Pharmaceutical Chemistry Journal最新文献_第4页

Radiosynthesis of 99MTc-Montelukast as a Novel Potential Radiopharmaceutical Model for Lung Scanning 将 99MTc-Montelukast 放射性合成作为肺部扫描的新型潜在放射性药物模型

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-07 DOI: 10.1007/s11094-024-03179-x

M. A. Motaleb, I. T. Ibrahim, H. A. Shweeta, S. M. Abd El-Halem

{"title":"Radiosynthesis of 99MTc-Montelukast as a Novel Potential Radiopharmaceutical Model for Lung Scanning","authors":"M. A. Motaleb, I. T. Ibrahim, H. A. Shweeta, S. M. Abd El-Halem","doi":"10.1007/s11094-024-03179-x","DOIUrl":"https://doi.org/10.1007/s11094-024-03179-x","url":null,"abstract":"Montelukast, a leukotriene receptor antagonist with a high affinity and selectivity for the cysteinyl leukotriene receptor type-1, was radiolabeled with 99mTc using a direct tagging procedure. The processing parameters—amounts of both montelukast and reducing agent, pH of the reaction mixture, reaction temperature, time of reaction, and in vitro stability of the 99mTc-montelukast complex—were thoroughly investigated. The 99mTc-montelukast complex had a percent radiolabeling yield of 92 ± 0.23 and an in vitro stability of 6 hours. According to biological distribution studies, the maximum uptake of 99mTc-montelukast complex for the lungs was 35.89 ± 1.03 % injected activity/gm tissue at 15 minutes following injection and remained high in the lungs for another hour (15.88 ± 0.39%), whereas the washout of mice organs appeared to primarily occur via the urinary tract. Because the 99mTc-montelukast complex is not a blood product, it is safer. To summarize, the 99mTc-montelukast complex is a new radiopharmaceutical that might be utilized for perfusion imaging of the lungs that is both safer and more useful.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"10 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-08-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141948674","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

Attenuation of Cardiomyocyte Hypertrophy Via Inhalation of Isosteviol-Loaded Exosome in Mice 在小鼠体内吸入异甾烷醇外泌体可减轻心肌细胞肥大

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-06 DOI: 10.1007/s11094-024-03183-1

Haihua Guo, Meng Li, Changhong Ke, Yue Lin, Zizhao Zhai, Guanlin Wang, Suqing Zhao, Tingyuan Pang

{"title":"Attenuation of Cardiomyocyte Hypertrophy Via Inhalation of Isosteviol-Loaded Exosome in Mice","authors":"Haihua Guo, Meng Li, Changhong Ke, Yue Lin, Zizhao Zhai, Guanlin Wang, Suqing Zhao, Tingyuan Pang","doi":"10.1007/s11094-024-03183-1","DOIUrl":"https://doi.org/10.1007/s11094-024-03183-1","url":null,"abstract":"Isosteviol has been investigated with a cardio-treating effect on cardiomyocyte hypertrophy. However, its hydrophilicity suppressed its efficient cellular uptake for targeting the heart. Exosomes were seen as delivery vesicles with excellent histocompatibility; thus, an isosteviol-loaded exosome (Istv-exo) was prepared for cardiopulmonary delivery in this study. For in vivo evaluation, the Istv-exo and isosteviol saline solution was used for inhalation or intragastric administration on Sprague–Dawley rats for an assay of dynamic distribution. The higher biodistribution of Istv-exo in the lung and heart has been confirmed by the dynamic content curve. Istv-exo/isosteviol solution was administered by inhalation/intragastrically to Myh6-/- mice, a cardiomyocyte hypertrophy model, to explore the therapeutic effect. The heart function of the mice was measured using echocardiography and in situ imaging was used to analyze the morphology of the heart. The higher level of left ventricular internal dimension, ejection fraction, and cardiac output in echocardiography indicated that Istv-exo enhanced improvement of myocardial function. The attenuation of cardiomyocyte hypertrophy in mice treated with inhalation of Istv-exo determined that it contributed to the reversal of pathological hypertrophy phenotypes. Wheat germ agglutinin staining confirmed that cardiomyocyte hypertrophy was reversed to varying degrees in the Istv-exo, intragastrical isosteviol, and positive control groups. Hematoxylin and eosin staining exhibited the enlarging left ventricular and thinning ventricular wall of the treated mice. Drastically less collagen fiber was observed in the positive control group and Istv-exo group. The inhalation administration of isosteviol-loaded exosomes may be better in therapy for cardiomyocyte hypertrophy than intragastric usage of isosteviol.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"2013 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-08-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141948677","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

