Recent Advances in Inflammation & Allergy Drug Discovery最新文献

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The Evaluation of Safety Property and Apoptotic Efficacy of α-L-Guluronic Acid (G2013), as a Novel NSAID, Under In Vitro Examination on L929 and Hepatocellular Carcinoma Cell Lines. α- l -古鲁醛酸(G2013)作为一种新型非甾体抗炎药对L929和肝癌细胞系的安全性、特性和凋亡作用的体外研究
IF 0.4
Recent Advances in Inflammation & Allergy Drug Discovery Pub Date : 2022-01-01 DOI: 10.2174/2772434416666210909111912
Shahrzad Hassani, Jalil Tavakol Afshari, Fahimeh Jafarnezhad-Ansariha, Abbas Mirshafiey
{"title":"The Evaluation of Safety Property and Apoptotic Efficacy of α-L-Guluronic Acid (G2013), as a Novel NSAID, Under <i>In Vitro</i> Examination on L929 and Hepatocellular Carcinoma Cell Lines.","authors":"Shahrzad Hassani,&nbsp;Jalil Tavakol Afshari,&nbsp;Fahimeh Jafarnezhad-Ansariha,&nbsp;Abbas Mirshafiey","doi":"10.2174/2772434416666210909111912","DOIUrl":"https://doi.org/10.2174/2772434416666210909111912","url":null,"abstract":"<p><strong>Background: </strong>Many investigations have expanded this concept that liver chronic inflammation has an essential role in persistent cell damages along with altering the liver microenvironment leading to fibrosis, cirrhosis, and finally, hepatocellular carcinoma (HCC). To reduce inflammation and relieve symptoms, Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) are commonly used; however, their long-term usage can lead to severe adverse events on vital organs like the liver. Interestingly, the α-L-Guluronic Acid (G2013), as a novel NSAID with immunomodulatory properties, has shown the inhibitory effects on inflammation and metastasis in experimental models.</p><p><strong>Objective: </strong>This study was conducted to determine the effects of G2013 on cytotoxicity and induction of apoptosis, as a new therapeutic target for cancer therapy, in the HepG2 cell line and the mouse fibroblast cell line L929, as a control.</p><p><strong>Methods: </strong>MTT assay and flow cytometry method were carried out using the different concentrations of G2013 (5, 15, 25, 50, 100, 200 and 400 μg/ml) in 3 distinct incubation times.</p><p><strong>Results: </strong>Our data showed that treatment of HepG2 cells with high concentration (400μg/mL) of G2013 could effectively cause a decrease in cell viability, so that they were statistically different after 72 hours compared to other concentrations (5 to 200 μg/ml) (p<0.05 and p<0.01, respectively). Moreover, the proportion of apoptosis of HepG2 cells at the dose of 200μg/mL considerably increased, suggesting that the induction of apoptosis by G2013 in HepG2 cells is dose- and time-dependent, which could promote its anticancer properties.</p><p><strong>Conclusion: </strong>The present study revealed that G2013 could induce apoptosis in the liver cancer model. Therefore, based on these findings, G2013 might be considered as a therapeutic option in cancer therapy.</p>","PeriodicalId":29815,"journal":{"name":"Recent Advances in Inflammation & Allergy Drug Discovery","volume":"15 1","pages":"9-15"},"PeriodicalIF":0.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39402456","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
Linezolid Intoxication with Extreme Lactate Blood Levels Successfully Treated with Dialytic Treatment in ICU: A Case Report. 重症监护病房透析治疗利奈唑胺中毒并乳酸血症1例。
IF 0.4
Recent Advances in Inflammation & Allergy Drug Discovery Pub Date : 2022-01-01 DOI: 10.2174/2772270816666220606111049
Lorenzo Schiavoni, Alessia Mattei, Giuseppe Pascarella, Alessandro Strumia, Antonio Nenna, Massimo Chello, Felice E Agrò
