Cardiovascular & hematological agents in medicinal chemistry最新文献

{"title":"WITHDRAWN: Pyridazine Derivatives: Molecular Docking ADMET Prediction and Synthesis for Antihypertensive Activity","authors":"Gagandeep Kaur, Ankur Thakur, Lovish Sharma, Nidhi Rani","doi":"10.2174/0118715257316272240807075752","DOIUrl":"10.2174/0118715257316272240807075752","url":null,"abstract":"<p><p>The article has been withdrawn at the request of the authors of the journal Cardiovascular & Hematological Agents in Medicinal Chemistry.</p><p><p>Bentham Science apologizes to the readers of the journal for any inconvenience this may have caused.</p><p><p>The Bentham Editorial Policy on Article Withdrawal can be found at https://benthamscience.com/editorial-policies-main.php</p><p><strong>Bentham science disclaimer: </strong>It is a condition of publication that manuscripts submitted to this journal have not been published and will not be simultaneously submitted or published elsewhere. Furthermore, any data, illustration, structure or table that has been published elsewhere must be reported, and copyright permission for reproduction must be obtained. Plagiarism is strictly forbidden, and by submitting the article for publication the authors agree that the publishers have the legal right to take appropriate action against the authors, if plagiarism or fabricated information is discovered. By submitting a manuscript the authors agree that the copyright of their article is transferred to the publishers if and when the article is accepted for publication.</p>","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-08-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142006103","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}

{"title":"Correction of Warfarin Coagulopathy for Non-bleeding Patients in the Outpatient Setting at an Ambulatory Care Organization: Application of Vitamin K Guidance.","authors":"Aaminah Khan, David DeiCicchi, Peter Collins, Ashwini Ranade, Kathy Zaiken","doi":"10.2174/0118715257286369240527055010","DOIUrl":"https://doi.org/10.2174/0118715257286369240527055010","url":null,"abstract":"<p><strong>Background: </strong>Warfarin is an effective anticoagulant but requires close International Normalized Ratio (INR) monitoring and may occasionally require correction of excessive anticoagulation. Current guidelines provide limited practical guidance on the administration of vitamin K for the management of supratherapeutic INR levels ≥ 5.0 in non-bleeding outpatients.</p><p><strong>Objective: </strong>Based on expert consensus and guidelines, the Atrius Health Anticoagulation Management Services (AMS) has developed internal guidance for oral vitamin K use in highly selected populations. This study will describe the internal guidance for oral vitamin K use and present associated results and clinical outcomes.</p><p><strong>Methods: </strong>Episodes with INR > 5.0 were included, with vitamin K considered for episodes with INR ≥ 6. Moreover, compelling indications and exclusions to select ideal patients for vitamin K intervention were also defined.</p><p><strong>Results: </strong>Overall, episodes were managed conservatively; of the 246 collected episodes of excessive anticoagulation, in 18 episodes (7%), patients received vitamin K, and in 228 (93%) episodes, patients did not receive vitamin K. The mean index INR was 6.0 (range 5.0 - 10.5, SD 1.07), with nearly 57% of episodes achieving INR correction and 15% of episodes developing INR overcorrection. High thrombotic risk patients, regardless of hemorrhagic risk, were less likely to receive vitamin K. Three episodes (1.2%) resulted in bleeding complications. No thrombotic complications occurred during the 30-day follow-up of the index INR value ≥ 5.0.</p><p><strong>Conclusion: </strong>Our internal guidance is a novel, standardized approach that serves as a decision support tool for the management of warfarin-associated coagulopathy and vitamin K intervention using patient-specific characteristics and index INR values. This guidance may assist other anticoagulation management services with practical applications and require validation in a prospective clinical trial.</p>","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-06-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141285611","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}

