DARU Journal of Pharmaceutical Sciences最新文献

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Antimicrobial activity and mechanism of anti-MRSA of phloroglucinol derivatives. 氯代葡萄糖苷衍生物的抗微生物活性和抗 MRSA 的机理。
IF 3.6 4区 医学
DARU Journal of Pharmaceutical Sciences Pub Date : 2024-06-01 Epub Date: 2024-01-22 DOI: 10.1007/s40199-024-00503-4
Xianjing Yang, Xinjiao Gao, Jiayi Ou, Gong Chen, Lianbao Ye
{"title":"Antimicrobial activity and mechanism of anti-MRSA of phloroglucinol derivatives.","authors":"Xianjing Yang, Xinjiao Gao, Jiayi Ou, Gong Chen, Lianbao Ye","doi":"10.1007/s40199-024-00503-4","DOIUrl":"10.1007/s40199-024-00503-4","url":null,"abstract":"<p><strong>Background: </strong>In previous studies, authors have completed the total synthesis of several phloroglucinol natural products and synthesized a series of their derivatives, which were tested with good biological activities.</p><p><strong>Objectives: </strong>To discover anti-MRSA lead compound and study their mechanism of action.</p><p><strong>Methods: </strong>Phloroglucinol derivatives were tested to investigate their activities against several gram-positive strains including Methicillin-resistant Staphylococcus aureus (MRSA). The mechanism study was conducted by determining extracellular potassium ion concentration, intracellular NADPH oxidase content, SOD activity, ROS amount in MRSA and MRSA survival rate under A5 treatment. The in vitro cytotoxicity test of A5 was conducted.</p><p><strong>Results: </strong>The activity of monocyclic compounds was stronger than that of bicyclic compounds, and compound A5 showed the best MIC value of 0.98 μg/mL and MBC value of 1.95 μg/mL, which were 4-8 times lower than that of vancomycin. The mechanism study of A5 showed that it achieved anti-MRSA effect through membrane damage, which is proved by increased concentration of extracellular potassium ion after A5 treatment. Another possible mechanism is the over ROS production induced cell death, which is suggested by observed alternation of several reactive oxygen species (ROS) related indicators including NADPH concentration, superoxide dismutase (SOD) activity, ROS content and bacterial survival rate after A5 treatment. The cytotoxicity results in vitro showed that A5 was basically non-toxic to cells.</p><p><strong>Conclusion: </strong>Acylphloroglucinol derivative A5 showed good anti-MRSA activity, possibly via membrane damage and ROS-mediated oxidative stress mechanism. It deserves further exploration to be a potential lead for the development of new anti-MRSA agent.</p>","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":" ","pages":"177-187"},"PeriodicalIF":3.6,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11087386/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139511468","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Immediate hypersensitivity reaction to levetiracetam: a case report study. 左乙拉西坦的即时超敏反应:一例病例报告研究。
IF 2.5 4区 医学
DARU Journal of Pharmaceutical Sciences Pub Date : 2024-06-01 Epub Date: 2023-11-02 DOI: 10.1007/s40199-023-00488-6
Mahnaz Sadat Hosseini, Soha Namazi
{"title":"Immediate hypersensitivity reaction to levetiracetam: a case report study.","authors":"Mahnaz Sadat Hosseini, Soha Namazi","doi":"10.1007/s40199-023-00488-6","DOIUrl":"10.1007/s40199-023-00488-6","url":null,"abstract":"<p><strong>Background: </strong>Anticonvulsant drugs are one of the most common causes of delayed hypersensitivity reactions, such as drug reaction with eosinophilia and systemic symptoms (DRESS), Stevens-Johnson syndrome (SJS), and toxic epidermal necrolysis (TEN). These reactions are more prevalent with aromatic anticonvulsant drugs such as phenytoin and carbamazepine. However, immediate hypersensitivity reactions such as urticaria, angioedema, and anaphylaxis with anticonvulsant drugs are rare. We describe a 51-year-old woman who developed spreading skin rashes on her wrists with urticaria and pruritus 24 h after receiving intravenous levetiracetam.</p><p><strong>Conclusion: </strong>Clinicians should be aware of immediate hypersensitivity reactions with intravenous levetiracetam.</p>","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":" ","pages":"435-438"},"PeriodicalIF":2.5,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11087434/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71421479","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Fruit vinegar as a promising source of natural anti-inflammatory agents: an up-to-date review. 果醋作为一种有前途的天然抗炎剂来源:最新的评论。
