Future Journal of Pharmaceutical Sciences最新文献

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Exploring drug-induced liver injury: comprehensive insights into mechanisms and management of hepatotoxic agents
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-03-28 DOI: 10.1186/s43094-025-00788-5
Ahmed K. Saleh, Thanaa A. El-Masry, Aya H. El-Kadem, Nada A. Ashour, Nageh A. El-Mahdy
{"title":"Exploring drug-induced liver injury: comprehensive insights into mechanisms and management of hepatotoxic agents","authors":"Ahmed K. Saleh,&nbsp;Thanaa A. El-Masry,&nbsp;Aya H. El-Kadem,&nbsp;Nada A. Ashour,&nbsp;Nageh A. El-Mahdy","doi":"10.1186/s43094-025-00788-5","DOIUrl":"10.1186/s43094-025-00788-5","url":null,"abstract":"<div><h3>Background</h3><p>Drug-induced liver injury (DILI) is a significant adverse drug reaction, manifesting through a range of clinical presentations from mild liver enzyme to acute liver failure.</p><h3>Main text</h3><p>This review provides a comprehensive overview of DILI, emphasizing the differences between intrinsic and idiosyncratic DILI. The underlying molecular mechanisms, like mitochondrial dysfunction, oxidative stress, and immune-mediated responses, are discussed in detail. The epidemiology of DILI is explored through various retrospective and prospective studies, highlighting the role of specific medications and individual susceptibility factors. The review also addresses the challenges in diagnosing DILI and the impact on drug development and clinical practice.</p><h3>Conclusion</h3><p>DILI poses a significant clinical threat due to its potential for causing acute liver failure and associated mortality. To improve patient outcomes, further research is crucial to identify effective therapeutic interventions.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00788-5","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143726662","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Nanocomposites in focus: tailoring drug delivery for enhanced therapeutic outcomes
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-03-28 DOI: 10.1186/s43094-025-00789-4
Aditi Gupta, Paresh Patel, Shreeraj Shah, Kaushika Patel
{"title":"Nanocomposites in focus: tailoring drug delivery for enhanced therapeutic outcomes","authors":"Aditi Gupta,&nbsp;Paresh Patel,&nbsp;Shreeraj Shah,&nbsp;Kaushika Patel","doi":"10.1186/s43094-025-00789-4","DOIUrl":"10.1186/s43094-025-00789-4","url":null,"abstract":"<div><h3>Background</h3><p>Nanocomposites made of nanoscale materials may be employed to create innovative drug delivery systems that interface better with biological membranes and selectively deliver drugs to specific cells for targeted and personalized treatment. Due to its versatility and usage in construction, marine, car, aerospace, defense, and biological disciplines, nanocomposites research is expanding. Many researchers are introducing nanoparticles to the matrix to improve their qualities.</p><h3>Main body of the abstract</h3><p>As categorized into polymeric, metallic, and ceramic nanocomposites, the performance characteristics of nanocomposites are improved by different sophisticated top-down and bottom-up preparation methods including in situ polymerization, intercalation techniques, sol–gel, and hydrothermal. These materials can be used for applications such as controlled release, targeted delivery within cells, and pH-responsive systems which take advantage of tumor microenvironments. They improve the efficacy of cancer therapy by modulating the immune system through an immune checkpoint blockade, including PD-1/PD-L1. The composition of polymeric and metallic nanocomposites and the formulations incorporating them are briefed in this work, along with the justification of preference of nanocomposites over other conventional composite materials. Characterization techniques that are employed to study the nanocomposites including X-ray diffraction, scanning electron microscope, transmission electron microscope, Fourier-transform infrared spectroscopy, thermogravimetry, and differential scanning calorimetric are summarized in depth.