Future Journal of Pharmaceutical Sciences最新文献

{"title":"Detection, isolation, characterization, analytical method development with validation and in-silico analysis of new impurity in rivaroxaban","authors":"Manohar Reddy Epuru,&nbsp;Jagadam Saroja,&nbsp;Veera Venkata Nanda Kishore Pilli,&nbsp;Ravinder Reddy Vennapureddy","doi":"10.1186/s43094-025-00763-0","DOIUrl":"10.1186/s43094-025-00763-0","url":null,"abstract":"<div><h3>Background</h3><p>For rivaroxaban (RRBN) to be safe and effective, its quality and impurities need to be evaluated. One new impurity (IMP-20.15/2.57) was found during the analysis of intermediate stage compound of RRBN production. The isolation of IMP-20.15/2.57 was achieved by preparative HPLC, using 10 mM ammonium acetate and acetonitrile (gradient elution mode) as mobile phase. The IMP-20.15/2.57 was elucidated using mass spectrometer, FT-IR and NMR (¹H and ¹³C) techniques. A gradient RP-HPLC method was developed for IMP-20.15/2.57 quantification in RRBN API. The chromatographic separation of IMP-20.15/2.57 was done on a Zorbax Eclipse XDB [C18 3.0 mm × 15 cm, 3.5 µm] column with UV detection programmed at 250 nm. Solution A (methanol and buffer have been blended in a 05:95 v/v ratio) and Solution B (acetonitrile) make up the gradient mobile phase. The three batches of RRBN API were analyzed with the developed gradient RP-HPLC approach for the content of IMP-20.15/2.57. Risk assessment tests for IMP-20.15/2.57 were conducted utilizing in silico programs.</p><h3>Results</h3><p>The IMP-20.15/2.57 was elucidated as 4-(4-(2-hydroxy-3-(2-hydroxy-3-(4-(3-oxomorpholino) phenyl amino) propyl amino) propyl amino) phenyl) morpholin-3-one using mass spectrometer, FT-IR and NMR (¹H and ¹³C) techniques. The novel approach was evaluated in accordance with ICH requirements for linearity (0.2495–1.4971 µg/mL; R²-0.99958), accuracy (109.97–117.71% recovery), precision (0.6015–0.9211%RSD), specificity (996.5 peak purity), robustness (no significant variation in retention time and resolution), and quantification limitations (0.2495 µg/mL). The results were deemed appropriate. It became apparent that the IMP-20.15/2.57 content in three batches of RRBN API were below the quantification limits. The <i>in-silico</i> program suggested that there was certainly no possibility of mutagenicity with IMP-20.15/2.57.</p><h3>Conclusion</h3><p>The present gradient RP-HPLC approach suits best for the IMP-20.15/2.57 quantification in RRBN API and offers more effective ways to guarantee the safety of patients and the quality of RRBN.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00763-0","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143373248","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":"Safety profiles of IDH inhibitors: a pharmacovigilance analysis of the FDA Adverse Event Reporting System (FAERS) database","authors":"Ximu Sun,&nbsp;Han Zhou,&nbsp;Yanming Li,&nbsp;Yanhui Luo,&nbsp;Qixiang Guo,&nbsp;Yixin Sun,&nbsp;Chenguang Jia,&nbsp;Bin Wang,&nbsp;Maoquan Qin,&nbsp;Peng Guo","doi":"10.1186/s43094-025-00769-8","DOIUrl":"10.1186/s43094-025-00769-8","url":null,"abstract":"<div><h3>Background</h3><p>With the increased use of isocitrate dehydrogenase (IDH) inhibitors in acute myeloid leukemia (AML) and cholangiocarcinoma, the toxicity of these drugs is a growing concern. This study aimed to evaluate the adverse events (AEs) of IDH inhibitors based on the Food and Drug Administration Adverse Event Reporting System (FAERS) database.</p><h3>Methods</h3><p>AE reports for IDH inhibitors (enasidenib, ivosidenib, and olutasidenib) were collected and analyzed from the time of launch through the first quarter of 2024. Only IDH inhibitors reported as the target drug and coded as the primary suspect (PS) were included in the analysis. AEs were standardized and classified according to the preferred term (PT) and system organ classification (SOC) in the Medical Dictionary for Regulatory Activities (MedDRA) version 26.0. Disproportionality analyses including the reporting odds ratio and the Bayesian confidence propagation neural network were performed in data mining to assess IDH inhibitor-relatedAEs. Differentiation syndrome was the AE of special interest.