Saudi Pharmaceutical Journal最新文献

{"title":"Impacts of Anabolic-androgenic steroid supplementation on female health and offspring: Mechanisms, side effects, and medical perspectives","authors":"Beatriz Menegate Santos ,&nbsp;Jessica Peres Alves de Souza ,&nbsp;Luísa Rodrigues de Paula Goulart ,&nbsp;Jéssica Castro Pereira Petrine ,&nbsp;Fernando Henrique Ferrari Alves ,&nbsp;Bruno Del Bianco-Borges","doi":"10.1016/j.jsps.2024.102205","DOIUrl":"10.1016/j.jsps.2024.102205","url":null,"abstract":"<div><div>The increasing prevalence of Anabolic–androgenic steroids (AAS) among women, driven by the pursuit of improved body aesthetics, characterized by higher lean mass and reduced adipose tissue, raises significant health concerns, particularly due to the limited knowledge regarding their effects on the female organism. Prolonged use and/or high doses of AAS are linked to various harmful side effects, including mood changes, psychiatric disorders, voice deepening, clitoromegaly, menstrual irregularities, and cardiovascular complications, prompting medical societies to discourage their widespread use due to insufficient evidence supporting their safety and efficacy. Studies in female rodents have shown that AAS can lead to increased aggression, inflammation, reduced neuronal density, and negative impacts on the myocardium and blood vessels. Additionally, maternal administration of androgens during pregnancy can adversely affect offspring’s reproductive, neuronal, and metabolic health, resulting in long-term impairments. The complexity of the mechanisms underlying AAS effects, and their potential genotoxicity remains poorly understood. This review aims to elucidate the various ways in which AAS can impact female physiology and that of their offspring, highlight commonly used anabolic substances, and discuss the positions of medical societies regarding AAS use.</div></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 12","pages":"Article 102205"},"PeriodicalIF":3.0,"publicationDate":"2024-11-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142706194","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Bioadhesive hybrid system of niosomes and pH sensitive in situ gel for itraconazole ocular delivery: Dual approach for efficient treatment of fungal infections","authors":"Mohamed M. Badran ,&nbsp;Areej Alsubaie ,&nbsp;Mounir M. Salem Bekhit ,&nbsp;Abdullah H. Alomrani ,&nbsp;Aliyah Almomen ,&nbsp;Mohamed Abbas Ibrahim ,&nbsp;Doaa Hasan Alshora","doi":"10.1016/j.jsps.2024.102208","DOIUrl":"10.1016/j.jsps.2024.102208","url":null,"abstract":"<div><div>Itraconazole (ITZ) is a highly effective antifungal agent. However, its oral application is associated with systemic toxicity and poor topical use. The present study aims to improve the antifungal activity of ITZ by loading it into bioadhesive niosomes. This approach is considered to enhance the ocular permeation of ITZ, thereby boosting its efficacy against fungal infections. Therefore, it was encapsulated into niosomes (F1) and subsequently coated with hyaluronic acid (HA; F2), chitosan (CS; F3), or a bilayer of CS/HA (F4). In addition, they were further incorporated into pH-sensitive <em>in situ</em> gels. This dual approach is expected to increase the amount of corneal-permeated ITZ, facilitating more effective management of ocular fungal infection.</div><div>Firstly, the niosomes were prepared by hydrating proniosomes using span 60, cholesterol, and phospholipid. ITZ-niosomes showed an increase in vesicle size from 165.5 ± 3.4 (F1) to 378.2 ± 7.2 nm (F3). The zeta potential varied within −20.9 ± 2.1 (F1), −29.5 ± 3.1 (F2), 32.3 ± 1.9 (F3), and 22.6 ± 1.3 mV (F4). The high EE% values ranged from 78.1 ± 2.2 % to 86.6 ± 2.9 %. Regarding ITZ release, F1 demonstrated a high release profile, whereas bioadhesive niosomes showed sustained release patterns. Furthermore, <em>in situ</em> gels containing niosomes displayed excellent gelling capacity and viscosity. Remarkably, F3 laden-<em>in situ</em> gels (F3-ISG) demonstrated the highest <em>ex vivo</em> corneal permeability of ITZ and antifungal activity with a safety effect. These results indicate that F3-ISG presents a promising strategy for boosting the ocular delivery of ITZ, that could help in treating ocular fungal infections.</div></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 12","pages":"Article 102208"},"PeriodicalIF":3.0,"publicationDate":"2024-11-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142706196","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Budget impact analysis of baricitinib for treatment of alopecia areata: A Saudi hospital perspective","authors":"A. Alshahrani ,&nbsp;S. Al-Aqeel ,&nbsp;M. Alshahrani ,&nbsp;S. Alqahtani ,&nbsp;S.T. Alhawwashi ,&nbsp;M.S. Al-Nasser ,&nbsp;M. Zaitoun","doi":"10.1016/j.jsps.2024.102204","DOIUrl":"10.1016/j.jsps.2024.102204","url":null,"abstract":"<div><h3>Objectives</h3><div>To perform a budget impact analysis (BIA) of the adoption of baricitinib for the management of alopecia areata (AA) by a Saudi public sector payer.