</p><h3>Short conclusion</h3><p>The described work is a comprehensive review on nanocomposite-based drug delivery system, including importance, manufacturing techniques, formulation development, characterization, and molecular targets. The several opportunities to be explored, limitations prevalent in the area, and future perspectives are discussed to bring revolution in the field of drug delivery and other biomedical applications.</p><p>The figure explains the fabrication of biopolymer nanocomposites by incorporating polysaccharides, proteins, and polynucleotides with carbon nanomaterials, mineral nanoparticles, and metal nanostructures. Examples include materials for drug delivery, flexible sensors and monitors, energy sources, and lightweight load-bearing structures, focusing on processable, realizable, and sustainable materials (created by BioRender).</p><h3>Graphical abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00789-4","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143726666","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Allosteric modulation of laeviganoid-based clerodane diterpenes derivatives in muscarinic acetylcholine M1 receptor against tinnitus: a structure-based virtual screening approach
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-03-11 DOI: 10.1186/s43094-025-00783-w
Jacilene Silva, Matheus Nunes da Rocha, Victor Moreira de Oliveira, Caio Henrique Alexandre Roberto, Francisco Nithael Melo Lúcio, Márcia Machado Marinho, Hélcio Silva dos Santos, Emmanuel Silva Marinho
{"title":"Allosteric modulation of laeviganoid-based clerodane diterpenes derivatives in muscarinic acetylcholine M1 receptor against tinnitus: a structure-based virtual screening approach","authors":"Jacilene Silva,&nbsp;Matheus Nunes da Rocha,&nbsp;Victor Moreira de Oliveira,&nbsp;Caio Henrique Alexandre Roberto,&nbsp;Francisco Nithael Melo Lúcio,&nbsp;Márcia Machado Marinho,&nbsp;Hélcio Silva dos Santos,&nbsp;Emmanuel Silva Marinho","doi":"10.1186/s43094-025-00783-w","DOIUrl":"10.1186/s43094-025-00783-w","url":null,"abstract":"<div><h3>Background</h3><p>Chronic tinnitus is a complication that affects the central nervous system, specifically the auditory cortex, causing a phantom perception of sounds and noises without any external acoustic stimulus. It is more frequent in men than in women and can be caused by excessive exposure to auditory stimuli. The main modulator of auditory functions, particularly in terms of neuroplasticity in the auditory system, is the M1 muscarinic acetylcholine receptor (mAChR M1). In the literature, natural oxygenated heterocyclic compounds have been used to develop drugs that act on the central nervous system (CNS), including clerodane diterpenes. The aim of this study was to evaluate the modulatory action of a series of naturally occurring clerodane diterpenes against chronic tinnitus.</p><h3>Results</h3><p>The structure-based virtual screening revealed that Laeviganoid derivatives L1-8 share structural similarities with other oxygenated heterocyclic compounds that modulate mAChR M1. The prediction of pharmacokinetic properties highlighted the L4 derivative as a potential candidate for distribution in the CNS due to its high cell permeability (P<sub>app,A→B</sub> = 1.9 × 10<sup>−5</sup> cm/s) and metabolic stability. Molecular docking simulations indicate that the ligand interacts with the active site of mAChR M1 through hydrophobic interactions with residues Tyr106, Trp378, Tyr381 and Tyr404, with an affinity energy of approximately − 8.7 kcal/mol. Molecular dynamics simulations have shown that the L4/M1 complex is stable as a function of time (200 ns).</p><h3>Conclusion</h3><p>The in silico results suggest that the L4 can perform allosteric modulation of mAChR M1 in the treatment of tinnitus, as it can bind to the same interaction site as the tiotropium.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-03-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00783-w","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143583638","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Unveiling metabolome heterogeneity in three species from Coccoloba and Ruprechtia through multiple approaches of UPLC/HRMS and chemometric analysis in relation to antidiabetic, antioxidant and antiglycation activities
