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Alpha-lipoic acid alleviates testicular dysfunction induced by olanzapine in male rats, involvement of adiposity, oxidative stress, inflammation, and male hormonal factors α -硫辛酸可减轻奥氮平引起的雄性大鼠睾丸功能障碍、肥胖、氧化应激、炎症和雄性激素因素的参与
Pharmacological Research - Reports Pub Date : 2025-03-01 DOI: 10.1016/j.prerep.2025.100043
Samir AE Bashandy , Fatma A. Morsy , Yousef S. Bashandy , Marawan A. Elbaset , Bassim M.S.A. Mohamed
{"title":"Alpha-lipoic acid alleviates testicular dysfunction induced by olanzapine in male rats, involvement of adiposity, oxidative stress, inflammation, and male hormonal factors","authors":"Samir AE Bashandy ,&nbsp;Fatma A. Morsy ,&nbsp;Yousef S. Bashandy ,&nbsp;Marawan A. Elbaset ,&nbsp;Bassim M.S.A. Mohamed","doi":"10.1016/j.prerep.2025.100043","DOIUrl":"10.1016/j.prerep.2025.100043","url":null,"abstract":"<div><div>Olanzapine, classified as an atypical antipsychotic pharmacological agent, has been linked with the onset of metabolic syndrome and reproductive dysfunction. The objective of this investigation was to examine the protective properties of alpha-lipoic acid (ALA) in counteracting the metabolic and reproductive disturbances induced by olanzapine in a rat model. Adult Wistar rats were allocated into four distinct groups: a control group, an olanzapine-treated group (10 mg/kg), and two groups receiving olanzapine in conjunction with alpha-lipoic acid (50 or 100 mg/kg). The treatment regimen was administered over a duration of 8 weeks. The group exposed to olanzapine exhibited statistically significant reductions in luteinizing hormone, testosterone levels, sperm motility, sperm count, and relative weights of reproductive organs, alongside an elevation in inflammatory markers (TNF-α and IL-6), oxidative stress (MDA, SOD and GSH), sperm abnormalities, body weight gain, and fat deposition when contrasted with control subjects. Notably, the concomitant administration of alpha-lipoic acid (at doses of 50 or 100 mg/kg) resulted in a partial, dose-dependent amelioration of the adverse effects induced by olanzapine. Specifically, alpha-lipoic acid (100 mg/kg) alleviated the harmful consequences of olanzapine on reproductive hormones, sperm quality metrics, organ weights, oxidative stress levels, and inflammatory markers. Furthermore, alpha-lipoic acid exhibited advantageous effects on body weight and fat accumulation. These observations indicate that alpha-lipoic acid may serve as a viable adjunctive therapeutic strategy to mitigate the metabolic and reproductive side effects associated with olanzapine administration. Additional investigations are necessary to clarify the underlying mechanisms of these protective effects and their potential clinical ramifications.</div></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"3 ","pages":"Article 100043"},"PeriodicalIF":0.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144107930","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
Potentiation of endocannabinoid signaling alleviates depressive-like behavior in diabetic mice 内源性大麻素信号增强可减轻糖尿病小鼠的抑郁样行为
Pharmacological Research - Reports Pub Date : 2025-03-01 DOI: 10.1016/j.prerep.2025.100037
Anuradha Kesharwani , Devidas Lahamge , Shubhankar Kumar Singh , Velayutham Ravichandiran , Vipan Kumar Parihar
{"title":"Potentiation of endocannabinoid signaling alleviates depressive-like behavior in diabetic mice","authors":"Anuradha Kesharwani ,&nbsp;Devidas Lahamge ,&nbsp;Shubhankar Kumar Singh ,&nbsp;Velayutham Ravichandiran ,&nbsp;Vipan Kumar Parihar","doi":"10.1016/j.prerep.2025.100037","DOIUrl":"10.1016/j.prerep.2025.100037","url":null,"abstract":"<div><div>People with poorly managed diabetes frequently feel repressed pleasure and are more prone to developing anxiety and depression. The molecular reasons causing the increased incidence of mood and cognitive impairments after hyperglycemia remain unknown. However, current research suggests that disturbances in the endocannabinoid (eCB) system play a critical role in the initiation and progression of diabetes-related mood and cognitive deficits. Our findings reveal that lower levels of two critical eCB, anandamide (AEA) and 2-arachidonoylglycerol (2-AG), in the medial prefrontal cortex (mPFC) are related to increased anxiety-like and depressive-like behavior in diabetic mice. Additionally, the brains of diabetic mice exhibit elevated levels of Fatty Acid Amide Hydrolase (FAAH), an important enzyme involved in the metabolism of AEA and 2AG, which contributes to the polarization of microglia and the promotion of chronic neuroinflammation. Furthermore, cannabidiol (CBD), a non-psychoactive component of cannabis, administered intraperitoneally for two weeks, improves mood and memory in diabetic mice via transforming the eCB system, as evidenced by higher levels of AEA and 2-AG. The cellular changes induced by CBD treatment in the mPFC included notable modulation of microglia towards a beneficial anti-inflammatory M2 phenotype and a reduction in microglial hypertrophy. CBD therapy resulted in several beneficial molecular alterations in the mPFC, such as a reduction in proinflammatory cytokine levels, an elevation in 2AG and AEA, and a suppression of HMGB1-TLR4 pathway activation. The administration of CBD did not influence the activity of the NAPE-PLD and DAGL-α enzymes, responsible for the synthesis of 2AG and AEA. This indicates that the therapeutic benefits of CBD are not dependent on the enhanced synthesis of AEA and 2AG. Additionally, the administration of CBD significantly reduces fasting blood glucose levels in diabetic mice, indicating that the positive effects of CBD on the brain function of diabetic mice are likely facilitated by enhanced glucose metabolism.</div></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"3 ","pages":"Article 100037"},"PeriodicalIF":0.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143833816","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
Chemical structures, extraction methods and health benefits of okra-derived polysaccharides (ODPs): emphasis on their antioxidant, antihyperlipidemic and antidiabetic actions 秋葵多糖的化学结构、提取方法及保健作用:重点介绍其抗氧化、抗高脂血症和抗糖尿病作用
Pharmacological Research - Reports Pub Date : 2025-03-01 DOI: 10.1016/j.prerep.2025.100038
Ahmed Olatunde , Abdulazeez Ridwanullah Eyitayo , Abdulrashid Mohammed , Suleiman Yusuf Alhaji , Abubakar Ibrahim Bawa
{"title":"Chemical structures, extraction methods and health benefits of okra-derived polysaccharides (ODPs): emphasis on their antioxidant, antihyperlipidemic and antidiabetic actions","authors":"Ahmed Olatunde ,&nbsp;Abdulazeez Ridwanullah Eyitayo ,&nbsp;Abdulrashid Mohammed ,&nbsp;Suleiman Yusuf Alhaji ,&nbsp;Abubakar Ibrahim Bawa","doi":"10.1016/j.prerep.2025.100038","DOIUrl":"10.1016/j.prerep.2025.100038","url":null,"abstract":"<div><div>Okra-derived polysaccharides (ODPs) are among the most predominant and prominent complex compounds in okra (<em>Abelmoschus esculentus</em> L. Moench) and have caused increasing interest in the area of functional foods due to their wide applications. Although the literature on their pharmacological properties is still scanty, ODPs show structural diversity and related therapeutic actions, including alleviation of diabetes and related disorders including impaired lipid accumulation and cellular oxidation. In support of their therapeutic potential, these complex compounds confer low toxicity and relatively good bioavailability profiles. The extraction methods for these complex carbohydrates have a significant influence on their extraction yields, monosaccharide compositions, structural characteristics and pharmacological properties. In line with this, rhamnogalacturonan I, II and homogalacturonan were reported to be the most common types. The monomers constituting these complex polysaccharides from okra, including arabinose; galactose; galacturonic acid; glucose; glucuronic acid; mannose and rhamnose, were extracted by different techniques such as ultrasound-assisted, microwave-assisted, pressurized water and hot-water extractions. The present review comprehensively highlights the documented preclinical (<em>in vitro</em> and <em>in vivo</em>) studies on the ameliorative roles of ODPs against diabetes, oxidative stress and hyperlipidemia. However, clinical trials of ODPs against several disorders, including diabetes are yet to be documented. Therefore, these compounds are recommended for clinical investigations and more preclinical studies to further unveil their effectiveness and health-promoting functions against diabetes and related impairments such as cellular oxidation and defective lipid accumulations. Also, this will further establish these complex polysaccharides from okra as functional function agents with therapeutic properties.