IF 2.5 4区 医学
DARU Journal of Pharmaceutical Sciences Pub Date : 2024-06-01 Epub Date: 2023-12-01 DOI: 10.1007/s40199-023-00493-9
Driss Ousaaid, Meryem Bakour, Hassan Laaroussi, Asmae El Ghouizi, Badiaa Lyoussi, Ilham El Arabi
{"title":"Fruit vinegar as a promising source of natural anti-inflammatory agents: an up-to-date review.","authors":"Driss Ousaaid, Meryem Bakour, Hassan Laaroussi, Asmae El Ghouizi, Badiaa Lyoussi, Ilham El Arabi","doi":"10.1007/s40199-023-00493-9","DOIUrl":"10.1007/s40199-023-00493-9","url":null,"abstract":"<p><strong>Objectives: </strong>Fruit vinegar is one of the most famous fruit byproducts worldwide with several unique properties. There are two types of fruit vinegar, artisanal and industrial, for consumers to choose from. This review aims to assess for the first time the phytochemistry of fruit vinegar and its anti-inflammatory effects.</p><p><strong>Method: </strong>The present work was conducted based on a literature search that selected the relevant papers from indexed databases such as Scopus, Science Direct, MDPI, PubMed, Hindawi, and Web of Science. We used numerous terms to assure a good search in different databases, including fruit vinegar, phytochemistry, bioavailability and bioaccessibility, and anti-inflammatory effect. All articles were selected based on their relevance, quality, and problematic treatment.</p><p><strong>Results: </strong>Literature data have shown that vinegar has a long medicinal history and has been widely used by different civilizations, due to its richness in bioactive molecules, vinegar plays an important role in the prevention and treatment of various inflammatory diseases, including atopic dermatitis, mastitis, asthma, arthritis, acute pancreatitis, and colitis. Fruit vinegar consumption benefit is highly dependent on its chemical composition, especially organic acids and antioxidants, which can act as nutraceuticals.</p><p><strong>Conclusion: </strong>Fruit vinegar has a rich chemical composition, including organic acids that can be transformed in the digestive system into compounds that play an important role in health-promoting features such as anti-inflammatory effects throughout the control of intestinal microbiota and pro-inflammatory cytokine production.</p>","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":" ","pages":"307-317"},"PeriodicalIF":2.5,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11087403/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138470079","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Evaluation of 1,10-phenanthroline-based hydroxamate derivative as dual histone deacetylases/ribonucleotide reductase inhibitor with antitumor activities 评估 1,10-菲罗啉基羟酰胺衍生物作为组蛋白去乙酰化酶/核糖核苷酸还原酶双重抑制剂的抗肿瘤活性
IF 3.6 4区 医学
DARU Journal of Pharmaceutical Sciences Pub Date : 2024-04-29 DOI: 10.1007/s40199-024-00514-1
Manasa Gangadhar Shetty, Padmini Pai, Bipasa Dey, Kapaettu Satyamoorthy, Suranjan Shil, Usha Yogendra Nayak, Ashwini T, Babitha Kampa Sundara
{"title":"Evaluation of 1,10-phenanthroline-based hydroxamate derivative as dual histone deacetylases/ribonucleotide reductase inhibitor with antitumor activities","authors":"Manasa Gangadhar Shetty, Padmini Pai, Bipasa Dey, Kapaettu Satyamoorthy, Suranjan Shil, Usha Yogendra Nayak, Ashwini T, Babitha Kampa Sundara","doi":"10.1007/s40199-024-00514-1","DOIUrl":"https://doi.org/10.1007/s40199-024-00514-1","url":null,"abstract":"<h3 data-test=\"abstract-sub-heading\">Background</h3><p>Aberrant expression of histone deacetylases (HDACs) and ribonucleotide reductase (RR) enzymes are commonly observed in various cancers. Researchers are focusing on these enzymes in cancer studies with the aim of developing effective chemotherapeutic drugs for cancer treatment. Targeting both HDAC and RR simultaneously with a dual HDAC/RR inhibitor has exhibited enhanced effectiveness compared to monotherapy in cancer treatment, making it a promising strategy.