{"title":"Sildenafil Effect on Atrial Natriuretic Peptide Level in Pulmonary Hypertensive Rats.","authors":"Mukhallad A Aljanabi, Nasr Alrabadi, Sahar H Mahmoud, Razan Haddad, Karem H Alzoubi","doi":"10.2174/0118715257293794240516075211","DOIUrl":"https://doi.org/10.2174/0118715257293794240516075211","url":null,"abstract":"<p><strong>Background: </strong>Pulmonary Hypertension (PH) leads to changes in pulmonary vascular architecture, hypertrophy of the right ventricle, and heart failure. Sildenafil is a drug that can modulate PH by inducing smooth muscle relaxation and vasodilation.</p><p><strong>Aims: </strong>To investigate the ability of sildenafil to alleviate the monocritaline (MCT)-induced PH in rats and to estimate the role and its effect on the atrial natriuretic peptide (ANP) levels.</p><p><strong>Methods: </strong>28 adult male rats were divided randomly into four groups: Group A (control group; n=7). Group B (MCT-treated group; n=7) was given a single dose of MCT 60 mg/kg subcutaneously. Group C (The reversal group; n=7) received a single dose of MCT 60 mg/kg subcutaneously for three weeks and then sildenafil at 50 mg/kg/day, given daily for another three weeks. Group D (The prevention group; n=7) simultaneously received a single dose of MCT 60 mg/kg subcutaneously and sildenafil daily at 50 mg/kg for three weeks.</p><p><strong>Results: </strong>The animals in the prevention group showed a significant decrease in ANP levels compared to the reversal and MCT-treated groups. This decrease was associated with a significant reduction in the Fulton index ratio in the prevention group compared to the reversal group. The nitric oxide levels were also significantly higher in the reversal group than in the control group.</p><p><strong>Conclusion: </strong>Preventive sildenafil treatment was associated with a significant decrease in ANP levels and reduced MCT-induced cardiac hypertrophy in rats.</p>","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141156037","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}

{"title":"Mavacamten: A Review of a Novel Therapeutic Approach for Hypertrophic Cardiomyopathy.","authors":"Ayesha Abdul Qadir Memon, Areeba Shamim, Sanoober Mirza, Muhammad Osama, Iyad Naeem Muhammad, Calvin R Wei","doi":"10.2174/0118715257283752240325082733","DOIUrl":"https://doi.org/10.2174/0118715257283752240325082733","url":null,"abstract":"Hypertrophic Cardiomyopathy (HCM) is a heart disease that can cause left ventricular hypertrophy, arrhythmias, heart failure, and sudden cardiac death. Currently, pharmacological treatment is limited and ineffective. Mavacamten (CamzyosTM) is a cardiac myosin inhibitor developed as a therapeutic option to reduce myocardial contractility and restoration of myocardial function. The Food and Drug Administration (FDA) approved the use of Mavacamten in 2022 for HCM symptoms. Clinical studies have proven that Mavacamten can reduce Left Ventricular Outflow Tract (LVOT) involvement, cardiac hypercontraction, and hypertrophy. This review provides an overview of HCM, its pathophysiology, current treatments, synthesis of Mavacamten, and the clinical trials of Mavacamten.","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":"8 4","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-04-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140739047","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}

{"title":"Redox-signalling and Redox Biomarkers in Cardiovascular Health and Disease.","authors":"Yasmin Sultana, Damanpreet Kaur Lang, Thomson Santosh Alex, Rakhi Khabiya, Akanksha Dwivedi, Saikat Sen, Raja Chakraborty","doi":"10.2174/0118715257282030240130095754","DOIUrl":"https://doi.org/10.2174/0118715257282030240130095754","url":null,"abstract":"<p><p>Overproduction of reactive nitrogen and oxygen species (RNS and ROS) has been linked to the pathogenesis of diabetes, hypertension, hyperlipidemia, stroke, angina, and other cardiovascular diseases. These species are produced in part by the mitochondrial respiratory chain, NADPH oxidase, and xanthine oxidase. RNS and ROS both contribute to oxidative stress, which is necessary for the development of cardiovascular disorders. In addition to ROS species like hydroxyl ion, hydrogen peroxide, and superoxide anion, RNS species like nitric oxide, peroxynitrous acid, peroxynitrite, and nitrogen dioxide radicals have also been linked to a number of cardiovascular conditions. They promote endothelial dysfunction, vascular inflammation, lipid peroxidation, and oxidative damage, all of which contribute to the development of cardiovascular pathologies. It's crucial to understand the mechanisms that result in the production of RNS and ROS in order to identify potential therapeutic targets. Redox biomarkers serve as indicators of oxidative stress, making them crucial tools for diagnosing and predicting cardiovascular states. The advancements in proteomics, metabolomics, genomics, and transcriptomics have made the identification and detection of these small molecules possible. The following redox biomarkers are notable examples: 3-nitrotyrosine, 4-hydroxy-2-nonenal, 8- iso-prostaglandin F2, 8-hydroxy-2-deoxyguanosine, malondialdehyde, Diacron reactive oxygen metabolites, total thiol, and specific microRNAs (e.g. miRNA199, miRNA21, miRNA1254, miRNA1306-5p, miRNA26b-5p, and miRNA660-5p) are examples. Although redox biomarkers have great potential, their clinical applicability faces challenges. Redox biomarkers frequently have a short half-life and exist in small quantities in the blood, making them challenging to identify and measure. The interpretation of biomarker data may also be influenced by confounding factors and the complex interplay of various oxidative stress pathways. Therefore, in-depth validation studies and the development of sensitive and precise detection methods are needed to address these problems. In the search for redox biomarkers, cutting-edge techniques like mass spectrometry, immunoassays, and molecular diagnostics are applied. New platforms and technologies have made it possible to accurately detect and monitor redox biomarkers, which facilitates their use in clinical settings. Our expanding knowledge of RNS and ROS involvement in cardiovascular disorders has made it possible to develop redox biomarkers as diagnostic and prognostic tools. Overcoming the challenges associated with their utility and utilizing advanced detection techniques, which will improve their clinical applicability, will ultimately benefit the management and treatment of cardiovascular conditions.</p>","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140320123","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}