</p><h3>Results</h3><p>The reports number of enasidenib, ivosidenib, and olutasidenib was 11 616 357, 10 067 250, and 2 563 464, respectively. A total of 80 enasidenib-related signals involving 15 SOCs, 78 ivosidenib-related signals involving 17 SOCs, and 7 olutasidenib-related signals involving 4 SOCs were obtained. The most signals reported were “blood and lymphatic system disorders,” “infections and infestations,” and “nervous system disorders” in enasidenib. For signals of ivosidenib, the most frequently reported were “gastrointestinal disorders,” “general disorders and administration site conditions,” and “injury, poisoning and procedural complications.” Ivosidenib was the only IDH inhibitor with signals in “cardiac disorders.” Differentiation syndrome events were reported in 89, 40, and 2 cases for enasidenib, ivosidenib, and olutasidenib, respectively. The median time to onset was 26–31 days for ivosidenib and enasidenib. AML was the most common indication in the differentiation syndrome reports.</p><h3>Conclusions</h3><p>Our study identifies potential AE signals associated with IDH inhibitors and provides a broader understanding of the safety. The safety profiles highlight the need for long-term safety monitoring of IDH inhibitor recipients. Promptly monitoring and intervention in specific organ systems depending on the type of IDH inhibitor may improve the overall survival or enhance the quality of life. In the future, it will be necessary to validate our findings in prospective large-scale studies and to investigate the underlying mechanisms.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-02-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00769-8","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143361603","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":"Pharmacognostic analysis and antimalarial evaluation of quercetin in Ilex umbellulata bark using HPTLC, in vitro screening, molecular docking, and network pharmacology","authors":"James H. Zothantluanga,&nbsp;Dipak Chetia,&nbsp;Yasangam Umbon,&nbsp;T. C. Lalhriatpuii,&nbsp;Dhritiman Roy,&nbsp;Nidahun Lamare,&nbsp;Salem Lalvenhimi","doi":"10.1186/s43094-025-00771-0","DOIUrl":"10.1186/s43094-025-00771-0","url":null,"abstract":"<div><h3>Background</h3><p>The bark of <i>Ilex umbellulata</i> is traditionally used for the treatment of many diseases such as malaria. Despite its traditional relevance, the pharmacognostic parameters and pharmacological properties remained unexplored. In this study, we aim to develop the missing pharmacognostic parameters with modern analytical techniques and carry out multi-step computational studies to study the antimalarial potential of <i>I. umbellulata</i>.</p><h3>Results</h3><p>The bark was 2–6 mm thick, composed of different colored layers, and was bitter-sweet in taste. Powdered microscopy revealed the presence of starch granules, calcium oxalate crystals, cork cells, trichomes, and fibers. Physicochemical properties such as ash values (total, acid-insoluble, and water-soluble), extractive values (petroleum ether, chloroform, ethyl acetate, methanol, aqueous, 80% MeOH), moisture content, swelling index, fluorescence, and pH of the bark were determined. FT-IR fingerprint profiling of petroleum ether, chloroform, ethyl acetate, methanol, aqueous, and 80% MeOH extracts revealed characteristic bands at different wavelengths that are indicative of the presence of certain functional groups. HPTLC fingerprint profiling with a mobile phase of hexane: ethyl acetate: formic acid (4.5:5.5:0.5 v/v) revealed 9 characteristic peaks. With a mobile phase of toluene: ethyl acetate: formic acid (5:4:0.2 v/v), the validated TLC densitometric studies revealed the presence of 2.07 mg of quercetin (<i>R</i>_f = 0.477 ± 0.005) in 100 mg of 80% MeOH bark extract of <i>I. umbellulata</i>. JazQSAR web tool previously developed by us predicts the IC₅₀ of quercetin against <i>Plasmodium falciparum</i> as 3.88 ± 0.35 µM, which was not far from the practically observed value for quercetin. Multi-target molecular docking with a validated docking protocol revealed that quercetin could potentially interact with 20 proteins of <i>P. falciparum</i> that are highly expressed during the schizont and trophozoite stages. Network pharmacology studies revealed that quercetin could potentially alleviate malaria mainly by inhibiting pro-inflammatory response through the action of IL-4, IL-10, and IL-13 and by triggering the immune system.