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种子水提取物中α-葡萄糖苷酶抑制剂的筛选

Screening of Aqueous Extract of Seeds for Alpha-Glucosidase Inhibitors.

作者信息

Lawal Tajudeen Afolayan

机构信息

Department of Biochemistry and Forensic Science, Faculty of Science, Nigeria Police Academy, Wudil, Kano, Nigeria.

出版信息

Biochem Res Int. 2022 May 14;2022:3492203. doi: 10.1155/2022/3492203. eCollection 2022.

DOI:10.1155/2022/3492203
PMID:35607491
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9124114/
Abstract

Activity of -glucosidase enzyme in the gastrointestinal tract has been implicated in postprandial hyperglycaemia. If not properly controlled, postprandial hyperglycaemia might progress to diabetes mellitus, a metabolic syndrome. Diabetes is associated with many complications such as retinopathy, heart attack, nephropathy, neuropathy, stroke, and lower limb amputation. Antidiabetic medications presently in use have little effect on postprandial glycaemic excursion and hence do not bring down the blood glucose level to baseline. This study extracted, fractionated, and screened the aqueous extract of seeds for hypoglycaemic potential. Inhibitory effects of the fractions and subfractions of the extract on -glucosidase activity were investigated. The most active subfraction was subjected to Fourier transform infrared (FTIR) and gas chromatography mass spectroscopy (GC-MS) analysis to elucidate the active components. The active subfraction showed a significant inhibition ( < 0.05) on -glucosidase. The subfraction competitively inhibits -glucosidase (with IC50 = 09.48 ± 0.58 g/mL), though less potent than the standard drug, acarbose (IC50 = 06.45 ± 0.47 g/mL). FTIR analysis of the subfraction showed the presence of carbonyl group, hydroxy group, carboxyl group, double bonds, methylene, and methyl groups. GC-MS analysis suggests the presence of cis-11,14-eicosadienoic acid, catechin, and chlorogenic acid as the active components. In conclusion, the components obtained from this study can be synthesised in the laboratory to further confirm their hypoglycaemic activity. The most active subfraction can be explored further to confirm its inhibitory activity against the enzyme and to determine its extent in the treatment of diabetes mellitus in vivo.

摘要

胃肠道中α-葡萄糖苷酶的活性与餐后高血糖有关。如果控制不当,餐后高血糖可能会发展为糖尿病,一种代谢综合征。糖尿病与许多并发症相关,如视网膜病变、心脏病发作、肾病、神经病变、中风和下肢截肢。目前使用的抗糖尿病药物对餐后血糖波动影响很小,因此不能将血糖水平降至基线。本研究提取、分离并筛选了种子的水提取物的降血糖潜力。研究了提取物的各馏分和亚馏分对α-葡萄糖苷酶活性的抑制作用。对活性最高的亚馏分进行傅里叶变换红外光谱(FTIR)和气相色谱-质谱联用(GC-MS)分析,以阐明活性成分。活性亚馏分对α-葡萄糖苷酶表现出显著抑制作用(P<0.05)。该亚馏分竞争性抑制α-葡萄糖苷酶(IC50 = 9.48±0.58μg/mL),尽管效力低于标准药物阿卡波糖(IC50 = 6.45±0.47μg/mL)。该亚馏分的FTIR分析表明存在羰基、羟基、羧基、双键、亚甲基和甲基。GC-MS分析表明活性成分包括顺式-11,14-二十碳二烯酸、儿茶素和绿原酸。总之,本研究获得的成分可在实验室合成以进一步确认其降血糖活性。可进一步探索活性最高的亚馏分,以确认其对该酶的抑制活性,并确定其在体内治疗糖尿病的程度。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aaa1/9124114/96f7663d83b9/BRI2022-3492203.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aaa1/9124114/573eb7aadde1/BRI2022-3492203.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aaa1/9124114/3d28e70d37e1/BRI2022-3492203.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aaa1/9124114/4d947273656f/BRI2022-3492203.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aaa1/9124114/4d780bf91a09/BRI2022-3492203.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aaa1/9124114/bc9a4a8be71b/BRI2022-3492203.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aaa1/9124114/96f7663d83b9/BRI2022-3492203.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aaa1/9124114/573eb7aadde1/BRI2022-3492203.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aaa1/9124114/3d28e70d37e1/BRI2022-3492203.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aaa1/9124114/4d947273656f/BRI2022-3492203.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aaa1/9124114/4d780bf91a09/BRI2022-3492203.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aaa1/9124114/bc9a4a8be71b/BRI2022-3492203.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aaa1/9124114/96f7663d83b9/BRI2022-3492203.006.jpg

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