Iranian Journal of Pharmaceutical Research最新文献

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The Glucagon-Like Peptide-1 (GLP-1) Receptor Agonist Liraglutide Regulates Sirtuin-1-Mediated Neutrophil Extracellular Traps to Improve Diabetes-Induced Bone Metabolism Imbalance. 胰高血糖素样肽-1 (GLP-1)受体激动剂利拉鲁肽调节sirtuin -1介导的中性粒细胞胞外陷阱,改善糖尿病诱导的骨代谢失衡。
IF 1.8 4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2024-11-13 eCollection Date: 2024-01-01 DOI: 10.5812/ijpr-148139
Shuai Zhong, Liangzhi Huang, Tingting Lin, Yanyan Li, Bin Deng, Dezhi Kong, Zhanlin Liao, Zugui Huang
{"title":"The Glucagon-Like Peptide-1 (GLP-1) Receptor Agonist Liraglutide Regulates Sirtuin-1-Mediated Neutrophil Extracellular Traps to Improve Diabetes-Induced Bone Metabolism Imbalance.","authors":"Shuai Zhong, Liangzhi Huang, Tingting Lin, Yanyan Li, Bin Deng, Dezhi Kong, Zhanlin Liao, Zugui Huang","doi":"10.5812/ijpr-148139","DOIUrl":"10.5812/ijpr-148139","url":null,"abstract":"<p><strong>Background: </strong>Diabetes mellitus (DM) is a chronic metabolic disorder that disrupts normal bone remodeling.</p><p><strong>Objectives: </strong>This study aimed to investigate how the glucagon-like peptide-1 (GLP-1) receptor agonist liraglutide (LIR) addresses bone metabolism imbalances induced by type-II diabetes.</p><p><strong>Methods: </strong>Type-II diabetic rat models were established through a single intraperitoneal injection of streptozotocin (STZ). Blood glucose levels were measured using a blood glucose meter, and insulin levels were assessed using an assay kit. Bone formation markers [alkaline phosphatase (ALP), osteocalcin (OCN), and procollagen I N-terminal propeptide (PINP)] and bone resorption markers [tartrate-resistant acid phosphatase (TRACP) and CTX-1] were monitored using assay kits. Bone marrow mesenchymal stem cells (BMSCs) were cultured in vitro under high-fat and high-glucose (HFHS) conditions to mimic diabetic bone metabolism dysregulation. Neutrophil extracellular traps (NETs) formation was examined through immunofluorescent staining and Western blot analysis.</p><p><strong>Results: </strong>Liraglutide was found to reduce STZ-induced NETs formation, as indicated by decreased expression of cit-H3 by 36.90% - 53.57%, myeloperoxidase (MPO) by 55.81% - 65.12%, NE by 53.95% - 65.17%, and PAD4 by 46.81% - 63.83%, alongside increased Sirtuin-1 (SIRT1) expression in femur tissue (70.71% - 91.19%). In vitro, LIR enhanced osteogenesis and inhibited apoptosis, effects that were partially reversed by SIRT1 knockdown. Additionally, SIRT1 knockdown partially restored LIR-induced reductions in oxidative stress, inflammation, and NETs formation.</p><p><strong>Conclusions: </strong>LIR mitigates diabetes-induced bone metabolism imbalance by inhibiting NETs formation through SIRT1 mediation.</p>","PeriodicalId":14595,"journal":{"name":"Iranian Journal of Pharmaceutical Research","volume":"23 1","pages":"e148139"},"PeriodicalIF":1.8,"publicationDate":"2024-11-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11892751/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143596880","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Apoptotic Impact of Heliox Cold Plasma on a Cervical Cell Line Using Gold Nanoparticle-Doped Graphene Oxide Nanosheets. 使用金纳米颗粒掺杂氧化石墨烯纳米片的螺旋冷等离子体对子宫颈细胞系细胞凋亡的影响。
IF 1.8 4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2024-11-12 eCollection Date: 2024-01-01 DOI: 10.5812/ijpr-150385
Mahsa Vatani, Simzar Hosseinzadeh, Amirhossein Sari, Hamidreza Ghomi Marzdashti, Azam Rahimpour, Roya Fattahi
{"title":"Apoptotic Impact of Heliox Cold Plasma on a Cervical Cell Line Using Gold Nanoparticle-Doped Graphene Oxide Nanosheets.","authors":"Mahsa Vatani, Simzar Hosseinzadeh, Amirhossein Sari, Hamidreza Ghomi Marzdashti, Azam Rahimpour, Roya Fattahi","doi":"10.5812/ijpr-150385","DOIUrl":"10.5812/ijpr-150385","url":null,"abstract":"<p><strong>Background: </strong>Invasive cervical cancer is recognized as the second most common malignancy in women after breast cancer.</p><p><strong>Objectives: </strong>This study investigates, for the first time, the effect of gold nanoparticle-doped graphene oxide (GO) nanosheets on the human epithelial carcinoma (HeLa) cell line in the presence of heliox cold plasma.