Current Pharmaceutical Design - Volume 31, Issue 24, 2025
Volume 31, Issue 24, 2025
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The Molecular Mechanisms of Natural Medicinal Active Ingredients Interfering with Male Fertility
Authors: Wen-Wen Zhao, Liu Yang, Ye-Bin Yang, Ran Guo, Xing-Sheng Xiao and Yi-Min ChengThe challenges posed by excessive global population growth remain significant. Hormonal female contraceptive pills, which have been approved for over 60 years, serve as an important means of contraception; however, many women experience adverse effects after taking these pills, including abnormalities in blood clotting, dizziness, headaches, and vomiting. In this context, male contraceptives have emerged as a prominent area of research. Unfortunately, most male contraceptives are still in the experimental or clinical research stages. Therefore, screening for active ingredients that can specifically inhibit sperm function from natural drug active ingredient libraries holds substantial clinical and practical significance. In this manuscript, we review the inhibitory effects of various natural drug active monomers on sperm function and their underlying molecular mechanisms, aiming to provide theoretical insights for the future development of novel male contraceptives.
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Skin Aging: Insights into the Role of Fatty Acids
The human skin, being the largest organ, provides defense against bacteria, toxins, and ultraviolet radiation. The skin may experience changes like dryness, photodamage, oxidative damage, and inflammation. This review explores sources of fatty acids and how they can prevent skin damage, with the goal of determining their potential for preventing skin aging. The role and significance of various mechanistic pathways and molecular targets involved in skin aging are highlighted. By using current research findings, this review contributes to a comprehensive understanding of how fatty acids may serve as a proactive approach to promoting youthful skin and mitigating the signs of skin aging. In addition to treating specific skin conditions, nutraceuticals offer immense potential to minimize, postpone, or prevent premature skin aging. The substances that are most frequently employed include carotenoids, polyunsaturated fatty acids, plant polyphenols, bioactive peptides, oligosaccharides, and vitamins. Numerous human trials have demonstrated the impact of supplementing with these items on indicators of aging. The most pertinent clinical and non-clinical investigations are assessed in this review. Based on the comprehensive understanding of the significant role of fatty acids in addressing skin aging, this review may open doors and offer avenues for future explorations.
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An Emerging Prospective of Antipsychotics for Treating Neurodegenerative Disorders
Authors: Bhavna Kumar, Arpita Sahoo, Manmohan Singhal, Garima Varshney, Tripti Haldar and Vikas BaliCNS illnesses specified by slow deprivation of especially preganglionic neurons, as opposed to the selective static neuronal loss caused by a toxic or metabolic condition, are known as Neurodegenerative disorders. Neurodegenerative disorders are differentiated clinically by behavioral or cognitive problems. The management and treatment of neurodegenerative disorders pose significant challenges, necessitating a multidimensional approach. While primarily designed for psychiatric conditions, antipsychotics have shown potential in ameliorating behavioral and psychological symptoms in neurodegenerative disorders such as Alzheimer's and Parkinson's diseases. This review explores the existing literature, highlighting the potential benefits, risks, and considerations associated with incorporating antipsychotics into the treatment paradigm for neurodegenerative disorders. Additionally, it discusses the evolving landscape of personalized treatment strategies, emphasizing the need for a multidisciplinary approach to optimize patient outcomes in the complex realm of neurodegenerative disorder management.
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Nanotechnology-based Approaches for Targeted Drug Delivery to the Small Intestine: Advancements and Challenges
Authors: Phool Chandra, Manav Ruhela, Prashant Kumar, Mayur Porwal, Anurag Verma, Himanshu Sharma and Neetu SachanNanotechnology has emerged as a promising avenue for targeted drug delivery to the small intestine, offering precise control over drug release and enhanced therapeutic efficacy. This review discusses recent advancements and challenges in nanotechnology-based approaches for targeted drug delivery to the small intestine. The small intestine presents unique challenges for drug delivery, including enzymatic degradation, low permeability, and rapid transit time. Nanotechnology offers solutions to these challenges by providing carriers capable of protecting drugs from degradation, enhancing their absorption, and facilitating site-specific delivery. Various nanocarrier systems have been explored for targeted drug delivery to the small intestine, including liposomes, polymeric nanoparticles, dendrimers, and solid lipid nanoparticles. These carriers can be functionalized with ligands targeting specific receptors or transporters expressed on the intestinal epithelium, enabling efficient uptake and intracellular delivery of drugs. Additionally, nanotechnology enables the controlled release of drugs, allowing for sustained and/or triggered release profiles tailored to the physiological conditions of the small intestine. This precise control over drug release can improve therapeutic outcomes while minimizing systemic side effects. Despite the significant progress in nanotechnology-based drug delivery to the small intestine, several challenges remain. These include achieving sufficient drug loading capacity, ensuring biocompatibility and safety of nanocarriers, and addressing regulatory concerns associated with their clinical translation. In conclusion, nanotechnology holds immense potential for targeted drug delivery to the small intestine, offering solutions to overcome the limitations of conventional drug delivery systems. Addressing the remaining challenges will be crucial for realizing the full therapeutic benefits of nanotechnology in treating diseases affecting the small intestine.
