A composition with improved sugar metabolism function and its preparation method and application

Abstract

The present application provides a kind of composition with improved sugar metabolism function and its preparation method and application, the composition is by 15-50 parts by weight of malpighia coccinea leaf extract, 5-20 parts by weight of orange peel extract and 30-70 parts by weight of xianghe extract composition according to weight part;The raw material components of the composition of the present application are derived from new resource food, food and water extract of edible vegetables, have good stability and water solubility, easy to be absorbed by human body, no toxic side effects, high safety, through multi-level, multi-target, multi-angle synergistic effect, reach the purpose of regulating sugar metabolism, maintaining the healthy level of blood sugar of organism.

Description

Technical Field

[0001] The present invention belongs to the technical field of functional foods, and in particular relates to a composition having the function of improving sugar metabolism, a preparation method thereof and an application thereof. Background Art

[0002] According to data released by the International Diabetes Federation in 2021, 537 million adults aged 20 to 79 suffer from diabetes worldwide, and the number of people with diabetes is expected to increase to 643 million and 783 million by 2030 and 2045, respectively. China has the largest number of adult diabetics in the world, reaching 141 million. In addition, approximately 170 million adults have impaired glucose tolerance and approximately 27 million adults have impaired fasting glucose. These groups are the "reserve army" of the diabetic population. Among them, more than 90% have type 2 diabetes, and the blood sugar control rate of the overall diabetic population is less than 50%. It is predicted that by 2045, the number of diabetics in China will reach 174 million. Diabetes has become a major public health problem that seriously affects the physical and mental health of the Chinese people.

[0003] Type 2 diabetes is a complex endocrine and metabolic syndrome, often caused by insulin resistance and pancreatic beta-cell dysfunction, with hyperglycemia as its clinical manifestation. The causes and mechanisms of type 2 diabetes are complex, and the tissues that contribute to hyperglycemia in type 2 diabetes are numerous. Dysfunction in tissues such as the gastrointestinal tract, pancreas, liver, muscle, fat, and kidneys ultimately leads to hyperglycemia.

[0004] Pancreatic α-amylase and intestinal α-glucosidase are the primary digestive enzymes for digesting carbohydrates in food. They are responsible for hydrolyzing carbohydrates in food into disaccharides and monosaccharides, respectively. Monosaccharides are absorbed into the bloodstream through the small intestine. α-glucosidase inhibitors competitively inhibit the catalytic activity of α-glucosidase, delaying the conversion of polysaccharides and disaccharides into absorbable monosaccharides and mitigating the rise in postprandial blood sugar. Representative drugs include acarbose and voglibose.

[0005] The liver is a central organ for glucose metabolism and plays a crucial role in regulating blood sugar and maintaining blood sugar homeostasis. The liver's regulation of blood sugar is primarily manifested in glycolysis, gluconeogenesis, glycogen synthesis, and the uptake, utilization, and release of glucose. Representative medications for improving insulin resistance include metformin.

[0006] Skeletal muscle and adipose tissue are insulin-dependent tissues that utilize glucose. Insulin resistance can lead to impaired glucose metabolism. Therefore, maintaining the normal physiological functions of skeletal muscle and adipose tissue is beneficial for activating the glucose transporter 4 (GLUT4) and preserving the integrity of the insulin signaling pathway. This allows insulin to regulate these tissues and promote glucose uptake. Representative medications for this include pioglitazone and rosiglitazone.

[0007] Under normal physiological concentrations, the kidneys reabsorb all filtered glucose. SGLT2 inhibitors work by inhibiting the activity of the sodium-glucose cotransporter 2 (SGLT2), thereby reducing renal glucose reabsorption and increasing urinary glucose excretion, thereby lowering blood sugar and its toxicity. Representative drugs include dapagliflozin and empagliflozin.

