Medicinal, Aromatic and Poisonous Plants Research Center (MAPRC), College of Pharmacy, King Saud University, PO Box 2457, Riyadh 11451, Saudi Arabia.
Department of Pharmacognosy, College of Pharmacy, King Saud University, PO Box 2457, Riyadh 11451, Saudi Arabia.
Biomolecules. 2019 Dec 30;10(1):61. doi: 10.3390/biom10010061.
is traditionally used in diabetes treatment in many Arabian countries; however, scientific evidence is lacking. Hence, the present study explored the antidiabetic and antioxidant activities of the plant extracts and their purified compounds. The methanolic crude extract of was partitioned using a two-solvent system. The -hexane fraction was purified by silica gel column chromatography to yield several compounds including katononic acid and 3-oxolupenal. Antidiabetic activities were assessed by α-amylase and α-glucosidase enzyme inhibition. Antioxidant capacities were examined by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) scavenging assays. Further, the interaction between enzymes (α-amylase and α-glucosidase) and ligands (3-oxolupenal and katononic acid) was followed by fluorescence quenching and molecular docking studies. 3-oxolupenal and katononic acid showed IC values of 46.2 μg/mL (101.6 µM) and 52.4 μg/mL (119.3 µM), respectively against the amylase inhibition. 3-oxolupenal (62.3 µg/mL or 141.9 μM) exhibited more potent inhibition against α-glucosidases compared to katononic acid (88.6 µg/mL or 194.8 μM). In terms of antioxidant activity, the relatively polar crude extract and -butanol fraction showed the greatest DPPH and ABTS scavenging activity. However, the antioxidant activities of the purified compounds were in the low to moderate range. Molecular docking studies confirmed that 3-oxolupenal and katononic acid interacted strongly with the active site residues of both α-amylase and α-glucosidase. Fluorescence quenching results also suggest that 3-oxolupenal and katononic acid have a good affinity towards both α-amylase and α-glucosidase enzymes. This study provides preliminary data for the plant's use in the treatment of type 2 diabetes mellitus.
在许多阿拉伯国家，传统上一直将 用于糖尿病治疗；然而，目前缺乏科学证据。因此，本研究探索了该植物提取物及其纯化化合物的抗糖尿病和抗氧化活性。 用两相溶剂系统对 的甲醇粗提取物进行了分配。 -己烷部分通过硅胶柱色谱法进行纯化，得到几种化合物，包括卡酮酸和 3-氧代羽扇豆醇。通过α-淀粉酶和α-葡萄糖苷酶抑制评估抗糖尿病活性。通过 2,2-二苯基-1-苦基肼（DPPH）和 2,2'-联氮-双（3-乙基苯并噻唑啉-6-磺酸）（ABTS）清除测定法检查抗氧化能力。此外，通过荧光猝灭和分子对接研究跟踪了酶（α-淀粉酶和α-葡萄糖苷酶）与配体（3-氧代羽扇豆醇和卡酮酸）之间的相互作用。3-氧代羽扇豆醇和卡酮酸对淀粉酶抑制的 IC 值分别为 46.2μg/mL（101.6μM）和 52.4μg/mL（119.3μM）。与卡酮酸（88.6μg/mL 或 194.8μM）相比，3-氧代羽扇豆醇（62.3μg/mL 或 141.9μM）对α-葡萄糖苷酶的抑制作用更强。就抗氧化活性而言，相对极性的粗提取物和 -丁醇部分显示出最强的 DPPH 和 ABTS 清除活性。然而，纯化化合物的抗氧化活性处于低至中等范围。分子对接研究证实，3-氧代羽扇豆醇和卡酮酸与α-淀粉酶和α-葡萄糖苷酶的活性位点残基强烈相互作用。荧光猝灭结果还表明，3-氧代羽扇豆醇和卡酮酸与α-淀粉酶和α-葡萄糖苷酶均具有良好的亲和力。本研究为该植物在治疗 2 型糖尿病中的应用提供了初步数据。
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