Current topics in medicinal chemistry最新文献

{"title":"Recent Advances in Nanocatalyzed One-Pot Sustainable Synthesis of Bioactive N, N-Heterocycles with Anticancer Activities: An Outlook of Medicinal Chemistry.","authors":"Sasadhar Majhi","doi":"10.2174/0115680266311149240822111827","DOIUrl":"https://doi.org/10.2174/0115680266311149240822111827","url":null,"abstract":"<p><p>N-heterocycles represent a predominant and unique class of organic chemistry. They have received a lot of attention due to their important chemical, biomedical, and industrial uses. Food and Drug Administration (FDA) approved about 75% of drugs containing N-based heterocycles, which are currently available in the market. N-Heterocyclic compounds exist as the backbone of numerous natural products and act as crucial intermediates for the construction of pharmaceuticals, veterinary items, and agrochemicals frequently. Among N-based heterocyclic compounds, bioactive N,N-heterocycles constitute a broad spectrum of applications in modern drug discovery and development processes. Cefozopran (antibiotic), omeprazole (antiulcer), enviradine (antiviral), liarozole (anticancer), etc., are important drugs containing N,N-heterocycles. The synthesis of N,Nheterocyclic compounds under sustainable conditions is one of the most active fields because of their significant physiological and biological properties as well as synthetic utility. Current research is demanding the development of greener, cheaper, and milder protocols for the synthesis of N,N-heterocyclic compounds to save mother nature by avoiding toxic metal catalysts, extensive application of energy, and the excessive use of hazardous materials. Nanocatalysts play a profound role in sustainable synthesis because of their larger surface area, tiny size, and minimum energy; they are eco-friendly and safe, and they provide higher yields with selectivity in comparison to conventional catalysts. It is increasingly demanding research to design and synthesize novel bioactive compounds that may help to combat cancer since the major causes of death worldwide are due to cancer. Hence, the important uses of nanocatalysts for the one-pot synthesis of biologically potent N,N-heterocycles with anticancer activities have been presented in this review.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.9,"publicationDate":"2024-09-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142119216","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Phytochemical Profile and Antioxidant and Protective Activities of Various Types of Extracts from Hyssopus officinalis L. and Grindelia robusta Nutt. Herb Grown in Poland","authors":"Monika Michalak, Ewelina Błońska-Sikora, Małgorzata Stryjecka, Martyna Zagórska-Dziok, Marta Klimek-Szczykutowicz, Agnieszka Szopa","doi":"10.2174/0115680266319052240819104310","DOIUrl":"https://doi.org/10.2174/0115680266319052240819104310","url":null,"abstract":"Introduction: The available literature indicates that Hyssopus officinalis and Grindelia robusta are raw materials with great potential for use in prevention and therapy. Therefore, the aims of this study were to assess the phytochemical profile and antioxidant and cytoprotective properties of extracts prepared using various solvents, additionally taking into account different methods of drying the plant material. Methods: Hydrodistilled oil was analysed by GC-MS. The chemical composition of the extracts was estimated by spectrophotometry and the HPLC–DAD method. Antioxidant activity was evaluated using DPPH and FRAP and measuring the intracellular level of ROS. Alamar Blue and Neutral Red tests were used to assess the cytotoxicity of the extracts on skin cells - keratinocytes and fibroblasts. Results: The major components of hyssop essential oil were cis- (44.9%) and trans- (18.2%) pinocamphone, while borneol (16.1%), and α-pinene (12.0%) were predominant in grindelia essential oil. Flavonoids were dominant in the extracts (water:ethanol, water:methanol, and water: glycerol) from hot-air dried hyssop herb, while phenolic acids were the predominant compounds in the grindelia herb extracts. The water:ethanol hyssop extract had the highest total content of flavonoids (42.26 mg CE/mL), among which isoquercitrin and rutin were present in the highest quantities (32.61 mg/mL and 21.47 mg/mL, respectively). In the case of grindelia, the highest total phenolic acid content (26.24 mg CAE/mL) was recorded in the water:ethanol extract, and the dominant compounds among them were 1,5-dicaffeoylquinic and chlorogenic acid (10.85 and 6.39 mg/mL, respectively). The water:ethanol extract from both plants also exhibited the highest antioxidant activity in the DPPH and FRAP tests (79.19% and 1.39 