</p><h3 data-test=\"abstract-sub-heading\">Objectives</h3><p>The objective of the study is to synthesize and assess the anti-cancer properties of a 1,10-phenanthroline-based hydroxamate derivative, characterizing it as a novel dual HDAC/RR inhibitor.</p><h3 data-test=\"abstract-sub-heading\">Methods</h3><p>The <i>N</i><sup>1</sup>-hydroxy-<i>N</i><sup>8</sup>-(1,10-phenanthrolin-5-yl)octanediamide (PA), a 1,10-phenanthroline-based hydroxamate derivative, was synthesized and structurally characterized. The compound was subjected to in vitro assessments of its anti-cancer, HDAC, and RR inhibitory activities. In silico docking and molecular dynamics simulations were further studied to explore its interactions with HDACs and RRM2.</p><h3 data-test=\"abstract-sub-heading\">Results</h3><p>The structurally confirmed PA exhibited antiproliferative activity in SiHa cells with an IC<sub>50</sub> of 16.43 μM. It displayed potent inhibitory activity against HDAC and RR with IC<sub>50</sub> values of 10.80 μM and 9.34 μM, respectively. Co-inhibition of HDAC and RR resulted in apoptosis-induced cell death in SiHa cells, mediated by the accumulation of reactive oxygen species (ROS). In silico docking studies demonstrated that PA can effectively bind to the active sites of HDAC isoforms and RRM2. Furthermore, PA demonstrated a more favorable interaction with HDAC7, displaying a docking score of -9.633 kcal/mol, as compared to the standard HDAC inhibitor suberoylanilide hydroxamic acid (SAHA), which exhibited a docking score of -8.244 kcal/mol against HDAC7.</p><h3 data-test=\"abstract-sub-heading\">Conclusion</h3><p>The present study emphasizes the prospect of designing a potential 1,10-phenanthroline hydroxamic acid derivative as a novel dual HDAC and RR-inhibiting anti-cancer molecule.</p><h3 data-test=\"abstract-sub-heading\">Graphical Abstract</h3>","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"30 1","pages":""},"PeriodicalIF":3.6,"publicationDate":"2024-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140812827","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
Evaluation of time-to-onset and outcome of cardiac adverse events related to pembrolizumab using post-marketing surveillance in Japanese patients 通过对日本患者进行上市后监测,评估与 Pembrolizumab 相关的心脏不良事件的发生时间和结果
IF 3.6 4区 医学
DARU Journal of Pharmaceutical Sciences Pub Date : 2024-04-26 DOI: 10.1007/s40199-024-00516-z
Yuko Kanbayashi, Eren Tsuchiya, Tadashi Shimizu, Mayako Uchida
{"title":"Evaluation of time-to-onset and outcome of cardiac adverse events related to pembrolizumab using post-marketing surveillance in Japanese patients","authors":"Yuko Kanbayashi, Eren Tsuchiya, Tadashi Shimizu, Mayako Uchida","doi":"10.1007/s40199-024-00516-z","DOIUrl":"https://doi.org/10.1007/s40199-024-00516-z","url":null,"abstract":"<h3 data-test=\"abstract-sub-heading\">Background</h3><p>Pembrolizumab has been widely used in patients since its release, but information on cardiac Adverse Events (AEs) related to pembrolizumab remains lacking, particularly in Japanese populations.</p><h3 data-test=\"abstract-sub-heading\">Objectives</h3><p>This study aims to evaluate time to onset, incidence rates, and outcomes for pembrolizumab-induced cardiac AEs in patients with cancer using the Japanese Adverse Drug Event Report database.</p><h3 data-test=\"abstract-sub-heading\">Methods</h3><p>We analysed data for the period from April 2004 to March 2022. Data on cardiac AEs were extracted and relative risks of AEs were estimated using the reporting odds ratio.</p><h3 data-test=\"abstract-sub-heading\">Results</h3><p>We analysed 2,021,907 reports and identified 15,306 reports of AEs caused by pembrolizumab. Of these, 399 cardiac AEs were associated with pembrolizumab. Signals were detected for six cardiac AEs: myocarditis, immune-mediated myocarditis, pericardial effusion, cardiac tamponade, pericarditis, and pericarditis malignant. A histogram of median times to onset showed occurrence from 33 (21–97) days for immune-mediated myocarditis to 138 (67–168) days for pericarditis malignant, but some cases occurred even more than 1 year after the start of administration. Among these, myocarditis was the most frequently reported (27.1%), with fatal cases also reported.