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Asian Pacific Journal of Tropical Medicine 2024年第2期17卷 47-60页

作者： Raghunath Hazra Amrita Kar Santanu Kar Mahapatra Department of Paramedical and allied health sciences Biodiversity and Environmental Studies Research CentreMidnapore City CollegeKuturiyaBhadutalaPaschim Medinipur-721129West BengalIndia

Visceral leishmaniasis(VL)is a neglected tropical disease,and this review has summarized the current treatment scenario and its *** also highlights alternative approaches used by research groups in India and around the world to develop cutting-edge and potent anti-leishmanial *** though numerous medications could be utilized to treat VL,the limitations of current treatments including their toxicity,cost,route of administration,and duration of doses,have contributed to the emergence of *** therapy might be a better option due to its shorter duration,easier route of administration,and ability to extend the lifespan of individual ***,there is a risk of not delivering both the drugs to the target site together,which can be overcome by the liposomal entrapment of those drugs and at a time knock an opportunity to reduce the dosage of amphotericin b if the combination drug provides a synergistic effect with ***,this review presents a novel strategy to fight against VL by introducing dual drug-loaded liposomes.

关键词： Visceral leishmaniasis Liposomal anti-leishmanial drug Dual drug liposome

Persicaria lanigera (Polygonaceae) leaf extract exhibits antiulcerogenic and antiproliferative activities against acetic acid-induced ulcerative colitis and cotton pellet-induced granuloma tissue in rats

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Asian Pacific Journal of Tropical biomedicine 2024年第7期14卷 269-278页

作者： Meshack Antwi-Adjei Ernest Obese Emmanuel Awintiig Adakudugu benjamin Aboagye Daniel Anokwah Akua Afriyie Karikari Roberta Antwi-Adjei Elvis Ofori Ameyaw Department of Pharmacology School of Medical SciencesUniversity of Cape CoastCape CoastGhana Department of Pharmacotherapeutics and pharmacy Practice School of Pharmacy and Pharmaceutical SciencesUniversity of Cape CoastCape CoastGhana Department of Forensic sciences School of Biological SciencesUniversity of Cape CoastCape CoastGhana Department of Pharmacognosy and Herbal Medicine School of Pharmacy and Pharmaceutical SciencesUniversity of Cape CoastCape CoastGhana Department of biomedical sciences School of Allied Health SciencesCollege of Agriculture and Natural SciencesUniversity of Cape CoastCape CoastGhana

Objective:To assess the effect of leaf extract of Persicaria lanigera on cotton pellet-induced granuloma tissue formation and acetic acid-induced ulcerative ***:Rats were randomly divided into six groups:normal control,negative control,positive control(dexamethasone or sulfasalazine)as well as Persicaria lanigera(100-600 mg/kg)-treated *** effects of the extracts on body weight,antioxidant,and hematological parameters,as well as mast cell proliferation,were *** addition,a histological evaluation was ***:Persicaria lanigera extract significantly decreased the mean exudate amount and suppressed granuloma tissue formation in a concentration-dependent manner in rats(Pct significantly increased body weight,improved hematological profile,reduced the disease activity index score and malondialdehyde level,as well as enhanced catalase and superoxide dismutase activities(Pcal evaluation showed Persicaria lanigera extract alleviated acetic acid-induced colonic damages,as evidenced by decreased cell necrosis,edema,and inflammatory cell ***:Persicaria lanigera extract possesses antiproliferative,antioxidative,and anti-colitis ***,its underlying mechanisms of action need further investigation.

关键词： colitis Persicaria lanigera Antioxidant cotton pellets Mast cells Granuloma tissue formation

Tetramic acid-motif natural products from a marine fungus Tolypocladium cylindrosporum Fb06 and their anti-Parkinson activities

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Marine Life Science & Technology 2024年第1期6卷 84-92页

作者： Yuna Jung chaesun Kwon Taeyeon Kim Jin Woo Lee Min-Kyoo Shin Sang Hee Shim Natural Products Research Institute College of PharmacySeoul National UniversitySeoul 08826Republic of Korea college of pharmacy and Research Institute of Pharmaceutical sciences Seoul National UniversitySeoul 08826Republic of Korea college of pharmacy Duksung Women’s UniversitySeoul 01369Republic of Korea

