Fayza A. Aljohany, Samyah D. Jastaniah, Fatima B. Alamri, Nahed O. Bawakid, Hanan I. Althagbi, Ashraf B. Abdel-Naim, Mohammad Y. Alfaifi, Magda M. Aly, Fitri Budiyanto, Walied M. Alarif
{"title":"阿拉伯草中呋喃基倍半萜的分子对接、抗菌、抗生物膜形成和抗增殖活性","authors":"Fayza A. Aljohany, Samyah D. Jastaniah, Fatima B. Alamri, Nahed O. Bawakid, Hanan I. Althagbi, Ashraf B. Abdel-Naim, Mohammad Y. Alfaifi, Magda M. Aly, Fitri Budiyanto, Walied M. Alarif","doi":"10.1186/s43094-025-00810-w","DOIUrl":null,"url":null,"abstract":"<div><h3>Background</h3><p><i>Euryops arabicus</i> is well known in the Arabian Peninsula as traditional herbal medicine. The plant synthesizes various types of flavonoids, terpenes, and furoermophilanes skeletons in either steroidal or nonsteroidal conformation, and this wide range of chemical compounds might play an increasingly prominent role in medicine. This study aimed to isolate pure secondary metabolites and assess their antibacterial, antiproliferation, and antibiofilm formation properties.</p><h3>Methods</h3><p>The organic extract of the areal parts of <i>E. arabicus</i> was chromatographically fractionated to afford pure compounds characterized using NMR, UV, and IR along with mass spectrometry. The activity of the isolated compounds was assessed against three cancer cells and a set of Gram-negative and positive bacteria.</p><h3>Results</h3><p>Four specific sesquiterpenoids were identified: 6β-senecioyloxy-1,10-dehydrofuranoeremophilan-9-one (<b>1</b>), 6β-acetoxy-9-oxoeuryopsin (<b>2</b>), 6β-(2′-methyl, 2′,3′-epoxy-butyryloxy)-euryopsin (<b>3</b>), and 6β-angloyloxy-1,10-dehydrofuraoeremophilan-9-one (<b>4</b>). Molecular docking studies indicated the epidermal growth factor receptor and methionyl-tRNA synthetase as probable antibacterial and antiproliferative activities of the compounds. In the in vitro studies, compounds <b>2</b> and<b> 4</b> showed remarkable activity against all examined Gram-negative and positive pathogens with inhibition diameters (mm) ranging from 13.1 ± 0.23 to 19.0 ± 0.44 and 12.9 ± 0.20 to 16.2 ± 0.23, respectively. Compounds <b>2</b> and <b>4</b> showed moderate biofilm formation inhibition of both <i>Pseudomonas aeruginosa</i> and <i>Staphylococcus aureus</i> with 58% and 79%, respectively. Moreover, the isolated sesquiterpenoids showed potent antiproliferative activities against MCF-7, HepG2, and HCT116 human cancer cells.</p><h3>Conclusion</h3><p>Four sesquiterpenoids were isolated from <i>E. arabicus</i>. Compound <b>2</b> showed a relatively high antibacterial and cytotoxic activity. Additional studies are recommended to substantiate the observed activities further.</p><h3>Graphical abstract</h3>\n<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4000,"publicationDate":"2025-05-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00810-w","citationCount":"0","resultStr":"{\"title\":\"Molecular docking, antimicrobial, antibiofilm formation, and antiproliferative activities of furano-based sesquiterpenoids from Euryops arabicus\",\"authors\":\"Fayza A. Aljohany, Samyah D. Jastaniah, Fatima B. Alamri, Nahed O. Bawakid, Hanan I. Althagbi, Ashraf B. Abdel-Naim, Mohammad Y. Alfaifi, Magda M. Aly, Fitri Budiyanto, Walied M. Alarif\",\"doi\":\"10.1186/s43094-025-00810-w\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><h3>Background</h3><p><i>Euryops arabicus</i> is well known in the Arabian Peninsula as traditional herbal medicine. The plant synthesizes various types of flavonoids, terpenes, and furoermophilanes skeletons in either steroidal or nonsteroidal conformation, and this wide range of chemical compounds might play an increasingly prominent role in medicine. This study aimed to isolate pure secondary metabolites and assess their antibacterial, antiproliferation, and antibiofilm formation properties.</p><h3>Methods</h3><p>The organic extract of the areal parts of <i>E. arabicus</i> was chromatographically fractionated to afford pure compounds characterized using NMR, UV, and IR along with mass spectrometry. The activity of the isolated compounds was assessed against three cancer cells and a set of Gram-negative and positive bacteria.