{"title":"Linezolid Intoxication with Extreme Lactate Blood Levels Successfully Treated with Dialytic Treatment in ICU: A Case Report.","authors":"Lorenzo Schiavoni,&nbsp;Alessia Mattei,&nbsp;Giuseppe Pascarella,&nbsp;Alessandro Strumia,&nbsp;Antonio Nenna,&nbsp;Massimo Chello,&nbsp;Felice E Agrò","doi":"10.2174/2772270816666220606111049","DOIUrl":"https://doi.org/10.2174/2772270816666220606111049","url":null,"abstract":"<p><strong>Introduction: </strong>Lactic acidosis is a rare but life-threatening complication associated with prolonged linezolid therapy. No specific treatment is suggested, except for antibiotic therapy interruption.</p><p><strong>Case report: </strong>A 70-years-old woman faced severe linezolid intoxication after antibiotics therapy initiation for infection of a surgical sternal wound. The patient suffered from a severe increment of blood lactate and thrombocytopenia. She was admitted to ICU twice, and due to dialytic treatment, linezolid and lactate serum levels came back to normality.</p><p><strong>Conclusion: </strong>More studies should be conducted to evaluate the human tissue storage sites of linezolid and the influence of various factors on its clearance and plasma concentrations in critically ill patients.</p>","PeriodicalId":29815,"journal":{"name":"Recent Advances in Inflammation & Allergy Drug Discovery","volume":"16 1","pages":"50-53"},"PeriodicalIF":0.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10684725","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: 1
Major Histocompatibility Complex Class II HLA-DRB1 Allelic Epitopes in Fibromyalgia. 纤维肌痛的主要组织相容性复合体II类HLA-DRB1等位基因表位。
IF 0.4
Recent Advances in Inflammation & Allergy Drug Discovery Pub Date : 2022-01-01 DOI: 10.2174/2772270816666220321162802
Basant K Puri, Gary S Lee, Armin Schwarzbach
{"title":"Major Histocompatibility Complex Class II <i>HLA-DRB1</i> Allelic Epitopes in Fibromyalgia.","authors":"Basant K Puri,&nbsp;Gary S Lee,&nbsp;Armin Schwarzbach","doi":"10.2174/2772270816666220321162802","DOIUrl":"https://doi.org/10.2174/2772270816666220321162802","url":null,"abstract":"<p><strong>Background: </strong>Preliminary evidence has pointed an association of the gene HLA-DRB1 with fibromyalgia. HLA-DRB1 alleles carrying the shared or susceptibility epitope encoding the five-amino acid motif QKRAA, QRRAA or RRRAA in positions 70 to 74 of the major histocompatibility complex class II DRβ chain are associated with several autoimmune diseases.</p><p><strong>Objective: </strong>The objective of this study was to test the hypothesis that susceptibility epitope-encoding HLA-DRB1 alleles are associated with fibromyalgia.</p><p><strong>Methods: </strong>Using a case-control design, the prevalence of susceptibility epitope-encoding HLADRB1 alleles in 27 white Caucasian patients fulfilling the revised diagnostic criteria for fibromyalgia of the American College of Rheumatology was compared with that in 27 white Caucasian ageand sex-matched healthy controls.</p><p><strong>Results: </strong>13 (48%) of the fibromyalgia patients had susceptibility epitope-coding HLA-DRB1 alleles compared with 15 (56%) of the controls (P = 0.785). The DRB1*01 allele encoding the protective epitope 70-DERAA-74 motif was found in one of the control subjects; none of the fibromyalgia patients had such a protective epitope.</p><p><strong>Conclusion: </strong>While the present study does not provide evidence supporting the potential role of HLA-DRB1 in the etiology of fibromyalgia, it does not exclude the possibility that there is a polygenic component to a putative genetic causative role.</p>","PeriodicalId":29815,"journal":{"name":"Recent Advances in Inflammation & Allergy Drug Discovery","volume":"16 1","pages":"16-18"},"PeriodicalIF":0.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10817001","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
A Novel Method for the Syntheses of Imidazo-Thiadiazoles as Potential Antioxidants and Anti-Inflammatory Agents. 咪唑-噻二唑类抗氧化剂和抗炎剂的新合成方法。