</p><p><strong>Methods: </strong>Graphene oxide nanosheets were synthesized using the Hummer method and then doped with gold nanoparticles. The nanoparticles were characterized by transmission electron microscopy (TEM), and the diffraction peaks of GO and gold nanoparticles were confirmed through X-ray diffraction (XRD) analysis. Additionally, the optical absorbance of the nanoparticles was measured in the range of 200 - 900 nm using UV-Visible spectroscopy. A plasma generator was fabricated to produce cold plasma using helium (He) and oxygen (O₂) gases at a 99:1 ratio. The radicals generated by the cold plasma were analyzed via optical emission spectroscopy (OES). Cell treatment was conducted by applying various concentrations of GO and GO/Au nanoparticles. Cellular phenotype was monitored through optical microscopy, and biocompatible concentrations of both nanoparticles were determined using the 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) assay. Subsequently, cold plasma at varying distances and durations was applied to the nanoparticle-treated cells. The generated radicals and the expression of apoptotic genes in treated cells were assessed using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and real-time PCR, respectively.</p><p><strong>Results: </strong>The width of the bacillus-like gold nanoparticles was 15.13 ± 0.96 nm. The cold plasma generated radicals such as N2I2⁺, N2II1⁻, He•, and O⁻•. XRD analysis confirmed the successful coupling of gold onto the GO nanosheets. The biocompatible concentrations of GO and GO/Au nanoparticles were found to be 30 µg/100 µL and 20 µg/100 µL, respectively, as determined by the MTT assay. Radical formation increased as incubation time was extended from 30 to 60 seconds. Furthermore, real-time PCR analysis demonstrated the highest levels of p53, Bax, and caspase 3/8 expression at a plasma exposure time of 60 seconds in the composite-treated group, while Bcl2 expression was significantly reduced.</p><p><strong>Conclusions: </strong>The findings suggest that the parameters of heliox cold plasma and the concentrations of GO/Au nanoparticles must be optimized to effectively induce apoptosis in cervical cancer cells.</p>","PeriodicalId":14595,"journal":{"name":"Iranian Journal of Pharmaceutical Research","volume":"23 1","pages":"e150385"},"PeriodicalIF":1.8,"publicationDate":"2024-11-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11892752/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143596750","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
C-Phycocyanin and Phycocyanobilin as a Novel Adjuvant in Hepatitis B Vaccine. c -藻蓝蛋白和藻蓝胆素作为乙型肝炎疫苗的新型佐剂。
IF 1.8 4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2024-11-09 eCollection Date: 2024-01-01 DOI: 10.5812/ijpr-147060
Nargess Abdali, Reza Tabaripour, Solaleh Javadi, Mehrab Nasirikenari, Mehdi Birjandi, Vahid Siavashi, Mohammad Reza Naghavi, Zahra Hasani, Ali Ahmari, Hossein Hanifi
{"title":"C-Phycocyanin and Phycocyanobilin as a Novel Adjuvant in Hepatitis B Vaccine.","authors":"Nargess Abdali, Reza Tabaripour, Solaleh Javadi, Mehrab Nasirikenari, Mehdi Birjandi, Vahid Siavashi, Mohammad Reza Naghavi, Zahra Hasani, Ali Ahmari, Hossein Hanifi","doi":"10.5812/ijpr-147060","DOIUrl":"https://doi.org/10.5812/ijpr-147060","url":null,"abstract":"<p><strong>Background: </strong>Vaccine adjuvants are components that enhance immune responses to an antigen. Given the importance of adjuvants, research on novel adjuvants with higher efficacy and fewer adverse effects remains crucial. <i>Spirulina</i> (<i>Arthrospira</i> sp.), an aqueous, photosynthetic, filamentous, spiral, multicellular microalga also classified as a cyanobacterium, is well known for its high protein content, vitamins, essential fatty acids, and amino acids. C-phycocyanin (C-PC) is one of the most significant proteins in <i>Spirulina</i>.</p><p><strong>Objectives: </strong>This study aimed to investigate the adjuvant capabilities of three <i>Spirulina</i>-derived substances-<i>Spirulina</i> extract, C-phycocyanin (C-PC), and phycocyanobilin (PCB)-in conjunction with the Hepatitis B surface antigen (HBsAg).