Fatma Abdelhakim Mohamed, Mohamed A. Salem, Mohammed N. A. Khalil, Ali M. El-Halawany, Amira S. El Senousy
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The potential of <i>Coccoloba uvifera, Coccoloba peltata</i> and <i>Ruprechtia salicifolia</i> total extracts and fractions as antioxidant, antidiabetic and anti-glycating agents was evaluated and correlated with their chemical composition via multiple approaches of metabolic profiling.</p><h3>Results</h3><p>All the total ethanolic extracts of plant leaves revealed remarkable antioxidant activities in terms of scavenging DPPH and ABTS radicals, as well as ferric reducing antioxidant power (FRAP). Despite having more or less comparable total phenolic and flavonoid contents, <i>C. uvifera</i> extract showed the highest inhibitory activity against <i>α</i>-glucosidase enzyme (IC<sub>50</sub> 7.985 ± 1.08 μg/mL), being more potent than acarbose (20-fold). All total extracts demonstrated moderately high anti-AGEs (> 63% inhibition) in BSA-fructose model. Among all examined fractions, <i>C. uvifera</i> 50% MeOH fraction exhibited the most potent antioxidant activity in DPPH, ABTS and FRAP assays (5697.33 ± 360.7, 3078.9 ± 249, 1664.02 ± 220 µM ascorbic acid equivalent/mg extract, respectively) and the highest <i>α</i>-glucosidase inhibitory activity (IC<sub>50</sub> 3.36 ± 1.04 μg/mL). A total of 140 compounds, belonging to different classes, were annotated in the three species via UPLC-HRMS, where flavonoids and phenolic acids represented the major classes. Multivariate and correlation analyses revealed the key phytochemicals contributing to <i>α</i>-glucosidase inhibition as 1-<i>O</i>-vanilloyl-hexoside, 1,3-<i>O</i>-diferuloylglycerol, drovomifoliol-<i>O</i>-glucopyranoside, protocatechuic acid glucoside, digalloyl glucose and coumaric acid sulphate.</p><h3>Conclusion</h3><p><i>C. uvifera</i> leaves extract and its 50% MeOH fraction had a superb potential to alleviate DM and its complications through their antioxidant, antiglycation and <i>α</i>-glucosidase inhibitory activities mediated by their versatile polyphenolic phytochemicals.</p><h3>Graphical abstract</h3><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":"2025-03-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00787-6","citationCount":"0","resultStr":"{\"title\":\"Unveiling metabolome heterogeneity in three species from Coccoloba and Ruprechtia through multiple approaches of UPLC/HRMS and chemometric analysis in relation to antidiabetic, antioxidant and antiglycation activities\",\"authors\":\"Fatma Abdelhakim Mohamed, Mohamed A. 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Despite having more or less comparable total phenolic and flavonoid contents, <i>C. uvifera</i> extract showed the highest inhibitory activity against <i>α</i>-glucosidase enzyme (IC<sub>50</sub> 7.985 ± 1.08 μg/mL), being more potent than acarbose (20-fold). All total extracts demonstrated moderately high anti-AGEs (> 63% inhibition) in BSA-fructose model. Among all examined fractions, <i>C. uvifera</i> 50% MeOH fraction exhibited the most potent antioxidant activity in DPPH, ABTS and FRAP assays (5697.33 ± 360.7, 3078.9 ± 249, 1664.02 ± 220 µM ascorbic acid equivalent/mg extract, respectively) and the highest <i>α</i>-glucosidase inhibitory activity (IC<sub>50</sub> 3.36 ± 1.04 μg/mL). A total of 140 compounds, belonging to different classes, were annotated in the three species via UPLC-HRMS, where flavonoids and phenolic acids represented the major classes. 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引用次数: 0