[0008] As mentioned above, currently blood sugar control is mainly based on Western medicine. These drugs have obvious effects in improving sugar metabolism, but they are expensive and have serious side effects. Summary of the Invention

[0009] The purpose of the present invention is to provide a composition with the function of improving sugar metabolism, as well as its preparation method and application. The raw material components are derived from new resource foods, medicinal and edible foods, and water extracts of edible vegetables. They have good stability and water solubility, are easily absorbed and utilized by the human body, have no toxic side effects, and are highly safe. Through multi-level, multi-target, and multi-angle synergistic effects, they achieve the purpose of regulating sugar metabolism and maintaining healthy blood sugar levels in the body.

[0010] In order to achieve the above technical objectives, the present invention adopts the following technical solutions:

[0011] A composition for improving sugar metabolism, comprising the following components in parts by weight:

[0012] 15-50 parts of Hubei crabapple leaf extract;

[0013] 5-20 parts of orange peel extract;

[0014] 30-70 parts of Helianthus annuus extract.

[0015] Furthermore, the composition is composed of the following components in parts by weight:

[0016] 25-40 parts of Hubei crabapple leaf extract;

[0017] 8-15 parts of orange peel extract;

[0018] 45-60 parts of Helianthus annuus extract.

[0019] In the present invention, the Hubei crabapple leaf extract is rich in flavonoids such as phlorizin and 3-hydroxyphlorizin, and its target is the small intestine and kidney. It inhibits the catalytic activity of α-glucosidase in the brush border of the small intestinal mucosa, reduces the rate of glucose decomposition from carbohydrates, reduces and delays the absorption of glucose by the small intestine, and thus reduces the peak blood sugar level after a meal; it inhibits sodium-glucose cotransporter 2 to reduce the renal reabsorption of glucose, increase urine sugar excretion, and thus reduce blood sugar and its toxicity. Tangerine peel extract contains flavonoids such as hesperidin, naringin, and nobiletin, and its target is the liver. It promotes glycolysis by activating the activity of glucose kinase and phosphofructokinase; inhibits gluconeogenesis or glycogenolysis by inhibiting the expression of glucose-6-phosphatase, reducing glucose production; and enhances the activity of glycogen synthase by inhibiting the activity of glycogen synthase kinase-3β, promoting glycogen synthesis in the liver. Xianghe extract contains flavonoids such as anthocyanins, which target skeletal muscle and adipose tissue. It activates the adenylate-activated protein kinase (AMPK) signaling pathway, enhances AMPK phosphorylation, and promotes the uptake and utilization of glucose by skeletal muscle and adipose tissue by upregulating the expression of glucose transporter 4.

[0020] The various natural active ingredients in the composition of the present invention work synergistically at multiple levels, multiple targets, and multiple angles to reduce postprandial blood sugar peaks, regulate liver glucose metabolism, and promote the uptake and utilization of glucose by skeletal muscle and adipose tissue, thereby increasing the sensitivity of insulin receptors and improving insulin resistance, thereby achieving the purpose of improving glucose metabolism and assisting in lowering blood sugar.

[0021] The present invention also provides a method for preparing the above composition, comprising the following steps:

[0022] (1) crushing dried crabapple leaves and tangerine peels to obtain crabapple leaf powder and tangerine peel powder respectively; beating fresh crabapple pulp to obtain crabapple pulp;

[0023] (2) The Hubei crabapple leaf powder is extracted by hot water-stirring dynamic extraction process, and the pH value of the aqueous solution is adjusted to be weakly alkaline. After extraction, the Hubei crabapple leaf extract is obtained by filtration;

[0024] The orange peel powder is extracted by hot water-stirring dynamic extraction process, and the pH value of the aqueous solution is adjusted to be weakly alkaline. After extraction, it is filtered to obtain the orange peel extract;

[0025] The lotus slurry is extracted by hot water-stirring dynamic extraction process, and the pH value of the aqueous solution is adjusted to be acidic, and filtered after extraction to obtain the lotus extract;

[0026] (3) vacuum concentrating each extract, spray drying to obtain each extract powder, and then weighing each extract powder according to the formula and fully mixing to obtain a mixture powder;

[0027] (4) The mixed powder is granulated with pure water or edible alcohol as a binder, passed through a 20-60 mesh sieve for granulation, and dried to a moisture content of ≤5wt% to obtain a composition.

