Institute of Chemistry and Biotechnology, Federal University of Alagoas, Maceio 57072-970, Brazil.
Department of Plant, Food, and Environmental Sciences, Faculty of Agriculture, Dalhousie University, 50 Pictou Road, Truro, NS B2N 5E3, Canada.
Molecules. 2022 Jun 24;27(13):4064. doi: 10.3390/molecules27134064.
The objective of this work was to investigate the antidiabetic, antiglycation, and antioxidant potentials of ethanolic extract of seeds of Brazilian fruits (PESE), a major by-product of the juice industry, and piceatannol (PIC), one of the main phytochemicals of PESE. PESE, PIC, and acarbose (ACB) exhibited IC for alpha-amylase, 32.1 ± 2.7, 85.4 ± 0.7, and 0.4 ± 0.1 µg/mL, respectively, and IC for alpha-glucosidase, 76.2 ± 1.9, 20.4 ± 7.6, and 252 ± 4.5 µg/mL, respectively. The IC of PESE, PIC, and sitagliptin (STG) for dipeptidyl-peptidase-4 (DPP-4) was 71.1 ± 2.6, 1137 ± 120, and 0.005 ± 0.001 µg/mL, respectively. PESE and PIC inhibited the formation of advanced glycation end-products (AGE) with IC of 366 ± 1.9 and 360 ± 9.1 µg/mL for the initial stage and 51.5 ± 1.4 and 67.4 ± 4.6 µg/mL for the intermediate stage of glycation, respectively. Additionally, PESE and PIC inhibited the formation of β-amyloid fibrils in vitro up to 100%. IC values for 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) scavenging activity of PESE and PIC were 20.4 ± 2.1, and 6.3 ± 1.3 µg/mL, respectively. IC values for scavenging hypochlorous acid (HOCl) were similar in PESE, PIC, and quercetin (QCT) with values of 1.7 ± 0.3, 1.2 ± 0.5, and 1.9 ± 0.3 µg/mL, respectively. PESE had no cytotoxicity to the human normal bronchial epithelial (BEAS-2B), and alpha mouse liver (AML-12) cells up to 100 and 50 µg/mL, respectively. However, 10 µg/mL of the extract was cytotoxic to non-malignant breast epithelial cells (MCF-10A). PESE and PIC were found to be capable of protecting cultured human cells from the oxidative stress caused by the carcinogen NNKOAc at 100 µM. The in vitro evidence of the inhibition of alpha-amylase, alpha-glucosidase, and DPP-4 enzymes as well as antioxidant and antiglycation activities, warrants further investigation of the antidiabetic potential of seeds and PIC.
本研究旨在探讨巴西莓种子乙醇提取物（PESE）和白藜芦醇（PIC）的抗糖尿病、抗糖化和抗氧化潜力。PESE、PIC 和阿卡波糖（ACB）对α-淀粉酶的 IC 分别为 32.1 ± 2.7、85.4 ± 0.7 和 0.4 ± 0.1 µg/mL，对α-葡萄糖苷酶的 IC 分别为 76.2 ± 1.9、20.4 ± 7.6 和 252 ± 4.5 µg/mL。PESE、PIC 和西他列汀（STG）对二肽基肽酶-4（DPP-4）的 IC 分别为 71.1 ± 2.6、1137 ± 120 和 0.005 ± 0.001 µg/mL。PESE 和 PIC 抑制晚期糖基化终产物（AGE）的形成，其对糖基化初始阶段和中间阶段的 IC 分别为 366 ± 1.9 和 360 ± 9.1 µg/mL，51.5 ± 1.4 和 67.4 ± 4.6 µg/mL。此外，PESE 和 PIC 可抑制体外β-淀粉样纤维的形成，最高可达 100%。PESE 和 PIC 对 1,1-二苯基-2-苦基肼自由基（DPPH）的清除活性的 IC 值分别为 20.4 ± 2.1 和 6.3 ± 1.3 µg/mL。PESE、PIC 和槲皮素（QCT）对次氯酸（HOCl）的清除活性的 IC 值相似，分别为 1.7 ± 0.3、1.2 ± 0.5 和 1.9 ± 0.3 µg/mL。PESE 在 100 µg/mL 及以下浓度时对人正常支气管上皮（BEAS-2B）和α小鼠肝（AML-12）细胞均无细胞毒性，而 10 µg/mL 的提取物对非恶性乳腺上皮细胞（MCF-10A）有细胞毒性。PESE 和 PIC 可保护培养的人细胞免受致癌剂 NNKOAc 在 100 µM 浓度下引起的氧化应激。PESE 和 PIC 在体外抑制α-淀粉酶、α-葡萄糖苷酶和 DPP-4 酶以及抗氧化和抗糖化活性的证据表明，巴西莓种子和 PIC 具有抗糖尿病的潜力，值得进一步研究。
