仙果叶提取物通过抗炎活性和抑制碳水化合物代谢酶对果糖喂养的链脲佐菌素注射大鼠的抗糖尿病作用。
Antidiabetic property of miracle fruit plant (Synsepalum dulcificum Shumach. & Thonn. Daniell) leaf extracts in fructose-fed streptozotocin-injected rats via anti-inflammatory activity and inhibition of carbohydrate metabolizing enzymes.
机构信息
Phytomedicine, Biochemical Pharmacology and Toxicology Unit, Department of Biochemistry, The Federal University of Technology, PMB 704, Akure, Nigeria; Department of Chemical Sciences, Biochemistry Unit, Afe Babalola University, PMB 5454 Ado Ekiti, Nigeria.
Phytomedicine, Biochemical Pharmacology and Toxicology Unit, Department of Biochemistry, The Federal University of Technology, PMB 704, Akure, Nigeria.
出版信息
J Ethnopharmacol. 2019 Nov 15;244:112124. doi: 10.1016/j.jep.2019.112124. Epub 2019 Jul 30.
ETHNOPHARMACOLOGICAL RELEVANCE
Miracle fruit plant (Synsepalum dulcificum) has many applications in folk medicine. The leaves are used traditionally to treat diabetes and other diseases. The antidiabetic potential of Synsepalum dulcificum leaves in rats has been studied but the mechanisms involved are yet to be elucidated.
AIM
The present study aimed to provide insight into the antidiabetic mechanisms of methanol and flavonoid-rich leaf extracts of Synsepalum dulcificum (MSD and FSD, respectively).
METHODS
In vivo effects of administering 30 mg/kg or 60 mg/kg MSD and FSD for 21 consecutive days to rats after type II diabetes was induced through 14 days of fructose feeding and injection of one dose of streptozotocin, were assessed. Glibenclamide (5 mg/kg) served as the reference drug. In addition, in vitro inhibitory activity of MSD and FSD on the carbohydrate metabolizing enzymes, α-amylase and glucokinase, were evaluated, with acarbose as the reference drug. Moreover, in silico analyses to elucidate the contribution of key polyphenolics to the antidiabetic activity of the extracts through docking with glucokinase were performed.
RESULTS
MSD and FSD significantly reduced HbA1c and serum levels of interleukin-6 and TNF-α (p < 0.05) in diabetic animals. Conversely, serum level of insulin and hepatic hexokinase activity were increased (p < 0.05) in extract treated groups. Both extracts showed α-amylase and α-glucosidase inhibitory activities. Quercetin, caffeic acid and chlorogenic acid in extracts showed strong binding affinities with glucokinase in the molecular docking analyses.
CONCLUSION
Results from this study indicate that increased insulin synthesis, reduction of inflammation and inhibition of carbohydrate metabolizing enzymes are likely mechanisms by which MSD and FSD exert antidiabetic action in type II diabetic rats.
民族药理学相关性
神秘果植物（Synsepalum dulcificum）在民间医学中有许多应用。传统上，叶子被用于治疗糖尿病和其他疾病。已经研究了 Synsepalum dulcificum 叶子在大鼠中的抗糖尿病潜力，但涉及的机制仍有待阐明。
目的
本研究旨在深入了解甲醇和富含类黄酮的神秘果叶提取物（MSD 和 FSD）的抗糖尿病机制。
方法
在诱导 II 型糖尿病后，通过 14 天果糖喂养和单次链脲佐菌素注射，连续 21 天给予大鼠 30mg/kg 或 60mg/kg MSD 和 FSD，评估 30mg/kg 或 60mg/kg MSD 和 FSD 的体内作用。格列本脲（5mg/kg）作为参考药物。此外，还评估了 MSD 和 FSD 对碳水化合物代谢酶α-淀粉酶和葡萄糖激酶的体外抑制活性，以阿卡波糖作为参考药物。此外，通过与葡萄糖激酶对接，进行了计算机模拟分析，以阐明提取物中关键多酚对其抗糖尿病活性的贡献。
结果
MSD 和 FSD 可显著降低糖尿病动物的 HbA1c 和血清白细胞介素-6 和 TNF-α水平（p<0.05）。相反，胰岛素和肝己糖激酶活性的血清水平在提取物处理组中增加（p<0.05）。两种提取物均显示出α-淀粉酶和α-葡萄糖苷酶抑制活性。提取物中的槲皮素、咖啡酸和绿原酸在分子对接分析中与葡萄糖激酶表现出很强的结合亲和力。
结论
本研究结果表明，增加胰岛素合成、减少炎症和抑制碳水化合物代谢酶可能是 MSD 和 FSD 在 II 型糖尿病大鼠中发挥抗糖尿病作用的机制。
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