Future Journal of Pharmaceutical Sciences最新文献

{"title":"The potential effect of scoparone in autophagic disruption associated with PCOS in Letrozole rat model: role of Nrf2 and Sirt1/LKB1/AMPK signaling","authors":"Ahmed S. Kamel,&nbsp;Nesrine S. El Sayed,&nbsp;Barbara Budzyńska,&nbsp;Krystyna Skalicka-Woźniak,&nbsp;Sarah S. El-Sayed","doi":"10.1186/s43094-025-00800-y","DOIUrl":"10.1186/s43094-025-00800-y","url":null,"abstract":"<div><h3>Background</h3><p>Polycystic ovarian syndrome (PCOS) is an inflammatory autophagy-deficient disorder with downregulated Nrf2. Scoparone (SCPN), a natural compound from Chinese medicine, directly activates Nrf2 and clinically showed promises in treating inflammatory disorders. Studies reported SCPN’s ability to induce autophagy; yet no study tested SCPN’s ability in correcting disturbed autophagy in PCOS. The present research aim was to examine SCPN’s influence on PCOS-associated autophagic disturbances.</p><h3>Methods</h3><p>PCO was induced by Letrozole (1 mg/kg, p.o.) for 21 days and SCPN (12.5 mg/kg, i.p.) either alone or in parallel with an autophagy inhibitor, 3-methyl adenine, for 7 days.</p><h3>Results</h3><p>Hematoxylin and eosin (H&amp;E) staining revealed reduced ovarian cysts with mature follicles recovery with SCPN. The immunolabeled ovarian tissues demonstrated that SCPN increased nuclear factor erythroid 2-related factor 2 (Nrf2) expression together with autophagic markers Beclin1, microtubule-associated protein light chain 3 (LC3), and autophagy enzyme 7 while decreasing P62. This signaling activation may be interpreted by autophagic signals upregulation; Sirtuin 1/liver kinase B1/AMP-activated protein kinase (Sirt1/LKB1/AMPK). A downregulation of inflammatory mediators, viz. tumor necrosis factor-alpha (TNF-α) and p65-nuclear factor kappa B (NF-κB) in PCOS ovaries, is associated by restoration of estradiol and FSH/LH balance. Concomitantly, SCPN abrogated testosterone and anti-Müllerian hormone levels besides insulin resistance and leptin levels.</p><h3>Conclusions</h3><p>The current study showed mutual link between Nrf2 and autophagic pathway. SCPN showed anti-inflammatory character with autophagic improvement in PCOS may be through Nrf2 activation.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-04-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00800-y","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143826592","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}

{"title":"Luteolin mitigates doxorubicin-induced hepatotoxicity and neurotoxicity: modulating the liver–brain axis via IRE1α/GRP78/ATF6 endoplasmic reticulum stress pathways and miRNA-199a-5p expression","authors":"Rasha D. Abdrabou,&nbsp;Rania M. Salama,&nbsp;Reem N. El-Naga,&nbsp;Samar S. Azab","doi":"10.1186/s43094-025-00793-8","DOIUrl":"10.1186/s43094-025-00793-8","url":null,"abstract":"<div><h3>Background</h3><p>Doxorubicin (DOX) has long been a foundational drug in cancer therapeutics. Despite its proven efficacy, the persistent challenge of mitigating its associated side effects, notably hepatotoxicity and neurotoxicity, underscores the necessity for intervention. Luteolin (LUT) is a naturally derived flavonoid with a spectrum of bioactive characteristics, involving anti-apoptotic, antioxidant, anti-inflammatory, and anti-cancer attributes. This study investigates the possible protective effect of LUT against DOX-induced hepatotoxicity and neurotoxicity, focusing on its modulation of the endoplasmic reticulum (ER) stress pathways and miRNA 199a- 5p expression. Forty-eight male Sprague Dawley rats were assigned to six groups: control, LUT (200 mg/kg), DOX (3.5 mg/kg, i.p.) administered twice per week for 3 weeks, and three treatment groups that received daily oral gavage of LUT at doses of 50, 100, and 200 mg/kg for 3 weeks alongside DOX.</p><h3>Results</h3><p>Behavioral assessments revealed the best improvements in rats co-treated with LUT high dose (200 mg/kg), paralleled by the mitigation of neurodegeneration in the cortex and hippocampal areas of the brain. The hepatoprotective effect of LUT (200 mg/kg) demonstrated a notable decrease in liver enzymes and restoration of hepatocytic architecture, coupled with upregulation of miRNA-199a-5p and suppression of glucose-regulated protein 78 (GRP78). LUT inhibited ER stress via suppressing the inositol-requiring enzyme 1 alpha (IRE1α)/protein kinase R-like endoplasmic reticulum kinase (PERK)/eukaryotic initiation factor 2 alpha (eIF2α)/activating transcription factor 6 (ATF6) axes, thereby inhibiting apoptosis.</p><h3>Conclusions</h3><p>LUT 200 mg/kg is efficacious in alleviating DOX-induced hepatic injury and neurotoxicity via dampening ER stress pathways.</p><h3>Graphical abstract</h3>\u0000<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":"2025-04-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00793-8","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143830925","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}