An Efficient Catalyst-Free One-Pot Synthesis and In Vitro Biological Activity Evaluation of Novel Isoquinoline Derivatives of Fatty Acids 新型脂肪酸异喹啉衍生物的高效无催化剂一锅合成及体外生物活性评估

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-06 DOI: 10.1007/s11094-024-03189-9

Razieh Rahimizadeh, Akbar Mobinikhaledi, Hassan Moghanian, Mahta Mobinikhaledi, Seyedeh sara Kashaninejad

{"title":"An Efficient Catalyst-Free One-Pot Synthesis and In Vitro Biological Activity Evaluation of Novel Isoquinoline Derivatives of Fatty Acids","authors":"Razieh Rahimizadeh, Akbar Mobinikhaledi, Hassan Moghanian, Mahta Mobinikhaledi, Seyedeh sara Kashaninejad","doi":"10.1007/s11094-024-03189-9","DOIUrl":"https://doi.org/10.1007/s11094-024-03189-9","url":null,"abstract":"There is good evidence that fatty acid derivatives have antibacterial activity and represent a promising approach to developing the next generation of antibacterial agents. In the present work, some new isoquinolin derivatives were synthesized via the Betti reaction. Three-component reaction of aryl aldehydes, 2,7-naphthalenediol and ammonium carboxylate of fatty acids with different chains in EtOH under reflux conditions offered related isoquinolin compounds in good to excellent yields. Some advantages of this procedure are short reaction times, free catalyst, high yield of products and easy work-up. The structure of synthesized compounds was characterized by IR, 1H, and 13C NMR data as well as microanalysis results. In addition, these novel materials were evaluated for their biological activities against Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 25922) bacteria. The obtained data confirm that isoquinolin derivatives 4c, 4e, 4f, 4g, 4m, 4n, 4p, 4q exert excellent antimicrobial activity against these tested bacterial strains.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"13 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-08-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141948675","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

High-Performance Liquid Chromatography Assay for Ondansetron in Bulk and Pharmaceutical Formulations 散装和药物制剂中昂丹司琼的高效液相色谱分析

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-06 DOI: 10.1007/s11094-024-03195-x

Saba Razzak, Somia Gul

{"title":"High-Performance Liquid Chromatography Assay for Ondansetron in Bulk and Pharmaceutical Formulations","authors":"Saba Razzak, Somia Gul","doi":"10.1007/s11094-024-03195-x","DOIUrl":"https://doi.org/10.1007/s11094-024-03195-x","url":null,"abstract":"Ondansetron (OND), a serotonin type-3 receptor antagonist exhibits antiemetic activity by blocking both centrally as well as peripherally. It is one of the most common empiric options for the treatment of nausea and vomiting of different etiologies such as chemotherapy-induced nausea vomiting (CINV), radiation-induced NV, postoperative NV as well as off-labeled drugs used in pregnancy. For the quantitative determination of ondansetron in bulk and pharmaceutical dosage form, a simple reversed-phase HPLC method was successfully developed and validated. Nucleodur 100 – 10 C18 column (216 mm, 4.6 mm, and 5 μm) was used. The solvent system was methanol: water: acetonitrile (80:15:5, v/v/v), whose pH was adjusted to 2.8 by using a few drops of ortho-phosphoric acid, delivered at a flow rate of 1ml/min. Eluents were detected at a wavelength of 308 nm. The proposed method was found to be specific, sensitive and linear (R2 > 0.9999) within a desired range of 0.15 – 5 μg/ml, accurate (99.61 – 100.23%), precise (0.004 – 0.2%), and showed good robustness and ruggedness. The limit of detection and quantification was 0.27 μg/ml and 0.8 μg/ml, respectively. A statistically paired sample t-test for the analysis of precision was employed. The proposed method was applied to different marketed formulations.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"3 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-08-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141948676","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

Protective Effects of Raspberry Ketone against Isoproterenol-Induced Cardiac Hypertrophy in Wistar Rats 覆盆子酮对异丙肾上腺素诱导的 Wistar 大鼠心肌肥大的保护作用

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-03 DOI: 10.1007/s11094-024-03181-3

