Rouzbehan Sahere, Moein Soheila, Homaei Ahmad, Moein Mahmood Reza
a Molecular Medicine Research Center, Hormozgan Health Institute, Hormozgan University of Medical Sciences , Bandar Abbas , IR Iran.
b Biochemistry Department, Faculty of Medicine , Hormozgan University of Medical Sciences , Bandar Abbas , IR Iran.
Pharm Biol. 2017 Dec;55(1):1483-1488. doi: 10.1080/13880209.2017.1306569.
Glucosidases are a group of enzymes playing crucial roles in digestion of carbohydrates. Glucosidase inhibitors can reduce carbohydrate digestion rate and have the potential to prevent development of type 2 diabetes. The Labiatae is one of the largest plant families grown globally and many studies that have isolated new pharmaceutical compounds. In folk medicine, some of Labiatae plants such as Zataria multiflora Boiss, Salvia mirzayanii Rech. F. & Esfand, and Otostegia persica Boiss are consumed for the treatment of diabetes.
This study investigates the inhibitory effects of different fractions of three mentioned species extracts on α-glucosidase.
Ethanol extracts of these plants leaves were fractionated using petroleum ether, chloroform, ethyl acetate, and n-butanol solutions. The duration of this study was 12 months. To measure enzyme inhibition, 5 μL of the enzyme, 20 μL of substrate and samples were used and for evaluation mode of inhibition, constant amounts of α-glucosidase were incubated with rising concentrations of substrate (PNPG).
The results revealed that the ethyl acetate fraction of Zataria multiflora (IC = 0.35 ± 0.01 mg/mL) and petroleum ether fraction of Salvia mirzayanii (IC = 0.4 ± 0.11 mg/mL) were the most potent inhibitors of α-glucosidase in comparison with the other samples and acarbose as the standard (IC = 7 ± 0.19 mg/mL). All of the samples exhibited noncompetitive-uncompetitive inhibition.
It can be inferred from this study that α-glucosidase inhibitory potential of the studied extracts may be a marker of antidiabetic potential of these extracts.
葡萄糖苷酶是一组在碳水化合物消化过程中起关键作用的酶。葡萄糖苷酶抑制剂可降低碳水化合物消化率，具有预防2型糖尿病发生的潜力。唇形科是全球种植的最大植物科之一，许多研究已从中分离出新型药物化合物。在民间医学中，一些唇形科植物，如伊朗藏茴香、米尔扎丹参和波斯绵参，被用于治疗糖尿病。
本研究调查上述三种植物提取物的不同馏分对α-葡萄糖苷酶的抑制作用。
这些植物叶片的乙醇提取物用石油醚、氯仿、乙酸乙酯和正丁醇溶液进行分馏。本研究为期12个月。为测定酶抑制作用，使用5μL酶、20μL底物和样品，为评估抑制模式，将恒定数量的α-葡萄糖苷酶与不断增加浓度的底物（对硝基苯-α-D-吡喃葡萄糖苷）一起孵育。
结果显示，与其他样品及作为标准品的阿卡波糖（IC50 = 7 ± 0.19 mg/mL）相比，伊朗藏茴香的乙酸乙酯馏分（IC50 = 0.35 ± 0.01 mg/mL）和米尔扎丹参的石油醚馏分（IC50 = 0.4 ± 0.11 mg/mL）是最有效的α-葡萄糖苷酶抑制剂。所有样品均表现出非竞争性-非竞争性抑制。
从本研究可以推断，所研究提取物的α-葡萄糖苷酶抑制潜力可能是这些提取物抗糖尿病潜力的一个标志。