[0028] Furthermore, in step (2), the pH value of the aqueous solution of the Hubei crabapple leaf powder is 8-9, the extraction temperature is 80-90°C, and the number of extractions is 2-3 times; the pH value of the aqueous solution of the tangerine peel powder is 8-9, the extraction temperature is 80-90°C, and the number of extractions is 2-3 times; the pH value of the aqueous solution of the lotus pulp is 2-4, the extraction temperature is 55-70°C, and the number of extractions is 2-3 times.

[0029] Furthermore, in step (3), the pressure of vacuum concentration is -0.07 to -0.09 MPa, and the temperature is 65 to 75°C.

[0030] Furthermore, in step (3), the inlet air temperature of the spray drying is 170-185°C, and the outlet air temperature is 75-85°C.

[0031] The present invention also provides an application of the composition, which is used to prepare functional food or health food with the function of improving sugar metabolism.

[0032] Furthermore, auxiliary materials are added to the composition to prepare tablets, oral liquids, capsules, granules, powders or pills to obtain functional foods or health foods with the function of improving sugar metabolism.

[0033] The present invention has the following advantages and beneficial effects:

[0034] (1) The Hubei crabapple leaf extract, tangerine peel extract, and Xianghe extract in the composition of the present invention are derived from water extracts of new resource foods, medicinal and edible foods, and edible vegetables. They are highly safe, have good stability and water solubility, are easily absorbed and utilized by the human body, and the raw materials are easily available.

[0035] (2) The various natural active ingredients in the composition of the present invention work synergistically at multiple levels, multiple targets, and multiple angles to reduce postprandial blood glucose peaks, regulate liver glucose metabolism, and promote the uptake and utilization of glucose by skeletal muscle and adipose tissue, thereby increasing the sensitivity of insulin receptors and improving insulin resistance, thereby achieving the purpose of improving glucose metabolism and assisting in lowering blood glucose. DETAILED DESCRIPTION

[0036] In order to better understand the technical content of the present invention, specific examples are provided below to further illustrate the present invention. The following examples are merely illustrative and the present invention is not limited to these examples.

[0037] Example 1

[0038] The composition with the function of improving sugar metabolism comprises the following components by weight:

[0039] Hubei leaf extract 35 parts;

[0040] Orange peel extract 10 parts;

[0041] Xianghe extract 55 parts.

[0042] The preparation method mainly comprises the following steps:

[0043] (1) Dry Hubei leaf and orange peel are crushed to obtain Hubei leaf powder and orange peel powder, respectively; fresh Xianghe is pulped to obtain Xianghe slurry;

[0044] (2) The Hubei leaf powder is extracted by hot water-stirring dynamic extraction process, and the pH value of the aqueous solution is adjusted to 8.5-9, the temperature is 85°C, and after extraction for 2 times, filtration is performed to obtain Hubei leaf extract;

[0045] The orange peel powder is extracted by hot water-stirring dynamic extraction process, and the pH value of the aqueous solution is adjusted to 8.5-9, the temperature is 85°C, and after extraction for 2 times, filtration is performed to obtain orange peel extract;

[0046] The Xianghe slurry is extracted by hot water-stirring dynamic extraction process, and the pH value of the aqueous solution is adjusted to 2.5-3, the temperature is 60°C, and after extraction for 2 times, filtration is performed to obtain Xianghe extract;

[0047] (3) Each extract is vacuum concentrated at a pressure of-0.08 MPa and a temperature of 70°C, and then spray dried to obtain an extract powder, with the inlet air temperature set to 180°C and the outlet air temperature set to 80°C; the extract powders are weighed according to the formula, mixed in a three-dimensional mixer for 20 min, and then mixed to obtain a mixture powder;

[0048] (4) The mixture is granulated by a swing granulator with pure water as a binder, sieved through a 40-mesh sieve, and dried at 60°C until the moisture content is ≤5wt%, to obtain the composition.