</p><h3 data-test=\"abstract-sub-heading\">Conclusion</h3><p>This study focused on cardiac AEs caused by pembrolizumab as post-marketing AEs. Patients should be monitored not only at the time of administration, but also over time for signs of these AEs, especially myocarditis, as some patients may have serious outcomes.</p><h3 data-test=\"abstract-sub-heading\">Graphical abstract</h3>\u0000","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"14 1","pages":""},"PeriodicalIF":3.6,"publicationDate":"2024-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140804998","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
Microbiological acceptance criteria, specifications of herbal drugs and herbal drug preparations in various pharmacopoeias: a global scenario 各种药典中草药和草药制剂的微生物验收标准和规格:全球情况
IF 3.6 4区 医学
DARU Journal of Pharmaceutical Sciences Pub Date : 2024-04-13 DOI: 10.1007/s40199-024-00510-5
Ramesh Munukuntla, Akhilesh Tiwari, Ravi Shankar Yadav, A. Jayanthy, Subhash Chandra Verma, Raman Mohan Singh
{"title":"Microbiological acceptance criteria, specifications of herbal drugs and herbal drug preparations in various pharmacopoeias: a global scenario","authors":"Ramesh Munukuntla, Akhilesh Tiwari, Ravi Shankar Yadav, A. Jayanthy, Subhash Chandra Verma, Raman Mohan Singh","doi":"10.1007/s40199-024-00510-5","DOIUrl":"https://doi.org/10.1007/s40199-024-00510-5","url":null,"abstract":"<h3 data-test=\"abstract-sub-heading\">Purpose</h3><p>A pharmacopoeia is a compendium of guidelines and criteria for drug quality. It was established by a national or regional entity and has legal significance. This applies to administration of drugs in a particular nation or region.</p><h3 data-test=\"abstract-sub-heading\">Method</h3><p>In this study, the differences and similarities of microbiological acceptance criteria, specifications for microbial enumeration of herbal drugs and herbal drug preparations in 14 national and international pharmacopeias were investigated.</p><h3 data-test=\"abstract-sub-heading\">Results</h3><p>It was found that 12 pharmacopeias have given separate microbial limits for total aerobic microbial count (TAMC) and total yeast and mold count (TYMC), and a list of specified microorganisms for which acceptance criteria are defined. However, similarities were noticed in Ph.Eur, Ph. Helv and, BP. <i>Salmonella, and Escherichia coli</i> are the most common pathogens specified for herbal preparations in which boiling water is added prior to use and for internal use in all Pharmacopoeias because they serve as indicators of potential contamination.</p><h3 data-test=\"abstract-sub-heading\">Conclusion</h3><p>From this study, it can be concluded that the differences in microbial limit tests and their acceptance criteria as specified in the various pharmacopoeias need to be harmonized. It will become a more convenient option for global drug manufacturers to import/export herbal drugs, and this would also eliminate the burden of performing various analytical methods and comply with different microbial acceptance criteria set by various pharmacopoeias. The comparative data obtained from this study will be used to develop strategies for revisions of pharmacopoeias in a harmonized manner with respect to microbiological acceptance criteria, specifications for microbial enumeration of herbal drugs and herbal drug preparations.</p>","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"24 1","pages":""},"PeriodicalIF":3.6,"publicationDate":"2024-04-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140601986","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
Developing an AI-based prediction model for anaphylactic shock from injection drugs using Japanese real-world data and chemical structure-based analysis 利用日本真实世界数据和基于化学结构的分析,开发基于人工智能的注射药物过敏性休克预测模型
IF 3.6 4区 医学
DARU Journal of Pharmaceutical Sciences Pub Date : 2024-04-05 DOI: 10.1007/s40199-024-00511-4
Tomoyuki Enokiya, Kaito Ozaki