{"title":"Preventive role of rottlerin in endotoxin-induced uveitic glaucoma in rats","authors":"Nidhi Kumari,&nbsp;Ashmita Das,&nbsp;Nirdesh Kumar,&nbsp;Geeta Singh,&nbsp;Urvashi Jain,&nbsp;Amrita Singh,&nbsp;Surendra H. Bodakhe","doi":"10.1186/s43094-025-00798-3","DOIUrl":"10.1186/s43094-025-00798-3","url":null,"abstract":"<div><h3>Background</h3><p>Rottlerin is a natural polyphenolic compound obtained from dried ripe fruits of <i>Mallotus philippinensis</i> and is primarily used as a PKCδ inhibitor. The effectiveness of rottlerin was checked in the endotoxin-induced glaucoma models, focusing on its impact on intraocular pressure, inflammation, and optic nerve protection. For this study, both pure and extracted rottlerin were used. Extracted rottlerin was characterised by determining its melting point, conducting gas chromatography-mass spectrometry analysis, Nuclear magnetic resonance analysis, and measuring its wavelength and retardation factor. The acute toxicity study was carried out using Organization for Economic Co-operation and development guideline 405 (acute eye irritation test).</p><h3>Result</h3><p>Pure and extracted rottlerin showed decreased intraocular pressure and reduced inflammation, lenticular opacity, and retinal damage. These results are attributed to an increase in antioxidant levels, maintenance of lipid peroxidation, enzyme level (Na⁺ ATPase, K⁺ ATPase), ionic balance (Na⁺, K⁺), and a decrease in the level of nitric oxide.</p><h3>Conclusion</h3><p>Rottlerin (pure) as well as rottlerin (extracted) has demonstrated potential in managing uveitic glaucoma. Its multifaceted mechanisms not only target inflammation and oxidative stress but also promote tissue regeneration and slow disease progression. This makes rottlerin a promising candidate for further clinical research as a potential treatment for uveitic glaucoma.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-04-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00798-3","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143821933","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}

{"title":"Clinical pharmacist-led anticoagulation stewardship program: improve physician adherence to evidence-based guidelines and reduce anticoagulant-related medication errors","authors":"Heba M. El-Bosily,&nbsp;Khaled R. Abd El Meguid,&nbsp;Nagwa A. Sabri,&nbsp;Marwa Adel Ahmed","doi":"10.1186/s43094-025-00791-w","DOIUrl":"10.1186/s43094-025-00791-w","url":null,"abstract":"<div><h3>Background</h3><p>Due to their high risk of medication errors (MEs) and the potentially devastating thrombotic and bleeding events, anticoagulants are a class of high-risk medications that require regular monitoring by healthcare professionals. The pharmacist is in the ideal position to provide patient care during anticoagulation therapy which is still prone to inappropriate prescribing. The pharmacist is capable of anticoagulation therapy monitoring, provision of drug information, dosing protocol preparation, drug interaction screening, and educating patients. It has been demonstrated that specialized anticoagulation management programs enhance clinical safety and quality of anticoagulant therapy. This study aimed to evaluate the effect of implementing a pharmacist-led anticoagulation stewardship program in reducing anticoagulant-related MEs. We conducted a prospective pre-and post-intervention study in a tertiary hospital on 233 patients with 4132 anticoagulant doses to assess the impact of this program implementation.</p><h3>Results</h3><p>This study found that MEs were significantly reduced after implementing the anticoagulation stewardship program. Specifically, the “Medication without indication” and the “Incorrect dose (low dose)” types of MEs were remarkably decreased from 14.4% pre- to 3.3% post-, and from 47.6% pre- to 28.7% post-implementation, respectively. Interestingly, the “Wrong route” disappeared in the post-implementation phase of the study. The proportion of wrong doses/total doses decreased from 0.474 ± 0.044 to 0.432 ± 0.04 (<i>p</i> = 0.003), while category F decreased from 8.3% to 4.7% (<i>p</i> = 0.001). Physician adherence to evidence-based guidelines (EBG) improved as full adherence increased from 38.8 to 60.2% (<i>p</i> = 0.001) and non-adherence decreased from 26.7 to 3.4% (<i>p</i> = 0.001). These statistically significant findings further suggest valuable clinical benefits since implementing this pharmacist-led program could improve patient outcomes by reducing ME and increasing physician adherence to EBG guidelines.</p><h3>Conclusions</h3><p>Although the study was limited by the hospital clinical pharmacist team's working hours, as they work 12 h/day rather than 24, and hence, the program was only observed during this time, the study concluded that the anticoagulation stewardship program encouraged the safe use of anticoagulants, lessened MEs and their severity, and improved physician adherence to EBG. Future studies should assess the effect of such programs on other clinical outcomes beyond MEs and determine their impact on healthcare costs.</p><p><i>Clinical Trial registration</i>: Clinicaltrials.gov: NCT03812848. Date: January 1, 2018.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-04-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00791-w","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143818103","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}