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-03-11 DOI: 10.1186/s43094-025-00787-6
Fatma Abdelhakim Mohamed, Mohamed A. Salem, Mohammed N. A. Khalil, Ali M. El-Halawany, Amira S. El Senousy
{"title":"Unveiling metabolome heterogeneity in three species from Coccoloba and Ruprechtia through multiple approaches of UPLC/HRMS and chemometric analysis in relation to antidiabetic, antioxidant and antiglycation activities","authors":"Fatma Abdelhakim Mohamed,&nbsp;Mohamed A. Salem,&nbsp;Mohammed N. A. Khalil,&nbsp;Ali M. El-Halawany,&nbsp;Amira S. El Senousy","doi":"10.1186/s43094-025-00787-6","DOIUrl":"10.1186/s43094-025-00787-6","url":null,"abstract":"<div><h3>Background</h3><p>Diabetes mellitus (DM) is a major intricate metabolic disorder, being one of the chief causes of mortality worldwide. <i>Coccoloba</i> and <i>Ruprechtia</i> are two of the most intriguing polyphenol-rich genera within the Polygonaceae family. The potential of <i>Coccoloba uvifera, Coccoloba peltata</i> and <i>Ruprechtia salicifolia</i> total extracts and fractions as antioxidant, antidiabetic and anti-glycating agents was evaluated and correlated with their chemical composition via multiple approaches of metabolic profiling.</p><h3>Results</h3><p>All the total ethanolic extracts of plant leaves revealed remarkable antioxidant activities in terms of scavenging DPPH and ABTS radicals, as well as ferric reducing antioxidant power (FRAP). Despite having more or less comparable total phenolic and flavonoid contents, <i>C. uvifera</i> extract showed the highest inhibitory activity against <i>α</i>-glucosidase enzyme (IC<sub>50</sub> 7.985 ± 1.08 μg/mL), being more potent than acarbose (20-fold). All total extracts demonstrated moderately high anti-AGEs (&gt; 63% inhibition) in BSA-fructose model. Among all examined fractions, <i>C. uvifera</i> 50% MeOH fraction exhibited the most potent antioxidant activity in DPPH, ABTS and FRAP assays (5697.33 ± 360.7, 3078.9 ± 249, 1664.02 ± 220 µM ascorbic acid equivalent/mg extract, respectively) and the highest <i>α</i>-glucosidase inhibitory activity (IC<sub>50</sub> 3.36 ± 1.04 μg/mL). A total of 140 compounds, belonging to different classes, were annotated in the three species via UPLC-HRMS, where flavonoids and phenolic acids represented the major classes. Multivariate and correlation analyses revealed the key phytochemicals contributing to <i>α</i>-glucosidase inhibition as 1-<i>O</i>-vanilloyl-hexoside, 1,3-<i>O</i>-diferuloylglycerol, drovomifoliol-<i>O</i>-glucopyranoside, protocatechuic acid glucoside, digalloyl glucose and coumaric acid sulphate.</p><h3>Conclusion</h3><p><i>C. uvifera</i> leaves extract and its 50% MeOH fraction had a superb potential to alleviate DM and its complications through their antioxidant, antiglycation and <i>α</i>-glucosidase inhibitory activities mediated by their versatile polyphenolic phytochemicals.</p><h3>Graphical abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-03-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00787-6","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143583515","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Repurposing the antimalarial chloroquine: a potential therapy for hepatic injury in a rat model of hindlimb ischemia–reperfusion by modulating apoptosis, autophagy, inflammation, and oxidative stress
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-03-11 DOI: 10.1186/s43094-025-00781-y
Miar M. Sherif, Hanan S. El-Abhar, Hala M. Fawzy, Amany M. Gad, Dalaal M. Abdallah
