LU501691B1

LU501691B1 - Composition with weight-losing and lipid-lowering activity and product

Info

Publication number: LU501691B1
Application number: LU501691A
Authority: LU
Inventors: Jingjing Dai; Wan Sun; Maowa Li
Original assignee: Eternal Grace Pte Ltd
Priority date: 2022-03-18
Filing date: 2022-03-18
Publication date: 2022-09-19

Abstract

The present disclosure provides a composition with weight-losing and lipid-lowering activity, and belongs to the technical field of food and health care products. The composition with the weight-losing and lipid-lowering activity is prepared from green tea extract, citrus extract and betaine. The three components in the composition reduce energy intake of a human body from different mechanisms, inhibit further generation of adipocytes and promote oxidative decomposition of the existing adipocytes.

Description

COMPOSITION WITH WEIGHT-LOSING AND LIPID-LOWERING LUS01691

ACTIVITY AND PRODUCT TECHNICAL FIELD

[0001] The present disclosure relates to the technical field of foods and health-care products, and particularly relates to a composition with weight-losing and lipid-lowering activity and a product.

BACKGROUND ART

[0002] More than 95% of obese patients belong to simple obesity. The direct cause is that calorie intake is greater than consumption, which leads to excessive energy synthesis of fat and induces obesity. A large number of studies have shown that obesity is closely related to a variety of diseases such as insulin resistance, diabetes, non-alcoholic fatty liver disease, hypertension, hyperlipidemia, coronary atherosclerosis, osteoarthritis, obstructive sleep apnea. Obesity has become a major public health problem worldwide, and it is of great social significance to increase the research on the prevention and treatment of obesity.

[0003] Weight loss can reduce excess body fat, reduce body weight, reduce the risk of obesity, alleviate the occurrence of obesity complications, and improve the health conditions of patients. At present, the prevention and treatment of obesity mainly include diet control, exercise therapy, surgical therapy, drug therapy, natural product intervention, etc. Diet control and exercise therapy require high willpower and have a low success rate. However, surgical therapy and drug therapy have high side effects and limited application. Natural plant extracts have high acceptance level and rapid development, however, most of the existing natural plant extracts are based on the mechanism of increasing satiety and reducing food intake to lose weight, which requires the change in dietary habits in actual applications, so the weight loss effect is not ideal, and patients cannot persist. Therefore, there is a need for a weight loss product that can reduce the body weights through the comprehensive effect of different weight loss mechanisms, is safe and free of side effects.

SUMMARY

[0004] In view of this, the present disclosure aims at providing a composition with weight-losing and lipid-lowering activity. The fat intake of human bodies can be reduced through different lipid-lowering and weight-losing mechanisms and the fat consumption is increased; and meanwhile, the composition also has the effects of resisting oxidization, lowering blood lipid, etc. and is safe and has no side effect.

[0005] In order to achieve the above object, the present disclosure provides the following technical solutions:

[0006] A composition with weight-losing and lipid-lowering activity comprises the following components in parts by weight: 20-30 parts of green tea extract, 10-20 parts of citrus extract and 0.5-5 parts of betaine.

[0007] Preferably, the composition comprises 25 parts of green tea extract, 15 parts of 1 citrus extract and 1 part of betaine. Among them, the green tea extract can effectively LU501691 inhibit the activity of digestive enzymes, reduce the digestion and absorption process of carbohydrates and fats in the body, to achieve the effect of losing weight; promote the oxidation of mitochondria in the liver and reduce the accumulation of fat in the internal organs and liver; alleviate high-fat diet-induced obesity and metabolic syndrome, reduce lipid absorption, and reduce the level of inflammatory cytokines. It has antioxidant effects and can significantly reduce the risk of obesity complications. The citrus extract can increase the P-oxidation of fat, stimulate fat decomposition, induce apoptosis of adipocytes, and reduce the amount of existing fat; inhibit the differentiation of pre-adipocytes into mature adipocytes and reduce the formation of adipocytes. The betaine can not only protect the liver, but also inhibit fat production and stimulate fatty acid oxidation, thereby regulating lipid metabolism and increasing the expression of lipid catabolism enzymes, playing a role in weight loss. The three types of components in the composition of the present disclosure are synergistic, reducing the energy intake of the human body from different mechanisms respectively, inhibiting the further formation of adipocytes, and promoting the oxidative decomposition of existing adipocytes. Meanwhile, the composition can relieve the metabolic syndrome and related diseases caused by obesity while lose weight, and is safe and effective.

