-benzyl-2-bromocarbonyls,through a cascade C(sp^(3))-Br/C(sp^(2))-H bond cleavage,double C-C bond formation,and aromatization *** developed protocol provides a convenient,efficient,and green approach to a variety of tetralin-1-carboxamide derivatives with good functional group ***,the resulting products could also undergo the Licl-mediated mono-decarboxylative cyclization process to further furnish the architecturally novel bridged polycyclic imides with excellentcis-diastereoselectivities.

关键词： Annulation Metal-free Photoredox catalysis Tetralin-1-carboxamide Cyclic imides Synthetic methods C-C coupling Radical reactions Reaction mechanisms

Paclitaxel-lipid prodrug liposomes for improved drug delivery and breast carcinoma therapy

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Chinese Chemical Letters 2024年第2期35卷 335-340页

作者： Xin Wu Xinmei Chen Xinyu Wang Haisheng He Jianming Chen Wei Wu Key Laboratory of Smart Drug Delivery of MOE School of PharmacyFudan UniversityShanghai 201203China Department of pharmacy Fujian University of Traditional Chinese MedicineFuzhou 350122China Shanghai Wei Er Lab Shanghai 201707China Shanghai Skin Disease Hospital Tongji University School of MedicineShanghai 200443China

Paclitaxel(PTX)is widely applied for the treatment of unresectable and metastasis breast carcinoma as well as other cancers,whereas its efficacy is always impeded by poor *** are one kind of the most successful drug carriers which are capable of solubilizing PTX and improving patients’tolerance owing to excellent biocompatibility and ***,poor compatibility between PTX and liposomes compromises the stability,drug loading and anti-tumor capacity of liposomal *** address this issue,three lipids with various chain lengths,namely,myristic acid(MA,14C),palmitic acid(PA,16C)and stearic acid(SA,18C),were conjugated to PTX via ester bonds and the synthesized prodrugs with high lipophilicity were further formulated into liposomes,*** liposomes show high stability and drug loadings,as well as sustained drug *** chain lengths of lipids are negatively correlated with drug release and enzymatic conversion rates,which further impact the pharmacokinetics,tumor accumulation,and anti-tumor efficacy of liposomal *** rapid nor slow drug release facilitates high tumor accumulation as well as anti-tumor efficacy of *** all liposomes,PTX-PA-loaded liposomes show the longest circulation and highest tumor accumulation of PTX and exert the most potent anti-tumor capacities in vivo,owing to its moderate drug release and enzymatic conversion *** its superior safety,PTX-PA liposomes hold potential for further clinical translation.

关键词： Paclitaxel Lipids Prodrugs Liposomes Drug release Chemotherapy

Patients’Knowledge, Attitude and Practices on Disposal Methods of Expired and Unused Medicines: Implication for Creation of Drug Take-Back Program

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Pharmacology & pharmacy 2024年第4期15卷 113-128页

作者： Martin Kampamba Zebedy Kalambwa Billy Chabalenge Janipher Zulu Steward Mudenda Tadious Chimombe Webrod Mufwambi Audrey Hamachila Mashebe Innocent Ngula Christabel Nang’andu Hikaambo Department of pharmacy School of Health Sciences University of Zambia Lusaka Zambia Department of Medicines Control Zambia Medicines Regulatory Authority Lusaka Zambia Department of pharmacy School of Health Sciences Levy Mwanawasa Medical University Lusaka Zambia

Background: Handling of medicines is a day-to-day activity by patients and many health care providers. However, multiple studies have brought to light inappropriate disposal methods for expired and unused medication (EUM). Improper disposal of expired and unused medicines is hazardous both to humans and the environment. Objective: This sought to measure patients’ knowledge, attitude, and practices on disposal methods of EUM. Methods: A cross-sectional study was carried out among 384 patients at three outpatient pharmacies at the University Teaching Hospitals (UTHs). The structured questionnaire was used to collect data and STAT version 15.1 was used to analyse the data. Results: 384 respondents participated in this study and, at some point, had EUM. In this study, 356 (92.7%) of the participants reported that they had never heard of a drug take-back system. Most of the participants 285 (74.2%) and 239 (62.2%) kept and donated their unused medicine, respectively. Additionally, 244 (63.5%), 212 (55.2%), and 176 (44.8%) of the participants disposed of expired medicines in the bin or garbage, flushed them in toilets or sinks, or burned them, respectively. Occupation was significantly associated with unsafe disposal of unused medicine [P-value = 0.019]. Conclusion and Relevance: Knowledge of safe disposal methods for EUM was good amongst most participants. However, used unsafe disposal methods. The majority of the participants exhibited positive attitude concerning safe disposal methods. This study highlights the need for drug-take-back program creation in Zambia.

