Medical application of artabsin A and B as alpha-glucosidase inhibitors and accordingly as materials for preparing antidiabetic drugs
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A technology of glucosidase and galactone, applied in the field of medicine
Active Publication Date: 2020-02-07
南京泓纬医药科技有限公司
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[0006] At present, there is no report that enigninactone A and B are use
Method used
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Embodiment 1
[0018] 1. Test materials
[0019] α-glucosidase (yeast) was purchased from Shanghai Jingke Chemical Technology Co., Ltd.
[0020] p-nitrobenzene-β-D-galactopyranoside and DMSO were analytically pure.
[0021] The purity of acarbose, enininactone A and enininactone B is not less than 98%.
[0022] The brand of 96-well plate is Corning.
[0023] 2. Test method
[0024] According to the method disclosed in the literature (Study on lanolin-type triterpenoids in Chizhi and its α-glucosidase inhibitory activity, Chinese herbal medicine, 2017):
[0025] Solution preparation: take α-glucosidase to prepare 0.2U / mL enzyme solution; take p-nitrophenyl-β-D-galactopyranoside (PNPG) to prepare 2.5mM PNPG solution; prepare pH6 according to conventional formula .8 potassium phosphate buffer solution.
[0026] The inhibition test was carried out in a 96-well plate, and the 140 μL potassium phosphate buffer solution (pH6.8) reaction system in each well contained 20 μL of 0.2 U / mL α-glucosi...
Embodiment 2
[0033] A hypoglycemic tablet, the formula of which comprises 10 mg of cyanolactone A or 10 mg of cyanolactone B, 90 g of starch, and 3 g of magnesium stearate.
[0034] Preparation process: Take enigninactone A or enigninactone B, add starch and magnesium stearate, mix evenly, granulate, dry, and compress into tablets.
Embodiment 3
[0036] A hypoglycemic capsule, the formula of which comprises 10 mg of enigninactone A or enigninactone B, 90 g of starch and 3 g of magnesium stearate.
[0037] Preparation process: Take enigninactone A or enigninactone B, add starch and magnesium stearate, mix evenly, granulate, dry, and pack into capsules.
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Abstract
The invention discloses medical application of artabsin A and B as alpha-glucosidase inhibitors and accordingly as materials for preparing antidiabetic drugs. Research results of the embodiment show that the artabsin A and B have significant inhibition effects on alpha-glucosidase, the inhibition intensities of the artabsin A and B are higher than that of a positive drug acarbose, and thus both the artabsin A and B can be used for preparing the antidiabetic drugs. Furthermore, compared with the artabsin A, the artabsin B has the significantly higher inhibition intensity on the alpha-glucosidase, the inhibition intensity of the artabsin B is 15 times or more that of the artabsin A, and thus the artabsin B is an antidiabetic drug with better prospects.
Description
technical field [0001] The invention belongs to the field of medicine, and in particular relates to the medical use of cylindrolactone A and B as an α-glucosidase inhibitor and further used to prepare hypoglycemic drugs. Background technique [0002] Enininactone A and eninininactone B are a pair of isomers, the difference is only in one connection -OH and -CH 3 The chirality of the carbon atom is different, and the chemical structural formulas of cinnamate A and B are as follows: [0003] [0004] Starch in food is digested by salivary enzymes in the mouth, acid in the stomach, and tryptic amylase in the digestive tract into oligosaccharides, disaccharides, and trisaccharides containing a small number of glucose molecules, and finally passes through the brush border membrane of the small intestinal villi epithelial cells Existing membrane-bound enzymes, maltotriose and disaccharide hydrolase (α-glucosidase, sucrase, maltase), etc. are decomposed into monosaccharides, an...
Claims
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