Hypoglycemic traditional Chinese medicine composition for inhibiting amylase and preparation method of hypoglycemic traditional Chinese medicine composition

Abstract

The preparation method comprises the following steps: respectively weighing the following medicinal materials in percentage by mass: 40% of fructus chebulae immaturus, 40% of fructus hippophae, 10% of silybum marianum and 10% of fructus lycii, and crushing; 10 times of 75-95% ethanol is added into fructus chebulae immaturus, 10 times of 15-95% ethanol is added into fructus hippophae, 10 times of 95% ethanol is added into silybum marianum, 10 times of 15-55% ethanol is added into fructus lycii, reflux extraction is performed in a water bath at the temperature of 60-80 DEG C for 1-2 h, extraction is repeated for 2-3 times, filtrate is combined, and suction filtration is performed; concentrating and drying; purifying and preparing; and carrying out reduced-pressure vacuum concentration. The process is simple, the side effect is small, the amylase inhibition effect is good, and the hypoglycemic effect is remarkable.

Description

Technical Field

[0001] The present invention relates to the technical field of traditional Chinese medicine composition preparation, and particularly relates to an anti-diabetic traditional Chinese medicine composition for inhibiting amylase and a preparation method thereof. Background Art

[0002] Diabetes is a chronic metabolic disease characterized by hyperglycemia and is currently the third most common chronic non-communicable disease after cancer and cardiovascular diseases. In recent years, diabetes has shown a trend of getting younger, and the prevalence rate has been increasing year by year. Data released by the International Diabetes Federation in 2021 showed that there were approximately 540 million diabetes patients aged 20 to 79 years globally, and this number may increase to 640 million by 2030, imposing a huge health and economic burden on individuals and society. Inhibiting the activity of α-amylase is an effective way to improve postprandial blood glucose. α-Amylase is a key digestive enzyme for carbohydrate hydrolysis. Inhibition of its activity can delay the decomposition of carbohydrates such as starch, and the generation and absorption of glucose also slow down accordingly, thereby reducing blood glucose levels. Summary of the Invention

[0003] The purpose of the present invention is to provide an anti-diabetic traditional Chinese medicine composition with amylase inhibitory activity, which has a significant hypoglycemic effect.

[0004] An anti-diabetic traditional Chinese medicine composition for inhibiting amylase activity, calculated by mass percentage, the raw materials are composed of the following components: 40% of Terminalia chebula Retz. fruits, 40% of Hippohgae rhamnoides L. fruits, 10% of Silybum marianum (L.) Gaertn. fruits, and 10% of Lycium barbarum L. fruits.

[0005] Terminalia chebula Retz. fruits, also known as "Tibetan green fruits", are the dried young fruits of the plant Terminalia chebula Retz. of the Combretaceae family and are used as heat-clearing and detoxifying drugs in traditional Chinese medicine clinical practice for compound compatibility in the treatment of diseases such as pneumonia, laryngitis, tonsillitis, pharyngitis, and bacillary dysentery. Terminalia chebula Retz. fruits are rich in tannins and phenolic acid components, and the main chemical components are chebulinic acid, chebelleric acid, and gallic acid, etc.

[0006] Silybum marianum (L.) Gaertn. is a plant of the genus Silybum in the Asteraceae family. Its dried and mature fruits are used as medicine, with a bitter and cool taste, and have the effects of clearing heat and detoxifying, soothing the liver and gallbladder, etc. Modern research has proven that Silybum marianum (L.) Gaertn. is rich in chemical components, mainly including silymarin, silybum protein, and silybum oil, etc. Silymarin is the main functional substance in Silybum marianum (L.) Gaertn., which is a flavonoid compound and has the effects of antioxidant, lipid-lowering, antihypertensive, antidiabetic, anti-atherosclerotic, anti-obesity, liver protection, and anti-cancer.

[0007] Sea buckthorn is a deciduous shrub or tree belonging to the genus Hippophae in the Elaeagnaceae family and contains many nutritionally active components such as vitamins, carotenoids, polyphenols, fatty acids, and phytosterols. Sea buckthorn has many health benefits, such as antioxidant, anti-cancer, anti-hyperlipidemic, anti-obesity, anti-inflammatory, antibacterial, antiviral, dermatological, neuroprotective, and liver-protective activities, etc.

