Anti-inflammatory & anti-allergy agents in medicinal chemistry最新文献

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Prepubertal Continuous Dietary Folate Fortification Enhances the Brain Function of Adult Mice by Modulating Antioxidant Status, Inflammation, and Brain Neurotransmitter Levels. 青春期前连续膳食叶酸强化通过调节抗氧化状态、炎症和脑神经递质水平来增强成年小鼠的脑功能。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2023-01-01 DOI: 10.2174/0118715230249814230925060325
Olakunle J Onaolapo, Anthony T Olofinnade, Folusho O Ojo, Joshua Falade, Adejoke Y Onaolapo
{"title":"Prepubertal Continuous Dietary Folate Fortification Enhances the Brain Function of Adult Mice by Modulating Antioxidant Status, Inflammation, and Brain Neurotransmitter Levels.","authors":"Olakunle J Onaolapo, Anthony T Olofinnade, Folusho O Ojo, Joshua Falade, Adejoke Y Onaolapo","doi":"10.2174/0118715230249814230925060325","DOIUrl":"10.2174/0118715230249814230925060325","url":null,"abstract":"<p><strong>Background: </strong>The benefits of folic acid supplementation have been documented in several studies. However, while evidence exists regarding its benefits for growth and haematologic parameters, its possible effects on the brain have been less examined.</p><p><strong>Objectives: </strong>The study aimed to examine the benefits of dietary folic acid supplementation (beginning in the prepubertal period) on neurobehaviour, oxidative stress, inflammatory parameters, and neurotransmitter levels in adult mice.</p><p><strong>Methods: </strong>Forty-eight prepubertal male mice were assigned into four groups of 12 animals each. Mice were grouped into normal control (fed standard diet) and three groups fed folic acid supplemented diet at 2.5, 5, and 10 mg/kg of feed. Animals were fed a standard diet or folic acid-supplemented diet for eight weeks during which food intake and body weight were assessed. On postnatal day 78, animals were exposed to the open-field, Y-maze, radial arm maze, elevated plus maze, bar test, and models of behavioural despair. 24 hours after the last behavioural test, animals were made to fast overnight and then sacrificed by cervical dislocation. Blood was then taken for the assessment of blood glucose, leptin, and insulin levels. Homogenates of brain tissue were prepared and used for the assessment of biochemical parameters.</p><p><strong>Results: </strong>Results showed a concentration-dependent increase in body weight, and improved antioxidant status, memory scores, and acetylcholine levels. Also, a decrease in food intake, blood glucose, insulin, and leptin levels was observed. A reduction in open-field behaviour, anxiety-related behaviour, and proinflammatory markers, was also observed.</p><p><strong>Conclusion: </strong>The beneficial effect of prepubertal continuous dietary folate fortification on the brain (as the animal ages) has been shown in this study.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"198-209"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49687116","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Development of 7H-pyrrolo[2,3-d]pyrimidin-4-amine Derivatives Using QSARINS Tool as BTK Inhibitors for the Treatment of Rheumatoid Arthritis. 基于QSARINS工具的7h -吡咯[2,3-d]嘧啶-4-胺衍生物BTK抑制剂治疗类风湿关节炎的研究
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2023-01-01 DOI: 10.2174/0118715230272263231103094710
Shital M Patil, Kalyani D Asgaonkar, Pradnya Magdum, Vaishnavi Chinde, Aishwarya Edake, Akshata Naik
{"title":"Development of 7H-pyrrolo[2,3-d]pyrimidin-4-amine Derivatives Using QSARINS Tool as BTK Inhibitors for the Treatment of Rheumatoid Arthritis.","authors":"Shital M Patil, Kalyani D Asgaonkar, Pradnya Magdum, Vaishnavi Chinde, Aishwarya Edake, Akshata Naik","doi":"10.2174/0118715230272263231103094710","DOIUrl":"10.2174/0118715230272263231103094710","url":null,"abstract":"<p><strong>Background: </strong>Rheumatoid arthritis (RA) is a chronic autoimmune disease characterized by inflammation of the joints, leading to pain, swelling, and joint deformity. Effective management of RA involves the use of disease-modifying drugs that can slow down disease progression and alleviate symptoms. Among the potential targets for RA treatment is Bruton's tyrosine kinase (BTK), which plays a crucial role in B-cell signalling and contributes to the pathogenesis of RA.</p><p><strong>Aims: </strong>QSARINS (QSAR-INSUBRIA) is software used for the development and validation of Quantitative Structure-Activity Relationship (QSAR) analysis. In the present work, this software was explored for pharmacophore optimization of the pyrrolo-pyrimidine nucleus for anti-rheumatoid activity.</p><p><strong>Methods: </strong>A series of pyrrolo-pyrimidine derivatives were used to build the QSAR models. These models were generated to identify structural features that correlate significantly with the activity. We followed the assessment of statistical parameters to ensure thorough validation of all the QSAR models. The QSAR models demonstrating better statistical performance were selected, and descriptors of these models were analysed.</p><p><strong>Results: </strong>The results showed that the QSAR models were highly statistically robust and exhibited a strong external predictive ability. Their structural features were also deduced.</p><p><strong>Conclusion: </strong>This QSAR study provided crucial information about the specific molecular features that can be used for the optimization of the pharmacophores. This research provides valuable insights into the structural features essential for BTK inhibition and paves the way for the design and development of novel anti-rheumatic agents targeting BTK in RA.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"236-249"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138453449","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Evaluation of the Capparis Herbacea Willd's Chemistry, Antioxidant and Cytotoxic Activity. 草芥化学、抗氧化和细胞毒活性的评价。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2023-01-01 DOI: 10.2174/0118715230281697231115074426