</p><p><strong>Methods: </strong>Vaccine groups received the vaccine and adjuvants three times at two-week intervals, administered either orally or by injection in encapsulated or naked forms. To use the injectable form while preventing antigenic effects from the C-PC protein portion, the PCB portion was isolated and used as an injectable adjuvant.</p><p><strong>Results: </strong>The highest levels of interferon gamma (IFN-γ) and interleukin 4 (IL-4) stimulation were observed in the naked PCB form with the vaccine. In both oral and injectable forms of PCB and C-PC, results indicated an increased expression of Hepatitis B surface antibodies (HBsAb) in response to the antigen. The absence of a significant difference between C-PC and <i>Spirulina</i> extract in oral form suggested that the adjuvant effect of this microalga was primarily due to the C-PC compound. Additionally, the injectable form of PCB led to the highest HBsAb expression level. This enhancement of the humoral immune response indicated that these compounds have potential as adjuvants in both oral and injectable forms.</p><p><strong>Conclusions: </strong>These findings suggest the potential for improved Hepatitis B vaccine efficacy with this novel adjuvant, paving the way for further evaluation with other vaccines.</p>","PeriodicalId":14595,"journal":{"name":"Iranian Journal of Pharmaceutical Research","volume":"23 1","pages":"e147060"},"PeriodicalIF":1.8,"publicationDate":"2024-11-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11742379/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143005285","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The COVID-19 Pandemic and the Resilience of the Pharmaceutical Supply Chain: Lessons from Past Experiences and Strategies for the Future. 2019冠状病毒病大流行与药品供应链的复原力:过去的经验教训和未来的战略。
IF 1.8 4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2024-11-05 eCollection Date: 2024-01-01 DOI: 10.5812/ijpr-152723
Mohamad Ali Aivazi, Hamid Reza Rasekh, Mohammad Peikanpour, Farzad Peiravian, Sajjad Esmaeili, Leila Zarei
{"title":"The COVID-19 Pandemic and the Resilience of the Pharmaceutical Supply Chain: Lessons from Past Experiences and Strategies for the Future.","authors":"Mohamad Ali Aivazi, Hamid Reza Rasekh, Mohammad Peikanpour, Farzad Peiravian, Sajjad Esmaeili, Leila Zarei","doi":"10.5812/ijpr-152723","DOIUrl":"https://doi.org/10.5812/ijpr-152723","url":null,"abstract":"<p><strong>Background: </strong>The pharmaceutical supply chain (PSC) faced numerous challenges, particularly during the COVID-19 crisis. Due to the supply chain (SC) 's vulnerabilities, it requires enhanced capabilities to address these challenges. In Iran, specific economic and political issues have intensified the vulnerabilities of the PSC.</p><p><strong>Objectives: </strong>This study investigates the issues caused by the COVID-19 crisis in the PSC, identifies and characterizes these issues, and recommends appropriate courses of action to address future SC disruptions.</p><p><strong>Methods: </strong>This study is a qualitative-quantitative analysis conducted in Iran during the COVID-19 crisis. Qualitative thematic analysis was performed from July 2022 until May 2023. Semi-structured, in-depth, face-to-face interviews with 23 Iranian PSC specialists were conducted until saturation was reached. The qualitative phase was analyzed using MAXQDA 2021. The quantitative phase included a survey of 547 individuals working in pharmaceutical manufacturing in Iran, with the questionnaires analyzed using SPSS 26.</p><p><strong>Results: </strong>In the qualitative phase, the research identified two main themes: (1) vulnerabilities and (2) capabilities, along with 15 subthemes providing solutions to enhance the resilience of the PSC. In the quantitative phase, findings from 64 questionnaires highlighted major vulnerabilities and capabilities necessary to create a resilient SC. The median score for vulnerabilities was 5.12, while the median score for capabilities was 5.39.</p><p><strong>Conclusions: </strong>According to the questionnaire results, the quantitative findings indicate that capabilities received a higher score, suggesting that this sector of the PSC demonstrated better resilience against the pandemic. This study, with its contextual focus, mixed-method approach, comprehensive analysis of vulnerabilities and capabilities, and sector-specific insights, offers a novel contribution to the understanding of SC resilience within Iranian pharmaceutical manufacturing. It also has the potential to promote further research in other sectors of the PSC.