European Journal of Medicinal Chemistry Reports最新文献

{"title":"Potential of apitherapy in the management of cardiovascular diseases","authors":"Rimpa Karmakar,&nbsp;Sakshi Soni,&nbsp;Vandana Soni,&nbsp;Umesh Kumar Patil","doi":"10.1016/j.ejmcr.2025.100256","DOIUrl":"10.1016/j.ejmcr.2025.100256","url":null,"abstract":"<div><div>Apitherapy has been used as an adjunctive medical practice in several countries, and bee products or apitherapeutic agents are being consistently utilized for millennia by humanity to treat and prevent an assortment of illnesses. This review sought to explore the relationship between apitherapy and scientific research and experimental trials utilizing bee products within the domain of cardiology. Numerous studies conducted <em>in vivo</em> along with <em>in vitro</em> indicate that these products may have potential benefits in the prevention and management of cardiovascular diseases (CVDs). This concise review of research reveals new facets of the biological activities of many bee products: honey, propolis, bee venom, pollen, royal jelly, beeswax, and bee bread, as naturally occurring and intriguing remedies for common CVDs. There are undoubtedly some intriguing mechanisms in bee products that aid in the treatment and prevention of CVDs. Future research with larger sample sizes and improved techniques is needed to validate the relationship between bee products and CVD risk factors. Conclusively, bee products seem to have the potential to lower cardiovascular disease risk factors; however, more research is required to fully grasp these benefits. Even if our knowledge of bee products has greatly expanded, it is still crucial to fully utilize its potential, standardize its use, and share the results in academic and non-academic settings to further investigate its potential in the area of cardiology.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"13 ","pages":"Article 100256"},"PeriodicalIF":0.0,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143487774","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}

{"title":"Epigallocatechin-gallate ameliorates polystyrene microplastics-induced oxido-inflammation and mitochondria-mediated apoptosis in testicular cells via modulation of Nrf2/HO-1, /mTOR/Atg-7, and Cx-43/NOX-1 levels","authors":"Mega Obukohwo Oyovwi ,&nbsp;Emeka Williams Ugwuishi ,&nbsp;Onoriode Andrew Udi ,&nbsp;Adedeji David Atere ,&nbsp;Arientare Rume Rotu ,&nbsp;Emmanuel Igho Odokuma ,&nbsp;Victor Oghenekparobo Emojevwe ,&nbsp;Gideon Temitope Olowe ,&nbsp;Eze Kingsley Nwangwa ,&nbsp;Benneth Ben-Azu","doi":"10.1016/j.ejmcr.2024.100243","DOIUrl":"10.1016/j.ejmcr.2024.100243","url":null,"abstract":"<div><div>The study aimed to investigate the impact of Epigallocatechin-gallate (EGCG) on polystyrene microplastics (PS-MPs) induced reproductive anomalies in rats. To induce reproductive toxicity, PS-MPs were administered at a dose of 0.01 mg/kg/bw for several weeks. Following this, rats were treated with oral doses of 80 mg/kg/bw EGCG for 8 weeks. PS-MPs increase MDA levels while decreasing SOD, CAT, and GSH activity. EGCG administration reduces these effects. Inflammatory markers like NF-κB, IL-1β, TNF-α, NOX-1, and NLRP3 inflammasome are upregulated with PS-MPs but downregulated with EGCG treatment. Cx-43, Nrf2, HO-1, mTOR, and Atg-7 decrease with PS-MPs but increase with EGCG co-treatment. PS-MPs also increase NLRP3 levels, but EGCG treatment inhibits this effect. EGCG enhances sperm quality by raising motility, count, viability, and decreasing the ratio of aberrant and dead spermatozoa. Additional evidence for the reduced spermatogenesis was provided by histopathological scoring. Testicular tissue was subjected to PS-MP-induced oxidative stress, apoptosis, and inflammation; however, EGCG therapy reversed these effects and enhanced sperm quality. Overall, the PS-MPs-induced reproductive toxicity in rats appears to have potential for therapy with EGCG supplementation due to the modulation of Nrf2/HO-1, mTOR/Atg-7, and Cx-43/NOX-1 levels, as well as the prevention of mitochondria-mediated apoptosis and oxido-inflammation.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"13 ","pages":"Article 100243"},"PeriodicalIF":0.0,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143160323","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}

