Current drug discovery technologies最新文献

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Delineating CYP2C19-Mediated Interactions: Network Pharmacology Investigation of Ilaprazole and Clopidogrel versus Conventional Proton Pump Inhibitors. 描述cyp2c19介导的相互作用:伊拉唑和氯吡格雷与传统质子泵抑制剂的网络药理学研究。
Current drug discovery technologies Pub Date : 2024-12-31 DOI: 10.2174/0115701638334244241224062453
Priyadharshini Ananthathandavan, Damodharan Narayanasamy
{"title":"Delineating CYP2C19-Mediated Interactions: Network Pharmacology Investigation of Ilaprazole and Clopidogrel versus Conventional Proton Pump Inhibitors.","authors":"Priyadharshini Ananthathandavan, Damodharan Narayanasamy","doi":"10.2174/0115701638334244241224062453","DOIUrl":"10.2174/0115701638334244241224062453","url":null,"abstract":"<p><strong>Background: </strong>Clopidogrel, an antiplatelet drug commonly used in cardiovascular disease, is metabolized by the liver mainly through CYP2C19. Concomitant use of Proton pump inhibitors along with clopidogrel may affect the potency of clopidogrel by CYP2C19 inhibition. However, a novel PPI, ilaprazole is known to differ in its pharmacokinetic features, given the potential differences between ilaprazole’s interactions and their metabolism with clopidogrel. Network pharmacology investigation could be a useful tool to evaluate the drug-drug interaction between them.</p><p><strong>Methodology: </strong>The molecular structures and targets were retrieved from PubChem and SwissTargetPrediction to establish the information related to the identified drugs. The possible shared targets between the clopidogrel and PPIs were explored by a Venn analysis. Subsequently, Protein-Protein Interaction networks were established using the STRING database. Hub genes were also determined using the Cytoscape cytoHubba plugin.</p><p><strong>Results & discussion: </strong>Ilaprazole (13.6%) and pantoprazole (13.6%) were characterized by fewer targets being shared with clopidogrel compared to conventional PPIs (14.9%). Moreover, CYP2C19 was not a hub gene in ilaprazole and pantoprazole interactions, which indicated no significant CYP2C19 involvement. On the other hand, CYP2C19 functioned as a hub gene in the interactions with rabeprazole, lansoprazole, dexlansoprazole, omeprazole, and esomeprazole. As a result, patients receiving pantoprazole and ilaprazole would be at a lower risk for developing adverse cardiovascular events by maintaining the clopidogrel therapeutic effect.</p><p><strong>Conclusion: </strong>The application of the network pharmacology technique allows us to consider the potential for different effects of PPIs on clopidogrel and its metabolism via CYP2C19. There is a lower chance of experiencing adverse effects from an interaction between ilaprazole and clopidogrel as ilaprazole has not been linked to CYP2C19. More research is necessary to confirm these results and provide clinical guidance for patients undergoing clopidogrel and PPI combination therapy.</p>","PeriodicalId":93962,"journal":{"name":"Current drug discovery technologies","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143018146","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
Importance of Computer-Aided Drug Design in Modern Pharmaceutical Research. 计算机辅助药物设计在现代药物研究中的重要性。
Current drug discovery technologies Pub Date : 2024-12-31 DOI: 10.2174/0115701638361318241230073123
Uma Agarwal, Rajiv Kumar Tonk, Swati Paliwal
{"title":"Importance of Computer-Aided Drug Design in Modern Pharmaceutical Research.","authors":"Uma Agarwal, Rajiv Kumar Tonk, Swati Paliwal","doi":"10.2174/0115701638361318241230073123","DOIUrl":"https://doi.org/10.2174/0115701638361318241230073123","url":null,"abstract":"<p><strong>Background: </strong>Computer-Aided Drug Design (CADD) approaches are essential in the drug discovery and development process. Both academic institutions and pharmaceutical and biotechnology corporations utilize them to enhance the efficacy of bioactive compounds.</p><p><strong>Objective: </strong>This study aims to entice researchers by investigating the benefits of Computer-Aided Drug and Design (CADD) and its fundamental principles. The main focus is to speed up the drug discovery process, improve accuracy, and reduce the time and financial resources needed, ultimately making a positive impact on public health.