[0008] Lycium barbarum is a plant of the genus Lycium in the Solanaceae family and is mainly distributed in the northwestern, southwestern, central, southern, and eastern regions of China. It was first recorded in "Shennong Ben Cao Jing". It has a sweet taste and a neutral nature, enters the liver and kidney meridians, and has the effects of nourishing the liver and kidney, and improving eyesight with essence. It is commonly used in the treatment of dizziness and tinnitus caused by liver and kidney yin deficiency, deficiency of essence and vitality, weakness of the waist and knees, and other diseases. Modern pharmacological research shows that Lycium barbarum has a variety of chemical components, mainly including polysaccharides, flavonoids, anthocyanins, etc., and has pharmacological effects such as enhancing immunity, anti-aging, anti-tumor, anti-fatigue, hypoglycemic and lipid-regulating, and neuroprotective effects.

[0009] As another object of the present invention, the present invention also provides a preparation method of the above hypoglycemic traditional Chinese medicine composition, and the specific steps are as follows:

[0010] Step 1, extraction of medicinal materials: Weigh the fruits of Terminalia myriocarpa, sea buckthorn, Silybum marianum, and Lycium barbarum according to mass percentages, crush them, and pass through a 40-80 mesh sieve. Add 10 times of ethanol with different concentrations, and perform water bath reflux extraction for multiple times. Combine the filtrates and perform suction filtration;

[0011] Step 2, concentration and drying: Concentrate and dry the above-mentioned filtered extract under reduced pressure and vacuum;

[0012] Step 3, purification and preparation: Take the extract from Step 2, dissolve it in an ethanol solution, adsorb it with AB-8 resin, elute it with ultrapure water, and then elute it with 50% ethanol, and collect the ethanol eluate;

[0013] Step 4, concentration and drying: Concentrate the ethanol eluate collected in Step 3 under reduced pressure and vacuum.

[0014] Preferably, after the fruits of Terminalia myriocarpa are crushed, 75% - 95% ethanol is added for extraction; after the fruits of sea buckthorn are crushed, 15% - 95% ethanol is added for extraction; after the fruits of Silybum marianum are crushed, 95% ethanol is added for extraction; after the fruits of Lycium barbarum are crushed, 15% - 55% ethanol is added for extraction.

[0015] Preferably, in Step 1, water bath reflux extraction is carried out at 60 - 80 °C for 1 - 2 h, and the extraction is repeated 2 - 3 times.

[0016] Preferably, the drying temperature in Step 2 and Step 4 is 40 - 60 °C.

[0017] Preferably, Step 3 is specifically as follows: Take the extract obtained in Step 2, add 75% ethanol solution to dissolve it to a concentration of 1 g / mL, adsorb it with AB-8 resin for 5 h, elute it with ultrapure water for 5 column volumes, and then elute it with 5 times of 50% ethanol, and collect the ethanol eluate.

[0018] The present invention has the following beneficial effects:

[0019] 1. Simple process: No special or complex process steps are involved in the preparation process of this product.

[0020] 2. Small side effects: During the preparation process of this product, there is no need to synthesize and modify the structure of natural products, reducing the generation of human side effects; there is no need to add auxiliary drugs additionally, maintaining the pure natural origin of the ingredients.

[0021] 3. High inhibition rate: Compared with other hypoglycemic products, the traditional Chinese medicine composition of the present invention has a good inhibitory effect on amylase and a significant hypoglycemic effect. Specific embodiments

[0022] Example 1

[0023] This example provides a preparation method of a hypoglycemic traditional Chinese medicine composition for inhibiting amylase activity, and the specific steps are as follows:

[0024] (1) Medicinal material extraction: Weigh Fructus Chebulae 40%, Fructus Hippophae 40%, Silybum marianum 10%, and Fructus Lycii 10% respectively according to mass percentage, crush them, and pass through a 60-mesh sieve. Add 10 times of 95% ethanol to Fructus Chebulae, 10 times of 75% ethanol to Fructus Hippophae, 10 times of 95% ethanol to Silybum marianum, and 10 times of 35% ethanol to Fructus Lycii, and reflux and extract in a water bath at 70°C for 1.5 h. Repeat the extraction 3 times, combine the filtrates, and filter by suction;

[0025] (2) Concentration and drying: Concentrate and dry the extract filtered in Step (1) under reduced pressure and vacuum, at a temperature of 50°C;

[0026] (3) Purification and preparation: Take the extract obtained in Step (2), add 75% ethanol solution to dissolve it to a concentration of 1 g / mL, adsorb it with AB-8 resin for 5 h, elute it with ultrapure water for 5 column volumes, and then elute it with 5 times of 50% ethanol, and collect the ethanol eluate;

[0027] (4) Concentration and drying: Concentrate the 50% ethanol eluate collected in Step (3) under reduced pressure and vacuum, at a temperature of 50°C.

