Composition with hypoglycemic effect and application thereof

Abstract

The invention provides a composition with a hypoglycemic effect and application thereof.The composition comprises a dark plum extract, a pericarpium citri reticulatae extract and a fennel extract, the mass ratio of the dark plum extract to the pericarpium citri reticulatae extract to the fennel extract is (1-5): (1-5): (1-5), and the composition is prepared from common food as a raw material, is safe in component and free of toxic and side effects and has a good hypoglycemic effect. Compared with a single component, the composition has a stronger alpha-glucosidase activity inhibition effect, can promote glucose uptake of cells, achieves the purpose of reducing blood glucose through dual mechanisms, and can be prepared into an oral product for long-term glucose control management of people in need.

Description

Technical Field

[0001] The present invention relates to the field of compositions, and particularly relates to a composition with hypoglycemic effect and its application. Background Art

[0002] With the improvement of modern living standards, the problem of high blood sugar has become increasingly serious, becoming a prominent health hazard. Common drugs for reducing high blood sugar, such as miglitol, voglibose, and acarbose, etc., are prone to side effects such as digestive system disorders, flatulence, and liver poisoning, and some patients have poor drug tolerance, resulting in limited use; while natural products have small side effects and good tolerance. Therefore, it is of great significance to search for natural products with blood sugar-lowering effects.

[0003] Patent CN116058504A discloses a synergistic hypoglycemic composition and a hypoglycemic health drink, which take blueberry, polygonatum sibiricum, and inonotus obliquus as the main raw materials and can achieve good blood sugar-lowering effects. However, blueberry and inonotus obliquus among them do not belong to food raw materials, and there are safety risks in taking them for a long time. Patent CN118178576A discloses a hypoglycemic formula of medicinal and edible homologous plants, which is composed of cassia seed, eucommia ulmoides male flower, pomelo, corn silk, konjac, hawthorn, kudzu root, tartary buckwheat, balsam pear, camel milk, salvia miltiorrhiza, purslane, safflower, and achyranthes bidentata, etc., and can stably lower blood sugar and has functions such as improving pancreatic islet secretion and regulating human immunity. However, the composition of this formula is complex, it is difficult to control the quality of each component, and it is difficult to fully exert the efficacy of each component. Summary of the Invention

[0004] Aiming at the deficiencies of the prior art, the purpose of the present invention is to provide a composition with hypoglycemic effect and its application. The composition includes fructus mume extract, pericarpium citri reticulatae extract, and fructus foeniculi extract, which has a significant inhibitory effect on α-glucosidase activity, and can significantly improve the glucose uptake ability of insulin-resistant cells, has a good hypoglycemic effect, and can be made into an oral product for pre-meal or post-meal blood sugar control management of people in need.

[0005] The present invention provides a composition with hypoglycemic effect, including fructus mume extract, pericarpium citri reticulatae extract, and fructus foeniculi extract, and the mass ratio of the fructus mume extract, pericarpium citri reticulatae extract, and fructus foeniculi extract is 1 - 5:1 - 5:1 - 5.

[0006] As a further improvement of the above solution, the mass ratio of the fructus mume extract, pericarpium citri reticulatae extract, and fructus foeniculi extract is 1 - 5:1 - 5:1.

[0007] As a further improvement of the above solution, the mass ratio of the fructus mume extract, pericarpium citri reticulatae extract, and fructus foeniculi extract is 1:1:1.

[0008] As a further improvement of the above solution, the smoked plum extract, tangerine peel extract and fennel extract are respectively obtained by water extraction using smoked plum, tangerine peel and fennel as raw materials.

[0009] As a further improvement of the above solution, the water extraction process includes the following steps: drying and pulverizing the raw materials of smoked plum, tangerine peel and fennel, mixing them with water at a solid-liquid ratio of 1 g: 5 - 20 mL, performing ultrasonic extraction, concentrating and freeze-drying to obtain the smoked plum extract, tangerine peel extract and fennel extract.

[0010] As a further improvement of the above solution, the water extraction process includes the following steps: drying the raw materials of smoked plum, tangerine peel and fennel at 40 - 60 °C for 50 - 70 min, pulverizing and sieving through a 20 - 40 mesh sieve, mixing them with water at a solid-liquid ratio of 1 g: 5 - 20 mL, performing ultrasonic extraction for 15 - 40 min, filtering, repeating the extraction 2 - 4 times, combining the filtrates, performing vacuum concentration and then freeze-drying to obtain the smoked plum extract, tangerine peel extract and fennel extract.

