Pharmaceutical Chemistry Journal最新文献_第7页

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

Study of Impurity Profiles in Raw Materials and Tablets of Rutin and Its Production Process: Correlation Analysis 芦丁原材料和片剂中的杂质概况及其生产工艺研究：相关性分析

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-06-21 DOI: 10.1007/s11094-024-03152-8

Xinyu Kuang, Dandan Shen, Qun Wu, Linggao Zeng, Wei Zhang, Jianhua Wang

{"title":"Study of Impurity Profiles in Raw Materials and Tablets of Rutin and Its Production Process: Correlation Analysis","authors":"Xinyu Kuang, Dandan Shen, Qun Wu, Linggao Zeng, Wei Zhang, Jianhua Wang","doi":"10.1007/s11094-024-03152-8","DOIUrl":"https://doi.org/10.1007/s11094-024-03152-8","url":null,"abstract":"An HPLC-UV method with high sensitivity and good resolution, calculated by the principal component external standard method with correction factors and detailed methodological validation according to ICH guidelines, was developed for the accurate detection of impurities in three different extraction processes of rutin raw materials and their tablets, and the determination of impurity profiles by LC-MS/MS. In this study, nine impurities (>0.1%) were mainly isolated and identified, four of which were process impurities, and the other five were degradation products. The results of the correlation between impurity profiles and production processes showed that the impurity content of rutin tablets correlated positively with the impurity level of the raw materials used, which correlated significantly with the extraction process. The finished rutin under the alkali-dissolution and acid-sedimentation refining method had low purity and the highest impurity content. In contrast, the number of impurities and the total amount of impurities detected in rutin by the secondary recrystallization process with methanol washing were the lowest, and were mainly process impurities. This further indicates that generating degradation impurities could be avoided, and a suitable refining process could effectively reduce impurities. This study provides an essential basis for manufacturers to optimize the process parameters of rutin raw materials.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"18 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141526671","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 of New Conjugates of Edaravone and 1-Aminoadamantanes and Their Interaction with NMDA Receptors in Rats 依达拉奉和 1-氨基金刚烷新共轭物的合成及其与大鼠 NMDA 受体的相互作用

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-06-21 DOI: 10.1007/s11094-024-03134-w

V. V. Grigoriev, A. Yu. Aksinenko, T. V. Goreva, A. V. Gabrelyan, T. A. Epishina

引用次数: 0

Variability of the Constituent Composition of Mentha piperita L. Essential Oil 薄荷精油成分的可变性

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-06-21 DOI: 10.1007/s11094-024-03142-w

A. N. Alibegov, A. M. Aliev, G. K. Radjabov, F. A. Vagabova, A. M. Musaev

引用次数: 0

Quality Management System in Production of Reference Materials 标准物质生产质量管理体系

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-06-21 DOI: 10.1007/s11094-024-03150-w

V. S. Pyzhov, V. I. Gegechkori, V. A. Darina, E. A. Pogrebinskaya

引用次数: 0

Effect of Quercetin and its Derivatives on the Excretory Function of Rat Kidneys 槲皮素及其衍生物对大鼠肾脏排泄功能的影响

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-06-21 DOI: 10.1007/s11094-024-03135-9

E. N. Zaitseva, A. I. Altareva, A. V. Dubishchev, V. A. Kurkin, O. V. Sharova

{"title":"Effect of Quercetin and its Derivatives on the Excretory Function of Rat Kidneys","authors":"E. N. Zaitseva, A. I. Altareva, A. V. Dubishchev, V. A. Kurkin, O. V. Sharova","doi":"10.1007/s11094-024-03135-9","DOIUrl":"https://doi.org/10.1007/s11094-024-03135-9","url":null,"abstract":"The optimal diuretic doses of quercetin and rutin (5 mg/kg) and dihydroquercetin and hyperoside (1 mg/kg) were determined in experiments on white rats with a single intragastric administration. The mechanism of action of sodium quercetin and its derivatives on glomerular filtration and tubular transport was studied in acute experiments. Quercetin, dihydroquercetin, rutin, and hyperoside with a single intramuscular injection at the above doses contributed to an increase in diuresis, saluresis, creatinine clearance (except for rutin), and excreted sodium fraction by an average of 141%, 203%, 153%, and 189%, respectively (p < 0.05). Rutin also led to a decrease in the creatinine concentration index (by an average of 79%, p < 0.05). The diuretic furosemide with a single intramuscular injection at the threshold dose of 1 mg/kg increased diuresis, saluresis, and excreted sodium fraction (by an average of 187%, p < 0.05), like the effect of the quercetin derivatives; decreased the creatinine concentration index (by an average of 62%, p < 0.05); and did not affect creatinine clearance identically to the effect of rutin.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"13 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141526522","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

Effect of Formulation Parameters and Physiological Environment on Amlodipine Release Kinetics Encapsulated in Biodegradable Polymers and Optimized by Design Methodology 可生物降解聚合物包封的配方参数和生理环境对氨氯地平释放动力学的影响及设计方法的优化

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-05-28 DOI: 10.1007/s11094-024-03129-7

Naima Ifourah, Sandrine Cammas-Marion, Hayet Belkacemi

{"title":"Effect of Formulation Parameters and Physiological Environment on Amlodipine Release Kinetics Encapsulated in Biodegradable Polymers and Optimized by Design Methodology","authors":"Naima Ifourah, Sandrine Cammas-Marion, Hayet Belkacemi","doi":"10.1007/s11094-024-03129-7","DOIUrl":"https://doi.org/10.1007/s11094-024-03129-7","url":null,"abstract":"In this study, two polyelectrolytes, chitosan and propyl methyl cellulose carbonate, were associated by crosslinking with tripolyphosphate (TPP), to prepare microspheres loaded with amlodipine besylate (Aml). The formulations were optimized by Box–Behnken experimental design, in which three factors, four responses were studied to check the effect of independent variables (concentration of TPP, pH of TPP solution, and pH of a polymer mixture) on responses: zeta potential, particle size, polydispersity index and entrapment efficiency. The optimal encapsulation efficiency was around 92.43%, the zeta potential on average 41.75 mV, and the minimum mean particle size was 310 nm. The effects of the parameters on changes in structure, crystallinity, and surface charges of polymers, by crosslinking in microparticles, were identified by FT-IR, XRD, and dynamic light scattering analyses. The encapsulation parameters and the environment media influenced the mechanism of release and the kinetics model, which was greater in the duodenal medium at pH 5.5 (Q = 100%). The microencapsulation by nontoxic polymers in water is a good method of preparing amlodipine-loaded microspheres, which are intended for the oral route, with optimal dose release in the duodenal medium. This represents the target site for absorption of the drug, in the pulmonary sphere.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"132 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-05-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141166912","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

Design, Synthesis and Biological Evaluation of 7-Azaindole Analogues as Novel Antiproliferative Agent and Tyrosine Protein Kinase SRC Inhibitors 作为新型抗增殖剂和酪氨酸蛋白激酶 SRC 抑制剂的 7-氮杂吲哚类似物的设计、合成和生物学评价

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-05-17 DOI: 10.1007/s11094-024-03120-2

Neha Sharma, Anurag, Monika Sachdeva

引用次数: 0