Orynbassar Tleuberlina, Asem Mamurova, Zhanar Iskakova, Yelaman Aibuldinov, Ainagul Kolpek, Yeldar Kopishev, Gulbarshyn Satbaeva, Zhazira Mukazhanova, Meruyert Kurmanbayeva
{"title":"Evaluation of the <i>Capparis Herbacea Willd's</i> Chemistry, Antioxidant and Cytotoxic Activity.","authors":"Orynbassar Tleuberlina, Asem Mamurova, Zhanar Iskakova, Yelaman Aibuldinov, Ainagul Kolpek, Yeldar Kopishev, Gulbarshyn Satbaeva, Zhazira Mukazhanova, Meruyert Kurmanbayeva","doi":"10.2174/0118715230281697231115074426","DOIUrl":"10.2174/0118715230281697231115074426","url":null,"abstract":"<p><strong>Background: </strong>The <i>Capparidaceae</i> family includes the medicinal herb <i>Capparis herbacea</i> Willd. The aerial and underground parts of plant <i>C.herbacea</i> were studied for their chemical composition, antioxidant, and cytotoxic properties.</p><p><strong>Methods: </strong>Using gas chromatography with mass spectrometric detection (7890A/5975C), 94 chemicals were identified in ethanol extract from leaves, roots, seeds, and stems of <i>C. herbacea</i>. Main components were (leaves) phytol 18.16%, hexanedioic acid, bis(2-ethylhexyl) ester 16.75%, vitamin E 11.95%, (roots) sucrose 13.94%, hexadecanoic acid, ethylester 22.80%, octadecanoic acid, ethylester 37.77%; (seeds) hexadecanoic acid, ethylester 13.96%, ethyl9.cis.,11.trans.-octadecadienoate 48.54%, bis(2-ethylhexyl) phthalate 9.77%; (stems) 1-propene-1,2,3-tricarboxylic acid, tributyl ester 42.69%, and tributylacetylcitrate 19.63%. Nine components were identified in the makeup of the <i>C. herbacea</i> sample's essential oil using the method of chromatography-mass spectrometry.</p><p><strong>Results: </strong>The main components were (in%): T-cadinol (29.56), meta-cymene (16.12), pulegone (14.11), and σ-amorphene (12.26). Chloroform and methanol extracts of <i>Capparis herbacia</i> roots at concentrations of 1 mg/ml showed higher average antioxidant activity, while ethyl acetate root extract at concentrations of 0.75 and 1 mg/ml showed higher average antioxidant activity compared to gallic acid AOA.</p><p><strong>Conclusion: </strong>In addition, plant extracts have cytotoxic activity. Essential oils of leaves and stems, fruit and roots of <i>Capparis herbacia</i> plants exhibited cytotoxicity, all larvae died, and larval mortality was 96%.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"261-272"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138453450","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Reduction of eNOS in Vascular Smooth Muscle by Salt Independently of Hypertension. 盐对血管平滑肌中 eNOS 的影响与高血压无关。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2016-01-01 Epub Date: 2016-09-22 DOI: 10.2174/1871523015666160922164224
Natalia L. Rukavina Mikusic, María I. Rosón, Silvana L. Della Penna, Marcelo R Choi, Susana Gorzalczany, Elsa Zotta, Jorge E Toblli, Belisario E Fernández
{"title":"Reduction of eNOS in Vascular Smooth Muscle by Salt Independently of Hypertension.","authors":"Natalia L. Rukavina Mikusic, María I. Rosón, Silvana L. Della Penna, Marcelo R Choi, Susana Gorzalczany, Elsa Zotta, Jorge E Toblli, Belisario E Fernández","doi":"10.2174/1871523015666160922164224","DOIUrl":"https://doi.org/10.2174/1871523015666160922164224","url":null,"abstract":"<p><strong>Background: </strong>Endothelial nitric oxide synthase (eNOS) is known to be expressed in endothelium and smooth muscle cells of arteries. The aim of this study was to investigate the expression of eNOS in intimal and medial layer of aorta from rats fed with a high salt diet and its modulation by losartan and tempol.</p><p><strong>Methods: </strong>Rats were fed during three weeks with: normal salt diet (NS, 0.4% NaCl); high salt diet (HS, 8% NaCl); NS plus tempol 1 mM (NS-T); HS plus tempol (HS-T); NS plus losartan 40mg.kg-1 (NS-L) and HS plus losartan (HS-L). Systolic blood pressure was recorded by the tail cuff method. Rats were then anaesthetized and the thoracic aorta and small arteries (bronchial branches of aorta) were processed to evaluate the expression of eNOS and aquaporin-1 (AQP-1) by immunohistochemistry.</p><p><strong>Results: </strong>HS group showed increased systolic blood pressure, increased eNOS and AQP-1 immunoexpression in the aorta intimal layer, and decreased eNOS immunoexpression in the aorta medial layer, respect to NS group. Losartan and tempol prevented hypertension and changes in the expression of eNOS and AQP-1 of the intimal layer. However, only tempol increased the expression of eNOS elicited by sodium overload in the medial layer of the aorta and small arteries respect to HS group.</p><p><strong>Conclusions: </strong>A high salt diet decreases eNOS expression in vascular smooth muscle layers of aorta and small arteries, which is reversed by tempol. These results suggest an adverse effect of oxidative stress on vascular eNOS in rats fed a high salt diet independently of hypertension.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":"15 2","pages":"135-144"},"PeriodicalIF":0.0,"publicationDate":"2016-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140041222","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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