Pharmaceutical Chemistry Journal最新文献_第7页

Resveratrol, Tyrosol and Their Derivatives Inhibit Platelet Activating Factor Biosynthetic Enzymes in Homogenized U-937 Cells 白藜芦醇、酪醇及其衍生物抑制匀浆 U-937 细胞中的血小板活化因子生物合成酶

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-06-22 DOI: 10.1007/s11094-024-03137-7

Filio Petsini, Maria Detopoulou, Ioannis K. Kostakis, Elizabeth Fragopoulou, Smaragdi Antonopoulou

{"title":"Resveratrol, Tyrosol and Their Derivatives Inhibit Platelet Activating Factor Biosynthetic Enzymes in Homogenized U-937 Cells","authors":"Filio Petsini, Maria Detopoulou, Ioannis K. Kostakis, Elizabeth Fragopoulou, Smaragdi Antonopoulou","doi":"10.1007/s11094-024-03137-7","DOIUrl":"https://doi.org/10.1007/s11094-024-03137-7","url":null,"abstract":"Platelet activating factor (PAF) is a potent lipid mediator involved in inflammation, among other pathophysiological conditions. Bioactive compounds from foods have been suggested to suppress inflammation as well as regulate PAF biosynthesis. Phenolics, such as resveratrol and tyrosol, and their acetylated derivatives, inhibited PAF biosynthetic enzymes’ activity, namely acetyl-coenzyme A: lyso–platelet-activating factor acetyltransferases (lysoPAF-AT), and 1-alkyl-2-acetyl-sn-glycerol cholinephosphotransferase (PAF-CPT) under inflammatory stimuli. This study investigates whether resveratrol and tyrosol lipophilic derivatives are capable of affecting the activity of the two isoforms of lysoPAF-AT along with the activity of PAF-CPT compared with the initial compounds under basal conditions. The derivatives were chemically synthesized and the experiments were conducted either with or without pre-incubation of homogenized U-937 cells and the phenolics and the enzyme activities were determined. Pre-incubation experiments resulted in lower half inhibitory concentration (IC50) than those without pre-incubation, reaching a 5-fold difference between them. Moreover, there were differences among parent compounds and their derivatives, suggesting a dependence on the differently substituted groups of the phenolics. PAF-CPT tends to be less phenolic structure dependent than lysoPAF-ATC, whereas the other isoform, lysoPAF-ATE, was less sensitive in general. Resveratrol and its derivatives were more potent than the tyrosolic compounds, regardless of the enzyme test or the conditions of the experiment. The use of phenolic lipophilic derivatives in pharmaceuticals and in food preparation may overcome the limitations of natural phenolics with regard to their weak solubility and stability in a lipophilic environment.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"31 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-06-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141526516","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Chemical Compositions and Pharmacological Activities of Iberis amara L. (A Review) Iberis amara L.的化学成分和药理活性（综述）

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-06-22 DOI: 10.1007/s11094-024-03145-7

Xingyu Liu, Xiaohan Wang, Hans Gregersen, Jing Zuo

引用次数: 0

Toxicity and Antihypoxic Activity of a Preparation Containing a Complex Compound of 5-Hydroxy-6-Methyluracil with N-Acetyl Cysteine 含有 5-羟基-6-甲基尿嘧啶与 N-乙酰半胱氨酸复合物的制剂的毒性和抗缺氧活性

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-06-22 DOI: 10.1007/s11094-024-03131-z

G. G. Kutlugildina, Yu. S. Zimin, A. R. Gimadieva, E. F. Repina, E. R. Kudoyarov

引用次数: 0

Synthesis and Biological Evaluation of Arctigenin-Dipeptide Derivatives as Potential Anti-Fatigue Agents 作为潜在抗疲劳剂的 Arctigenin-二肽衍生物的合成与生物学评价

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-06-22 DOI: 10.1007/s11094-024-03140-y