[0028] Perform high-throughput screening for amylase inhibition on the prepared traditional Chinese medicine composition: Based on the decomposition of the substrate corn starch by α-amylase, measure the change in turbidity at 660 nm, so as to determine the inhibitory ability of the extract on α-amylase.

[0029] Through calculation, the combined effect of extracting Terminalia chebula Retz. with 40% by weight and 95% ethanol, Hippohgae rhamnoides L. with 40% by weight and 75% ethanol, Silybum marianum (L.) Gaertn. with 10% by weight and 95% ethanol, and Lycium barbarum L. with 10% by weight and 35% ethanol is as follows: the amylase inhibition rate is 88.29%.

[0030] Example 2

[0031] This example provides a method for preparing a hypoglycemic traditional Chinese medicine composition for inhibiting amylase activity, and the specific steps are as follows:

[0032] (1) Medicinal material extraction: Weigh Terminalia chebula Retz. 40%, Hippohgae rhamnoides L. 40%, Silybum marianum (L.) Gaertn. 10%, and Lycium barbarum L. 10% by mass percentage respectively, crush them, and pass through a 60-mesh sieve. Add 10 times of 75% ethanol to Terminalia chebula Retz., 10 times of 75% ethanol to Hippohgae rhamnoides L., 10 times of 95% ethanol to Silybum marianum (L.) Gaertn., and 10 times of 35% ethanol to Lycium barbarum L., and reflux and extract in a water bath at 70 °C for 1.5 h. Repeat the extraction 3 times, combine the filtrates, and perform suction filtration;

[0033] (2) Concentration and drying: Vacuum concentrate and dry the extract filtered in step (1) under reduced pressure at a temperature of 50 °C;

[0034] (3) Purification and preparation: Take the extract in step (2), add a 75% ethanol solution to dissolve it to a concentration of 1 g / mL, adsorb it with AB-8 resin for 5 h, wash it with ultrapure water for 5 column volumes, and then elute it with 5 times of 50% ethanol, and collect the ethanol eluate;

[0035] (4) Concentration and drying: Vacuum concentrate the 50% ethanol eluate collected in step (3) under reduced pressure at a temperature of 50 °C.

[0036] Perform high-throughput screening for amylase inhibition on the prepared traditional Chinese medicine composition: Based on the decomposition of the substrate corn starch by α-amylase, measure the change in turbidity at 660 nm, so as to determine the inhibitory ability of the extract on α-amylase.

[0037] Through calculation, the combined effect of extracting Terminalia chebula Retz. with 40% by weight and 75% ethanol, Hippohgae rhamnoides L. with 40% by weight and 75% ethanol, Silybum marianum (L.) Gaertn. with 10% by weight and 95% ethanol, and Lycium barbarum L. with 10% by weight and 35% ethanol is as follows: the amylase inhibition rate is 86.36%.

[0038] Example 3

[0039] This example provides a method for preparing a hypoglycemic traditional Chinese medicine composition for inhibiting amylase activity, and the specific steps are as follows:

[0040] (1) Medicinal material extraction: Weigh 40% of Terminalia chebula Retz., 40% of Hippohgae rhamnoides L., 10% of Silybum marianum (L.) Gaertn., and 10% of Lycium barbarum L. by mass percentage respectively, crush them, and pass through a 60-mesh sieve. Add 10 times of 95% ethanol to Terminalia chebula Retz., 10 times of 15% ethanol to Hippohgae rhamnoides L., 10 times of 95% ethanol to Silybum marianum (L.) Gaertn., and 10 times of 35% ethanol to Lycium barbarum L., reflux and extract in a water bath at 70°C for 1.5 h, repeat the extraction 3 times, combine the filtrates, and filter by suction;

[0041] (2) Concentration and drying: Concentrate and dry the filtered extract in step (1) under reduced pressure and vacuum, at a temperature of 50°C;

[0042] (3) Purification and preparation: Take the extract in step (2), add 75% ethanol solution to dissolve it to a concentration of 1 g / mL, adsorb it with AB-8 resin for 5 h, wash it with ultrapure water for 5 column volumes, and then elute it with 5 times of 50% ethanol, and collect the ethanol eluate;

[0043] (4) Concentration and drying: Concentrate the 50% ethanol eluate collected in step (3) under reduced pressure and vacuum, at a temperature of 50°C.