{"title":"Developing an AI-based prediction model for anaphylactic shock from injection drugs using Japanese real-world data and chemical structure-based analysis","authors":"Tomoyuki Enokiya, Kaito Ozaki","doi":"10.1007/s40199-024-00511-4","DOIUrl":"https://doi.org/10.1007/s40199-024-00511-4","url":null,"abstract":"<h3 data-test=\"abstract-sub-heading\">Background</h3><p>This study aims to develop an AI-based prediction model for injection drugs that cause anaphylactic shock using Japanese Real-World Data (JADER database) and chemical structure-based analysis.</p><h3 data-test=\"abstract-sub-heading\">Methods</h3><p>Data sourced from the JADER database included adverse drug reaction reports from April 2004 to December 2020. Only drugs with an adverse reaction named \"anaphylactic shock\" were selected for analysis. For model building, various models were constructed to predict anaphylactic shock-inducing drugs, such as logistic regression, LASSO, XGBoost, RF, SVM, and NNW. These models used chemical properties and structural similarities as feature variables. Dimension reduction was applied using principal component analysis. The dataset was split into training (80%) and validation (20%) sets. Six different models were trained and optimized through fivefold cross-validation.</p><h3 data-test=\"abstract-sub-heading\">Results</h3><p>From April 2004 to December 2020, 947 drugs with the adverse reaction name \"anaphylactic shock\" were extracted from the JADER database. 320 drugs were excluded due to analytical challenges, and another 400 were removed due to their administration route. 227 drugs were finalized as target medicines. For model validation, the performance of each model was evaluated based on metrics like AUCs of ROC curve, sensitivity, and specificity. Additionally, two ensemble models, constructed from the six models were assessed using bootstrap sampling. Interestingly, it was identified that mepivacaine structural similarity had the highest importance in the final model.</p><h3 data-test=\"abstract-sub-heading\">Conclusions</h3><p>The study successfully developed an AI-based prediction model for anaphylactic shock inducing-injection drugs. The model would offer potential for drug safety evaluation and anaphylactic shock risk assessment.</p><h3 data-test=\"abstract-sub-heading\">Graphical abstract</h3>\u0000","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"62 1","pages":""},"PeriodicalIF":3.6,"publicationDate":"2024-04-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140585777","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 amide and diterpene alkaloids with anticholinesterase activity from Delphinium cyphoplectrum roots 从 Delphinium cyphoplectrum 根中提取的具有抗胆碱酯酶活性的新酰胺和二萜生物碱
IF 3.6 4区 医学
DARU Journal of Pharmaceutical Sciences Pub Date : 2024-03-18 DOI: 10.1007/s40199-024-00509-y
Arash Salehi, Behzad Zolfaghari, Mahmoud Aghaei, Hajar Sirous, Morteza Sadeghi, Mohammad Reza Gholami, Parham Reisi, Mustafa Ghanadian
{"title":"New amide and diterpene alkaloids with anticholinesterase activity from Delphinium cyphoplectrum roots","authors":"Arash Salehi, Behzad Zolfaghari, Mahmoud Aghaei, Hajar Sirous, Morteza Sadeghi, Mohammad Reza Gholami, Parham Reisi, Mustafa Ghanadian","doi":"10.1007/s40199-024-00509-y","DOIUrl":"https://doi.org/10.1007/s40199-024-00509-y","url":null,"abstract":"&lt;h3 data-test=\"abstract-sub-heading\"&gt;Background&lt;/h3&gt;&lt;p&gt;The cholinergic hypothesis posits a robust correlation between the onset of Alzheimer’s disease and a pronounced deficit in acetylcholine, a pivotal neurotransmitter crucial for the central cholinergic nervous system’s function, pivotal for memory and learning. Diterpene alkaloids exhibit intricate and distinctive chemical structures that facilitate their passage through the blood-brain barrier. Moreover, their potent pharmacological attributes render them promising candidates for addressing central nervous system disorders.&lt;/p&gt;&lt;h3 data-test=\"abstract-sub-heading\"&gt;Objectives&lt;/h3&gt;&lt;p&gt;This investigation aims to scrutinize the alkaloidal composition of &lt;i&gt;Delphinium cyphoplectrum&lt;/i&gt; (Ranunculaceae) roots, further exploring their anticholinesterase inhibitory activity and mode of inhibition.