Wanbo Zeng, Siyuan Li, Weiguo Shi, Junjie Tan, Xiang Li, Liang Xu

{"title":"Synthesis and Biological Evaluation of Arctigenin-Dipeptide Derivatives as Potential Anti-Fatigue Agents","authors":"Wanbo Zeng, Siyuan Li, Weiguo Shi, Junjie Tan, Xiang Li, Liang Xu","doi":"10.1007/s11094-024-03140-y","DOIUrl":"https://doi.org/10.1007/s11094-024-03140-y","url":null,"abstract":"Fatigue is a physiological phenomenon experienced by the human body when it undergoes prolonged physical and mental exertion, which can have detrimental effects on both health and work productivity. Previous research has demonstrated that arctigenin (ArcG) has the ability to enhance the physical performance of mice during exercise. In this study, five ArcG derivatives containing different dipeptides coupled via an ethoxy linker were synthesized and tested for their activities to improve exercise performance in mice. All of the derivatives extended the exhaustion distance of mice in the running wheel test. Derivative Z-B-4 exhibited the highest activity, showing that the mice ran a distance 1.3-fold greater than that of the ArcG group and 3.4-fold greater than that of the sport control group. Furthermore, Z-B-4 was found to increase the concentrations of superoxide dismutase (SOD) and catalase (CAT), while simultaneously decreasing levels of lactic acid (LA) and blood urea nitrogen (BUN) during exercise. This study provides new references and promising lead compounds for the development of antifatigue agents.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"14 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-06-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141526520","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Physical Stability of Ibuprofen Upon Co-Milling with Caffeine and Polyvinylpyrrolidone at Room Temperature 布洛芬在室温下与咖啡因和聚乙烯吡咯烷酮共研磨时的物理稳定性

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-06-21 DOI: 10.1007/s11094-024-03148-4

M. Bejaoui, R. Djemi, S. Kouass, H. Galai

{"title":"Physical Stability of Ibuprofen Upon Co-Milling with Caffeine and Polyvinylpyrrolidone at Room Temperature","authors":"M. Bejaoui, R. Djemi, S. Kouass, H. Galai","doi":"10.1007/s11094-024-03148-4","DOIUrl":"https://doi.org/10.1007/s11094-024-03148-4","url":null,"abstract":"The purpose of this work is to investigate the physical stability of a ternary amorphous system (Ibuprofen, Caffeine, Polyvinylpyrrolidone (PVP K30)) generated by co-milling technique at room temperature, as well as the intermolecular interactions that could contribute to physical stabilization of amorphous ibuprofen (a poorly water-soluble drug). The milled mixtures were characterized by x-ray diffraction (XRD), infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and scanning electronic microscopy (SEM). As shown by XRD results, amorphous Ibuprofen maintains its physical stability even after exposure to high humidity levels (RH = 75%, T = 40°C) for 6 months. FTIR results highlighted the establishment of hydrogen bonds in the binary and ternary systems involving the carboxylic group of Ibuprofen. At higher amounts (more than 75%), the polyvinylpyrrolidone has totally amorphized drug/caffeine mixtures and inhibited polymorphic transition of Caffeine (Form II ≥ Form I) which occurred at higher temperatures. Thus, this polymer has shown an ability to stabilize amorphous solid dispersion (Ibuprofen: Caffeine) and preserve the chemical structure of each molecule.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"59 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141526670","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Review of the Modern Market of Reagents for the Detection of Bacterial Endotoxins in Drugs 检测药物中细菌内毒素的现代试剂市场回顾

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-06-21 DOI: 10.1007/s11094-024-03149-3

O. V. Shapovalova, A. O. Tutnova, N. P. Neugodova, G. A. Sapozhnikova

引用次数: 0

Cytotoxic and Apoptosis-Inducing Activities of Iridium Complexes Bearing 2-Phenylimidazo[4,5-f][1,10]-Phenanthroline Derivatives in Human Cancer Cells 含有 2-苯基咪唑并[4,5-f][1,10]-菲罗啉衍生物的铱络合物在人类癌细胞中的细胞毒性和凋亡诱导活性

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-06-21 DOI: 10.1007/s11094-024-03139-5

