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Natural Products from Marine-Derived Fungi with Anti-Inflammatory Activity. 具有抗炎活性的海洋真菌天然产物
IF 4.9 2区 医学
Marine Drugs Pub Date : 2024-09-25 DOI: 10.3390/md22100433
Yikang Qiu, Shiji Chen, Miao Yu, Jueying Shi, Jiayu Liu, Xiaoyang Li, Jiaxing Chen, Xueping Sun, Guolei Huang, Caijuan Zheng
{"title":"Natural Products from Marine-Derived Fungi with Anti-Inflammatory Activity.","authors":"Yikang Qiu, Shiji Chen, Miao Yu, Jueying Shi, Jiayu Liu, Xiaoyang Li, Jiaxing Chen, Xueping Sun, Guolei Huang, Caijuan Zheng","doi":"10.3390/md22100433","DOIUrl":"https://doi.org/10.3390/md22100433","url":null,"abstract":"<p><p>Inflammation is considered as one of the most primary protective innate immunity responses, closely related to the body's defense mechanism for responding to chemical, biological infections, or physical injuries. Furthermore, prolonged inflammation is undesirable, playing an important role in the development of various diseases, such as heart disease, diabetes, Alzheimer's disease, atherosclerosis, rheumatoid arthritis, and even certain cancers. Marine-derived fungi represent promising sources of structurally novel bioactive natural products, and have been a focus of research for the development of anti-inflammatory drugs. This review covers secondary metabolites with anti-inflammatory activities from marine-derived fungi, over the period spanning August 2018 to July 2024. A total of 285 anti-inflammatory metabolites, including 156 novel compounds and 11 with novel skeleton structures, are described. Their structures are categorized into five categories: terpenoids, polyketides, nitrogen-containing compounds, steroids, and other classes. The biological targets, as well as the in vitro and in vivo screening models, were surveyed and statistically summarized. This paper aims to offer valuable insights to researchers in the exploration of natural products and the discovery of anti-inflammatory drugs.</p>","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"22 10","pages":""},"PeriodicalIF":4.9,"publicationDate":"2024-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11509926/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142516499","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Semisynthesis, Structure Elucidation and Anti-Mycobacterium marinum Activity of a Series of Marine-Derived 14-Membered Resorcylic Acid Lactones with Interesting Ketal Groups. 具有有趣酮基的一系列海洋衍生 14 单元 Resorcylic Acid 内酯的半合成、结构解析和抗褐藻分枝杆菌活性。
IF 4.9 2区 医学
Marine Drugs Pub Date : 2024-09-25 DOI: 10.3390/md22100431
Jun-Na Yin, Cui-Fang Wang, Xiu-Li Zhang, Ya-Jie Cheng, Yan-Wei Wu, Qun Zhang, Chang-Lun Shao, Mei-Yan Wei, Yu-Cheng Gu
{"title":"Semisynthesis, Structure Elucidation and Anti-<i>Mycobacterium marinum</i> Activity of a Series of Marine-Derived 14-Membered Resorcylic Acid Lactones with Interesting Ketal Groups.","authors":"Jun-Na Yin, Cui-Fang Wang, Xiu-Li Zhang, Ya-Jie Cheng, Yan-Wei Wu, Qun Zhang, Chang-Lun Shao, Mei-Yan Wei, Yu-Cheng Gu","doi":"10.3390/md22100431","DOIUrl":"https://doi.org/10.3390/md22100431","url":null,"abstract":"<p><p>The incidence of <i>Mycobacterium marinum</i> infection is on the rise; however, the existing drug treatment cycle is lengthy and often requires multi-drug combination. Therefore, there is a need to develop new and effective anti-<i>M. marinum</i> drugs. Cochliomycin A, a 14-membered resorcylic acid lactone with an acetonide group at C-5' and C-6', exhibits a wide range of antimicrobial, antimalarial, and antifouling activities. To further explore the effect of this structural change at C-5' and C-6' on this compound's activity, we synthesized a series of compounds with a structure similar to that of cochliomycin A, bearing ketal groups at C-5' and C-6'. The <i>R</i>/<i>S</i> configuration of the diastereoisomer at C-13' was further determined through an NOE correlation analysis of CH<sub>3</sub> or CH<sub>2</sub> at the derivative C-13' position and the H-5' and H-6' by means of a 1D NOE experiment. Further comparative <sup>1</sup>H NMR analysis of diastereoisomers