Inhibitory activities of cyanidin and its glycosides and synergistic effect with acarbose against intestinal α-glucosidase and pancreatic α-amylase.
Inhibitory activities of cyanidin and its glycosides and synergistic effect with acarbose against intestinal α-glucosidase and pancreatic α-amylase.
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DOI：
10.3390/ijms11093387
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发表时间：
2010-09-20
影响因子：
5.6
通讯作者：
Adisakwattana S
中科院分区：
文献类型：
--
作者：
Akkarachiyasit S;Charoenlertkul P;Yibchok-Anun S;Adisakwattana S
矢车菊素及其苷类是一种天然的膳食色素，对人类有潜在的益处，特别是在预防和治疗糖尿病方面。本文研究了矢车菊素及其苷类化合物体外抑制肠道α-葡萄糖苷酶和胰腺α-淀粉酶的构效关系。结果表明，矢车菊素及其苷类是比麦芽糖酶更特异的肠道蔗糖酶抑制剂。矢车菊素-3-半乳糖苷和矢车菊素-3-葡萄糖苷是对肠蔗糖酶和胰腺α-淀粉酶最有效的抑制剂，IC 50值分别为0.50 ± 0.05和0.30 ± 0.01 mM。结果表明，矢车菊素3-O-位葡萄糖和半乳糖的结构差异是影响小肠蔗糖酶和胰腺α-淀粉酶抑制的重要因素。矢车菊素-3-葡萄糖苷、矢车菊素-3-半乳糖苷或矢车菊素-3，5-二葡萄糖苷与低浓度阿卡波糖的组合显示出对肠麦芽糖酶和蔗糖酶的协同抑制作用。还发现矢车菊素或矢车菊素-3-葡萄糖苷与低浓度阿卡波糖的组合具有协同抑制作用。这一发现可能为天然存在的肠道α-葡萄糖苷酶和胰腺α-淀粉酶抑制剂用于预防和治疗糖尿病及其并发症提供新的见解。
Cyanidin and its glycosides are naturally dietary pigments which have been indicated as promising candidates to have potential benefits to humans, especially in the prevention and treatment of diabetes mellitus. We investigated the structure activity relationships of cyanidin and its glycosides to inhibit intestinal α-glucosidases and pancreatic α-amylase in vitro. The results found that cyanidin and its glycosides are more specific inhibitors of intestinal sucrase than intestinal maltase. Cyanidin-3-galactoside and cyanidin-3-glucoside were the most potent inhibitors against intestinal sucrase and pancreatic α-amylase with IC50 values of 0.50 ± 0.05 and 0.30 ± 0.01 mM, respectively. Our findings indicate that the structural difference between glucose and galactose at the 3-O-position of cyanidin was an important factor for modulating the inhibition of intestinal sucrase and pancreatic α-amylase. The combination of cyandin-3-glucoside, cyanidin-3- galactoside or cyanidin-3,5-diglucosides with a low concentration of acarbose showed synergistic inhibition on intestinal maltase and sucrase. The synergistic inhibition was also found for a combination of cyanidin or cyanidin-3-glucoside with a low concentration of acarbose. The findings could provide a new insight into a use for the naturally occurring intestinal α-glucosidase and pancreatic α-amylase inhibitors for the prevention and treatment of diabetes and its complications.
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