Doğukan Mutlu, Cengiz İpek, Çiğdem Şahin, Şevki Arslan

{"title":"Cytotoxic and Apoptosis-Inducing Activities of Iridium Complexes Bearing 2-Phenylimidazo[4,5-f][1,10]-Phenanthroline Derivatives in Human Cancer Cells","authors":"Doğukan Mutlu, Cengiz İpek, Çiğdem Şahin, Şevki Arslan","doi":"10.1007/s11094-024-03139-5","DOIUrl":"https://doi.org/10.1007/s11094-024-03139-5","url":null,"abstract":"In recent years, there has been growing exploration of organometallic transition metal complexes as promising options for developing anticancer agents that offer the potential of reduced toxicity compared with the commonly utilized cisplatin analogs. In this respect, iridium complexes containing 2-phenylimidazo- [4,5-f][1,10]-phenanthroline derivatives with different substituents were investigated in different cell lines as potential anticancer agents. All the compounds exhibited potent cytotoxic activity against Caco-2, HeLa, A549, and MDA-MB-231 cell lines. EC50 values of compound 1 were found to be 6.44 μM for Caco-2, 24.78 μM for HeLa, 9.14 μM for A549, and 4.45 μM for the MDA-MB-231 cell line. Similarly, EC50 of 3 was found at 15.07, 14.15, 10.33, and 4.48 μM respectively. The EC50 value of 2 was found to be 12.71 μM for Caco-2, 24.31 μM for HeLa, and 7.44 μM for MDA-MB-231 cells. EC50 values of compound 4 were found to be 28.20 μM for Caco-2, 12.79 μM for HeLa, 8.33 μM for A549, and 3.76 μM for the MDA-MB-231 cell line. The results of gene expression and flow-cytometry analysis showed that the compounds caused the induction of apoptosis in all cancer cell lines by changing caspase 3, Bcl-2, and Bax proteins. The obtained results demonstrate that compounds could be introduced as potent agents to prevent the progression of certain types of cancer. However, preclinical and clinical trials will be needed to evaluate these complexes to obtain safe, effective, and optimal therapeutic drugs for cancer patients.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"29 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141526525","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

E1231 Alleviates Diabetic Cardiomyopathy by Regulating the Silent Information Regulator 1/Peroxisome Proliferator-Activated Receptor-γ Coactivator-1α/Nuclear Factor Erythroid 2-Related Factor 2 Pathway E1231 通过调节沉默信息调节器 1/Peroxisome Proliferator-Activated Receptor-γ Coactivator-1α/Nuclear Factor Erythroid 2-Related Factor 2 通路减轻糖尿病心肌病的病情

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-06-21 DOI: 10.1007/s11094-024-03138-6

Yunxia Cui, Hongjun Lou, Qi Guo, Guiyun Qi, Xi Gao

{"title":"E1231 Alleviates Diabetic Cardiomyopathy by Regulating the Silent Information Regulator 1/Peroxisome Proliferator-Activated Receptor-γ Coactivator-1α/Nuclear Factor Erythroid 2-Related Factor 2 Pathway","authors":"Yunxia Cui, Hongjun Lou, Qi Guo, Guiyun Qi, Xi Gao","doi":"10.1007/s11094-024-03138-6","DOIUrl":"https://doi.org/10.1007/s11094-024-03138-6","url":null,"abstract":"We aimed to investigate the underlying function and mechanism of E1231 against diabetic cardiomyopathy (DCM). H9c2 cells were exposed to either 33 mmol/L mannitol or an identical concentration of glucose (high glucose, HG) in vitro. In vivo, diabetes mellitus (DM) mice were induced by injection of 60 mg/kg streptozotocin intraperitoneally. E1231 was used to treat cells (5 mmol/L) or animals (40 mg/kg), and subsequent assays were conducted to determine its effect on DCM-associated manifestations. Western blot was employed to evaluate protein expressions of the silent information regulator 1 (SIRT1), peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α), and nuclear factor erythroid 2-related factor 2 (Nrf2). In vitro, treatment with E1231 significantly reduced oxidative stress and apoptosis induced by HG via activating the SIRT1-PGC-1α/Nrf2 pathway in H9c2 cells, compared to cardiomyocytes under HG conditions. In vivo, DM mice showed up-regulated SIRT1, PGC-1α, and Nrf2 expression, with protection against cardiac fibrosis, dysfunction, and oxidative stress impairment. The study demonstrated that E1231 alleviates cardiac dysfunction via activating the SIRT1-PGC-1α signaling pathway in DCM, leading to the activation of Nrf2. Therefore, E1231 has the potential to facilitate the treatment of DCM.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"4 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141505511","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Analytical Quality by Design Approach for the Development and Validation of Liquid Chromatographic Procedure for the Estimation of Abrocitinib 用分析质量设计法开发和验证用于阿罗西替尼估算的液相色谱分析程序