[0049] Comparative Example 1

[0050] The same as Example 1, except that the formula is only 100 parts by weight of Hubei leaf extract.

[0051] Comparative Example 2

[0052] The same as Example 1, except that the formula is only 100 parts by weight of orange peel extract.

[0053] Comparative Example 3

[0054] The same as Example 1, except that the formula is only 100 parts by weight of Xianghe extract.

[0055] Comparative Example 4

[0056] Same as Example 1, except that the formula comprises 63 parts by weight of Malus melongena leaf extract and 37 parts by weight of tangerine peel extract.

[0057] Comparative Example 5

[0058] Same as Example 1, except that the formula comprises 72 parts by weight of Malus hupehensis leaf extract and 28 parts by weight of Helianthus annuus extract.

[0059] Comparative Example 6

[0060] Same as Example 1, except that the formula comprises 60 parts by weight of tangerine peel extract and 40 parts by weight of lotus root extract.

[0061] 1. Animal test on auxiliary hypoglycemic function

[0062] 1.1 Experimental Animals: 5- to 6-week-old SPF male Kunming mice, weighing 20 ± 2 g, were purchased from Changsha Slake Jingda Biotechnology Co., Ltd. Mice were housed in 20 cages, each containing 5 mice. They were given free access to food and water and acclimated for 5 days at a temperature of 24 ± 2°C, a relative humidity of 40% to 70%, and regular lighting for 12 h daily.

[0063] 1.2 Model Establishment: A type 2 diabetes model was established by continuously feeding a high-sugar, high-fat diet for 4-5 weeks and then administering streptozotocin (STZ) intraperitoneally. A control group of mice was fed a standard maintenance diet and intraperitoneally administered an equal volume of 0.1 mol / L citrate buffer (pH 4.2). Other groups were administered 60 mg / kg of 1% STZ solution for three consecutive days. One week after the injection, mice were assessed for fasting blood glucose levels; mice with fasting blood glucose levels between 11.1 and 25 mmol / L were considered type 2 diabetic.

[0064] 1.3 Animal grouping: Mice with fasting blood glucose concentrations between 11.1 and 25 mmol / L after modeling were evenly divided into 10 groups according to body weight and fasting blood glucose concentration, with 10 mice in each group. They were gavaged according to Table 1, with a gavage volume of 0.1 mL / 10 g body weight.

[0065] Table 1 Grouping of animal hypoglycemic experiments

[0066]

[0067] 1.4 Measurement indicators: Record the weight changes of mice, measure fasting blood glucose, glucose tolerance, serum insulin, liver tissue glycogen and glucokinase activity.

[0068] Fasting blood glucose (FBG): Before grouping and at regular intervals after dosing, blood was drawn from the tail vein of mice for FBG measurement. All animals were fasted for 12 hours (without water withdrawal). Blood was then drawn from the tail vein and measured using a Sinopreneur Glucose Meter and test strips.

[0069] Determination of glucose tolerance test (OGTT): After 6 weeks of continuous oral administration, mice in each group were fasted for 12 hours (water was not withheld during fasting), and blood was collected from the tail vein to measure the blood glucose level before glucose administration (i.e., 0 hour). Then, each group of animals was fed 2.5 g / kg of glucose, and the blood glucose levels of each group were measured 0.5 and 2.0 hours after glucose administration, and the area under the blood glucose curve (AUC) was calculated.

[0070] AUC = [0.5 × (0-hour blood glucose + 0.5-hour blood glucose) ÷ 2] + [1.5 × (0.5-hour blood glucose + 2-hour blood glucose) ÷ 2]

[0071] Insulin determination: After 6 weeks of continuous oral administration, the animals in each group were fasted for 12 hours (water was not withheld during fasting). Eyeballs were removed and blood was collected. The blood was allowed to settle for 30 minutes and then centrifuged at 3500 rpm for 15 minutes. The supernatant was collected and stored at -20°C until use. The serum insulin content of each group of mice was measured according to the operating procedures of a commercial test kit. The insulin resistance index (IRI) and insulin sensitivity index (ISI) were calculated using the HomaModel using the following formulas: IRI = [fasting serum insulin × fasting blood glucose] ÷ 22.5, and ISI = ln[1 / (fasting serum insulin × fasting blood glucose)].