showed the difference in the chemical shift (<i>δ</i>) value of the diastereoisomers. The synthetic compounds were screened for their anti-microbial activities in vitro. Compounds <b>15</b>-<b>24</b> and <b>28</b>-<b>35</b> demonstrated promising activity against <i>M. marinum</i>, with MIC<sub>90</sub> values ranging from 70 to 90 μM, closely approaching the MIC<sub>90</sub> of isoniazid. The preliminary structure-activity relationships showed that the ketal groups with aromatic rings at C-5' and C-6' could enhance the inhibition of <i>M. marinum</i>. Further study demonstrated that compounds <b>23</b>, <b>24</b>, <b>29</b>, and <b>30</b> had significant inhibitory effects on <i>M. marinum</i> and addictive effects with isoniazid and rifampicin. Its effective properties make it an important clue for future drug development toward combatting <i>M. marinum</i> resistance.</p>","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"22 10","pages":""},"PeriodicalIF":4.9,"publicationDate":"2024-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11509596/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142503319","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Red Seaweed (Rhodophyta) Phycocolloids: A Road from the Species to the Industry Application. 红藻植物胶质:从物种到产业应用之路。
IF 4.9 2区 医学
Marine Drugs Pub Date : 2024-09-25 DOI: 10.3390/md22100432
Madalena Mendes, João Cotas, Diana Pacheco, Kay Ihle, Alina Hillinger, Miguel Cascais, João Carlos Marques, Leonel Pereira, Ana M M Gonçalves
{"title":"Red Seaweed (Rhodophyta) Phycocolloids: A Road from the Species to the Industry Application.","authors":"Madalena Mendes, João Cotas, Diana Pacheco, Kay Ihle, Alina Hillinger, Miguel Cascais, João Carlos Marques, Leonel Pereira, Ana M M Gonçalves","doi":"10.3390/md22100432","DOIUrl":"https://doi.org/10.3390/md22100432","url":null,"abstract":"<p><p>Seaweed polysaccharides are versatile both in their functions in seaweed physiology and in their practical applications in society. However, their content and quality vary greatly. This review discusses the main factors that influence the yield and quality of polysaccharides, specifically carrageenans and agars (sulfated galactans) found in red algae species (Rhodophyta). In addition, its historical, current, and emerging applications are also discussed. Carrageenan has been influenced mainly by photosynthetically active radiation (PAR) and nitrogen, while its relationship with temperature has not yet been replicated by recent studies. Agar's seasonal trend has also been found to be more ambiguous than stated before, with light, temperature, nutrients, and pH being influencing factors. In this review, it is also shown that, depending on the compound type, seaweed polysaccharides are influenced by very different key factors, which can be crucial in seaweed aquaculture to promote a high yield and quality of polysaccharides. Additionally, factors like the extraction method and storage of polysaccharides also influence the yield and quality of these compounds. This review also highlights the drawbacks and inadequacy inherent from the conventional (or current) extraction technology approaches.</p>","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"22 10","pages":""},"PeriodicalIF":4.9,"publicationDate":"2024-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11509213/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142503317","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Valorization of the Invasive Blue Crabs (Callinectes sapidus) in the Mediterranean: Nutritional Value, Bioactive Compounds and Sustainable By-Products Utilization. 地中海入侵蓝蟹(Callinectes sapidus)的价值:营养价值、生物活性化合物和可持续副产品利用。
IF 4.9 2区 医学
Marine Drugs Pub Date : 2024-09-23 DOI: 10.3390/md22090430
Rosaria Arena, Giuseppe Renda, Giovanna Ottaviani Aalmo, Frédéric Debeaufort, Concetta Maria Messina, Andrea Santulli