</p><h3>Conclusions</h3><p>The pharmacognostic parameters of <i>I. umbellulata</i> bark may be used as quality control parameters to aid in identification and authentication and to prevent adulteration. The results obtained from the multi-target molecular docking and network pharmacology studies support the use of <i>I. umbellulata</i> as a traditional herbal remedy against malaria.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-02-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00771-0","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143361604","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":"Cancer multi-omics-based differential expression analysis and prognostic potential of identified hub targets of myco-metabolites for breast carcinoma and lung carcinoma","authors":"Singh Shreya,&nbsp;Debadatta Mohapatra,&nbsp;Gaurav Gopal Naik,&nbsp;Pooja Kathait,&nbsp;Soki Malang,&nbsp;Pradeep Patel,&nbsp; Shambhavi,&nbsp;Gulzar Alam,&nbsp;Alakh N. Sahu","doi":"10.1186/s43094-025-00768-9","DOIUrl":"10.1186/s43094-025-00768-9","url":null,"abstract":"<div><h3>Background</h3><p>Breast carcinoma (BC) and lung carcinoma (LC) have the highest incidence and mortality rates worldwide. In prior work, studied sample hub targets contributing to anticancer potential against BC and LC were identified through network pharmacology. In the present work, web servers UALCAN, GEPIA2, and KM plotter were used to explore the genomic and proteomic expression of these hub targets, along with their prognosis potential in BC and LC.</p><h3>Results</h3><p>Differential hub targets SRC, MAPK3, PTPN11, JAK2, ESR1, and HAP900A1 for BC and PTPN11, JAK2, ESR1, EGFR, and MAPK3 for LC, showed good prognostic potentials. Collectively, PTPN11, JAK2, and ESR1 were overlapped differential expressed hub targets involved in the significantly good prognosis of both carcinoma.</p><h3>Conclusion</h3><p>These differentially expressed hub targets may be taken into account for future BC and LC treatments due to their strong prognostic potential.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-02-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00768-9","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143184762","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":"Blue applicability grade index assessment and response surface modelling to synchronous determination of metformin hydrochloride, vildagliptin and dapagliflozin propanediol monohydrate by HPTLC method","authors":"Pintu Prajapati,&nbsp;Krutika Patil,&nbsp;Dhrumi Naik,&nbsp;Veera Shakar Pulusu,&nbsp;Anzarul Haque,&nbsp;Mohd Abul Kalam,&nbsp;Shailesh Shah","doi":"10.1186/s43094-025-00770-1","DOIUrl":"10.1186/s43094-025-00770-1","url":null,"abstract":"<div><p>Diabetes mellitus is major chronic disease found in human due to stressful lifestyle and bad food habit. Recently, the Central Drugs Standard Control Organization of India has approved combination of metformin hydrochloride, vildagliptin and dapagliflozin propanediol monohydrate for the management of diabetes mellitus. Numerous chromatographic methods have been published in the literature for estimation of these anti-diabetic drugs on individual basis and their combinations. But these chromatographic analyses promoted usage of toxic organic solvents which are harmful to the environment and aquatic animal lives. In addition, no chromatographic method was found in the literature for simultaneous estimation of these anti-diabetic drugs using green solvents. In recent days, white analytical chemistry approach has been introduced in the literature for development and assessment of green, accurate, precise, cost-effective and user-friendly chromatographic methods. Hence, white analytical chemistry-driven risk-based HPTLC method was developed for synchronous estimation of these anti-diabetic drugs using green solvents and response surface modelling. The analytical quality risk assessment was applied for identification of critical method variables and response variables using risk priority number ranking and filtering method. The critical method variables were linked with critical response variables using response surface modelling by Box–Behnken