[0011] As a further improvement of the above solution, the water extraction process includes the following steps: drying the raw materials of smoked plum, tangerine peel and fennel at 50 °C for 60 min, pulverizing and sieving through a 24 mesh sieve, mixing them with water at a solid-liquid ratio of 1 g: 10 mL, performing ultrasonic extraction for 30 min, filtering, repeating the extraction 2 times, combining the filtrates, performing vacuum concentration and then freeze-drying to obtain the smoked plum extract, tangerine peel extract and fennel extract.

[0012] As a further improvement of the above solution, the composition further includes excipients or additives that can be used in food or medicine, and the excipients or additives are one or more of fillers, flavoring agents, antioxidants, thickeners and emulsifiers.

[0013] As a further improvement of the above solution, the filler is one or more of starch, calcium carbonate, maltitol, sorbitol, microcrystalline cellulose.

[0014] As a further improvement of the above solution, the flavoring agent is one or more of sucrose, peppermint oil, essence, citric acid, erythritol, glacial acetic acid, lactic acid, neotame.

[0015] As a further improvement of the above solution, the antioxidant is one or more of vitamin C, vitamin E, tea polyphenols, ascorbyl palmitate, theaflavin.

[0016] As a further improvement of the above solution, the thickener is one or more of sodium alginate, xanthan gum, gelatin, guar gum, agar, locust bean gum.

[0017] As a further improvement of the above solution, the emulsifier includes one or more of sucrose fatty acid esters, phospholipids, Tweens, and Spans.

[0018] An application of the composition according to any one of the above, including using the composition as a raw material to prepare an oral preparation for reducing blood sugar.

[0019] As a further improvement of the above solution, the oral preparation is powder, granule, capsule, tablet, oral solution, emulsion or gel candy.

[0020] Compared with the prior art, the beneficial effects of the present invention are as follows: The composition of the present invention uses extracts of smoked plum, dried tangerine peel and fennel as the main raw materials. Smoked plum can relieve the lung, astringe the intestine and promote the production of body fluid. Dried tangerine peel can regulate qi and strengthen the spleen, dry dampness and resolve phlegm. Fennel can warm yang and dispel cold, regulate qi and relieve pain. Taking them in combination can improve the symptoms of spleen deficiency and dampness accumulation, and excessive thirst and drinking in people with hyperglycemia, achieving the purpose of conditioning the body. It has been proved by experiments that the hypoglycemic composition prepared by the present invention has a good inhibitory effect on the activity of α-glucosidase, and the promoting effect on the glucose uptake of insulin-resistant cells is also significantly better than any single component thereof. It can achieve the purpose of reducing blood sugar through a dual mechanism. Moreover, compared with the common hypoglycemic products in the prior art, the hypoglycemic composition prepared by the present invention uses food raw materials, has high safety, and is more suitable for the long-term blood sugar control management of people in need. Description of the Drawings

[0021] In order to more clearly illustrate the technical solutions in the embodiments of the present invention or the prior art, the following will briefly introduce the drawings required to be used in the embodiments. Obviously, the following drawings are some embodiments of the present invention. For those of ordinary skill in the art, without creative efforts, other drawings can also be obtained based on these drawings.

[0022] Figure 1 It is the inhibitory effect of the hypoglycemic compositions prepared in Examples 2-5 and Comparative Examples 1-20 on the activity of α-glucosidase; Figure 2 It is the inhibitory effect of the hypoglycemic compositions and single extracts prepared in Examples 2-5 and Comparative Examples 21-24 on the activity of α-glucosidase; Figure 3 It is the determination result of the glucose consumption in insulin-resistant HepG2 cells by the samples in each group of Test Example 2. Detailed Embodiments

[0023] To facilitate the understanding of the present invention, the following will describe the present invention more comprehensively and meticulously in combination with the embodiments of the specification and the drawings. However, the protection scope of the present invention is not limited to the following specific embodiments.

