Drug Target Insights最新文献

{"title":"In vivo analgesic, anti-inflammatory, sedative, muscle relaxant activities, and docking studies of 3',4',7,8-tetrahydroxy-3-methoxyflavone isolated from <i>Pistacia chinensis</i>.","authors":"Abdur Rauf, Umer Rashid, Najla Al Masoud, Zuneera Akram, Anees Saeed, Naveed Muhammad, Taghrid S Alomar, Saima Naz, Marcello Iriti","doi":"10.33393/dti.2024.2745","DOIUrl":"10.33393/dti.2024.2745","url":null,"abstract":"<p><strong>Background: </strong><i>Pistacia chinensis</i> is extensively employed in traditional medicine. This study aimed to isolate and evaluate the therapeutic effects of 3'4'78-tetrahydroxy-3-methoxyflavone from <i>P. chinensis</i> crude extract.</p><p><strong>Materials and methods: </strong>The study utilized column chromatography for isolation. The plant extract and its isolated compound were assessed for in vivo analgesic (hot plate model), anti-inflammatory (carrageenan-induced paw edema), sedative (open field model), and muscle relaxing properties (inclined plane and traction test).</p><p><strong>Results: </strong>In the thermal-induced analgesic model, a significant analgesic effect was observed for the extract (25, 50, and 100 mg/kg) and the isolated compound (2.5, 5, 10, and 15 mg/kg) at higher doses. The extract (100 mg/kg) significantly prolonged latency time (21.98 seconds) after 120 minutes of administration. The isolated compound elevated the latency time (20.03 seconds) after 30 minutes, remaining significant up to 120 minutes with a latency time of 24.11 seconds. The anti-inflammatory effect showed a reduction in inflammatory reactions by 50.23% (extract) and 67.09% (compound) after the fifth hour of treatment. Both samples demonstrated significant sedative effects, with the extract hindering movement by 54.11 lines crossed compared to the negative control (180.99 lines). The isolated compound reduced the number of lines crossed to 15.23±SEM compared to the negative control. Both samples were also significant muscle relaxants. Docking studies indicated that the compound's therapeutic effect is due to inhibiting COX and nociceptive pathways.</p><p><strong>Conclusion: </strong>The isolated compound from <i>Pistacia chinensis</i> exhibits significant analgesic, anti-inflammatory, sedative, and muscle relaxing properties, with potential therapeutic applications by inhibiting COX and nociceptive pathways.</p>","PeriodicalId":11326,"journal":{"name":"Drug Target Insights","volume":"18 ","pages":"47-53"},"PeriodicalIF":2.0,"publicationDate":"2024-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11188735/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141431594","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Molecular targets and therapeutic potential of baicalein: a review.","authors":"Kavita Munjal, Yash Goel, Vinod Kumar Gauttam, Hitesh Chopra, Madhav Singla, Smriti, Saurabh Gupta, Rohit Sharma","doi":"10.33393/dti.2024.2707","DOIUrl":"10.33393/dti.2024.2707","url":null,"abstract":"<p><strong>Aim: </strong>Researchers using herbs and natural products to find new drugs often prefer flavonoids because of their potential as antioxidants and anti-inflammatories. The planned review addressed baicalein research findings in detail. This manuscript provides a complete review of baicalein's potential pharmacological effects along with several molecular targets for better understanding of its therapeutic activities.</p><p><strong>Materials and methods: </strong>We targeted the review on in vitro and in vivo studies reported on baicalein. For this, the literature is gathered from the database available on search engines like PubMed, ScienceDirect, Scopus, and Google Scholar up to 21 December 2023. The keywords \"<i>Scutellaria baicalensis</i>\", \"<i>Oroxylum indicum</i>\", \"<i>Neuroprotective</i>\", \"<i>Cardioprotective</i>\", \"<i>Toxicity studies</i>\", and \"<i>Baicalein</i>\" were used to fetch the content.</p><p><strong>Results: </strong>Baicalein's molecular receptor binding approach has shown anticancer, antidiabetic, antimicrobial, antiaging, neuroprotective, cardioprotective, respiratory protective, gastroprotective, hepatic protective, and renal protective effects. The synergistic effects of this drug with other selective herbs are also contributed towards significant therapeutic potential.</p><p><strong>Conclusion: </strong>This systematic review article from a contemporary and scientific perspective offers fresh insight into <i>S. baicalensis</i>, <i>O. indicum</i>, and its bioactive component baicalein as a potential complementary medicine. Baicalein may be transformed into more efficacious and acceptable evidence-based medicine. However, we recommend more clinical and mechanistic approaches to confirm safety and efficacy of baicalein.