Written by Mohamed Abdelrahman
Published on Vol 5 Issue 2, 2025
Doxorubicin is widely used for cancer therapy but is limited by its cardiotoxic effects. Traditional approaches, such as lowering the drug dose, aim to reduce cardiac side effects but may compromise anticancer efficacy. This study investigates whether Roflumilast can protect heart cells from Doxorubicin-induced inflammation and premature cellular aging, and explores the role of SIRT1 in this process. H9c2 cardiomyocytes were exposed to 5 μmol/L Doxorubicin to induce cell injury. Cell survival wa
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Written by George Adams
Published on Vol 5 Issue 2, 2025
Evidence from clinical trials such as INPULSIS-ON indicates that extended use of nintedanib is generally safe for patients with idiopathic pulmonary fibrosis (IPF). Nevertheless, real-world data on long-term therapy are scarce. This study examined how effective and tolerable prolonged nintedanib treatment is when used in everyday clinical care. This retrospective review included 104 individuals diagnosed with IPF who received nintedanib. Patients were divided into two cohorts: those who maintain
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Written by Chen Wei
Published on Vol 5 Issue 2, 2025
Cisplatin (DDP) remains a primary chemotherapeutic agent for treating non-small cell lung cancer (NSCLC), but the development of drug resistance limits its clinical efficacy. This study aimed to explore the role of RASSF1A in modulating DDP resistance in NSCLC and to elucidate the underlying molecular mechanisms. Expression levels of RASSF1A and microtubule-associated protein 1S (MAP1S) were assessed using qRT-PCR and Western blotting, while their interaction was verified by co-immunoprecipitati
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Written by Carlos Mendes
Published on Vol 5 Issue 2, 2025
This research investigated whether Lactobacillus plantarum KSFY06 (LP-KSFY06) could prevent acute liver damage caused by combined D-galactose and lipopolysaccharide (D-Gal/LPS) exposure in mice. The antioxidant activity of LP-KSFY06 was first examined using in vitro radical scavenging assays. In mice, the effects on liver injury were assessed through organ weight indices, serum liver function markers, oxidative stress parameters, inflammatory cytokines, gene expression levels, and histological e
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Written by Yuki Nakamura
Published on Vol 5 Issue 2, 2025
Effective ocular delivery of tacrolimus remains challenging due to rapid clearance and low bioavailability. This study aimed to design an in situ gel incorporating tacrolimus-loaded solid lipid nanoparticles (TAC-SLNs) for improved therapeutic outcomes in immune conjunctivitis. The TAC-SLNs in situ gel was optimized and evaluated for particle morphology, size, surface charge, drug encapsulation efficiency, loading capacity, and release profile in vitro. Pharmacokinetic and pharmacodynamic studie
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Written by Pedro Almeida
Published on Vol 5 Issue 2, 2025
Numerous bacteria and actinomycetes rely on L-cysteine biosynthesis to enhance their tolerance to antibacterial agents and to sustain persistent infections, a phenomenon that contributes to the emergence of antimicrobial resistance—one of the most critical global public health challenges. As the enzymatic pathway responsible for L-cysteine production is absent in mammalian cells, it represents an attractive and selective target for therapeutic intervention. In this study, we describe the identif
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Written by Kenji Nakamura
Published on Vol 5 Issue 2, 2025
Four isobutyric acid derivatives, including two nitro- and two acetamido-substituted analogues, were synthesized through a two-step procedure and fully characterized by spectroscopic techniques. Treatment of 3T3-L1 adipocytes with compounds 1–4 resulted in elevated mRNA expression levels of PPARγ and GLUT-4, two well-established molecular targets in diabetes therapy, whereas no detectable induction of PPARα expression was observed in vitro. Computational docking and molecular dynamics simulation
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Written by Chloe Martin
Published on Vol 5 Issue 2, 2025
Recent advancements in coordination chemistry and its biological applications have made a significant impact in chemical biology. Motivated by this progress, we have synthesized a new benzimidazole-based imine ligand, 2-((E)-((1H-benzo[d]-2-yl)methylimino)methyl)-4-fluorophenol (HBMF), and investigated its complexes with Co(III) and Cu(II) ions. The metal complexes (C1–C4) were prepared in two distinct stoichiometries: a 2:1 (HBMF: metal ion) ratio and a 1:1:1 ratio (HBMF: metal ion: 1,10-phenan
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Written by Yasmin Rahman
Published on Vol 5 Issue 2, 2025
