Current topics in medicinal chemistry最新文献

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Combining Thiophene-Triazole Hybrids with Bothropic Antivenom to Enhance Its Inhibitory Effect Against the Coagulant Activity of Bothrops Jararaca, B. Neuwiedi, and B. Jararacussu Snake Venoms. 噻吩-三唑复合物与Bothropic抗蛇毒血清联合增强对Jararaca、B. Neuwiedi和B. Jararacussu蛇毒凝血活性的抑制作用。
IF 3.3 4区 医学
Current topics in medicinal chemistry Pub Date : 2026-04-15 DOI: 10.2174/0115680266460346260318041601
Brenda Bairral de Oliveira, Eladio Flores Sanchez, Danielle Pagliaminuto Portella, Vitor Francisco Ferreira, Fernando de Carvalho da Silva, Daniel Tadeu Gomes Gonzaga, Andre Lopes Fuly
{"title":"Combining Thiophene-Triazole Hybrids with Bothropic Antivenom to Enhance Its Inhibitory Effect Against the Coagulant Activity of Bothrops Jararaca, B. Neuwiedi, and B. Jararacussu Snake Venoms.","authors":"Brenda Bairral de Oliveira, Eladio Flores Sanchez, Danielle Pagliaminuto Portella, Vitor Francisco Ferreira, Fernando de Carvalho da Silva, Daniel Tadeu Gomes Gonzaga, Andre Lopes Fuly","doi":"10.2174/0115680266460346260318041601","DOIUrl":"https://doi.org/10.2174/0115680266460346260318041601","url":null,"abstract":"<p><strong>Introduction: </strong>Snakebite envenomation causes approximately 5 million incidents, 130,000 deaths, and 400,000 amputations annually worldwide. Thus, the objective of this work was to assess the ability of 16 thiophene-triazole hybrid compounds (6a-6h and 7a-7h) to inhibit the coagulant activity of Bothrops jararaca, B. neuwiedi, and B. jararacussu venoms in combination with commercial antibothropic antivenom.</p><p><strong>Method: </strong>In the experimental prevention protocol, human plasma or commercial fibrinogen was incubated for 60 seconds at 37°C with the study compounds, with or without antivenom, followed by the addition of snake venoms. In the treatment protocol, each venom was incubated with plasma or fibrinogens for 60 seconds at 37°C, and then the study compounds, with or without antivenom, were added to the medium. Clotting was monitored using a digital coagulometer.</p><p><strong>Results: </strong>The study compounds inhibited the coagulation of plasma and fibrinogen caused by B. neuwiedi venom under both protocols, but they did not inhibit B. jararacussu venom under the treatment protocol. Overall, the coagulation inhibition was more effective when the study compounds were mixed with antivenom, and some compounds achieved complete prevention of venom- induced coagulation.</p><p><strong>Discussion: </strong>A combination of compounds with antivenom enhanced efficacy in preventing the coagulant activity of Bothrops venoms.</p><p><strong>Conclusion: </strong>A drug cocktail comprising the most active compounds mixed with antivenom may be a promising strategy to improve the treatment of envenomation by these snake species.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147722018","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}
引用次数: 0
Purpurogallin: A Multi-targeting Benzotropolone with Promising Anti-cancer and Chronic Disease Applications. Purpurogallin:一种具有抗癌和慢性疾病应用前景的多靶点苯并曲polone。
IF 3.3 4区 医学
Current topics in medicinal chemistry Pub Date : 2026-04-10 DOI: 10.2174/0115680266430982260324184212
Navin Kumar Tailor
{"title":"Purpurogallin: A Multi-targeting Benzotropolone with Promising Anti-cancer and Chronic Disease Applications.","authors":"Navin Kumar Tailor","doi":"10.2174/0115680266430982260324184212","DOIUrl":"https://doi.org/10.2174/0115680266430982260324184212","url":null,"abstract":"<p><p>Purpurogallin is a naturally occurring benzotropolone derivative, first isolated from oak nutgalls, and has emerged as a molecule of significant biomedical interest due to its broad spectrum of bioactivities. It exhibits anticancer, antioxidant, anti-inflammatory, anti-platelet, anti-thrombotic, antibacterial, antimalarial, diabetic nephropathy, and neuroprotective properties. Mechanistically, purpurogallin modulates several key