Pub Date : 2025-03-18DOI: 10.1007/s13659-025-00501-2
Olusesan Ojo, Idris Njanje, Dele Abdissa, Tarryn Swart, Roxanne L. Higgitt, Rosemary A. Dorrington
The rapid emergence of drug-resistant microbial pathogens has posed challenges to global health in the twenty-first century. This development has significantly made most antibiotics ineffective in the treatment of infections they cause, resulting in increasing treatment costs and annual death rates. To address the challenge posed by these pathogens, we explore the potential of secondary metabolites from Aspergillus species as a source of new and effective therapeutic agents to treat drug-resistant infections. Terpenoids, a distinct group of natural products, are extensively distributed in plants and fungi, and have been attributed with significant antibacterial, anticancer, and antiviral activities. In this review, we present an overview of Aspergillus species, and review the novel terpenoids isolated from them from 2019 to April 2024, highlighting anti-infective activity against members of the ESKAPE pathogens. We further focus on the strategies through which the structural framework of these new terpenoids could be modified and/or optimized to feed a pipeline of new lead compounds targeting microbial pathogens. Overall, this review provides insight into the therapeutic applications of terpenoids sourced from Aspergillus species and the potential for the discovery of new compounds from these fungi to combat antimicrobial resistance.
Graphical Abstract
{"title":"Newly isolated terpenoids (covering 2019–2024) from Aspergillus species and their potential for the discovery of novel antimicrobials","authors":"Olusesan Ojo, Idris Njanje, Dele Abdissa, Tarryn Swart, Roxanne L. Higgitt, Rosemary A. Dorrington","doi":"10.1007/s13659-025-00501-2","DOIUrl":"10.1007/s13659-025-00501-2","url":null,"abstract":"<div><p>The rapid emergence of drug-resistant microbial pathogens has posed challenges to global health in the twenty-first century. This development has significantly made most antibiotics ineffective in the treatment of infections they cause, resulting in increasing treatment costs and annual death rates. To address the challenge posed by these pathogens, we explore the potential of secondary metabolites from <i>Aspergillus</i> species as a source of new and effective therapeutic agents to treat drug-resistant infections. Terpenoids, a distinct group of natural products, are extensively distributed in plants and fungi, and have been attributed with significant antibacterial, anticancer, and antiviral activities. In this review, we present an overview of <i>Aspergillus</i> species, and review the novel terpenoids isolated from them from 2019 to April 2024, highlighting anti-infective activity against members of the ESKAPE pathogens. We further focus on the strategies through which the structural framework of these new terpenoids could be modified and/or optimized to feed a pipeline of new lead compounds targeting microbial pathogens. Overall, this review provides insight into the therapeutic applications of terpenoids sourced from <i>Aspergillus</i> species and the potential for the discovery of new compounds from these fungi to combat antimicrobial resistance.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":718,"journal":{"name":"Natural Products and Bioprospecting","volume":"15 1","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-03-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s13659-025-00501-2.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143638552","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Phytochemical study of the n-BuOH extract of Ilex asprella resulted in the discovery of ten new pentacyclic triterpenoid glycosides, comprising nine ursane-type glycosides (1−9) and one oleanane-type glycoside (10), along with seven known compounds (11−17). Compound 1 is the first reported 19,22-epoxy ursane triterpenoid glycoside, whereas 4 and 5 are rare examples of ursane triterpenoid glycosides containing a 28,19-lactone group. The structural characterization of these compounds was achieved using spectroscopic and chemical techniques, as well as single-crystal X-ray analysis. Compounds 7, 12, 15, and 17 exhibited moderate cytotoxic activities against H1975 and HCC827 cancer cells.