{"title":"Repurposing the antimalarial chloroquine: a potential therapy for hepatic injury in a rat model of hindlimb ischemia–reperfusion by modulating apoptosis, autophagy, inflammation, and oxidative stress","authors":"Miar M. Sherif,&nbsp;Hanan S. El-Abhar,&nbsp;Hala M. Fawzy,&nbsp;Amany M. Gad,&nbsp;Dalaal M. Abdallah","doi":"10.1186/s43094-025-00781-y","DOIUrl":"10.1186/s43094-025-00781-y","url":null,"abstract":"<div><h3>Background</h3><p>Besides its local injurious effect, hindlimb hypoxia/reperfusion (HL-H/R) can escalate leading to multiple organ dysfunction syndrome.</p><h3>Purpose of the study</h3><p>This study explores chloroquine’s therapeutic potential in protecting liver tissue from collateral damage caused by HL-H/R, focusing on its effects on inflammation, oxidative stress, autophagy, and apoptosis.</p><h3>Methods and results</h3><p>Male Wistar rats were apportioned into three distinct groups, control, HL-H/R model (90 min/8 days), and HL-H/R + chloroquine (7 days). Western blot, ELISA, immunohistochemical, and histopathology techniques revealed that post-administration of chloroquine caused an upturn in liver architecture and function. The antimalarial drug also abated the hepatic content of the surrogate inflammatory marker TNF-α and downregulated the protein expression of <i>p</i>-MAPK p38. This was allied with a reduction in NF-κB p65 the transcription factor but increased the anti-inflammatory marker interleukin (IL)-10. Moreover, chloroquine amended the interrupted redox balance by reducing the HL-H/R induced increase in reactive oxygen and nitrogen species. Chloroquine leveled off hepatic levels of the lipid peroxide marker MDA, the DNA damage parameter 8-OHdG, as well as NO while enhancing the antioxidant capacity by increasing TAC. These beneficial effects entailed the inhibition of apoptotic cell demise by enhancing the anti-apoptotic marker Bcl-2 and reducing the apoptotic markers Bax and caspase-3. Finally, chloroquine succeeded in curbing the autophagy process where it decreased Beclin-1 and LC3-II, two autophagosome markers, along with the lysosomal parameter cathepsin-D.</p><h3>Conclusion</h3><p>To recapitulate, chloroquine post-administration improved the injurious remote actions of HL-H/R on the liver by its anti-inflammatory (MAPK p38/NF-κB p65/TNF-α, IL-10) and antioxidant (MDA, 8-OHdG, NO, TAC) properties as well as halting the autophagy (Beclin-1, LC3-II, cathepsin-D) and apoptosis (Bcl-2, Bax, caspase-3)-mediated hepatic death to improve liver function (ALT, AST) and structure.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-03-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00781-y","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143583639","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Therapeutic potential of ursolic acid (UA) and their derivatives with nanoformulations to combat nosocomial pathogens
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-03-11 DOI: 10.1186/s43094-025-00785-8
Umesh Chand, Pramod Kumar Kushawaha
{"title":"Therapeutic potential of ursolic acid (UA) and their derivatives with nanoformulations to combat nosocomial pathogens","authors":"Umesh Chand,&nbsp;Pramod Kumar Kushawaha","doi":"10.1186/s43094-025-00785-8","DOIUrl":"10.1186/s43094-025-00785-8","url":null,"abstract":"<div><h3>Background</h3><p>Ursolic acid (UA) is a natural pentacyclic triterpene derived from fruit, herbs, and other plants of the terpenoid category. UA has multi-dynamic antimicrobial activity against various pathogens. However, its poor water solubility, low intestinal mucosal absorption, and low bioavailability restrict its clinical application. Nanotechnology can overcome these deficiencies with various nanoformulations: nanoemulsion, nanoparticles, nanoemulgels, liposomes, and supramolecular gel. UA and its derivatives are used as therapeutic agents and have immunomodulatory functions.</p><h3>The main body of abstract</h3><p>Nanoformulations are popularly known as a promising delivery system for several drugs to increase their therapeutic efficacy. UA can act on many cellular targets such as bacterial cell envelop, efflux pump, enzymatic inhibition, and other microbial (fungal and virus) virulence factors, demonstrating that it can be a potential biomedicinal agent for antibacterial, antifungal, and antiviral activity. Various nanoformulations of UA have been reported to decrease the MIC of the available drugs against various nosocomial pathogens such as <i>Staphylococcus aureus, Escherichia coli, Streptococcus pneumoniae, Klebsiella pneumoniae,</i> and <i>Pseudomonas aeruginosa.