Future Journal of Pharmaceutical Sciences最新文献

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Pharmacognostic analysis and antimalarial evaluation of quercetin in Ilex umbellulata bark using HPTLC, in vitro screening, molecular docking, and network pharmacology
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-02-06 DOI: 10.1186/s43094-025-00771-0
James H. Zothantluanga, Dipak Chetia, Yasangam Umbon, T. C. Lalhriatpuii, Dhritiman Roy, Nidahun Lamare, Salem Lalvenhimi
{"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><sub>f</sub> = 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 IC<sub>50</sub> 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}
引用次数: 0
Cancer multi-omics-based differential expression analysis and prognostic potential of identified hub targets of myco-metabolites for breast carcinoma and lung carcinoma
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-02-05 DOI: 10.1186/s43094-025-00768-9
Singh Shreya, Debadatta Mohapatra, Gaurav Gopal Naik, Pooja Kathait, Soki Malang, Pradeep Patel,  Shambhavi, Gulzar Alam, Alakh N. Sahu
{"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}
引用次数: 0
Blue applicability grade index assessment and response surface modelling to synchronous determination of metformin hydrochloride, vildagliptin and dapagliflozin propanediol monohydrate by HPTLC method
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-02-03 DOI: 10.1186/s43094-025-00770-1
Pintu Prajapati, Krutika Patil, Dhrumi Naik, Veera Shakar Pulusu, Anzarul Haque, Mohd Abul Kalam, Shailesh Shah
{"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}
引用次数: 0
HSP90 inhibitors promote cell death by degrading Met and BCR::ABL1 in both imatinib-resistant and -sensitive chronic myeloid leukemia cells
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-01-27 DOI: 10.1186/s43094-025-00767-w
Masanobu Tsubaki, Taira Matsuo, Rie Komori, Noriaki Nagai, Tetsushi Yamamoto, Shozo Nishida
{"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}
引用次数: 0
Hepatoprotective potential of Chrysin in a rat model of isoniazid- and rifampicin-induced hepatic injury: suppression of matrix metalloproteinase and transforming growth factor β
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-01-27 DOI: 10.1186/s43094-025-00766-x
Deepa Mandlik, Akhilesh Tokey, Rohit Lokhande, Yash Dagadu, Heena Choudhary, Satish Mandlik
{"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}
引用次数: 0
Natural products targeting ubiquitination to combat kidney fibrosis
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-01-23 DOI: 10.1186/s43094-024-00757-4
Lianhua Li, Xinhui Huang, Yao Chen, Jibin Liu, Yuhang Qiao, Wenyu Fan, Peiqing Zhang, Xiaoming Yan, Ming Chen
{"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}
引用次数: 0
Evaluation of efficacy and safety of coenzyme Q10 in pediatric hemodialysis patients: a randomized controlled trial 评估辅酶Q10在儿童血液透析患者中的有效性和安全性:一项随机对照试验
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-01-21 DOI: 10.1186/s43094-024-00752-9
Salma A. Rahman Sharaf, Sarah Farid Fahmy, Heba M. Adel Abou Zaghla, Ahmed Hussein Hassan, Sara Mahmoud Zaki
{"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}
引用次数: 0
Novel tetracycline hybrids: synthesis, characterization, docking studies and in-vitro evaluation of antibacterial activity 新型四环素杂交种:合成、表征、对接研究和体外抗菌活性评价
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-01-15 DOI: 10.1186/s43094-025-00764-z
Mansi Shah, Bhanubhai Suhagia, Sunita Goswami, Sneha Sagar, Arpit Patwari
{"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 <sup>1</sup>HNMR. 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}
引用次数: 0
Abatement by Alhagi maurorum of lead-induced nephrotoxicity in rats: emphasis on Nrf2/HO-1 毛藻对铅致大鼠肾毒性的抑制作用:重点研究Nrf2/HO-1
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-01-14 DOI: 10.1186/s43094-025-00761-2
Mardi M. Algandaby
{"title":"Abatement by Alhagi maurorum of lead-induced nephrotoxicity in rats: emphasis on Nrf2/HO-1","authors":"Mardi M. Algandaby","doi":"10.1186/s43094-025-00761-2","DOIUrl":"10.1186/s43094-025-00761-2","url":null,"abstract":"<div><h3>Background</h3><p>Lead (Pb) is a heavy metal with extreme toxicity and numerous industrial uses. It produces nephrotoxicity with notable changes in renal architecture and function. The <i>Alhagi maurorum</i> (AM) belongs to the family <i>Fabaceae</i> and is native to the Middle East area. In the present study, the potential nephroprotective effects of AM in Pb-intoxicated rats were evaluated.