[0072] Assays for hepatic glycogen content and glucokinase activity: Mice were sacrificed by dislocation, and the livers were immediately placed in an ice bath. The livers were then washed with ice-cold saline and dried with filter paper. An appropriate amount of liver was weighed and homogenized to a 10% slurry with ice-cold saline. The slurry was then placed in an ice bath for assays of hepatic glycogen content and glucokinase activity. The hepatic glycogen content and glucokinase activity of the liver tissues of each group of mice were assayed according to the protocols of a commercial assay kit.

[0073] 1.5 Data statistical analysis: One-way analysis of variance was performed using SPSS 19.0 statistical software, and the data were expressed as mean ± standard deviation. P < 0.05 and P < 0.01 indicated statistical significance.

[0074] Table 2 Effects of different groups on the body weight of diabetic mice ( n=10)

[0075]

[0076] Note: In the same column, # indicates P < 0.05 and ## indicates P < 0.01 when compared with the model group.

[0077] As can be seen from Table 2, there was no significant difference in the initial body weight of the mice in each group. Before oral administration, the body weight of the mice in the model group was significantly lower than that in the normal control group, and there was no significant difference in the body weight of the mice in the drug-treated groups and the model group. After 6 weeks of continuous oral administration, the body weight of the mice in the model group was significantly lower than that before oral administration, while the body weight of the mice treated with drug administration was higher than that of the model group. Among them, the Example 1 group, the positive control group, and the comparative examples 4 to 5 groups showed significant differences (P < 0.05), indicating that the composition has a certain inhibitory effect on the weight loss of mice caused by type 2 diabetes, and the inhibitory effect is better than that of the comparative examples 1 to 6 groups.

[0078] Table 3 Effects of different groups on fasting blood glucose in diabetic mice ( n=10)

[0079]

[0080] Note: In the same column, # indicates P < 0.05 and ## indicates P < 0.01 when compared with the model group.

[0081] As shown in Table 3, before oral administration, the fasting blood glucose of the model group mice was significantly higher than that of the normal control group (P < 0.01), and there was no significant difference between the drug-administered groups and the model group. After 2 weeks of oral administration, except for the normal control group, the fasting blood glucose of the mice in other groups showed varying degrees of increase, and there was no significant difference between the groups. After 4 weeks of oral administration, compared with the model group, the fasting blood glucose of the mice in Example 1 group, the positive control group and the comparative example 4-5 groups were significantly reduced (P < 0.05), and the reduction in the Example 1 group was higher than that in the comparative example 1-6 groups. After 6 weeks of oral administration, the fasting blood glucose of the mice in the comparative example 1, 4 and 5 groups was significantly lower than that in the model group (P < 0.05), while the fasting blood glucose of the mice in the Example 1 group and the positive control group was extremely significantly lower than that in the model group (P < 0.01), and the reduction in the Example 1 group was also significantly higher than that in the comparative example 1-6 groups.

[0082] Table 4 Effects of continuous oral administration for 6 weeks on glucose tolerance in diabetic mice ( n=10)

[0083]

[0084]

[0085] Note: In the same column, # indicates P < 0.05 and ## indicates P < 0.01 when compared with the model group.

[0086] As shown in Table 4, compared with the normal control group, the oral glucose tolerance of the model group mice was significantly impaired, and the area under the blood glucose curve was significantly increased, with a very significant difference (P < 0.01). After 6 weeks of continuous oral administration, the area under the blood glucose curve of each treatment group was reduced compared with the model group. Among them, the difference between Example 1 and the positive control group and the model group was very significant (P < 0.01), and the difference between the comparative example groups 1, 4, and 5 and the model group was significant (P < 0.05). In addition, the Example 1 group was superior to the comparative example groups 1 to 6, showing an excellent effect in improving impaired glucose tolerance in mice.