{"title":"Valorization of the Invasive Blue Crabs (<i>Callinectes sapidus</i>) in the Mediterranean: Nutritional Value, Bioactive Compounds and Sustainable By-Products Utilization.","authors":"Rosaria Arena, Giuseppe Renda, Giovanna Ottaviani Aalmo, Frédéric Debeaufort, Concetta Maria Messina, Andrea Santulli","doi":"10.3390/md22090430","DOIUrl":"https://doi.org/10.3390/md22090430","url":null,"abstract":"<p><p>The blue crab (<i>Callinectes sapidus</i>), originally from the western Atlantic Ocean, has recently spread to the Mediterranean and is now considered one of the one hundred most invasive species in that region. This opportunistic species, known for its adaptability to different temperatures and salinities, negatively impacts biodiversity and human activities such as fishing and tourism in the Mediterranean. However, the blue crab is gaining interest as a potential food resource due to its high nutritional value and delicate, sweet flavor. Its meat is rich in protein (14% to 30%), omega-3 fatty acids (EPA and DHA) and other essential nutrients beneficial for human health such as vitamins, and minerals. Utilizing this species in the production of new foods could help mitigate the negative impact of its invasiveness and offer economic opportunities. One challenge with this potential resource is the generation of waste. Approximately 6-8 million tonnes of crab shells are produced worldwide each year, leading to disposal problems and concerns regarding environmental sustainability. To improve economic and environmental sustainability, there is a need to valorize these residues, which are an important source of proteins, lipids, chitin, minerals, and pigments that can be processed into high-value-added products. However, especially in areas with industrial pollution, attention should be paid to the heavy metal (Cd and As) contents of blue crab shells. Studies suggest that blue crab by-products can be used in various sectors, reducing environmental impacts, promoting a circular economy, and creating new industrial opportunities.</p>","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"22 9","pages":""},"PeriodicalIF":4.9,"publicationDate":"2024-09-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11433173/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142349542","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Characterization and Genomic Analyses of dsDNA Vibriophage vB_VpaM_XM1, Representing a New Viral Family. dsDNA噬纤维病毒 vB_VpaM_XM1 的特征和基因组分析,它代表了一个新的病毒家族。
IF 4.9 2区 医学
Marine Drugs Pub Date : 2024-09-21 DOI: 10.3390/md22090429
Zuyun Wei, Xuejing Li, Chunxiang Ai, Hongyue Dang
{"title":"Characterization and Genomic Analyses of dsDNA Vibriophage vB_VpaM_XM1, Representing a New Viral Family.","authors":"Zuyun Wei, Xuejing Li, Chunxiang Ai, Hongyue Dang","doi":"10.3390/md22090429","DOIUrl":"https://doi.org/10.3390/md22090429","url":null,"abstract":"<p><p>A novel vibriophage vB_VpaM_XM1 (XM1) was described in the present study. Morphological analysis revealed that phage XM1 had <i>Myovirus</i> morphology, with an oblate icosahedral head and a long contractile tail. The genome size of XM1 is 46,056 bp, with a G + C content of 42.51%, encoding 69 open reading frames (ORFs). Moreover, XM1 showed a narrow host range, only lysing <i>Vibrio xuii</i> LMG 21346 (T) JL2919, <i>Vibrio parahaemolyticus</i> 1.1997, and <i>V. parahaemolyticus</i> MCCC 1H00029 among the tested bacteria. One-step growth curves showed that XM1 has a 20-min latent period and a burst size of 398 plaque-forming units (PFU)/cell. In addition, XM1 exhibited broad pH, thermal, and salinity stability, as well as strong lytic activity, even at a multiplicity of infection (MOI) of 0.001. Multiple genome comparisons and phylogenetic analyses showed that phage XM1 is grouped in a clade with three other phages, including <i>Vibrio</i> phages Rostov 7, X29, and phi 2, and is distinct from all known viral families that have ratified by the standard genomic analysis of the International Committee on Taxonomy of Viruses (ICTV). Therefore, the above four phages might represent a new viral family, tentatively named <i>Weiviridae</i>. The broad physiological adaptability of phage XM1 and its high lytic activity and host specificity indicated that this novel phage is a good candidate for being used as a therapeutic bioagent against infections caused by certain <i>V. parahaemolyticus</i> strains.</p>","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"22 9","pages":""},"PeriodicalIF":4.9,"publicationDate":"2024-09-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11432961/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142349535","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis and Characterization of a Novel Chitosan-Based Nanoparticle-Hydrogel Composite System Promising for Skin Wound Drug Delivery. 新型壳聚糖纳米粒子-水凝胶复合系统的合成与表征,有望用于皮肤伤口给药