[0008] Preferably, the mass percentage of EGCG in the green tea extract is 30-80%, more preferably 60%, and the EGCG is epigallocatechin gallate.

[0009] Preferably, a method for preparing the green tea extract comprises the following steps: mixing green tea with ethanol with the volume percent fraction of 40-80%, extracting at 25-50°C for 15-60 min, repeatedly extracting for 2-4 times, combining filtrates, concentrating under reduced pressure, and performing spray drying to obtain the green tea extract; More preferably, comprising: mixing green tea with ethanol with the volume percent fraction of 75%, extracting at 40°C for 30 min, repeatedly extracting for 3 times, combining filtrates, concentrating under reduced pressure, and performing spray drying to obtain the green tea extract.

[0010] Preferably, the mass volume ratio of green tea to ethanol is 1: (10-25), and more preferably 1: 20.

[0011] Preferably, the content of flavone is 10-30%, and more preferably 20% in the citrus extract.

[0012] Preferably, the citrus extract comprises a pomelo extract and/or an orange extract.

[0013] Preferably, a method for preparing the citrus extract comprises the following steps: squeezing and crushing citrus fruits or peels, mixing with a solvent, extracting at 25-50°C for 10-120 min, filtering, placing the resulting filtrate at 2-8°C for 4-12 h, performing vacuum concentration on the supernatant, and drying, to obtain the citrus extract; More preferably, comprising: squeezing and crushing citrus fruits or peels, mixing with a solvent, extracting at 35°C for 60 min, filtering, placing the resulting filtrate at 4°C for 8 h, performing vacuum concentration on the supernatant, and drying, to obtain the citrus extract.

2

[0014] Preferably, the mass ratio of the citrus fruits or peels to the solvent is 1: (2-10), LU501691 and more preferably 1: 5.

[0015] Preferably, the solvent comprises water or ethanol with the volume percent fraction of 30-50%, and more preferably, the solvent is ethanol with the volume percent fraction of 40%.

[0016] Preferably, the drying comprises vacuum drying or spray drying, and more preferably vacuum drying.

[0017] The present disclosure also provides a product with weight-losing and lipid-lowering activity. The product is prepared into tablets, granules or capsules from the composition and auxiliary materials, or is prepared into foods by matching the composition with other edible components.

[0018] The sources of the raw materials involved in the present disclosure are not particularly limited, and commercially available products known in the art can be used.

[0019] Compared with the prior art, the present disclosure has the following beneficial effects.

[0020] The present disclosure provides a composition with weight-losing and lipid-lowering activity, comprising the components of green tea extract, citrus extract and betaine. Among them, the green tea extract can inhibit the activity of digestive enzymes, reduce the digestion and absorption of carbohydrates and fats in the body, thereby reducing energy intake; promote the oxidation of mitochondria in the liver and reduce the accumulation of fats in the internal organs. The citrus extract can promote the oxidation of fat at the molecular level, stimulate the decomposition, induce the apoptosis of adipocytes, and inhibit the formation of adipocytes. On the one hand, it can reduce the quantity and quality of existing adipocytes, and on the other hand, it can prevent the formation of new adipocytes. Betaine protects the liver and inhibits adipogenesis, reduces hepatic lipid accumulation, and increases systemic energy consumption. The three types of components in the composition of the present disclosure are synergistic, reducing the energy intake of the human body from different mechanisms respectively, inhibiting the further formation of adipocytes, and promoting the oxidative decomposition of existing adipocytes. Meanwhile, the composition can relieve the metabolic syndrome and related diseases caused by obesity while lose weight, and is safe and effective.

BRIEF DESCRIPTION OF THE DRAWINGS

[0021] FIG. 1 shows the weight difference of three groups of mice after 8 weeks in Test Example 1, wherein SD represents a control group, GTP represents a single-formula group, GCB represents a compound group, and **p<0.01, n=10;

[0022] FIG. 2 shows the difference of total cholesterol (left figure) and triglyceride (right figure) of three groups of mice before and after 8 weeks in the Test Example 1. SD represents a control group, GTP represents a single-formula group, GCB represents a compound group, and **p<0.01, n=10; and

[0023] FIG. 3 shows the difference of high-density lipoprotein (left figure)and low-density lipoprotein (right figure) of three groups of mice before and after 8 weeks 3 in Test Example 1. SD represents a control group, GTP represents a single-formula LU501691 group, GCB represents a compound group, and **p<0.01, n=10.