[0044] Perform high-throughput screening for amylase inhibition on the prepared traditional Chinese medicine composition: Based on the decomposition of the substrate corn starch by α-amylase, measure the change in turbidity at 660 nm, so as to determine the inhibitory ability of the extract on α-amylase.

[0045] Through calculation, the combined effect of using 40% of Terminalia chebula Retz. extracted with 95% ethanol, 40% of Hippohgae rhamnoides L. extracted with 15% ethanol, 10% of Silybum marianum (L.) Gaertn. extracted with 95% ethanol, and 10% of Lycium barbarum L. extracted with 35% ethanol is: the amylase inhibition rate is 87.05%.

[0046] Example 4

[0047] This example provides a preparation method of a hypoglycemic traditional Chinese medicine composition for inhibiting amylase activity, and the specific steps are as follows:

[0048] (1) Medicinal material extraction: Weigh 40% of Terminalia chebula Retz., 40% of Hippohgae rhamnoides L., 10% of Silybum marianum (L.) Gaertn., and 10% of Lycium barbarum L. by mass percentage respectively, crush them, and pass through a 60-mesh sieve. Add 10 times of 95% ethanol to Terminalia chebula Retz., 10 times of 75% ethanol to Hippohgae rhamnoides L., 10 times of 95% ethanol to Silybum marianum (L.) Gaertn., and 10 times of 15% ethanol to Lycium barbarum L., reflux and extract in a water bath at 70°C for 1.5 h, repeat the extraction 3 times, combine the filtrates, and filter by suction;

[0049] (2) Concentration and drying: Concentrate and dry the filtered extract in step (1) under reduced pressure and vacuum, at a temperature of 50°C;

[0050] (3) Purification and preparation: Take the extract from step (2), add 75% ethanol solution to dissolve it to a concentration of 1 g / mL, adsorb it with AB-8 resin for 5 h, elute it with ultrapure water for 5 column volumes, and then elute it with 5 times of 50% ethanol, and collect the ethanol eluate;

[0051] (4) Concentration and drying: Concentrate the 50% ethanol eluate collected in step (3) under reduced pressure and vacuum, at a temperature of 50 °C.

[0052] Perform high-throughput screening for amylase inhibition on the prepared traditional Chinese medicine composition: Based on the decomposition of the substrate corn starch by α-amylase, measure the change in turbidity at 660 nm, so as to determine the inhibitory ability of the extract on α-amylase.

[0053] Through calculation, the combined effect of using 40% of Fructus Chebulae, extracting with 95% ethanol, 40% of Hippohgae rhamnoides L., extracting with 75% ethanol, 10% of Silybum marianum (L.) Gaertn., extracting with 95% ethanol, and 10% of Lycium barbarum L. fruits, extracting with 15% ethanol is: the amylase inhibition rate is 86.15%.

[0054] Comparative Example 1

[0055] Compared with Example 1, in this comparative example, weigh 35% of Fructus Chebulae, 35% of Hippohgae rhamnoides L., 15% of Silybum marianum (L.) Gaertn., and 15% of Lycium barbarum L. by mass percentage, and the rest are the same as in Example 1. After testing, the amylase inhibition rate is 82.58%.

[0056] Comparative Example 2

[0057] Compared with Example 1, in this comparative example, weigh 30% of Fructus Chebulae, 30% of Hippohgae rhamnoides L., 20% of Silybum marianum (L.) Gaertn., and 20% of Lycium barbarum L. by mass percentage, and the rest are the same as in Example 1. After testing, the amylase inhibition rate is 78.38%.

[0058] Comparative Example 3

[0059] Compared with Example 1, in this comparative example, Fructus Chebulae is extracted with 15% ethanol at 10 times the amount, and the rest are the same as in Example 1. After testing, the amylase inhibition rate is 43.69%.

