Current pharmaceutical design最新文献_第4页

Therapeutic Role of Scutellarein in Neurological Disorders. 黄芩苷在神经系统疾病中的治疗作用。

IF 2.6 4区医学

Current pharmaceutical design Pub Date : 2025-01-07 DOI: 10.2174/0113816128336901241125092132

Rohit Kumar, Sucharitha Bai, Rahul Shukla, Saba Naqvi

引用次数: 0

BACE-1 and ADAM-10 as Potential Peripheral Biomarkers for Alzheimer's Disease. BACE-1和ADAM-10作为阿尔茨海默病的潜在外周生物标志物

IF 2.6 4区医学

Current pharmaceutical design Pub Date : 2025-01-07 DOI: 10.2174/0113816128339561241120135914

Carlo Cervellati, Alessandro Trentini, Marco Zuin, Gianmarco Mola, Raffaella Riccetti, Cristina Manfrinato, Domenico Sergi, Gerhard Multhaup, Giovanni Zuliani

引用次数: 0

Modified Taohong Siwu Decoction Improved Cardiac Function after Myocardial Infarction by Activating PI3K/Akt Signaling Pathway. 桃红四物汤通过激活PI3K/Akt信号通路改善心肌梗死后心功能。

IF 2.6 4区医学

Current pharmaceutical design Pub Date : 2025-01-07 DOI: 10.2174/0113816128341178241028062518

Han Li, Zhi-Rong Luo, Meng-Ying Huang, Hao Cai, Ping-Ping Lu, Yan-Wu Xu, Ming-Jie Li, Hai-Dong Guo

{"title":"Modified Taohong Siwu Decoction Improved Cardiac Function after Myocardial Infarction by Activating PI3K/Akt Signaling Pathway.","authors":"Han Li, Zhi-Rong Luo, Meng-Ying Huang, Hao Cai, Ping-Ping Lu, Yan-Wu Xu, Ming-Jie Li, Hai-Dong Guo","doi":"10.2174/0113816128341178241028062518","DOIUrl":"https://doi.org/10.2174/0113816128341178241028062518","url":null,"abstract":"Introduction: Taohong Siwu decoction (THSWD), a traditional prescription for enhancing blood circulation and eliminating blood stasis, primarily comprises peach kernel, safflower, angelica, chuanxiong, and rehmannia. Modified Taohong Siwu decoction (MTHSWD), an advanced version of THSWD, incorporates additional ingredients such as epimedium, cinnamon, and salvia miltiorrhiza. This addition serves to augment its efficacy in warming yang and promoting blood circulation. MTHSWD has excellent heart protection in cardiac damage, which indicates a promising application prospect. However, the mechanisms are yet unclear.Methods: In this study, network pharmacology and molecular docking studies demonstrated that the effects of MTHSWD may be significantly influenced by the PI3K/Akt signaling pathway. In addition, to verify this mechanism, three groups were divided and randomly selected from among the 35 Sprague-Dawley rats: Myocardial infarction (MI) group, THSWD group, and MTHSWD group.Results: MTHSWD greatly improved fractional shortening as well as ejection fraction and reduced the infarct size. MTHSWD attenuated cell apoptosis by activating the Akt pathway in infarcted areas. In vitro, the cytoprotective effects of MTHSWD on H9C2 cells were significantly attenuated when PI3K/Akt was inhibited.Conclusion: Therefore, the study found that MTHSWD had a positive effect on heart function after myocardial infarction by activating the Akt pathway.","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142946093","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

Mechanistic Insights into the Role of MCP-1 in Diverse Liver Pathological Conditions: A Recent Update. MCP-1在多种肝脏病理状况中的作用机制：最新进展。

IF 2.6 4区医学

Current pharmaceutical design Pub Date : 2025-01-06 DOI: 10.2174/0113816128332969241120030733