Graphical abstract
{"title":"Asprecosides A–J, ten new pentacyclic triterpenoid glycosides with cytotoxic activity from the roots of Ilex asprella","authors":"Yuwei Wu, Baihui Zhang, Wenxian Li, Lihua Peng, Weilin Qiao, Wei Li, De-an Guo","doi":"10.1007/s13659-025-00499-7","DOIUrl":"10.1007/s13659-025-00499-7","url":null,"abstract":"<div><p>Phytochemical study of the <i>n</i>-BuOH extract of <i>Ilex asprella</i> resulted in the discovery of ten new pentacyclic triterpenoid glycosides, comprising nine ursane-type glycosides (<b>1</b>−<b>9</b>) and one oleanane-type glycoside (<b>10</b>), along with seven known compounds (<b>11</b>−<b>17</b>). Compound <b>1</b> is the first reported 19,22-epoxy ursane triterpenoid glycoside, whereas <b>4</b> and <b>5</b> are rare examples of ursane triterpenoid glycosides containing a 28,19-lactone group. The structural characterization of these compounds was achieved using spectroscopic and chemical techniques, as well as single-crystal X-ray analysis. Compounds <b>7</b>, <b>12</b>, <b>15</b>, and <b>17</b> exhibited moderate cytotoxic activities against H1975 and HCC827 cancer cells.</p><h3>Graphical abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":718,"journal":{"name":"Natural Products and Bioprospecting","volume":"15 1","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-03-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s13659-025-00499-7.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143602380","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Five novel emestrin-type epipolythiodioxopiperazines (ETPs), prenylemestrins C−G (1–5), along with two known ETPs, prenylemestrin A (6) and prenylemestrin B (7), were obtained from Aspergillus nidulans. Their structures were characterized by spectroscopic data, X-ray crystallographic data, ECD comparisons and calculations. Prenylemestrins C−G (1 − 5) represent a rare class of ETPs, characterized by a 2,5-dithia-7,9-diazabicyclo[4.2.2]decane-8,10-dione core involving a hemiterpene moiety. Notably, compound 6 exhibited moderate cytotoxicity, inducing G2/M cell cycle arrest and apoptosis of L1210 cells by regulating the PI3K/AKT signaling pathway and mitochondrial apoptotic mechanisms.
Graphical Abstract
{"title":"Emestrin-type epipolythiodioxopiperazines from Aspergillus nidulans with cytotoxic activities by regulating PI3K/AKT and mitochondrial apoptotic pathways","authors":"Pengkun Li, Qin Li, Aimin Fu, Yang Xiao, Chunmei Chen, Hucheng Zhu, Changxing Qi, Wei Wei, Yuan Zhou, Yonghui Zhang","doi":"10.1007/s13659-025-00498-8","DOIUrl":"10.1007/s13659-025-00498-8","url":null,"abstract":"<div><p>Five novel emestrin-type epipolythiodioxopiperazines (ETPs), prenylemestrins C−G (<b>1</b>–<b>5</b>), along with two known ETPs, prenylemestrin A (<b>6</b>) and prenylemestrin B (<b>7</b>), were obtained from <i>Aspergillus nidulans</i>. Their structures were characterized by spectroscopic data, X-ray crystallographic data, ECD comparisons and calculations. Prenylemestrins C−G (<b>1</b> − <b>5</b>) represent a rare class of ETPs, characterized by a 2,5-dithia-7,9-diazabicyclo[4.2.2]decane-8,10-dione core involving a hemiterpene moiety. Notably, compound <b>6</b> exhibited moderate cytotoxicity, inducing G2/M cell cycle arrest and apoptosis of L1210 cells by regulating the PI3K/AKT signaling pathway and mitochondrial apoptotic mechanisms.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":718,"journal":{"name":"Natural Products and Bioprospecting","volume":"15 1","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-03-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s13659-025-00498-8.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143581091","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Natural products play a crucial role in new drug development, but their druggability is often limited by uncertain molecular targets and insufficient research on mechanisms of action. In this study, we developed a new RPL19-TRAPKI-seq method, combining CRISPR/Cas9 and TRAP technologies, to investigate these mechanisms. We identified and validated seven ribosomal large subunit surface proteins suitable for TRAP, selecting RPL19 for its high enrichment. We successfully established a stable cell line expressing EGFP-RPL19 using CRISPR knock-in and verified its efficiency and specificity in enriching ribosomes and translating mRNA. Integrated with next-generation sequencing, this method allows precise detection of translating mRNA. We validated RPL19-TRAPKI-seq by investigating rapamycin, an mTOR inhibitor, yielding results consistent with previous reports. This optimized TRAP technology provides an accurate representation of translating mRNA, closely reflecting protein expression levels. Furthermore, we investigated SBF-1, a 23-oxa-analog of natural saponin OSW-1 with significant anti-tumor activity but an unclear mechanism. Using RPL19-TRAPKI-seq, we found that SBF-1 exerts its cytotoxic effects on tumor cells by disturbing cellular oxidative phosphorylation. In conclusion, our method has been proven to be a promising tool that can reveal the mechanisms of small molecules with greater accuracy, setting the stage for future exploration of small molecules and advancing the fields of pharmacology and therapeutic development.