[0060] Comparative Example 4

[0061] Compared with Example 1, in this comparative example, Hippohgae rhamnoides L. is extracted with 0% ethanol at 10 times the amount, and the rest are the same as in Example 1. After testing, the amylase inhibition rate is 46.66%.

[0062] Comparative Example 5

[0063] Compared with Example 1, in this comparative example, Silybum marianum (L.) Gaertn. is extracted with 15% ethanol at 10 times the amount, and the rest are the same as in Example 1. After testing, the amylase inhibition rate is 84.83%.

[0064] Comparative Example 6

[0065] In this comparative example, compared with Example 1, the wolfberry fruit was extracted with 10 times the amount of 95% ethanol, and the rest was the same as in Example 1. The amylase inhibition rate was 83.73%.

[0066] Comparative Example 7

[0067] In this comparative example, compared with Example 1, the fructus chebulae was removed, and the rest was the same as in Example 1. The amylase inhibition rate was 50.47%.

[0068] Comparative Example 8

[0069] In this comparative example, compared with Example 1, the seabuckthorn fruit was removed, and the rest was the same as in Example 1. The amylase inhibition rate was 48.17%.

[0070] Comparative Example 9

[0071] In this comparative example, compared with Example 1, the silybum marianum was removed, and the rest was the same as in Example 1. After testing, the amylase inhibition rate was 85.47%.

[0072] Comparative Example 10

[0073] In this comparative example, compared with Example 1, the wolfberry fruit was removed, and the rest was the same as in Example 1. After testing, the amylase inhibition rate was 85.26%.

[0074] From the test results, the traditional Chinese medicine composition obtained by the present invention through selecting a specific medicinal material ratio and under specific extraction and purification conditions has excellent hypoglycemic effect (inhibiting amylase activity).

[0075] The above are only the preferred embodiments of the present invention. All equivalent changes and modifications made according to the scope of the patent application of the present invention shall fall within the scope covered by the present invention.

Claims

1. A preparation method of a hypoglycemic traditional Chinese medicine composition for inhibiting amylase, characterized in that: It includes the following steps: Step 1, medicinal material extraction: Weigh Fructus Chebulae, Hippohgae rhamnoides L., Silybum marianum (L.) Gaertn., and Fructus Lycii medicinal materials respectively according to mass percentage, crush them, and pass through a 40 - 80 mesh sieve. Add 10 times of ethanol with different concentrations, perform water bath reflux extraction for multiple times, combine the filtrates, and perform suction filtration; Step 2, concentration and drying: Concentrate and dry the above - filtered extract under reduced pressure in a vacuum; Step 3, purification and preparation: Take the extract from Step 2, dissolve it in an ethanol solution, adsorb it with AB - 8 resin, elute it with ultrapure water, then elute it with 50% ethanol, and collect the ethanol eluate; Step 4, concentration and drying: Concentrate the ethanol eluate collected in Step 3 under reduced pressure in a vacuum.

2. The preparation method according to claim 1, wherein: By mass percentage, the raw materials in Step 1 are composed of 40% Fructus Chebulae, 40% Hippohgae rhamnoides L., 10% Silybum marianum (L.) Gaertn., and 10% Fructus Lycii.

3. The preparation method according to claim 1, characterized in that: After crushing the Fructus Chebulae medicinal material, extract it with 75% - 95% ethanol; after crushing the Hippohgae rhamnoides L. medicinal material, extract it with 15% - 95% ethanol; after crushing the Silybum marianum (L.) Gaertn. medicinal material, extract it with 95% ethanol; after crushing the Fructus Lycii medicinal material, extract it with 15% - 55% ethanol.

4. The preparation method according to claim 1, wherein: In Step 1, perform water bath reflux extraction at 60 - 80 °C for 1 - 2 h, and repeat the extraction 2 - 3 times.

5. The preparation method according to claim 1, characterized in that: The drying temperature in Step 2 and Step 4 is 40 - 60 °C.

6. The preparation method according to claim 1, characterized in that: Step 3 is specifically: Take the extract from Step 2, dissolve it in a 75% ethanol solution until the concentration is 1 g / mL, load the sample and adsorb it with AB - 8 resin for 5 h, elute it with ultrapure water for 5 column volumes, then elute it with 5 times of 50% ethanol, and collect the ethanol eluate.

7. A traditional Chinese medicine composition with hypoglycemic activity prepared by using the preparation method described in any one of claims 1 - 6.