design. The analytical design space was navigated control strategy was framed for robust densitometric estimation of anti-diabetic drugs. The chromatographic method was validated as per ICH Q2 (R2) guideline. The developed method was applied for synchronous assay of multiple combinations of metformin, vildagliptin and dapagliflozin using single chromatographic condition to save time, cost and resources for analysis. The assay results of these anti-diabetic drug combinations were found to be complied with the respective labelled claim of the drugs. The developed and published chromatographic methods were assessed for their redness, greenness, blueness and whiteness profiles using green analytical metrics and RGB model scoring system. The proposed method was found to be green, cost-effective, robust and user-friendly for synchronous estimation of metformin, vildagliptin and dapagliflozin.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-02-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00770-1","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143108283","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":"HSP90 inhibitors promote cell death by degrading Met and BCR::ABL1 in both imatinib-resistant and -sensitive chronic myeloid leukemia cells","authors":"Masanobu Tsubaki,&nbsp;Taira Matsuo,&nbsp;Rie Komori,&nbsp;Noriaki Nagai,&nbsp;Tetsushi Yamamoto,&nbsp;Shozo Nishida","doi":"10.1186/s43094-025-00767-w","DOIUrl":"10.1186/s43094-025-00767-w","url":null,"abstract":"<div><h3>Background</h3><p>Chronic myeloid leukemia is associated with a more favorable prognosis following treatment with BCR::ABL1 tyrosine kinase inhibitors (TKIs). Nonetheless, about 40% of affected individuals with CML display resistance or intolerance towards BCR::ABL1 TKIs. Heat shock protein 90 (HSP90) functions as a molecular chaperone and is known for its overexpression in various types of cancer, thereby HSP90 is a potential candidate for the treatment of BCR::ABL1 TKI-resistant and -sensitive CML. In present study, we aimed to investigate whether HSP90 inhibitors promote cell death in imatinib-resistant and -sensitive CML cells.</p><h3>Results</h3><p>KW-2478 and NVP-AUY922, which are HSP90 inhibitors, promoted cell death in both imatinib-resistant and -sensitive CML cells. Imatinib-resistant cells showed greater sensitivity to HSP90 inhibitors in comparison to imatinib-sensitive cells. KW-2478 inhibited the activation of Akt, extracellular regulated protein kinase 1/2, and c-Jun N-terminal kinase 1/2 in imatinib-resistant and -sensitive CML cells by promoting Met and BCR::ABL1 degradation.</p><h3>Conclusion</h3><p>These findings indicate inhibition of HSP90 such as KW-2478 and NVP-AUY922 as potential candidates for CML therapy.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-01-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00767-w","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143109419","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":"Hepatoprotective potential of Chrysin in a rat model of isoniazid- and rifampicin-induced hepatic injury: suppression of matrix metalloproteinase and transforming growth factor β","authors":"Deepa Mandlik,&nbsp;Akhilesh Tokey,&nbsp;Rohit Lokhande,&nbsp;Yash Dagadu,&nbsp;Heena Choudhary,&nbsp;Satish Mandlik","doi":"10.1186/s43094-025-00766-x","DOIUrl":"10.1186/s43094-025-00766-x","url":null,"abstract":"<div><h3>Background</h3><p>The ability of Chrysin (CHY) to scavenge free radicals has been widely explored. The scope of the research was to show that CHY protects the rat liver against damage caused by the drugs isoniazid (INH) and rifampicin (RFM).</p><h3>Results</h3><p>Rats were divided into 6 groups, each of which had six rats. Isoniazid (100 mg/kg, p.o.) and rifampicin (100 mg/kg, p.o.) were administered to Group II to VI rats for 21 days; this caused hepatocellular damage. CHY was administered in the dose of 50, 75, and 100 mg/kg, p.o. body weight to Group III to V rats before administration of INH + RFM. In this study, Group VI Silymarin (100 mg/kg, p.o.) functioned as the standard drug. The blood was drawn as the study was done, and tests for oxidative stress indicators, haematological parameters, biochemical parameters, and pro-inflammatory cytokines were performed. The liver samples were