</div></div><div><h3>Methods</h3><div>A BIA model was developed to calculate the expected financial impact under two scenarios: the baseline scenario, which reflects the current mix of treatments without baricitinib, and the projected scenario, in which baricitinib is adopted. The model assumed that patients with severe AA and those with mild-to-moderate AA who did not respond to other treatments were eligible for baricitinib treatment. The model input was based on published evidence, expert opinions, and the Saudi Expert Consensus Statement on the Diagnosis and Management of AA.</div></div><div><h3>Results</h3><div>Assuming a hypothetical total eligible population of 368 patients received different AA treatments over the 12-months study period. The aggregated 5-years cost in the baseline scenario was SR 5,836,616. Upon the introduction of baricitinib as an alternative treatment for severe AA, the projected aggregated budget impact was SR 7,473,138. Sensitivity analysis showed that the results were most sensitive to AA prevalence, percentage of severe AA, and predicted market share for baricitinib over the 5-year time horizon.</div></div><div><h3>Conclusion</h3><div>The addition of baricitinib to formularies is likely to increase the cost impact from a government hospital perspective. However, this addition expands the treatment options for patients with AA and may result in improved outcomes. Future cost-effectiveness analyses are recommended to estimate the cost per incremental improvement in the outcomes.</div></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 12","pages":"Article 102204"},"PeriodicalIF":3.0,"publicationDate":"2024-11-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142661312","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Real-World safety and effectiveness of evolocumab in primary hypercholesterolemia and mixed dyslipidemia in Saudi Arabia","authors":"Abdulaali R. Almutairi ,&nbsp;Walaa A. Alshahrani ,&nbsp;Ghaida K. Alhathlol ,&nbsp;Fatimah Alsheikh ,&nbsp;Abdulaziz Alakeel ,&nbsp;Majed S. Al Yami ,&nbsp;Mohammad Fouda ,&nbsp;Omar A. Almohammed ,&nbsp;Meshal S. Alhamed ,&nbsp;Awatif Hafiz ,&nbsp;Hussam Kutbi ,&nbsp;Alaa Bagalagel ,&nbsp;Aisha Alharbi ,&nbsp;Mashael Alaboud ,&nbsp;Sarah Aljohani ,&nbsp;Waddah Ashram","doi":"10.1016/j.jsps.2024.102203","DOIUrl":"10.1016/j.jsps.2024.102203","url":null,"abstract":"<div><h3>Introduction</h3><div>Evolocumab’s short-term efficacy and safety were proven in phase-3 clinical trial, but its long-term safety and effectiveness in the Saudi population are yet to be studied. The aim of this study was to assess the long-term safety and effectiveness of evolocumab in Saudi patients with primary hypercholesterolemia or mixed dyslipidemia.</div></div><div><h3>Method</h3><div>A retrospective cohort study evaluated adult patients who had newly been prescribed evolocumab for hypercholesterolemia or mixed dyslipidemia. Safety events included myocardial infarction, unstable angina, stroke, transient ischemic attack, heart failure, rhabdomyolysis, renal dysfunction, and myalgia. Effectiveness outcomes included changes in lipid profiles from baseline, assessed at 6-, 12-, 18-, and 24-month.</div></div><div><h3>Results</h3><div>The study sample were 469 who newly prescribed evolocumab, from which 69.1 % being male, were included. The most prevalent comorbidities were coronary artery disease, diabetes, and hypertension. Statin was the most commonly used therapy. The most common adverse events at 6-month follow-up, based on the incidence rate per 1000 person-years, were coronary revascularization (63.20), myalgia (44.96), myocardial infarction (31.53), unstable angina (31.49), heart failure (26.94), rhabdomyolysis without renal dysfunction (8.93), transient ischemic attack (4.46), and rhabdomyolysis with renal dysfunction (4.46). Stroke incidence increased with follow-up length, from 8.87 per 1000 person-years at 6 months to 12.84 per 1000 person-years at 24 months. Evolocumab use significantly reduced LDL and total cholesterol levels at 6, 12, 18, and 24 months follow-up, while having no significant effect on HDL or triglycerides levels.</div></div><div><h3>Conclusion</h3><div>Evolocumab appeared to be safe and effective therapeutic option for patients with primary hypercholesterolemia or mixed dyslipidemia to potentially reduce LDL levels to therapeutic levels when statins are insufficient.