Archiv der Pharmazie最新文献_第6页

The anti-Acinetobacter baumannii therapeutic potential of azole hybrids: A mini-review 杂唑类药物抗鲍曼不动杆菌治疗潜力综述

IF 4.3 3区医学

Archiv der Pharmazie Pub Date : 2025-03-04 DOI: 10.1002/ardp.202400592

Zhi Xu, Junna Liu, Yafei Zhuang

{"title":"The anti-Acinetobacter baumannii therapeutic potential of azole hybrids: A mini-review","authors":"Zhi Xu, Junna Liu, Yafei Zhuang","doi":"10.1002/ardp.202400592","DOIUrl":"https://doi.org/10.1002/ardp.202400592","url":null,"abstract":"Acinetobacter baumannii is one of the major causes of severe hospital- and community-acquired infections, posing a significant threat to human lives. A. baumannii has already generated resistance to almost all of the currently available antibiotics, but no new class of antibacterials have been launched for the treatment of infections caused by A. baumannii in the last half century, creating an urgent need to develop novel antibacterials. Azoles as a broad class of five-membered nitrogen-containing aromatic heterocycles are privileged pharmacophores widely found in pharmaceuticals. Azoles could target on diverse enzymes, proteins, and receptors in A. baumannii via various noncovalent interactions. Particularly, azole hybrids have potential advantages in increasing therapeutic efficacy and circumventing drug resistance, representing useful scaffolds for the discovery of novel anti-A. baumannii agents. This review outlines the current scenario of the antibacterial therapeutic potential of azole hybrids against A. baumannii, developed from 2020 onwards, aiming to provide potential candidates for further preclinical/clinical evaluations and facilitate the rational design of more effective candidates.","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"358 3","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143554217","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Discovery of a novel 2,4-thiazolidinedione derivative as dual inhibitor of β-catenin/TCF4 interaction and tubulin polymerization in colon cancer cells 发现一种新的2,4-噻唑烷二酮衍生物作为结肠癌细胞中β-连环蛋白/TCF4相互作用和微管蛋白聚合的双重抑制剂

IF 4.3 3区医学

Archiv der Pharmazie Pub Date : 2025-03-04 DOI: 10.1002/ardp.202400796

Yating Guo, Meng Cao, Zhaohui Li, Hongfei Zhou, Zhuo Chen, Qianbin Li

{"title":"Discovery of a novel 2,4-thiazolidinedione derivative as dual inhibitor of β-catenin/TCF4 interaction and tubulin polymerization in colon cancer cells","authors":"Yating Guo, Meng Cao, Zhaohui Li, Hongfei Zhou, Zhuo Chen, Qianbin Li","doi":"10.1002/ardp.202400796","DOIUrl":"https://doi.org/10.1002/ardp.202400796","url":null,"abstract":"Hyperactivation of the Wnt/β-catenin signaling pathway has been widely recognized as a pathogenic mechanism for colorectal cancer (CRC). Based on a previously reported lead compound, iCRT14, a series of 2,4-thiazolidinedione derivatives were designed, synthesized, and evaluated in vitro for their antiproliferative activity against colon cancer cells. Compound 15k exhibited the most potent activity against the HCT116 and SW480 cell lines. Compound 15k inhibited Wnt/β-catenin signaling by disrupting the protein–protein interactions between β-catenin and TCF4. Compound 15k simultaneously inhibited tubulin polymerization, disorganized the microtubule network, and arrested the cell cycle at the G2/M phase, offering an additional mechanism of action and 15k induced cell apoptosis by activating caspase-3 and poly(ADP-ribose) polymerase. Additionally, compound 15k inhibited cell migration without affecting the levels of β-catenin protein. These results offer guidance for developing the current series as potential new anticancer therapeutics.","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"358 3","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143554218","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A simplified optimization approach for sample preparation workflow in LC-MS-based quantitative proteomic analysis: Biological samples to peptides 基于lc - ms的定量蛋白质组学分析中样品制备流程的简化优化方法：生物样品到多肽

