Pharmaceutical Chemistry Journal最新文献_第3页

A7, A Novel Analog of Curcumin, Induces Cell Apoptosis Through Suppressing TGF-βR/MEK/ERK Pathway in A549 Cells 姜黄素的一种新型类似物 A7 通过抑制 A549 细胞中的 TGF-βR/MEK/ERK 通路诱导细胞凋亡

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-09-14 DOI: 10.1007/s11094-024-03208-9

Pan Yu, Weiya Cao, Qianli Tang, Ruiqing Yan, Xinlan Tan, Zheyu Li

{"title":"A7, A Novel Analog of Curcumin, Induces Cell Apoptosis Through Suppressing TGF-βR/MEK/ERK Pathway in A549 Cells","authors":"Pan Yu, Weiya Cao, Qianli Tang, Ruiqing Yan, Xinlan Tan, Zheyu Li","doi":"10.1007/s11094-024-03208-9","DOIUrl":"https://doi.org/10.1007/s11094-024-03208-9","url":null,"abstract":"Lung cancer is the leading cause of cancer death worldwide and curcumin is a natural polyphenol product with a diversity of antitumor activities. However, its clinical utility is limited due to its relatively low instability and poor bioavailability. This study evaluates the antitumor activity and the underlying mechanism of eight new curcumin analogs in A549 cells. Cell proliferation, migration and apoptosis were examined, respectively, through MTT assay, clone formation, wound healing, transwell, JC-1 staining, Bcl-2 activity, and caspase 3 activity. Protein levels of TGF-βR, MEK, and ERK were determined via western blotting. The binding mode of the ligand and the receptor was simulated by molecular docking studies. Compound A7 was found as the most potent analog (IC50 = 25.78 μM) compared to curcumin (IC50 = 42.30 μM). A7 exposure suppressed A549 cell migration and induced apoptosis with significant differences. Western blot and molecular docking studies demonstrated that the potential mechanism may relate to regulating the TGF-βR/MEK/ERK signaling pathway. Therefore, inhibiting this signaling pathway may provide a potential therapeutic strategy for lung cancer.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"47 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-09-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142269265","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

Antiproliferative Activity Compounds Isolated from the Marine Fungus Penicillium terrigenum 从海洋真菌青霉中分离出的抗增殖活性化合物

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-09-13 DOI: 10.1007/s11094-024-03204-z

Fan-ying Wu, Si-yuan Liu, Jie Feng

引用次数: 0

Modern Approaches to Mathematical Modeling of the Process of Direct Pressing of Tablets 直接压片工艺数学建模的现代方法

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-27 DOI: 10.1007/s11094-024-03194-y

V. B. Markeev, E. V. Blynskaya, S. V. Tishkov, K. V. Alekseev, V. K. Alekseev

引用次数: 0

Determination of the Rosmarinic Acid Content in Mentha piperita L. Leaves by HPLC 用高效液相色谱法测定薄荷叶中的迷迭香酸含量

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-16 DOI: 10.1007/s11094-024-03191-1

V. A. Kurkin, M. A. Kazakova, A. R. Mubinov

引用次数: 0

Validated UV-Spectrophotometric Method for Pirfenidone Estimation in Bulk Drug, Marketed Tablet, and Nanoparticle Formulation 经验证的紫外分光光度法测定散装药物、上市片剂和纳米颗粒制剂中的吡非尼酮含量

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-16 DOI: 10.1007/s11094-024-03196-w