Sahil Dhengle, Krushna Ch Maharana, Sarasa Meenakshi, Sanjiv Singh

{"title":"Mechanistic Insights into the Role of MCP-1 in Diverse Liver Pathological Conditions: A Recent Update.","authors":"Sahil Dhengle, Krushna Ch Maharana, Sarasa Meenakshi, Sanjiv Singh","doi":"10.2174/0113816128332969241120030733","DOIUrl":"https://doi.org/10.2174/0113816128332969241120030733","url":null,"abstract":"Monocyte chemoattractant protein-1 (MCP-1) is regarded as a crucial proinflammatory cytokine that controls the migration and entry of macrophages. It has been demonstrated that chemokine ligand 2 and its receptor, Chemokine receptor 2, are both implicated in several liver disorders. In a similar context, immunity mediators are overexpressed and stimulated by MCP-1. Additionally, MCP-1 alters the physiology of the hepatocytes, promoting immunologic and inflammatory responses beyond regular metabolism. Alcoholism and other factor including abnormal diet stimulate the liver's synthesis of MCP-1, which can result in inflammation in liver. Studies shows how MCP-1' linked to various liver disorders like Alcoholic liver disease, liver fibrosis, Non- alcoholic fatty liver disease, Hepatitis, Hepatic steatosis, hepatocellular cancer, primary biliary cirrhosis. MCP-1 not only predicts the onset, progression, and prognosis of the illness, but it is also directly related to the degree and stage of liver inflammation. In this review, we will explore the mechanism and connection between MCP-1's overexpression in liver disorders, further how it can be linked as a therapeutic biomarker in the above scenario.","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-01-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142946090","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

Unlocking Therapeutic Potential: Mesenchymal Stem Cells-derived Exosomes in IUA Treatment, Current Status and Perspectives. 释放治疗潜力：间充质干细胞来源的外泌体在IUA治疗中的现状和前景。

IF 2.6 4区医学

Current pharmaceutical design Pub Date : 2025-01-06 DOI: 10.2174/0113816128337236241210080728

Yasamin Rajabloo, Abdulridha Mohammed Al-Asady, Amir Avan, Majid Khazaei, Mikhail Ryzhikov, Seyed Mahdi Hassanian

{"title":"Unlocking Therapeutic Potential: Mesenchymal Stem Cells-derived Exosomes in IUA Treatment, Current Status and Perspectives.","authors":"Yasamin Rajabloo, Abdulridha Mohammed Al-Asady, Amir Avan, Majid Khazaei, Mikhail Ryzhikov, Seyed Mahdi Hassanian","doi":"10.2174/0113816128337236241210080728","DOIUrl":"https://doi.org/10.2174/0113816128337236241210080728","url":null,"abstract":"Intrauterine adhesion (IUA) is a condition caused by damage to the basal uterine layer which can lead to partial or full occlusion of the uterine cavity. Although traditional treatment options have been useful in mild and moderate cases, they have been unsatisfactory in severe IUA cases. Therefore, it is essential to improve the treatment strategies of IUA. Recent studies have demonstrated that Mesenchymal stem cells (MSCs) exert their therapeutic effects via the paracrine secretion of several substances including extracellular vesicles (EV) also called exosomes. MSC-derived exosomes (MSC-Exos) do not have the limitations of MSCs including immunogenicity and tumorigenicity. However, exosomes have limitations in terms of identification, isolation, purification, and origin. The clinical application of exosomes requires quality control and increased standardization in isolation and culture serum. This review summarizes therapeutic potentials of MSC-Exos and explores their potential clinical implications as diagnostic, therapeutic targets as well as prognostic markers in managing IUA.","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-01-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142946102","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

Bioactive Secondary Metabolites from Bauhinia variegata Linn. Roots: Isolation, Characterization, and Cytotoxic Evaluation. 紫荆次生代谢产物的生物活性研究。根：分离，表征和细胞毒性评价。

IF 2.6 4区医学

Current pharmaceutical design Pub Date : 2025-01-06 DOI: 10.2174/0113816128299481240223054918

Yousaf Kamal, Nighat Fatima, Amara Mumtaz, Irum Shahzadi, Abdul Mannan, Gerardo D Anaya-Eugenio, Eric Daniel Salinas Arellano, Madiha Ahmed, Zahid Hussain, Esperanza J Carcache de Blanco