</div></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 12","pages":"Article 102203"},"PeriodicalIF":3.0,"publicationDate":"2024-11-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142661313","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Otostegia fruticosa (Forssk.) – A comprehensive insight of its ethnopharmacology, phytochemistry, and pharmacological activities","authors":"Mohammed F. Hawwal ,&nbsp;Sarfaraz Ahmed ,&nbsp;Perwez Alam ,&nbsp;Omer I. Fantoukh ,&nbsp;Gadah A. AlHamoud ,&nbsp;Hattan A. Alharbi ,&nbsp;Waleed A. Alobaid ,&nbsp;Hanan Khojah","doi":"10.1016/j.jsps.2024.102189","DOIUrl":"10.1016/j.jsps.2024.102189","url":null,"abstract":"<div><div>Otostegia fruticosa<!--> <!-->(Forssk.) is a shrub of the Lamiaceae family with a wide geographic distribution in Saudi Arabia, Western and Eastern Africa, Ethiopia, and the Middle East. The current study provides an overview of recent developments in the knowledge of<!--> <em>O. fruticosa</em>’s<!--> <!-->ethnobotanical, pharmacological, and phytochemical properties. In folkloric medicine, it has been used since ancient times for gastrointestinal disorders, oral health, ocular irritation, antiparasitic, diarrhea, tonsillitis, arthritis, respiratory complications, and sunstroke treatment. Pharmacological investigations of its antibacterial, antioxidant, anti-inflammatory, cytotoxic, analgesic, larvicidal, nephroprotective, and other effects further validated its folklore practice. A range of diterpenoids, triterpenes, flavonoids, and essential oils have been found in<!--> <em>O. fruticosa</em>, according to phytochemical studies, which are thought to be responsible for the pharmacological effects of this plant species. This scientific review summarizes the most important secondary metabolites isolated from the <em>O</em>. <em>fruticosa</em>. It also summarizes the biological activities, providing insights into further scientific exploration.</div></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 11","pages":"Article 102189"},"PeriodicalIF":3.0,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142554976","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Cytochrome c and cancer cell metabolism: A new perspective","authors":"Bader Alshehri","doi":"10.1016/j.jsps.2024.102194","DOIUrl":"10.1016/j.jsps.2024.102194","url":null,"abstract":"<div><div>Cytochrome <em>c</em> is a vital electron carrier in the mitochondrial respiratory chain. When the outer membrane of mitochondria becomes permeable, cytochrome <em>c</em> is discharged into the cytoplasm, where it initiates the intrinsic apoptosis pathway. The complex interaction between cytochrome <em>c</em> and apoptosis protease-activating factor-1 (Apaf-1) leads to the formation of the apoptosome and activation of a cascade of caspases, highlighting the critical role of cytochrome <em>c</em> in controlling cell death mechanisms. Additionally, cytochrome <em>c</em> undergoes post-translational modifications, especially phosphorylation, which intricately regulate its roles in both respiration and apoptosis. These modifications add layers of complexity to how cytochrome <em>c</em> effectively controls cellular functions. cytochrome <em>c</em> becomes a lighthouse in the intricate web of cancer, its expression patterns providing hints about prognosis and paths toward treatment. Reduced levels of cytochrome <em>c</em> have been observed in cancer tissues, indicating a potential inhibition of apoptosis. For instance, in glioma tissues, cytochrome <em>c</em> levels were lower compared to healthy tissues, and this reduction became more pronounced in advanced stages of the disease. However, the role of cytochrome <em>c</em> in cancer becomes more intricate as it becomes intertwined with the metabolic reprogramming of cancer cells. This suggests that cytochrome <em>c</em> plays a crucial role in tumor progression and resistance to treatment. Viewing cytochrome <em>c</em> as a molecular mosaic reveals that it is not merely a protein, but also a central player in determining cellular fate. This realization opens up exciting avenues for potential advancements in cancer diagnosis and treatment strategies. Despite the advancements made, the narrative surrounding cytochrome <em>c</em> remains incomplete, urging further exploration into its complexities and the biological implications linked to cancer. cytochrome <em>c</em> stands as a beacon of hope and a promising target for therapy in the battle against cancer, particularly due to its significant involvement in tumor metabolism. It holds the potential for a future where innovative solutions can be developed to address the intricate challenges of cellular fate. In this review, we have endeavored to illuminate the multifaceted domain of cytochrome <em>c</em> drawing connections among apoptosis, metabolic reprogramming, and the Warburg effect in the context of cancer.