摘要
目的利用内蒙古道地中药材资源优势,从天然植物草药中寻找高效、低毒的α-葡萄糖苷酶抑制剂,为药食同源的降糖药物开发提供研究基础。方法以对硝基苯基-α-D葡萄糖吡喃苷(PNPG)为底物,建立α-葡萄糖苷酶抑制剂体外筛选模型,并对中药材水提物进行筛选。对抑制活性较高的中药材水提物进行酶动力学实验,考察其作用机制,同时对其主要成分进行分析。结果50种中药材中,共筛选出α-葡萄糖苷酶抑制效果强于对照的中药材13种,分别是地榆、锁阳、麻黄、大黄、赤芍、紫草、沙苑子、蒺藜、黄芩、关黄柏、桔梗、升麻、甘草,其中锁阳和地榆的半抑制浓度分别为0.00516 mg/ml和0.00174 mg/ml,表现最为突出。二者的动力学研究显示,锁阳和地榆水提物对α-葡萄糖苷酶的抑制作用都是可逆的,其作用类型属于线性混合型抑制,水提物与阿卡波糖的联合抑制均表现为拮抗作用。成分分析显示,地榆的总黄酮、总多糖、总多酚、总皂苷含量均高于锁阳,两种药材水提物中生物活性成分的含量都表现为总黄酮>总多糖>总多酚>总皂苷。结论地榆、锁阳、麻黄等天然中药材水提物具有一定的体外降糖效果,可以明显抑制α-葡萄糖苷酶活性。
Objective To explore highly efficient and low-toxicityα-glucosidase inhibitors from natural herbal medicines by leveraging the advantages of genuine Chinese medicinal material resources in Inner Mongolia,in order to provide a research basis for the development of hypoglycemic drugs with homology of medicine and food.Methods An in vitro screening model forα-glucosidase inhibitors was established using PNPG as the substrate,and the water extracts of Chinese medicinal materials was screened.Enzymatic kinetics experiments were conducted to investigate the mechanism of action of water extracts with high inhibitory activity from Chinese medicinal materials,and their main components were analyzed.Results Out of 50 types of Chinese medicinal materials tested,13 were screened out for their strongerα-glucosidase inhibition effects than the control.They were Sanguisorba officinalis,Cynomorium songaricum,Ephedra sinica,Rheum palmatum,Paeonia lactiflora,Arnebia euchroma,Astragalus complanatus,Tribulus terrestris,Scutellaria baicalensis,Phellodendron amurense,Platycodon grandiflorum,Cimicifugae and Glycyrrhiza uralensis.The semi-inhibitory concentrations of Cynomorium songaricum and Sanguisorba officinalis were found to be 0.00516 mg/ml and 0.00174 mg/ml,respectively,which were the most significant.Kinetic studies of them demonstrated that the inhibition onα-glucosidase by water extracts from Cynomorium songaricum and Sanguisorba officinalis was reversible,being a linear mixed type of inhibition;the combined inhibition of water extracts with acarbose showed an antagonistic effect.Component analysis revealed that the contents of total flavonoids,total polysaccharides,total polyphenols and total saponins in Sanguisorba officinalis were higher than those in Cynomorium songaricum,and the content of bioactive components in the water extracts of two kinds of medicinal materials showed total flavonoids>total polysaccharides>total polyphenols>total saponins.Conclusion The water extracts from natural Chinese medicinal materials such as Sanguisorba officinalis,Cynomorium songaricum and Ephedra sinica have a certain hypoglycemic effect in vitro,and can significantly inhibitα-glucosidase activity.
作者
薛昕
姜丽丽
李晶
邓凤
徐宋瑶
孙计桃
边艳超
牛丽丽
Xue Xin;Jiang Lili;Li Jing;Deng Feng;Xu Songyao;Sun Jitao;Bian Yanchao;Niu Lili(Laboratory of Biochemistry and Genetics,College of Basic Medicine,Inner Mongolia Medical University,Hohhot 010110,China;Key Laboratory of Molecular Pathology,Inner Mongolia Medical University,Hohhot 010110,China)
出处
《实用药物与临床》
2025年第2期121-126,共6页
Practical Pharmacy and Clinical Remedies
基金
内蒙古自治区高等学校科学研究项目(NJZY22650)。
关键词
中草药
水提物
Α-葡萄糖苷酶
作用机制
成分分析
Chinese herbal medicines
Water extracts
α-glucosidase
Mechanism of action
Component analysis