</p><p><strong>Method: </strong>A comprehensive literature search was conducted using databases such as PubMed and Scopus, focusing on studies published till 2024. The selection of studies was based on their analysis of the connection between contemporary pharmaceutical research and computer-aided drug design, with a focus on both structure-based and ligand-based drug design strategies can include molecular docking, fragment-based drug discovery, de novo drug design, pharmacophore modelling, Quantitative structure-activity relationship, 3D-QSAR, homology modelling, in silico absorption-distribution- metabolism-excretion-toxicity, and machine learning/deep learning.</p><p><strong>Result: </strong>Computer-Aided Drug Design (CADD) approaches are mathematical tools used to modify and measure certain characteristics of possible drug candidates. These methods are implemented in various applications. These encompass a variety of software products that are accessible to the public and can be purchased for corporate use. The CADD method is used at several stages of the drug development process, including as a foundation for chemical synthesis and biological testing. It provides information for the development of future SAR (Structure-Activity Relationship), resulting in enhanced molecules in terms of their activity and ADME (Absorption, Distribution, Metabolism, and Excretion). CADD techniques are predominantly employed to analyze and assess the affinity of large molecules for specific biomolecules, such as DNA, RNA, proteins, and enzymes, which serve exclusively as receptors. CADD improves the selection of lead compounds by predicting various parameters, including drug-likeness, physicochemical properties, pharmacokinetics, and toxicity. The application of CADD in drug modelling is to tackle challenges such as cost and time constraints. Modern computer-assisted drug discovery necessitates conducting virtual screening and high-throughput screening (HTS).</p><p><strong>Conclusion: </strong>Computer-aided drug design plays a crucial role for academic institutions and leading pharmaceutical companies in the development of drugs that enhance potency with the significance of reducing both time and costs.</p>","PeriodicalId":93962,"journal":{"name":"Current drug discovery technologies","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142985695","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
A Comprehensive Review on Immunoregulatory Effects of Phytochemicals. 植物化学物质免疫调节作用研究综述
Current drug discovery technologies Pub Date : 2024-12-02 DOI: 10.2174/0115701638326442241118053543
Shikha Sharma, Utkarsh Sharma, Neha Dangi, Mukesh K Gupta, Anurag Agrawal, Suraj N Mali, Bimal Krishna Banik
{"title":"A Comprehensive Review on Immunoregulatory Effects of Phytochemicals.","authors":"Shikha Sharma, Utkarsh Sharma, Neha Dangi, Mukesh K Gupta, Anurag Agrawal, Suraj N Mali, Bimal Krishna Banik","doi":"10.2174/0115701638326442241118053543","DOIUrl":"https://doi.org/10.2174/0115701638326442241118053543","url":null,"abstract":"<p><p>An efficient immune system in the host body plays a crucial role in the preservation of normal biological and immune reactions and processes, as well as the intrinsic environment. This is because the immune system is responsible for fighting off foreign invaders. A healthy immune system strengthens the body's defense against infections, illnesses, and other unwelcome pathogens, thereby reducing the risk of allergic reactions and autoimmune diseases. Innate immune cells and acquired immune system components interact in a corrective fashion to produce optimal immune responses. In recent years, researchers have begun to focus on the immune system as a potential primary target of toxicity from chemical, pharmacological, and environmental exposure. Sex, age, stress, malnutrition, alcohol, genetic variability, lifestyles, environmental pollutants, and chemotherapy are just a few of the many elements that might modify the host's immunological responses. The production, amplification, attenuation, or suppression of immunological responses are all examples of immunomodulation. There are a wide variety of synthetic and traditional treatments available, and many of them cause major side effects and develop pathogenic resistance very quickly. Natural substances called phytochemicals play a crucial role in regulating the body's immune system. Risk factors for immune response changes are discussed, as is the immunomodulatory action of phytochemicals like glycosides, alkaloids, phenolic acids, flavonoids, saponins, tannins, sterols, and steroids.</p>","PeriodicalId":93962,"journal":{"name":"Current drug discovery technologies","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-12-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142775856","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