Vasim Khan, Sumit Sharma, Aamir khan, Uma Bhandari, Syed Ehtaishamul Haque

{"title":"Protective Effects of Raspberry Ketone against Isoproterenol-Induced Cardiac Hypertrophy in Wistar Rats","authors":"Vasim Khan, Sumit Sharma, Aamir khan, Uma Bhandari, Syed Ehtaishamul Haque","doi":"10.1007/s11094-024-03181-3","DOIUrl":"https://doi.org/10.1007/s11094-024-03181-3","url":null,"abstract":"Raspberry ketone (RK) is an active constituent obtained from Rubus idaeus (Rosaceae), which has been traditionally used against diabetes, hypertension, etc. The objective of this study was to assess the cardioprotective effect of RK against isoproterenol (ISO)-induced cardiac hypertrophy in Wistar rats. Rats were arbitrarily divided into six groups and were treated daily with raspberry ketone (100 and 200 mg/kg), fenofibrate (80 mg/kg) and propranolol (10 mg/kg) along with ISO (3 mg/kg, subcutaneously) for 28 days. Twenty-four hours after the last dose administration, serum and heart tissue samples from the animals were taken and their hemodynamic (blood pressure, heart rate], biochemical (CK-MB, LDH, troponin-T, PPAR-α, apolipoprotein C III, c-reactive protein, total cholesterol, triglycerides, high-density lipoprotein, low-density lipoprotein, very-low-density lipoprotein, malondialdehyde, reduced glutathione, superoxide dismutase, catalase, Na+-K+-ATPase, total antioxidant capacity, and nitric oxide), histopathological, and immunohistochemical (caspase-3, nuclear factor-κB, tumor necrosis factor-α) analysis was performed along with gravimetric analysis. Administration of ISO significantly altered the cardiac integrity and physiology and these changes were significantly averted by the administration of RK (100 and 200 mg/kg). These results were also found to be comparable with those of the standard drugs, fenofibrate and propranolol. The assessment of cardiac morphology by histopathological and immunohistochemical analysis further validated these results. This study thus demonstrated that RK at doses of 100 and 200 mg/kg showed a dose-dependent decrease in inflammation, oxidative stress, and dyslipidemia against ISO-induced cardiac hypertrophy in Wistar rats, which could be due to agonistic action of RK at PPAR-α receptor subtype.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"19 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-08-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141948508","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 2-ethyl-6-methylpyridinol-3-yl-thiooctanoate and its Non-Esterified Components on the Behavior of Rats in an Elevated Plus Maze 2-乙基-6-甲基吡啶醇-3-基硫代辛酸酯及其非酯化成分对大鼠在高架正迷宫中行为的影响

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-03 DOI: 10.1007/s11094-024-03178-y

I. A. Volchegorskii, S. I. Grobovoi, A. I. Sinitskii, I. Y. Miroshnichenko, L. M. Rassokhina, R. R. Mihajlov

{"title":"Effect of 2-ethyl-6-methylpyridinol-3-yl-thiooctanoate and its Non-Esterified Components on the Behavior of Rats in an Elevated Plus Maze","authors":"I. A. Volchegorskii, S. I. Grobovoi, A. I. Sinitskii, I. Y. Miroshnichenko, L. M. Rassokhina, R. R. Mihajlov","doi":"10.1007/s11094-024-03178-y","DOIUrl":"https://doi.org/10.1007/s11094-024-03178-y","url":null,"abstract":"The effect of thioctic acid (TA), 2-ethyl-6-methyl-3-hydroxypyridine hydrochloride (emoxypine), and their ester derivative (2-ethyl-6-methylpyridinol-3-yl-thiooctanoate, thioxypine) on the behavior of rats in an elevated plus maze (EPM) was studied. Intraperitoneal administration (three times) of TA, emoxypine, and their equimolar mixture in single doses of 36.25, 72.5, and 145 μmol/kg enhanced individual manifestations of anxious behavior in the EPM but did not cause full-blown anxiogenic effects. Similar pro-anxiogenic effects were observed when TA was administered in a dose of 36.25 μmol/kg and emoxypine in doses of 72.5 and 145 μmol/kg. The equimolar mixture of the non-esterified components of thioxypine had a pro-anxiogenic effect in doses of 36.25 and 72.5 μmol/kg. Combination of TA and 2-ethyl-6-methyl-3-hydroxypyridine into the ester potentiated their pro-anxiogenic activity, which manifested as an extensive anxiogenic effect of thioxypine when administered three times in a dose of 145 μmol/kg.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"73 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-08-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141948506","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

A Comparison Study Using Microneedle, Transdermal Gel, and Tape Strip-Based Delivery of Caffeine Infused with Chemical Enhancers: Characterizations and Ex-vivo Study 使用微针、透皮凝胶和胶布条给药注入化学增强剂的咖啡因的比较研究：特性和体内外研究

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-03 DOI: 10.1007/s11094-024-03180-4

