University of Applied Sciences Upper Austria, 4600 Wels, Austria.
Austrian Competence Center for Feed and Food Quality, Safety and Innovation, 4600 Wels, Austria.
Nutrients. 2019 Jul 3;11(7):1512. doi: 10.3390/nu11071512.
Inhibition of intestinal glucose resorption can serve as an effective strategy for the prevention of an increase in blood glucose levels. We have recently shown that various extracts prepared from guava () inhibit sodium-dependent glucose cotransporter 1 (SGLT1)- and glucose transporter 2 (GLUT2)-mediated glucose transport in vitro (Caco-2 cells) and in vivo (C57BL/6N mice). However, the efficacy in humans remains to be confirmed. For this purpose, we conducted a parallelized, randomized clinical study with young healthy adults. Thirty-one volunteers performed an oral glucose tolerance test (OGTT) in which the control group received a glucose solution and the intervention group received a glucose solution containing a guava fruit extract prepared by supercritical CO extraction. The exact same extract was used for our previous in vitro and in vivo experiments. Blood samples were collected prior to and up to two hours after glucose consumption to quantitate blood glucose and insulin levels. Our results show that, in comparison to the control group, consumption of guava fruit extract resulted in a significantly reduced increase in postprandial glucose response over the basal fasting plasma glucose levels after 30 min (Δ control 2.60 ± 1.09 mmol/L versus Δ intervention 1.96 ± 0.96 mmol/L; = 0.039) and 90 min (Δ control 0.44 ± 0.74 mmol/L versus Δ intervention -0.18 ± 0.88 mmol/L; = 0.023). In addition, we observed a slightly reduced, but non-significant insulin secretion (Δ control 353.82 ± 183.31 pmol/L versus Δ intervention 288.43 ± 126.19 pmol/L, = 0.302). Interestingly, storage time and repeated freeze-thawing operations appeared to negatively influence the efficacy of the applied extract. Several analytical methods (HPLC-MS, GC-MS, and NMR) were applied to identify putative bioactive compounds in the CO extract used. We could assign several substances at relevant concentrations including kojic acid (0.33 mg/mL) and 5-hydroxymethylfurfural (2.76 mg/mL). Taken together, this clinical trial and previous in vitro and in vivo experiments confirm the efficacy of our guava fruit extract in inhibiting intestinal glucose resorption, possibly in combination with reduced insulin secretion. Based on these findings, the development of food supplements or functional foods containing this extract appears promising for patients with diabetes and for the prevention of insulin resistance. Trial registration: 415-E/2319/15-2018 (Ethics Commissions of Salzburg).
肠道葡萄糖吸收抑制可作为预防血糖升高的有效策略。我们最近发现,番石榴的各种提取物可抑制体外(Caco-2 细胞)和体内(C57BL/6N 小鼠)钠依赖性葡萄糖协同转运蛋白 1(SGLT1)和葡萄糖转运蛋白 2(GLUT2)介导的葡萄糖转运。然而,其在人类中的疗效仍有待证实。为此,我们对年轻健康成年人进行了一项平行、随机的临床研究。31 名志愿者进行了口服葡萄糖耐量试验(OGTT),对照组给予葡萄糖溶液,干预组给予超临界 CO2 提取的番石榴果提取物的葡萄糖溶液。与我们之前的体外和体内实验使用的是完全相同的提取物。在葡萄糖摄入前和摄入后两小时采集血样,以定量检测血糖和胰岛素水平。我们的结果表明,与对照组相比,摄入番石榴果提取物可显著降低餐后血糖反应相对于基础空腹血糖水平,在 30 分钟时(对照组增加 2.60±1.09mmol/L,干预组增加 1.96±0.96mmol/L; = 0.039)和 90 分钟时(对照组增加 0.44±0.74mmol/L,干预组增加-0.18±0.88mmol/L; = 0.023)。此外,我们观察到胰岛素分泌略有减少,但无统计学意义(对照组增加 353.82±183.31pmol/L,干预组增加 288.43±126.19pmol/L, = 0.302)。有趣的是,储存时间和反复冻融操作似乎会降低应用提取物的疗效。我们应用了几种分析方法(HPLC-MS、GC-MS 和 NMR)来鉴定 CO 提取物中可能的生物活性化合物。我们可以在相关浓度下分配几种物质,包括曲酸(0.33mg/mL)和 5-羟甲基糠醛(2.76mg/mL)。综上所述,这项临床试验以及之前的体外和体内实验证实了我们的番石榴果提取物抑制肠道葡萄糖吸收的功效,可能与减少胰岛素分泌有关。基于这些发现,开发含有这种提取物的食品补充剂或功能性食品似乎对糖尿病患者和预防胰岛素抵抗具有前景。试验注册:415-E/2319/15-2018(萨尔茨堡伦理委员会)。