IF 0.4
Recent Advances in Inflammation & Allergy Drug Discovery Pub Date : 2022-01-01 DOI: 10.2174/2772270816666220410130059
Dattatraya G Raut, Raghunath B Bhosale, Anjana S Lawand, Mahesh G Hublikar, Vikas D Kadu, Sandeep B Patil
{"title":"A Novel Method for the Syntheses of Imidazo-Thiadiazoles as Potential Antioxidants and Anti-Inflammatory Agents.","authors":"Dattatraya G Raut,&nbsp;Raghunath B Bhosale,&nbsp;Anjana S Lawand,&nbsp;Mahesh G Hublikar,&nbsp;Vikas D Kadu,&nbsp;Sandeep B Patil","doi":"10.2174/2772270816666220410130059","DOIUrl":"https://doi.org/10.2174/2772270816666220410130059","url":null,"abstract":"<p><strong>Background: </strong>A literature survey revealed that many imidazo-thiadiazole molecules were used as key intermediates for the development of novel drugs. The synthesized imidazo-thiadiazole derivatives were tested for their in vitro antioxidant and anti-inflammatory properties. The purpose of this research paper is to provide readers with information regarding diseases caused by free radicals.</p><p><strong>Objective: </strong>The objective of this study is to develop novel antioxidant and anti-inflammatory drugs.</p><p><strong>Methods: </strong>Imidazo-thiadiazole derivatives 5a-f were synthesized through cyclo-condensation reactions in two steps. First, the synthesis of 2-amino-thiadiazole derivatives from substituted aromatic carboxylic acids and thiosemicarbazide by using POCl<sub>3</sub> as a solvent as well as a catalyst was performed. In the next step, imidazo-thiadiazoles were prepared from 2-amino-thiadiazole derivatives with appropriate α-haloketones in the presence of polyethylene glycol-300 (PEG-300) as a green solvent. These imidazo- thiadiazole derivatives were prepared by using a novel method. The synthesized compounds were in vitro tested for their antioxidant and anti-inflammatory activities.</p><p><strong>Results: </strong>In vitro evaluation report showed that nearly all molecules possess potential antioxidant activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO), superoxide radical (SOR), and hydrogen peroxide (H<sub>2</sub>O<sub>2</sub>) radical scavenging activity. Most of the imidazo-thiadiazole derivatives have shown significant anti-inflammatory activity as compared to diclofenac sodium as a reference standard.</p><p><strong>Conclusion: </strong>In the search for novel therapies to treat inflammation and oxidation, we have made efforts to develop anti-inflammatory and antioxidant agents with a preeminent activity. Imidazo-thiadiazoles 5a, 5e as well as 5f showed potential anti-inflammatory activity. All tested imidazo-thiadiazole deriv-atives (5a-f) showed potential antioxidant activity against one more radical scavenging species as com-pared to ascorbic acid as the reference standard. Thus, imidazo-thiadiazole derivatives constitute an interesting template for the design and development of new antioxidant as well as anti-inflammatory agents.</p>","PeriodicalId":29815,"journal":{"name":"Recent Advances in Inflammation & Allergy Drug Discovery","volume":"16 1","pages":"19-25"},"PeriodicalIF":0.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10684685","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
Cell-free Therapy for Inflammatory Diseases: Opportunities and Challenges. 炎性疾病的无细胞治疗:机遇与挑战。
IF 0.4
Recent Advances in Inflammation & Allergy Drug Discovery Pub Date : 2022-01-01 DOI: 10.2174/2772270816666211220152218
Khan Sharun, Kuldeep Dhama, Kaveri Jambagi, Abhijit M Pawde, Amarpal
