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A kind of α-glucosidase activity inhibitor
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An active inhibitor, a technology of glucosidase, applied in the direction of organic active ingredients, medical preparations containing active ingredients, pharmaceutical formulations, etc., can solve problems such as liver damage
Active Publication Date: 2019-08-06
南通励成生物技术有限公司
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Problems solved by technology
Common hypoglycemic drugs—acarbose, miglitol, and voglibose are all chemically or semichemically synthesized. Although they have a certain hypoglycemic effect, there are bloating, diarrhea, and liver damage in clinical application. and other side effects, so we need to find α-glucosidase inhibitors with less natural side effects from nature
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Embodiment 1
[0025] The extraction of embodiment 1 tea pigment
[0026] Dried Yixing black tea leaves: 80% ethanol by volume = 1:20-30 (g:mL), soaked for 24 hours, filtered, the filtrate was concentrated and evaporated with ethanol, then dissolved in water to obtain alcohol-extracted tea pigment; the filter residue was heated at 60°C Water extraction for 2 hours, repeated 2-3 times, combining each extraction solution, evaporating water to obtain concentrated water-extracted tea pigment. Add equal volumes of chloroform to the alcohol-extracted tea pigment and the water-extracted tea pigment respectively, extract 3-5 times, remove protein and caffeine, and keep the respective water phases for subsequent extraction steps respectively.
[0027] An equal volume of ethyl acetate was added to the aqueous phase, extracted three times and the ethyl acetate phases were combined to obtain an ethyl acetate phase and an aqueous phase.
[0028] For the ethyl acetate phase obtained in the previous step,...
Embodiment 2
[0031] The lyophilized alcohol-soluble and water-soluble theaflavins were made into 25µg / ml, 20µg / ml, 10µg / ml, 5µg / ml, 2.5µg / ml, 1µg / ml with distilled water, and the effect of each dilution concentration on α- Inhibitory ability of glucosidase, and calculate IC 50 . After determination, the IC of alcohol-soluble theaflavins and water-soluble theaflavins 50 They were 3.94µg / ml and 8.19µg / ml, alcohol-soluble theaflavins had a better inhibitory effect on α-glucosidase than water-soluble theaflavins.
Embodiment 3
[0033] The alcohol-soluble and water-soluble thearubigins after freeze-drying were made into 25µg / ml, 20µg / ml, 10µg / ml, 5µg / ml, 2.5µg / ml, 1µg / ml with distilled water, and the effect of each dilution concentration on α- Inhibitory ability of glucosidase, and calculate IC 50 . After determination, the IC of alcohol-soluble thearubigin and water-soluble thearubigin 50 They were 3.24µg / ml and 4.50µg / ml respectively. The inhibitory effect of alcohol-soluble thearubigin on α-glucosidase was slightly better than that of water-soluble thearubigin.
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Abstract
The invention discloses a novel alpha-glucosidase active inhibitor, belonging to the field of functional factors of functional foods and medicines; tea pigments in the invention can be used for strongly inhibiting alpha-glucosidase activity; the IC50 of alcohol-soluble theaflavin, the IC50 of thearubigin and the IC50 of theabrownin are 3.94 mu g / ml, 3.24 mu g / ml and 75.43 mu g / ml respectively; the half inhibition rate IC 50 of alcohol-soluble theaflavin, the half inhibition rate IC50 of thearubigin and the half inhibition rate IC50 of theabrownin are 8.19 mu g / ml, 4.50 mu g / ml and 6.98 mu g / ml respectively; the alpha-glucosidase inhibition effect of alcohol-soluble tea pigments or water-soluble tea pigments is far prior to that of the common hypoglycemic medicine, namely acarbose (acarbose IC50=1.04 mg / ml); and therefore, the novel alpha-glucosidase active inhibitor can be used as a food additive or a medicine for treating diabetes. Because of being pure natural pigments extracted from tea leaves, the tea pigments are safe, nontoxic and better in blood sugar decreasing effect; the advantages of the tea pigments are imponderable by acarbose; and therefore, the novel alpha-glucosidase active inhibitor has the application prospect for being developed into a health-care product or a novel hypoglycaemic medicine.
Description
technical field [0001] The invention relates to an α-glucosidase activity inhibitor, which belongs to the field of functional factors and medicines of functional foods. Background technique [0002] Diabetes is a global endocrine system disease characterized by hyperglycemia, of which type Ⅱ diabetes accounts for more than 90%. Lowering blood sugar levels is an important way to prevent and treat diabetes. Some studies predict that the number of diabetic patients in the world will increase from 171 million in 2000 to 366 million in 2030, and the incidence rate will remain high, while the number of diabetics in developing countries may double. According to the report of the International Diabetes Federation, 5 million people die from diabetes every year in the world. By the end of 2014, the cost of diabetes treatment has exceeded 566 billion. Therefore, the work of preventing and treating diabetes is urgent. [0003] α-glucosidase inhibitors can delay the conversion of polysa...
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