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The medicinal use of enigninactone a and b as an α-glucosidase inhibitor and then for the preparation of hypoglycemic drugs
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A kind of technology of engeninolactone and hypoglycemia, which is applied in the field of medicine to achieve the effect of high inhibition intensity
Active Publication Date: 2022-02-15
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 used as α-glucosidase inhibitors and then used to prepare hypoglycemic drugs
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 the medical use of enigninactone A and B as an α-glucosidase inhibitor and further used in the preparation of hypoglycemic drugs. The research result of the embodiment of the present invention shows that enigninactone A and enigninactone B all have significant inhibitory effect on α-glucosidase, and the inhibitory intensity of the two is better than that of the positive drug acarbose, and both can For the preparation of hypoglycemic drugs. Further, compared with enigninactone A, enigninactone B has a significantly higher inhibitory intensity on α-glucosidase, which is more than 15 times that of enigninactone A, and is a more promising hypoglycemic drugs.
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 few 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, and glucose, l...
Claims
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