</div></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 12","pages":"Article 102194"},"PeriodicalIF":3.0,"publicationDate":"2024-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142586837","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Rise of implantable drugs: A chronicle of breakthroughs in drug delivery systems","authors":"Kampanart Huanbutta ,&nbsp;Vivek Puri ,&nbsp;Ameya Sharma ,&nbsp;Inderbir Singh ,&nbsp;Pornsak Sriamornsak ,&nbsp;Tanikan Sangnim","doi":"10.1016/j.jsps.2024.102193","DOIUrl":"10.1016/j.jsps.2024.102193","url":null,"abstract":"<div><div>In recent years, implantable drug delivery systems (IDDSs) have undergone significant advancements because they offer many advantages to patients and health care professionals. Miniaturization has reduced the size of these devices, making them less invasive and easier to implant. Remote control provides more precise medication delivery and dosage. Biodegradable implants are an additional advancement in implantable drug delivery systems that eliminate the need for surgical removal. Smart implants can monitor a patient’s condition and adjust their drug doses. Long-acting implants also provide sustained drug delivery for months or even years, eliminating the need for regular medication dosing, and wireless power and data transmission technology enables the use of devices that are more comfortable and less invasive. These innovations have enhanced patient outcomes by enabling more precise administration, sustained drug delivery, and improved health care monitoring. With continued research and development, it is anticipated that IDDSs will become more effective and provide patients with improved health outcomes. This review categorizes and discusses the benefits and limitations of recent novel IDDSs for their potential therapeutic use.</div></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 12","pages":"Article 102193"},"PeriodicalIF":3.0,"publicationDate":"2024-10-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142577458","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A systematic review of obesity burden in Saudi Arabia: Prevalence and associated co-morbidities","authors":"Hussain A. Al-Omar ,&nbsp;Ali Alshehri ,&nbsp;Saleh A. Alqahtani ,&nbsp;Hana Alabdulkarim ,&nbsp;Ali Alrumaih ,&nbsp;Mahmoud S. Eldin","doi":"10.1016/j.jsps.2024.102192","DOIUrl":"10.1016/j.jsps.2024.102192","url":null,"abstract":"<div><h3>Introduction</h3><div>Saudi Arabia has experienced an increasing trend in obesity prevalence in the last three decades; obesity is a significant risk factor for non-communicable diseases, which may cause healthcare and economic burdens. In this systematic review, we aim to explore the obesity prevalence, obesity-related complications (ORCs), and the economic burden of obesity in Saudi Arabia.</div></div><div><h3>Methods</h3><div>Literature searches for relevant local studies across Saudi Arabia spanning 2012 to 2022 were performed in PubMed and EMBASE, along with supplementary searches for relevant congress abstracts. Only studies that discussed obesity prevalence in Saudi Arabia in relation to any gender or age group, the prevalence of ORCs in Saudi Arabia for any gender or age group, and/or the economic burden of obesity and how it impacts the healthcare system in Saudi Arabia, and were published in the English language, were selected for inclusion. No age or gender restrictions were imposed.</div></div><div><h3>Results</h3><div>The prevalence of obesity in Saudi Arabia ranged from 20% to 39% and up to 19.4% among adults and adolescents, respectively. The most reported ORCs were hypertension (67.6%), type 2 diabetes (60.7%), and hypercholesterolaemia (51.3%), and an association between obesity and ORCs was established, showing an increased risk with increasing body mass index. The economic burden of obesity across Saudi Arabia was estimated to be 6.4 billion US dollars (USD) for treatment and management.</div></div><div><h3>Conclusion</h3><div>Obesity affects a substantial proportion of the Saudi general population and is a significant burden on individuals, as demonstrated by the prevalence of ORCs. Multifaceted, short- and long-term approaches involving interventions that operate at multiple levels and target both individuals and communities are urgently needed; there is a particular need for a national strategy and a specific, systems-based policy. Further research will help increase awareness of obesity and its management, which will be crucial for transforming the healthcare system under <span><span>Vision 2030</span></span>.