</i></p><h3>Short conclusion</h3><p>This review highlights several traditional and modern UA extraction and purification techniques. This also focuses on the therapeutic and pharmaceutical uses of the UA and its derivatives to treat different types of nosocomial infections. Further, UA’s comprehensive molecular mechanism of antimicrobial activity has been discussed.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-03-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00785-8","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143583612","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Revealing the anti-senescence effects and related mechanisms of flavonoid extracts from the buds of Wikstroemia chamaedaphne Meisn on D-galactose-induced PC12 cells based on network pharmacology and transcriptomics 基于网络药理学和转录组学揭示Wikstroemia chamaedaphne Meisn芽中黄酮类提取物对D-半乳糖诱导的PC12细胞的抗衰老作用及相关机制
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-03-10 DOI: 10.1186/s43094-025-00784-9
Xiu-Ying Zhao, Wen-Qian Liu, Li-Wei Zhang, Shi-Fei Li
{"title":"Revealing the anti-senescence effects and related mechanisms of flavonoid extracts from the buds of Wikstroemia chamaedaphne Meisn on D-galactose-induced PC12 cells based on network pharmacology and transcriptomics","authors":"Xiu-Ying Zhao,&nbsp;Wen-Qian Liu,&nbsp;Li-Wei Zhang,&nbsp;Shi-Fei Li","doi":"10.1186/s43094-025-00784-9","DOIUrl":"10.1186/s43094-025-00784-9","url":null,"abstract":"<div><h3>Background</h3><p>Natural products are an important source of drugs or lead compounds for the treatment of senescence. The buds of <i>Wikstroemia chamaedaphne</i> Meisn are a traditional Chinese medicine to cure edema, schizophrenia and epilepsy. A flavonoid extract of <i>W. chamaedaphne</i> (FEW) was prepared from the methanolic extract of <i>W. chamaedaphne</i> by our group previously, which was including eight flavonoids with a content of (55.19 ± 0.32) %. In this study, the anti-senescence effects and related mechanisms of FEW on D-galactose-induced PC12 cells were investigated for the first time.</p><h3>Results</h3><p>High doses of D-galactose could induce PC12 cell senescence, whereas FEW could delay PC12 cell senescence by decreasing SA-β-gal positivity, increasing SOD activity, reducing MDA levels, improving cell morphology, inhibiting cell cycle arrest and down-regulating the expression of senescence-related proteins P16, P21 and P53. Subsequently, potential mechanisms underlying anti-senescence effects of FEW were elucidated through integration of network pharmacology and transcriptomics. The main signaling pathways involved by FEW were found to be cancer signaling pathway, FOXO signaling pathway, PI3k–Akt signaling pathway, AGE–RAGE signaling pathway, protein digestion and uptake, etc. The anti-senescence effects of FEW may be related to the PI3k–Akt signaling pathway as revealed by western blot experiments.</p><h3>Conclusion</h3><p>Our study revealed that FEW has anti-senescence effects. This may suggest that FEW acts as an anti-senescence agent for age-related neurological diseases.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-03-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00784-9","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143583655","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
NeuroAid™-II (MLC901) provides neuroprotection and enhances neuronal cell survival against kainic acid-induced excitotoxicity in vitro by activating the PI3K/AKT pathway
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-03-07 DOI: 10.1186/s43094-025-00782-x
Anam Anjum, Muhammad Dain Yazid, Muhammad Fauzi Daud, Jalilah Idris, Angela Min Hwei Ng, Amaramalar Selvi Naicker, Ohnmar Htwe Ismail, Ramesh Kumar Athi Kumar, Yogeswaran Lokanathan