IF 4.3 3区医学

Archiv der Pharmazie Pub Date : 2025-03-04 DOI: 10.1002/ardp.202400911

Surendra Fartade, Tarang Jadav, Niraj Rajput, Pinaki Sengupta

{"title":"A simplified optimization approach for sample preparation workflow in LC-MS-based quantitative proteomic analysis: Biological samples to peptides","authors":"Surendra Fartade, Tarang Jadav, Niraj Rajput, Pinaki Sengupta","doi":"10.1002/ardp.202400911","DOIUrl":"https://doi.org/10.1002/ardp.202400911","url":null,"abstract":"Quantitative proteomics, an integral subfield within proteomics, is pivotal for elucidating complex biological processes. By integrating with other omics data, quantitative proteomics facilitates system-level analysis and significantly advances our understanding of cellular networks and disease mechanisms. The ongoing advancements in quantitative proteomics technology significantly boost its importance by improving analytical accuracy. This review focuses on quantitative proteomics employing liquid chromatography-mass spectrometry (LC-MS), a cornerstone technique renowned for its sensitivity, selectivity, accuracy, and throughput. The efficacy of LC-MS proteomics is heavily reliant on sample preparation, which encompasses protein extraction, total protein estimation, reduction, alkylation, digestion, and cleanup. For the very first time, this article provides a detailed examination of sample preparation methods offering insights and guidelines that researchers can utilize to refine their experimental protocols which were not critically evaluated before. By optimizing sample preparation workflows, researchers can enhance the robustness and reproducibility of their proteomic studies. By understanding the complexities of sample preparation in quantitative proteomics, researchers can optimize their experimental workflow to improve the robustness and reproducibility of their results. This review provides a comprehensive overview of sample preparation strategies in quantitative proteomics using LC-MS, discussing the underlying principles and key considerations for each step. By delving into the complexities of sample preparation, this article aims to aid researchers in optimizing their workflows to achieve robust and reproducible results, which ultimately drive innovations and breakthroughs in biomedical research and healthcare.","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"358 3","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143554669","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Advances in the activity of resveratrol and its derivatives in cardiovascular diseases 白藜芦醇及其衍生物在心血管疾病中的活性研究进展

IF 4.3 3区医学

Archiv der Pharmazie Pub Date : 2025-02-16 DOI: 10.1002/ardp.202400865

Yaling Peng, Xing Zheng, Si Zhang, Zhongqin Luo, Li Song, Hongfei Chen, Xu Yao

引用次数: 0

Issue Information: Arch Pharm (2/2025) 发行信息：Arch Pharm (2/2025)

IF 4.3 3区医学

Archiv der Pharmazie Pub Date : 2025-02-13 DOI: 10.1002/ardp.2570002

引用次数: 0

Antiviral metabolites from Passiflora edulis: An in vitro, phytochemical, and computational studies 西番莲中的抗病毒代谢物：体外、植物化学和计算研究

IF 4.3 3区医学

Archiv der Pharmazie Pub Date : 2025-02-13 DOI: 10.1002/ardp.202400853

Abeer H. Elmaidomy, Michelle Teutsch, Jochen Bodem, Ruqaiah I. Bedaiwi, Mubarak A. Alzubaidi, Hisham A. Abou-Zied, Usama Ramadan Abdelmohsen