DETAILED DESCRIPTION OF THE EMBODIMENTS

[0024] The technical solutions provided by the present disclosure will be described in detail below with reference to the embodiments, but they should not be construed as limiting the protection scope of the present disclosure.

[0025] Example 1

[0026] Preparation of green tea extract: mix 10 g of green tea with 200 ml of ethanol with the volume percent fraction of 75%, extracting at 40°C for 30 min, repeatedly extracting for 3 times, combining filtrates, concentrating under reduced pressure, and performing spray drying to obtain the green tea extract. The mass percentage of EGCG in green tea extract is 60%.

[0027] Preparation of citrus extract: squeeze and crush 10 g of fresh citrus fruits, mix with 50 ml of ethanol with the volume percent fraction of 40%, extract at 35°C for 60 min, filter, place the resulting filtrate at 4°C for 8 h, perform vacuum concentration on the supernatant, and vacuum drying, to obtain the citrus extract. The flavanone content in the citrus extract is 20%.

[0028] Mix the green tea extract, the citrus extract and betaine according to a mass ratio of 25:15:1 to obtain a composition with weight-losing and lipid-lowering activity.

[0029] Example 2

[0030] Preparation of green tea extract: mix 10 g of green tea with 100 ml of ethanol with the volume percent fraction of 80%, extracting at 25°C for 60 min, repeatedly extracting for 4 times, combining filtrates, concentrating under reduced pressure, and performing spray drying to obtain the green tea extract. The mass percentage of EGCG in green tea extract is 80%.

[0031] Preparation of citrus extract: squeeze and crush 10 g of citrus peels, mix with a 100 ml of water, extract at 50°C for 10 min, filter, place the resulting filtrate at 2°C for 12 h, perform vacuum concentration on the supernatant, and vacuum drying, to obtain the citrus extract. The flavanone content in the citrus extract is 30%.

[0032] Mix the green tea extract, the citrus extract and betaine according to a mass ratio of 20:10:0.5 to obtain a composition with weight-losing and lipid-lowering activity.

[0033] Example 3

[0034] Preparation of green tea extract: mix 10 g of green tea with 250 ml of ethanol with the volume percent fraction of 40%, extracting at 450°C for 15 min, repeatedly extracting for 2 times, combining filtrates, concentrating under reduced pressure, and performing spray drying to obtain the green tea extract. The mass percentage of EGCG in green tea extract is 30%.

[0035] Preparation of citrus extract: squeeze and crush 10 g of fresh citrus fruit, mixing with a 100 ml of ethanol with the volume percent fraction of 30%, extract at 35°C for 120 min, filter, place the resulting filtrate at 8°C for 4 h, perform vacuum concentration on the supernatant, and vacuum drying, to obtain the citrus extract. The flavanone content in the citrus extract is 28%.

4

[0036] Mix the green tea extract, the orange extract and betaine according to a mass LU501691 ratio of 26:18:3 to obtain a composition with weight-losing and lipid-lowering activity.

[0037] Example 4

[0038] The preparation method of green tea extract is the same as that in Example 1.

[0039] Preparation of citrus extract: squeeze and crush 10 g of fresh citrus fruits, mix with 50 ml of ethanol with the volume percent fraction of 40%, extract at 35°C for 60 min, filter, place the resulting filtrate at 4°C for 8 h, perform vacuum concentration on the supernatant, and vacuum drying, to obtain the citrus extract. The flavanone content in the citrus extract is 20%.

[0040] Mix the green tea extract, the citrus extract and betaine according to a mass ratio of 25:15:1 to obtain a composition with weight-losing and lipid-lowering activity.

[0041] Example 5

[0042] Tablets with weight-losing and lipid-lowering activity

[0043] Accurately weigh 250 g of green tea extract of Example 1, 150 g of citrus extract of Example 1, 10 g of betaine and 190 g of starch, mix them gradiently, use 30 mL of ethanol with the volume percent fraction of 75% as a binder, to make soft materials, then sieve through a 20-mesh sieve to make granules, boil and dry, control the moisture content of granules to be less than 5%, add 20 g of magnesium stearate to the granules, mix, perform tabletting and coating, to obtain 1,000 tablets, 0.6 g/tablet. Each tablet contains 250 mg of green tea extract, 150 mg of citrus extract, and 10 mg of betaine.

