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Molecular Mechanism for the α-Glucosidase Inhibitory Effect of Wheat Germ Peptides
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2021-12-07 , DOI: 10.1021/acs.jafc.1c06098 Weiwei Liu 1 , Hongyan Li 1 , Yangyang Wen 2 , Yingli Liu 1 , Jing Wang 1 , Baoguo Sun 1
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2021-12-07 , DOI: 10.1021/acs.jafc.1c06098 Weiwei Liu 1 , Hongyan Li 1 , Yangyang Wen 2 , Yingli Liu 1 , Jing Wang 1 , Baoguo Sun 1
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Wheat germ peptides (WGPs) have various benefits to human health, while their antidiabetes mechanism remains unknown. In this study, the α-glucosidase inhibition activity of WGPs was identified, exhibiting an IC50 value of 6.87 mg/mL. By further filtrating them into five groups according to molecular weight (Mw), the fraction with Mw < 1 kDa displayed the highest inhibitory activity with an IC50 of 2.10 mg/mL. The addition of 2 mg/mL WGPs with Mw < 1 kDa effectively reduced the glucose-releasing rate on everted intestine sleeves. By virtual screening and HPLC-QTOF-MS/MS, LDLQR, AGGFR, and LDNFR were identified and synthesized for the first time, and their IC50 values were 8.59, 8.66, and 9.21 mM, respectively. Molecular docking and amino acid composition analysis results showed that the high content of C-terminal Arg residues in the peptides could be the essential reason for their α-glucosidase inhibition activity. This study paved a way to utilize WGPs as potential antidiabetes ingredients for the food industry.
中文翻译：
小麦胚芽肽抑制α-葡萄糖苷酶作用的分子机制
小麦胚芽肽 (WGPs) 对人类健康有多种益处，但其抗糖尿病机制尚不清楚。在这项研究中，WGPs 的 α-葡萄糖苷酶抑制活性得到了鉴定，其 IC 50值为 6.87 mg/mL。通过进一步根据分子量（M w）将它们过滤成五组，M w < 1 kDa 的级分显示出最高的抑制活性，IC 50为2.10 mg/mL。添加M w < 1 kDa的 2 mg/mL WGPs有效地降低了外翻肠套上的葡萄糖释放率。通过虚拟筛选和 HPLC-QTOF-MS/MS 首次鉴定合成了 LDLQR、AGGFR 和 LDNFR，其 IC50 个值分别为 8.59、8.66 和 9.21 mM。分子对接和氨基酸组成分析结果表明，肽中C端Arg残基含量高可能是其抑制α-葡萄糖苷酶活性的本质原因。这项研究为利用 WGP 作为食品工业潜在的抗糖尿病成分铺平了道路。
更新日期：2021-12-22
中文翻译：
小麦胚芽肽抑制α-葡萄糖苷酶作用的分子机制
小麦胚芽肽 (WGPs) 对人类健康有多种益处，但其抗糖尿病机制尚不清楚。在这项研究中，WGPs 的 α-葡萄糖苷酶抑制活性得到了鉴定，其 IC 50值为 6.87 mg/mL。通过进一步根据分子量（M w）将它们过滤成五组，M w < 1 kDa 的级分显示出最高的抑制活性，IC 50为2.10 mg/mL。添加M w < 1 kDa的 2 mg/mL WGPs有效地降低了外翻肠套上的葡萄糖释放率。通过虚拟筛选和 HPLC-QTOF-MS/MS 首次鉴定合成了 LDLQR、AGGFR 和 LDNFR，其 IC50 个值分别为 8.59、8.66 和 9.21 mM。分子对接和氨基酸组成分析结果表明，肽中C端Arg残基含量高可能是其抑制α-葡萄糖苷酶活性的本质原因。这项研究为利用 WGP 作为食品工业潜在的抗糖尿病成分铺平了道路。
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