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Pharmacological and Molecular Docking Investigation of Leaves of Eriobotrya japonica: Antioxidant, Enzyme Inhibition, and Anti-Inflammatory Effects

熊果酸 化学 绿原酸 枇杷属 抗氧化剂 芦丁 IC50型 没食子酸 生物化学 槲皮素 阿布茨 槲皮素 立体化学 粳稻 DPPH 色谱法 体外 生物 植物
作者
Pao‐Jen Kuo,Liting Chen,Sin‐Min Li,Zih-Rong Chen,Jih‐Jung Chen
出处
期刊:Antioxidants [Multidisciplinary Digital Publishing Institute]
卷期号:14 (4): 413-413
标识
DOI:10.3390/antiox14040413
摘要

Leaves of Eriobotrya japonica have long been utilized in traditional Chinese medicine (TCM) for treating pulmonary inflammation and stomach disorders. This study extends their pharmacological applications by evaluating the antioxidant, anti-α-glucosidase, anti-acetylcholinesterase (AChE), and anti-inflammatory activities of solvent extracts and isolated bioactive components through an integrative approach combining extraction, bioassays, and molecular docking. Solvent extracts prepared with varying polarities exhibited distinct bioactivities, with the 100 °C water and methanol extracts displaying the strongest antioxidant potential. The ethyl acetate extract exhibited potent α-glucosidase inhibition, whereas the n-hexane extract demonstrated significant AChE inhibitory activity. Among the isolated compounds, epicatechin (5) (SC50 = 7.83 ± 0.34 μM) and rutin (6) (SC50 = 6.69 ± 0.25 μM) showed superior ABTS and superoxide scavenging activities, respectively, compared to the positive controls (BHT and cynaroside). Ursolic acid (2) exhibited stronger α-glucosidase inhibition (IC50 = 10.68 ± 0.76 μM) than acarbose (IC50 = 419.93 ± 29.15 μM), while tormentic acid (4) demonstrated superior AChE inhibition compared to chlorogenic acid. Ursolic acid (2) also displayed NO inhibition (IC50 = 20.18 ± 1.46 μM) comparable to quercetin (IC50 = 17.05 ± 1.63 μM), with Western blot analysis confirming its potent iNOS inhibitory activity. Molecular docking further supported these findings, revealing that ursolic acid (2) exhibited stronger binding affinity to α-glucosidase (−8.7 kcal/mol) than acarbose (−5.1 kcal/mol), tormentic acid (4) displayed higher binding energy to AChE (−8.8 kcal/mol) compared to chlorogenic acid (−7.8 kcal/mol), and ursolic acid (2) (−7.5 kcal/mol) showed a binding affinity to iNOS similar to that of quercetin (−7.7 kcal/mol). These results highlight the strong potential of E. japonica leaf extracts and bioactive compounds as natural antioxidants, enzyme inhibitors, and anti-inflammatory agents, supporting their development as dietary supplements or therapeutic candidates for managing oxidative stress, hyperglycemia, neurodegenerative diseases, and inflammatory disorders.
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