Tetramic acid-containing natural products are attracting significantly increasing attention from biologists and chemists due to their intriguing structures and biological *** the present study,two new tetramic acid alkaloids tolypyridone I(1)and tolypyridone J(2),together with five known ones(3–7),were isolated from cultures of a marine fungus Tolypocladium cylindrosporum Fb06 isolate obtained from a marine sediment in beaufort sea of North *** structures were elucidated using 1D,2D NMR,and *** configurations were established on the basis of 1H coupling constants,ROESY correlations and DP4 *** 2 was isolated as mixtures of rotational isomers with c-3 to c-7 axis between 4-hydroxy-2-pyridone and 1-ethyl-3,5-dimethylcyclohexane,hindering *** our unbiased screening to discover neuroprotective compounds in an in vitro Parkinson’s disease(PD)model,SH-SY5Y dopaminergic cells were treated with isolated compounds followed by treatment with 1-methyl-4-phenylpyridinium(MPP^(+)),a parkinsonian *** tested compounds,F-14329(7)significantly protected cells from MPP^(+)-induced ***^(+)-mediated cell death is known to be related to the regulation of bcl-2 family proteins,specifically the down-regulation of anti-apoptotic bcl-2 and the up-regulation of pro-apoptotic bax *** with 2 mmol/L of MPP^(+)for 24 h significantly reduced bcl-2 levels compared to control treated with ***,treatment with F-14329(7)attenuated such *** study demonstrates that tetramic acid-motif compounds could be potential lead compounds for treating PD.

关键词： Tolypocladium cylindrosporum Tetramic acid Tolypyridone Parkinson’s disease

In silico identification of antiviral compounds for the treatment of chikungunya virus infection:qsar modelling and md simulation analysis

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Medicine in Novel Technology and Devices 2024年第2期22卷 102-114页

作者： Hayder M Abdulhamza Muthanna S.Farhan Sara.S Hassan Hany Aqeel Al-Hussainy Amjad Ibrahim Oriabi Department of pharmacy Kut University CollegeAlkutWasit52001Iraq Department of Pharmaceutical chemistry College of PharmacyUniversity of BaghdadBaghdadIraq Al-Manara college for Medical sciences Department of PharmacyIraq Department of pharmacy Hilla University CollegeBabylonIraq dr Hany Akeel Institute Iraqi Medical Research CenterBaghdad10001Iraq

chikungunya virus(cHIKV),transmitted by arthropods,has gained global recognition for its impact on public *** has expanded globally,including Africa,Asia,and the Indian subcontinent,and has a helicase protein in its genome that is crucial for its ***,the study targeted the helicase protein of cHIKV with 745 antiviral compounds using an ML-based QSAR model and molecular *** binders(5279172,78161839,6474310,and 5330286)were selected for MD simulation based on the control(Silvestrol).All compounds had the highest binding scores,with 78161839 showing the most consistent RMSD and the least conformational variation,indicating high *** also showed the lowest binding free energy(ΔG¼31.31 kcal/mol),indicating energetically favourable *** and FEL also depicted the stable complex confirmation of the protein and 78161839 complex during the 100 ns ***,this study aimed to identify helicase function antiviral binders that could be experimentally tested for treating cHIKV.

关键词： chikungunya virus Machine learning based QSAR Molecular dynamic solution Helicase

Neurogenic potential of NG2 in neurotrauma:a systematic review

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Neural Regeneration Research 2024年第12期19卷 2673-2683页

作者： Yuri R.Rigo Radharani benvenutti Luis V.Portela Nathan R.Strogulski Departamento de bioquímica Instituto de Ciências Básicas da SaúdeUniversidade Federal do Rio Grande do Sul(UFRGS)Porto AlegreBrazil School of pharmacy and biomolecular sciences RCSI University of Medicine and Health SciencesDublinIreland School of biochemistry and Immunology Trinity Biomedical Sciences InstituteTrinity College DublinUniversity of DublinDublinIreland

Regenerative approaches towards neuronal loss following traumatic brain or spinal cord injury have long been considered a dogma in neuroscience and remain a cutting-edge area of *** is reflected in a large disparity between the number of studies investigating primary and secondary injury as therapeutic to rgets in spinal co rd and traumatic brain *** advances in biotechnology may have the potential to reshape the current state-of-the-art and bring focus to primary injury neurotrauma *** studies using neural-glial factor/antigen 2(NG2)cells indicate that they may differentiate into neurons even in the developed *** these cells show great potential to play a regenerative role,studies have been conducted to test various manipulations in neurotrauma models aimed at eliciting a neurogenic response from *** the present study,we systematically reviewed the experimental protocols and findings described in the scientific literature,which were peer-reviewed original research articles(1)describing preclinical experimental studies,(2)investigating NG2 cells,(3)associated with neurogenesis and neurotrauma,and(4)in vitro and/or in vivo,available in PubMed/MEDLINE,Web of Science or ScOPUS,from 1998 to ***,we have reviewed a total of 1504 papers,and summarized findings that ultimately suggest that NG2 cells possess an inducible neurogenic potential in animal models and in *** also discriminate findings of NG2 neurogenesis promoted by different pharmacological and genetic approaches over functional and biochemical outcomes of traumatic brain injury and spinal co rd injury models,and provide mounting evidence for the potential benefits of manipulated NG2 cell ex vivo transplantation in primary injury *** findings indicate the feasibility of NG2 cell neurogenesis strategies and add new players in the development of therapeutic alternatives for neurotrauma.

