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<p>Chronic inflammation is a key driver of many non-communicable diseases, yet current pharmacological therapies are often limited by adverse effects and poor accessibility. Engineered sucrose-derived glycosides from sugarcane offer a sustainable, food-derived candidate with the potential to modulate inflammatory pathways safely and effectively. We developed a dual synthetic approach combining enzymatic and acid-catalyzed glycosylation to generate targeted glycosides. Products were purified and characterized using HPLC, LC-MS, and NMR, achieving high yields and analytical reproducibility. Anti-inflammatory efficacy was evaluated in LPS-stimulated THP-1 macrophages via cytokine assays, while bioavailability was assessed using Caco-2 monolayers. Stability testing in simulated gastric and intestinal fluids and cytotoxicity profiling were also performed. All experiments were conducted in triplicate and analyzed using one-way ANOVA with Tukey’s post hoc test. All glycosides demonstrated high yields (84.9–86.4%), significant cytokine suppression (TNF-α: −35.2% ± 1.8%; IL-6: −33.1% ± 1.5%; <i>p</i> &lt; 0.001), and favorable permeability (2.3–2.5 × 10⁻⁶ cm/s) with &gt; 90% stability under gastrointestinal conditions. No cytotoxicity was observed up to 200 µM. While sucrose-derived glycosides have been reported in related literature to influence NF-κB and MAPK signaling, the present study did not directly evaluate these pathways. Therefore, any mechanistic interpretation remains hypothetical and requires targeted validation. This is the first integrated demonstration of scalable, high-purity, sugarcane-derived glycosides with moderate but statistically significant in vitro anti-inflammatory activity, measurable intestinal permeability in the Caco-2 model, and food-grade stability. These findings support their development as next-generation nutraceuticals, supporting further investigation toward food-grade applications.</p>

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Enzymatic and chemical glycosylation of sugarcane-derived sucrose yields glycosides with moderate anti-inflammatory activity in vitro

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年7月9日

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  • Zhaojie Chen,
  • Jinhui Chang,
  • Yong Jin

摘要

Chronic inflammation is a key driver of many non-communicable diseases, yet current pharmacological therapies are often limited by adverse effects and poor accessibility. Engineered sucrose-derived glycosides from sugarcane offer a sustainable, food-derived candidate with the potential to modulate inflammatory pathways safely and effectively. We developed a dual synthetic approach combining enzymatic and acid-catalyzed glycosylation to generate targeted glycosides. Products were purified and characterized using HPLC, LC-MS, and NMR, achieving high yields and analytical reproducibility. Anti-inflammatory efficacy was evaluated in LPS-stimulated THP-1 macrophages via cytokine assays, while bioavailability was assessed using Caco-2 monolayers. Stability testing in simulated gastric and intestinal fluids and cytotoxicity profiling were also performed. All experiments were conducted in triplicate and analyzed using one-way ANOVA with Tukey’s post hoc test. All glycosides demonstrated high yields (84.9–86.4%), significant cytokine suppression (TNF-α: −35.2% ± 1.8%; IL-6: −33.1% ± 1.5%; p < 0.001), and favorable permeability (2.3–2.5 × 10⁻⁶ cm/s) with > 90% stability under gastrointestinal conditions. No cytotoxicity was observed up to 200 µM. While sucrose-derived glycosides have been reported in related literature to influence NF-κB and MAPK signaling, the present study did not directly evaluate these pathways. Therefore, any mechanistic interpretation remains hypothetical and requires targeted validation. This is the first integrated demonstration of scalable, high-purity, sugarcane-derived glycosides with moderate but statistically significant in vitro anti-inflammatory activity, measurable intestinal permeability in the Caco-2 model, and food-grade stability. These findings support their development as next-generation nutraceuticals, supporting further investigation toward food-grade applications.