Pharmacia最新文献

Microneedle and drug delivery across the skin: An overview 微针和跨皮肤给药：综述

IF 1.1

Pharmacia Pub Date : 2024-01-10 DOI: 10.3897/pharmacia.71.e112503

Iman Hamdan

引用次数: 0

Nephroprotective effects of Equisetum ramosissimum L. extract in streptozotocin-induced diabetic rats 马钱子提取物对链脲佐菌素诱导的糖尿病大鼠的肾保护作用

IF 1.1

Pharmacia Pub Date : 2024-01-09 DOI: 10.3897/pharmacia.71.e113659

Raheeq Khairy Abdullah, Reem A. Issa, M. Abu-Samak, Beisan A. Mohammad, M. Abbas, S. Awwad

{"title":"Nephroprotective effects of Equisetum ramosissimum L. extract in streptozotocin-induced diabetic rats","authors":"Raheeq Khairy Abdullah, Reem A. Issa, M. Abu-Samak, Beisan A. Mohammad, M. Abbas, S. Awwad","doi":"10.3897/pharmacia.71.e113659","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e113659","url":null,"abstract":"Diabetes is a widespread health issue that impacts people all over the globe. The Equisetum ramosissimum L. plant has numerous traditional uses and pharmacological properties, including antidiabetic effects.The objective of this study was to thoroughly examine the advantages of incorporating extracts from the aerial components of E. ramosissimum to control diabetic nephropathy. The phytochemical constituents of E. ramosissimum extract were explored using phytochemical and HPLC analysis, focusing on phenols and flavonoid content. The effect of plant extract was evaluated on different kidney function parameters linked to diabetic nephropathy (fasting blood glucose, creatinine, uric acid, and urea) in streptozotocin induced-diabetic rats. Histopathological changes in the liver were also examined. The results showed methanol and ethanol extracts of E. ramosissimum have a total content of phenols (equivalent to gallic acid, 7.62 and 8.97 mg/g) and flavonoids (equivalent to quercetin, 8.87 and 12.86 mg/g), respectively. After conducting the UHPLC-MS/MS analysis, it was found that both the methanol and ethanol extracts contained isoferulic acid, ISO-Orientin, myristic acid, linoelaidic acid, rutin, and 3-Glu-7-Rha quercetin. Additionally, isoferulic acid, myristic acid, linoelaidic acid, rutin, and 3-Glu-7-Rha quercetin were present in the extracts. The ethanol extract of E. ramosissimum significantly impacted STZ-induced diabetic mice by reducing their fasting blood glucose levels, and their creatinine and urea levels (P < 0.005). In conclusion, E. ramosissimum ethanol extract has shown potential effects to counteract some diabetes consequences on kidney function. Therefore, further studies are required to investigate its effect on other diabetes-related complications.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"21 8","pages":""},"PeriodicalIF":1.1,"publicationDate":"2024-01-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139441417","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Spectroscopic and thermodynamic characterization of the interaction of a new synthesized antitumor drug candidate 2H4MBBH with human serum albumin 一种新合成的抗肿瘤候选药物 2H4MBBH 与人血清白蛋白相互作用的光谱和热力学表征

IF 1.1

Pharmacia Pub Date : 2024-01-09 DOI: 10.3897/pharmacia.71.e112385

S. Abarova, Katerina Stoitchkova, Svetlin Tzonev, Maria Argirova, D. Yancheva, N. Anastassova, Boris Tenchov

引用次数: 0

A 36-year-old woman with a parathyroid cyst 一名患有甲状旁腺囊肿的 36 岁女性

IF 1.1

Pharmacia Pub Date : 2024-01-04 DOI: 10.3897/pharmacia.71.e115504

Iveta Nedeva, V. Vodenicharov, V. Karamfilova, Y. Assyov

引用次数: 0

Amstirdam coffee ameliorates Lp-PLA2 and the inflammatory response in an atherosclerosis rats 阿姆斯特丹咖啡可改善动脉粥样硬化大鼠的脂蛋白-PLA2 和炎症反应

IF 1.1

Pharmacia Pub Date : 2024-01-04 DOI: 10.3897/pharmacia.71.e106817

W. Nafisah, Annia Zhafarina Dalilati, Y. Christina, Mochammad Fitri Atho'illah, Muhaimin Rifa’ia, T. Noor, Alexander Patera Nugraha