关键词： Attitude Disposal Methods Expired Medicines Knowledge Practices Unused Medicines

Roles of Community Pharmacists in Screening and Disseminating of Information about Non-Steroidal Anti-Inflammatory Drugs Risks: Implications for Drug Safety Assessment

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Pharmacology & pharmacy 2024年第4期15卷 129-145页

作者： Martin Kampamba Progress Mulenga Steward Mudenda Billy Chabalenge Jenipher Zulu Tadius Chimombe Webrod Mufwambi Mashebe Innocent Ngula Audrey Hamachila Jimmy Hangoma Christabel Nang’andu Hikaambo Department of pharmacy School of Health Sciences University of Zambia Lusaka Zambia Department of Medicines Control Zambia Medicines Regulatory Authority Lusaka Zambia Department of pharmacy School of Health Sciences Levy Mwanawasa Medical University Lusaka Zambia

Background: The increasing use of non-steroidal anti-inflammatory drugs (NSAIDs) both on prescription and over the counter raises a major global health concern because of the risks associated with their use if no proper guidance is given by the health care provider. This study assessed the roles of community pharmacists in screening and disseminating information about the risks associated with NSAID use in Zambia. Methodology: This was a national cross-sectional study in which a structured self-administered questionnaire was administered to 245 registered community pharmacists in Zambia. Stata/BE, version 15.1 (Stata Corporation, College Station, Texas, USA) and multivariate logistic regression model was used to determine factors associated with information dissemination about ADRs of NS-NSAIDs. Results: 231 of the 245 distributed questionnaires were returned giving a response rate of 94.3%. All (100%) participating community pharmacists claimed to have practiced dispensing NSAIDs. However, only 26 (11.0%) and 71 (30.8%) regularly screened for risk factor of selective COX-2 NSAIDS (SC2-NSAIDS) and non-selective NSAIDS (NS-NSAIDs) respectively. Information dissemination on adverse drug reactions (ADRs) of SC2-NSAIDS was regularly provided by only 22 (9.5%) of pharmacists while that of NS-NSAIDs was regularly provided by 49 (21.2%). In the multivariate logistic regression model, being the owner of a pharmacy (AOR: 5.4, CI: 1.84 - 16.4) was significantly associated with information dissemination about ADRs of NS-NSAIDs while an hour increase in the working hours per day (AOR: 0.9, CI: 0.64 - 0.95) was associated with less likelihood of information dissemination. Conclusion: Pharmacists working in community pharmacies in Zambia did not regularly screen and disseminate information about the risks associated with NSAID use. Therefore, pharmacists should be able to screen and monitor patients at risk and be aware of the majority of risk factors while dispensing NSAIDs to m

关键词： Community Pharmacists Non-Steroidal Anti-Inflammatory Drug Risk Screening

Computational fluid dynamics simulation and experimental study on mixing performance of a three-dimensional circular cyclone-type microreactor

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Chinese Chemical Letters 2024年第4期35卷 382-388页

作者： Shiyu Hou Maolin Sun Liming Cao Chaoming Liang Jiaxin Yang Xinggui Zhou Jinxing Ye Ruihua Cheng school of Chemical Engineering East China University of Science and TechnologyShanghai 200237China school of Biomedical and Pharmaceutical Sciences Guangdong University of TechnologyGuangzhou 510006China school of pharmacy East China University of Science and TechnologyShanghai 200237China