&lt;/p&gt;&lt;h3 data-test=\"abstract-sub-heading\"&gt;Method&lt;/h3&gt;&lt;p&gt;Innovative chromatography techniques were repetitively employed to purify the alkaloids. Acetylcholinesterase (AChE) inhibition assays were conducted using Ellman’s tests. The mode of inhibition was meticulously characterized through Michaelis-Menten, and Lineweaver-Burk plots. Conducting molecular docking studies, we employed the AUTO DOCK 4.2 software package.&lt;/p&gt;&lt;h3 data-test=\"abstract-sub-heading\"&gt;Results&lt;/h3&gt;&lt;p&gt;Eight alkaloids were identified including five C19-diterpene alkaloids (6,14,16,18-tetramethoxy-1,7,8-trihydroxy-4-methylaconitane (&lt;b&gt;1&lt;/b&gt;), 6,16,18-trimethoxy-1,7,8,14-tetrahydroxy-4-methylaconitane (&lt;b&gt;2&lt;/b&gt;), 6,8,16,18-tetramethoxy-1,7,14-trihydroxy-4-methylaconitane (&lt;b&gt;3&lt;/b&gt;), 6,14,16-trimethoxy-1,7,8,18-tetrahydroxy-4-methylaconitane (&lt;b&gt;4&lt;/b&gt;), and 14-&lt;i&gt;O&lt;/i&gt;-acetyl-8,16-dimethoxy-1,6,7,18-tetrahydroxy-4-methylaconitane (&lt;b&gt;5&lt;/b&gt;)), an epoxy C18-diterpene alkaloid (6,8,16-trimethoxy-1,7,14-trihydroxy-3,4-epoxyaconitane (&lt;b&gt;6&lt;/b&gt;)), a known (pyrrolidin-2-one (&lt;b&gt;7&lt;/b&gt;) and an undescribed amide alkaloid (1-(2’-hydroxylethylamine)-3,5,5,-trimethyl-1,5-dihydro-2H-pyrrol-2-one (&lt;b&gt;8&lt;/b&gt;). All diterpene alkaloids underwent assessment for acetylcholinesterase (AChE) inhibition assay and displayed noteworthy AChE activity, surpassing that of the reference drug (with IC&lt;sub&gt;50&lt;/sub&gt; values of 13.7, 21.8, 23.4, 28.2, 40.4, and 23.9 for compounds &lt;b&gt;1&lt;/b&gt;–&lt;b&gt;6&lt;/b&gt;, respectively, in comparison to 98.4 for Rivastigmine). Analysis of Michaelis-Menten and Lineweaver-Burk plots represents an uncompetitive mode of inhibition for compound &lt;b&gt;1&lt;/b&gt; on AChE. Notably, computational docking simulations indicated that all diterpene alkaloids were accommodated within the same enzymatic cleft as the reference ligand, and displaying superior free binding energy values (from − 10.32 to -8.59 Kcal.mol&lt;sup&gt;−1&lt;/sup&gt;) in contrast to Rivastigmine (-6.31 Kcal.mol&lt;sup&gt;−1&lt;/sup&gt;).&lt;/p&gt;&lt;h3 data-test=\"abstract-sub-heading\"&gt;Conclusion&lt;/h3&gt;&lt;p&gt;The phytochemical analysis conducted on the roots of &lt;i&gt;Delphinium cyphoplectrum&lt;/i&gt; yielded the identification of eight alkaloidal co","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"132 1","pages":""},"PeriodicalIF":3.6,"publicationDate":"2024-03-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140156188","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
Development of brimonidine niosomes laden contact lenses for extended release and promising delivery system in glaucoma treatment 开发含溴莫尼定iosomes的隐形眼镜,为青光眼治疗提供缓释和前景广阔的给药系统
IF 3.6 4区 医学
DARU Journal of Pharmaceutical Sciences Pub Date : 2023-12-29 DOI: 10.1007/s40199-023-00500-z
Shresthi Tripathi, Khushwant S. Yadav
{"title":"Development of brimonidine niosomes laden contact lenses for extended release and promising delivery system in glaucoma treatment","authors":"Shresthi Tripathi, Khushwant S. Yadav","doi":"10.1007/s40199-023-00500-z","DOIUrl":"https://doi.org/10.1007/s40199-023-00500-z","url":null,"abstract":"<h3 data-test=\"abstract-sub-heading\">Background</h3><p>Increased intraocular pressure is a common symptom of glaucoma. In severe circumstances, it may result in loss of eyesight. Glaucoma treatment is difficult due to ocular physiological barriers that prevent medications from reaching the afflicted area. Traditional formulations (eye drops) have a short residence period and are rapidly drained away via the nasolacrimal duct, resulting in increased adverse drug responses and lower efficacy. The usage of nanoparticles such as niosomes could be one potential answer to these problems. While niosomes improve drug penetration, they have little effect on ocular retention of the medication. Contact lenses containing niosomes can assist to overcome this disadvantage.</p><h3 data-test=\"abstract-sub-heading\">Objective</h3><p>This study aims to prepare and evaluate Brimonidine niosomes laden contact lenses for the treatment of Glaucoma.