{"title":"Antiviral metabolites from Passiflora edulis: An in vitro, phytochemical, and computational studies","authors":"Abeer H. Elmaidomy, Michelle Teutsch, Jochen Bodem, Ruqaiah I. Bedaiwi, Mubarak A. Alzubaidi, Hisham A. Abou-Zied, Usama Ramadan Abdelmohsen","doi":"10.1002/ardp.202400853","DOIUrl":"https://doi.org/10.1002/ardp.202400853","url":null,"abstract":"Yellow fever (YF) is a mosquito-borne virus with high mortality rates, affecting regions in South America and Africa. Despite the effectiveness of YF vaccines, increased global demand and reports of rare, severe side effects have spurred the search for safer therapeutic alternatives. Current treatments lack specific antiviral drugs approved for YF, underscoring the need for new, effective therapies. This study investigated the potential of Passiflora edulis f. edulis leaf and stem extracts as antiviral agents against the yellow fever virus (YFV). In vitro tests showed that the extracts significantly reduced YFV viral loads by twofold in Huh-7 cells and 1.5-fold in Vero-h-Slam cells at a concentration of 50 µg/mL, with a smaller reduction at 25 µg/mL and no cytotoxic effects on either cell line. Phytochemical analysis identified a new C-deoxyhexosyl flavone, luteolin-8-(1-C-β-boivinopyranosyl)-4′1-O-β-d-glucopyranoside, along with several known compounds. Protein–protein interaction (PPI) network analysis using the STRING database and Cytoscape software revealed key hub genes, including IFNA1, IL7R, CD19, IL2RA, and IFNG, crucial in antiviral defense. Molecular docking studies further evaluated how these compounds interact with the YFV NS2B-NS3 protease, essential for viral replication. Molecular dynamics (MD) simulations confirmed the stability of these interactions over a 120-nanosecond period, supporting the compounds’ antiviral potential. This study demonstrates the promise of Passiflora edulis metabolites as a foundation for developing novel YFV therapies by combining computational and experimental insights.","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"358 2","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-02-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143396844","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Targeting the isoprenoid pathway in choleste biosynthesis: An approach to identify isoprenoid biosynthesis inhibitors 以胆固醇生物合成中的异戊二烯途径为目标：鉴定异戊二烯生物合成抑制剂的方法

IF 4.3 3区医学

Archiv der Pharmazie Pub Date : 2025-02-13 DOI: 10.1002/ardp.202400807

Maximilian Liebl, Florian Olander, Christoph Müller

{"title":"Targeting the isoprenoid pathway in choleste biosynthesis: An approach to identify isoprenoid biosynthesis inhibitors","authors":"Maximilian Liebl, Florian Olander, Christoph Müller","doi":"10.1002/ardp.202400807","DOIUrl":"https://doi.org/10.1002/ardp.202400807","url":null,"abstract":"The development of novel cholesterol biosynthesis inhibitors is a task of major concern due to the diverse roles of cholesterol and its precursors in physiological processes. Therefore, appropriate screening assays are required, which can be used to identify and quantify specific inhibitors targeting the desired enzyme. Here, we developed a whole-cell screening assay based on a HL60 cell line, which can be used to characterize inhibitors interacting with enzymes of the isoprenoid part of cholesterol biosynthesis. Due to the change of the isoprenoid pattern under enzyme inhibition, an identification of the targeted enzyme is possible. With the described assay, we can distinguish between free and pyrophosphorylated isoprenoids after enzymatic cleavage in cellular and extracellular matrices. The approach was validated in line with the European Medicines Agency guideline on bioanalytical method validation. As proof of concept, literature-described inhibitors of the isoprenoid pathway were tested. We characterized the effect of 11 isoprenoid biosynthesis inhibitors, and we identified 6-fluoromevalonate as an isopentenyl pyrophosphate isomerase inhibitor, a biological activity that was previously unknown. Furthermore, isoprenoid patterns revealed that, independent of the analyzed matrix, the predominant form of the detected isoprenoids were dephosphorylated isoprenoids and only small amounts were present as pyrophosphates.","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"358 2","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-02-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/ardp.202400807","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143396845","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Natural products against tau hyperphosphorylation-induced aggregates: Potential therapies for Alzheimer's disease 抗tau蛋白过度磷酸化诱导聚集体的天然产物：阿尔茨海默病的潜在疗法。

IF 4.3 3区医学

Archiv der Pharmazie Pub Date : 2025-01-30 DOI: 10.1002/ardp.202400721

Gustavo Basurto-Islas, Maximiliano Caye Diaz, Lizeth M. Zavala Ocampo, Melchor Martínez-Herrera, Perla Y. López-Camacho