</p>","PeriodicalId":11326,"journal":{"name":"Drug Target Insights","volume":"18 ","pages":"30-46"},"PeriodicalIF":2.7,"publicationDate":"2024-06-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11168303/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141317155","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"RBD mutations at the residues K417, E484, N501 reduced immunoreactivity with antisera from vaccinated and COVID-19 recovered patients.","authors":"Dablu Lal Gupta, Jhasketan Meher, Anjan Kumar Giri, Arvind K Shukla, Eli Mohapatra, Manisha M Ruikar, D N Rao","doi":"10.33393/dti.2024.3059","DOIUrl":"10.33393/dti.2024.3059","url":null,"abstract":"<p><strong>Introduction: </strong>It is unclear whether induced spike protein-specific antibodies due to infections with SARS-CoV-2 or to the prototypic Wuhan isolate-based vaccination can immune-react with the emerging variants of SARS-CoV-2.</p><p><strong>Aim/objectives: </strong>The main objective of the study was to measure the immunoreactivity of induced antibodies postvaccination with Covishield™ (ChAdOx1 nCoV-19 coronavirus vaccines) or infections with SARS-CoV-2 by using selected peptides of the spike protein of wild type and variants of SARS-CoV-2.</p><p><strong>Methodology: </strong>Thirty patients who had recovered from SARS-CoV-2 infections and 30 individuals vaccinated with both doses of Covishield™ were recruited for the study. Venous blood samples (5 mL) were collected at a single time point from patients within 3-4 weeks of recovery from SARS-CoV-2 infections or receiving both doses of Covishield™ vaccines. The serum levels of total immunoglobulin were measured in both study groups. A total of 12 peptides of 10 to 24 amino acids length spanning to the receptor-binding domain (RBD) of wild type of SARS-CoV-2 and their variants were synthesized. The serum levels of immune-reactive antibodies were measured using these peptides.</p><p><strong>Results: </strong>The serum levels of total antibodies were found to be significantly (p<0.001) higher in the vaccinated individuals as compared to COVID-19 recovered patients. Our study reported that the mutations in the RBD at the residues K417, E484, and N501 have been associated with reduced immunoreactivity with anti-sera of vaccinated people and COVID-19 recovered patients.</p><p><strong>Conclusion: </strong>The amino acid substitutions at the RBD of SARS-CoV-2 have been associated with a higher potential to escape the humoral immune response.</p>","PeriodicalId":11326,"journal":{"name":"Drug Target Insights","volume":"18 ","pages":"20-26"},"PeriodicalIF":2.7,"publicationDate":"2024-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11163369/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141300360","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Tuberculosis research: Quo vadis.","authors":"Nerges F Mistry","doi":"10.33393/dti.2024.3076","DOIUrl":"10.33393/dti.2024.3076","url":null,"abstract":"","PeriodicalId":11326,"journal":{"name":"Drug Target Insights","volume":"18 ","pages":"27-29"},"PeriodicalIF":2.7,"publicationDate":"2024-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11149609/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141247629","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The dark side of drug repurposing. From clinical trial challenges to antimicrobial resistance: analysis based on three major fields.","authors":"Iyad Y Natsheh, Majd M Alsaleh, Ahmad K Alkhawaldeh, Duaa K Albadawi, Maisa' M Darwish, Mohammed Jamal A Shammout","doi":"10.33393/dti.2024.3019","DOIUrl":"10.33393/dti.2024.3019","url":null,"abstract":"<p><p>Drug repurposing is a strategic endeavor that entails the identification of novel therapeutic applications for pharmaceuticals that are already available in the market. Despite the advantageous nature of implementing this particular strategy owing to its cost-effectiveness and efficiency in reducing the time required for the drug discovery process, it is essential to bear in mind that there are various factors that must be meticulously considered and taken into account. Up to this point, there has been a noticeable absence of comprehensive analyses that shed light on the limitations of repurposing drugs. The primary aim of this review is to conduct a thorough illustration of the various challenges that arise when contemplating drug repurposing from a clinical perspective in three major fields-cardiovascular, cancer, and diabetes-and to further underscore the potential risks associated with the emergence of antimicrobial resistance (AMR) when employing repurposed antibiotics for the treatment of noninfectious and infectious diseases. The process of developing repurposed medications necessitates the application of creativity and innovation in designing the development program, as the body of evidence may differ for each specific case. In order to effectively repurpose drugs, it is crucial to consider the clinical implications and potential drawbacks that may arise during this process. By comprehensively analyzing these challenges, we can attain a deeper comprehension of the intricacies involved in drug repurposing, which will ultimately lead to the development of more efficacious and safe therapeutic approaches.