</div></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"3 ","pages":"Article 100038"},"PeriodicalIF":0.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143888127","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
Alzheimer's disease – An overview of nano herbal formulations 阿尔茨海默病-纳米草药配方概述
Pharmacological Research - Reports Pub Date : 2025-03-01 DOI: 10.1016/j.prerep.2025.100042
Vishal Shivaji Patil , Swapnali Sachin Patil , Snehal Rajendra Patil , Akanksha Shahaji Pawar , Amol Somnath Shete
{"title":"Alzheimer's disease – An overview of nano herbal formulations","authors":"Vishal Shivaji Patil ,&nbsp;Swapnali Sachin Patil ,&nbsp;Snehal Rajendra Patil ,&nbsp;Akanksha Shahaji Pawar ,&nbsp;Amol Somnath Shete","doi":"10.1016/j.prerep.2025.100042","DOIUrl":"10.1016/j.prerep.2025.100042","url":null,"abstract":"<div><h3>Background</h3><div>The progressive neurological condition known as Alzheimer’s disease (AD) mainly affects elderly persons. Memory loss, cognitive decline, and the build-up of beta-amyloid (Aβ) plaques and neurofibrillary tangles in the brain are some of its distinguishing characteristics. The benefits of current treatment choices are limited, generally fail to effectively stop progression of the disease, and are typically linked to adverse effects that lower quality of life.</div></div><div><h3>Main body</h3><div>Herbal medicines are viable solutions for treating AD, according to recent research, especially when paired with nanotechnology. These formulations seek to overcome important issues with traditional treatments, such as poor permeability and low solubility across the blood-brain barrier (BBB). When used with herbal medicine, nanotechnology provides creative answers to these problems that may improve therapeutic delivery and efficacy. With an emphasis on their use in treatment of AD, this paper examines the relationship between herbal medicine and nanotechnology. It looks at the legal environment and intellectual property rights surrounding herbal nanoformulations, emphasizing need for more thorough research to fully comprehend their modes of action and prospective applications. Additionally, it compiles information on patents and ongoing studies, offering a summary of developments in area.</div></div><div><h3>Conclusion</h3><div>The therapy of Alzheimer's disease can be revolutionized by incorporating herbal treatments into nanostructured compositions. Such advances have the potential to transform treatment approaches by boosting therapeutic results and delivery systems. This review highlights the significance of ongoing research and development in this area, providing promise for improved outcomes and more efficient management of Alzheimer's disease patients.</div></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"3 ","pages":"Article 100042"},"PeriodicalIF":0.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144123233","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
Exosomes and their roles in major depressive disorder: An overview of the research progress and perspectives 外泌体及其在重度抑郁症中的作用:研究进展与展望
Pharmacological Research - Reports Pub Date : 2025-03-01 DOI: 10.1016/j.prerep.2025.100035
Mei Tian , Shuo Yi , Zhao Li , Linzhi Li , Liwen Fang , Qin Ru