</p>","PeriodicalId":14595,"journal":{"name":"Iranian Journal of Pharmaceutical Research","volume":"23 1","pages":"e152723"},"PeriodicalIF":1.8,"publicationDate":"2024-11-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11742386/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143005146","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Curcumin-Etoposide Synergy: Unveiling the Molecular Mechanisms of Enhanced Apoptosis and Chemoresistance Attenuation in Breast Cancer. 姜黄素-依托泊苷协同作用:揭示乳腺癌细胞凋亡增强和化疗耐药衰减的分子机制。
IF 1.8 4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2024-11-05 eCollection Date: 2024-01-01 DOI: 10.5812/ijpr-150978
Bahar Jaberian Asl, Reza Afarin, Mahdi Hatami, Amineh Dehghani Madiseh, Mohammadreza Roshanazadeh, Mojtaba Rashidi
{"title":"Curcumin-Etoposide Synergy: Unveiling the Molecular Mechanisms of Enhanced Apoptosis and Chemoresistance Attenuation in Breast Cancer.","authors":"Bahar Jaberian Asl, Reza Afarin, Mahdi Hatami, Amineh Dehghani Madiseh, Mohammadreza Roshanazadeh, Mojtaba Rashidi","doi":"10.5812/ijpr-150978","DOIUrl":"https://doi.org/10.5812/ijpr-150978","url":null,"abstract":"<p><strong>Background: </strong>Combining natural compounds with chemotherapeutic agents has emerged as a promising approach for cancer treatment. Curcumin (Cur), a natural polyphenol, is known for its anti-cancer properties, including the ability to induce apoptosis and arrest cell cycle progression.</p><p><strong>Objectives: </strong>This study aimed to evaluate the effects of Cur and etoposide (ETO), both individually and in combination, on the induction of apoptosis in breast cancer (BC) cell lines.</p><p><strong>Methods: </strong>The impact of Cur and ETO on cell proliferation was assessed using MTT viability assays. Apoptosis induction by these drugs was evaluated through Annexin V flow cytometry and caspase-3 and caspase-9 activity assays. Quantitative real-time PCR was employed to measure Bax and Bcl-2 gene expression levels. Western blotting was conducted to determine protein levels of p53, p21, Bax, and Bcl-2.</p><p><strong>Results: </strong>A non-significant dose of ETO was selected based on MTT assay results and combined with 75 µM of Cur. Curcumin enhanced ETO's pro-apoptotic effect by increasing caspase activities. The combination of Cur and ETO significantly reduced Bcl-2 gene expression while upregulating Bax expression. Furthermore, treatment with this combination elevated the protein levels of p53, p21, and Bax, compared to ETO or Cur alone, while significantly decreasing Bcl-2 protein levels.</p><p><strong>Conclusions: </strong>Cur has the potential to amplify ETO-induced apoptosis in BC cells. This combination may offer a promising therapeutic approach for BC.</p>","PeriodicalId":14595,"journal":{"name":"Iranian Journal of Pharmaceutical Research","volume":"23 1","pages":"e150978"},"PeriodicalIF":1.8,"publicationDate":"2024-11-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11742740/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143005301","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Effect of Micronized Purified Flavonoid Fraction Containing Hesperidin and Diosmin on Vincristine-Induced Neuropathy in Rats; the Role of Nitric Oxide Pathway. 含橙皮苷和薯蓣皂苷的微量纯化类黄酮提取物对长春新碱所致大鼠神经病变的影响一氧化氮途径的作用
IF 1.8 4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2024-11-02 eCollection Date: 2025-01-01 DOI: 10.5812/ijpr-154455
Nikoo Abharian, Nima Naderi, Noushin Nikray, Mona Khoramjouy, Shokoofe Noori, Hamed Shafaroodi, Mehrdad Faizi