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-06-21 DOI: 10.1007/s11094-024-03153-7

Narikimalli Ashritha, Galla Rajitha

{"title":"Analytical Quality by Design Approach for the Development and Validation of Liquid Chromatographic Procedure for the Estimation of Abrocitinib","authors":"Narikimalli Ashritha, Galla Rajitha","doi":"10.1007/s11094-024-03153-7","DOIUrl":"https://doi.org/10.1007/s11094-024-03153-7","url":null,"abstract":"Analytical quality by design-based HPLC procedure has been developed for the estimation of Abrocitinib in bulk and tablets. Design-Expert®-13 was employed for Response Surface Methodology. ANOVA was applied for responses statistical analysis. Buffer pH, flow rate, % organic composition of mobile phase, column and organic modifier were considered as CMPs. Retention time, number of theoretical plates and tailing factor were considered as CQAs. The CMPs that have a significant impact on CQAs were screened utilizing a 12-run 25 Plackett-Burman design. Following screening investigation, CMPs that have a substantial effect on the CQAs were selected and CMPs of HPLC procedure were optimized employing a 22-run 53 central-composite design. The optimized procedure suggested by the desirability functions approach utilizing a 55.8:44.2 ratio pH 3.25 ammonium formate buffer and acetonitrile with 1.0 mL/min flow rate as a mobile phase, an Inertsil ODS (150×4.6 mm, 3.5 μm) column as a stationary phase with 5 mins run time resulting in maximum desirability, 1.000. At 3.575 min, Abrocitinib retention time was observed. The optimized procedure was validated and stress studies were executed in accordance to the ICHQ2(R1) and ICHQ1A guidelines respectively. In accordance with the literature, it is evident that this is the initial reported RP HPLC procedure for Abrocitinib estimation.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"44 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141526524","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Synthesis, Molecular Modeling and Biological Assessment of Aryloxymethyl 1,3,4-Thiadiazole and 1,2,4-Triazole-5-Thione Derivatives as Potential Cox Inhibitors 作为潜在 Cox 抑制剂的芳氧基甲基 1,3,4-噻二唑和 1,2,4-三唑-5-硫酮衍生物的合成、分子建模和生物学评估

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-06-21 DOI: 10.1007/s11094-024-03136-8

Mohammad Musa Shirzad, Keriman Ozadali-Sari, Oya Unsal-Tan, Abbas Ali Husseini, Erhan Palaska

{"title":"Synthesis, Molecular Modeling and Biological Assessment of Aryloxymethyl 1,3,4-Thiadiazole and 1,2,4-Triazole-5-Thione Derivatives as Potential Cox Inhibitors","authors":"Mohammad Musa Shirzad, Keriman Ozadali-Sari, Oya Unsal-Tan, Abbas Ali Husseini, Erhan Palaska","doi":"10.1007/s11094-024-03136-8","DOIUrl":"https://doi.org/10.1007/s11094-024-03136-8","url":null,"abstract":"Thiadiazole and triazole-5-thione derivatives are five membered heterocyclic compounds showing cyclooxygenase inhibition activities. Based on this observation a series of novel aryloxymethyl 1,3,4-thiadiazole and 1,2,4-triazole-5-thione derivatives were synthesized and their biological activities evaluated. The suggested chemical structure of synthesized compounds was confirmed using FT-IR, Mass, 1H-NMR, and 13C-NMR spectrometric methods and elemental analysis. The biological activity or potency of synthesized compounds was evaluated using a COX inhibitor screening assay kit (Cayman Chemical Company), and indomethacin and NS398 as standard compounds. Compounds 2b and 3b showed good inhibitory activity against COX-2 and COX-1 enzymes respectively. The obtained data indicate that compound 2b is more selective to COX-2 and compound 3b is more selective to COX-1 compared with other synthesized compounds. These two compounds show promising selectivity and could be a starting point for future research in this area.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"357 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141526526","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0