{"title":"Design, synthesis, and biological evaluation of new tetrahydropyrimidine derivatives as multitarget anti-inflammatory agents","authors":"Ahmed R. Ali ,&nbsp;Ahmed K. Al-Kubeisi ,&nbsp;Bassma H. Elwakil ,&nbsp;Amira Abd-Elfattah Darwish ,&nbsp;Tahani M. Almutairi ,&nbsp;Maram M. Elshatanofy ,&nbsp;Tareq Q. Alshargabi ,&nbsp;Maged A. El Sawy","doi":"10.1016/j.ejmcr.2025.100259","DOIUrl":"10.1016/j.ejmcr.2025.100259","url":null,"abstract":"<div><div>In an innovative strategy for addressing inflammatory conditions, new 2-oxo-1,2,3,4-tetrahydropyrimidine derivatives were synthesized and subsequently assessed for their multitarget anti-inflammatory effects on various biomarkers, including IL-6, TNF-α, IL-1β, NF-κB, iNOS, MAPK, and ERK, through <em>in vitro</em> experimentation. The presence of LPS was found to significantly increase the levels of IL-6, TNF-α, and IL-1 beta. However, treatment with the tetrahydropyrimidine derivatives, especially compound <strong>4d</strong> with an IC₅₀ value of 0.4–0.69 μM, led to a substantial reduction in these cytokine levels. Furthermore, LPS was observed to upregulate the expression of MAPK and ERK, as well as NF-κB and iNOS, but these were significantly diminished following treatment with the tetrahydropyrimidines, particularly the compound identified as <strong>4d</strong>, which exhibited an IC₅₀ value of 0.2–0.62 μM for NF-κB, iNOS and MAPK. The molecular docking studies conducted on the three enzymes revealed notable binding characteristics and affinities, thereby reinforcing their biological functions.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"13 ","pages":"Article 100259"},"PeriodicalIF":0.0,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143548638","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}

{"title":"Preparation and pharmacological characterization of the enantiomers of the anticancer agent R/S-N-3-cyanophenyl-N'-(6-tert-butoxycarbonylamino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)urea: Identification of the R-enantiomer as the active eutomer","authors":"Michael Schnekenburger ,&nbsp;Eric Goffin ,&nbsp;Matthieu Schoumacher ,&nbsp;Nikolay Tumanov ,&nbsp;Ange Mouithys-Mickalad ,&nbsp;Pascal de Tullio ,&nbsp;Johan Wouters ,&nbsp;Philippe Lebrun ,&nbsp;Marc Diederich ,&nbsp;Bernard Pirotte","doi":"10.1016/j.ejmcr.2024.100244","DOIUrl":"10.1016/j.ejmcr.2024.100244","url":null,"abstract":"<div><div>R/S-N-3-cyanophenyl-N'-(6-tert-butoxycarbonylamino-3,4-dihydro-2,2-dimethyl-2<em>H</em>-1-benzopyran-4-yl)urea (BPDZ 711, <strong>4</strong>) initially designed as a K_ATP channel opener, was found to exhibit diverse biological activities. The compound inhibited insulin release from rat pancreatic islets, indicating a potential effect on glucose metabolism. Oxygraphy measurements on chronic myeloid leukemia (CML) K-562 cells revealed an impact on cellular respiration. Additionally, the compound demonstrated inhibitory activity on histone deacetylase class III enzymes (sirtuins), linking metabolic and epigenetic regulation. This was corroborated by its effect on protein acetylation and modulation of the extracellular pH of treated CML cells. Alterations in CML cells' nuclear morphology and the release of high-mobility group box 1 (HMGB1) protein confirmed mechanisms related to cellular stress and immunogenic cell death. BPDZ 711 preserved the viability of peripheral blood mononuclear cells, thus demonstrating excellent differential toxicity.</div><div>Since BPDZ 711 is a racemate, the present study focused on the preparation of the two enantiomers and examined the possibility that each isomer could display a distinct pharmacological profile. Our data revealed that the R-enantiomer (<strong>5</strong>) of BPDZ 711 was consistently the most biologically active compound (eutomer), making it the reference compound for future drug discovery and development.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"13 ","pages":"Article 100244"},"PeriodicalIF":0.0,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143160324","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}