{"title":"Effect of Micronized Purified Flavonoid Fraction Containing Hesperidin and Diosmin on Vincristine-Induced Neuropathy in Rats; the Role of Nitric Oxide Pathway.","authors":"Nikoo Abharian, Nima Naderi, Noushin Nikray, Mona Khoramjouy, Shokoofe Noori, Hamed Shafaroodi, Mehrdad Faizi","doi":"10.5812/ijpr-154455","DOIUrl":"10.5812/ijpr-154455","url":null,"abstract":"<p><strong>Background: </strong>Chemotherapy-induced peripheral neuropathy (CIPN) is a potential complication that can develop following cancer chemotherapy.</p><p><strong>Objectives: </strong>Due to limited medical interventions for the prevention and management of CIPN caused by vincristine, a painful and common complication, further research to find the mechanisms of CIPN and the development of effective preventive and therapeutic strategies is needed.</p><p><strong>Methods: </strong>We induced CIPN in male Wistar rats by administering intraperitoneal vincristine (VCR) at a dose of 0.1 mg/kg for 10 days. Treatment involved micronized purified flavonoid fraction (MPFF) containing hesperidin and diosmin (MPFF; Daflon<sup>®</sup>) at doses of 50, 100, and 200 mg/kg. Our investigation focused on levels of inflammatory factors (TNF-α, IL-6) in the dorsal root ganglion (DRG) tissue and included a series of behavioral tests: Von Frey, grip strength, rotarod, open field, and hot plate tests. To examine the role of the nitric oxide (NO) pathway in the effects of MPFF on VCR-induced peripheral neuropathy (VIPN), we also tested the effect of L-arginine (100 mg/kg i.p.) as a NO precursor and L-NAME (20 mg/kg i.p.) as a nitric oxide synthase (NOS) inhibitor.</p><p><strong>Results: </strong>Based on our behavioral tests, MPFF (50, 100, 200 mg/kg) effectively reduced some symptoms of VIPN, including mechanical allodynia and hyperalgesia. Notably, TNF-α and IL-6 levels in the DRG tissue of the groups treated with 100 and 200 mg/kg of MPFF showed a significant reduction in inflammatory factors. These results underscore the potential of MPFF and the role of the NO signaling pathway in alleviating neuropathic pain caused by VCR.</p><p><strong>Conclusions: </strong>Micronized purified flavonoid fraction may be an effective treatment for VIPN by reducing mechanical allodynia, thermal hyperalgesia, and TNF-α and IL-6 levels in DRG tissue. The NO pathway may play a role in the effectiveness of MPFF in treating VIPN.</p>","PeriodicalId":14595,"journal":{"name":"Iranian Journal of Pharmaceutical Research","volume":"24 1","pages":"e154455"},"PeriodicalIF":1.8,"publicationDate":"2024-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12297021/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144730961","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Dual COX-2/TNF-α Inhibitors as Promising Anti-inflammatory and Cancer Chemopreventive Agents: A Review. COX-2/TNF-α双抑制剂作为抗炎和癌症化学预防药物的研究进展
IF 1.8 4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2024-10-29 eCollection Date: 2024-01-01 DOI: 10.5812/ijpr-151312
Mobina Tajdari, Amirreza Peyrovinasab, Maryam Bayanati, Mohammad Ismail Mahboubi Rabbani, Amir Hossein Abdolghaffari, Afshin Zarghi
{"title":"Dual COX-2/TNF-α Inhibitors as Promising Anti-inflammatory and Cancer Chemopreventive Agents: A Review.","authors":"Mobina Tajdari, Amirreza Peyrovinasab, Maryam Bayanati, Mohammad Ismail Mahboubi Rabbani, Amir Hossein Abdolghaffari, Afshin Zarghi","doi":"10.5812/ijpr-151312","DOIUrl":"10.5812/ijpr-151312","url":null,"abstract":"<p><p>Cyclooxygenases (COX) play a pivotal role in inflammation and are responsible for the production of prostaglandins (PGs). Two types of COXs have been identified as key biological targets for drug design: Constitutive COX-1 and inducible COX-2. Nonsteroidal anti-inflammatory drugs (NSAIDs) target COX-1, while selective COX-2 inhibitors are designed for COX-2. These COX isoforms are involved in multiple physiological and pathological pathways throughout the body. Overproduction of tumor necrosis factor-alpha (TNF-α) plays a role in COX-2's inflammatory activity. Tumor necrosis factor-alpha can contribute to cardiac fibrosis, heart failure, and various cancers by upregulating the COX-2/PGE2 axis. Therefore, suppressing COX activity has emerged as a potentially effective treatment for chronic inflammatory disorders and cancer. This review explores the mechanisms of TNF-α-induced COX-2/PGE2 expression, a significant pathophysiological feature of cancer development. Furthermore, we summarize chemical compounds with dual COX-2/TNF-α inhibitory actions, providing an overview of their structure-activity relationship. These insights may contribute to the development of new generations of dual-acting COX-2/TNF-α inhibitors with enhanced efficacy.</p>","PeriodicalId":14595,"journal":{"name":"Iranian Journal of Pharmaceutical Research","volume":"23 1","pages":"e151312"},"PeriodicalIF":1.8,"publicationDate":"2024-10-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11742592/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143005360","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Dipeptidyl Peptidase-4 Inhibitors: A Systematic Review of Structure-Activity Relationship Studies. 二肽基肽酶-4抑制剂:结构-活性关系研究的系统综述。