{"title":"Exosomes and their roles in major depressive disorder: An overview of the research progress and perspectives","authors":"Mei Tian ,&nbsp;Shuo Yi ,&nbsp;Zhao Li ,&nbsp;Linzhi Li ,&nbsp;Liwen Fang ,&nbsp;Qin Ru","doi":"10.1016/j.prerep.2025.100035","DOIUrl":"10.1016/j.prerep.2025.100035","url":null,"abstract":"<div><div>Major depressive disorder, a debilitating neurological disorder, remains enigmatic in its etiology, and current treatments are still inadequate. Therefore, unraveling its pathogenesis and discovering novel therapeutics is imperative. Exosomes are small extracellular nanoscale vesicles containing biomolecules, such as lipids, proteins, and nucleic acids, and have the ability to facilitate intercellular communication. Their potential as diagnostic indicators and therapeutic agents in conditions like autoimmune diseases, cardiovascular diseases, and cancer has been increasingly recognized. This review briefly introduces the relationship between exosomes and major depressive disorder, providing a systematic overview of how exosomal constituents contribute to the pathogenesis and progression. Furthermore, it underscores the significance of exosome research for advancing diagnostic and therapeutic approaches in major depressive disorder, offering a promising avenue for developing more effective clinical strategies.</div></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"3 ","pages":"Article 100035"},"PeriodicalIF":0.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143777158","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Insights into the antibacterial activity of Limosilactobacillus fermentum curd isolate against gram-positive and gram-negative pathogenic bacteria 发酵乳杆菌分离物对革兰氏阳性和革兰氏阴性致病菌抑菌活性的研究
Pharmacological Research - Reports Pub Date : 2025-03-01 DOI: 10.1016/j.prerep.2025.100034
Suchhanda Nandi , Shyamapada Mandal
{"title":"Insights into the antibacterial activity of Limosilactobacillus fermentum curd isolate against gram-positive and gram-negative pathogenic bacteria","authors":"Suchhanda Nandi ,&nbsp;Shyamapada Mandal","doi":"10.1016/j.prerep.2025.100034","DOIUrl":"10.1016/j.prerep.2025.100034","url":null,"abstract":"<div><div>It is widely known that lactic acid bacteria (LAB), commonly found in fermented products like curd, extends health benefits and antibacterial properties, particularly in traditional Chinese medicine (TCM). In spite of the growing demand for sweet curd contained in earthen pots in our region, no research has specifically explored its unique properties. This study aims to address this gap by examining the probiotic characteristics, antibacterial activity and consumer appeal of sweet curd in earthen pots. A sweet curd sample containing in an earthen pot was microbiologically cultured to isolate LAB applying conventional methods and 16S rRNA gene sequencing. The strain thus isolated was identified to be <em>Limosilactobacillus fermentum</em> 406B, showed broad-spectrum antibacterial activity against gram-positive: <em>Staphylococcus aureus</em>, <em>Bacillus cereus</em>, <em>Streptococcus pneumoniae</em> and <em>Listeria monocytogenes</em> and gram-negative: <em>Escherichia coli</em>, <em>Pseudomonas aeruginosa</em>, <em>Acinetobacter baumannii</em> and <em>Proteus vulgaris</em> bacterial pathogens. Antimicrobial property and minimum inhibitory concentration (MIC) were assessed by agar well diffusion and broth dilution method, respectively. Initial tests based on colony morphology, gram staining and biochemical assays confirmed it as a <em>Lactobacillus</em> species, with sequencing confirming its identity as <em>Limosilactobacillus fermentum</em> 406B. The strain demonstrated excellent physiological tolerance to NaCl, bile, low pH and varying temperatures, confirming its suitability as a probiotic. Additionally, safety tests showed that it was non-pathogenic, as it tested negative for gelatinase and DNase production and displayed an acceptable antibiotic susceptibility profile. With a cumulative probiotic potential (CPP) of 100 %, <em>L. fermentum</em> 406B holds significant promise as a probiotic strain. These results underscore the strain’s potential not just in TCM but also as a prospective biotherapeutic agent, considering its extensive antibacterial activity and robust safety profile.</div></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"3 ","pages":"Article 100034"},"PeriodicalIF":0.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143686034","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","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 protective potential of Blighia sapida on the behavioural and hematobiochemical disruption in kerosene-exposed Clarias gariepinus: In Vivo and In Silico evaluation 油皮Blighia sapida对暴露于煤油的Clarias gariepinus行为和血液生化破坏的保护潜力:体内和计算机评价