</p><h3>Results</h3><p>AM methanolic extract was standardized in reference to its main phenolic compounds orientin, rutin, and quercetin. Acute oral toxicity studies indicated that the extract is safe for animals. Rats were allocated into five groups and treated for 28 days as follows: control, AM (200 mg/kg, orally), Pb (15 mg/kg, orally), Pb + AM (100 mg/kg), and Pb + AM (200 mg/kg). Pb administration markedly increased serum cystatin C, urea, creatinine levels, and urinary NAG. Pb also caused renal histopathological alterations. However, AM o-treatment ameliorated such pathological changes. In addition, AM treatment prevented Pb-induced accumulation of malondialdehyde (MDA), attenuated glutathione (GSH) depletion, and catalase (CAT) and superoxide dismutase (SOD) exhaustion. AM guarded against Pb-induced enhanced the protein expression of interleukin-6 (IL-6), tumor necrosis factor-alpha (TNF-α), cyclooxygenase-2 (COX-2), and nuclear factor-kappa B (NF-κB). Further, AM significantly prevented Pb-induced upregulation of mRNA levels of Bax and downregulation of Bcl-2. These effects were associated with increased levels of heme oxygenase-1 (HO-1) and nuclear factor erythroid 2-related factor 2 (Nrf2) in renal tissue.</p><h3>Conclusion</h3><p>AM guards against Pb-induced nephrotoxicity in rats that involve, at least partly, the antioxidant, anti-inflammatory, and anti-apoptotic activities as well as the modulation of HO-1 and Nrf2 expression.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-01-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00761-2","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142976608","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
Stability indicating eco-friendly HPLC method development and validation for the estimation of bisoprolol fumarate and telmisartan 富马酸比索洛尔和替米沙坦的高效液相色谱测定方法的建立与验证
IF 3.4
Future Journal of Pharmaceutical Sciences Pub Date : 2025-01-14 DOI: 10.1186/s43094-025-00760-3
Hitanshi Darji, Pratima Prajapati, Zarna Dedania, Ronak Dedania
{"title":"Stability indicating eco-friendly HPLC method development and validation for the estimation of bisoprolol fumarate and telmisartan","authors":"Hitanshi Darji,&nbsp;Pratima Prajapati,&nbsp;Zarna Dedania,&nbsp;Ronak Dedania","doi":"10.1186/s43094-025-00760-3","DOIUrl":"10.1186/s43094-025-00760-3","url":null,"abstract":"<div><h3>Background</h3><p>Telmisartan and bisoprolol fumarate together are two medications that diminish arterial pressure. The current study comprises an evaluation of the proposed methodology's greenness regarding the HPLC method used to govern the medication mixture regardless of dose form A novel stability suggesting HPLC method's environmental effect was evaluated using the greenness metrics. Stress conditions comprising acidic, alkaline, oxidative, thermal, and photolytic degradation were applied for both of the medications.</p><h3>Results</h3><p>The RP—HPLC method employing a reversed-phase C<sub>18</sub> column with a gradient approach, the HPLC chromatography was carried out. The mobile phase consisted of acetonitrile, methanol, and phosphate buffer (60:35:5, %v/v/v), with the stationary phase being the Unisphere C<sub>18</sub> column Agela Tech. The RP-HPLC method uses UV detection at 224 nm with chromatographic purification spanning linearities of 2.5–12.5 μg/mL for bisoprolol fumarate and 40.0–200.0 μg/mL for telmisartan, correspondingly. The procedure is accurate and precise, as demonstrated by an outcome that % RSD inside the permissible range. Additionally, various stressors were introduced to the medications. The approach's green credentials with respect to solvent utilization, chemical substances, expenditure of energy, and waste formation have been verified by the greenness data collected during the evaluation. No chromatographic or spectrum impediments caused by formulation additives have been observed.</p><h3>Conclusion</h3><p>Bisoprolol fumarate and telmisartan could be measured simultaneously using the devised RP-HPLC method, which was simple, quick, sensitive, accurate, precise, linear, and stability indicating. The proposed approach showed ecological friendliness, robustness, sensitivity, and ease of use. As a result, the devised method could be applied to the regular quality checking of tablets and bulk medications.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2025-01-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00760-3","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142976540","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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