mmol/L, respectively, for grindelia and 67.61% and 1.04 mmol/L for hyssop) and was most effective at reducing the level of ROS in cells. In addition, water:ethanol extracts may have a positive impact on the viability of skin cells in vitro. Conclusion: Water:ethanol extracts from H. officinalis and G. robusta herb are promising sources of active compounds and may find application as natural materials with valuable biological properties, which require further in vitro and in vivo testing.","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":"68 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142184538","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthetic Strategies of Highly Bioactive Scaffold Bis(indolyl)methane Under Greener Condition- A Comprehensive Review","authors":"Arijit Kundu, Chhanda Mukhopadhyay","doi":"10.2174/0115680266319238240821080203","DOIUrl":"https://doi.org/10.2174/0115680266319238240821080203","url":null,"abstract":"Bis(indolyl)Methanes are a major class of heterocycles with considerable promise for technological and biological applications and being fluorescent active as well. Considering the extensive quantity of work on various synthetic techniques, the objective of this study is to measure the previous and current status of research studies related to different types of Bis(indolyl)methane (BIM) derivatives. Currently, research is focused on developing green synthetic strategies for dependable, sustainable and environmentally friendly synthetic processes. The present literature describes the formation of BIM moieties starting from suitable precursors using conventional reaction procedures, as well as reactions mediated by microwaves, ultrasounds, organocatalysts, transition metal catalysts, metal-free ionic liquid catalysts, and other environmentally friendly reaction protocols. The current review discusses the explosive development of different environmentally friendly synthesis routes for bis(indolyl)methane and its analogues during the past few decades. Moreover, this study includes the biological activities such as antibacterial, anticancer, anti-inflammatory, etc., of BIM derivatives, which have been investigated in recent years.","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":"5 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142184536","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Catalase: A Potential Pharmacologic Target for Hydrogen Peroxide in the Treatment of COVID-19","authors":"Aleksandr Urakov, Natalya Urakova, Aleksey Reshetnikov, Aleksey Shklyaev, Vladimir Nikolenko, Anatoly Osipov, Natalya Klyachko, Yulia Sorokina, Nikita Muhutdinov, Sergey Okovityi, Petr Shabanov","doi":"10.2174/0115680266322046240819053909","DOIUrl":"https://doi.org/10.2174/0115680266322046240819053909","url":null,"abstract":": This manuscript is a meta-analysis performed according to PRISMA guidelines. It shows that acute respiratory distress syndrome in COVID-19 complicated by airway obstruction with sputum and mucus, as well as cases of asphyxia with blood, serous fluid, pus, or meconium, can sometimes cause hypoxemia because the medical standard does not include intrapulmonary solutions that release oxygen. One promising avenue for finding and developing the necessary drugs may be the physical-chemical repurposing of hydrogen peroxide solution from antiseptics into inhaled and intrapulmonary mucolytics, pyolytics, and oxygen-releasing antihypoxants by replacing the acidic properties of hydrogen peroxide with alkaline properties. The fact is that an alkaline hydrogen peroxide solution liquefies said biological masses through alkaline saponification of lipid and protein-lipid complexes and simultaneously “blasts” the masses through catalase cleavage of hydrogen peroxide into water and oxygen gas, since these masses are rich in catalase. The results of the first experiments show that inhalation and intrapulmonary injections of alkaline hydrogen peroxide solutions can significantly optimize the treatment of suffocation and hypoxemia. Value of the data: 1. Why are these data useful? These data provide a new perspective way for intrapulmonary drugs and new technologies for the emergency increase of blood oxygenation through the lungs in asphyxia with thick sputum, mucus, pus, meconium and blood. 2. Who can benefit from these data? New drug developers, drug manufacturers, medical professionals providing emergency medical care, as well as pulmonologists, physiatrists, obstetricians and gynecologists can benefit from the data presented in this article. 