</p>","PeriodicalId":11326,"journal":{"name":"Drug Target Insights","volume":"18 ","pages":"8-19"},"PeriodicalIF":2.7,"publicationDate":"2024-05-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11094707/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140944204","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Long-term response with the atypical reaction to nivolumab in microsatellite stability metastatic colorectal cancer: A case report.","authors":"Nataliya Babyshkina, Nataliya Popova, Evgeny Grigoryev, Tatyana Dronova, Polina Gervas, Alexey Dobrodeev, Dmitry Kostromitskiy, Victor Goldberg, Sergey Afanasiev, Nadejda Cherdyntseva","doi":"10.33393/dti.2024.2637","DOIUrl":"10.33393/dti.2024.2637","url":null,"abstract":"<p><p>Immunotherapy has become an integral part of a comprehensive treatment approach to metastatic colorectal cancer (mCRC). Nivolumab (Opdivo) is a human immunoglobulin G4 monoclonal antibody that blocks the interaction between the programmed cell death 1 (PD-1) receptor and its ligands 1/2 (PD-L1/PD-L2), leading to inhibition of T-cell proliferation, cytokine secretion, and enhanced immune response. The US Food and Drug Administration (FDA) has approved this drug for use in high microsatellite instability (MSI-high)/deficiencies in mismatch repair (dMMR) advanced CRC patients. However, its efficacy is extremely limited in microsatellite stability (MSS)/mismatch repair proficient (pMMR) patients. We report a case of a 42-year-old man diagnosed with MSS/pMMR mCRC who has achieved a durable response to nivolumab after a progression under chemotherapy with antiangiogenic treatment. We observed for the first time an atypical response after 8 months of nivolumab treatment, with the regression of previous primary pulmonary lesions and the presence of new para-aortic lymph node lesions. This report demonstrates that a subset of pretreated mCRC patients with the MSS/pMMR phenotype may benefit from nivolumab and these patients need more attention.</p>","PeriodicalId":11326,"journal":{"name":"Drug Target Insights","volume":"18 ","pages":"4-7"},"PeriodicalIF":2.7,"publicationDate":"2024-01-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10813188/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139569111","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Evaluation of non-conformities in the drafting of bulletins for urine cytobacteriological examinations at Sikasso Hospital (Mali).","authors":"Luka Diarra, Moussa Mariko, Salif Traore, Safi Bazi Dicko, Aboudou Dolo, Moussa Coulibaly, Daouda Sidibé, Moumouni Daou, Hachimi Poma, Madou Traore, Ibrahim Guindo","doi":"10.33393/dti.2024.2670","DOIUrl":"10.33393/dti.2024.2670","url":null,"abstract":"<p><strong>Background: </strong>Non-compliance in the drafting of examination bulletins makes it difficult to perform them and interpret the results. With the aim of continuously improving laboratory services and guaranteeing the quality of urine cytobacteriological examination (ECBU) results, we initiated this study to evaluate non-compliance in the drafting of ECBU reports.</p><p><strong>Materials and methods: </strong>This was a retrospective descriptive cross-sectional study which focused on non-compliance in the drafting of ECBU reports analysed in the laboratory from January to December 2022.</p><p><strong>Results: </strong>During the study period, we collected 383 non-compliant ECBU reports out of 672, with a frequency of 56.99%. Non-compliances were related to age (2.68%), profession (24.40%), clinical information (6.70%) and residence (52.08%). The majority of non-compliant reports came from the medicine (35.51%) and urology (25.85%) departments.</p><p><strong>Conclusion: </strong>The high frequency of non-compliance is a cause for concern and is of concern to all prescribers in this hospital.</p>","PeriodicalId":11326,"journal":{"name":"Drug Target Insights","volume":"18 ","pages":"1-3"},"PeriodicalIF":2.7,"publicationDate":"2024-01-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10792388/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139490633","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Management of urinary tract infections in the era of antimicrobial resistance.","authors":"Ria Pothoven","doi":"10.33393/dti.2023.2660","DOIUrl":"https://doi.org/10.33393/dti.2023.2660","url":null,"abstract":"<p><p>Urinary tract infections (UTIs) are among the most common infections globally, imposing a substantial personal and economic burden on individuals and health resources. Despite international health concerns and sustained public awareness campaigns about the emergence of resistant microorganisms through the inappropriate therapeutic use of antimicrobial agents, the problem of antimicrobial resistance (AMR) is worsening, and AMR in UTIs represents a critical global healthcare issue. This narrative review summarizes evidence-based scientific material, recommendations from the current medical literature, and the latest clinical guidelines on antibiotic and antibiotic-sparing strategies for managing urological infections, including practical approaches to improve the management of patients with acute and recurrent UTIs (rUTIs) in routine clinical practice. Novel emerging therapies and prophylaxis options are described as potential alternatives to overcome the abuse and overuse of antibiotics and the practical application of the guideline recommendations and issues relating to best practice in managing UTIs.