{"title":"Cell-free Therapy for Inflammatory Diseases: Opportunities and Challenges.","authors":"Khan Sharun,&nbsp;Kuldeep Dhama,&nbsp;Kaveri Jambagi,&nbsp;Abhijit M Pawde,&nbsp;Amarpal","doi":"10.2174/2772270816666211220152218","DOIUrl":"https://doi.org/10.2174/2772270816666211220152218","url":null,"abstract":"<jats:sec>\u0000<jats:title />\u0000<jats:p />\u0000</jats:sec>","PeriodicalId":29815,"journal":{"name":"Recent Advances in Inflammation & Allergy Drug Discovery","volume":"15 1","pages":"5-8"},"PeriodicalIF":0.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39620993","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: 5
Quality of Life of Healthcare Workers Suffering from Occupational Contact Dermatitis. 职业性接触性皮炎医护人员的生活质量。
IF 0.4
Recent Advances in Inflammation & Allergy Drug Discovery Pub Date : 2022-01-01 DOI: 10.2174/1872213X14666210303155135
Amira Omrane, Asma Khedher, Chayma Harrathi, Maher Maoua, Taoufik Khalfallah, Lamia Bouzgarrou, Nejib Mrizak, Mohamed Adnene Henchi, Hichem Bel Hadj Ali
{"title":"Quality of Life of Healthcare Workers Suffering from Occupational Contact Dermatitis.","authors":"Amira Omrane,&nbsp;Asma Khedher,&nbsp;Chayma Harrathi,&nbsp;Maher Maoua,&nbsp;Taoufik Khalfallah,&nbsp;Lamia Bouzgarrou,&nbsp;Nejib Mrizak,&nbsp;Mohamed Adnene Henchi,&nbsp;Hichem Bel Hadj Ali","doi":"10.2174/1872213X14666210303155135","DOIUrl":"https://doi.org/10.2174/1872213X14666210303155135","url":null,"abstract":"<p><strong>Background: </strong>Healthcare workers are at a high risk of developing Occupational Dermatitis (OD). Affected workers often experience severe impairment of their Quality of Life (QoL). This study aimed to assess the skin-related QoL of healthcare workers with OD and to explore its related factors.</p><p><strong>Methods: </strong>A cross-sectional and exhaustive study was conducted among healthcare personnel of four public hospitals in the central region of Tunisia. All the cases of OD declared were included. Skin-related QoL was assessed using the validated Tunisian version of the \"Dermatology Life Quality Index\" (DLQI). Some related patents have also been discussed.</p><p><strong>Results: </strong>A total of 37 cases of OD were collected with an annual incidence of 4.2 cases per 10000 workers. The population was predominantly female (73%) and the mean age was 44.7±9.4 years. Nurses were the most represented occupational category (38%). Allergic contact dermatitis was the most frequent diagnosis (96%). The use of gloves was the most frequently reported occupational hazard (86%). The most frequently affected sites were hands (97%). The median score of DLQI was five. Multivariate analysis showed an association between the impairment of skin-related QoL and female gender (p = 0.04; OR = 19.3,84), exposure to disinfecting chemicals in the workplace (p = 0.01; OR = 17,306) and the absence of occupational reclassification (p = 0.01; OR = 21,567).</p><p><strong>Conclusion: </strong>About one-third of the population had an impaired quality of life. The score impairment was significantly related to the female gender, exposure to disinfecting chemicals and the absence of occupational reclassification.</p>","PeriodicalId":29815,"journal":{"name":"Recent Advances in Inflammation & Allergy Drug Discovery","volume":"15 1","pages":"44-51"},"PeriodicalIF":0.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25465624","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: 2
Neuroinflammation and Behavioral Deficit in Rotenone-Induced Neurotoxicity in Rats and the Possible Effects of Butanolic Extract of Centaurea africana. 鱼藤酮致大鼠神经毒性的神经炎症和行为缺陷及半马齿苋丁醇提取物的可能作用。
IF 0.4
Recent Advances in Inflammation & Allergy Drug Discovery Pub Date : 2022-01-01 DOI: 10.2174/2772270816666220105124730
Sabrina Hadjira, Amira Mansour, Ramdane Seghiri, Ahmed Menad, Fadila Benayache, Samir Benayache, Souad Ameddah