IF 4.9 2区 医学
Marine Drugs Pub Date : 2024-09-21 DOI: 10.3390/md22090428
Yueying Huang, Shuting Hao, Jiayu Chen, Mengyuan Wang, Ziheng Lin, Yanan Liu
{"title":"Synthesis and Characterization of a Novel Chitosan-Based Nanoparticle-Hydrogel Composite System Promising for Skin Wound Drug Delivery.","authors":"Yueying Huang, Shuting Hao, Jiayu Chen, Mengyuan Wang, Ziheng Lin, Yanan Liu","doi":"10.3390/md22090428","DOIUrl":"https://doi.org/10.3390/md22090428","url":null,"abstract":"<p><p>As a natural preservative, nisin is widely used in the food industry, while its application in biomedicine is limited due to its susceptibility to interference from external conditions. In this study, a nanoparticle-hydrogel composite system was designed to encapsulate and release nisin. Nisin nanoparticles were identified with a smooth, spherical visual morphology, particle size of 122.72 ± 4.88 nm, polydispersity coefficient of 0.473 ± 0.063, and zeta potential of 23.89 ± 0.37 mV. Based on the sample state and critical properties, three temperature-sensitive hydrogels based on chitosan were ultimately chosen with a rapid gelation time of 112 s, outstanding reticular structure, and optimal swelling ratio of 239.05 ± 7.15%. The composite system exhibited the same antibacterial properties as nisin, demonstrated by the composite system's inhibition zone diameter of 17.06 ± 0.83 mm, compared to 20.20 ± 0.58 mm for nisin, which was attributed to the prolonged release effect of the hydrogel at the appropriate temperature. The composite system also demonstrated good biocompatibility and safety, making it suitable for application as short-term wound dressings in biomedicine due to its low hemolysis rate of less than 2%. In summary, our nanoparticle-based hydrogel composite system offers a novel application form of nisin while ensuring its stability, thereby deepening and broadening the employment of nisin.</p>","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"22 9","pages":""},"PeriodicalIF":4.9,"publicationDate":"2024-09-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11433214/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142349540","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Aquatic Biomaterial Repositories: Comprehensive Guidelines, Recommendations, and Best Practices for Their Development, Establishment, and Sustainable Operation. 水生生物材料库:开发、建立和可持续运营水生生物材料库的综合指南、建议和最佳做法》(Comprehensive Guidelines, Recommendations, and Best Practices for Their Development, Establishment, and Sustainable Operation)。
IF 4.9 2区 医学
Marine Drugs Pub Date : 2024-09-20 DOI: 10.3390/md22090427
Christiana Tourapi, Eleni Christoforou, Susana P Gaudêncio, Marlen I Vasquez
{"title":"Aquatic Biomaterial Repositories: Comprehensive Guidelines, Recommendations, and Best Practices for Their Development, Establishment, and Sustainable Operation.","authors":"Christiana Tourapi, Eleni Christoforou, Susana P Gaudêncio, Marlen I Vasquez","doi":"10.3390/md22090427","DOIUrl":"https://doi.org/10.3390/md22090427","url":null,"abstract":"<p><p>The alarming pace of species extinction severely threatens terrestrial and aquatic ecosystems, undermining the crucial ecological services vital for environmental sustainability and human well-being. Anthropogenic activities, such as urbanization, agriculture, industrialization, and those inducing climate change, intensify these risks, further imperiling biodiversity. Of particular importance are aquatic organisms, pivotal in biodiscovery and biotechnology. They contribute significantly