{"title":"Synthesis, evaluation of the biological activity against Trypanosoma cruzi and Leishmania donovani. Preliminary in silico ADMET studies of 5-nitroimidazole derivatives","authors":"Miguel A. Rodríguez ,&nbsp;Ali Mijoba ,&nbsp;Nereida J. Parra-Giménez ,&nbsp;Zuleyma Blanco ,&nbsp;Katiuska Chávez ,&nbsp;Alirica I. Suárez ,&nbsp;Esteban Fernandez-Moreira ,&nbsp;Hegira Ramírez ,&nbsp;Jaime E. Charris","doi":"10.1016/j.ejmcr.2025.100248","DOIUrl":"10.1016/j.ejmcr.2025.100248","url":null,"abstract":"<div><div>The synthesis and evaluation of the biological activity of a series of 5-nitroimidazole hybrids is described. The structures of the synthesized hybrids were confirmed by spectral analysis FT-IR, ¹H NMR, ¹³C NMR, MS, and by Elemental Analysis. The toxicity (ADME/Tox) assessment study were carried out to predict the molecular properties associated with pharmacokinetic aspects of novel compounds. The trypanocidal and leishmanicidal activities of all synthesized hybrids were evaluated, compounds <strong>7a</strong> and <strong>8b</strong> were active against the epimastigote form of <em>T. cruzi</em>. Compound <strong>10b</strong> showed marginal activity against the promastigote form of <em>L. donovani</em>. Sulfonyl derivative <strong>8b</strong> was the most promising compound with IC₅₀: 9.58 ± 2.02 μM and with a selectivity index (SI) greater than 31.31, that justifies the description as a promising hit for further study as a possible antichagasic agent.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"13 ","pages":"Article 100248"},"PeriodicalIF":0.0,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143264575","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}

{"title":"Photochemical internalization of mRNA using a photosensitizer and nucleic acid carriers","authors":"Hayaki Maemoto ,&nbsp;Ryohei Suzaki ,&nbsp;Kazunori Watanabe ,&nbsp;Keiji Itaka ,&nbsp;Takashi Ohtsuki","doi":"10.1016/j.ejmcr.2024.100242","DOIUrl":"10.1016/j.ejmcr.2024.100242","url":null,"abstract":"<div><div>mRNA has great potential for therapeutic applications because it can encode a variety of proteins and antigens, in addition to advantages over DNA in terms of gene expression without genomic integration, nuclear localization, or transcription. However, therapeutic applications of mRNA require safe and effective delivery into target cells. Therefore, we aimed to investigate photochemical internalization (PCI) as a promising strategy for delivering mRNA to target cells. In this strategy, mRNA is taken up into cells by endocytosis, accumulates in endosomes, and is released in a light-dependent manner from the endosomes using an endosome-accumulating photosensitizer, aluminum phthalocyanine disulfonate (AlPcS_2a), in combination with nucleic acid carrier molecules. We compared the efficacy of various nucleic acid carriers, including branched polyethyleneimine (bPEI) and poly{N'-[N-(2-aminoethyl)-2-aminoethyl] aspartamide} (PAsp(DET)) under the same conditions for PCI-based mRNA delivery. Our results indicated that bPEI and PAsp(DET) at low N/P ratios exhibited efficient light-enhancement of mRNA expression by PCI with AlPcS_2a. Notably, bPEI exhibited the highest light-dependent mRNA delivery among the carriers evaluated (including cationic polymers, cationic peptides, and lipids), whereas PAsp(DET) showed promise for clinical use because of its lower toxicity compared with bPEI. This PCI strategy allows effective cytosolic mRNA delivery at low N/P ratios, thereby reducing cationic carrier molecule-induced cytotoxicity. This method allows spatiotemporal control of protein expression and holds potential for novel light-dependent mRNA therapies. Overall, this study provided valuable insights into optimizing mRNA delivery systems for therapeutic applications.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"13 ","pages":"Article 100242"},"PeriodicalIF":0.0,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143160280","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}