Pharmacological Research - Reports Pub Date : 2025-03-01 DOI: 10.1016/j.prerep.2025.100036
M.B. Adekola , O.C. Ojelade , S.A. Olurode , T.O. Adebowale , A.O. Akinde , J.T. Apata , A.F. Adesina , P. Oyeyemi , C.U. Alichi , O.T. Ajala
{"title":"The protective potential of Blighia sapida on the behavioural and hematobiochemical disruption in kerosene-exposed Clarias gariepinus: In Vivo and In Silico evaluation","authors":"M.B. Adekola ,&nbsp;O.C. Ojelade ,&nbsp;S.A. Olurode ,&nbsp;T.O. Adebowale ,&nbsp;A.O. Akinde ,&nbsp;J.T. Apata ,&nbsp;A.F. Adesina ,&nbsp;P. Oyeyemi ,&nbsp;C.U. Alichi ,&nbsp;O.T. Ajala","doi":"10.1016/j.prerep.2025.100036","DOIUrl":"10.1016/j.prerep.2025.100036","url":null,"abstract":"<div><h3>Introduction</h3><div>The discharge of petroleum products poses significant toxicological risks to aquatic life and the environment, undermining Sustainable Development Goals (SDG 14). Members of the Sapindaceae family, to which <em>Blighia sapida</em> belongs, have been utilized for the treatment of blood, heart, urinary and mental disorders. The study investigated the protective effects of ethanol extract (EE) from <em>Blighia sapida</em> stem-bark on <em>Clarias gariepinus</em> sub-adults using their behavioral, biochemical, hematological parameters, as well as <em>in silico</em> evaluation.</div></div><div><h3>Methods</h3><div>The study randomly divided 189 <em>Clarias gariepinus</em> into nine groups (G) in triplicates with seven fish to make 27 treatment tanks. The groups were G1: control, G2: 100 mL kerosene, G3: 200 mL kerosene, G4: 100 mL kerosene + 50 mg/kg bwt.EE, G5: 100 mL kerosene + 100 mg/kg bwt.EE, G6: 100 mL kerosene + 150 mg/kg bwt.EE, G7: 200 mL kerosene + 50 mg/kg bwt.EE, G8: 200 mL kerosene + 100 mg/kg bwt.EE, G9: 200 mL kerosene + 150 mg/kg bwt.EE. The experimental setup was repeated every other day for 28 days in a 30 L plastic aquaria. Behavioral parameters such as active swimming, aggression, jumping, air gulping, slothful movement, and feed response were recorded before and during the treatment using the focal sampling technique. Gas chromatography- mass spectrometry (GC-MS) of the ethanol extract was analyzed. <em>In silico</em> molecular docking studies were used to analyze the binding interactions with CYP<sub>450</sub> 2E1.</div></div><div><h3>Results</h3><div>The observed behavioral alterations were normalized in a dose-dependent manner at the end of the experiment, the extract mitigated kerosene-induced biochemical disruptions, reducing ALT, AST, and creatinine levels. The levels of disruptions in hematology at 100- and 200-mL kerosene exposure was restored close to control values. However, the EE displayed amelioration on the effects of kerosene. <em>In silico</em> analysis revealed high negative binding interactions between compounds identified in the extract and CYP 450 2E1. Better docking scores further validate the protective potential of the top three compounds [9-Octadecenoic acid (-7.9 kCal/mol.), (<em>E</em>)-, Hexadecanamide (-7.5 kCal/mol.), 9-Octadecenamide, (<em>Z</em>)- (-7.8 kCal/mol.)] identified in <em>B. sapida</em> ethanol extract against the molecular protein target compared with ademethionine, the standard drug (-6.6 kCal/mol.). The study concluded that <em>Blighia sapida</em> extract shows promises as a sustainable intervention against kerosene-induced toxicity in aquatic organisms. Also, the top three compounds fingerprinted from the extract of this plant, unlike the standard compound, exhibited adequate drug-like properties.</div></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"3 ","pages":"Article 100036"},"PeriodicalIF":0.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143768675","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis, characterization and evaluation of antioxidant and antibacterial activities of novel isatin-derived hydrazone derivatives of N-amino-11-azaartemisinin n-氨基-11-阿扎霉素新型异黄酮衍生腙衍生物的合成、表征及抗氧化抗菌活性评价
Pharmacological Research - Reports Pub Date : 2025-03-01 DOI: 10.1016/j.prerep.2025.100033