to natural product chemistry, drug development, and various biotechnological applications. To safeguard these invaluable resources, establishing and maintaining aquatic biomaterial repositories (ABRs) is imperative. This review explores the complex landscape of ABRs, emphasizing the need for standardized procedures from collection to distribution. It identifies key legislative and regulatory frameworks, such as the Nagoya Protocol and EU directives, essential for ensuring responsible and equitable biorepository operations. Drawing on extensive literature and database searches, this study compiles existing recommendations and practices into a cohesive framework with which to guide the establishment and sustainable management of ABRs. Through collaborative efforts and adherence to best practices, ABRs can play a transformative role in the future of marine biotechnology and environmental conservation.</p>","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"22 9","pages":""},"PeriodicalIF":4.9,"publicationDate":"2024-09-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11433314/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142349533","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Immunomodulatory Effects of Halichondrin Isolated from Marine Sponges and Its Synthetic Analogs in Oncological Applications. 从海洋海绵中分离的卤虫菊酯及其合成类似物在肿瘤学应用中的免疫调节作用
IF 4.9 2区 医学
Marine Drugs Pub Date : 2024-09-20 DOI: 10.3390/md22090426
Dinusha Shiromala Dissanayake, Dineth Pramuditha Nagahawatta, Jung-Suck Lee, You-Jin Jeon
{"title":"Immunomodulatory Effects of Halichondrin Isolated from Marine Sponges and Its Synthetic Analogs in Oncological Applications.","authors":"Dinusha Shiromala Dissanayake, Dineth Pramuditha Nagahawatta, Jung-Suck Lee, You-Jin Jeon","doi":"10.3390/md22090426","DOIUrl":"https://doi.org/10.3390/md22090426","url":null,"abstract":"<p><p>Marine natural products comprise unique chemical structures and vast varieties of biological activities. This review aims to summarize halichondrin, a marine natural product, and its synthetic analogs along with its therapeutic properties and mechanisms. Halichondrin and its analogs, derived from marine sponges, exhibit potent antineoplastic properties, making them promising candidates for cancer therapeutics. These compounds, characterized by their complex molecular structures, have demonstrated significant efficacy in inhibiting microtubule dynamics, leading to cell cycle arrest and apoptosis in various cancer cell lines. Several types of halichondrins such as halichondrins B, C, norhalichondrin B, and homohalichondrin B have been discovered with similar anticancer and antitumor characteristics. Since naturally available halichondrins show hurdles in synthesis, recent advancements in synthetic methodologies have enabled the development of several halichondrin analogs, such as E7389 (eribulin), which have shown improved therapeutic indices. Eribulin has shown excellent immunomodulatory properties by several mechanisms such as reprogramming tumor microenvironments, facilitating the infiltration and activation of immune cells, and inhibiting microtubule dynamics. Despite promising results, challenges remain in the synthesis and clinical application of these compounds. This review explores the mechanisms underlying the immunomodulatory activity of halichondrin and its analogs in cancer therapy, along with their clinical applications and potential for future drug development.</p>","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"22 9","pages":""},"PeriodicalIF":4.9,"publicationDate":"2024-09-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11432918/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142349537","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis of Marine (-)-Pelorol and Future Perspectives. 海洋 (-)-Pelorol 的合成与未来展望。
IF 4.9 2区 医学
Marine Drugs Pub Date : 2024-09-19 DOI: 10.3390/md22090425
Antonio Rosales Martínez, Ignacio Rodríguez-García