Graphical Abstract
{"title":"Advanced RPL19-TRAPKI-seq method reveals mechanism of action of bioactive compounds","authors":"Di Zhu, Junchi Hu, Renke Tan, Xiaofeng Lin, Ruina Wang, Junyan Lu, Biao Yu, Yongmei Xie, Xiaohua Ni, Chunmin Liang, Yongjun Dang, Wei Jiang","doi":"10.1007/s13659-025-00500-3","DOIUrl":"10.1007/s13659-025-00500-3","url":null,"abstract":"<div><p>Natural products play a crucial role in new drug development, but their druggability is often limited by uncertain molecular targets and insufficient research on mechanisms of action. In this study, we developed a new RPL19-TRAP<sup>KI</sup>-seq method, combining CRISPR/Cas9 and TRAP technologies, to investigate these mechanisms. We identified and validated seven ribosomal large subunit surface proteins suitable for TRAP, selecting RPL19 for its high enrichment. We successfully established a stable cell line expressing EGFP-RPL19 using CRISPR knock-in and verified its efficiency and specificity in enriching ribosomes and translating mRNA. Integrated with next-generation sequencing, this method allows precise detection of translating mRNA. We validated RPL19-TRAP<sup>KI</sup>-seq by investigating rapamycin, an mTOR inhibitor, yielding results consistent with previous reports. This optimized TRAP technology provides an accurate representation of translating mRNA, closely reflecting protein expression levels. Furthermore, we investigated SBF-1, a 23-oxa-analog of natural saponin OSW-1 with significant anti-tumor activity but an unclear mechanism. Using RPL19-TRAP<sup>KI</sup>-seq, we found that SBF-1 exerts its cytotoxic effects on tumor cells by disturbing cellular oxidative phosphorylation. In conclusion, our method has been proven to be a promising tool that can reveal the mechanisms of small molecules with greater accuracy, setting the stage for future exploration of small molecules and advancing the fields of pharmacology and therapeutic development.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":718,"journal":{"name":"Natural Products and Bioprospecting","volume":"15 1","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-03-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s13659-025-00500-3.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143554085","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Ganoderma polysaccharides (GPs), derived from various species of the Ganoderma genus, exhibit diverse bioactivities, including immune modulation, anti-tumor effects, and gut microbiota regulation. These properties position GPs as dual-purpose agents for medicinal and functional food development. This review comprehensively explores the structural complexity of six key GPs and their specific mechanisms of action, such as TLR signaling in immune modulation, apoptosis pathways in anti-tumor activity, and their prebiotic effects on gut microbiota. Additionally, the structure–activity relationships (SARs) of GPs are highlighted to elucidate their biological efficacy. Advances in green extraction techniques, including ultrasonic-assisted and enzymatic methods, are discussed for their roles in enhancing yield and aligning with sustainable production principles. Furthermore, the review addresses biotechnological innovations in polysaccharide biosynthesis, improving production efficiency and making large-scale production feasible. These insights, combined with ongoing research into their bioactivity, provide a solid foundation for developing health-promoting functional food products that incorporate GPs. Furthermore, future research directions are suggested to optimize biosynthesis pathways and fully harness the health benefits of these polysaccharides.