signaling pathways, including NF-κB, MAPK, c-Fos, NFATc1, and TNNT2, which are central to inflammation, apoptosis, and cellular proliferation. Its anticancer potential is underscored by its ability to inhibit crucial oncogenic targets such as Pololike kinases (PLKs), xanthine oxidase, and catechol-O-methyltransferase (COMT). These interactions disrupt cancer cell growth, induce apoptosis, and maintain cellular redox homeostasis. Additionally, its structural resemblance to tropolone-based pharmacophores enhances its utility as a scaffold in anticancer drug development, allowing for strategic chemical modifications to improve efficacy and selectivity. Recent research highlights its promise in the treatment of oxidative stressrelated disorders, including diabetic nephropathy and neurodegenerative diseases, through its potent redox-modulating capabilities. This multifaceted bioactivity profile positions purpurogallin as a compelling candidate for therapeutic advancement. This review delves into the current body of evidence on purpurogallin's biological effects, molecular mechanisms, and synthesis, emphasizing its dual functionality in targeting cancer-related signaling and oxidative stress. Such findings support further investigation into its pharmacological optimization and development as a lead compound in future drug discovery efforts.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147671255","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}
引用次数: 0
A Review on the Development of Semisynthetic Phytochemicals in the Discovery of Anticancer Drugs. 半合成植物化学物质在抗癌药物发现中的研究进展。
IF 3.3 4区 医学
Current topics in medicinal chemistry Pub Date : 2026-04-10 DOI: 10.2174/0115680266467530260405204054
Fatma Zehra Alkac, Cem Yamali
{"title":"A Review on the Development of Semisynthetic Phytochemicals in the Discovery of Anticancer Drugs.","authors":"Fatma Zehra Alkac, Cem Yamali","doi":"10.2174/0115680266467530260405204054","DOIUrl":"https://doi.org/10.2174/0115680266467530260405204054","url":null,"abstract":"<p><p>Cancer is a serious public health problem worldwide, and research into the development of new targeted cancer drugs is continuing intensively. A wide variety of approaches have been developed, ranging from traditional cytotoxic agents to modern targeted therapies, antibody-drug conjugates, immunotherapies, and advanced drug delivery systems, etc. The integration of omics strategies, bioinformatics, network pharmacology, molecular docking, molecular dynamics simulation, and artificial intelligence techniques into the process has accelerated the development of modern cancer treatments. While the search for different cancer treatment methods and anticancer drugs continues intensively, semi-synthetic drug designs still attract attention. As most targeted anticancer drugs are insufficient in clinical treatment, natural products and their derivatives are important in new multi-targeted anticancer drug research. Alongside traditional plant-derived anticancer agents, cardamonin, harmin, podophyllotoxin, β-carboline, magnolol, α-onocerin, boehmeriasin A, parthenolide, celastrol, pinosembrin, furochromone, curcumin, diosgenin, betulinic acid, ursolic acid, honokiol, goniodiol, scopoletin, caffeic acid, and pinocembrin derivatives have attracted interest due to their enhanced efficacy and selectivity relative to their natural analogs. These phytochemicals or their derivatives offer new strategies and have the potential to reduce the side effects of traditional treatments and overcome drug resistance. This review aims to discuss recent semisynthetic advancements in natural product research for anticancer drug development. It demonstrates that several semisynthetic anticancer candidates with enhanced selective anticancer effects compared to natural precursors have been developed, and that problems such as low bioactivity, poor solubility, or selectivity issues can be effectively resolved through the rational design of the chemical structures of their natural analogs.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147671032","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}