</p><h3>Results</h3><p>Four specific sesquiterpenoids were identified: 6β-senecioyloxy-1,10-dehydrofuranoeremophilan-9-one (<b>1</b>), 6β-acetoxy-9-oxoeuryopsin (<b>2</b>), 6β-(2′-methyl, 2′,3′-epoxy-butyryloxy)-euryopsin (<b>3</b>), and 6β-angloyloxy-1,10-dehydrofuraoeremophilan-9-one (<b>4</b>). Molecular docking studies indicated the epidermal growth factor receptor and methionyl-tRNA synthetase as probable antibacterial and antiproliferative activities of the compounds. In the in vitro studies, compounds <b>2</b> and<b> 4</b> showed remarkable activity against all examined Gram-negative and positive pathogens with inhibition diameters (mm) ranging from 13.1 ± 0.23 to 19.0 ± 0.44 and 12.9 ± 0.20 to 16.2 ± 0.23, respectively. Compounds <b>2</b> and <b>4</b> showed moderate biofilm formation inhibition of both <i>Pseudomonas aeruginosa</i> and <i>Staphylococcus aureus</i> with 58% and 79%, respectively. Moreover, the isolated sesquiterpenoids showed potent antiproliferative activities against MCF-7, HepG2, and HCT116 human cancer cells.</p><h3>Conclusion</h3><p>Four sesquiterpenoids were isolated from <i>E. arabicus</i>. Compound <b>2</b> showed a relatively high antibacterial and cytotoxic activity. 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Molecular docking, antimicrobial, antibiofilm formation, and antiproliferative activities of furano-based sesquiterpenoids from Euryops arabicus
Background
Euryops arabicus is well known in the Arabian Peninsula as traditional herbal medicine. The plant synthesizes various types of flavonoids, terpenes, and furoermophilanes skeletons in either steroidal or nonsteroidal conformation, and this wide range of chemical compounds might play an increasingly prominent role in medicine. This study aimed to isolate pure secondary metabolites and assess their antibacterial, antiproliferation, and antibiofilm formation properties.
Methods
The organic extract of the areal parts of E. arabicus was chromatographically fractionated to afford pure compounds characterized using NMR, UV, and IR along with mass spectrometry. The activity of the isolated compounds was assessed against three cancer cells and a set of Gram-negative and positive bacteria.
Results
Four specific sesquiterpenoids were identified: 6β-senecioyloxy-1,10-dehydrofuranoeremophilan-9-one (1), 6β-acetoxy-9-oxoeuryopsin (2), 6β-(2′-methyl, 2′,3′-epoxy-butyryloxy)-euryopsin (3), and 6β-angloyloxy-1,10-dehydrofuraoeremophilan-9-one (4). Molecular docking studies indicated the epidermal growth factor receptor and methionyl-tRNA synthetase as probable antibacterial and antiproliferative activities of the compounds. In the in vitro studies, compounds 2 and 4 showed remarkable activity against all examined Gram-negative and positive pathogens with inhibition diameters (mm) ranging from 13.1 ± 0.23 to 19.0 ± 0.44 and 12.9 ± 0.20 to 16.2 ± 0.23, respectively. Compounds 2 and 4 showed moderate biofilm formation inhibition of both Pseudomonas aeruginosa and Staphylococcus aureus with 58% and 79%, respectively. Moreover, the isolated sesquiterpenoids showed potent antiproliferative activities against MCF-7, HepG2, and HCT116 human cancer cells.
Conclusion
Four sesquiterpenoids were isolated from E. arabicus. Compound 2 showed a relatively high antibacterial and cytotoxic activity. Additional studies are recommended to substantiate the observed activities further.
期刊介绍：
Future Journal of Pharmaceutical Sciences (FJPS) is the official journal of the Future University in Egypt. It is a peer-reviewed, open access journal which publishes original research articles, review articles and case studies on all aspects of pharmaceutical sciences and technologies, pharmacy practice and related clinical aspects, and pharmacy education. The journal publishes articles covering developments in drug absorption and metabolism, pharmacokinetics and dynamics, drug delivery systems, drug targeting and nano-technology. It also covers development of new systems, methods and techniques in pharmacy education and practice. The scope of the journal also extends to cover advancements in toxicology, cell and molecular biology, biomedical research, clinical and pharmaceutical microbiology, pharmaceutical biotechnology, medicinal chemistry, phytochemistry and nutraceuticals.
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