Inhibitory activities and rules of plant gallotannins with different numbers of galloyl moieties on sucrase, maltase and α-amylase in vitro and in vivo

	Inhibitory activities and rules of plant gallotannins with different numbers of galloyl moieties on sucrase, maltase and α-amylase in vitro and in vivo
	Liu, Liying; Jia, Wenjing; Jiang, Sirong; Zhang, Guoying; Zhao, Jianzhong; Xu, Jiyu; Wang, Luya; Wu, Di; Tao, Jihong; Yue, Huilan
刊名	PHYTOMEDICINE
	2023
卷号	120
英文摘要	Background: alpha-Glucosidase inhibitors could effectively reduce postprandial blood glucose (PBG) levels and control the occurrence of complications of diabetes. Gallotannins (GTs) in plants have attracted much attention due to their significant alpha-glucosidase inhibitory activities in vitro. However, there is still a lack of systematic comparative studies to further elucidate inhibitory activities in vivo and in vitro of these compounds against alpha-glucosidase, especially for mammalian sucrase and maltase, and analyze their structure-activity relationship. Purpose: Determine the in vitro and in vivo inhibitory activities of five GTs with different number of galloyl moieties (GMs) on sucrase, maltase and alpha-amylase, and elucidate the relationship between alpha-glucosidase inhibitory activities and the number and connection mode of GMs. Methods: Molecular docking and dynamics were used to study the binding mode and binding ability of five GTs against sucrase, maltase and alpha-amylase. Then, the inhibitory activities and inhibitory mechanisms of these compounds on sucrase, maltase and alpha-amylase in vitro were studied using inhibitory assay and enzyme inhibition kinetics. Further, the hypoglycemic effects in vivo of these compounds were demonstrated by three poly-saccharides tolerance experiments on diabetes model mice. Results: The results of molecular docking showed that these compounds could bind to enzymes through hydrogen bonds, hydrophobic interactions, etc. In addition, the alpha-glucosidase inhibition comparative studies in vitro and in vivo demonstrated that the inhibitory activities of these compounds on all three sucrase, maltase and alpha-amylase were ranked as TA approximate to PGG > TeGG > TGG > 1GG, and their inhibitory activities increases with the increase in the number of GMs. Moreover, the hypoglycemic effects of 1,2,3,4,6-pentagalloylglucose (PGG) and tannic acid (TA) in vitro and in vivo were also confirmed to be equivalent to or even stronger than that of acarbose. Conclusion: alpha-Glucosidase inhibitory activities in vitro and in vivo of GTs were positively correlated with the number of GTs, and the more the number, the stronger the activity. However, PGG with five GTs and TA with ten GTs showed almost identical alpha-glucosidase inhibitory activities, possibly due to the reduced binding force with the enzyme caused by spatial hindrance.
内容类型	期刊论文
源URL	[http://210.75.249.4/handle/363003/61574]
专题	西北高原生物研究所_中国科学院西北高原生物研究所
推荐引用方式 GB/T 7714	Liu, Liying,Jia, Wenjing,Jiang, Sirong,et al. Inhibitory activities and rules of plant gallotannins with different numbers of galloyl moieties on sucrase, maltase and α-amylase in vitro and in vivo[J]. PHYTOMEDICINE,2023,120.
APA	Liu, Liying.,Jia, Wenjing.,Jiang, Sirong.,Zhang, Guoying.,Zhao, Jianzhong.,...&Zhao, Xiaohui.(2023).Inhibitory activities and rules of plant gallotannins with different numbers of galloyl moieties on sucrase, maltase and α-amylase in vitro and in vivo.PHYTOMEDICINE,120.
MLA	Liu, Liying,et al."Inhibitory activities and rules of plant gallotannins with different numbers of galloyl moieties on sucrase, maltase and α-amylase in vitro and in vivo".PHYTOMEDICINE 120(2023).