Computational Screening of Novel Nitroimidazole Candidates: Targeting Key Enzymes of Oral Anaerobes for Anti-Parasitic Potential. 新型硝基咪唑候选化合物的计算筛选:针对口腔厌氧菌关键酶的抗寄生虫潜力。
Current drug discovery technologies Pub Date : 2024-11-05 DOI: 10.2174/0115701638326365241029080310
Touhami Lanez, Maroua Lanez, Riad Lanez, Elhafnaoui Lanez, Badia Talbi-Lanez
{"title":"Computational Screening of Novel Nitroimidazole Candidates: Targeting Key Enzymes of Oral Anaerobes for Anti-Parasitic Potential.","authors":"Touhami Lanez, Maroua Lanez, Riad Lanez, Elhafnaoui Lanez, Badia Talbi-Lanez","doi":"10.2174/0115701638326365241029080310","DOIUrl":"10.2174/0115701638326365241029080310","url":null,"abstract":"<p><strong>Background: </strong>The study focuses on evaluating the parasitic potential of novel metronidazole analogs using computational methods. Specifically, it aims to target key enzymes of oral anaerobes, including UDP-N-acetylglucosamine 1-carboxyvinyltransferase (MurA) of Fusobacterium nucleatum and DNA topoisomerase (Topo) of Prevotella intermedia.</p><p><strong>Objective: </strong>The objective is to assess the pharmacokinetic and toxicity properties of 368 novel nitroimidazole candidates through virtual screening. Additionally, the study aims to determine the binding affinity of the most promising candidates with the target proteins through molecular docking analyses.</p><p><strong>Methods: </strong>A combinatorial library of nitroimidazole candidates was constructed, and virtual screening was performed. Molecular docking analyses were conducted to evaluate the binding affinity of selected compounds with MurA and Topo. Further investigation involved molecular dynamic simulation to assess the stability of the compounds within the active sites of MurA and Topo.</p><p><strong>Results: </strong>All selected compounds exhibited activity against both MurA and Topo. Among them, Mnz11, Mnz12, and Mnz15 demonstrated the lowest binding free energies and IC50 values. Molecular dynamic simulation indicated that these three compounds remained stable within the active sites of MurA and Topo, with RMSD values consistently below 2Å. Additionally, the antibacterial potential of the most potent compound, Mnz15, was evaluated against a series of oral microbes.</p><p><strong>Conclusion: </strong>The study concludes that the newly identified nitroimidazole candidates show promise as anti-parasitic agents, based on their activity against key enzymes of oral anaerobes and their pharmacokinetic properties evaluated through computational methods.</p>","PeriodicalId":93962,"journal":{"name":"Current drug discovery technologies","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-11-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142590774","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
Preliminary Characterization of the Vasorelaxant Effect of Thymus atlanticus (Ball) Roussine Using Optical Methods. 用光学方法初步鉴定大西洋胸腺(波尔)鲁辛的血管舒张效果
Current drug discovery technologies Pub Date : 2024-11-04 DOI: 10.2174/0115701638309612240726060844
Hamza Elbouny, Nabil Bouchebchoub, Brahim Ouahzizi, Rania Hajjami, Younes Filali-Zegzouti, Mohamed Yassine Amarouch, Chakib Alem
{"title":"Preliminary Characterization of the Vasorelaxant Effect of Thymus atlanticus (Ball) Roussine Using Optical Methods.","authors":"Hamza Elbouny, Nabil Bouchebchoub, Brahim Ouahzizi, Rania Hajjami, Younes Filali-Zegzouti, Mohamed Yassine Amarouch, Chakib Alem","doi":"10.2174/0115701638309612240726060844","DOIUrl":"https://doi.org/10.2174/0115701638309612240726060844","url":null,"abstract":"<p><strong>Background: </strong>Thymus atlanticus (Ball) Roussine is a Moroccan endemic thyme species that is traditionally used as an aromatic and medicinal plant. Several studies have demonstrated its pharmacological significance and therapeutic value.</p><p><strong>Objective: </strong>The current study aimed to assess the vasorelaxant effect of the aqueous extract of this species.</p><p><strong>Methods: </strong>The contractility of isolated rat aortas was investigated using the multi-well organ bath technique. This method was adapted and validated in our experimental conditions using epinephrine and hydralazine as vasoconstrictive and vasodilator agents, respectively. The application of 10 μM epinephrine induced a clear vasoconstriction of the aorta rings (Lumen reduction = 31.8±0.4%). However, hydralazine induced a dose-dependent relaxation with an EC50 value of 6.1±1.2 mM. For the aqueous extract of T. atlanticus, the aortic rings were precontracted with epinephrine, and then increasing concentrations (0.125-1 mg/mL) of this extract were added cumulatively.