[0024] In the embodiments of the present invention, the weights of the relevant components mentioned not only can refer to the specific contents of each component, but also can represent the proportional relationships of the weights between the components. Therefore, as long as the contents of the relevant components in the embodiments of the present invention are enlarged or reduced proportionally, they are within the scope disclosed by the present invention. Specifically, the mass described in the embodiments of the present invention can be mass units well-known in the chemical industry such as μg, mg, g, kg, etc.

[0025] Unless otherwise defined, all the technical terms used hereinafter have the same meanings as commonly understood by those skilled in the art. The technical terms used herein are only for the purpose of describing specific embodiments, and are not intended to limit the protection scope of the present invention.

[0026] Unless otherwise specifically stated, various raw materials, reagents, instruments, equipment, etc. used in the present invention can be obtained through market purchases, or can be prepared by existing methods.

[0027] Example 1 Smoked plums, dried tangerine peels, fennel, dendrobium, astragalus membranaceus, polygonatum sibiricum, polygonatum odoratum and lilium brownii were respectively dried at 50 °C for 60 min, pulverized, and then passed through a 24-mesh sieve. They were mixed with water at a solid-liquid ratio of 1 g:10 mL, ultrasonically extracted for 30 min, filtered, extracted twice repeatedly, and the filtrates were combined. After concentration under reduced pressure, they were freeze-dried to obtain smoked plum extract, dried tangerine peel extract, fennel extract, dendrobium extract, astragalus membranaceus extract, polygonatum sibiricum extract, polygonatum odoratum extract and lilium brownii extract.

[0028] Examples 2-5 According to the weight parts shown in Table 1, smoked plum extract, dried tangerine peel extract and fennel extract were respectively weighed and mixed to obtain a hypoglycemic composition.

[0029]

[0030] Comparative Examples 1-7 According to the weight parts shown in Table 2, dendrobium extract, polygonatum odoratum extract and lilium brownii extract were respectively weighed and mixed to obtain a hypoglycemic composition.

[0031]

[0032] Comparative Example 8 According to the weight parts shown in Table 3, polygonatum sibiricum extract, polygonatum odoratum extract and lilium brownii extract were respectively weighed and mixed to obtain a hypoglycemic composition.

[0033]

[0034] Comparative Example 9 According to the weight parts shown in Table 4, astragalus membranaceus extract, polygonatum odoratum extract and lilium brownii extract were respectively weighed and mixed to obtain a hypoglycemic composition.

[0035]

[0036] Comparative Example 10 Weigh the Dendrobium extract, Polygonatum sibiricum extract and Lilium brownii extract respectively according to the parts by weight shown in Table 5, and mix them to obtain the hypoglycemic composition.

[0037]

[0038] Comparative Examples 11 - 16 Weigh the Astragalus membranaceus extract, Polygonatum odoratum extract and Lilium brownii extract respectively according to the parts by weight shown in Table 6, and mix them to obtain the hypoglycemic composition.

[0039]

[0040] Comparative Examples 17 - 20 Weigh the Astragalus membranaceus extract, Prunus mume extract and Lilium brownii extract respectively according to the parts by weight shown in Table 7, and mix them to obtain the hypoglycemic composition.

[0041]

[0042] Test Example 1: Detect the inhibitory effect on α - glucosidase activity of the hypoglycemic compositions obtained in Examples 2 - 5 and Comparative Examples 1 - 20 according to the following steps.

[0043] 1. Solution preparation: (1) PBS solution (Phosphate - Buffered Saline): Weigh 0.546 g of NaH2PO4 and 6.449 g of Na2HPO4, dissolve them in water, adjust the pH to 6.8, and make up the volume to 500 mL to obtain a 0.1 mol / L PBS solution for standby; (2) pNPG (p - nitrophenyl pyranoside) solution: Accurately weigh 0.3766 g of pNPG, dissolve it with PBS solution, make up the volume to 50 mL, and then dilute it to prepare a 2.5 mmol / L pNPG solution, store it at 4°C for standby; (3) α - glucosidase solution: Dissolve it with PBS solution according to the instructions to prepare an α - glucosidase solution with a concentration of 0.35 U / mL, store it at 4°C for standby; (4) Na2CO3 termination solution: Weigh 2.12 g of Na2CO3, dissolve it with PBS solution, and make up the volume to 100 mL to obtain a 0.2 mol / L Na2CO3 solution for standby; (5)Hypoglycemic composition solution: The hypoglycemic compositions obtained in Examples 2-5 and Comparative Examples 1-20 were respectively dissolved in PBS solution to prepare a hypoglycemic composition solution with a concentration of 10 mg / mL.