</p>","PeriodicalId":11326,"journal":{"name":"Drug Target Insights","volume":"17 ","pages":"126-137"},"PeriodicalIF":2.7,"publicationDate":"2023-12-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10731245/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138828676","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Mortality rate and factors associated with mortality of carbapenem-resistant Enterobacteriaceae infection","authors":"Apichart So-ngern, Naphol Osaithai, Atibordee Meesing, Worawat Chumpangern","doi":"10.33393/dti.2023.2622","DOIUrl":"https://doi.org/10.33393/dti.2023.2622","url":null,"abstract":"Background: Carbapenem-resistant Enterobacteriaceae (CRE) is a serious pathogen with high mortality. Recognition of factors associated with mortality and treating these modifiable factors are crucial to reducing mortality.Objective: To determine the 30-day mortality and factors associated with a 30-day mortality of CRE infection.Methods: A retrospective cohort study was conducted between January 1, 2015, and December 31, 2019. All patients diagnosed with CRE infection aged ≥18 years were included. Multivariate logistic regression was used for evaluating the factors associated with 30-day mortality and presented as adjusted odds ratio (aOR) with 95% confidence interval (CI).Result: One hundred and ninety-four patients were enrolled. The 30-day mortality occurred in 75 patients (38.7%). The common antibiotic regimen was monotherapy and combination of carbapenem, colistin, amikacin, tigecycline, and fosfomycin. CRE isolates were susceptible to tigecycline (93.8%), colistin (91.8%), fosfomycin (89.2%), and amikacin (89.2%). The independent factors associated with 30-day mortality were an increasing simplified acute physiology (SAP) II score (aOR 1.11, 95% CI 1.05-1.16, p < 0.001), sepsis at time of CRE infection diagnosis (aOR 7.93, 95% CI 2.21-28.51, p = 0.002), pneumonia (aOR 4.48, 95% CI 1.61-12.44, p = 0.004), monotherapy (aOR 4.69, 95% CI 1.71-12.85, p = 0.003), and improper empiric antibiotic (aOR 5.13, 95% CI 1.83-14.40, p = 0.002).Conclusion: The overall 30-day mortality of CRE infection was high. The factors associated with mortality were an increasing SAP II score, sepsis at time of CRE infection diagnosis, pneumonia, monotherapy, and improper empiric antibiotic. The study suggested that proper empiric antibiotic and combination antibiotics might reduce mortality from CRE infection.","PeriodicalId":11326,"journal":{"name":"Drug Target Insights","volume":"431 ","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136104057","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":"Prevalence of antibiotic misuse in cases of pneumonia and diarrhea in Saudi Arabia.","authors":"Ebtehaj Saud Almughais,&nbsp;Fatmah Fahad Alreshidi,&nbsp;Hussain Gadelkarim Ahmed","doi":"10.33393/dti.2023.2614","DOIUrl":"10.33393/dti.2023.2614","url":null,"abstract":"<p><strong>Background: </strong>Antibiotic misuse is a major public health issue with long-term repercussions.</p><p><strong>Objective: </strong>The purpose of this investigation was to evaluate the effects of pneumonia and diarrhea, with an emphasis on antibiotic misuse.</p><p><strong>Methodology: </strong>This study included 410 participants (217 fathers and 193 mothers), of whom 239 purchased antibiotics for their children without a prescription, whereas 171 had a prescription or were unsure if one was required.</p><p><strong>Results: </strong>Antibiotics were used incorrectly by 58.1% of respondents. About 51.2% of participants said they were taking two antibiotics at the same time. Around 30% of people admitted to using antibiotics inefficiently. The most prevalent reason for use was \"viral and bacterial,\" followed by \"viral,\" and then \"bacterial,\" with 35%, 21%, and 20%, respectively. In addition, 22.4% of patients have used antibiotics for an unknown reason.</p><p><strong>Conclusion: </strong>Saudi parents of children with pneumonia and diarrhea abuse antibiotics. Saudi legislation banning medications without a prescription has helped reduce antibiotic abuse, but more community-based education and awareness are needed.</p>","PeriodicalId":11326,"journal":{"name":"Drug Target Insights","volume":"17 ","pages":"114-119"},"PeriodicalIF":2.7,"publicationDate":"2023-10-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/f9/1a/dti-17-114.PMC10563503.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41194567","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}