Andrade Catarina, Ferreres Federico, Gomes Nelson G M, Gil-Izquierdo Angel, Bapia Sorawit, Duangsrisai Sutsawat, Pereira David M, Andrade Paula B, Valentão Patrícia
REQUIMTE/LAQV, Laboratório de Farmacognosia, Departamento de Química, Faculdade de Farmácia, Universidade do Porto, R. Jorge Viterbo Ferreira, n° 228, 4050-313 Porto, Portugal.
Department of Food Technology and Nutrition, Molecular Recognition and Encapsulation (REM) Group, Universidad Católica de Murcia. UCAM, Campus Los Jerónimos, s/n, 30107 Murcia, Spain.
Food Res Int. 2020 Nov;137:109694. doi: 10.1016/j.foodres.2020.109694. Epub 2020 Sep 16.
Notwithstanding Gustavia gracillima Miers widespread distribution in neotropical regions, its chemical profile and biological properties remain uninvestigated. A methanol extract obtained from the flowers was characterized through HPLC-DAD-ESI/MS, nine ellagic acid derivatives and twelve kaempferol 3-O-glycosides being identified and quantitated for the first time at the species and genus. Preliminary cytotoxicity screening did not reveal noticeable effects upon gastrointestinal representative cell lines (AGS, Caco-2 and Hep G2), which further prompted us to evaluate the impact in a series of targets involved in metabolic disorders and associated complications. Despite of the moderate inhibition towards 5-lipoxygense activity, G. gracillima methanol extract displayed significant effects on carbohydrates-hydrolysing enzymes. In contrast with the antidiabetic reference drug acarbose, the extract was able to selectively inhibit yeast α-glucosidase activity (IC = 4.72 µg/mL), with negligible inhibitory effects upon α-amylase. Kinetic studies pointed to a model of mixed inhibition with a great binding activity, characterized by an inhibitory constant of 2.91 µg/mL. The notable inhibitory activity was also confirmed in α-glucosidase homogenates isolated from human intestinal cells (IC = 34.03 µg/mL). Moreover, the extract obtained from the flowers of G. gracillima displayed significant aldose reductase inhibition (IC = 61.88 µg/mL), as well as O and NO scavenging properties. A moderate inhibitory effect was also recorded against pancreatic lipase (IC = 362.17 µg/mL) through a mixed inhibition mode. Recorded data supports the potential incorporation of G. gracillima flowers on antidiabetic herbal formulations and/or supplements, with not only straight action on carbohydrates digestion, but also direct interference with targets involved on subsequent diabetes events, such as triglycerides metabolism, inflammation and radical-mediated stress.
尽管细叶嘉赐树（Gustavia gracillima Miers）在新热带地区广泛分布，但其化学特征和生物学特性仍未得到研究。通过高效液相色谱-二极管阵列检测-电喷雾电离质谱联用（HPLC-DAD-ESI/MS）对从其花朵中获得的甲醇提取物进行了表征，首次在该物种和属水平上鉴定并定量了9种鞣花酸衍生物和12种山奈酚3-O-糖苷。初步细胞毒性筛选未发现对胃肠道代表性细胞系（AGS、Caco-2和Hep G2）有明显影响，这进一步促使我们评估其对一系列参与代谢紊乱及相关并发症的靶点的影响。尽管细叶嘉赐树甲醇提取物对5-脂氧合酶活性有中度抑制作用，但对碳水化合物水解酶显示出显著作用。与抗糖尿病参考药物阿卡波糖相反，该提取物能够选择性抑制酵母α-葡萄糖苷酶活性（IC = 4.72 μg/mL），而对α-淀粉酶的抑制作用可忽略不计。动力学研究表明其为具有高结合活性的混合抑制模型，抑制常数为2.91 μg/mL。在从人肠道细胞分离的α-葡萄糖苷酶匀浆中也证实了其显著的抑制活性（IC = 34.03 μg/mL）。此外，从细叶嘉赐树花朵中获得的提取物对醛糖还原酶有显著抑制作用（IC = 61.88 μg/mL），以及具有清除超氧阴离子和一氧化氮的特性。通过混合抑制模式对胰脂肪酶也记录到中度抑制作用（IC = 362.17 μg/mL）。记录的数据支持将细叶嘉赐树花朵潜在地纳入抗糖尿病草药制剂和/或补充剂中，其不仅对碳水化合物消化有直接作用，还能直接干扰后续糖尿病相关事件所涉及的靶点，如甘油三酯代谢、炎症和自由基介导的应激。