</p><p><strong>Results: </strong>The results have indicated T. atlanticus extract to have a significant vasodilatory effect in a dose-dependent manner (EC50 = 0.52±0.03 mg/mL).</p><p><strong>Conclusion: </strong>The findings provide preliminary evidence of the vasorelaxant effect of the aqueous extract of T. atlanticus using a low-cost optical approach. However, the cellular and molecular mechanisms underlying this effect have yet to be revealed.</p>","PeriodicalId":93962,"journal":{"name":"Current drug discovery technologies","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-11-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142585213","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
AI in Clinical Trials and Drug Development: Challenges and Potential Advancements. 人工智能在临床试验和药物开发中的应用:挑战与潜在进步。
Current drug discovery technologies Pub Date : 2024-10-28 DOI: 10.2174/0115701638314252241016165345
Divyanshi Gupta, Pranay Wal, Ankita Wal, Sribhavani K R, Mudit Kumar, Krishna Chandra Panda, Mukesh Chandra Sharma
{"title":"AI in Clinical Trials and Drug Development: Challenges and Potential Advancements.","authors":"Divyanshi Gupta, Pranay Wal, Ankita Wal, Sribhavani K R, Mudit Kumar, Krishna Chandra Panda, Mukesh Chandra Sharma","doi":"10.2174/0115701638314252241016165345","DOIUrl":"https://doi.org/10.2174/0115701638314252241016165345","url":null,"abstract":"<p><p>Artificial intelligence (AI) is one of the fastest-growing fields in various industries, including engineering, architecture, medical and clinical research, aerospace, and others. AI, which is a combination of machine learning (ML), deep learning (DL), and human intelligence (HI), is revolutionizing drug discovery and development by making it more cost-effective and efficient. It is also being used in fields such as medicinal chemistry, molecular and cell biology, pharmacology, pharmacokinetics, formulation development, and toxicology. AI plays a crucial role in clinical testing by enhancing patient stratification, patient sample evaluation, and trial design, assisting in the identification of biomarkers, determining efficacy criteria, dose selection, trial length, and target patient population selection. The primary objective of this study is to emphasize the importance of AI in clinical trials and drug development, while also exploring the existing challenges and potential advancements in AI within the healthcare industry. A comprehensive literature review was conducted, covering the period from 1998 to 2023. The Science Direct, PubMed, and Google Scholar databases were searched for relevant information. A variety of publications, including Research Gate, Nature, MDPI, and Springer Link, provided pertinent data. This study aimed to gain a deeper understanding of the use of AI in clinical research and drug development, as well as its potential and limitations. We also discuss the benefits and main data limitations of the traditional trial and drug development approach. AI approaches are currently being used to overcome research obstacles and eliminate conceptual or methodological limitations. After discussing possible obstacles and coping mechanisms, we provide several recommendations to help individuals understand the challenges and difficulties associated with clinical research and drug development. It is essential for pharmaceutical companies to have a cutting-edge AI strategy if AI is to become a routine tool for clinical research and drug development.</p>","PeriodicalId":93962,"journal":{"name":"Current drug discovery technologies","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-10-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142549642","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
An Update on Clinically Evaluated Medicinal Plants for Psoriasis Management. 经临床评估可用于治疗牛皮癣的药用植物的最新进展。
Current drug discovery technologies Pub Date : 2024-10-28 DOI: 10.2174/0115701638327441241016014503
Ramin Ansari, Mahkameh Moradi Mehrabadi, Mahnaz Sadat Hosseini, Mehdi Ghahartars, Mohammad Mehdi Zarshenas