{"title":"Bioactive Secondary Metabolites from Bauhinia variegata Linn. Roots: Isolation, Characterization, and Cytotoxic Evaluation.","authors":"Yousaf Kamal, Nighat Fatima, Amara Mumtaz, Irum Shahzadi, Abdul Mannan, Gerardo D Anaya-Eugenio, Eric Daniel Salinas Arellano, Madiha Ahmed, Zahid Hussain, Esperanza J Carcache de Blanco","doi":"10.2174/0113816128299481240223054918","DOIUrl":"https://doi.org/10.2174/0113816128299481240223054918","url":null,"abstract":"Introduction: This study aims to isolate and characterize potential cytotoxic compounds from the roots of Bauhinia variegata Linn. (Caesalpiniaceae) and evaluate their activity against human cancer cell lines. Five compounds, namely β-sitosterol (1), piperine (2), piperolein B (3), retrofractamide A (4), and dehydropipernonaline (5), were isolated from B. variegata roots using various chromatographic procedures.Methods: The root extracts were prepared using aqueous and organic solvents, including n-hexane, ethyl acetate, and methanol. The isolated compounds were subjected to a sulforhodamine B cytotoxicity assay against DU-145 and PC-3 (prostate), HT-29 (colon), and MCF-7 (breast) human cancer cell lines. Among the isolates, compound 5 exhibited significant bioactivity against all tested cell lines. Compound 4 demonstrated in vitro activity, specifically against MCF-7 cancer cell lines.Results: Importantly, these compounds were identified for the first time from B. variegata roots. In conclusion, this study highlights the enhanced spectrum of cytotoxic activity exhibited by the isolated compounds. These findings encourage further investigation to elucidate the mechanism of action of these compounds against the respective cell lines.Conclusion: The identification and characterization of these bioactive compounds contribute to the understanding of the potential therapeutic applications of B. variegata in cancer treatment.","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-01-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142946087","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

Pyrimidine: A Privileged Scaffold for the Development of Anticancer Agents as Protein Kinase Inhibitors (Recent Update). 嘧啶：开发抗癌药物作为蛋白激酶抑制剂的有利支架（最近更新）。

IF 2.6 4区医学

Current pharmaceutical design Pub Date : 2025-01-03 DOI: 10.2174/0113816128346900241111115125

Mai M Zeid, Osama M Elbadry, Salwa El-Meligie, Rasha A Hassan

{"title":"Pyrimidine: A Privileged Scaffold for the Development of Anticancer Agents as Protein Kinase Inhibitors (Recent Update).","authors":"Mai M Zeid, Osama M Elbadry, Salwa El-Meligie, Rasha A Hassan","doi":"10.2174/0113816128346900241111115125","DOIUrl":"https://doi.org/10.2174/0113816128346900241111115125","url":null,"abstract":"The pyrimidine nucleus is a fundamental component of human DNA and RNA, as well as the backbone of many therapeutic agents. Its significance in medicinal chemistry is well-established, with pyrimidine derivatives receiving considerable attention due to their potent anticancer properties across various cancer cell lines. Numerous derivatives have been synthesized, drawing structural inspiration from known anticancer agents like dihydropyrimidine compounds, which include the active cores of drugs such as 5-fluorouracil and monastrol, both of which have demonstrated strong anticancer efficacy. Additionally, various pyrimidine derivatives have been developed through different synthetic pathways, exhibiting promising anticancer potential. In response to the growing need for effective cancer treatments, recent efforts have focused on synthesizing and exploring novel pyrimidine derivatives with improved efficacy and specificity. This review aims to highlight the versatility of pyrimidine-based compounds in cancer therapy, emphasizing not only their potency and binding affinity but also their optimal interaction with diverse biological targets. The goal is to facilitate the design of new pyrimidine derivatives with enhanced anticancer potential, providing effective solutions for the treatment of various cancer types.","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-01-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142946096","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

One-pot, Four-component Synthesis, Molecular Docking and Pharmacokinetic Studies of Tetra-substituted Imidazole Derivatives as Potential Mushroom Tyrosinase Inhibitors. 四取代咪唑类蘑菇酪氨酸酶抑制剂的一锅四组分合成、分子对接及药代动力学研究。

IF 2.6 4区医学

Current pharmaceutical design Pub Date : 2025-01-02 DOI: 10.2174/0113816128330769241113095033