subjected to histopathology. The administration of CHY (50, 75, and 100 mg/kg) restored serum biochemical, haematological, proteins, and lipid parameters. Due to the administration of CHY, the levels of superoxide dismutase (SOD), glutathione oxidase (GSH), myeloperoxidase (MPO) and catalase (CAT) were also restored. The inflammatory cytokines such as tumour necrosis factor-α (TNF-α), interleukin-6 (IL-6), interleukin-1β (IL-1β), matrix metalloproteinase-2 (MMP-2), matrix metalloproteinase-9 (MMP-9), transforming growth factor-β (TGF-β), malondialdehyde (MDA), myeloperoxidase (MPO) and nitric oxide (NO) levels were found to be decreased. The alterations in the biochemical parameters were reinforced by histological analysis of liver tissue.</p><h3>Conclusions</h3><p>It is concluded that the CHY protects against INH + RFM-induced oxidative liver injury in rats.</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":"2025-01-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00766-x","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143109440","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":"Natural products targeting ubiquitination to combat kidney fibrosis","authors":"Lianhua Li,&nbsp;Xinhui Huang,&nbsp;Yao Chen,&nbsp;Jibin Liu,&nbsp;Yuhang Qiao,&nbsp;Wenyu Fan,&nbsp;Peiqing Zhang,&nbsp;Xiaoming Yan,&nbsp;Ming Chen","doi":"10.1186/s43094-024-00757-4","DOIUrl":"10.1186/s43094-024-00757-4","url":null,"abstract":"<div><h3>Background</h3><p>Kidney fibrosis is a crucial component that contributes to end-stage renal disease and is the inevitable last pathological process in many progressive chronic kidney diseases (CKD). Ubiquitination, one of the most refined and widespread reversible post-translational modifications, plays a significant role in the development of renal fibrosis through its regulation and deubiquitination processes.</p><h3>Main body of the abstract</h3><p>Recent studies have shown that ubiquitination and deubiquitination represent promising intervention targets against renal fibrosis, with numerous natural products intervening in renal fibrosis by regulating the processes of ubiquitination and signal pathways such as transforming growth factor-<i>β</i>1/Smads (TGF-<i>β</i>1/Smads), Wnt/<i>β</i>-catenin, Janus kinase/signal transducer and activator of transcription/suppressor of cytokine signaling (JAK/STAT/SCOS), and nuclear factor erythroid-derived 2-like 2 (Nrf2), and then link.</p><h3>Conclusion</h3><p>Herein, we summarize the processes of ubiquitination and deubiquitination and introduce the interactions between ubiquitination and natural products. This is conducive to the development of new candidate drugs that intervene in renal fibrosis through the regulation of ubiquitination, representing a promising strategy to combat renal fibrosis with natural products.</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":"2025-01-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00757-4","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143108895","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":"Evaluation of efficacy and safety of coenzyme Q10 in pediatric hemodialysis patients: a randomized controlled trial","authors":"Salma A. Rahman Sharaf,&nbsp;Sarah Farid Fahmy,&nbsp;Heba M. Adel Abou Zaghla,&nbsp;Ahmed Hussein Hassan,&nbsp;Sara Mahmoud Zaki","doi":"10.1186/s43094-024-00752-9","DOIUrl":"10.1186/s43094-024-00752-9","url":null,"abstract":"<div><h3>Background</h3><p>There is evidence from clinical trials that coenzyme Q10 significantly improves mitochondrial function and decreases oxidative stress and cardiovascular disease in adult hemodialysis patients. However, we have never fully investigated its role in pediatric patients before. This study aimed to assess the effects of coenzyme Q10 supplementation on oxidative stress and inflammatory markers in pediatric hemodialysis patients. This was a prospective, randomized, double-blinded, placebo-controlled trial. Thirty-six pediatric hemodialysis patients were recruited and simply randomized to receive either oral coenzyme Q10 (3–5 mg/kg) daily or placebo daily for 12 weeks.