{"title":"Dicentrine and its N-oxide derivatives induces apoptotic and necrotic cell death in prostate cancer cell lines","authors":"Ranyelison S. Machado ,&nbsp;Daniela C. Tristão ,&nbsp;Natália M. Araújo ,&nbsp;Elias Jorge Muniz Seif ,&nbsp;Kayo Alexandre S. da Cruz ,&nbsp;Mirian G. Morale ,&nbsp;Ileana Gabriela S. de Rubio ,&nbsp;João Henrique G. Lago ,&nbsp;Rodrigo E. Tamura","doi":"10.1016/j.ejmcr.2025.100257","DOIUrl":"10.1016/j.ejmcr.2025.100257","url":null,"abstract":"<div><div>As part of our continuous research for the discovery of anticancer natural products, the effects of alkaloid (6a<em>S</em>)-dicentrine (<strong>1</strong>) and its respective (6a<em>S</em>,6<em>S</em>)- (<strong>1a</strong>) and (6a<em>S</em>,6<em>R</em>)-(<strong>1b</strong>) <em>N</em>-oxides against two prostate cancer cell lines (PC3 and DU145) were evaluated for the first time. Alkaloid <strong>1</strong> exhibited IC₅₀ values of 18.43 and 23.53 μM for both tested cells. On the other hand, <strong>1a</strong> demonstrated higher IC₅₀ values (46.36 and 33.85 μM) whereas <strong>1b</strong> displayed reduced activity (IC₅₀ &gt; 50 μM) for both cells. These results suggest that the stereochemistry of the <em>N</em>-oxide moiety plays an important role in the antitumor activity. Molecular docking indicated differential residue interactions between compounds <strong>1</strong>, <strong>1a</strong>, and <strong>1b</strong> with EGFR and TP53 which could result in their differential modulation. Alkaloid <strong>1</strong> induced strong necrotic and apoptotic cell death in all tested cell lines, while <strong>1a</strong> caused reduced necrotic and apoptotic cell death in PC3, a TP53-null cell line, moderate necrotic cell death in DU145, a mutant TP53 cell line, and strong necrotic death in HEK293, an embryonic kidney cell line with wild-type TP53. Alkaloid <strong>1b</strong> did not induce the death of PC3, but induced necrotic cell death in both DU145 and HEK293. The alkaloids were shown to efficiently modulate gene and protein expression and activate TP53 and EGFR pathways with potential implications for targeting tumors with specific TP53 mutations. Altogether, the obtained results showed that (6a<em>S</em>)-dicentrine (<strong>1</strong>) and its N-oxide derivatives, especially <strong>1a</strong>, displayed potential as antitumor agents and justify its continued investigation as a therapeutic candidate.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"13 ","pages":"Article 100257"},"PeriodicalIF":0.0,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143528732","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}

{"title":"Natural products combating EGFR-TKIs resistance in cancer","authors":"Li Xia ,&nbsp;Gaohui Zhu ,&nbsp;Qiyao Peng ,&nbsp;Xiuyang Li ,&nbsp;Xinrong Zou ,&nbsp;Wanping Zhang ,&nbsp;Lulu Zhao ,&nbsp;Xiong Li ,&nbsp;Ping Wu ,&nbsp;Aimin Luo ,&nbsp;Teng Yang ,&nbsp;Meizi Chen ,&nbsp;Teng Liu ,&nbsp;Yongbo Peng","doi":"10.1016/j.ejmcr.2025.100251","DOIUrl":"10.1016/j.ejmcr.2025.100251","url":null,"abstract":"<div><div>The role of natural products in cancer treatment has received substantial attention. Significantly, natural products can interact with multiple targets, which is meaningful in overcoming drug resistance synergistically. Resistance to epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitors (TKIs) is a significant cause of treatment failure in non-small cell lung cancer (NSCLC). In this review, we summarize the main resistance mechanisms to EGFR-TKIs and present that 67 reported natural products (from 2005 to 2024) demonstrate the potential to combat EGFR-TKIs resistance in cancer via at least 30 pathways, mainly including ROS, PD-L1, EGFR, MAPK, mTOR, HSP90, JNK, PTEN, and FOXO. Based on the rule of five evaluation of druggability, we can obtain 37 natural products suitable for further development. This review aims to systematically summarize recent advances of natural products in overcoming EGFR-TKIs resistance, and provide some inspirations for novel drug discovery in cancer including NSCLC.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"13 ","pages":"Article 100251"},"PeriodicalIF":0.0,"publicationDate":"2025-02-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143463840","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}