[0044] 2. Experimental procedures (1)Sample addition: Sample group: 50 μL of the hypoglycemic composition solution with a concentration of 10 mg / mL was respectively aspirated into EP tubes, and 100 μL of α-glucosidase solution with a concentration of 0.35 U / mL was added and mixed evenly; Sample blank control group: 50 μL of the hypoglycemic composition solution with a concentration of 10 mg / mL was respectively aspirated into EP tubes, and 100 μL of PBS solution was added and mixed evenly; Negative control group: 50 μL of PBS solution was aspirated into EP tubes, and 100 μL of α-glucosidase solution with a concentration of 0.35 U / mL was added and mixed evenly; Blank control group: 150 μL of PBS solution was added to EP tubes; (2)Enzymatic hydrolysis: All tubes were reacted at a constant temperature of 37 °C for 10 min; (3)Chromogenic reaction: 100 μL of pNPG solution with a concentration of 2.5 mmol / L was added to all tubes, and the reaction was carried out at a constant temperature of 37 °C for 20 min; (4)Termination: 50 μL of Na2CO3 solution with a concentration of 0.2 mol / L was added to terminate the reaction; (5)Detection: The reaction solutions in each tube were transferred, and the absorbance (A value) was measured at a wavelength of 400 nm. Each sample was measured in parallel 3 times.

[0045] 3. Data analysis According to the formula: Calculate and analyze the detection results. The α-glucosidase activity inhibition results of the hypoglycemic compositions obtained in Examples 2-5 and Comparative Examples 1-20 are as Figure 1 shown.

[0046] The results show that compared with the hypoglycemic compositions obtained in Comparative Examples 1-20, the hypoglycemic compositions obtained in Examples 2-5 have a better inhibitory effect on α-glucosidase activity.

[0047] Comparative Examples 21-24 According to the weight parts composition shown in Table 8, the dendrobium extract, tangerine peel extract and fennel extract were respectively weighed and mixed to obtain a hypoglycemic composition.

[0048]

[0049] According to the method shown in Test Example 1, the hypoglycemic compositions obtained in Comparative Examples 21-24 and the single extracts such as Prunus mume extract, Citrus reticulata Blanco extract, Foeniculum vulgare Mill. extract, and Dendrobium officinale extract were detected, and the results were compared with the α-glucosidase activity inhibition of the hypoglycemic compositions obtained in Examples 2-5. The results are as Figure 2 shown.

[0050] The results showed that among the single extracts, the Dendrobium officinale extract had a significantly stronger inhibitory effect on α-glucosidase activity than the Prunus mume extract. However, the hypoglycemic composition formed by Prunus mume, Citrus reticulata Blanco, and Foeniculum vulgare Mill. extracts had a significantly stronger inhibitory effect on α-glucosidase activity than the hypoglycemic composition formed by Dendrobium officinale, Citrus reticulata Blanco, and Foeniculum vulgare Mill. extracts, and was superior to any of the single extracts.

[0051] Research has shown that some natural products can also lower blood glucose levels by promoting cell uptake of glucose. To further study the hypoglycemic effect of the hypoglycemic composition of the present invention, experiments related to cell glucose uptake were carried out.

[0052] Test Example 2: 1. Preparation of sample solution: (1) Dissolve Prunus mume extract, Citrus reticulata Blanco extract, Foeniculum vulgare Mill. extract, and the hypoglycemic compositions obtained in Examples 2-5 in phosphate buffer (PBS solution), filter and sterilize to obtain a sample stock solution with a concentration of 10 mg / mL.

[0053] 2. Experimental steps: (1) Cell culture and model establishment Cell culture: Transfer the resuscitated HepG2 cells into a cell flask and grow them in Dulbecco's Modified Eagle Medium (DMEM). Add 10% fetal bovine serum (FBS), 50 U / mL penicillin, and 50 μg / mL streptomycin to the medium as a complete medium, and culture in an environment of 37°C and 5% CO2. Change the medium every other day. When the cells grow to 80%-90% confluence, passage them, and use them after 5 passages.