[0087] Table 5 Effects of different groups on glucose metabolism in diabetic mice ( n=10)

[0088]

[0089] Note: In the same column, # indicates P < 0.05 and ## indicates P < 0.01 when compared with the model group.

[0090] As shown in Table 5, the serum insulin, liver glycogen levels and liver glucokinase activity of the model group mice were significantly lower than those of the normal control group (P < 0.01), indicating that the synthesis of serum insulin, liver glucokinase activity and liver glycogen in diabetic mice was significantly reduced by the influence of high-sugar and high-fat diet and streptozotocin. After 6 weeks of continuous oral administration, the serum insulin, liver glycogen levels and glucokinase activity of the mice in Example 1, the positive control group and the comparative example 4-5 groups were all higher than those in the model group, and the differences were significant (P < 0.05). The three indicators of the other groups were also higher than those in the model group, but the differences were not significant. The composition has the effects of promoting the synthesis of serum insulin, liver glucokinase activity and liver glycogen in diabetic mice, and its effect on improving sugar metabolism is better than that of the comparative example 1-6 groups, and slightly better than that of the positive control group.

[0091] Table 6 Effects of different groups on insulin sensitivity in mice ( n=10)

[0092]

[0093]

[0094] Note: In the same column, # indicates P < 0.05 and ## indicates P < 0.01 when compared with the model group.

[0095] As shown in Table 6, the IRI level in the model group was significantly increased (P < 0.01), while the ISI level was significantly decreased (P < 0.01) compared with the normal control group. After 6 weeks of oral administration, the IRI levels of all the drug-treated groups, except for Comparative Example 2 and Comparative Example 3, were significantly decreased, while the ISI levels were significantly increased. Among them, the effect of Example 1 on improving the insulin sensitivity of mice was the best, better than Comparative Example 1 to 6 groups, and close to the effect of the positive control group.

Claims

1. A composition having the function of improving sugar metabolism, characterized in that: According to parts by weight, it is composed of the following components: 35 parts of Hubei crabapple leaf extract; 10 parts of orange peel extract; 55 parts of Helianthus annuus extract; The preparation method mainly comprises the following steps: (1) Crush dried Hubei crabapple leaves and tangerine peels to obtain Hubei crabapple leaf powder and tangerine peel powder respectively; and beat fresh tangerine peels to obtain tangerine peel pulp; (2) The Hubei crabapple leaf powder was extracted using a hot water-stirring dynamic extraction process, and the pH value of the aqueous solution was adjusted to 8.5-9 and the temperature was 85°C. After extraction twice, the Hubei crabapple leaf extract was obtained by filtration. The orange peel powder was extracted by hot water-stirring dynamic extraction process, and the pH value of the aqueous solution was adjusted to 8.5-9 and the temperature was 85°C. The orange peel extract was obtained by filtration after extraction twice. The water chestnut pulp was extracted by hot water-stirring dynamic extraction process, and the pH value of the aqueous solution was adjusted to 2.5-3, the temperature was 60℃, and the extraction was repeated twice and then filtered to obtain the water chestnut extract. (3) Each extract was vacuum concentrated at a pressure of -0.08 MPa and a temperature of 70°C; then, each extract powder was obtained by spray drying, and the inlet air temperature was set at 180°C and the outlet air temperature was set at 80°C; each extract powder was then weighed according to the formula and loaded into a three-dimensional mixer, and fully mixed for 20 minutes to obtain a mixture powder; (4) The mixture is granulated by a swing granulator with pure water as a binder and sieved through a 40-mesh sieve. The granules are dried at 60°C until the moisture content is ≤5wt%, thereby obtaining a composition.

2. The use of the composition according to claim 1, characterized in that The invention can be used for preparing functional food or health food with the function of improving sugar metabolism.

3. The use according to claim 2, characterized in that Add auxiliary materials to the composition to prepare tablets, oral liquids, capsules, granules, powders or pills to obtain functional food or health food with the function of improving sugar metabolism.

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