Recent Advances in Inflammation & Allergy Drug Discovery最新文献

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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
Transdermal Anti-inflammatory Delivery for Solid Lipid Nanoparticles of Ketoprofen by Microwave-assisted Microemulsion. 微波辅助微乳液经皮递送酮洛芬固体脂质纳米颗粒的抗炎作用
IF 1.1
Recent Advances in Inflammation & Allergy Drug Discovery Pub Date : 2022-01-01 DOI: 10.2174/2772270816666220126105802
Swati C Jagdale, Manisha S Bafna, Anuruddha R Chabukswar
{"title":"Transdermal Anti-inflammatory Delivery for Solid Lipid Nanoparticles of Ketoprofen by Microwave-assisted Microemulsion.","authors":"Swati C Jagdale, Manisha S Bafna, Anuruddha R Chabukswar","doi":"10.2174/2772270816666220126105802","DOIUrl":"10.2174/2772270816666220126105802","url":null,"abstract":"<p><strong>Aims: </strong>To prepare solid lipid nanopaticles (SLNs) of Ketoprofen (KP) using microwave method. Ketoprofen (KP) is 2-(3-benzolphenyl) propionic acid with anti-inflammatory, analgesic and antipyretic property. The drug has a short half-life of 120 mins. It belongs to BCS Class II drug. Gastric irritation is a major limitation for delivery because of acidic nature of the drug. The development of solid lipid nanoparticles with its transdermal drug delivery was the aim of the present work.</p><p><strong>Methods: </strong>Microwave-assisted microemulsion technique was used for the development of solid lipid nanoparticles. Stearic acid was used as lipid and tween 80 was used as a surfactant. By varying the type of lipid and input energy watt, batches were formulated. SLNs were evaluated for zeta potential, drug entrapment, particle size and in-vitro drug release. Crystallinity behaviour was determined by differential scanning calorimetry and powder X-ray diffraction. Anti-inflammatory activity was evaluated for batch M4 of SLNs. The gel was prepared for M4 batch. It was evaluated for viscosity, pH, drug content, in-vitro and ex-vivo diffusion study.</p><p><strong>Results: </strong>SLNs were developed successfully. Based on the size, entrapment efficiency, stability and drug release, batch M4 was selected. SLNs showed 74.8% entrapment efficiency. Forty-fold improvement was observed in the solubility. The particle size was 682.9 nm and average size 1047 nm. PDI was 0.685 and zeta potential was -29.5 mV. M4 SLNs batch of gel showed burst release followed by a controlled release for 8 hrs in in-vitro drug release.</p><p><strong>Conclusion: </strong>SLNs were successfully prepared by Microwave-assisted microemulsion technique. SLNs with anti-inflammatory activity were successfully developed with their transdermal delivery.</p>","PeriodicalId":29815,"journal":{"name":"Recent Advances in Inflammation & Allergy Drug Discovery","volume":" ","pages":"87-98"},"PeriodicalIF":1.1,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39861548","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
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
Molecular Docking and Dynamics Simulation Studies of a Dataset of NLRP3 Inflammasome Inhibitors. NLRP3 炎症小体抑制剂数据集的分子对接和动力学模拟研究。
IF 1.1
Recent Advances in Inflammation & Allergy Drug Discovery Pub Date : 2022-01-01 DOI: 10.2174/2772270816666220126103909
Igor J Dos Santos Nascimento, Thiago M de Aquino, Edeildo F da Silva-Júnior
{"title":"Molecular Docking and Dynamics Simulation Studies of a Dataset of NLRP3 Inflammasome Inhibitors.","authors":"Igor J Dos Santos Nascimento, Thiago M de Aquino, Edeildo F da Silva-Júnior","doi":"10.2174/2772270816666220126103909","DOIUrl":"10.2174/2772270816666220126103909","url":null,"abstract":"<p><strong>Background: </strong>The organism's defense against aggressive agents is performed by the innate immune system via activation of pattern-recognition receptors (PRRs). Initially, these agents are recognized by the immune system, resulting in the inflammatory response that activates the pathogen elimination and tissue repair. Inflammasomes are macromolecules related to the host's response to endo or exogenous aggressive agents. Thus, inflammation mediated by inflammasomes plays an important role in the pathogenesis of diseases, such as neurodegenerative disorders, autoimmune diseases, and type 2 diabetes, justifying their attractiveness as drug targets. One of the most important tasks remains in the ATPase nucleotide-binding oligomerization domain nucleotide- binding domain leucine-rich repeat-containing receptors protein 3 (NLRP3), in which the blocking of its oligomerization is related to the functional inhibition of inflammasomes. Here, we performed molecular docking and dynamics simulations for NP3-146, an analog of MCC950, to obtain information about the complex stability and main interactions with amino acid residues from NLRP3.