{"title":"Neuroinflammation and Behavioral Deficit in Rotenone-Induced Neurotoxicity in Rats and the Possible Effects of Butanolic Extract of <i>Centaurea africana</i>.","authors":"Sabrina Hadjira,&nbsp;Amira Mansour,&nbsp;Ramdane Seghiri,&nbsp;Ahmed Menad,&nbsp;Fadila Benayache,&nbsp;Samir Benayache,&nbsp;Souad Ameddah","doi":"10.2174/2772270816666220105124730","DOIUrl":"https://doi.org/10.2174/2772270816666220105124730","url":null,"abstract":"<p><strong>Background: </strong>Many studies have used rotenone (ROT) to create an experimental animal model of Parkinson's disease (PD) because of its ability to induce similar behavioral and motor deficits. PD is the most common age-related motoric neurodegenerative disorder. Neuroinflammation and apoptosis play an important role in the pathogenesis of this disease.</p><p><strong>Objective: </strong>This study investigated the effect of butanolic (n-BuOH) extract of Centaurea africana (200 mg/kg, 16 days) on a ROT-induced neurotoxicity model in male Wistar albino rats.</p><p><strong>Methods: </strong>Estimation of Tumor Necrosis Factor (TNF-α) and Nitric Oxide (NO) levels along with the myeloperoxidase (MPO) activity in brains was carried out in order to evaluate neuro-inflammation. Oxidative stress, Caspase 3 activity (apoptosis), and behavioral alterations were also evaluated.</p><p><strong>Results: </strong>In behavior assessment, using Ludolph Movement Analysis Scale, all ROT treated animals showed a decreased locomotor activity. The mitochondrial dysfunction induced by ROT was expressed by a decreased activity of complex I of the mitochondrial respiratory chain and increased lipid peroxidation and caspase 3. Co-treatment with the n-BuOH extract significantly restored the activity of complex I (65.41 %) compared to treatment with ROT alone. The n-BuOH extract also reduced the neuroinflammation in rat brains by reducing MPO activity (75.12 %), NO levels (77.43 %), and TNF-α (71.48 %) compared to the group treated with ROT.</p><p><strong>Conclusion: </strong>The obtained results indicated that C. africana n-BuOH extract exhibited a protective effect in rats.</p>","PeriodicalId":29815,"journal":{"name":"Recent Advances in Inflammation & Allergy Drug Discovery","volume":"15 1","pages":"35-43"},"PeriodicalIF":0.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39876469","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
Potential of Anti-inflammatory Molecules in the Chemoprevention of Breast Cancer. 抗炎分子在乳腺癌化学预防中的潜力。
IF 0.4
Recent Advances in Inflammation & Allergy Drug Discovery Pub Date : 2022-01-01 DOI: 10.2174/2772270816666220829090716
Vaishnavi Gadi, Saritha Shetty
{"title":"Potential of Anti-inflammatory Molecules in the Chemoprevention of Breast Cancer.","authors":"Vaishnavi Gadi,&nbsp;Saritha Shetty","doi":"10.2174/2772270816666220829090716","DOIUrl":"https://doi.org/10.2174/2772270816666220829090716","url":null,"abstract":"<p><p>Breast cancer is a global issue, affecting greater than 1 million women per annum. Over the past two decades, there have been numerous clinical trials involving the use of various pharmacological substances as chemopreventive agents for breast cancer. Various pre-clinical as well as clinical studies have established numerous anti-inflammatory molecules, including nonsteroidal anti-inflammatory drugs (NSAIDs) and dietary phytochemicals as promising agents for chemoprevention of several cancers, including breast cancer. The overexpression of COX-2 has been detected in approximately 40% of human breast cancer cases and pre-invasive ductal carcinoma in-situ lesions, associated with aggressive elements of breast cancer such as large size of the tumour, ER/PR negative and HER-2 overexpression, among others. Anti-inflammatory molecules inhibit COX, thereby inhibiting the formation of prostaglandins and inhibiting nuclear factor-κBmediated signals (NF-kB). Another probable explanation entails inflammation-induced degranulation, with the production of angiogenesis-regulating factors, such as vascular endothelial growth factor, which can be possibly regulated by anti-inflammatory molecules. Apart from NSAIDS, many dietary phytochemicals have the ability to decrease, delay, or stop the progression and/or incidence of breast cancer by their antioxidant action, regulating inflammatory and proliferative cell signalling pathways as well as inducing apoptosis. The rapid progress in chemoprevention research has also established innovative strategies that can be implemented to prevent breast cancer. This article gives a comprehensive overview of the recent advancements in using antiinflammatory molecules in the chemoprevention of breast cancer along with their mechanism of action, supported by latest preclinical and clinical data. The merits of anti-inflammatory chemopreventive agents in the prevention of cardiotoxicity have been described. We have also highlighted the ongoing research and advancements in improving the efficacy of using antiinflammatory molecules as chemopreventive agents.</p>","PeriodicalId":29815,"journal":{"name":"Recent Advances in Inflammation & Allergy Drug Discovery","volume":"16 2","pages":"60-76"},"PeriodicalIF":0.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9105896","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: 2
Syntheses, Molecular Docking and Biological Evaluation of 2-(2- hydrazinyl)thiazoles as Potential Antioxidant, Anti-Inflammatory and Significant Anticancer Agents. 2-(2-肼基)噻唑类潜在抗氧化、抗炎和抗癌药物的合成、分子对接及生物学评价
IF 0.4
Recent Advances in Inflammation & Allergy Drug Discovery Pub Date : 2022-01-01 DOI: 10.2174/2772270816666220902094019
Dattatraya G Raut, Raghunath B Bhosale, Anjana S Lawand, Mahesh G Hublikar, Vikas D Kadu, Sandeep B Patil, Prafulla B Choudhari
{"title":"Syntheses, Molecular Docking and Biological Evaluation of 2-(2- hydrazinyl)thiazoles as Potential Antioxidant, Anti-Inflammatory and Significant Anticancer Agents.","authors":"Dattatraya G Raut,&nbsp;Raghunath B Bhosale,&nbsp;Anjana S Lawand,&nbsp;Mahesh G Hublikar,&nbsp;Vikas D Kadu,&nbsp;Sandeep B Patil,&nbsp;Prafulla B Choudhari","doi":"10.2174/2772270816666220902094019","DOIUrl":"https://doi.org/10.2174/2772270816666220902094019","url":null,"abstract":"<p><strong>Background: </strong>Recently, researchers have worked on the development of new methods for the synthesis of bioactive heterocycles using polyethylene glycol as a green solvent. In this context, we report the synthesized 2-(2-hydrazinyl) thiazoles for their in vitro antioxidant, in vitro anti-inflammatory and in vitro anti-cancer activities.</p><p><strong>Objective: </strong>The objective of the study was to develop novel antioxidant, anti-inflammatory and anti-cancer drugs.</p><p><strong>Methods: </strong>At the outset, the condensation of substituted acetophenones 1, thiosemicarbazide 2, and α-haloketones 3 was carried out using PEG-400 (20 mL) in the presence of 5 mol% glacial acetic acid to afford thiosemicarbazones intermediate. Furthermore, these thiosemicarbazones were reacted with α-haloketones 3 to obtain appropriate 2-(2-hydrazinyl) thiazoles. The synthesized compounds were in vitro tested for their antioxidant, anti-inflammatory, and anti-cancer activity.</p><p><strong>Results: </strong>In vitro evaluation report showed that nearly all molecules possessed potential antioxidant activity against 2,2-Diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO), superoxide radical (SOR) and hydrogen peroxide (H<sub>2</sub>O<sub>2</sub>) radical scavenging activity. Most 2-(2-hydrazinyl) thiazoles derivatives have shown potential anti-inflammatory activity as compared to diclofenac sodium as a reference standard. 