Graphical abstract
{"title":"Structure–function insights of natural Ganoderma polysaccharides: advances in biosynthesis and functional food applications","authors":"Zhou-Wei Wu, Xue-Fang Zhao, Chen-Xi Quan, Xiao-Cui Liu, Xin-Yu Tao, Yu-jie Li, Xing-Rong Peng, Ming-Hua Qiu","doi":"10.1007/s13659-025-00496-w","DOIUrl":"10.1007/s13659-025-00496-w","url":null,"abstract":"<div><p><i>Ganoderma</i> polysaccharides (GPs), derived from various species of the <i>Ganoderma</i> genus, exhibit diverse bioactivities, including immune modulation, anti-tumor effects, and gut microbiota regulation. These properties position GPs as dual-purpose agents for medicinal and functional food development. This review comprehensively explores the structural complexity of six key GPs and their specific mechanisms of action, such as TLR signaling in immune modulation, apoptosis pathways in anti-tumor activity, and their prebiotic effects on gut microbiota. Additionally, the structure–activity relationships (SARs) of GPs are highlighted to elucidate their biological efficacy. Advances in green extraction techniques, including ultrasonic-assisted and enzymatic methods, are discussed for their roles in enhancing yield and aligning with sustainable production principles. Furthermore, the review addresses biotechnological innovations in polysaccharide biosynthesis, improving production efficiency and making large-scale production feasible. These insights, combined with ongoing research into their bioactivity, provide a solid foundation for developing health-promoting functional food products that incorporate GPs. Furthermore, future research directions are suggested to optimize biosynthesis pathways and fully harness the health benefits of these polysaccharides.</p><h3>Graphical abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":718,"journal":{"name":"Natural Products and Bioprospecting","volume":"15 1","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s13659-025-00496-w.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143533266","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Natural products are the important sources in cardiovascular drug development. In this study, twenty-nine buthutin derivatives were designed, synthesized, and evaluated for their NHE-1 inhibition and protective effects on cardiomyocyte injury. The structure of the newly synthesized compounds had been confirmed by 1H-NMR, 13C-NMR, and HR-ESI-MS spectra. Among all target compounds at 1 μM, compounds 9d, 9f, 9k, 9m, and 9n, with a protection ratio exceeding 30%, exerted stronger protective effects on H9c2 cardiomyocyte than positive control dexrazoxane and buthutin A. Meanwhile, compounds 9k, 9m, and 9o showed the significant NHE-1 inhibitory activities on H9c2 cardiomyocyte, all with a dpHi/min value less than 0.23. What is more, compounds 9k, 9m, 9o and buthutin A all exhibited the specificity on NHE-1 inhibition. Molecular modelling studies suggested the ability of compounds 9m and 9o to establish interactions with three hydrogen bonds to Asp267 and Glu346 of NHE-1, but also the ability with much lower CDOCKER energies than positive control cariporide and buthutin A. The structure–activity relationship (SAR) studies suggested that the presences of amide group, four-carbon linker, and para hydroxyl benzene ring were advantageous pharmacophores for above two pharmacological actions. This research would open new avenues for developing amide-guanidine-based cardioprotective agents.
Graphical Abstract
{"title":"Design, synthesis and biological evaluation of buthutin derivatives as cardioprotective agents","authors":"Yuan Liu, Fa-Qi Wang, Xin-Hao Hua, Shu-Han Yang, Li-Ning Wang, Yun-Sheng Xu, Chen-Yue Shao, Xiang-Bo Gou, Yu-Ming Liu","doi":"10.1007/s13659-025-00497-9","DOIUrl":"10.1007/s13659-025-00497-9","url":null,"abstract":"<div><p>Natural products are the important sources in cardiovascular drug development. In this study, twenty-nine buthutin derivatives were designed, synthesized, and evaluated for their NHE-1 inhibition and protective effects on cardiomyocyte injury. The structure of the newly synthesized compounds had been confirmed by <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, and HR-ESI-MS spectra. Among all target compounds at 1 μM, compounds <b>9d</b>, <b>9f</b>, <b>9k</b>, <b>9m</b>, and<b> 9n</b>, with a protection ratio exceeding 30%, exerted stronger protective effects on H9c2 cardiomyocyte than positive control dexrazoxane and buthutin A. Meanwhile, compounds <b>9k</b>, <b>9m</b>, and <b>9o</b> showed the significant NHE-1 inhibitory activities on H9c2 cardiomyocyte, all with a dpHi/min value less than 0.23. What is more, compounds <b>9k</b>, <b>9m</b>, <b>9o</b> and buthutin A all exhibited the specificity on NHE-1 inhibition. Molecular modelling studies suggested the ability of compounds <b>9m</b> and <b>9o</b> to establish interactions with three hydrogen bonds to Asp267 and Glu346 of NHE-1, but also the ability with much lower CDOCKER energies than positive control cariporide and buthutin A. The structure–activity relationship (SAR) studies suggested that the presences of amide group, four-carbon linker, and <i>para</i> hydroxyl benzene ring were advantageous pharmacophores for above two pharmacological actions. This research would open new avenues for developing amide-guanidine-based cardioprotective agents.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":718,"journal":{"name":"Natural Products and Bioprospecting","volume":"15 1","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-02-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s13659-025-00497-9.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143108404","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-01-24DOI: 10.1007/s13659-024-00493-5