{"title":"Effect of Syzygium cumini on Oxidative Stress Induced Cardiac Cellular Anomalies.","authors":"Renu Bhadana, Vibha Rani","doi":"10.2174/0118715257273859231211112731","DOIUrl":"https://doi.org/10.2174/0118715257273859231211112731","url":null,"abstract":"<p><strong>Introduction: </strong>Doxorubicin (Dox), an antineoplastic agent is used as a primary anticancerous drug against various types of cancers. However, its associated toxicity to the cardiovascular system is major. Literature has recorded the cases of mortality due to poor validation and lack of prediagnosis of Dox-induced cardiotoxicity. Therapeutic interventions using natural products having cardioprotective properties with low toxic outcomes hold therapeutic potential for future cardio-oncological therapies. Syzygium cumini (Black berry), a traditional Indian herbal plant, has been researched and found to exert cardioprotective, anti-inflammatory, and antioxidant activities, which have been credited due to the presence of polyphenols, flavonoids, and tannins.</p><p><strong>Methods: </strong>In the current research, we investigated the cardioprotective potential of Syzygium cumini against Doxorubicin-induced cardiotoxicity (DIC) in H9C2 cardiomyocytes. Methanolic seed extract preparation of Syzygium cumini was performed using the Soxhlet apparatus. Cell viability and cell death assays were performed to determine the cardiotoxic doses of Doxorubicin. Furthermore, the cardioprotective potential of Syzygium cumini extract against DIC was studied. Morphological and nuclear alterations in H9C2 cells were studied by microscopic assays using Giemsa, Haematoxylin-Eosin stain, and PI. The intracellular stress level and ROS production were studied using DCFH-DA followed by mitochondrial integrity analysis using fluorescent microscopic methods.</p><p><strong>Results: </strong>In the results, we investigated that Dox exerted a dose and time-dependent cardiotoxicity on H9C2 cardiomyocytes. Moreover, we observed that morphological and nuclear alterations caused by doxorubicin in dose-dependent manner were prevented by supplementing with Syzygium cumini polyphenols and it attenuated the oxidative stress in H9C2 cardiomyocytes effectively.</p><p><strong>Conclusion: </strong>Conclusively, Syzygium cumini possesses cardioprotective potential in H9C2 cardiomyocytes in dox-induced cardiotoxicity.</p>","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139652443","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}