[0044] Example 6

[0045] Capsules with weight-losing and lipid-lowering activity

[0046] Accurately weigh 200 g of green tea extract of Example 1, 200g of citrus extract of Example 1, 30 g of betaine and 370 g of starch, mix the raw materials gradiently, use 45 mL of ethanol with the volume percent fraction of 60% as a binder, make soft materials, sieve through a 14-mesh sieve to make granules, boil and dry, control the moisture content of granules to be less than 5%, then add into capsule filling molds, fill the capsules, polish, and sub-package to obtain 2,000 capsules, 0.4g per capsule. Each capsule contains 100 mg of green tea extract, 100 mg of citrus extract, and 15 mg of betaine.

[0047] Test Example 1

[0048] Mice test

[0049] Thirty Kunming male mice were randomly divided into groups (10 mice in each group) after feeding on a normal diet for 1 week. A control group (SD) with free drinking and feeding (high-fat diet) was given 50 mg/kg starch by gavage, a single-formula group (GTP) was given 50 mg/kg green tea extract (60% EGCG) by gavage, a compound group (GCB) was given 50 mg/kg of the formula (the formula composition was a composition with weight-losing and lipid-lowering activity obtained in Example 1 of the present disclosure) of the present disclosure, and raised for 8 weeks, and the body weights were recorded. Orbital blood was collected and centrifuged to obtain serum. Serum triglyceride (TG), cholesterol (TC), low-density lipoprotein (LDL) and high-density lipoprotein (HDL) levels were measured respectively, and the statistical analysis of data was performed by EXCEL one-way analysis of variance. The LU501691 specific results were shown in Tables 1 to 3.

[0050] Table 1 Body weights of three groups of mice before and after feeding for 8 weeks Avera SEM Initial body weight (g) ge (n=1 (2) 0)

30. 31. 31. 28 30. 31. 28. 30. 32. Control group 9 4 6 8 9 6 9 6 1 30.8 1.2 Single-formula 31. 33. 34. 30. 29. 30. 28. 28. 29. 306 20 group 5 2 3 0 9 2 3 8 3

31. 31. 29 29. 28. 32. 29. 30. 32.

30.7 1.5 Compound group 3 9 6 4 6 7 4 6 4 Avera SEM Body weights of mice after 8 weeks of feeding (g) ge (n=1 (2) 0)

42. 44. 44. 44. 47. 51. 45. 42. 48. Control group 4 1 3 9 4 8 5 7 3 45.7 2.8 ingle-f( 1 38. 41. 41. 43. 39. 35. 41. Single-formula 42 43 408 23 group 9 8 1 3 4 6 9

35. 35. 36. 42. 38. 38. 36. 38. 34. Compound group ” 9 5 1 4 4 4 5 8 37.4 2.1

[0051] As shown in Table 1 and FIG.1, there were significant differences between the control group, the single-formula group and the compound group. The body weights of mice in the single-formula group and compound group was significantly lower than that in the control group (p< 0.01), while the body weights of mice in the compound group was significantly lower than those in the single-formula group (p< 0.01).

[0052] Table 2 Total cholesterol and triglyceride levels of three groups of mice before and after feeding for 8 weeks . Average SEM Total chol | levels of fter 8 k 1 otal cholesterol levels of mice after 8 weeks (mmol/L) (mmol/L) (n=10) Contro 57 46 46 55 59 53 46 1 5.41 7 1 4 4 0 0 7 4.76 5.21 0.45 group Single formu 474 46 46 47 47 48 40 42 la 5 7 9 0 2 6 4 2 4.83 4.72 0.37 group Comp 371 47 51 44 44 54 46 48 ound 6 9 7 5 3 4 0 8 4.92 4.62 0.53 group . . ; Average SEM Trigl levels of fter 8 k 1 riglyceride levels of mice after 8 weeks (mmol/L) (mmol/L) (n=10) 6

Contro 38 39 35 37 39 41 42 ee 1 4.45 9 7 3 8 1 | 2 4.60 4.10 0.33 group Single -formu 35 36 42 35 36 36 3/7 la 3.43 4 4 1 7 3 5 2 3.86 3.71 0.21 group Comp 31 35 37 38 34 39 34 ound 3.18 8 8 1 | 6 3 2 4.37 3.66 0.37 group

[0053] As shown in Table 2 and FIG. 2, the total cholesterol levels of the mice in the single-formula group and the compound group were significantly lower than those in the control group (p<0.01). The total cholesterol levels of the mice in the compound group were slightly lower than those in the single-formula group, but there was no significant difference between the two groups. Analysis of triglyceride data showed that the triglyceride levels of mice in the single-formula group and the compound group were significantly lower than those in the control group (p<0.01), while the triglyceride levels of the mice in the compound group were slightly lower than those in the single-formula group, but there was no significant difference between the two groups.