引用次数: 0
Small Molecule Inhibitors Targeting Pathogenic Protein Aggregation in Neurodegenerative Diseases: Medicinal Chemistry and Mechanistic Insights. 神经退行性疾病中靶向致病性蛋白聚集的小分子抑制剂:药物化学和机制见解。
IF 3.3 4区 医学
Current topics in medicinal chemistry Pub Date : 2026-04-01 DOI: 10.2174/0115680266439510260223082224
Kishna Ram Senwar, Anjali Dhillon, Monu Yadav
{"title":"Small Molecule Inhibitors Targeting Pathogenic Protein Aggregation in Neurodegenerative Diseases: Medicinal Chemistry and Mechanistic Insights.","authors":"Kishna Ram Senwar, Anjali Dhillon, Monu Yadav","doi":"10.2174/0115680266439510260223082224","DOIUrl":"https://doi.org/10.2174/0115680266439510260223082224","url":null,"abstract":"<p><p>A hallmark of Neurodegenerative Diseases (NDs) is protein misfolding, aggregation, and accumulation in specific brain regions. The accumulation of insoluble, misfolded protein aggregates is usually referred to as amyloid formation. This process leads to cellular dysfunction, destruction of neurons, loss of neuronal connections in specific brain areas, and brain damage. Despite the involvement of distinct pathogenic proteins, the underlying mechanisms of misfolding and aggregate formation are remarkably similar across various NDs. In this review, we present a comprehensive overview of the medicinal chemistry and mechanistic insights into phytochemicals and synthetic small molecules with potential for the treatment of neurodegenerative disorders. Various small molecules have been reported to have therapeutic effects by inhibiting the misfolding, aggregation, and accumulation of pathogenic proteins, such as amyloid-β, tau, and α- synuclein. This review mainly covers natural product-derived small molecules, notably polyphenols (including flavonoids and non-flavonoid polyphenols), as well as other phytochemical classes, such as quinones and alkaloids, along with their possible mechanisms of action. In addition, synthetic small molecules, osmolytes, metal chelators, and repurposed drugs for neurodegenerative disorders are thoroughly discussed.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147608161","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}
引用次数: 0
Research Progress on Membranous Nephropathy-Related Antigens and Immune-Targeted Therapy. 膜性肾病相关抗原及免疫靶向治疗研究进展。
IF 3.3 4区 医学
Current topics in medicinal chemistry Pub Date : 2026-03-31 DOI: 10.2174/0115680266410507260224062006
Lu Sui, Zihang Jin, Yilin Meng, Haoze Wu, Ligeer Che, Li Sun
{"title":"Research Progress on Membranous Nephropathy-Related Antigens and Immune-Targeted Therapy.","authors":"Lu Sui, Zihang Jin, Yilin Meng, Haoze Wu, Ligeer Che, Li Sun","doi":"10.2174/0115680266410507260224062006","DOIUrl":"https://doi.org/10.2174/0115680266410507260224062006","url":null,"abstract":"<p><p>Chronic Kidney Disease (CKD) has emerged as a significant global public health concern, with membranous Nephropathy (MN) being the most prevalent pathological type of nephrotic syndrome in adults. MN is classified as an antibody-mediated autoimmune disease. There is a growing interest in the research of MN-related antigens. Furthermore, the treatment of MN predominantly relies on the administration of immunosuppressants, with traditional regimens such as corticosteroids and cyclophosphamide, which have significant side effects, and rituximab, having a 35-40% failure rate, highlighting the critical need for the development of specific and effective immunotherapy strategies. In this review, we summarized the research progress on newly discovered MN-related antigens, including exostosin 1/exostosin 2(EXT1/EXT2), Neural Cell Adhesion Molecule 1 (NCAM-1), Neural Epidermal Growth Factor-like 1 (NELL-1), Contactin 1 (CNTN1), Semaphorin 3B, High-Temperature Recombinant Protein A1 (HTRA1), protocadherin FAT atypical cadherin 1(FAT1) and Protocadherin 7(PCDH7). Among them, NELL-1 and HTRA1 