Kiran Dudhat, Janki Goswami, Dr. Harsha Patel

{"title":"Validated UV-Spectrophotometric Method for Pirfenidone Estimation in Bulk Drug, Marketed Tablet, and Nanoparticle Formulation","authors":"Kiran Dudhat, Janki Goswami, Dr. Harsha Patel","doi":"10.1007/s11094-024-03196-w","DOIUrl":"https://doi.org/10.1007/s11094-024-03196-w","url":null,"abstract":"The goal of the current research was to create an easy-to-understand, precise, and affordable UV-spectrophotometric method for measuring pirfenidone in bulk, in commercial formulations, and in nanoparticle form. The stock solution of pirfenidone was made using a phosphate buffer with a pH of 7.4, and the highest absorbance wavelength in the absorption spectrum was then identified. The standard curve was developed by preparing various working standard solutions from the aforementioned solution by dilution with the same diluents. This technique was also validated in accordance with International Council for Harmonization (ICH) guidelines. Pirfenidone showed the maximum absorptivity at 311 nm and the linearity range was found to be 10 – 50 μg/mL (R2 = 0.998). The limit of detection (LOD) and limit of quantification (LOQ) were 6.1140 μg/mL and 18.527 μg/mL respectively. The validity of all other parameters was determined to be acceptable. It was decided that the precision and accuracy were satisfactory. The developed processes were validated based on ICH standards. All of the validation parameters were found to be acceptable when compared with the standard values. Therefore, the suggested technique for pirfenidone determination in bulk drug and pharmaceutical formulation assays is applicable to everyday activities. The estimation of pirfenidone in pure form, commercial formulations, and nanoparticles was performed using an easy process that did not involve any potentially dangerous chemicals.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"4 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-08-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142207301","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 Acetaminophen Under Microwave Irradiation in the Presence of H-Clinoptilolite 微波辐照下在 H-Clinoptilolite 存在下合成对乙酰氨基酚

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-15 DOI: 10.1007/s11094-024-03193-z

G. H. Torosyan, P. A. Yesayan, H. H. Aleksanyan

引用次数: 0

The Effect of Naringenin and Ceftriaxone on a Rat Model of Pyelonephritis 柚皮苷和头孢曲松对大鼠肾盂肾炎模型的影响

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-14 DOI: 10.1007/s11094-024-03184-0

Sulieman Ibraheem Shelash Al-Hawary, Zeyad Duraid Najmuldeen, Rosario Mireya Romero-Parra, Shaker Shanawa Al-Hasnawi, Ali Kamil Kareem, Shaymaa Abdulhameed Khudair, Krishanveer Singh, Muataz S. Alhassan, Ahmed Hjazi, Shadia Hamoud Alshahrani

{"title":"The Effect of Naringenin and Ceftriaxone on a Rat Model of Pyelonephritis","authors":"Sulieman Ibraheem Shelash Al-Hawary, Zeyad Duraid Najmuldeen, Rosario Mireya Romero-Parra, Shaker Shanawa Al-Hasnawi, Ali Kamil Kareem, Shaymaa Abdulhameed Khudair, Krishanveer Singh, Muataz S. Alhassan, Ahmed Hjazi, Shadia Hamoud Alshahrani","doi":"10.1007/s11094-024-03184-0","DOIUrl":"https://doi.org/10.1007/s11094-024-03184-0","url":null,"abstract":"The aim of the present study was to evaluate the anti-pyelonephritis activity of naringenin alone or combined with ceftriaxone in a rat model. In all, 35 Wistar rats were randomly divided into five equal groups. Groups 2 – 5 underwent surgery and were infected with E. coli to induce pyelonephritis. Groups 1 and 2 were treated with normal saline and groups 3, 4, and 5 received ceftriaxone (60 mg/kg), naringenin (20 mg/kg), and ceftriaxone+naringenin, respectively for 1 week. Subsequently, the disc diffusion method and bacterial colony counting were performed. After six weeks, MDA and GSH levels, TOS, TAC, activities of GPx, CAT and SOD, and histopathological analyses were evaluated in the kidneys. A week after the ceftriaxone treatment and two weeks after the naringenin exposure, negative urinary bacterial colonies were observed. The combination of these drugs caused negative colonies during the first week. Naringenin alone or in combination with ceftriaxone significantly decreased renal MDAand TOS but increased TAC, GSH and activities of GPx, CAT and SOD compared with the pyelonephritic group. This combination revealed histopathological changes in the kidneys. Our data suggest synergism between naringenin and ceftriaxone in alleviating pyelonephritis-induced complications.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"70 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-08-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142207303","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

Microrna-155 as a Possible Pharmacological Target 可能的药理靶标 Microrna-155

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-13 DOI: 10.1007/s11094-024-03177-z

A. V. Golounina, T. A. Fedotcheva, N. L. Shimanovsky

引用次数: 0

In Silico Studies, Synthesis and Biological Evaluation of 4,5-Dehydrospisulosine Butyrate Ceramides as Potential Anticancer Agents 4,5-Dehydrospisulosine Butyrate 神经酰胺作为潜在抗癌剂的硅学研究、合成和生物学评价

