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50种物质对α-葡萄糖苷酶抑制活性的比较。

Comparison of inhibitory activities of 50 species against α-Glucosidase.

作者信息

Shojaeifard Zahra, Moheimanian Niloofar, Jassbi Amir Reza

机构信息

Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran.

出版信息

J Diabetes Metab Disord. 2023 Sep 26;22(2):1685-1693. doi: 10.1007/s40200-023-01301-6. eCollection 2023 Dec.

DOI:10.1007/s40200-023-01301-6
PMID:37975136
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10638318/
Abstract

OBJECTIVES

Type 2 diabetes is a common metabolic disease affecting millions of people worldwide. α-Glucosidase inhibitors can be used as one of the therapeutic approaches to decrease the postprandial glucose levels through the inhibition of carbohydrate hydrolysis. Medicinal plants are one of the main sources of α-glucosidase's natural inhibitors. In this study, we report the inhibitory effects of 50 different accessions of 32 species against α-glucosidase.

METHODS

To estimate the relative potency of the crude extracts, the inhibitory activities of the 80% methanol of the plants extracts were determined in three different concentrations (1000, 500 and 250 µg/ml) and compared to that of acarbose as the positive control.

RESULTS

and were stronger inhibitors than acarbose (p < 0.05) with IC values in the range of 26.23- 92.35 µg/mL. According to the LC-PDA-ESIMS and NMR analysis of crude extracts of the studied species, 8 phytochemicals including luteolin-7--glucoside ( luteolin-7--glucuronide (), apigenin-7--glucoside (), apigenin-7--glucuronide (), Hispidulin-7--glucuronide (), hispidulin-7--glucoside (), rosmarinic acid (), carnosol () and carnosic acid () were identified as the most common -glucosidase inhibitors. The above compounds constituted the major compounds in the active species in the range of 1.5-95.0%. Among them rosmarinic acid (39-95%) was detected in almost all potent α -glucosidase inhibitor species. Therefore, it can be considered as a biochemical marker in the antidiabetic species in addition to the other minor compounds.

CONCLUSIONS

Considering the high α-glucosidase inhibitory potential of the four- out of fifty species, they are suggested for further antidiabetic tests as potential medicinal plants.

摘要

目的

2型糖尿病是一种常见的代谢性疾病,影响着全球数百万人。α-葡萄糖苷酶抑制剂可作为一种治疗方法,通过抑制碳水化合物水解来降低餐后血糖水平。药用植物是α-葡萄糖苷酶天然抑制剂的主要来源之一。在本研究中,我们报告了32种50个不同种质对α-葡萄糖苷酶的抑制作用。

方法

为了评估粗提物的相对效力,测定了植物提取物80%甲醇在三种不同浓度(1000、500和250μg/ml)下的抑制活性,并与作为阳性对照的阿卡波糖进行比较。

结果

[具体物种1]和[具体物种2]是比阿卡波糖更强的抑制剂(p<0.05),IC值在26.23 - 92.35μg/mL范围内。根据对所研究[具体物种数量]物种粗提物的液相色谱-光电二极管阵列-电喷雾离子质谱(LC-PDA-ESIMS)和核磁共振(NMR)分析,鉴定出8种植物化学物质,包括木犀草素-7-O-葡萄糖苷([具体化学式1])、木犀草素-7-O-葡萄糖醛酸苷([具体化学式2])、芹菜素-7-O-葡萄糖苷([具体化学式3])、芹菜素-7-O-葡萄糖醛酸苷([具体化学式4])、圣草酚-7-O-葡萄糖醛酸苷([具体化学式5])、圣草酚-7-O-葡萄糖苷([具体化学式6])、迷迭香酸([具体化学式7])、鼠尾草酸([具体化学式8])和鼠尾草酚([具体化学式9])为最常见的α-葡萄糖苷酶抑制剂。上述化合物在活性[具体物种数量]物种中占主要化合物的比例在1.5 - 95.0%范围内。其中,几乎所有强效α-葡萄糖苷酶抑制剂物种中都检测到迷迭香酸(39 - 95%)。因此,除了其他次要化合物外,它可被视为抗糖尿病[具体物种数量]物种中的一种生化标志物。

结论

考虑到50个[具体物种数量]物种中有4个具有高α-葡萄糖苷酶抑制潜力,建议将它们作为潜在的药用植物进行进一步的抗糖尿病试验。