primarily serve as target antigens for primary MN, and their serum antibody titers show a strong correlation with disease activity. While EXT1/EXT2, NCAM1, CNTN-1, and FAT1 mainly act as target antigens for secondary MN. In addition, we evaluated the clinical applications and efficacy of novel immunosuppressants and therapeutic approaches, including new anti-CD20 antibodies, proteasome inhibitors, anti-plasma cell therapies, belimumab, complement inhibitors, and immunoadsorption. The new anti-CD20 agents represented by obalimumab and obinutuzumab, along with anti-plasma cell therapies such as daratumumab, have emerged as ideal alternatives for patients with rituximab resistance. Other therapeutic approaches, including complement inhibitors, immunoadsorption, and belimumab, have also exhibited their unique advantages.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147608205","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}
引用次数: 0
Preparation of Curcumin-Loaded Nanocarriers and its Application on Promoting Wound Healing. 姜黄素纳米载体的制备及其在伤口愈合中的应用。
IF 3.3 4区 医学
Current topics in medicinal chemistry Pub Date : 2026-03-31 DOI: 10.2174/0115680266397479250823161555
Jingyi Yuan, Jie Yu, Lijie Sun, Xiaobo Luo, Yang Liu, Xinrui Wang
{"title":"Preparation of Curcumin-Loaded Nanocarriers and its Application on Promoting Wound Healing.","authors":"Jingyi Yuan, Jie Yu, Lijie Sun, Xiaobo Luo, Yang Liu, Xinrui Wang","doi":"10.2174/0115680266397479250823161555","DOIUrl":"https://doi.org/10.2174/0115680266397479250823161555","url":null,"abstract":"<p><strong>Introduction: </strong>To address curcumin's limitations (e.g., poor solubility and low bioavailability), we developed a curcumin-loaded ZnMgAl-layered double hydroxide nanocomposite (Cur@LDHs), aiming to enhance its therapeutic efficacy in wound healing.</p><p><strong>Methods: </strong>The study involves the preparation of ZnMgAl-LDHs as the carrier and the synthesis of Cur@LDHs composites through co-precipitation. Characterization of the composites is performed using XRD and FT-IR. In vitro release experiments are conducted using the dialysis bag method, and stability tests are performed under different temperature conditions. Biocompatibility and cell migration assays are carried out on human skin fibroblast (HSF) cells. In vivo wound healing studies are performed on a rat model, with histological evaluation and ELISA assays for inflammatory factors.</p><p><strong>Results: </strong>The XRD and FT-IR analyses confirm the successful loading of curcumin onto LDHs. In vitro release experiments show that Cur@LDHs exhibit slow and sustained release characteristics, reducing the cytotoxicity of pure curcumin. Cell migration experiments indicate that Cur@LDHs significantly enhance the migration rate of HSF cells compared to pure curcumin. In vivo studies demonstrate that Cur@LDHs significantly promote wound healing, with reduced inflammatory responses and improved re-epithelialization and collagen deposition. The ELISA results show that Cur@LDHs effectively reduce the levels of IL-1β and TNF-α proteins in traumatic tissues.</p><p><strong>Discussion: </strong>The Cur@LDHs composite demonstrated significant potential in accelerating wound healing by synergizing the sustained release of curcumin with bioactive Zn2+/Mg2+ ions from the hydrotalcite carrier, which promoted fibroblast migration and collagen deposition. This dual-action mechanism-curcumin suppressing early inflammation (evidenced by reduced IL-1β/TNF-α) and LDH-released ions enhancing tissue regeneration-outperformed free curcumin or LDHs alone in both in vitro and in vivo models. While the system improved curcumin's stability and reduced cytotoxicity compared to conventional delivery methods, the study acknowledges limitations such as the lack of environmental simulations (humidity, infection) and a small animal cohort. Nevertheless, the results position Cur@LDHs as a promising bioactive wound dressing capable of stagespecific therapeutic intervention.</p><p><strong>Conclusion: </strong>Cur@LDHs demonstrated enhanced stability, sustained release, and reduced cytotoxicity compared to free curcumin. The composite synergistically accelerated wound healing in vitro (via HSF migration) and in vivo (90% wound closure by day 7 in rats) by modulating inflammation and promoting tissue regeneration. This study supports Cur@LDHs as a promising bioactive wound dressing.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147608151","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}