{"title":"The pyrazolo[4,3-c]pyrazole core as a novel and versatile scaffold for developing dual DYRK1A-CLK1 inhibitors targeting key processes of Alzheimer's disease pathology","authors":"Vaia-Argyro Bakalakou ,&nbsp;Barbara Mavroidi ,&nbsp;Amalia D. Kalampaliki ,&nbsp;Béatrice Josselin ,&nbsp;Stéphane Bach ,&nbsp;Alexios-Leandros Skaltsounis ,&nbsp;Panagiotis Marakos ,&nbsp;Nicole Pouli ,&nbsp;Maria Pelecanou ,&nbsp;Vassilios Myrianthopoulos ,&nbsp;Sandrine Ruchaud ,&nbsp;Ioannis K. Kostakis","doi":"10.1016/j.ejmcr.2024.100193","DOIUrl":"10.1016/j.ejmcr.2024.100193","url":null,"abstract":"<div><p>In the current study, we designed, synthesized, and characterized a series of substituted pyrazolo[4,3-<em>c</em>]pyrazoles. These novel compounds were evaluated <em>in vitro</em> for their inhibitory activity over a panel of protein kinases to determine their potential therapeutic applications against Alzheimer's disease. To gain deeper insight into the binding interactions between the most potent analogues and their respective kinase targets, advanced molecular simulations were performed. In parallel, the ability of pyrazolo[4,3-<em>c</em>]pyrazoles to inhibit Aβ40 aggregation was assessed using biophysical techniques such as circular dichroism and Thioflavin T assays. Our results highlight the specific heterocycle as a highly promising and synthetically versatile scaffold for developing inhibitors of both AD-relevant kinases and amyloid-β aggregation. Although more effort is needed to assess the possibility of developing multi-target inhibitors, pyrazolo[4,3-<em>c</em>]pyrazole analogues demonstrated significant activities against their individual targets, indicating substantial capacity of the heterocyclic scaffold for further optimization toward both directions. Overall, our findings emphasize the potential of properly substituted pyrazolo[4,3-<em>c</em>]pyrazoles as multifunctional agents targeting key processes in Alzheimer's disease pathology.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100193"},"PeriodicalIF":0.0,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2772417424000657/pdfft?md5=002c3aff6565dd193d3d19fb0567762c&pid=1-s2.0-S2772417424000657-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141846847","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}

{"title":"Chitosan nanocarriers: Pioneering encapsulation and targeted delivery of 5-fluorouracil - A comprehensive review","authors":"Mariyeh Rajaei ,&nbsp;Hamid Rashedi ,&nbsp;Fatemeh Yazdian ,&nbsp;Mehrab Pourmadadi ,&nbsp;Abbas Rahdar ,&nbsp;Sadanand Pandey","doi":"10.1016/j.ejmcr.2024.100172","DOIUrl":"https://doi.org/10.1016/j.ejmcr.2024.100172","url":null,"abstract":"<div><p>5-Fluorouracil (5FU) is a common chemotherapy drug for various cancers. It has exhibited large potentials for the treatment of both malignant and premalignant tumors. In the meantime, topical application of 5FU has been limited to surface pre-carcinogenic tumors. So far, a number of nano systems have been developed for encapsulation and targeted delivery of 5FU to improve its solubility, bioavailability, and functional characteristics, leading to the development of, for example, 5FU carriers in topical treatments. Due to their considerable advantages over ordinary therapies, nanotechnology-based drug delivery systems (DDSs), particularly polymeric nanocarriers (PNCs), have led to some sorts of evolution in many fields, including disease diagnosis and DDS. As a naturally occurring polymer, chitosan (CS) has long been regarded because of its biodegradability, biocompatibility, polycationic nature, non-toxicity, and non-allergenic nature. In addition, the pH-responsive nature of CS provides an exact drug dispersion in the cancer environment, converting it a promising carrier system. Utilization of 5-FU into carbon nanocarriers has indicated positive results such as targeted delivery to tumors and prevention of cancer activity. Researchers have successfully synthesized a handful of CS nanocarriers with distinctive characteristics for targeted delivery of 5FU; these come in different forms, including nano-sized particles (NPs), composites (NCs), emulsions (NEs), and fibers (NFs). This study reviews the mechanism of CS in different formulations by analyzing the physicochemical characteristics of the corresponding DDS in terms of morphology, surface charge, release profile, and encapsulation driving force. A more detailed analysis was performed on the most popular pharmaceutical applications of 5FU-loaded CS NPs. Effective facilitation of targeted delivery of 5FU and improvement of its therapeutic effects for various cancers by the CS were also indicated. Herein, the readers are introduced to nanoscale systems based on natural polymers like chitosan as promising platforms for cancer diagnosis and therapy. More recent discoveries on mechanistic anticancer behavior of 5FU-loaded CS NPs was further discussed.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100172"},"PeriodicalIF":0.0,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S277241742400044X/pdfft?md5=d21a89eb5ba26635f02c0456f9397ed5&pid=1-s2.0-S277241742400044X-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141097712","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}