{"title":"An Update on Clinically Evaluated Medicinal Plants for Psoriasis Management.","authors":"Ramin Ansari, Mahkameh Moradi Mehrabadi, Mahnaz Sadat Hosseini, Mehdi Ghahartars, Mohammad Mehdi Zarshenas","doi":"10.2174/0115701638327441241016014503","DOIUrl":"https://doi.org/10.2174/0115701638327441241016014503","url":null,"abstract":"<p><p>Psoriasis is a prevalent inflammatory disease affecting almost 0.5-5 % of the world population. Multiple treatment approaches have been developed to manage psoriasis so far. Although concerns exist in the long-term usage of conventional and biological agents in terms of safety, effectiveness, expensiveness, and tolerability, complementary and alternative medicine (CAM) is a promising point of view for future psoriasis management. In this study, databases including Scopus, PubMed, Google Scholar, and Web of Science were searched for relevant literature on herbal medications clinically evaluated for psoriasis, especially those originating from traditional medicine. About 40 relevant papers were selected by March 2023. Most of the studies were clinical trials on poly-herbal formulations from traditional Chinese medicine (TCM). There are controversial results regarding the efficacy of these herbal formulations in psoriasis mainly due to the variation in the study design. Moreover, the probable protective mechanisms and responsible herbal metabolites of these formulations are summarized. There is a global need for more in-vitro and in-vivo studies based on the standard protocols in terms of the evaluation of the safety and efficacy of topical/ systemic herbal preparations for psoriasis.</p>","PeriodicalId":93962,"journal":{"name":"Current drug discovery technologies","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-10-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142549643","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
In Vitro Antibacterial Activity of Adiantum capillus Veneris Extraction with Methanol, Chloroform, and Ether Solvents against Methicillin-resistant Staphylococcus aureus. 用甲醇、氯仿和乙醚溶剂提取的 Adiantum capillus Veneris 对耐甲氧西林金黄色葡萄球菌的体外抗菌活性。
Current drug discovery technologies Pub Date : 2024-10-25 DOI: 10.2174/0115701638313570241015045118
Mahdiyeh Ebrahimzadeh, Solmaz Rahbari, Reza Hosseini Doust, Faraz Mojab
{"title":"In Vitro Antibacterial Activity of Adiantum capillus Veneris Extraction with Methanol, Chloroform, and Ether Solvents against Methicillin-resistant Staphylococcus aureus.","authors":"Mahdiyeh Ebrahimzadeh, Solmaz Rahbari, Reza Hosseini Doust, Faraz Mojab","doi":"10.2174/0115701638313570241015045118","DOIUrl":"https://doi.org/10.2174/0115701638313570241015045118","url":null,"abstract":"<p><strong>Background: </strong>The increasing problem of multi-drug resistant (MDR) pathogens is a worldwide concern, especially in the pharmaceutical industry. At the same time, medicinal plants have renewed interest because of their wide variety of bioactive phytochemicals, which could be used to develop new antimicrobial drugs. This renewed interest is partly due to the growing resistance to traditional drugs and their associated side effects.</p><p><strong>Methods: </strong>The objective of this study is to assess the antimicrobial properties of the total extract and various fractions of Adiantum capillus veneris against Methicillin-resistant Staphylococcus aureus (MRSA). The aerial parts of Adiantum capillus veneris were subjected to extraction using methanol, chloroform, and ether, and the resulting extracts were tested for their antimicrobial activity against MRSA. Additionally, essential oil was obtained from the aerial parts using a Clevenger apparatus and boiling water. Furthermore, Gas Chromatography-Mass Spectrometry (GC/MS) was utilized to analyze the phytochemicals isolated from the extracts of Adiantum capillus veneris.</p><p><strong>Results: </strong>The essential oil was obtained through distillation and then analyzed using GC/MS. The antimicrobial activity was evaluated using the agar diffusion method.</p><p><strong>Conclusion: </strong>GC/MS analysis revealed that the composition was primarily phytol (59.9%), constituting 99.3% of phyto-constituents. However, both the total extract and the individual fractions exhibited no inhibitory effects against MRSA strains.</p>","PeriodicalId":93962,"journal":{"name":"Current drug discovery technologies","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142549644","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
Potential Role of Benzoic Acid and its Synthetic Derivatives to Alleviate Cancer: An Up-to-Date Review. 苯甲酸及其合成衍生物在缓解癌症方面的潜在作用:最新综述。
Current drug discovery technologies Pub Date : 2024-10-07 DOI: 10.2174/0115701638311865240904054111
Arvind Kumar, Kamal Yt, Arun K Mishra, Mhaveer Singh, Harpreet Singh, Niranjan Kaushik, Amrita Mishra