{"title":"Early Prognostic Instrumental and Laboratory Biomarkers in Post-MI.","authors":"Basheer Abdullah Marzoog","doi":"10.2174/0118715257281715240108092557","DOIUrl":"https://doi.org/10.2174/0118715257281715240108092557","url":null,"abstract":"<p><strong>Background: </strong>Post-myocardial infarction (MI) changes have been frequently reported in the literature and are associated with determining the prognosis.</p><p><strong>Aims: </strong>The aim of this study is to find a prognosis marker for the favorability of determination of the medium-term outcomes in patients with acute MI.</p><p><strong>Objectives: </strong>MI patients' prognosis is poorly understood and requires further elaboration.</p><p><strong>Materials and methods: </strong>A single center, cross-sectional cohort study involved 211 patients' medical history with acute MI, for the period 2014-2019, had been evaluated retrospectively for 76 parameters. The data was collected from the Republic Rehabilitation Mordovian Hospital. The described measurement units were used in the local laboratories to describe the values. The descriptive values were expressed in the mean average and standard deviation. For statistical analysis, descriptive statistics, t-test independent by groups and dependent by numerical variables for repeated analysis for the same patients, multinomial logistic regression, Pearson's correlation coefficient, ROC analysis, and for clarification purposes, diagrams and bar figures were used. For performing the statistical analysis, the SPSS program, version 28 was used.</p><p><strong>Results: </strong>Descriptive statistics showed a proportion of men to females 7:3. The mean age of the MI patients was 61.50 years (Std. Dev. ± 10.68), and the mean height of the sample was 171.00 cm (Std. Dev. ± 7.20). The mean body weight of the sample is 83.62 kg (Std. Dev. ± 12.35), and the body mass index (BMI) is 29.02 kg/m2 (Std. Dev. ± 5.07). The total hospitalization days are 14.79 (Std. Dev. ± 3.41). The mean heart rate (HR) beat per minute (bpm) was 79.03 (Std. Dev. ± 15.63), and the mean blood pressure was 138.53/84.09 mmHg (Std. Dev. ± 28.66/12.79). On the complete blood count (CBC), the mean level of the hemoglobin (Hb) 136.33 g/l (Std. Dev. ± 15.29), the mean level of the leukocytes (WBC) 8.76 /μl (Std. Dev. ± 2.77), the mean level of the red blood cells (RBC) 4.55 /μl (Std. Dev. ± 0.52), the mean level of the relative value of the lymphocytes 24.46 % (Std. Dev. ± 9.015), and the mean level of the thrombocytes 207.87 /μl (Std. Dev. ± 64.035). The mean erythrocytes segmentation rate (ESR) is 18.99 mm/hr (Std. Dev. ± 12.16). The regression analysis demonstrated that the dependent variable, complication, in particular, pericarditis, and the independent factor, concomitant disease, in particular, chronic heart failure, has a significant regression coefficient of 29.101 at p <0.05. Furthermore, the dependent variable, complication, in particular, pneumonitis, and the independent factor, concomitant disease, particularly, arrhythmia, have a significant regression coefficient of 21.937 at p <0.05.</p><p><strong>Conclusion: </strong>An elevated level of CPK-MB/LDH/Troponin I is linked to the development of arrhythmia. Patient","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139577138","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}

{"title":"The Genus Anabasis: A Review on Pharmacological and Phytochemical Properties.","authors":"Smail Amtaghri, Miloudia Slaoui, Mohamed Eddouks","doi":"10.2174/0118715257276051240111060414","DOIUrl":"https://doi.org/10.2174/0118715257276051240111060414","url":null,"abstract":"<p><p>The genus Anabasis has long been used in phytomedicine. The studied parts of Anabasis species are used as antirheumatic, diuretic, antidotes against poison, anti-erosion, anti-ulcer, and antidiabetic agents, as well as against headache and skin diseases. The objective of the present review was to summarize the phytochemical and pharmacological aspects related to the genus Anabasis. The results of this literature analysis show that among all the species of the Anabasis (A) family, A. aphylla, A. Iranica, A. aretioides, and A. articulata showed antibacterial activity; A. aretioides and A. articulata have antioxidant activity, A. aretioides and A. articulata have antidiabetic activity, A. articulata has cytotoxic activity and A. setifera, A. aretioides, and A. articulata exhibit anti-inflammatory activity. The Anabasis genus contains saponins, and alkaloids, such as anabasine, anabasamine, lupinine, jaxartinine, and triterpenic sapogenins. The study of 15 Anabasis plants has identified 70 compounds with an array of pharmacological activities especially antibacterial, antioxidant, antidiabetic, cytotoxic, and anti-inflammatory activities. However, there is a need for further studies on Anabasis plants before they can be fully used clinically as a potential drug.</p>","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139522225","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}