2-(2-Hydrazinyl) thiazoles derivatives showed significant anticancer activity for human leukemia cell line K-562 compared to adriamycin as a reference standard.</p><p><strong>Conclusion: </strong>All tested compounds showed potential 2,2-Diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide (NO) radical scavenging activity. Among the tested series, 4b, 4d and 4e exhibited good hydrogen peroxide and 4b, 4e, 4f and 4g showed excellent superoxide radical scavenging activity. In addition, the 4b, 4e and 4g compounds revealed potent in vitro anti-inflammatory activity against standard diclofenac sodium drug. 2-(2-Hydrazinyl) thiazole derivatives, such as 4c and 4d, showed significant anticancer activity against human leukemia cell line K-562. Thus, these molecules provide an interesting template for the design and development of new antioxidant, anti-inflammatory, and anti-cancer agents.</p>","PeriodicalId":29815,"journal":{"name":"Recent Advances in Inflammation & Allergy Drug Discovery","volume":"16 2","pages":"96-106"},"PeriodicalIF":0.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9091712","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
The Dopamine Gene Receptors (DRD1-5) Expression Alteration in Psoriasis Patients. 银屑病患者多巴胺基因受体(DRD1-5)表达改变
IF 0.4
Recent Advances in Inflammation & Allergy Drug Discovery Pub Date : 2022-01-01 DOI: 10.2174/2772270816666220629112414
Malihe Mohamadian, Hossein Mortazavi, Mina Makvand, Fatemeh Ahangari, Hasem Ahangari
{"title":"The Dopamine Gene Receptors (DRD<sub>1-5</sub>) Expression Alteration in Psoriasis Patients.","authors":"Malihe Mohamadian,&nbsp;Hossein Mortazavi,&nbsp;Mina Makvand,&nbsp;Fatemeh Ahangari,&nbsp;Hasem Ahangari","doi":"10.2174/2772270816666220629112414","DOIUrl":"https://doi.org/10.2174/2772270816666220629112414","url":null,"abstract":"<p><strong>Background: </strong>Psoriasis is a chronic inflammatory autoimmune disease that is considered linked to genetic and environmental factors such as stress. Since the neurotransmitter dopamine has a close association with stress configuration, it can be a candidate for relieving psoriasis representation. In addition to the CNS, immune cells can play a decisive role in regulating immune functions through dopamine synthesis and the expression of its receptors. Altered response of immune cells to dopamine as well as a distorted expression of dopamine receptors (DRs) in immune cells have been reported in some chronic inflammatory conditions.</p><p><strong>Objective: </strong>This study aims the evaluation of dopamine receptor (DR1-DR5) gene expression in mononuclear blood cells of psoriatic patients in comparison with normal individuals.</p><p><strong>Methods: </strong>We isolated peripheral mononuclear cells (PBMCs) from blood samples followed by total RNA extraction, cDNA synthesis, and real-time PCR using specific primer pairs.</p><p><strong>Results: </strong>We found that all types of DRs are expressed in the PBMCs of normal and psoriatic individuals. We also concluded that compared to controls, DR2 and DR4 were overexpressed in psoriasis patients while DR3 was low-expressed.</p><p><strong>Conclusion: </strong>Increased expression of DR2 and DR4 along with decreased expression of DR3 in PBMCs of psoriasis patients not only provide new insight into the pathogenesis of psoriasis but may also be effective in designing future therapeutic strategies attributable to psoriasis.</p>","PeriodicalId":29815,"journal":{"name":"Recent Advances in Inflammation & Allergy Drug Discovery","volume":"16 2","pages":"116-122"},"PeriodicalIF":0.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10546450","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}
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