Komal Rathi , Priyanka Yadav , Varun Rawat , Aditi Pandey , Achal Mukhija , Biswajit Saha , Ram Awatar Maurya , Ved Prakash Verma
{"title":"Synthesis, characterization and evaluation of antioxidant and antibacterial activities of novel isatin-derived hydrazone derivatives of N-amino-11-azaartemisinin","authors":"Komal Rathi ,&nbsp;Priyanka Yadav ,&nbsp;Varun Rawat ,&nbsp;Aditi Pandey ,&nbsp;Achal Mukhija ,&nbsp;Biswajit Saha ,&nbsp;Ram Awatar Maurya ,&nbsp;Ved Prakash Verma","doi":"10.1016/j.prerep.2025.100033","DOIUrl":"10.1016/j.prerep.2025.100033","url":null,"abstract":"<div><div>The rise of antibiotic-resistant bacterial infections and the associated oxidative stress highlight the urgent need for new therapeutic agents. Artemisinin <strong>1</strong> and isatins are both pharmacologically active compounds with significant antibacterial, antimalarial, anticancer, and antioxidant properties respectively. In this study, we synthesized and biologically evaluated a series of isatin-derived hydrazones <strong>14a-z</strong> of <em>N</em>-amino-11-azaartemisinin, aiming to address gaps in the development of effective drugs for oxidative stress and bacterial infections. The antioxidant activity was assessed through the DPPH radical scavenging assay, revealing compound <strong>14a</strong> (IC₅₀ = 1.54 ± 0.53 μg mL<sup>−1</sup>) as highly potent, comparable to L-ascorbic acid (IC₅₀ = 1.60 ± 0.62 μg mL<sup>−1</sup>). Notably, antibacterial tests highlighted compound <strong>14o</strong> as having superior efficacy (MIC = 0.25 μg mL<sup>−1</sup>) against <em>E. coli</em>, while <strong>14l</strong> exhibited excellent activity (MIC = 0.5 μg mL<sup>−1</sup>) against <em>Bacillus subtilis</em>. In addition to these biological evaluations, we explored the thermodynamic properties of synthesised compounds using isothermal titration calorimetry (ITC) and studied the thermal stability and degradation patterns through thermogravimetric analysis (TGA). These findings underscore the potential of isatin-derived hydrazones as novel drug candidates for combating bacterial infections and free-radical associated conditions, contributing to the ongoing search for innovative therapies in the face of growing resistance and global health challenges.</div></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"3 ","pages":"Article 100033"},"PeriodicalIF":0.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143552297","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Therapeutic potential and bioactive compounds of Apium graveolens: A phytopharmacological review 荆芥的治疗潜力和生物活性成分:植物药理学综述
Pharmacological Research - Reports Pub Date : 2025-03-01 DOI: 10.1016/j.prerep.2025.100039
Ghadi Daoud , Farogh Ahsan , Tarique Mahmood , Shahzadi Bano , Vaseem Ahamad Ansari , Syed Mehdi Hasan Zaidi , Jamal Akhtar Ansari
{"title":"Therapeutic potential and bioactive compounds of Apium graveolens: A phytopharmacological review","authors":"Ghadi Daoud ,&nbsp;Farogh Ahsan ,&nbsp;Tarique Mahmood ,&nbsp;Shahzadi Bano ,&nbsp;Vaseem Ahamad Ansari ,&nbsp;Syed Mehdi Hasan Zaidi ,&nbsp;Jamal Akhtar Ansari","doi":"10.1016/j.prerep.2025.100039","DOIUrl":"10.1016/j.prerep.2025.100039","url":null,"abstract":"<div><div><em>Apium graveolens</em> (<em>A. graveolens</em>), often referred to as celery, is a widely consumed vegetable with a long history of use in traditional medicine. It offers numerous health advantages, such as anti-inflammatory, antioxidant, and antihypertensive properties. Celery is used in both traditional medicine and modern pharmacology for its therapeutic effects. This review is justified to consolidate recent research on its medicinal properties. Emphasizing its therapeutic potential can steer future research and practical applications in pharmaceuticals, enhancing comprehension of its health benefits and encouraging its use in various treatments. Phytochemical studies have discovered numerous bioactive compounds in <em>A. graveolens</em>, such as flavonoids, phenolic acids, coumarins, and essential oils, all of which play a role in its extensive pharmacological effects. Studies have demonstrated that <em>A. graveolens</em> exhibits