Microchannels enable the fast and efficient mixing of multiphase *** this study, a millimeter-scale three-dimensional(3D) circular cyclone-type microreactor was designed for the *** flow characteristics and mixing intensity were simulated by computational fluid dynamics simulations at a flow rate range of 12–96 m L/min using a water/ethyl acetate *** the 3D variable-diameter structure,the microreactor induced paired opposite vortices and abruptly changed the local pressure to achieve a stable turbulent effect within the theoretical range of laminar *** injection simulations indicated that sufficient mixing units successfully promote fluid ***-coupling experiments showed a segregation index of X_S= 0.00,039 within a residence time of 9 *** experiments on the nbutanol/succinic acid/water system showed that the 3D circular cyclone-type microreactor achieved 100%extraction efficiency(E) in 4.25 s, and the overall volume mass transfer coefficient(K_La) reached 0.05–1.5s^(-1) in 12–96 m L/*** isolated yield of the phase transfer alkylation and oxidation reactions in the 3D circular cyclone-type microreactor achieved 99% within 36 s, which was superior to the coil microreactor and batch reactor.

关键词： Microfluidics Passive microreactor CFD simulation Extraction Liquid-liquid biphase reaction

Multifunctional nanoparticle-mediated combining therapy for human diseases

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Signal Transduction and Targeted Therapy 2024年第2期9卷 343-375页

作者： Xiaotong Li Xiuju Peng Makhloufi Zoulikha George Frimpong Boafo Kosheli Thapa Magar Yanmin Ju Wei He school of pharmacy China Pharmaceutical UniversityNanjing 2111198PR China Xiangya school of Pharmaceutical Sciences Central South UniversityChangsha 410013PR China Shanghai Skin Disease Hospital Tongji University School of MedicineShanghai 200443China

Combining existing drug therapy is essential in developing new therapeutic agents in disease prevention and *** preclinical investigations,combined effect of certain known drugs has been well established in treating extensive human *** to synergistic effects by targeting various disease pathways and advantages,such as reduced administration dose,decreased toxicity,and alleviated drug resistance,combinatorial treatment is now being pursued by delivering therapeutic agents to combat major clinical illnesses,such as cancer,atherosclerosis,pulmonary hypertension,myocarditis,rheumatoid arthritis,inflammatory bowel disease,metabolic disorders and neurodegenerative *** therapy involves combining or co-delivering two or more drugs for treating a specific ***(NP)-mediated drug delivery systems,i.e.,liposomal NPs,polymeric NPs and nanocrystals,are of great interest in combinatorial therapy for a wide range of disorders due to targeted drug delivery,extended drug release,and higher drug stability to avoid rapid clearance at infected *** review summarizes various targets of diseases,preclinical or clinically approved drug combinations and the development of multifunctional NPs for combining therapy and emphasizes combinatorial therapeutic strategies based on drug delivery for treating severe clinical ***,we discuss the challenging of developing NP-codelivery and translation and provide potential approaches to address the *** review offers a comprehensive overview for recent cutting-edge and challenging in developing NP-mediated combination therapy for human diseases.

关键词： drugs diseases prevention

Metal-organic framework and its composites modulate macrophage polarization in the treatment of inflammatory diseases

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Chinese Chemical Letters 2024年第5期35卷 45-56页

作者： Feifei Wang Hang Yao Xinyue Wu Yijian Tang Yang Bai Hui Chong Huan Pang school of Chemistry and Chemical Engineering Yangzhou UniversityYangzhou 225002China school of pharmacy Changzhou UniversityChangzhou 213164China State Key Laboratory of Coordination Chemistry Nanjing UniversityNanjing 210023China

Metal-organic framework(MOF)is a periodic sexual network structure with large surface area and high porosity,which is assembled by inorganic nodes and organic ligands through coordinate covalent *** have the advantages of controllable pore size and shape,large specific surface area,easy modification and more active *** addition,MOF based nanoenzymes display excellent enzyme catalytic activity due to their special structure and multiple exposed metal active sites,controlling the production of reactive oxygen species(ROS)in cells or the body,and thus regulating the polarization of *** article reviews the mechanism of MOF material regulating macrophage polarization and the function of macrophages with different *** utilizing the excellent properties of MOFs and the advantages of combining them with bioactive materials,we have discovered their excellent applications in the treatment of inflammatory ***,we discussed the current challenges and prospects faced by MOF based composite *** expect that the research in this developing field will play a more important role in combating inflammatory diseases in the field of nanomedicine.