{"title":"Amstirdam coffee ameliorates Lp-PLA2 and the inflammatory response in an atherosclerosis rats","authors":"W. Nafisah, Annia Zhafarina Dalilati, Y. Christina, Mochammad Fitri Atho'illah, Muhaimin Rifa’ia, T. Noor, Alexander Patera Nugraha","doi":"10.3897/pharmacia.71.e106817","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e106817","url":null,"abstract":"Coffee is a kind of daily beverage, and its correlation with cardiovascular disease and atherosclerosis is still debatable. The aim of this study is to investigate the effects of Amstirdam coffee extract (ACE) on lipoprotein-associated phospholipase A2 (Lp-PLA2) and the inflammatory response in atherosclerosis mouse models. The study used 25 Swiss male mice for five groups (n = 5): healthy mice fed a normal diet (N); mice fed a high-fat, high-fructose diet (HFFD); mice fed HFFD and treated with ACE at doses of 104 (D1), 520 (D2), and 5200 mg/kg BW (D3). The levels of Lp-PLA2, regulatory T cells (Tregs) (CD4+CD25+CD62L+, CD4+CD25+IL-10+, CD4+CD25+TGF-+), IL-10 (CD4+IL-10+), and TGF-B (CD4+TGF+) were analyzed using a flow cytometer. Histological analysis of the mouse aorta was done by hematoxylin and eosin (HE) staining. This study indicated a significant increase in total cholesterol (TC), triglyceride (TG), LDL, and Lp-PLA2 levels in the HFFD group. HFFD also reduced HDL, IL-10, and TGF produced by CD4 and Tregs compared with the normal group. ACE at all doses significantly reduced Lp-PLA2 levels compared with the HFFD group (p < 0.05). Interestingly, the administration of 520 mg/kg BW ACE (D2) increased the production of IL-10 significantly compared to other doses (p < 0.05). The D3 group possessed a high TGF- production and Treg expression level significantly different between groups (p < 0.05). Foam cells were mostly found in the aorta of the HFFD group compared to the normal and ACE treatment groups. This study suggested that ACE could reduce Lp-PLA2 enzyme activity and foam cell formation through the immunosuppressive activity of IL-10 and TGF cytokines.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"28 1","pages":""},"PeriodicalIF":1.1,"publicationDate":"2024-01-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139385842","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","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 tobacco smoking and alcohol consumption on semen quality and hormone reproductive levels in infertile males: A systematic review and meta analysis 吸烟和饮酒对不育男性精液质量和激素生殖水平的影响：系统综述和荟萃分析

IF 1.1

Pharmacia Pub Date : 2024-01-04 DOI: 10.3897/pharmacia.71.e113854

Ryan Ramon, S. M. Warli, Nur Rasyid, W. Atmoko

引用次数: 0

Molecular docking screening, dynamics simulations, ADMET, and semi-synthesis prediction of flavones and flavonols from the COCONUT database as potent bifunctional neuraminidase inhibitors 将 COCONUT 数据库中的黄酮和黄酮醇作为强效双功能神经氨酸酶抑制剂进行分子对接筛选、动力学模拟、ADMET 和半合成预测

IF 1.1

Pharmacia Pub Date : 2024-01-03 DOI: 10.3897/pharmacia.71.e114967

Thi-Kim-Quy Ha, N. Pham-Khanh, Thanh-Khiet Nguyen

{"title":"Molecular docking screening, dynamics simulations, ADMET, and semi-synthesis prediction of flavones and flavonols from the COCONUT database as potent bifunctional neuraminidase inhibitors","authors":"Thi-Kim-Quy Ha, N. Pham-Khanh, Thanh-Khiet Nguyen","doi":"10.3897/pharmacia.71.e114967","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e114967","url":null,"abstract":"Finding new neuraminidase (N) inhibitors to improve anti-influenza treatment is necessary because of the high mutation rates of N protein. Over 3,000 flavones/flavonols and their synthesized products from the COCONUT database were performed in silico docking screening with N1-H274Y-oseltamivir protein (PDB ID: 3CL0). Several derivatives containing nitrogen heterocyclic groups or aromatic rings showed higher anti-neuraminidase potential than that of laninamivir. Especially, the linker groups between the flavone aglycone and nitrogen heterocyclic group created the interactions with the triad of arginine residues Arg118-Arg292-Arg371, which suggested these compounds could become bifunctional inhibitors against the influenza virus strains at the sialic acid binding site and the adjacent 430-cavity position through triad of arginine residues binding. ADMET indicators and the synthesis design strategy of the most suitable compound, ethyl 4-{2-[(5-hydroxy-4-oxo-2-phenyl-4H-chromen-7-yl)oxy]acetyl}piperazine-1-carboxylate, were also successfully predicted and it could be a concerned candidate for further wet-lab synthesis, in vivo and clinical study.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"1 2","pages":""},"PeriodicalIF":1.1,"publicationDate":"2024-01-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139389060","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Molecular dynamic of omega-3 compounds as an anti-obesity agent into GPR-120 receptor 欧米茄-3 复合物作为抗肥胖剂进入 GPR-120 受体的分子动态变化

IF 1.1

Pharmacia Pub Date : 2023-12-18 DOI: 10.3897/pharmacia.70.e115501

Ida Musfiroh, G. Megawati, Dewi Marhaeni Diah Herawati, Okta Nama Putra, Evi Sylvia Nurrasjid