3. How can these data be used/reused for further insights or development of experiments? These data can be used to develop new drugs and new technologies for the treatment of suffocation and hypoxia in the final stage of COVID-19, severe asthma attacks, purulent obstructive bronchitis, blood asphyxia in cancer and wounded lung in intensive care and anesthesiology departments. In addition, these data can be used to modernize expectorant, mucolytic, pyolytic, hemolytic and meconiolytic and expand the arsenal of intrapulmonary drugs.","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":"7 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142184533","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Harnessing Natural Resources for Advancements in Dengue Virus Treatment","authors":"Nur Aina Najiha Amin Hapis, Nurshamimi Nor Rashid, Yeun-Mun Choo","doi":"10.2174/0115680266312717240821062535","DOIUrl":"https://doi.org/10.2174/0115680266312717240821062535","url":null,"abstract":": Dengue fever, caused by the Dengue virus (DENV) and transmitted by Aedes aegypti mosquitoes, has become endemic in over 100 countries. Despite considerable research, there is a lack of specific drugs for clinical use against dengue. Hence, further exploration to identify anti-- dengue compounds is essential. In recent years, natural products have gained attention for their antiviral properties. Plant-based medicines are particularly appealing due to their safety and low toxicity. This review summarizes natural compounds with potential antiviral activity against DENV, highlighting their mechanisms of action. Various compounds, from traditional herbal remedies to novel plant isolates, show promise against dengue, targeting crucial viral proteins like the envelope protein, proteases, and RNA polymerase. Exploring natural sources of antiviral agents against dengue is crucial. These compounds offer hope for effective treatments and mitigating dengue's global impact.","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":"28 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142184537","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Therapeutic Potential of Quercetin in Diabetic Neuropathy and Retinopathy: Exploring Molecular Mechanisms","authors":"Lunasmrita Saikia, Sm Abdul Aziz Barbhuiya, Kalyani Saikia, Pratap Kalita, Partha Pratim Dutta","doi":"10.2174/0115680266330678240821060623","DOIUrl":"https://doi.org/10.2174/0115680266330678240821060623","url":null,"abstract":"Diabetes mellitus poses a significant health challenge globally, often leading to debilitating complications, such as neuropathy and retinopathy. Quercetin, a flavonoid prevalent in fruits and vegetables, has demonstrated potential therapeutic effects in these conditions due to its antioxidant, anti-inflammatory, and neuroprotective properties. This review summarizes and provides a comprehensive understanding of the molecular mechanisms underlying the efficacy of quercetin in ameliorating diabetic neuropathy and retinopathy. A thorough search was carried out across scientific databases, such as SciFinder, PubMed, and Google Scholar, to gather pertinent literature regarding the effect of quercetin on diabetic neuropathy and retinopathy till February 2024. Preclinical studies indicate that quercetin mitigates neuropathic pain, sensory deficits, and nerve damage associated with diabetic neuropathy by improving neuronal function, reducing DNA damage, regulating pro-inflammatory cytokines, enhancing antioxidant enzyme levels and endothelial function, as well as restoring nerve injuries. In diabetic retinopathy, quercetin shows the potential to preserve retinal structure and function, inhibiting neovascularization, preventing retinal cell death, reducing pro-inflammatory cytokines, and increasing neurotrophic factor levels. Moreover, through modulating key signaling pathways, such as AMP-activated Protein Kinase (AMPK) activation, Glucose Transporter 4 (GLUT 4) upregulation, and insulin secretion regulation, quercetin demonstrates efficacy in reducing oxidative stress and inflammation, thereby protecting nerve and retinal tissues. Despite promising preclinical findings, challenges, such as limited bioavailability, necessitate further research to optimize quercetin’s clinical application in order to establish its optimal dosage, formulation, and long-term efficacy in clinical settings.","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":"24 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142184535","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pro-Inflammatory Signaling Cascade Markers, Oxidative Stress-Inflammatory Signaling Axis, and Chronic Total Occlusion of Tibial Artery in Elderly Patients Suffering from Occlusion of Coronary Arteries","authors":"Xia Li, Yongjuan Zhao, Hualan Zhou, Youdong Hu, Ying Chen, Dianxuan