引用次数: 0
Total Alkaloids of Yanhusuo Attenuate Chronic Cerebral Hypoperfusion-Induced Brain Injury: Mechanisms and Neuroprotection. 炎护索总生物碱对慢性脑低灌注性脑损伤的作用机制及神经保护作用。
IF 3.3 4区 医学
Current topics in medicinal chemistry Pub Date : 2026-03-30 DOI: 10.2174/0115680266432740260106075226
Bing Tian, Shuming Huang, Yutong Song, Biwei Bai, Jing Fang, Xiangming Sun, Chenxue Li, Yue Yang, Wenlan Li
{"title":"Total Alkaloids of Yanhusuo Attenuate Chronic Cerebral Hypoperfusion-Induced Brain Injury: Mechanisms and Neuroprotection.","authors":"Bing Tian, Shuming Huang, Yutong Song, Biwei Bai, Jing Fang, Xiangming Sun, Chenxue Li, Yue Yang, Wenlan Li","doi":"10.2174/0115680266432740260106075226","DOIUrl":"https://doi.org/10.2174/0115680266432740260106075226","url":null,"abstract":"<p><strong>Introduction: </strong>Rhizoma Corydalis, which contains alkaloids as its main active moieties, is widely used in the treatment of cerebrovascular disorders. The present study aimed to investigate the neuroprotective effects and mechanisms of the total alkaloid from Yanhusuo (YHTA) against chronic cerebral hypoperfusion (CCH).</p><p><strong>Methods: </strong>Sixty Sprague-Dawley (SD) rats were randomly divided into sham, model, YHTA lowdose, medium-dose, high-dose, and nimodipine positive group (n=10). A CCH model was established by performing bilateral common carotid artery occlusion. Cognitive function was assessed using behavioral tests, and neuronal morphological alterations were analyzed by histopathology. Immunohistochemistry was used to assess microvessel density and the protein expression of HIF- 1α, VEGF, and VEGFR-2. Neuronal apoptosis was detected by TUNEL assay. The protein levels of HIF-1α, VEGF, VEGFR-2, Bax, and Bcl-2 were measured by Western blotting.</p><p><strong>Results: </strong>YHTA treatment ameliorated CCH-induced cognitive impairment, alleviated neuronal damage, and increased the number of surviving neurons. All doses of YHTA inhibited neuronal apoptosis, which was associated with the upregulation of Bcl-2 and downregulation of Bax expression. Furthermore, YHTA promoted cerebral angiogenesis and upregulated the expression of HIF- 1α, VEGF, and VEGFR-2 proteins.</p><p><strong>Discussion: </strong>These results provide a pharmacological basis for the clinical application of Corydalis in cerebrovascular diseases and identify YHTA as a multi-target agent against vascular cognitive impairment and hypoperfusion-related neurodegeneration.</p><p><strong>Conclusion: </strong>YHTA protects against nerve damage caused by CCH in the hippocampus. The mechanism may involve activation of the HIF-1α/VEGF/VEGFR-2 pathway, modulating the expression of apoptosis-related proteins Bcl-2 and Bax, and inhibiting nerve cell apoptosis, thereby promoting the generation of microvessels in brain tissue, improving blood flow supply, accelerating the repair of neurons, and playing a role in neuroprotection.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147590754","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}
引用次数: 0
Quercetin and Cancer: Molecular Mechanisms and Signaling Pathway Modulation for Therapeutic Benefits. 槲皮素与癌症:治疗益处的分子机制和信号通路调节。
IF 3.3 4区 医学
Current topics in medicinal chemistry Pub Date : 2026-03-30 DOI: 10.2174/0115680266429919260224034527
Md Al Amin, Mehrukh Zehravi, Hasna Bouhenni, Kurratul Aiun Siddika, Jeetendra Kumar Gupta, Rajeshwar Vodeti, Uppuluri Varuna Naga Venkata Arjun, Patibandla Jahnavi, Gayathri K, Ramenani Hari Babu, Abdul Ajeed Mohathasim Billah, P Dharani Prasad, Safia Obaidur Rab, Koula Doukani, Talha Bin Emran