Mohit Kumar, Shivani Pannu, Shubham Singh, Syed Mahmood, Amit Bhatia

{"title":"A Comparison Study Using Microneedle, Transdermal Gel, and Tape Strip-Based Delivery of Caffeine Infused with Chemical Enhancers: Characterizations and Ex-vivo Study","authors":"Mohit Kumar, Shivani Pannu, Shubham Singh, Syed Mahmood, Amit Bhatia","doi":"10.1007/s11094-024-03180-4","DOIUrl":"https://doi.org/10.1007/s11094-024-03180-4","url":null,"abstract":"The transdermal route is considered one of the most favourable routes of drug delivery over other conventional routes. The stratum corneum (SC) is the main barrier to the delivery of drugs by the transdermal route. Many strategies are employed to overcome SC barrier properties like lipid vesicles, permeation enhancers, physical methods, etc. The main objective of this research article was to explore and compare a few chemical penetration enhancers in combination with physical means like tape stripping and microneedle to enhance the transdermal permeation of caffeine. The transdermal gel of caffeine was prepared by dissolving the drug in distilled water containing various concentrations of chemical penetration enhancers, including Arlasolve DMI, ethanol, transcutol P and DMSO. Ex-vivo skin permeation and skin deposition studies were conducted on the transdermal gel alone and in combination with the microneedle or tape-stripping methods. The HPLC method analyzed the total amount of caffeine that permeated through the skin sample. The formulations containing Arlasolve DMI as a penetration enhancer showed the maximum drug penetration among all the penetration enhancers. A combination of microneedles with Arlasolve DMI showed the best skin permeation among all the methods tested. It was clear from the results that Arlasolve DMI would be a better option to use as a penetration enhancer in the dermatological formulations of caffeine in combination with a microneedle-based permeation enhancement method.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"32 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-08-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141948511","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

New Derivative of Pyrrole and Carnosine: Synthesis, Physicochemical Properties, and Biological Acivity 吡咯和肉碱的新衍生物：合成、理化性质和生物活性

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-03 DOI: 10.1007/s11094-024-03185-z

T. N. Fedorova, O. I. Kulikova, V. A. Migulin, O. A. Muzychuk, D. A. Abaimov, S. L. Stvolinsky

引用次数: 0

Design, Development and In Vitro Assessment of Water-Soluble Calixarene: A Supramolecular-Based Nano-Carrier for Paclitaxel Drug Delivery 水溶性 Calixarene 的设计、开发和体外评估：用于紫杉醇给药的超分子纳米载体

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-03 DOI: 10.1007/s11094-024-03182-2

Jigar Raval, Riddhi Trivedi, Prajesh Prajapati

{"title":"Design, Development and In Vitro Assessment of Water-Soluble Calixarene: A Supramolecular-Based Nano-Carrier for Paclitaxel Drug Delivery","authors":"Jigar Raval, Riddhi Trivedi, Prajesh Prajapati","doi":"10.1007/s11094-024-03182-2","DOIUrl":"https://doi.org/10.1007/s11094-024-03182-2","url":null,"abstract":"In the area of drug development the solubility of an active ingredient plays a very crucial and vital part and is of the highest significance. Increasing importance is being placed on the research into active ingredient solubilization. The designing of a host guest complex with a compound that has a higher dissolubility profile can work with the solubilization of lipophilic drugs. In this research work optimized nano-carriers were effectively synthesized utilizing thin-film hydration strategies. The drug sulfonated calix[4]resorcinarene blend (1:10) containing ethanol was dispersed and sonicated with an estimated three cycles, at an amplitude 70 with a 20-s interval for an optimized time. The synthesized nanovesicles have an average diameter of 477.7 nm, a higher mono dispersity (PDI-0.282), and a greater loading capacity of the drugs is 95%. Atomic force microscopy in accordance with dynamic light-scattering spectra confirmed the spherical shape of paclitaxel-loaded sulfonated calix[4]resorcinarene nanovesicles. In vitro release of medication from nanovesicles affirmed the extended discharge pattern of drugs with r2 of 0.9902 compared with the commercial formulation available on the market. MTT assay is performed to access the toxicity of the sufonated calix[4]resorcinarene in vitro. IC50 values indicate that synthesized sufonated calix[4]resorcinarene shows better IC50 values than paclitaxel and taxol. The formulated nanovesicles from sulfonated calix[4]resorcinarene showed an ideal size with higher capacity for binding drug and provide better patient compliance, which are positive for their expected application as a modular drug delivery platform for anti-cancer drugs.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"59 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-08-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141948504","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 on the Structure, Solubilities, Antibacterial Activities and In Vivo Toxicity of Hesperetin and Norfloxacin Cocrystal 橙皮苷与诺氟沙星共晶的结构、溶解度、抗菌活性及体内毒性研究

4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-01 DOI: 10.1007/s11094-024-03205-y

Shouliang Qiu, Xuezhen Deng, Kun Qian, Jie Yang, Yuexing Ma

引用次数: 1