{"title":"Phytochemical profiling of Clerodendrum speciosum leaves and evaluation of their antioxidant, antihyperglycemic and antiarthritic activities in vitro","authors":"Sameh S. Elhady,&nbsp;Rania F. Abou El-Ezz,&nbsp;Gokhan Zengin,&nbsp;Rania T. Malatani,&nbsp;Mohamed L. Ashour,&nbsp;Fadia S. Youssef","doi":"10.1186/s43094-025-00792-9","DOIUrl":"10.1186/s43094-025-00792-9","url":null,"abstract":"<div><h3>Background</h3><p><i>Clerodendrum speciosum</i> is a hybrid of <i>C. thomsonae</i> and <i>C. splendens</i>. Many biological and phytochemical studies have been performed on <i>C. thomsonae</i> and <i>C. splendens</i>, but few studies have been conducted on <i>C. speciosum.</i> Its methanol extract previously showed antioxidant activity in vivo via<i> Caenorhabditis elegans</i> model owing to its richness in flavonoids and phenylpropanoids.</p><h3>Results</h3><p>Characterization of <i>C. speciosum</i> leaf volatile constituents (CSV) was performed via gas chromatography linked to mass spectrometry (GC–MS). This revealed the presence of 29 metabolites that belonged mainly to oxygenated monoterpenes, sesquiterpenes and their oxygenated compounds, fatty acids and their esters. The latter constituted the predominant metabolites, whereas linoleic acid (30.64%) is the major metabolite. Liquid chromatography linked to mass spectrometry (LC–MS) was performed on the ethyl acetate fraction of <i>C. speciosum</i> leaves (CSE). This resulted in a tentative assignment of twenty-four peaks, whereas six peaks were not identified. These identified metabolites mainly belonged to phenylpropanoids, whereas flavonoids, iridoid glycosides, phenolic acids and their derivatives were also detected. The leaf volatile constituents showed notable antiarthritic activity as evidenced by the significant inhibition of albumin denaturation with an IC₅₀ of 32.50 μg/mL comparable that of diclofenac sodium (15.12 μg/mL). The leaf ethyl acetate fraction revealed potent antioxidant effect estimated by 725.43 ± 5.95 mg TE/g, 333.82 ± 19.9 mg TE/g, 2.1 ± 0.08 mmol TE/g and 3.69 ± 0.3 mg EDTA/g. in cupric-reducing antioxidant capacity (CUPRAC), 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), phosphomolybdenum (PHD) and metal-chelating activity (MCA) assays, respectively. It showed a reasonable <i>α</i>-glucosidase and <i>α</i>-amylase inhibition estimated by 1.88 ± 0.05 and 0.14 ± 0.01 mmol ACAE/g, respectively. ADME/TOPAKT assessment, processed on the prevalent identified components detected in CSV, displayed acceptable pharmacodynamic, toxicity and pharmacokinetic behaviors for most tested compounds except for <i>n</i>-nonadecane and <i>n</i>-heptacosane and <i>n</i>-octacosane.</p><h3>Conclusion</h3><p>Thus, <i>C. speciosum</i> leaves could serve as a promising treasure for the treatment of many diseases such as arthritis and diabetes mellitus owing to its abundance with flavonoids and terpenoidal compounds.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-04-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00792-9","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143786656","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}

{"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}

{"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}

{"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_app,A→B = 1.9 × 10⁻⁵ 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}

{"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 (IC₅₀ 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 (IC₅₀ 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}

{"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}