</div></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 11","pages":"Article 102192"},"PeriodicalIF":3.0,"publicationDate":"2024-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142535929","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Captagon: A comprehensive bibliometric analysis (1962–2024) of its global impact, health and mortality risks","authors":"Seraphina Fong ,&nbsp;Alessandro Carollo ,&nbsp;Andrea Rossato ,&nbsp;Elisabeth Prevete ,&nbsp;Gianluca Esposito ,&nbsp;Ornella Corazza","doi":"10.1016/j.jsps.2024.102188","DOIUrl":"10.1016/j.jsps.2024.102188","url":null,"abstract":"<div><div>Captagon is a synthetic stimulant combining amphetamine and theophylline. Initially introduced in 1961 as a treatment for hyperactivity, depression, and narcolepsy, Captagon was later classified as a Schedule 1 controlled substance due to its addictive and hallucinogenic properties. Despite its global prohibition in 1986, the trade of counterfeit products is widespread, especially in south-east Europe and far-east Asia, with its production being on the rise in Middle Eastern regions. This paper presents a quantitative data-driven bibliometric analysis of the existing literature on Captagon up to July 2024. It aims to delineate the structure and development of knowledge surrounding the substance, including key contributing countries, authors, prominent sources, and recurring thematic keywords. The quantitative and data-driven results were then used to guide the narrative discussion on Captagon. Findings indicate that current research predominantly focuses on Captagon’s use and impact in conflict zones, often exploring its interaction with other substances used by civilians and militias. Results also show a growing trend in Captagon research, with Saudi Arabia, Jordan, and Iraq emerging as main contributors to the literature. Despite the attention in specific regions, a considerable gap remains in understanding the mechanisms of action of Captagon (particularly regarding its metabolism, toxicology, mortality risk), and in developing protocols for its discontinuation. Additionally, the drug’s inconsistent composition requires further analyses to better predict risks and establish effective management strategies. Addressing these gaps will be crucial for the development of novel interventions and policies to mitigate the adverse effects of Captagon and improve public health systems worldwide.</div></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 11","pages":"Article 102188"},"PeriodicalIF":3.0,"publicationDate":"2024-10-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142535928","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pharmacological investigations of newly synthesized oxazolones and imidazolones as COX-2 inhibitors","authors":"Iqra Saleem Naz Babari ,&nbsp;Muhammad Islam ,&nbsp;Hamid Saeed ,&nbsp;Humaira Nadeem ,&nbsp;Hassaan Anwer Rathore","doi":"10.1016/j.jsps.2024.102191","DOIUrl":"10.1016/j.jsps.2024.102191","url":null,"abstract":"<div><div>Oxazoles and Imidazoles are heterocyclic compounds with significant biological activities. The present study explores the pharmacological effects of some new oxazole and imidazole derivatives as potential COX-2 inhibitors. Docking studies of the compounds against targeted proteins COX-2 and TACE manifested good binding affinities for both the targets supporting their anti-inflammatory potential. Compounds (3F-A, 3F-B, N-A, N-B) were evaluated for <em>in vivo</em> anti-inflammatory effects by carrageenan-induced paw edema. Among all, compound N-A was found to be the most effective as it displayed most pronounced reduction in inflammation that was comparable to indomethacin. The <em>in vivo</em> tissue antioxidant activity was performed for estimation of the level of catalase, GSH, GST, and thiobarbituric acid in paw tissue. The results exhibited that targeted compounds improved the oxidative stress and restored the expression of enzymes. H &amp;E staining revealed that aforesaid compounds displayed well-defined restoration of cellular damage. Compound NA exhibited maximum structural and functional preservation. Reduction in the expression of inflammatory markers was also analyzed by ELISA and maximum reduction in protein expression (COX-2 and TNF-a) was observed for compound N-B. Quantification of mRNA was done using PCR and a decrease in the expression of COX-2 mRNA level in treatment groups was depicted by all the new compounds but N-B showed maximum reduction in enzyme expression. All the results obtained from the present study have shown the significant anti-inflammatory potential of new compounds via the COX-2 inhibition pathway.</div></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 11","pages":"Article 102191"},"PeriodicalIF":3.0,"publicationDate":"2024-10-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142535934","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}