Hesham R. El-Seedi, Mohamed S. Refaey, Nizar Elias, Mohamed F. El-Mallah, Faisal M. K. Albaqami, Ismail Dergaa, Ming Du, Mohamed F. Salem, Haroon Elrasheid Tahir, Maria Dagliaa, Nermeen Yosri, Hongcheng Zhang, Awg H. El-Seedi, Zhiming Guo, Shaden A. M. Khalifa
Marine natural products have long been recognized as a vast and diverse source of bioactive compounds with potential therapeutic applications, particularly in oncology. This review provides an updated overview of the significant advances made in the discovery and development of marine-derived anticancer drugs between 2019 and 2023. With a focus on recent research findings, the review explores the rich biodiversity of marine organisms, including sponges, corals, algae, and microorganisms, which have yielded numerous compounds exhibiting promising anticancer properties. Emphasizing the multifaceted mechanisms of action, the review discusses the molecular targets and pathways targeted by these compounds, such as cell cycle regulation, apoptosis induction, angiogenesis inhibition, and modulation of signaling pathways. Additionally, the review highlights the innovative strategies employed in the isolation, structural elucidation, and chemical modification of marine natural products to enhance their potency, selectivity, and pharmacological properties. Furthermore, it addresses the challenges and opportunities associated with the development of marine-derived anticancer drugs, including issues related to supply, sustainability, synthesis, and clinical translation. Finally, the review underscores the immense potential of marine natural products as a valuable reservoir of novel anticancer agents and advocates for continued exploration and exploitation of the marine environment to address the unmet medical needs in cancer therapy
Graphical Abstract
{"title":"Marine natural products as a source of novel anticancer drugs: an updated review (2019–2023)","authors":"Hesham R. El-Seedi, Mohamed S. Refaey, Nizar Elias, Mohamed F. El-Mallah, Faisal M. K. Albaqami, Ismail Dergaa, Ming Du, Mohamed F. Salem, Haroon Elrasheid Tahir, Maria Dagliaa, Nermeen Yosri, Hongcheng Zhang, Awg H. El-Seedi, Zhiming Guo, Shaden A. M. Khalifa","doi":"10.1007/s13659-024-00493-5","DOIUrl":"10.1007/s13659-024-00493-5","url":null,"abstract":"<div><p>Marine natural products have long been recognized as a vast and diverse source of bioactive compounds with potential therapeutic applications, particularly in oncology. This review provides an updated overview of the significant advances made in the discovery and development of marine-derived anticancer drugs between 2019 and 2023. With a focus on recent research findings, the review explores the rich biodiversity of marine organisms, including sponges, corals, algae, and microorganisms, which have yielded numerous compounds exhibiting promising anticancer properties. Emphasizing the multifaceted mechanisms of action, the review discusses the molecular targets and pathways targeted by these compounds, such as cell cycle regulation, apoptosis induction, angiogenesis inhibition, and modulation of signaling pathways. Additionally, the review highlights the innovative strategies employed in the isolation, structural elucidation, and chemical modification of marine natural products to enhance their potency, selectivity, and pharmacological properties. Furthermore, it addresses the challenges and opportunities associated with the development of marine-derived anticancer drugs, including issues related to supply, sustainability, synthesis, and clinical translation. Finally, the review underscores the immense potential of marine natural products as a valuable reservoir of novel anticancer agents and advocates for continued exploration and exploitation of the marine environment to address the unmet medical needs in cancer therapy</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":718,"journal":{"name":"Natural Products and Bioprospecting","volume":"15 1","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-01-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11759743/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143031800","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-01-20DOI: 10.1007/s13659-024-00492-6
Eleonora Spinozzi, Marta Ferrati, Cecilia Baldassarri, Paolo Rossi, Guido Favia, Giorgio Cameli, Giovanni Benelli, Angelo Canale, Livia De Fazi, Roman Pavela, Luana Quassinti, Cristiano Giordani, Fabrizio Araniti, Loredana Cappellacci, Riccardo Petrelli, Filippo Maggi
Mosquitoes (Diptera: Culicidae) are vectors of various pathogens of public health concern and replacing conventional insecticides remains a challenge. In this regard, natural products represent valuable sources of potential insecticidal compounds, thus increasingly attracting research interest. Commiphora myrrha (T.Nees) Engl. (Burseraceae) is a medicinal plant whose oleo-gum resin is used in food, cosmetics, fragrances, and pharmaceuticals. Herein, the larvicidal potential of its essential oil (EO) was assessed on four mosquito species (Aedes albopictus Skuse, Aedes aegypti L., Anopheles gambiae Giles and Anopheles stephensi Liston), with LC50 values ranging from 4.42 to 16.80 μg/mL. The bio-guided EO fractionation identified furanosesquiterpenes as the main larvicidal compounds. A GC–MS-driven untargeted metabolomic analysis revealed 32 affected metabolic pathways in treated larvae. The EO non-target toxicity on Daphnia magna Straus (LC50 = 4.51 μL/L) and its cytotoxicity on a human kidney cell line (HEK293) (IC50 of 14.38 μg/mL) were also assessed. This study shows the potential of plant products as innovative insecticidal agents and lays the groundwork for the possible exploitation of C. myrrha EO in sustainable approaches for mosquito management.