antioxidant, anti-inflammatory, antimicrobial, antihypertensive, antidiabetic, hepatoprotective, and other pharmacological effects. The presence of compounds such as apigenin, luteolin, and phthalides plays a pivotal role in these therapeutic effects by modulating various biological pathways, including oxidative stress, inflammatory cascades, and lipid metabolism. These compounds also exhibit diuretic effects, promoting urine production and aiding in toxin removal, thereby alleviating stress on the kidneys. The clinical evidence supporting the efficacy of <em>A. graveolens</em> in humans is still limited; its abundant phytochemical profile and new preclinical findings indicate its promise as an adjunctive therapeutic agent. This review provides a scientific basis for the continued exploration and use of <em>A. graveolens</em> in modern medicine, highlighting its role in promoting its pharmacological aspects through its diverse bioactive components.</div></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"3 ","pages":"Article 100039"},"PeriodicalIF":0.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143898640","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
Therapeutic potentials of trihydroxylflavonone-7-rhamnoglucoside against hepatocellular Lesch-Nyhan Syndrome induced by mixture of caffeine and KBrO3 via NOS/cAMP/PKA and DARPP-32, BDNF/TrkB signaling cascades 三羟基黄酮-7-鼠李糖甙通过NOS/cAMP/PKA和DARPP-32、BDNF/TrkB信号级联对咖啡因和KBrO3混合诱导的肝细胞Lesch-Nyhan综合征的治疗潜力
Pharmacological Research - Reports Pub Date : 2025-03-01 DOI: 10.1016/j.prerep.2025.100040
J.K. Akintunde , P. Adeyemi , O.H. Alonge , S.O. Salami , A.D. Ate , T.E. Oladele , O.A. Akinbode , D.A. Fadare
{"title":"Therapeutic potentials of trihydroxylflavonone-7-rhamnoglucoside against hepatocellular Lesch-Nyhan Syndrome induced by mixture of caffeine and KBrO3 via NOS/cAMP/PKA and DARPP-32, BDNF/TrkB signaling cascades","authors":"J.K. Akintunde ,&nbsp;P. Adeyemi ,&nbsp;O.H. Alonge ,&nbsp;S.O. Salami ,&nbsp;A.D. Ate ,&nbsp;T.E. Oladele ,&nbsp;O.A. Akinbode ,&nbsp;D.A. Fadare","doi":"10.1016/j.prerep.2025.100040","DOIUrl":"10.1016/j.prerep.2025.100040","url":null,"abstract":"<div><div>The management of Lesch-Nyhan Syndrome (LNS) associated with hepatocellular toxicosis has remained in the speculative phase. Also, due to numerous pharmacological capacities of 4,5,7-Trihydroxylflavonone-7-rhamnoglucoside popularly known as naringin, it may be a potent therapeutic flavonoid against hepatic LNS. We therefore studied the effect of 4,5,7-Trihydroxylflavonone-7-rhamnoglucoside on rats’ hepatic cells exhibiting LNS through NOS/cAMP/PKA/DARPP-32 and BDNF/TrkB signaling pathways. Sixty-seven male rats were divided into nine (n = 7) groups. Group I received distilled water only. Group II and III were exposed to 100 mg/kg KBrO<sub>3</sub> and 250 mg/kg caffeine, respectively. Group IV was co-exposed to 100 mg/kg KBrO<sub>3</sub> and 250 mg/Kg caffeine. Group V and VI were exposed to 100 mg/kg KBrO<sub>3</sub> each plus 100 mg/kg haloperidol and 50 mg/kg naringin, respectively. Group VII received 250 mg/kg caffeine + 50 mg/kg naringin. Group VIII received 100 mg/kg KBrO<sub>3</sub> + 250 mg/kg caffeine + 50 mg/kg naringin. Group IX received 50 mg/kg naringin. Exposure to KBrO<sub>3</sub> and/or caffeine for 21 days induced hepatocellular damage with alterations of ATP hydrolytic enzymes, neurotransmitter enzymes, arginase, PDE-5<sup>1</sup>, MDA and NO levels. Also, genes associated with hepatic LNS were up-regulated and characterized by periportal inflammation and vascular congestion. Post-treatment with 4,5,7-Trihydroxylflavonone-7-rhamnoglucoside for 14 days reverted the hepatic LNS in an <em>in vivo</em> model. We therefore concluded that bio-stimulation of TrKB/BDNF and DARPP-32 levels by 4,5,7-Trihydroxylflavonone-7-rhamnoglucoside may prolong the functionality of liver among individuals suffering from LNS.</div></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"3 ","pages":"Article 100040"},"PeriodicalIF":0.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143922084","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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