Recent preclinical findings have identified selective inhibitors of sirtuin 2 (SIRT2) as potential therapeutic agents for treating age-related diseases, but none have advanced to clinical trials. The growing adoption of machine learning (ML) techniques in drug discovery has demonstrated their transformative potential, yet there remains a lack of large-scale, robust ML models for identifying novel SIRT2 inhibitors. To fill this gap, we developed SIRT2i_Predictor, a machine-learning-based tool des
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Written by Lucas Almeida
Published on Vol 5 Issue 2, 2025
Seventeen novel derivatives of (Z)-methyl 3-(4-oxo-2-thioxothiazolidin-5-ylidene)methyl)-1H-indole-2-carboxylate were synthesized and tested for antimicrobial properties. These compounds demonstrated remarkably potent antibacterial activity against eight different bacterial strains, significantly outperforming the standard antibiotics ampicillin and streptomycin by factors of 10 to 50. Compound 8 was identified as the most effective antibacterial agent. Furthermore, the compounds showed good to
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Written by Daniel R. Wilson
Published on Vol 5 Issue 2, 2025
Computational and informatics-driven methodologies have become essential components of modern drug discovery, particularly for the development of targeted anticancer agents with improved selectivity and minimized adverse effects. In the present study, three previously unreported compounds were conceived through a structure-based design strategy and subsequently synthesized. In silico screening predicted favorable pharmacokinetic and toxicity-related properties, as well as strong binding affinity
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Written by Nadine Laurent
Published on Vol 5 Issue 2, 2025
Ursodeoxycholic acid (UDCA) is a well-established treatment for liver conditions, with its derivative, U12, showing notable anti-hepatoma effects in prior research. However, U12’s low polarity and the requirement for high dosages pose challenges to its druglikeness. In this study, twelve new derivatives of U12 were synthesized using substitution, esterification, and amidation methods, aimed at improving its pharmacological properties. Testing of these derivatives on hepatoma cell lines (HepG2) r
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Written by Maria Gonzalez
Published on Vol 5 Issue 2, 2025
Histone deacetylase 6 has emerged as a significant therapeutic target due to its essential role in neurological, inflammatory, and other pathological conditions. At present, no HDAC6-targeting agents have received FDA approval, and most pipeline candidates exhibit limitations, including insufficient target occupancy, inadequate brain exposure, and poor tolerability. A small number of clinical-stage candidates exist, primarily for non-CNS malignancies. Yet, their pharmacokinetic drawbacks preclud
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Written by Oliver Grant
Published on Vol 5 Issue 2, 2025
In-silico modeling and computer-aided drug design benefit from the virtual evaluation of promising lead chemotherapeutic phytochemicals sourced from medicinal plants, which is accomplished by orienting and scoring ligands within a target protein's active binding cavity. The phytochemical exploration of a Pterocephalus frutescens n-butanol extract afforded the isolation and structural determination of three iridoids alongside four flavonoids, established respectively as Geniposide (1), Genipo
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Written by Hiroshi Nakamura
Published on Vol 5 Issue 2, 2025
In clinical practice, the Zuojin Pill (ZJP) is commonly used to manage chronic atrophic gastritis (CAG) and effectively alleviates symptoms such as emesis, discomfort, and abdominal bloating. Yet, the mechanistic basis for ZJP’s therapeutic action in CAG remains unclear. The objective of this work was to define the distinctive role of ZJP in CAG management along with its potential mode of action. An experimental CAG model was generated through alternating exposure to ammonia solution and sodium
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Written by Ali Hassan
Published on Vol 5 Issue 2, 2025
Standard chemotherapeutic regimens fail to provide adequate clinical outcomes in breast cancer owing to pervasive multidrug resistance. Here, we engineered dual-sensitization anti-resistant nanoparticles to manage recalcitrant breast cancer, seeking to capitalize on the combined benefits of photodynamic therapy and chemotherapy. A hyaluronic acid (HA) derivative and a chlorin e6 (Ce6) photosensitizer derivative were manufactured and validated by mass spectrometry. These compounds and the chemoth
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Written by Sanjay Kulkarni
Published on Vol 5 Issue 2, 2025
Identifying new biological activities in already-discovered hit compounds is a fundamental challenge in modern medicinal chemistry. Our investigation examined the previously studied 3-[5-(1H-indol-3-ylmethylene)-4-oxo-2-thioxothiazolidin-3-yl]-propionic acid (Les-6614) for antimicrobial, antifungal, anti-allergic, and antitumor activities. Cytotoxicity profiling, molecular docking, and SwissADME online target prediction were also carried out. The findings revealed that Les-6614 possesses modest
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