{"title":"A Three-year Retrospective Study Looking at Preventing Hospital Acquired Thrombosis.","authors":"Vipin Kammath, Anuj Gupta, Alexander Bald, Gavin Hope, Nisheeth Kansal, Ahmad Al Samaraee, Vish Bhattacharya","doi":"10.2174/0118715257269027231228114930","DOIUrl":"10.2174/0118715257269027231228114930","url":null,"abstract":"<p><strong>Background: </strong>Hospital-acquired venous thromboembolism (HA-VTE) is defined as cases of venous thromboembolism (VTE) that occur in a hospital and within ninety days of a hospital admission. Deep vein thromboses (DVTs) most commonly occur within the deep veins of the pelvis and legs. If the thrombus dislodges and travels to the lungs, it can result in a pulmonary embolus (PE). VTE is associated with significant morbidity and mortality, accounting for almost 10% of all hospital deaths. If risk factors are correctly identified and VTE prophylaxis is prescribed, VTE can be a preventable condition. In 2010, NHS England launched The National Venous Thromboembolism Prevention Programme. This included NICE guidance, and a VTE risk assessment tool, which must be completed for at least 95% of patients on admission. The National Thrombosis Survey, published by Thrombosis UK, studied how this program was implemented locally, and audited HA-VTE prevention strategies nationally.</p><p><strong>Objectives: </strong>Using the Thrombosis Survey and NICE guidance as an aide, this study collects data about hospital-acquired DVT (HA-DVT) at the Queen Elizabeth Hospital in Gateshead (QEH) and aims to: 1. Identify cases of HA-DVT and understand the clinical circumstances surrounding these cases 2. Assess the quality of VTE preventative measures at QEH 3. Outline potential improvement in reducing the incidence of HA-VTE at this hospital Methods: This retrospective cohort study used electronic records to identify all cases of DVT between April 2019 and April 2022 at QEH. Cases of HA-DVT were defined as: a positive ultrasound doppler report and either the case occurring in the 90 days following an inpatient stay, or beyond two days into an admission. For these cases of HA-DVT, we recorded the: reason for admission; admitting specialty; presence of an underlying active cancer and deaths occurring within 90 days of diagnosis. We assessed the quality of VTE preventative measures, by recording the: completion of VTE risk assessments; prescription of weight-adjusted pharmacological VTE prophylaxis and provision of VTE prophylaxis on discharge. For HA-DVT cases occurring within 90 days of an inpatient stay, the preventative measures were assessed on the original admission. Electronic records were used to record the completion rate of the National VTE risk assessment tool for all inpatients during this time frame.</p><p><strong>Results: </strong>The VTE risk assessment tool was completed for 98.5% of all admissions. One hundred and thirty-five cases of HA-DVT were identified between April 2019 and April 2022. Sixteen patients with HA-DVT did not have VTE prophylaxis prescribed on admission. Eleven of these patients had a clearly documented reason why anticoagulation was avoided. In HA-DVT cases where pharmacological VTE prophylaxis was prescribed, 23% were prescribed an inappropriate dose for their weight. If anticoagulation was required on discharge, this was p","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":" ","pages":"212-222"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139577135","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}

{"title":"Anti-angiogenic Potential of Trans-chalcone in an <i>In Vivo</i> Chick Chorioallantoic Membrane Model: An ATP Antagonist to VEGFR with Predicted Blood-brain Barrier Permeability.","authors":"Anna Senrung, Tanya Tripathi, Nikita Aggarwal, Divya Janjua, Arun Chhokar, Joni Yadav, Apoorva Chaudhary, Kulbhushan Thakur, Tejveer Singh, Alok Chandra Bharti","doi":"10.2174/0118715257250417231019102501","DOIUrl":"10.2174/0118715257250417231019102501","url":null,"abstract":"<p><strong>Background: </strong>Glioblastoma multiforme (GBM) is characterized by massive tumorinduced angiogenesis aiding tumorigenesis. Vascular endothelial growth factor A (VEGF-A) via VEGF receptor 2 (VEGFR-2) constitutes majorly to drive this process. Putting a halt to tumordriven angiogenesis is a major clinical challenge, and the blood-brain barrier (BBB) is the prime bottleneck in GBM treatment. Several phytochemicals show promising antiangiogenic activity across different models, but their ability to cross BBB remains unexplored.</p><p><strong>Methods: </strong>We screened over 99 phytochemicals having anti-angiogenic properties reported in the literature and evaluated them for their BBB permeability, molecular interaction with VEGFR-2 domains, ECD2-3 (extracellular domains 2-3) and TKD (tyrosine kinase domain) at VEGF-A and ATP binding site, cell membrane permeability, and hepatotoxicity using <i>in silico</i> tools. Furthermore, the anti-angiogenic activity of predicted lead Trans-Chalcone (TC) was evaluated in the chick chorioallantoic membrane.</p><p><strong>Results: </strong>Out of 99 phytochemicals, 35 showed an efficient ability to cross BBB with a probability score of > 0.8. Docking studies revealed 30 phytochemicals crossing benchmark binding affinity < -6.4 kcal/mol of TKD with the native ligand ATP alone. Out of 30 phytochemicals, 12 showed moderate to low hepatotoxicity, and 5 showed a violation of Lipinski's rule of five. Our <i>in silico</i> analysis predicted TC as a BBB permeable anti-angiogenic compound for use in GBM therapy. TC reduced vascularization in the CAM model, which was associated with the downregulation of VEGFR-2 transcript expression.</p><p><strong>Conclusion: </strong>The present study showed TC to possess anti-angiogenic potential <i>via</i> the inhibition of VEGFR-2. In addition, the study predicted TC to cross BBB as well as a safe alternative for GBM therapy, which needs further investigation.</p>","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":" ","pages":"187-211"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71490018","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}