关键词： neural-glial antigen 2 neural-glial factor 2 neuron differentiation NG2 cell regeneration spinal cord injury(ScI) traumatic brain injury(TbI)

Molecular characterization of an outbreak-involved bacillus anthracis strain confirms the spillover of anthrax from West Africa

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Infectious Diseases of Poverty 2024年第1期13卷 93-94页

作者： Shuchao Wang Roland Suluku Mohamed b.Jalloh Ahmed F.Samba baogui Jiang Yubiao Xie Doris Harding Mengyao Zhang Foday Sahr Mahmud E.Sesay James S.Squire Mohamed A.Vandi Moinina N.Kallon Shoufeng Zhang Rongliang Hu Yuee Zhao Zhiqiang Mi changchun Veterinary Research Institute Chinese Academy of Agricultural Sciences Changchun China Department of Animal sciences School of Agriculture and Food Sciences Njala University Njala Sierra Leone Department of Microbiology College of Medicine and Allied Health Sciences University of Sierra Leone Freetown Sierra Leone Ministry of Agriculture and Food sciences Freetown Sierra Leone beijing Institute of Microbiology and Epidemiology Beijing China Ministry of health and Sanitation Freetown Sierra Leone beijing Institute of biotechnology Beijing China

background Anthrax,a zoonotic disease caused by the spore-forming bacterium bacillus anthracis,remains a major global public health concern,especially in countries with limited *** Leone,a West African country historically plagued by anthrax,has almost been out of report on this disease in recent *** this study,we described a large-scale anthrax outbreak affecting both animals and humans and attempted to characterize the *** The causative agent of the animal outbreak in Port Loko District,Sierra Leone,between March and May 2022 was identified using the nanopore sequencing technique.A nationwide active surveillance was implemented from May 2022 to June 2023 to monitor the occurrence of anthrax-specific symptoms in *** cases were subsequently verified using quantitative polymerase chain ***-genome sequencing was accomplished by combining long-read and short-read sequencing *** phylogenetic analysis was performed based on the full-chromosome single nucleotide *** The outbreak in Port Loko District,Sierra Leone,led to the death of 233 animals between March 26th and May 16th,*** ruled out the initial suspicion of Anaplasma species and successfully identified *** as the causative agent of the *** a result of the government's prompt response,out of the 49 suspected human cases identifed during the one-year active surveillance,only 6 human cases tested positive,all within the frst month after the official declaration of the *** phylogenetic analysis indicated that the baSL2022 isolate responsible for the outbreak was positioned in the ***.153 clade within the TransEuroAsian group of *** We successfully identifed a large-scale anthrax outbreak in Sierra *** causative isolate of ***,baSL2022,phylogenetically bridged other lineages in ***.153 clade and neighboring genetic groups,***.144 and ***.148,

关键词： Molecular identification Anthrax bacillus anthracis Sierra Leone Phylogeny Single nucleotide polymorphism

Practical guide:Glucagon-like peptide-1 and dual glucosedependent insulinotropic polypeptide and glucagon-like peptide-1 receptor agonists in diabetes mellitus

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World Journal of Diabetes 2024年第3期15卷 331-347页

作者： Saleh Fahad Alqifari Omar Alkomi Abdullah Esmail Khadijeh Alkhawami Shahd Yousri Mohamad Ayham Muqresh Nawwarah Alharbi Abdullah A Khojah Ahmed Aljabri Abdulrahman Allahham Kousalya Prabahar Hanan Alshareef Mohammed Aldhaeefi Tariq Alrasheed Ali Alrabiah Laila A Albishi Department of pharmacy Practice Faculty of PharmacyUniversity of TabukTabuk 71491Saudi Arabia Department of clinical sciences Sulaiman Alrajhi University-College of MedicineAl Bukayriyah 52726Saudi Arabia Department of Family Medicine Dr.Soliman Fakeeh Hospital DSFHJeddah 21461Saudi Arabia Department of pharmacy Practice Faculty of PharmacyKing Abdulaziz UniversityJeddah 22252Saudi Arabia clinical and Administrative pharmacy sciences College of PharmacyHoward UniversityWashingtonDC 20059United States Department of Internal Medicine Faculty of MedicineUniversity of TabukTabuk 71491Saudi Arabia Department of pharmacy Practice Raabe College of PharmacyOhio Northern UniversityOhioOH 45810United States Department of Pediatric Faculty of MedicineUniversity of TabukTabuk 71491Saudi Arabia