Muhammad Naseem, Hummera Rafique, Sadia Roshan, Zaman Ashraf, Fouzia Perveen, Muhammad Tayyab

{"title":"One-pot, Four-component Synthesis, Molecular Docking and Pharmacokinetic Studies of Tetra-substituted Imidazole Derivatives as Potential Mushroom Tyrosinase Inhibitors.","authors":"Muhammad Naseem, Hummera Rafique, Sadia Roshan, Zaman Ashraf, Fouzia Perveen, Muhammad Tayyab","doi":"10.2174/0113816128330769241113095033","DOIUrl":"https://doi.org/10.2174/0113816128330769241113095033","url":null,"abstract":"Introduction: An efficient and four-component one-pot facile synthesis of tetra-substituted imidazole is achieved by cyclo-condensation reaction of benzil with subsequent successive substitution of aromatic aldehydes, ester substituted amine and ammonium acetate via refluxing the mixture for almost two hours at 140°C.Method: The ending point of the understudy reaction was examined by TLC after regular intervals. Synthesized 1,2,4-tetrasubstituted imidazoles were characterized by physical data and the structural features were analyzed using spectroscopic techniques such as FTIR, NMR and elemental analysis.Results: The inhibition potential of fabricated compounds was evaluated against the mushroom based Tyrosinase (polyphenol oxidase) enzyme. Tetra-substituted imidazole derivatives demonstrated significant potent tyrosinase inhibition activities.Conclusion: Pharmacokinetic mechanism and molecular docking studies were also carried out.","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142930850","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

Virtual Screening Identifies Inhibitors of SARS-CoV-2 Main Protease through Pharmacophore and Similarity Approaches. 利用药效团和相似性方法虚拟筛选SARS-CoV-2主要蛋白酶抑制剂

IF 2.6 4区医学

Current pharmaceutical design Pub Date : 2025-01-02 DOI: 10.2174/0113816128358219241210101947

Mohammad A Khanfar, Mohammad Saleh

{"title":"Virtual Screening Identifies Inhibitors of SARS-CoV-2 Main Protease through Pharmacophore and Similarity Approaches.","authors":"Mohammad A Khanfar, Mohammad Saleh","doi":"10.2174/0113816128358219241210101947","DOIUrl":"https://doi.org/10.2174/0113816128358219241210101947","url":null,"abstract":"Introduction: The emergence of SARS-CoV-2 and the COVID-19 pandemic highlighted the urgent need for novel antiviral therapies. The main protease (Mpro) of SARS-CoV-2 is a key enzyme in viral replication and a promising therapeutic target.Methods: This study employed virtual screening approaches to identify potential Mpro inhibitors, leveraging both structure- and ligand-based methods.Results: Two optimum pharmacophore models were built from hundreds of crystallographic structures of Mpro, validated through ROC curve analysis and Dynophores dynamic simulations. These models captured ≈ 60K hits from six diverse compound libraries made of more than 3 million compounds. Additionally, a ligandbased similarity search using ROCS software identified 1024 potential hits based on shape and atom-based comparisons with co-crystallized ligands. Subsequent molecular docking and filtering based on physicochemical properties and structural diversity yielded 16 and 6 hits from structure- and ligand-based screening, respectively. Molecular dynamics simulations were conducted on the top-scoring hits to assess their binding stability within the Mpro active site. SCR00943 demonstrated stable binding, interacting favorably with key residues, including the catalytic dyad, resulting in a binding affinity of -61.2 kcal/mol.Conclusion: This virtual screening campaign identified promising Mpro inhibitors, showcasing the potential of computational approaches to accelerate drug discovery efforts against COVID-19.","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142930853","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

Revolutionizing Cancer Treatment: Unveiling the Power of CAR T-cell Therapy. 革命性的癌症治疗：揭示CAR - t细胞疗法的力量。

IF 2.6 4区医学

Current pharmaceutical design Pub Date : 2025-01-02 DOI: 10.2174/0113816128336391241107112957

Amir Hossein Barjasteh, Mostafa Saebi, Mahmoud Mahmoudi, Ramiar Kamal Kheder, Seyed Isaac Hashemy, Fatemeh Forouzanfar, Seyed-Alireza Esmaeili

引用次数: 0