{"title":"NeuroAid™-II (MLC901) provides neuroprotection and enhances neuronal cell survival against kainic acid-induced excitotoxicity in vitro by activating the PI3K/AKT pathway","authors":"Anam Anjum,&nbsp;Muhammad Dain Yazid,&nbsp;Muhammad Fauzi Daud,&nbsp;Jalilah Idris,&nbsp;Angela Min Hwei Ng,&nbsp;Amaramalar Selvi Naicker,&nbsp;Ohnmar Htwe Ismail,&nbsp;Ramesh Kumar Athi Kumar,&nbsp;Yogeswaran Lokanathan","doi":"10.1186/s43094-025-00782-x","DOIUrl":"10.1186/s43094-025-00782-x","url":null,"abstract":"<div><p>In the twenty-first century, in vitro models of excitotoxic injury, leveraging advanced cellular and molecular technologies, offer a promising alternative to animal studies. These models provide a more precise understanding of injury mechanisms. Method: This study utilizes kainic acid (KA), a potent glutamate receptor agonist, to induce excitotoxicity, oxidative stress, and mitochondrial dysfunction, resulting in motor neuron (MN) degeneration. Mature, differentiated NSC-34 MNs were exposed to different concentrations of KA (0.1, 0.5, and 1 mM) to induce neurodegeneration and apoptosis. Following KA treatment, cells were either treated with MLC901 (NeuroAiD™ II) or left untreated. The effects were assessed through cell viability assays, immunocytochemistry with antibiotic staining, and analysis of key markers in the PI3K/AKT signaling pathway. KA exposure resulted in significant neurodegeneration and apoptosis, as indicated by a reduction in cell viability, a decrease in Tubulin beta-III expression, and downregulation of regenerative markers, including AKT, p-AKT, and GAP43. Additionally, the apoptotic marker p-GSK3β was upregulated in KA-treated cells. In contrast, MLC901 treatment alleviated these detrimental effects. MLC901 restored Tubulin beta-III expression and reversed the downregulation of PI3K/AKT signaling markers (AKT, p-AKT, GAP43). Furthermore, MLC901 treatment led to a reduction in the apoptotic marker p-GSK3β. This study demonstrates that KA induces necrotic and apoptotic cell damage, mimicking secondary injury mechanisms typical of neurodegenerative diseases. MLC901 shows promise as a neuroprotective agent, counteracting KA-induced excitotoxicity and highlighting its potential therapeutic application in neuroprotection.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-03-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00782-x","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143564465","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
UPLC-ESI–MS/MS phytochemical profile, in vitro, in vivo, and in silico anti-Alzheimer’s activity assessment of Pithecellobium dulce (Roxb.) Benth. leaves Pithecellobium dulce (Roxb.) Benth.叶片的 UPLC-ESI-MS/MS 植物化学成分概况、体外、体内和硅学抗阿尔茨海默氏症活性评估
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-03-05 DOI: 10.1186/s43094-025-00776-9
Alaa A. Elhewehy, Ahlam M. El-fishawy, Ahmed A. El-Rashedy, Ahmed M. Fayez, Marwa A. A. Fayed, Engy Mohsen
{"title":"UPLC-ESI–MS/MS phytochemical profile, in vitro, in vivo, and in silico anti-Alzheimer’s activity assessment of Pithecellobium dulce (Roxb.) Benth. leaves","authors":"Alaa A. Elhewehy,&nbsp;Ahlam M. El-fishawy,&nbsp;Ahmed A. El-Rashedy,&nbsp;Ahmed M. Fayez,&nbsp;Marwa A. A. Fayed,&nbsp;Engy Mohsen","doi":"10.1186/s43094-025-00776-9","DOIUrl":"10.1186/s43094-025-00776-9","url":null,"abstract":"<div><h3>Background</h3><p>Alzheimer's (AD) is a neurological disorder that worsens the quality of life and raises the need for caretakers with no available curative medication for the illness. Therefore, there is a growing concern about the use of herbal medicine, as it is cost-effective, has minimal side effects, and could slow AD progression and enhance patients' quality of life, making it a viable adjuvant therapy. <i>Pithecellobium dulce</i> (Roxb.) Benth F. Leguminosae is widely consumed in several countries to treat various illnesses. This study used in vitro, in vivo, and in silico studies to investigate the potential use of <i>P. dulce</i> leaves' methanolic extract in treating and preventing Alzheimer's disease.