南瓜籽油生育酚抗糖尿病作用的体内实验验证：基于计算对接的支持。
Tocopherol from seeds of Cucurbita pepo against diabetes: validation by in vivo experiments supported by computational docking.
出版信息
J Formos Med Assoc. 2013 Nov;112(11):676-90. doi: 10.1016/j.jfma.2013.08.003.
BACKGROUND/PURPOSE: Tocopherol from raw pumpkin seeds has been reported to be effective in the alleviation of diabetes through its antioxidant activities. This study evaluates the antidiabetic activities of the tocopherol fraction of raw seeds of Cucurbita pepo L. (CPSE) in a diabetic rat model. In addition, the putative action mechanisms of its botanicals were computationally investigated.
METHODS
Seed water activity (Aw) was assessed. Tocopherol was extracted and quantified from raw seed oil. The effect of CPSE was studied in poloxamer-407 (PX-407)-induced type 2 diabetic Wistar rats. Glycemic, insulinemic, and lipid profiles, as well as lipid peroxidation status, were evaluated. Glucagon like peptide-1 (GLP-1) content in the cecum was evaluated and histopathological analysis of the pancreas was performed. Further, HYBRID and FRED docking were performed for 10 documented CPSE botanicals, for putative action mechanisms concerning three proteins [protein-tyrosine phosphatase 1B (PTP-1B), peroxisome proliferator-activated receptor gamma (PPAR-γ), and dipeptidyl peptidase IV (DPP-IV)] known to have diabetic therapeutic potential.
RESULTS
The Aw of raw seeds was found to be 0.544 ± 0.002. Using tocopherol standards, HPLC determination of CPSE revealed the presence of tocopherol isomers (α, β, γ, and δ). The tocopherol content was found to be 107.4 ± 2.9 mg/100 g of CPSE. When compared to diabetic control (DC) rats, the CPSE-treated diabetic rats presented a significant amelioration of glycemia, insulinemia, and lipid dysmetabolism. A remarkable reduction in oxidative markers and improved cecal and pancreatic characteristics were also observed. Tocopherol isomers have shown a considerable interaction potential with the aforesaid proteins in docking.
CONCLUSION
The results provide pharmacological evidence of CPSE as an antihyperglycemic mediated by the interaction of various botanicals with multiple targets operating in diabetes mellitus (DM).
背景/目的：从生南瓜籽中提取的生育酚因其抗氧化活性已被报道可有效缓解糖尿病。本研究评估了生葫芦巴种子生育酚（CPSE）在糖尿病大鼠模型中的抗糖尿病活性。此外，还通过计算方法研究了其植物的可能作用机制。
方法
评估种子水分活度（Aw）。从生籽油中提取并定量生育酚。在聚氧乙烯 407（PX-407）诱导的 2 型糖尿病 Wistar 大鼠中研究 CPSE 的作用。评估血糖、胰岛素和血脂谱以及脂质过氧化状态。评估盲肠中胰高血糖素样肽-1（GLP-1）的含量，并对胰腺进行组织病理学分析。此外，还对 10 种已记录的 CPSE 植物进行了 HYBRID 和 FRED 对接，以研究与三种具有糖尿病治疗潜力的蛋白质（蛋白酪氨酸磷酸酶 1B（PTP-1B）、过氧化物酶体增殖物激活受体γ（PPAR-γ）和二肽基肽酶 IV（DPP-IV））有关的可能作用机制。
结果
发现生种子的 Aw 为 0.544±0.002。使用生育酚标准品，通过 HPLC 测定 CPSE 发现存在生育酚异构体（α、β、γ 和 δ）。CPSE 的生育酚含量为 107.4±2.9mg/100g CPSE。与糖尿病对照组（DC）大鼠相比，CPSE 治疗的糖尿病大鼠血糖、胰岛素血症和脂质代谢异常得到显著改善。还观察到氧化标志物显著减少以及盲肠和胰腺特征得到改善。在对接中，生育酚异构体与上述蛋白质显示出相当大的相互作用潜力。
结论
这些结果为 CPSE 作为一种通过各种植物与糖尿病中多个靶点相互作用介导的抗高血糖作用提供了药理学证据。
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