</p><h3>Results</h3><p>Using the Mann–Whitney test, children in the intervention group showed a significant reduction in the median percent change of blood urea nitrogen from baseline of − 58.18 versus − 9.6 in the placebo group (<i>p</i> = 0.002). The median percent change of serum malondialdehyde significantly decreased by − 55.68 in the intervention group, while it increased by 39.75 in the placebo group (<i>p</i> &lt; 0.001). Additionally, the median percent change from baseline in serum tumor necrosis factor-α levels significantly decreased by − 46.69 in the intervention group and increased by 8.5 in the placebo group (<i>p</i> = 0.03).</p><h3>Conclusion</h3><p>Supplementation of oral coenzyme Q10 may have beneficial effects on oxidative stress and inflammatory markers in pediatric hemodialysis patients. This study emphasized the potential efficacy of an average coenzyme Q10 dose of 4 mg/kg/day in pediatric hemodialysis patients; this gives the green light for other researchers to confidently evaluate larger doses as an attempt to control the systemic inflammation in this patient population. Further research is needed to determine whether coenzyme Q10 treatment improves clinical outcomes such as infection, hospitalization, cardiovascular events, and mortality in pediatric hemodialysis patients.</p><p><i>Trial Registration</i> Clinical trials.gov, NCT05170893, Registered 28 December 2021, https://clinicaltrials.gov/study/NCT05170893?cond=NCT05170893&amp;rank=1.</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":"2025-01-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00752-9","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142995748","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":"Novel tetracycline hybrids: synthesis, characterization, docking studies and in-vitro evaluation of antibacterial activity","authors":"Mansi Shah,&nbsp;Bhanubhai Suhagia,&nbsp;Sunita Goswami,&nbsp;Sneha Sagar,&nbsp;Arpit Patwari","doi":"10.1186/s43094-025-00764-z","DOIUrl":"10.1186/s43094-025-00764-z","url":null,"abstract":"<div><h3>Background</h3><p>The biggest menace in the world today is the infection caused by pathogenic bacteria in humans, where majority of the available antibiotics fail to provide therapeutic results due to resistance. The discovery of new molecules is the need of the hour and several research groups worldwide are contributing to fight this scare. This work highlights our efforts towards discovering novel tetracycline hybrids that could serve as potent agents against several pathogenic bacterial strains causing infections. In total, ten compounds were synthesized which were chemically conjugates of Minocycline, an age-old tetracycline, and naturally occurring aldehydes and ketones available from the plant sources. Structural characterization of these compounds was done using Mass and ¹HNMR. Molecular docking was carried out in order to predict the binding affinity of these compounds to various bacterial enzymes and known protein targets and to establish the structure–activity relationships. Molecular dynamic simulation studies and in silico pharmacokinetic and toxicity prediction studies were done to determine in silico pharmacokinetics and toxicity of compounds. In-vitro antibacterial activities were done using standard protocols against gram positive bacteria like <i>Enterococcus faecalis, Staphylococcus aureus</i> and gram-negative bacteria like <i>Klebsiella pneumoniae, Pseudomonas aeruginosa and Escherichia coli</i>.</p><h3>Results</h3><p>Promising results were obtained viz. compound 1,2 and 10 were found to be more potent against <i>Staphylococcus aureus</i>, compound 1 against <i>Enterococcus</i> <i>faecalis</i>, compound 2 and 3 against <i>Escherichia coli</i>, compound 7 and 8 against <i>Pseudomonas aeruginosa</i> and compound 7 against <i>Klebsiella pneumoniae</i> when compared with minocycline as standard compound.</p><h3>Conclusion</h3><p>All the synthesized compounds were screened for their anti-bacterial activity against gram positive and gram negative microorganisms. Amongst the ten synthesized minocycline hybrids, four minocycline hybrids exhibited potent antibacterial activity as compared to minocycline. These hybrids can serve as a promising lead compound for antibiotic drug discovery.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00764-z","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142976530","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}