{"title":"Potential Role of Benzoic Acid and its Synthetic Derivatives to Alleviate Cancer: An Up-to-Date Review.","authors":"Arvind Kumar, Kamal Yt, Arun K Mishra, Mhaveer Singh, Harpreet Singh, Niranjan Kaushik, Amrita Mishra","doi":"10.2174/0115701638311865240904054111","DOIUrl":"https://doi.org/10.2174/0115701638311865240904054111","url":null,"abstract":"<p><p>Unregulated cell division is one of the main causes of cancer. These cancerous cells negatively impact nearby healthy cells. Cancer can occur anywhere in the body. Normal cell division occurs when cells grow, reproduce, and divide as the body needs. As a normal cascade of cell growth and division, when the cells get damaged, they undergo death, and normal cells develop. However, sometimes, this process is not followed, and abnormal or damaged cells start to grow and multiply several times more than normal. This particular process may form the basis of cancer. There is a research gap in terms of identifying personalized synthetic anticancer therapy, which may be based on individual patient characteristics with an aim to optimize treatment efficacy and minimize adverse effects. While searching for new bioactive compounds, it has been observed that organic molecules with benzoic acid (BA) moiety possess significant anticancer potential. Several works of literature reported the use of BA from natural or synthetic sources to synthesize bioactive chemicals. It has been observed that several natural products also contain BA moiety, and the presence of this moiety is considered responsible for several important biological activities. Therefore, in order to chemically synthesize a wide variety of potent biologically active compounds, benzoic acid as a basic moiety in the form of a scaffold can be employed. Other synthetic compounds with BA scaffolds include furosemide, tetracaine, and bumetanide. The current article aims to focus on past and present work done on BA derivatives and to emphasize the molecular pathways involved in cancer treatment. The future prospects for research in this area are encouraging as researchers are striving to advance synthetic BA derivatives. This could possibly contribute to more efficient treatments and better results for cancer patients.</p>","PeriodicalId":93962,"journal":{"name":"Current drug discovery technologies","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-10-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142396227","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
Liquisolid Technique for Solubility Enhancement of Poorly Soluble Drug - A Brief Review. 用于提高难溶性药物溶解度的 Liquisolid 技术--简要回顾。
Current drug discovery technologies Pub Date : 2024-10-04 DOI: 10.2174/0115701638318659240923074614
Amaresh Prusty, Bikash Ranajn Jena, Vivek Barik, Piyali Khamkat, Bhakti Bhusan Barik
{"title":"Liquisolid Technique for Solubility Enhancement of Poorly Soluble Drug - A Brief Review.","authors":"Amaresh Prusty, Bikash Ranajn Jena, Vivek Barik, Piyali Khamkat, Bhakti Bhusan Barik","doi":"10.2174/0115701638318659240923074614","DOIUrl":"https://doi.org/10.2174/0115701638318659240923074614","url":null,"abstract":"<p><p>Most of the newly discovered drug candidates are lipophilic and poorly water-soluble, making it a significant challenge for the pharmaceutical industry to formulate suitable drug delivery systems. This review gives insight into an overview of the liquisolid technique (LST) and summarizes the progress of its various applications in drug delivery. This novel technique involves converting liquid drugs or drugs in a liquid state (such as solutions, suspensions, or emulsions) into dry, nonadherent, free-flowing, and readily compressible powder mixtures by blending or spraying a liquid dispersion onto specific powder carriers and coating materials. In Liquisolid systems, the liquid medication is absorbed into the interior framework of carriers. Once the carrier's interior is saturated with liquid medication, a liquid layer forms on the surface of the carrier particles, which is instantly adsorbed by the fine coating material. As a result, a dry, free-flowing, and compressible powder mixture is formed. Compared to other solubility enhancement techniques, s.a. micronization, inclusion complexation, microencapsulation, nanosuspension, and self-nano emulsions, LST is relatively simple to prepare and may offer a cost-effective solution to enhance the solubility of poorly water-soluble drugs enhancing its bioavailability in drug formulation and delivery.</p>","PeriodicalId":93962,"journal":{"name":"Current drug discovery technologies","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-10-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142396226","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}
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