关键词： Metal-organic framework Inflammation Macrophage polarization Reactive oxygen species Nanozyme activity

Boswellic acids: a review on its pharmacological properties, molecular mechanism and bioavailability

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Traditional Medicine Research 2024年第10期9卷 64-74页

作者： Na Cui Ming-Jie Li Yi-Wen Wang Qian Meng Ya-Jun Shi Yi Ding Department of pharmacy 3201 HospitalHanzhong 723000China Department of pharmacy Xijing HospitalFourth Military Medical UniversityXi’an 710032China school of pharmacy Shaanxi University of Traditional Chinese medicineXianyang 712046China

Boswellic acids is a general term for a series of pentacyclic triterpenoid compounds that are isolated from the oleogin resin of the Boswellia genus and serve as the main active *** exhibits a wide range of biological activities,such as anti-inflammatory,anti-cancer,antibacterial,antiviral,hepatoprotective,neuroprotective,anti-diabetic,and anti-thrombotic *** a result,it has gained significant recognition among practitioners of traditional Chinese and Indian *** biological effects may be associated with multiple molecular targets and signal transduction ***,the poor pharmacokinetic properties of the substance lead to lower bioavailability,which affects its *** address this issue,scientists have proposed a number of strategies,such as solid dispersions,phytosome®technologies,and novel drug delivery *** article aims to provide a comprehensive overview for boswellic acids on the phytochemistry,molecular mechanisms,potential therapeutic applications,and strategies to improve bioavailability.

关键词： boswellic acids molecular mechanism pharmacological properties bioavailability

Aloe emodin promotes mucosal healing by modifying the differentiation fate of enteroendocrine cells via regulating cellular free fatty acid sensitivity

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Acta Pharmaceutica Sinica B 2024年第9期14卷 3964-3982页

作者： Weilian Bao Jiaren Lyu Guize Feng Linfeng Guo Dian Zhao Keyuan You Yang Liu Haidong Li Peng Du Daofeng Chen Xiaoyan Shen Department of Pharmacology&the Key Laboratory of Smart Drug Delivery Ministry of Education School of PharmacyFudan UniversityShanghai 201210China Department of Natural Medicine School of PharmacyFudan UniversityShanghai 201210China Department of Colorectal and Anal Surgery Xinhua HospitalShanghai Jiao Tong University School of MedicineShanghai 200092China Shanghai Colorectal Cancer Research Center Shanghai 200092China

The proper differentiation and reorganization of the intestinal epithelial cell population is critical to mucosal regeneration post *** retaining cells(LRCs)expressing SRY-box transcription factor 9(SOX9)promote epithelial repair by replenishing LGR5 t intestinal stem cells(ISCs).While,LRCs are also considered precursor cells for enteroendocrine cells(EECs)which exacerbate mucosal damage in inflammatory bowel disease(IBD).The factors that determine LRC-EEC differentiation and the effect of intervening in LRC-EEC differentiation on IBD remain *** this study,we investigated the effects of a natural anthraquinone called aloe emodin(derived from the Chinese herb rhubarb)on mucosal healing in IBD *** findings demonstrated that aloe emodin effectively interfered with the differentiation to EECs and preserved a higher number of SOX9t LRCs,thereby promoting mucosal ***,we discovered that aloe emodin acted as an antagonist of free fatty acid receptors(FFAR1),suppressing the FFAR1-mediated Gbg/serine/threonine-protein kinase(AKT)pathway and promoting the translocation of forkhead box protein O1(FOXO1)into the nucleus,ultimately resulting in the intervention of differentiation *** findings reveal the effect of free fatty acid accessibility on EEC differentiation and introduce a strategy for promoting mucosal healing in IBD by regulating the FFAR1/AKT/FOXO1 signaling pathway.

关键词： LRCs ISCs EECs IBD SOX9 Aloe emodin FFAR1 FOXO1

Cytokine Storm:The Novel Mechanism for Sleep Deprivation-induced Multiple Organ Dysfunction Syndrome

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Neuroscience Bulletin 2024年第7期40卷 1031-1033页

作者： Liwen Wang Huimei Liu Li Qin Lanfang Li Institute of pharmacy and Pharmacology University of South ChinaHengyang 421001China Hengyang Medical school University of South ChinaHengyang 421001China

It is well known that sleep is one of the inevitable activities of daily living and it is one of the most important factors contributing to human *** in mammals is a cyclic occurrence of two distinct states,rapid eye ... 详细信息

关键词： NREM Sleep movement