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Targeting Anaplastic Lymphoma Kinase in Oncology: Identification and Computational Validation of Novel Inhibitors for Anaplastic Large Cell Lymphoma, Non-small Cell Lung Cancer, and Neuroblastoma
BackgroundAnaplastic Lymphoma Kinase (ALK) is implicated in several cancers, including anaplastic large cell lymphoma, non-small cell lung cancer, and neuroblastoma. Targeted inhibition of ALK represents a promising therapeutic strategy.
AimsThis study aimed to identify and evaluate potential ALK inhibitors using virtual screening and computational analyses to determine their binding stability, affinity, and dynamic behavior, ultimately assessing their potential as therapeutic agents for ALK-driven cancers.
ObjectiveThe objective of this study was to identify potential ALK inhibitors using virtual screening techniques and to evaluate their binding affinities and stability through computational analyses.
MethodsThis study utilized virtual screening to identify potential ALK inhibitors from the MTiOpen Screen Diverse library and selected three compounds (24331480, 26536128, and 24353407) based on their binding affinities. These compounds underwent optimization using Density Functional Theory (DFT) and were re- docked to confirm binding stability. Molecular dynamics simulations, hydrogen bond analysis, MM/PBSA calculations, and PCA-based free energy landscape analysis were also carried out.
ResultsThe re-docking experiments confirmed the stable and strong binding affinities of the selected compounds to the ALK active site. Molecular dynamics simulations revealed stable interactions throughout the 200 ns simulation period. Hydrogen bond analysis demonstrated consistent hydrogen bonds between key residues and the inhibitors. MM/PBSA calculations indicated favorable binding free energies, suggesting strong binding affinities. Finally, PCA-based free energy landscape analysis highlighted energetically favorable binding modes.
ConclusionThe identified compounds (24331480, 26536128, and 24353407) exhibited promising inhibitory potential against ALK. These findings warrant further experimental validation to confirm their potential as therapeutic agents for ALK-driven cancers.
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Mesenchymal Stem Cell-conditioned Medium Attenuated CoCl2-induced Injury of Renal Tubular Epithelial Cells by Inhibiting NCOA1, HIF-1α, and Sox9
Authors: Yiping Liu, Yongda Lin, Ziqiang Wang, Wenzhuang Tang, Chunling Liao and Tianbiao ZhouBackgroundsRenal interstitial fibrosis (RIF) constitutes the ultimate pathological alteration in nearly all chronic kidney diseases (CKD). Mesenchymal stem cell conditioned medium (MSC-CM) exhibits an alleviating impact on renal fibrosis. However, the underlying mechanism remains unclear. The objective of this study was to explore whether MSC-CM regulates the expression of α-smooth muscle actin (α-SMA), Transforming growth factor-β1 (TGF-β1), Hypoxia-inducible factor-1α (HIF-1α), Nuclear receptor coactivators (NCOA1), and SRY-related high mobility (Sox9).
MethodsRat renal tubular epithelial cells (RTECs), NRK-52E, were treated with diverse concentrations of Cobalt chloride (CoCl2) for 24 hours. The survival rate and protein expression of NRK-52E cells exposed to different concentrations of CoCl2 were determined to identify the final concentration. Three groups of NRK-52E cells were employed in the experiment: the normal control group, the 400 μM CoCl2 group, and the MSC-CM + 400 μM CoCl2 group. The cell morphology was observed by an inverted phase contrast microscope and scanning electron microscope, and the protein expressions of α-SMA, TGF-β1, HIF-1α, NCOA1, and Sox9 were detected.
ResultsThe microscopic findings demonstrated that MSC-CM was able to decrease the degree of cytochemical hypoxia damage in NRK-52E cells induced by CoCl2. Immunofluorescence and Western blot analyses also affirmed a similar tendency. The upregulation of α-SMA, TGF-β1, HIF-1α, NCOA1, and Sox9 triggered by CoCl2 could be inhibited following MSC-CM intervention.
ConclusionOur findings indicate that MSC-CM exerts a protective effect on RTECs by down-regulating α-SMA, TGF-β1, HIF-1α, NCOA1, and Sox9.
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Volumes & issues
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Volume 31 (2025)
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Volume (2025)
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Volume 30 (2024)
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Volume 29 (2023)
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Volume 28 (2022)
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Volume 27 (2021)
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Volume 26 (2020)
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Volume 25 (2019)
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Volume 24 (2018)
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Volume 23 (2017)
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Volume 22 (2016)
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Volume 21 (2015)
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Volume 20 (2014)
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Volume 19 (2013)
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Volume 18 (2012)
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Volume 17 (2011)
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Volume 16 (2010)
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Volume 15 (2009)
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Volume 14 (2008)
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Volume 13 (2007)
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Volume 12 (2006)
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Volume 11 (2005)
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Volume 10 (2004)
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Volume 9 (2003)
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Volume 8 (2002)
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Volume 7 (2001)
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Volume 6 (2000)
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