{"title":"Molecular dynamic of omega-3 compounds as an anti-obesity agent into GPR-120 receptor","authors":"Ida Musfiroh, G. Megawati, Dewi Marhaeni Diah Herawati, Okta Nama Putra, Evi Sylvia Nurrasjid","doi":"10.3897/pharmacia.70.e115501","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e115501","url":null,"abstract":"Obesity is a cause of comorbid diseases such as type 2 diabetes mellitus, dyslipidemia, hypertension which is based on low-level chronic inflammation. The GPR-120 receptor plays a role in insulin sensitization which is related to diabetes mellitus which is a comorbid obesity. Omega-3 fatty acids are believed to possess anti-inflammatory properties, hence potentially serving as a preventive measure against obesity-related comorbidities. The aim of this study is to do a stability analysis of the binding affinity between nine specific chemicals derived from omega-3 and the active site of the human GPR120 receptor using molecular dynamics simulations. Docking analysis was performed using Discovery Studio Visualizer, AutoDock Tools 1.5.6, and molecular dynamic simulation with AMBER 16. In this study, we used neurotensin 8–13 as a natural ligand to bind with the neurotensin receptor. Based on the neurotensin receptor docking results, the ΔG values for the following compounds are close to the values for neurotensin 8–13 -6.41 kcal/mol; docosahexaenoic acid -8.96 kcal/mol; eicosapentaenoic acid -7.41 kcal/mol; and heneicosapentaenoic acid -6.34 kcal/mol. Neurotensin 8–13 forms hydrogen bonds with TYR146, ARG213, and PHE344 of the neurotensin receptor, whereas docosahexaenoic acid forms hydrogen bonds with TYR146. Meanwhile, the average RMSD fluctuations for each system, namely docosahexaenoic acid, eicosapentaenoic acid, and heneicosapentaenoic acid, were 0.672, 0.437, and 0.650, respectively. The SASA of the neurotensin receptor-ligand complex showed similar fluctuations, with the average values for docosahexaenoic acid, eicosapentaenoic acid, and heneicosapentaenoic acid being 230.40, 229.89, and 230.20 nm2.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"35 S144","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-12-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138965195","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Lead drug discovery from imidazolinone derivatives with Aurora kinase inhibitors 从咪唑啉酮衍生物与极光激酶抑制剂中发现先导药物

IF 1.1

Pharmacia Pub Date : 2023-12-18 DOI: 10.3897/pharmacia.70.e114935

Bathula Sivakumar, Ilango Kaliappan

{"title":"Lead drug discovery from imidazolinone derivatives with Aurora kinase inhibitors","authors":"Bathula Sivakumar, Ilango Kaliappan","doi":"10.3897/pharmacia.70.e114935","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e114935","url":null,"abstract":"Cancer is the second leading cause of death worldwide, and breast cancer accounts for 6.27 million cases in the year 2022. In the present study, Quantitative Structural Activity Relationship (QSAR) studies were performed on a dataset of 39 molecules of Imidazolinone analogues using in random selection using QSARINS Software. The statistically validated (R2 = 0.8429 Q2loo = 0.7558) MLR model was used to predict the bioactivity of novel leads. Moreover, high-scoring compounds were exposed to molecular docking and molecular dynamic modeling study. Intended derivatives 1–23 exhibited the anticipated bioactivity using a QSAR model. Aforementioned molecules were tested for binding affinities with the target protein and the majority of them demonstrated excellent interactions with binding pocket residues. Molecular dynamics simulations using Desmond for 100 ns of top complexes 1, 7, 9, 13 and 19 showed critical structural data concerning Aurora kinase inhibition. There were stable hydrophobic and hydrophilic interfaces in the dynamic site of compounds with a leading chemical structure. The chemical interacts to the (PDB: 1MQ4) structure in a stable way, according to RMSD, RMSF, RoG, H-bond, and SASA analysis. Furthermore, the docking results have been confirmed by MM-PBSA and MM-GBSA. Based on our findings, we reported the inclusion of the necessary structural features of imidazolinone derivatives leads to the development of the potent candidates for further development.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"337 ","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-12-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139173347","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

UHPLC-Orbitrap screening of oleraindoles in hydromethanolic extracts of Portulaca oleracea 超高效液相色谱-轨道阱（UHPLC-Orbitrap）筛选马齿苋水甲醇提取物中的欧来吲哚类化合物

IF 1.1

Pharmacia Pub Date : 2023-12-18 DOI: 10.3897/pharmacia.70.e113577

Y. Voynikov, R. Gevrenova, D. Zheleva-Dimitrova, V. Balabanova, Irina Nikolova, Lyubomir Marinov, Iossif Benbassat, G. Momekov

引用次数: 0