Reduced glucose uptake usually occurs in type 2 diabetes due to down-regulation of brain glucose transporters. The potential of kolaviron, a biflavonoid from Garcinia kola to stimulate glucose uptake and suppress glucose-induced oxidative toxicity were investigated in rat brain. Its molecular interactions with the target proteins were investigated in silico. Kolaviron was incubated with excised rat brain in the presence of glucose for 2 h, with metformin serving as a positive control. Kolaviron caused a significant (p < 0.05) increase in glucose uptake, glutathione level, superoxide dismutase, catalase, ATPase, ENTPDase and 5’-nucleotidase activities, while concomitantly depleting malondialdehyde level, acetylcholinesterase and butyrylcholinesterase activities compared to brains incubated with glucose only. Electron microscopy (SEM and TEM) analysis revealed kolaviron had little or no effect on the ultrastructural morphology of brain tissues as evidenced by the intact dendritic and neuronal network, blood vessels, mitochondria, synaptic vesicles, and pre-synaptic membrane. SEM-EDX analysis revealed a restorative effect of glucose-induced alteration in brain elemental concentrations, with total depletion of aluminum and zinc. MTT analysis revealed kolaviron had no cytotoxic effect on HT-22 cells. Molecular docking revealed a potent interaction between kolaviron and catalase at the SER114 and MET350 residues, with a binding energy of 12 kcal/mol. Taken together, these results portray the potential of kolaviron to stimulate glucose uptake while concomitantly coffering a neuroprotective effect.

由于脑葡萄糖转运蛋白的下调，葡萄糖摄取减少通常发生在 2 型糖尿病中。在大鼠大脑中研究了 kolaviron（一种来自藤黄可乐的双黄酮类化合物）刺激葡萄糖摄取和抑制葡萄糖诱导的氧化毒性的潜力。在计算机上研究了它与靶蛋白的分子相互作用. 将 Kolaviron 与切除的大鼠脑在葡萄糖存在下孵育 2 小时，二甲双胍作为阳性对照。与仅用葡萄糖孵育的大脑相比，Kolaviron 导致葡萄糖摄取、谷胱甘肽水平、超氧化物歧化酶、过氧化氢酶、ATP 酶、ENTPDase 和 5'-核苷酸酶活性显着增加（p < 0.05），同时伴随消耗丙二醛水平、乙酰胆碱酯酶和丁酰胆碱酯酶活性。电子显微镜（SEM 和 TEM）分析表明，如完整的树突和神经元网络、血管、线粒体、突触小泡和突触前膜所证明的，kolaviron 对脑组织的超微结构形态几乎没有影响或没有影响。SEM-EDX 分析揭示了葡萄糖诱导的脑元素浓度变化的恢复作用，随着铝和锌的完全消耗。MTT 分析显示 kolaviron 对 HT-22 细胞没有细胞毒作用。分子对接揭示了 kolaviron 和过氧化氢酶在 SER114 和 MET350 残基处的有效相互作用，结合能为 12 kcal/mol。总之，这些结果描绘了 kolaviron 在刺激葡萄糖摄取同时提供神经保护作用的潜力。