Guo","doi":"10.2174/0115680266306301240821073416","DOIUrl":"https://doi.org/10.2174/0115680266306301240821073416","url":null,"abstract":"Introduction: Oxidative response is a risk factor in the progression of arterial atherosclerosis. Objective: This research study aimed to examine the effects of oxidative response on atherosclerotic susceptibility as well as the development of arteriosclerosis occlusions of the tibial artery through pro-inflammatory mediator genes in elderly patients with occlusion of coronary arteries. Methods: We determined that oxidative stress biomarkers (Malondialdehyde-modified Low-density Lipoprotein (MDA-LDL), Oxidized Low-density Lipoprotein (Ox-LDL) as well as Heme Oxygenase- 1 (HO-1)] and the expressions of pro-inflammatory mediator genes [Toll-like Receptor 4 (TLR4), Nuclear Factor kappa-B (NF-κB), Myeloid Differentiating factor 88 (MyD88) and Growth Arrest-specific gene 6 (GAS6)] have an impact on the severity of arteriosclerosis occlusions of tibial artery in elderly patients suffering from occlusion of coronary arteries. Results: Levels of MDA-LDL, Ox-LDL, HO-1, TLR4, NF-κB, MyD88, and GAS6 were increased in the occlusion of tibial arteries + two-vessel coronary occlusion group compared to the CON group and occlusion of tibial arteries + one-vessel coronary occlusion group, respectively (p &lt; 0.001); they were also elevated in occlusion of tibial arteries + multiple-vessel coronary occlusion group compared to occlusion of tibial arteries + one-vessel coronary occlusion group and occlusion of tibial arteries + two-vessel coronary occlusion group, respectively (P &lt; 0.001). This has indicated the key roles of oxidative stress and pro-inflammatory mediator genes in arteriosclerosis occlusions of tibial artery in elderly patients with occlusion of coronary arteries. Conclusion: Oxidative response may promote the expressions of inflammatory genes and enhance susceptibility to arteriosclerosis occlusions of the tibial artery in elderly patients with chronic total coronary occlusions.","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":"23 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142184534","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Ligand-Based Approach for Multi-Target Drug Discovery: PTML Modeling of Triple-Target Inhibitors.","authors":"Valeria V Kleandrova, M Natália D S Cordeiro, Alejandro Speck-Planche","doi":"10.2174/0115680266325897240815112505","DOIUrl":"https://doi.org/10.2174/0115680266325897240815112505","url":null,"abstract":"<p><strong>Background: </strong>Cancers are complex multi-genetic diseases that should be tackled in multi-target drug discovery scenarios. Computational methods are of great importance to accelerate the discovery of multi-target anticancer agents. Here, we employed a ligand-based approach by combining a perturbation-theory machine learning model derived from an ensemble of multilayer perceptron networks (PTML-EL-MLP) with the Fragment-Based Topological Design (FBTD) approach to rationally design and predict triple-target inhibitors against the cancerrelated proteins named Tropomyosin Receptor Kinase A (TRKA), poly[ADP-ribose] polymerase 1 (PARP-1), and Insulin-like Growth Factor 1 Receptor (IGF1R).</p><p><strong>Methods: </strong>We extracted the chemical and biological data from ChEMBL. We applied the Box- Jenkins approach to generate multi-label topological indices and subsequently created the PTML-EL-MLP model.</p><p><strong>Results: </strong>Our PTML-EL-MLP model exhibited an accuracy of around 80%. The application FBTD permitted the physicochemical and structural interpretation of the PTML-EL-MLP model, thus enabling a) the chemistry-driven analysis of different molecular fragments with a positive influence on the multi-target activity and b) the use of those favorable fragments as building blocks to virtually design four new drug-like molecules. The designed molecules were predicted as triple-target inhibitors against the aforementioned cancer-related proteins.</p><p><strong>Conclusion: </strong>Our study envisages the capabilities of combining PTML modeling with FBTD for the generation of new chemical diversity for multi-target drug discovery in oncology research and beyond.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.9,"publicationDate":"2024-08-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142016620","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Literature-based Survey of Medicinal Plants Since 1900: A Case Study to Treat Cancer in the Sultanate of Oman.","authors":"Asif Khan, Ajmal Khan, Waheed Murad, Sobia Ahsan Halim, Hammad Ahmad Jan, Mohammed Al-Broumi, Ahmed Al-Harrasi","doi":"10.2174/0115680266318053240819100111","DOIUrl":"https://doi.org/10.2174/0115680266318053240819100111","url":null,"abstract":"<p><strong>Ethnopharmacological relevance: </strong>Due to the high prevalence of cancer, researchers for the past decades have made considerable efforts for its management and treatment. Medicinal plants have always been exploited to discover novel anticancer agents. Oman's huge biodiversity has created a rich source of traditional medicine.