IF 1.8 4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2024-10-29 eCollection Date: 2024-01-01 DOI: 10.5812/ijpr-151581
Maryam Bayanati, Mohammad Ismail Mahboubi Rabbani, Shirin Sirous Kabiri, Bahareh Mir, Elham Rezaee, Sayyed Abbas Tabatabai
{"title":"Dipeptidyl Peptidase-4 Inhibitors: A Systematic Review of Structure-Activity Relationship Studies.","authors":"Maryam Bayanati, Mohammad Ismail Mahboubi Rabbani, Shirin Sirous Kabiri, Bahareh Mir, Elham Rezaee, Sayyed Abbas Tabatabai","doi":"10.5812/ijpr-151581","DOIUrl":"10.5812/ijpr-151581","url":null,"abstract":"<p><strong>Context: </strong>Dipeptidyl peptidase 4 (DPP-4) is a serine exopeptidase enzyme that hydrolyzes the amide bond at the N-terminal of peptides. This enzyme converts incretins, such as glucagon-like peptide I and glucose-dependent insulinotropic peptide, into their inactive forms, thereby preventing them from stimulating insulin secretion. Numerous studies have confirmed the role of DPP-4 in the pathophysiology of type 2 diabetes, leading to the development of various DPP-4 inhibitors. In recent years, research on DPP-4 inhibitors has expanded significantly, resulting in the creation of both non-peptidomimetic heterocyclic compounds and peptidomimetic scaffolds.</p><p><strong>Evidence acquisition: </strong>This systematic review summarizes all recent advances related to DPP-4 inhibitors up to 2024. It begins by outlining the biochemical characteristics of DPP-4 and general pharmacological principles of DPP-4 inhibition, followed by an overview of the latest developments from recent publications. The review provides valuable insights into the pharmacophores necessary for ligand-protein interactions, aimed at understanding the structure-activity relationship of novel DPP-4 inhibitors. Data for this review was collected from sources including ScienceDirect, PubMed, and Scopus.</p><p><strong>Results: </strong>This review highlights various chemical scaffolds that have been explored in the development of novel DPP-4 inhibitors. It emphasizes scaffolds with significant DPP-4 inhibitory activity, including azoles, azines, sulfonamides, and quinolone motifs. The article also details the structure-activity relationships of newly developed analogs, providing a comprehensive overview of recent advancements in this area.</p><p><strong>Conclusions: </strong>Despite moderate progress in the development of novel DPP-4 inhibitors, emerging molecular aspects of DPP-4 intervention show great promise for future therapeutic developments.</p>","PeriodicalId":14595,"journal":{"name":"Iranian Journal of Pharmaceutical Research","volume":"23 1","pages":"e151581"},"PeriodicalIF":1.8,"publicationDate":"2024-10-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11892788/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143596757","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Expression of Concern for Paraquat Exposure Up-regulates Cyclooxygenase-2 in the Lungs, Liver, and Kidneys in Rats [Iran J Pharm Res. 2013; 12(4): e125760]. 百草枯暴露对大鼠肺、肝、肾中环氧合酶-2表达的影响[J] . journal of nurses training; 2013;12 (4): e125760]。
IF 1.8 4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2024-10-28 eCollection Date: 2024-01-01 DOI: 10.5812/ijpr-151659
Editor-In-Chief Ijpr
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引用次数: 0
Advancements and Applications of Artificial Intelligence in Pharmaceutical Sciences: A Comprehensive Review. 人工智能在制药科学中的进展与应用综述
IF 1.8 4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2024-10-15 eCollection Date: 2024-01-01 DOI: 10.5812/ijpr-150510
Negar Mottaghi-Dastjerdi, Mohammad Soltany-Rezaee-Rad
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引用次数: 0
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