</p><h3>Results</h3><p>The in vitro study showed that the extract inhibited 77% of the acetylcholinesterase (AChE) activity, and the IC<sub>50</sub> value was 19.23 ± 1.02 µg/ml. The in vivo study of scopolamine-induced Alzheimer's confirmed the result by significantly inhibiting AChE, dopamine, noradrenaline, and malondialdehyde levels and increasing acetylcholine, and glutathione levels. A phytochemical analysis of the leaves methanolic extract using UPLC-ESI–MS/MS revealed 67 compounds of different chemical classes, 22 flavonoids, 17 phenolic and organic acids, 8 fatty acids, 3 sterols, 6 amino acids and alkaloids, 5 coumarins, and 2 anthraquinones, 1 sugar, 1 lignin, 1 terpene, and 1 hydrocarbon. It was found that 5, 7, 3′, 4′, 5′-pentahydroxy-3, 6, 8-tri-methoxy flavone had the strongest binding affinity for AChE (− 18.8 kcal/mol). Different computational modeling methods were employed, including principal component analysis, ligand-residue interaction, dynamics cross-correlation matrices analysis, and thermodynamics calculation. The binding of 5, 7, 3′, 4′, 5′-pentahydroxy-3, 6, 8-tri-methoxy flavone to ACh protein decreased the fluctuation and influenced the ligand optimum orientation on the AChE protein conformational space. Additionally, the drug binding energy of AChE and the residue correlation in the 5, 7, 3′, 4′, 5′-pentahydroxy-3, 6, 8-tri-methoxy flavone-AChE system was increased.</p><h3>Conclusion</h3><p>The <i>P. dulce</i> extract contains secondary metabolites that could promisingly be a safe and effective natural treatment for Alzheimer's complications through the antioxidant activity, acetylcholinesterase, dopamine, and noradrenaline inhibition activities and also by increasing the acetylcholine level in the brain.</p><h3>Graphical abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-03-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00776-9","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143553944","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A short-term cross-sectional retrospective study on procalcitonin as a diagnostic aid for various infectious diseases
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-03-03 DOI: 10.1186/s43094-025-00773-y
D Kiran Khanna, K M Divya Jayalakshmi, D Arun, S Jayavardhini, S Hemanth Karthikaa, S Sumetha, Karthik Thiyagarajan
{"title":"A short-term cross-sectional retrospective study on procalcitonin as a diagnostic aid for various infectious diseases","authors":"D Kiran Khanna,&nbsp;K M Divya Jayalakshmi,&nbsp;D Arun,&nbsp;S Jayavardhini,&nbsp;S Hemanth Karthikaa,&nbsp;S Sumetha,&nbsp;Karthik Thiyagarajan","doi":"10.1186/s43094-025-00773-y","DOIUrl":"10.1186/s43094-025-00773-y","url":null,"abstract":"<div><h3>Background</h3><p>Procalcitonin (PCT) was first described in the early 1960s as a precursor of calcitonin that is synthesized mainly in the thyroid and lung tissues. It is an immediate biosynthetic product in response to bacterial toxins and the pro-inflammatory cytokines, which in turn makes it a distinctive biomarker for bacterial infections. The present analysis deals with the study on the biochemical characteristics, production pathways, and clinical uses of PCT as a diagnostic tool.</p><h3>Methods</h3><p>During March and June 2024, a cross-sectional study was performed, among 357 patients with the proper characteristics who were admitted to the hospital and got their PCT levels, there were those who had respiratory, cardiac, gastrointestinal, and systemic infections. The exclusion criteria were the hospital stay of less than 24 h and a few noninfectious diseases.</p><h3>Results</h3><p>The higher PCT levels (&gt; 0.5 ng/mL) reliably informed about the presence of bacterial infections like pneumonia, endocarditis, urinary tract infections, and sepsis. PCT levels demonstrated trivial increase in viral as well as fungal infections. The study ratified the significant relationship between PCT levels and the severity of bacterial infections, thus backing its usefulness in the diagnosis and treatment control.</p><h3>Conclusion</h3><p>Procalcitonin is increasingly emerging as a trustworthy biomarker for bacterial infections, thus helping in the early diagnosis, guiding targeted antibiotic therapy, and reducing inappropriate antibiotic use. Its high specificity for bacterial etiology has largely contributed to the success and potency of antibiotic stewardship programs.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-03-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00773-y","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143533265","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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