{"title":"Natural products against tau hyperphosphorylation-induced aggregates: Potential therapies for Alzheimer's disease","authors":"Gustavo Basurto-Islas, Maximiliano Caye Diaz, Lizeth M. Zavala Ocampo, Melchor Martínez-Herrera, Perla Y. López-Camacho","doi":"10.1002/ardp.202400721","DOIUrl":"10.1002/ardp.202400721","url":null,"abstract":"Alzheimer's disease (AD) is a progressive neurodegenerative disorder characterized by cognitive decline and memory impairments and is considered the most prevalent form of dementia. Among the contributing factors to AD lies the hyperphosphorylation of the microtubule-associated protein tau. Phosphorylated tau reduces its affinity for microtubules and triggers other posttranslational modifications that result in its aggregation and assembly into filaments. These structures progressively accumulate within neurons leading to neurodegeneration. While current AD medications often involve undesirable side effects, the exploration of natural products as a potential therapeutic alternative has gained considerable attention. Numerous compounds have shown potential capacity for reducing tau pathology through different mechanisms, such as inhibiting kinases to reduce tau hyperphosphorylation, enhancing phosphatase activity, and blocking fibril formation. Since tau hyperphosphorylation-induced aggregation is pivotal in AD onset, this review aims to elucidate the potential of natural products in modulating this crucial molecular mechanism.","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"358 1","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11781347/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143062241","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Synthesis and biological investigation of peptidomimetic SARS-CoV-2 main protease inhibitors bearing quinoline-based heterocycles at P3 P3位点含喹啉类杂环的拟肽型SARS-CoV-2主要蛋白酶抑制剂的合成及生物学研究

IF 4.3 3区医学

Archiv der Pharmazie Pub Date : 2025-01-28 DOI: 10.1002/ardp.202400812

Sara Rossi, Graziano Deidda, Lia Fiaschi, Roberta Ibba, Mariachiara Pieroni, Maria Dichiara, Gabriele Carullo, Stefania Butini, Anna Ramunno, Simone Brogi, Marco Lolicato, Cristina Arrigoni, Noemi Cabella, Laura Bavagnoli, Giovanni Maga, Ilenia Varasi, Camilla Biba, Ilaria Vicenti, Sandra Gemma, Emmanuele Crespan, Maurizio Zazzi, Giuseppe Campiani

{"title":"Synthesis and biological investigation of peptidomimetic SARS-CoV-2 main protease inhibitors bearing quinoline-based heterocycles at P3","authors":"Sara Rossi, Graziano Deidda, Lia Fiaschi, Roberta Ibba, Mariachiara Pieroni, Maria Dichiara, Gabriele Carullo, Stefania Butini, Anna Ramunno, Simone Brogi, Marco Lolicato, Cristina Arrigoni, Noemi Cabella, Laura Bavagnoli, Giovanni Maga, Ilenia Varasi, Camilla Biba, Ilaria Vicenti, Sandra Gemma, Emmanuele Crespan, Maurizio Zazzi, Giuseppe Campiani","doi":"10.1002/ardp.202400812","DOIUrl":"10.1002/ardp.202400812","url":null,"abstract":"In the last few years, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has been the cause of a worldwide pandemic, highlighting the need for novel antiviral agents. The main protease (Mpro) of SARS-CoV-2 was immediately identified as a crucial enzyme for viral replication and has been validated as a drug target. Here, we present the design and synthesis of peptidomimetic Mpro covalent inhibitors characterized by quinoline-based P3 moieties. Structure–activity relationships (SARs) were also investigated at P1 and P2, as well as for different warheads. The binding modes of the designed inhibitors were assessed using X-ray crystallographic and molecular docking studies. The identified Mpro inhibitors were tested for their antiviral activities in cell-based assays, and the results were encouraging. The SAR studies presented here can contribute to the future design of improved inhibitors by addressing some of the current or prospective issues regarding Mpro inhibitors currently used in therapy.","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"358 1","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-01-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143051113","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

FDA-approved drugs featuring macrocycles or medium-sized rings fda批准的具有大环或中等环的药物。

IF 4.3 3区医学

Archiv der Pharmazie Pub Date : 2025-01-25 DOI: 10.1002/ardp.202400890

Youlong Du, Anas Semghouli, Qian Wang, Haibo Mei, Loránd Kiss, Daniel Baecker, Vadim A. Soloshonok, Jianlin Han

引用次数: 0