Practical guide:Glucagon-like peptide-1 and dual glucosedependent insulinotropic polypeptide and glucagon-like peptide-1 receptor agonists in diabetes mellitus common second-line choice after metformin for treating *** considerations can make selecting and switching between different GLP-1 RAs *** study aims to provide a comprehensive guide for the usage of GLP-1 RAs and dual GIP and GLP-1 RAs for the management of T2DM.

关键词： Glucagon-like peptide-1 receptor agonist Diabetes mellitus Metabolic syndrome Dual glucose-dependent insulinotropic polypeptide and glucagon-like peptide-1 receptor agonist clinical practice Endocrinology

Ascophyllum nodosum and Fucus vesiculosus ameliorate restenosis via improving inflammation and regulating the PTEN/PI3K/AKT signaling pathway

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Food Science and Human Wellness 2024年第3期13卷 1711-1728页

作者： crystal Ngofi Zumbi chun-Hsu Pan Hui-Yu Huang chieh-Hsi Wu Program in clinical drug Development from Herbal Medicine College of PharmacyTaipei Medical UniversityTaipei 11031China Program in drug Discovery and Development Industry College of PharmacyTaipei Medical UniversityTaipei 11031China School of pharmacy Taipei Medical UniversityTaipei 11031China Graduate Institute of Metabolism and Obesity sciences Taipei Medical UniversityTaipei 11031China

Restenosis is a common complication following coronary *** traditional use of seaweeds for health benefits has increasingly been explored,however few studies exist reporting its protective effects on the development of restenosis and gut *** aim of this study was to investigate the potential of seaweed extracts(SE) of Ascophyllum nodosum and Fucus vesiculosus in inhibiting intimal hyperplasia in a rat model of restenosis and its underlying mechanisms in macrophages and vascular smooth muscle cells(vSMcs).16S rRNA sequencing was done to investigate the regulatory effect of SE on the gut microbiome of injured *** indicated by the results,SE significantly inhibited the progression of intimal hyperplasia in vivo,attenuated inflammation in macrophages and could inhibit the proliferation,dedifferentiation and migration of *** was observed through immunoblotting assays that treatment with SE significantly upregulated PTEN expression in macrophages and inhibited the upregulation of PI3K and AKT expression in ***,according to the 16S rRNA gene sequencing analysis,supplementation with SE modulated gut microbiota composition in injured *** conclusion,SE could ameliorate intimal hyperplasia by inhibiting inflammation and vSMcs proliferation through the regulation of the PTEN/PI3K/AKT pathway and modulating the gut microbiome.

关键词： Ascophyllum nodosum Fucus vesiculosus PTEN/PI3K/AKT Restenosis Macrophage Vascular smooth muscle cells Gut microbiota

Glucose-mediated mitochondrial reprogramming by cholesterol export at TM4SF5-enriched mitochondria-lysosome contact sites

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cancer communications 2024年第1期44卷 47-75页

作者： Ji Eon Kim So-Young Park chulhwan Kwak Yoonji Lee Dae-Geun Song Jae Woo Jung Haesong Lee Eun-Ae Shin Yangie Pinanga Kyung-hee Pyo Eun Hae Lee Wonsik Kim Soyeon Kim chang-Duck Jun Jeanho Yun Sun choi Hyun-Woo Rhee Kwang-Hyeon Liu Jung Weon Lee Department of pharmacy College of PharmacySeoul National UniversitySeoulRepublic of Korea Research Institute of Pharmaceutical sciences College of PharmacySeoul National UniversitySeoulRepublic of Korea bK21 FOUR community-based Intelligent Novel drug Discovery Education Unit College of Pharmacy and Research Institute of Pharmaceutical SciencesKyungpook National UniversityDaeguRepublic of Korea Department of chemistry Seoul National UniversitySeoulRepublic of Korea college of pharmacy Chung-Ang UniversitySeoulRepublic of Korea Natural Product Informatics Research center Korea Institute of Science and Technology(KIST)Gangneung-siGangwon-doRepublic of Korea School of Life sciences Gwangju Institute of Science and Technology(GIST)GwangjuRepublic of Korea Department of biochemistry College of MedicineDong-A UniversityBusanRepublic of Korea Global AI drug Discovery center College of Pharmacy and Graduate School of Pharmaceutical SciencesEwha Womans UniversitySeoulRepublic of Korea Interdisciplinary Program in Genetic Engineering Seoul National UniversitySeoulRepublic of Korea