{"title":"Synthesis of Marine (-)-Pelorol and Future Perspectives.","authors":"Antonio Rosales Martínez, Ignacio Rodríguez-García","doi":"10.3390/md22090425","DOIUrl":"https://doi.org/10.3390/md22090425","url":null,"abstract":"<p><p>Meroterpenoid-type marine natural compounds have attracted an increasing amount of attention due to their peculiar chemical structures and their potential for the development of therapeutically important probes. Within this group of substances pelorol stands out; it is a natural compound isolated from marine organisms with a unique structure and an interesting biological profile. In this article, we summarize and highlight the most interesting aspects of the synthetic procedures towards this compound, which have two common key steps. The first is the coupling of a drimanyl derivative with a compound derived from an arene. The second is a Friedel-Crafts cyclization which forms the C ring of the natural product. Despite the synthetic advances achieved so far, we consider that a more efficient synthetic procedures could be carried out, since their synthetic routes are difficult to scale up due to numerous reaction steps and the limitations imposed by the use of some reagents. In this article, we present a new and versatile retrosynthetic analysis of (-)-pelorol and analogs, which is highly desirable for their easy preparation and subsequent broad study of their biological activities. This is a retrosynthetic route that could improve those reported in the literature in terms of cost-effectiveness.</p>","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"22 9","pages":""},"PeriodicalIF":4.9,"publicationDate":"2024-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11433074/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142349541","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Staurosporine as a Potential Treatment for Acanthamoeba Keratitis Using Mouse Cornea as an Ex Vivo Model 以小鼠角膜为体内外模型,用司陶罗孢林治疗棘阿米巴角膜炎的潜力
IF 5.4 2区 医学
Marine Drugs Pub Date : 2024-09-18 DOI: 10.3390/md22090423
Rubén L. Rodríguez-Expósito, Ines Sifaoui, Lizbeth Salazar-Villatoro, Carlos J. Bethencourt-Estrella, José J. Fernández, Ana R. Díaz-Marrero, Robert Sutak, Maritza Omaña-Molina, José E. Piñero, Jacob Lorenzo-Morales
{"title":"Staurosporine as a Potential Treatment for Acanthamoeba Keratitis Using Mouse Cornea as an Ex Vivo Model","authors":"Rubén L. Rodríguez-Expósito, Ines Sifaoui, Lizbeth Salazar-Villatoro, Carlos J. Bethencourt-Estrella, José J. Fernández, Ana R. Díaz-Marrero, Robert Sutak, Maritza Omaña-Molina, José E. Piñero, Jacob Lorenzo-Morales","doi":"10.3390/md22090423","DOIUrl":"https://doi.org/10.3390/md22090423","url":null,"abstract":"Acanthamoeba is a ubiquitous genus of amoebae that can trigger a severe and progressive ocular disease known as Acanthamoeba Keratitis (AK). Furthermore, current treatment protocols are based on the combination of different compounds that are not fully effective. Therefore, an urgent need to find new compounds to treat Acanthamoeba infections is clear. In the present study, we evaluated staurosporine as a potential treatment for Acanthamoeba keratitis using mouse cornea as an ex vivo model, and a comparative proteomic analysis was conducted to elucidate a mechanism of action. The obtained results indicate that staurosporine altered the conformation of actin and tubulin in treated trophozoites of A. castellanii. In addition, proteomic analysis of treated trophozoites revealed that this molecule induced overexpression and a downregulation of proteins related to key functions for Acanthamoeba infection pathways. Additionally, the ex vivo assay used validated this model for the study of the pathogenesis and therapies of AK. Finally, staurosporine eliminated the entire amoebic population and prevented the adhesion and infection of amoebae to the epithelium of treated mouse corneas.","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"7 1","pages":""},"PeriodicalIF":5.4,"publicationDate":"2024-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142252562","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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
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