[0054] Cell model establishment: Adjust the cell concentration to 1×10 5 cell / mL, inoculate it in a 96-well culture plate, and culture it in an environment of 37°C and 5% CO2 for 24 h. The cells adhere and grow, and discard the culture solution. Serum-starve for 24 h, and then add insulin at 10 -7 mol / L and incubate for 24 h (without FBS) to obtain a HepG2 cell insulin resistance model.

[0055] (2) Detection of glucose consumption After incubating the cells with insulin for 24 h, aspirate the supernatant, wash twice with PBS, add the sample solution (the original sample solution is diluted to a concentration of 1 mg / mL in complete medium), collect the culture supernatant after incubating for 24 h, and use a glucose detection kit (Shanghai Beyotime Biotechnology Co., Ltd.) to detect the glucose content in the supernatant.

[0056] Measure the OD values of the cell culture supernatant in each well and the blank well without inoculated cells (culture medium with known sugar content) at 630 nm with an enzyme-labeled instrument, calculate the glucose content in the culture medium of each well according to the standard concentration of glucose, and subtract the average sugar content of the blank well without inoculated cells to calculate the glucose consumption. 。

[0057] The results are as Figure 3 shown. The results show that the glucose consumption of the sample group treated with a single extract is slightly lower than that of the model group, while the glucose consumption of the sample group treated with the hypoglycemic composition is significantly higher than that of the model group, indicating that compared with a single extract, the use of the hypoglycemic composition obtained in Examples 2-5 of the present invention can significantly improve the glucose uptake ability of insulin-resistant cells. In addition, among the sample groups treated with the hypoglycemic composition, the glucose consumption of the cells treated with the hypoglycemic composition obtained in Example 2 is closer to that of the blank group, indicating that combining Prunus mume extract, Citrus reticulata Blanco extract and Foeniculum vulgare Mill. extract in a mass ratio of 1:1:1 can achieve a better hypoglycemic effect.

[0058] The above are only the preferred embodiments of the present application and are not intended to limit the present application. Any modifications, equivalent substitutions, and improvements made within the spirit and principle of the present application shall be included in the protection scope of the present application.

Claims

1. A composition with hypoglycemic effect, characterized in that, It includes smoked plum extract, tangerine peel extract and fennel extract, and the mass ratio of the smoked plum extract, tangerine peel extract and fennel extract is 1 - 5:1 - 5:1 - 5.

2. The composition according to claim 1, characterized in that, The mass ratio of the smoked plum extract, tangerine peel extract and fennel extract is 1 - 5:1 - 5:

1.

3. The composition according to claim 1, wherein The mass ratio of the smoked plum extract, tangerine peel extract and fennel extract is 1:1:

1.

4. The composition according to any one of claims 1 to 3, characterized in that, The smoked plum extract, tangerine peel extract and fennel extract are respectively obtained by water extraction treatment using smoked plum, tangerine peel and fennel as raw materials.

5. The composition according to claim 4, wherein The water extraction treatment includes the following steps: drying and pulverizing the raw materials of smoked plum, tangerine peel and fennel, mixing them with water according to a solid - liquid ratio of 1 g:5 - 20 mL, performing ultrasonic extraction, concentrating and freeze - drying to obtain the smoked plum extract, tangerine peel extract and fennel extract.

6. The composition according to claim 5, characterized in that, The water extraction treatment includes the following steps: drying the raw materials of smoked plum, tangerine peel and fennel at 50 °C for 60 min, pulverizing and passing through a 24 - mesh sieve, mixing them with water according to a solid - liquid ratio of 1 g:10 mL, performing ultrasonic extraction for 30 min, filtering, repeating the extraction 2 times, combining the filtrates, performing vacuum concentration and then freeze - drying to obtain the smoked plum extract, tangerine peel extract and fennel extract.

7. The composition according to any one of claims 1-6, characterized in that, The composition further includes excipients or additives that can be used in food or medicine, and the excipients or additives are one or more of fillers, flavoring agents, antioxidants, thickeners and emulsifiers.

8. Use of the composition according to any one of claims 1-7, characterized in that, It includes using the composition as a raw material to prepare an oral preparation for reducing blood sugar.

9. The application according to claim 8, wherein The oral preparation is powder, granule, capsule, tablet, oral solution, emulsion or gel candy.

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