{"title":"Essential oil and furanosesquiterpenes from myrrh oleo-gum resin: a breakthrough in mosquito vector management","authors":"Eleonora Spinozzi, Marta Ferrati, Cecilia Baldassarri, Paolo Rossi, Guido Favia, Giorgio Cameli, Giovanni Benelli, Angelo Canale, Livia De Fazi, Roman Pavela, Luana Quassinti, Cristiano Giordani, Fabrizio Araniti, Loredana Cappellacci, Riccardo Petrelli, Filippo Maggi","doi":"10.1007/s13659-024-00492-6","DOIUrl":"10.1007/s13659-024-00492-6","url":null,"abstract":"<p>Mosquitoes (Diptera: Culicidae) are vectors of various pathogens of public health concern and replacing conventional insecticides remains a challenge. In this regard, natural products represent valuable sources of potential insecticidal compounds, thus increasingly attracting research interest. <i>Commiphora myrrha</i> (T.Nees) Engl. (Burseraceae) is a medicinal plant whose oleo-gum resin is used in food, cosmetics, fragrances, and pharmaceuticals. Herein, the larvicidal potential of its essential oil (EO) was assessed on four mosquito species (<i>Aedes albopictus</i> Skuse, <i>Aedes aegypti</i> L., <i>Anopheles gambiae</i> Giles and <i>Anopheles stephensi</i> Liston), with LC<sub>50</sub> values ranging from 4.42 to 16.80 μg/mL. The bio-guided EO fractionation identified furanosesquiterpenes as the main larvicidal compounds. A GC–MS-driven untargeted metabolomic analysis revealed 32 affected metabolic pathways in treated larvae. The EO non-target toxicity on <i>Daphnia magna</i> Straus (LC<sub>50</sub> = 4.51 μL/L) and its cytotoxicity on a human kidney cell line (HEK293) (IC<sub>50</sub> of 14.38 μg/mL) were also assessed. This study shows the potential of plant products as innovative insecticidal agents and lays the groundwork for the possible exploitation of <i>C. myrrha</i> EO in sustainable approaches for mosquito management.</p>","PeriodicalId":718,"journal":{"name":"Natural Products and Bioprospecting","volume":"15 1","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-01-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s13659-024-00492-6.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142995335","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-01-16DOI: 10.1007/s13659-024-00487-3
Joan Labara Tirado, Andrei Herdean, Peter J. Ralph
Microalgae’s adaptability and resilience to Earth’s diverse environments have evolved these photosynthetic microorganisms into a biotechnological source of industrially relevant physiological functions and biometabolites. Despite this, microalgae-based industries only exploit a handful of species. This lack of biodiversity hinders the expansion of the microalgal industry. Microalgal bioprospecting, searching for novel biological algal resources with new properties, remains a low throughput and time-consuming endeavour due to inefficient workflows that rely on non-selective sampling, monoalgal culture status and outdated, non-standardized characterization techniques. This review will highlight the importance of microalgal bioprospecting and critically explore commonly employed methodologies. We will also explore current advances driving the next generation of smart algal bioprospecting focusing on novel workflows and transdisciplinary methodologies with the potential to enable high-throughput microalgal biodiscoveries. Images adapted from (Addicted04 in Wikipedia File: Australia on the globe (Australia centered).svg. 2014.; Jin et al. in ACS Appl Bio Mater 4:5080–5089, 2021; Kim et al. in Microchim Acta 189:88, 2022; Tony et al. in Lab on a Chip 15, 19:3810–3810; Thermo Fisher Scientific INC. in CTS Rotea Brochure).