</p><h3 data-test=\"abstract-sub-heading\">Methods</h3><p>Brimonidine niosomes were prepared using thin film hydration method and evaluated. The contact lenses were soaked in the niosomal formulation at varying intervals (3–10 days). Thereafter, the contact lenses were evaluated for %transmittance, %swelling index, drug quantification and in vitro drug release. The pharmacodynamic studies were conducted to assess the reduction in intraocular pressure (IOP) in albino rabbits. The research compared the results of the reduction in intraocular pressure caused by Brimonidine niosomes laden contact lenses with a marketed preparation of niosomes.</p><h3 data-test=\"abstract-sub-heading\">Results</h3><p>Higher concentration of the drug was loaded in contact lenses loaded with Brimonidine niosomes compared to the marketed formulation, by soaking method. The contact lenses exhibited an optimal %transmittance of 98.02 ± 0.36 and %swelling index of 50.35 ± 0.57. Increase in the soaking time up to 7 days led to an increase in the drug concentration in the contact lenses. However, no further increase was observed after the 7th day due to saturation of the contact lenses. Brimonidine niosomes laden contact lenses provided a reduction in intraocular pressure that was similar to the marketed preparation. Further, the contact lenses provided extended release up to 20 h.</p><h3 data-test=\"abstract-sub-heading\">Conclusion</h3><p>Brimonidine niosomes laden contact lenses exhibited superior drug loading through the soaking method, displaying optimal %transmittance and %swelling index. Soaking for 7 days increased drug concentration in contact lenses with no further increase due to saturation. These lenses reduced intraocular pressure like the marketed formulation, offering extended release for 20 h.</p><h3 data-test=\"abstract-sub-heading\">Graphical abstract</h3>\u0000","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"132 1","pages":""},"PeriodicalIF":3.6,"publicationDate":"2023-12-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139063358","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
Artificial viruses: A nanotechnology based approach 人造病毒:基于纳米技术的方法
IF 3.6 4区 医学
DARU Journal of Pharmaceutical Sciences Pub Date : 2023-12-18 DOI: 10.1007/s40199-023-00496-6
{"title":"Artificial viruses: A nanotechnology based approach","authors":"","doi":"10.1007/s40199-023-00496-6","DOIUrl":"https://doi.org/10.1007/s40199-023-00496-6","url":null,"abstract":"<h3>Abstract</h3> <span> <h3>Objectives</h3> <p>The main objective of this work was to review and summarise the detailed literature available on viral nanoparticle and the strategies utilised for their manufacture along with their applications as therapeutic agents.</p> </span> <span> <h3>Data acquisition</h3> <p>The reported literature related to development and application of virus nanoparticles have been collected from electronic data bases like ScienceDirect, google scholar, PubMed by using key words like “viral nanoparticles”, “targeted drug delivery” and “vaccines” and related combinations.</p> </span> <span> <h3>Result</h3> <p>From the detailed literature survey, virus nanoparticles were identified as carriers for the targeted delivery. Due to the presence of nanostructures in virus nanoparticles, these protect the drugs from the degradation in the gastrointestinal tract and in case of the delivery of gene medicine, they carry the nucleic acids to the target/susceptible host cells. Thus, artificial viruses are utilised for targeted delivery to specific organ in biomedical and biotechnological areas.</p> </span> <span> <h3>Conclusion</h3> <p>Thus, virus nanoparticles can be considered as viable option as drug/gene carrier in various healthcare sectors especially drug delivery and vaccine and can be explored further in future for the development of better drug delivery techniques.</p> </span> <span> <h3>Graphical Abstract</h3> <p> <span> <span> <img alt=\"\" src=\"https://static-content.springer.com/image/MediaObjects/40199_2023_496_Figa_HTML.png\"/> </span> </span></p> </span>","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"4 1","pages":""},"PeriodicalIF":3.6,"publicationDate":"2023-12-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138717215","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
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