{"title":"Quercetin and Cancer: Molecular Mechanisms and Signaling Pathway Modulation for Therapeutic Benefits.","authors":"Md Al Amin, Mehrukh Zehravi, Hasna Bouhenni, Kurratul Aiun Siddika, Jeetendra Kumar Gupta, Rajeshwar Vodeti, Uppuluri Varuna Naga Venkata Arjun, Patibandla Jahnavi, Gayathri K, Ramenani Hari Babu, Abdul Ajeed Mohathasim Billah, P Dharani Prasad, Safia Obaidur Rab, Koula Doukani, Talha Bin Emran","doi":"10.2174/0115680266429919260224034527","DOIUrl":"https://doi.org/10.2174/0115680266429919260224034527","url":null,"abstract":"<p><p>Quercetin, a natural flavonoid found in vegetables and fruits, has been demonstrated to have potential anticancer properties. This review investigates the molecular mechanisms of quercetin's effectiveness in cancer prevention and treatment. The diverse effects of quercetin on key molecular signaling pathways, including PI3K/Akt, MAPK, NF-κB, and Wnt/β-catenin, are investigated for their roles in cell cycle progression, apoptosis, and metastasis. Quercetin effectively targets specific cancer signaling pathways, demonstrating promising therapeutic benefits such as the inhibition of proliferation, apoptosis, and suppression of metastasis. The review highlights the synergistic effects of quercetin in combination with conventional chemotherapy and radiotherapy, underscoring its potential to overcome drug resistance and enhance treatment efficacy. It investigates the underlying molecular complexities of quercetin's anticancer effects, providing valuable insights for developing targeted therapeutic strategies and optimizing quercetin-based cancer management interventions. The review explores quercetin's potential to combat drug resistance and enhance treatment efficacy, suggesting further research on optimal dosages, treatment regimens, and targeted patient populations. Furthermore, this review highlights quercetin's potent anticancer properties, suggesting further exploration for targeted therapies and improved cancer management strategies.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147590713","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}
引用次数: 0
Unraveling the Antimicrobial and Antibiofilm Activity of Ag-phendione and Cu-phendione Against Multidrug-resistant Klebsiella pneumoniae Using Shotgun Proteomics. 利用鸟枪蛋白组学研究银-苯二酮和铜-苯二酮对耐多药肺炎克雷伯菌的抑菌活性和抗菌膜活性。
IF 3.3 4区 医学
Current topics in medicinal chemistry Pub Date : 2026-03-30 DOI: 10.2174/0115680266427748251230071309
Gabriela Seabra, Victor Corasolla Carregari, Inglid Souza da Mata, Domingos da Silva Leite, Andre Souza Dos Santos, Ana Paula Ferreira Nunes
{"title":"Unraveling the Antimicrobial and Antibiofilm Activity of Ag-phendione and Cu-phendione Against Multidrug-resistant Klebsiella pneumoniae Using Shotgun Proteomics.","authors":"Gabriela Seabra, Victor Corasolla Carregari, Inglid Souza da Mata, Domingos da Silva Leite, Andre Souza Dos Santos, Ana Paula Ferreira Nunes","doi":"10.2174/0115680266427748251230071309","DOIUrl":"https://doi.org/10.2174/0115680266427748251230071309","url":null,"abstract":"<p><strong>Introduction: </strong>Multidrug-resistant (MDR) Klebsiella pneumoniae infections are associated with high mortality, prolonged hospitalization, and limited treatment options, representing a global healthcare challenge. The coordination compounds [Ag(1,10-phenanthroline-5,6- dione)2]ClO4 (Ag-phendione) and [Cu(1,10-phenanthroline-5,6-dione)3(ClO4)2] (Cu-phendione) have previously demonstrated antimicrobial and antibiofilm activity against MDR Gram-negative bacilli.</p><p><strong>Methods: </strong>This study investigated their mechanisms of action by combining classical microbiology with shotgun proteomics. Minimum inhibitory and bactericidal concentrations (MIC/MBC), timekill assay, and antibiofilm effects were determined, while nanoESI-LC-MS/MS identified proteins modulated in MDR K. pneumoniae.