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-13 DOI: 10.1007/s11094-024-03188-w

Parleen Kaur, Sonia Sharma, Vinay Randhawa, Navneet Agnihotri, Ramandeep Kaur, Vasundhara Singh

{"title":"In Silico Studies, Synthesis and Biological Evaluation of 4,5-Dehydrospisulosine Butyrate Ceramides as Potential Anticancer Agents","authors":"Parleen Kaur, Sonia Sharma, Vinay Randhawa, Navneet Agnihotri, Ramandeep Kaur, Vasundhara Singh","doi":"10.1007/s11094-024-03188-w","DOIUrl":"https://doi.org/10.1007/s11094-024-03188-w","url":null,"abstract":"In the present work, synthesis of 4,5-dehydrospiulosine and its chain analogues (7-9) as potential Sphingosine Kinase I inhibitors has been achieved via the diastereoselective Grignard reaction and stereoselective cross-metathesis reaction followed by N-acylation with p-nitrophenyl butyrate to give the corresponding butyrate ceramides (10-12). All compounds were obtained in high yield and purity. Molecular docking simulation studies were performed for the synthesized compounds that indicated their varying binding affinities with the Sphingosine Kinase 1 (SPHK1) protein. Following, molecular dynamics simulations were performed for the SPHK1-compound (10) complex that indicated compound (10) to be structurally and energetically stable within the binding pocket of SPHK1. Further, the biological evaluation studies, as potential anti-prostate cancer agents and as anti-colon cancer agents by inhibiting the SPHK1 of all synthesized compounds (7-12) on PC-3 cell lines and HCT-116 cell lines by the SRB method were done. Compound N-((2S,3S,E)-3-hydroxyheptadec-4-en-2-yl) butyramide (10) exhibited remarkable cytotoxicity with an IC50 value of 0.018 μM against PC-3 cell lines and 0.076 μM against HCT-116 cell lines, whereas compound (11) showed best cytotoxicity with an IC50 value of 0.062 μM against HCT-116 cell lines.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"1 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-08-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142207305","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

Features of the Accumulation of Flavonoids in Medicinal Plant Raw Materials of the Synanthropic Flora of Rostov Region 罗斯托夫州协同植物区系药用植物原料中黄酮类化合物的积累特点

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-12 DOI: 10.1007/s11094-024-03192-0

Yu. A. Pavlova, N. A. Dyakova, A. A. Vervikina, A. I. Slivkin

{"title":"Features of the Accumulation of Flavonoids in Medicinal Plant Raw Materials of the Synanthropic Flora of Rostov Region","authors":"Yu. A. Pavlova, N. A. Dyakova, A. A. Vervikina, A. I. Slivkin","doi":"10.1007/s11094-024-03192-0","DOIUrl":"https://doi.org/10.1007/s11094-024-03192-0","url":null,"abstract":"Inconsistencies in literature data on the environmental features of the biosynthesis of polyphenol biologically active substances in medicinal plant raw materials were found particularly for flavonoids, which are important secondary metabolites that significantly contribute to the response to abiotic and anthropogenic stress. The goal of the study was to elucidate features of the accumulation of flavonoids in medicinal plant raw materials of the synanthropic flora of Rostov Region using Morozovsky District as an example. The accumulation of flavonoids in samples of knotgrass herb (Polygonum aviculare L.), wormwood (Artemisia absinthium L.), and common yarrow (Achillea millefolium L.) of the synanthropic flora of Rostov Region was characterized with a significant variability depending on the harvesting site. Samples of medicinal plant raw materials collected in several urbocenoses displayed induced flavonoid accumulation as compared with samples from control territories. This could be explained by activation under the anthropogenic load of the key enzyme for flavonoid biosynthesis (phenylalanine ammonia lyase), which is highly induced by stress. However, samples collected in areas of significant anthropogenic impact (mainly along a category IA highway or railroad trunkline) were characterized by a reduced content of flavonoids. This was probably due to excessive environmental pollution going beyond the endurance of the species and causing suppression of the enzyme systems.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"101 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-08-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142207304","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