</p><p><strong>Objective: </strong>The current survey has aimed to document the traditionally used medicinal plants of Oman and their therapeutic role in the treatment of cancer.</p><p><strong>Material method: </strong>This study comprises of literature-based survey through different databases, including Google, Scopus, Google Scholar, Web of Science, Science Direct, Springer Link, BioMed Central and PubMed.</p><p><strong>Results: </strong>The current review revealed a total of 57 plant species that belong to 35 families that are used in the treatment of cancer in Oman. Most documented plants belong to Solanaceae (6 sp.), Apocyanaceae (5 sp.) and Lamiaceae (4 sp.). The literature reveals that the residents of the area mostly use leaves (38.5%) and prepare their recipes in the form of decoction (40.3%). Moreover, herbs are the most dominant life form (43.85%). Among all forms of cancer in Oman, breast (47%), wound (26), and lung cancer (0.5%) were found dominantly. A literature study confirmed that the medicinal plants used for cancer in Oman are rich in phytochemicals such as quercetin, allicin, coumarin, alliin, kaempferol, solamargine, rutin, lupeol, ursolic acid and luteolin that have shown significant biological activities including anti-cancer potential. It reflects the efficacy of these plants to be used as a medicine in clinical trials. Among all, Boswellia sacra Flueck. is of key importance due to the presence Boswellic acid being used for the treatment of different types of cancer.</p><p><strong>Conclusion: </strong>The residents of Oman have great knowledge about the traditional use of medicinal plants for the treatment of various diseases like cancer. The therapeutic potential and physiological efficacy of Omani medicinal plants should be further explored at a molecular level via in vivo and in vitro experiments.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.9,"publicationDate":"2024-08-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142016621","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Protective Effects of Chitosan-Loaded Pomegranate Peel Extract Nanoparticles on Infertility in Diabetic Male Rats.","authors":"Farah Said, Amel Ramadan Omar, Ayman Saber Mohamed, Ahmed Imam Dakrory, Mennatallah H Abdelaziz","doi":"10.2174/0115680266308882240806175831","DOIUrl":"https://doi.org/10.2174/0115680266308882240806175831","url":null,"abstract":"<p><strong>Background: </strong>Diabetes Mellitus (DM) is known to have an impact on the health of the male reproductive system. It is linked to low sperm quality, increased oxidative stress, and an increased generation of reactive oxygen species in the seminal fluid. Pomegranate extract has phenolic compounds and significant protective properties against oxidative stress, male sex hormone disruptions, and sperm abnormalities.</p><p><strong>Objective: </strong>The current study aimed to evaluate the effectiveness of Pomegranate Peel Extract Nanoparticles (PPENPs) on male fertility in diabetic rats.</p><p><strong>Methods: </strong>DM was induced in rats by intraperitoneal injection of streptozotocin (60 mg/kg). Twenty-four rats were divided into four groups, 6 rats in each group: control, DM, DM+empty NPs (60 mg/kg, orally), and DM+PPENPs (60 mg/kg, orally).</p><p><strong>Results: </strong>Administration of PPENPs increased the levels of insulin, FSH, LH, testosterone, catalase, glutathione reduced, and semen fructose. PPENPs also improved sperm quality, as seen by improvements in sperm morphology, motility, count, and the ability of metabolically active spermatozoa to convert blue resazurin dye to pink resorufin. However, PPENPs decreased levels of glucose, malonaldehyde, nitric oxide, and sperm abnormalities. Also, histological investigation of the PPENPs showed improvement in testis tissue architecture and increased the diameter size of seminiferous tubules and germinative layer thickness.</p><p><strong>Conclusion: </strong>Our investigation proved that the treatment of PPENPs has a protective effect on the reproductive system of male diabetic rats, improving fertility parameters, healthy sperm profiles, and the antioxidant system.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.9,"publicationDate":"2024-08-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142016679","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}