</p><p><strong>Methods: </strong>By using the crystalized structure recently deposited in the protein data bank (7alv), molecular docking in GOLD software and molecular dynamics simulations in GROMACS software were performed to generate the RMSD RMSF, R<sub>g,</sub> SASA, and H-bond plots.</p><p><strong>Results: </strong>The results of RMSD, RMSF, R<sub>g</sub>, SASA, and H-bond plots of both complexes confirmed the stability at the active site. Besides, the analyses of the most stable conformation showed that the main interactions are performed with Ala<sup>227</sup>, Ala<sup>228</sup>, Pro<sup>352</sup>, Ile<sup>411</sup>, Phe<sup>575</sup>, and Arg<sup>578</sup> residues.</p><p><strong>Conclusion: </strong>This report confirmed the stability of NP3-146, similar to the known inhibitor MCC950, providing useful information for designing NLRP3 inhibitors.</p>","PeriodicalId":29815,"journal":{"name":"Recent Advances in Inflammation & Allergy Drug Discovery","volume":" ","pages":"80-86"},"PeriodicalIF":1.1,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39861547","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
Hand, Foot, and Mouth Disease: A Narrative Review. 手足口病:叙述性回顾。
IF 0.4
Recent Advances in Inflammation & Allergy Drug Discovery Pub Date : 2022-01-01 DOI: 10.2174/1570180820666221024095837
Alexander K C Leung, Joseph M Lam, Benjamin Barankin, Kin Fon Leong, Kam Lun Hon
{"title":"Hand, Foot, and Mouth Disease: A Narrative Review.","authors":"Alexander K C Leung,&nbsp;Joseph M Lam,&nbsp;Benjamin Barankin,&nbsp;Kin Fon Leong,&nbsp;Kam Lun Hon","doi":"10.2174/1570180820666221024095837","DOIUrl":"https://doi.org/10.2174/1570180820666221024095837","url":null,"abstract":"<p><strong>Background: </strong>Hand, foot, and mouth disease is a common viral disease in childhood. Because the disease has the potential to reach epidemic levels and mortality is high in some countries, early recognition of this disease is of paramount importance.</p><p><strong>Objective: </strong>This purpose of this article is to familiarize pediatricians with the clinical manifestations and management of hand, foot, and mouth disease.</p><p><strong>Methods: </strong>A search was conducted in February 2022 in PubMed Clinical Queries using the key term \"hand, foot, and mouth disease\". The search strategy included all clinical trials, observational studies, and reviews published within the past 10 years. Only papers published in English were included in this review.</p><p><strong>Results: </strong>Hand, foot, and mouth disease is characterized by a painful oral enanthem and asymptomatic exanthem on the palms and soles. Children younger than 5 years are most commonly affected. Hand, foot, and mouth disease caused by enterovirus A71 is more severe and has a higher rate of complications than that attributed to other viruses such as coxsackievirus A16. Circulatory failure secondary to myocardial impairment and neurogenic pulmonary edema secondary to brainstem damage are the main causes of death. Fortunately, the disease is usually benign and resolves in 7 to10 days without sequelae. Given the self-limited nature of most cases, treatment is mainly symptomatic and supportive. Intravenous immunoglobulin should be considered for the treatment of severe/complicated hand, foot, and mouth disease and has been recommended by several national and international guideline committees. Currently, there are no specific antiviral agents approved for the treatment of the disease. Drugs such as ribavirin, suramin, mulberroside C, aminothiazole analogs, and sertraline have emerged as potential candidates for the treatment of hand, foot, and mouth disease. Vaccination of susceptible individuals in high-risk areas and good personal hygiene are important preventative measures to combat the disease.</p><p><strong>Conclusion: </strong>Familiarity of the disease including its atypical manifestations is crucial so that a correct diagnosis can be made, and appropriate treatment initiated. A timely diagnosis can help avoid contact with the affected individual and decrease the risk of an outbreak.</p>","PeriodicalId":29815,"journal":{"name":"Recent Advances in Inflammation & Allergy Drug Discovery","volume":"16 2","pages":"77-95"},"PeriodicalIF":0.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10596704","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
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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