Graphical abstract
微藻对地球多样化环境的适应性和恢复力使这些光合微生物进化成为与工业相关的生理功能和生物代谢物的生物技术来源。尽管如此，以微藻为基础的工业只开发了少数几种物种。生物多样性的缺乏阻碍了微藻产业的发展。微藻生物勘探，寻找具有新特性的新型生物藻类资源，仍然是一个低通量和耗时的努力，由于低效的工作流程，依赖于非选择性采样，单藻培养状态和过时的，非标准化的表征技术。本文将强调微藻生物勘探的重要性，并对常用的方法进行批判性的探讨。我们还将探讨推动下一代智能藻类生物勘探的当前进展，重点关注新颖的工作流程和跨学科方法，具有实现高通量微藻生物发现的潜力。图片改编自维基百科文件：全球的澳大利亚（以澳大利亚为中心）.svg。2014年。Jin et al. journal of chengdu electromechanical college, 2011；Kim et al. in microchem学报189:88,2022；Tony et al. in Lab on a Chip, 15 (1):3810 - 3810；赛默飞世尔科技有限公司（CTS Rotea手册）。图形抽象
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Pub Date : 2025-01-08DOI: 10.1007/s13659-024-00495-3
Wenta Tan, Shuo Fu, Yufei Wang, Bojun Hu, Guiquan Ding, Li Zhang, Wen Zhang, Guanhua Du, Junke Song
Anchusa italica Retz. (AIR), a traditional herbal remedy, is commonly applied in managing heart and brain disorders. However, its specific function and mechanism in acute cerebral ischemia–reperfusion injury (CIRI) are not fully understood. This research focused on the interventional effects and potential mechanisms of AIR extract (AIRE) in a rat model of CIRI. The model was established using the filament occlusion method, which involved blocking the middle cerebral artery for 1.5 h and then removing the filament to restore blood flow. Transcriptomic and metabolomic analyses were conducted to explore the molecular pathways and metabolites affected by AIRE. ATP level was measured using an ATP assay kit. Additionally, RT-qPCR and western blot tests were conducted to evaluate the influence of AIRE on the Wnt signaling pathway and mitochondrial function. Transcriptomic and metabolomic analyses indicated that AIRE regulated the Wnt signaling pathway in CIRI and modulated metabolites associated with mitochondrial energy metabolism, such as citrate and succinate. ATP assay result demonstrated that AIRE enhanced ATP production in CIRI. Further, RT-qPCR and western blot analyses revealed that AIRE activated the Wnt/β-catenin signaling pathway and corrected mitochondrial dysfunction. These results proposed that AIRE mitigated mitochondrial energy metabolism deficits in CIRI via the Wnt/β-catenin pathway. By restoring the balance of mitochondrial function and energy metabolism, AIRE might offer a potentially therapeutic strategy for addressing CIRI.
Graphical Abstract
Anchusa italica Retz。（AIR）是一种传统的草药，通常用于治疗心脏和大脑疾病。然而，其在急性脑缺血再灌注损伤（CIRI）中的具体功能和机制尚不完全清楚。本研究主要探讨AIR提取物（AIRE）对大鼠CIRI模型的干预作用及其可能机制。模型采用脑丝闭塞法，即阻断大脑中动脉1.5 h后取出脑丝恢复血流。转录组学和代谢组学分析探讨了AIRE影响的分子途径和代谢物。ATP检测试剂盒检测ATP水平。此外，通过RT-qPCR和western blot检测AIRE对Wnt信号通路和线粒体功能的影响。转录组学和代谢组学分析表明，AIRE调节CIRI中的Wnt信号通路，并调节与线粒体能量代谢相关的代谢物，如柠檬酸盐和琥珀酸盐。ATP测定结果表明，AIRE能促进CIRI细胞ATP的生成。此外，RT-qPCR和western blot分析显示，AIRE激活了Wnt/β-catenin信号通路，纠正了线粒体功能障碍。这些结果表明，AIRE通过Wnt/β-catenin途径减轻了CIRI的线粒体能量代谢缺陷。通过恢复线粒体功能和能量代谢的平衡，AIRE可能为解决CIRI提供潜在的治疗策略。图形抽象
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