background:Transmembrane 4 L six family member 5(TM4SF5)translocates subcellularly and functions metabolically,although it is unclear how intracellu-lar TM4SF5 translocation is linked to metabolic *** is thus of interests to understand how the traffic dynamics of TM4SF5 to subcellular endosomal membranes are correlated to regulatory roles of ***:Here,we explored the metabolic significance of TM4SF5 localization at mitochondria-lysosome contact sites(MLcSs),using in vitro cells and in vivo animal systems,via approaches by immunofluorescence,proximity labelling based proteomics analysis,organelle reconstitution ***:Upon extracellular glucose repletion following depletion,TM4SF5 became enriched at MLcSs via an interaction between mitochondrial FK506-binding protein 8(FKbP8)and lysosomal *** labeling showed molecular clustering of phospho-dynamic-related protein I(drP1)and certain mitophagy receptors at TM4SF5-enriched MLcSs,leading to mitochondrial fis-sion and ***4SF5 bound NPc intracellular cholesterol transporter 1(NPc1)and free cholesterol,and mediated export of lysosomal cholesterol to mitochondria,leading to impaired oxidative phosphorylation but intact tri-carboxylic acid(TcA)cycle andβ-*** mouse models,hepatocyte Tm4sf5 promoted mitophagy and cholesterol transport to mitochondria,both with positive relations to liver ***:Our findings suggested that TM4SF5-enriched MLcSs regu-late glucose catabolism by facilitating cholesterol export for mitochondrial reprogramming,presumably while hepatocellular carcinogenesis,recapitulating aspects for hepatocellular carcinoma metabolism with mitochondrial repro-gramming to support biomolecule synthesis in addition to glycolytic energetics.

关键词： cholesterol fluorescent imaging glucose catabolism hepatocellular carcinogenesis mem-brane contact sites mitochondria function mitophagy oxidative phosphorylation protein-protein interaction tetraspanin

Generic Interpretable Reaction condition Predictions with Open Reaction condition Datasets and Unsupervised Learning of Reaction center

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Research 2024年第2期2023卷 773-794页

作者： Xiaorui Wang chang-Yu Hsieh Xiaodan Yin Jike Wang Yuquan Li Yafeng Deng Dejun Jiang Zhenxing Wu Hongyan Du Hongming chen Yun Li Huanxiang Liu Yuwei Wang Pei Luo Tingjun Hou Xiaojun Yao dr.Neher's biophysics Laboratory for lnnovative drug Discovery State Key Laboratory of Quality Research in Chinese MedicineMacao Institute for Applied Research in Medicine and HealthMacao University of Science and TechnologyMacao999078China innovation Institute for Artificial Intelligence in Medicine of Zhejiang University College of Pharmaceutical SciencesZhejiang UniversityHangzhou310058China Faculty of Applied sciences Macao Polytechnic UniversityMacao999078China college of chemistry and chemical Engineering Lanzhou UniversityLanzhou730000China carbon Silicon AI Technology co. LtdHangzhouZhejiang 310018China center of chemistry and chemical biology Guangzhou Regenerative Medicine and Health Guangdong LaboratoryGuangzhou 510530China college of pharmacy Shaanxi University of Chinese MedicineXianyangShaanxi712044China

Effective synthesis planning powered by deep learning(DL)can significantly accelerate the discovery of new drugs and ***,most DL-assisted synthesis planning methods offer either none or very limited capability to recommend suitable reaction conditions(Rcs)for their reaction ***,the prediction of Rcs with a DL framework is hindered by several factors,including:(a)lack of a standardized dataset for benchmarking,(b)lack of a general prediction model with powerful representation,and(c)lack of *** address these issues,we first created 2 standardized Rc datasets covering a broad range of reaction classes and then proposed a powerful and interpretable Transformer-based Rc predictor named *** careful design of the model architecture,pretraining method,and training strategy,Parrot improved the overall top-3 prediction accuracy on catalysis,solvents,and other reagents by as much as 13.44%,compared to the best previous model on a newly curated ***,the mean absolute error of the predicted temperatures was reduced by about 4℃.Furthermore,Parrot manifests strong generalization capacity with superior cross-chemical-space prediction *** analysis indicates that Parrot effectively captures crucial chemical information and exhibits a high level of interpretability in the prediction of *** proposed model Parrot exemplifies how modern neural network architecture when appropriately pretrained can be versatile in making reliable,generalizable,and interpretable recommendation for Rcs even when the underlying training dataset may still be limited in diversity.

关键词： versatile absolute generalization