</p><p><strong>Results: </strong>MIC values ranged from 3.125 mg/L to 12.5 mg/L for Ag-phendione and from 12.5 mg/L to 50 mg/L for Cu-phendione. Both compounds exhibited early antimicrobial effects ( ≤ 3 h), inhibited biofilm formation, and disrupted mature biofilms in a dose-dependent manner. Proteomic analysis revealed modulation of proteins related to NAD⁺ synthesis, carbohydrate metabolism (notably trehalose), DNA replication and repair, oxidoreductase activity, and plasmid partitioning.</p><p><strong>Discussion: </strong>The modulation of these proteins correlates with the observed antimicrobial and antibiofilm activity of the coordination compounds, suggesting potential targets for further validation. Interestingly, several proteins modulated by these compounds are also affected by classical antibiotics such as meropenem and colistin, suggesting partially convergent mechanisms involving central metabolism and redox homeostasis.</p><p><strong>Conclusion: </strong>Ag-phendione and Cu-phendione are promising candidates for the development of novel therapeutics against MDR K. pneumoniae. Future studies should validate key targets through genetic knockouts or enzyme activity assays to clarify the mechanisms underlying these effects.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147590747","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}
引用次数: 0
Traditional Herbs in Asthma Management: Mechanisms of Action. 传统中药在哮喘治疗中的作用机制。
IF 3.3 4区 医学
Current topics in medicinal chemistry Pub Date : 2026-03-30 DOI: 10.2174/0115680266425544260310044339
Sonia Singh
{"title":"Traditional Herbs in Asthma Management: Mechanisms of Action.","authors":"Sonia Singh","doi":"10.2174/0115680266425544260310044339","DOIUrl":"https://doi.org/10.2174/0115680266425544260310044339","url":null,"abstract":"<p><p>Asthma is a chronic inflammatory respiratory disease that affects millions of individuals globally, with its prevalence steadily rising. Over the past decade, extensive research has been conducted to unravel the molecular and cellular mechanisms underlying asthma. Among these, aberrant T helper type 2 (Th2) inflammation is pivotal, primarily mediated by cytokines such as IL-5, IL-4, and IL-13. Studies indicate that approximately 50% of mild-to-moderate asthma cases and a substantial proportion of chronic asthma cases are driven by Th2-dependent immune responses. In contrast, Th2-low asthma, which does not rely on Th2 cytokines, is mediated by alternative inflammatory pathways involving IL-17 and TNF-α. Recent findings suggest that asthma pathogenesis is not solely dependent on inflammation. Emerging evidence highlights the role of non-inflammatory mechanisms, including protein kinases, adapter proteins, ORMDL3, gasdermin B, and microRNAs, in driving disease progression. These molecules contribute to airway remodeling, hyper-responsiveness, and immune dysregulation, independent of classical inflammatory pathways. Traditional Chinese Medicine (TCM) has long been recognized as a complementary and alternative therapeutic approach for managing asthma. In recent years, scientific research has increasingly validated the efficacy of TCM in alleviating asthma symptoms, making it a focal point for novel drug discovery. Active compounds extracted from Chinese medicinal plants have demonstrated potential in regulating immune responses and modulating key signaling pathways involved in asthma progression. These bioactive ingredients exert their effects at multiple levels, restoring immune equilibrium, reducing airway inflammation, and mitigating bronchial hyperreactivity. By integrating modern scientific methodologies with traditional knowledge, the exploration of Chinese herbal medicine has the potential to yield innovative and effective treatment strategies for asthma, offering new hope to patients worldwide.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147590724","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}
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