摘要
背景糖尿病（DM）是一种主要的复杂代谢紊乱，是世界范围内导致死亡的主要原因之一。Coccoloba和Ruprechtia是蓼科中最有趣的两个富含多酚的属。通过多种代谢谱分析方法，评价了秋球藻、秋球藻和水杨花总提取物和组分作为抗氧化、抗糖尿病和抗糖化药物的潜力，并与它们的化学成分进行了关联。结果植物叶片总乙醇提取物对DPPH、ABTS自由基的清除能力和铁还原能力均有显著提高。尽管总酚和类黄酮含量大致相当，但葡萄树提取物对α-葡萄糖苷酶的抑制活性最高（IC50为7.985±1.08 μg/mL），比阿卡波糖（20倍）更有效。在bsa -果糖模型中，所有总提取物均表现出中等水平的抗ages（63%的抑制作用）。在DPPH、ABTS和FRAP实验中，50% MeOH提取物的抗氧化活性最高（分别为5697.33±360.7、3078.9±249、1664.02±220µM抗坏血酸当量/mg提取物），α-葡萄糖苷酶抑制活性最高（IC50为3.36±1.04 μg/mL）。通过UPLC-HRMS共检测到140个不同类别的化合物，其中黄酮类和酚酸类为主要类别。多因素分析和相关分析显示，抑制α-葡萄糖苷酶的主要植物化学物质为1- o -香草叶-己糖苷、1,3- o -二阿魏酰基甘油、巯基- o -葡萄糖苷、原儿茶酸葡萄糖苷、二烯丙基葡萄糖和香豆酸硫酸盐。uvifera叶提取物及其50% MeOH组分通过其多酚类植物化学物质介导的抗氧化、抗糖化和α-葡萄糖苷酶抑制活性，具有极好的缓解糖尿病及其并发症的潜力。图形抽象
Unveiling metabolome heterogeneity in three species from Coccoloba and Ruprechtia through multiple approaches of UPLC/HRMS and chemometric analysis in relation to antidiabetic, antioxidant and antiglycation activities
Background
Diabetes mellitus (DM) is a major intricate metabolic disorder, being one of the chief causes of mortality worldwide. Coccoloba and Ruprechtia are two of the most intriguing polyphenol-rich genera within the Polygonaceae family. The potential of Coccoloba uvifera, Coccoloba peltata and Ruprechtia salicifolia total extracts and fractions as antioxidant, antidiabetic and anti-glycating agents was evaluated and correlated with their chemical composition via multiple approaches of metabolic profiling.
Results
All the total ethanolic extracts of plant leaves revealed remarkable antioxidant activities in terms of scavenging DPPH and ABTS radicals, as well as ferric reducing antioxidant power (FRAP). Despite having more or less comparable total phenolic and flavonoid contents, C. uvifera extract showed the highest inhibitory activity against α-glucosidase enzyme (IC50 7.985 ± 1.08 μg/mL), being more potent than acarbose (20-fold). All total extracts demonstrated moderately high anti-AGEs (> 63% inhibition) in BSA-fructose model. Among all examined fractions, C. uvifera 50% MeOH fraction exhibited the most potent antioxidant activity in DPPH, ABTS and FRAP assays (5697.33 ± 360.7, 3078.9 ± 249, 1664.02 ± 220 µM ascorbic acid equivalent/mg extract, respectively) and the highest α-glucosidase inhibitory activity (IC50 3.36 ± 1.04 μg/mL). A total of 140 compounds, belonging to different classes, were annotated in the three species via UPLC-HRMS, where flavonoids and phenolic acids represented the major classes. Multivariate and correlation analyses revealed the key phytochemicals contributing to α-glucosidase inhibition as 1-O-vanilloyl-hexoside, 1,3-O-diferuloylglycerol, drovomifoliol-O-glucopyranoside, protocatechuic acid glucoside, digalloyl glucose and coumaric acid sulphate.
Conclusion
C. uvifera leaves extract and its 50% MeOH fraction had a superb potential to alleviate DM and its complications through their antioxidant, antiglycation and α-glucosidase inhibitory activities mediated by their versatile polyphenolic phytochemicals.
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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