[0054] Table 3 High-density lipoprotein and low-density lipoprotein levels in three groups of mice before and after feeding for 8 weeks Averag High-density lipoprotein (HDLC) levels in mice after 8 e SEM weeks (mmol/L) (mmol/ (n=10) L) Control 036 070 072 080 084 085 054 065 °° 07 0.15 group 4 Single-form 087 082 073 074 089 092 116 123 !‘° 00 0.18 ula group 9 Compound 117 096 083 138 097 133 104 105 !? 106 0.19 group 3 Averag Low-density lipoprotein (LDLC) levels in mice after 8 weeks e SEM (mmol/L) (mmol/ (n=10) L) Control 1.64 185 150 154 157 163 165 165 ‘© 167 0.11 group 8 Single-form 156 133 136 138 139 140 149 152 12 141 0.12 ula group 3 Compound 115 124 125 125 130 137 138 138 13 130 0.10 group 9

[0055] As shown in Table 3 and FIG. 3, after 8 weeks of feeding, the high-density lipoprotein levels of mice in the single-formula group and the compound group were significantly higher than those of the control group (p<0.01), and the low-density 7 lipoprotein levels were also significantly lower than those of the control group LU501691 (p<0.01). 0.01). The compound group was significantly higher than the single-formula group in the two indexes (p<0.05). It indicated that the composition with weight-losing and lipid-lowering activity of the present disclosure can enhance the transport and consumption of fat in serum, and reduce the risk of obesity and obesity complications.

[0056] Test example 2

[0057] Human trial

[0058] The subjects were recruited, aged 20-50 years old, BMI > 24. A total of 61 subjects, with an average age of 38.7+8.5, were randomly divided into 3 groups, including a negative control group (n=20), a positive control group (n=20), and a test group (n=21). The subjects in the negative control group took placebo, those in the positive control group took EGCG tablets (each tablet contained 400 mg of green tea extract), and those in the test group took the tablets of Example 5 of the present disclosure, twice a day, 3 pills each time, and continuously took 8 weeks. During the whole period, they did not control their diet, did not increase exercise deliberately, and were forbidden to take other diet foods and medicines. After 8 weeks, their body weights were weighed by a weight scale, and their abdominal circumferences were measured by a tape. More than 3% was recorded as effective, more than 6% was recorded as markedly effective, and less than 3% was recorded as ineffective. The results were shown in Tables 4 and 5.

[0059] Table 4 Changes in body weights in human trial Number Number of Number of Number of Total Group of markedly effective ineffective effective subjects effective cases cases cases rate Control 20 0 2 18 10% group Single-for mula 20 2 10 12 60% group Compoun 21 4 15 2 90.5% d group

[0060] Table 5 Changes in abdominal circumference in human trial Number Number of Number of Number of Total Group of markedly effective ineffective effective subjects effective cases cases cases rate Control „0 0 1 19 5% group Single-for mula 20 1 12 10 65% group Compoun 3 3 15 3 85.7% d group

[0061] As shown in Tables 4 and 5, the weight loss effect of the single-formula group and the compound group was higher than that of the control group, and the effect of the 8 compound group was better than that of the single-formula group. It indicated that the LU501691 compound formula provided by the present disclosure had the effect of losing weight, and at the same time, during the trial, no adverse reactions such as gastrointestinal discomfort occurred in the subjects who participated in the human trial.

[0062] The foregoing description merely describes the preferred embodiments of the present disclosure. It should be noted that for those of ordinary skill in the art, several improvements and modifications can be made without departing from the principle of the present disclosure, and these improvements and modifications shall also fall within the scope of protection of the present disclosure. 9

Claims

WHAT IS CLAIMED IS: LUS01691

1. A composition with weight-losing and lipid-lowering activity comprises the following components in parts by weight: 20-30 parts of a green tea extract, 10-20 parts of a citrus extract and 0.5-5 parts of betaine.

2. The composition according to claim 1, wherein the mass percentage of EGCG in the green tea extract is 30-80%.

3. The composition according to claim 1, wherein a method for preparing the green tea extract comprises the following steps: mixing green tea with ethanol with the volume percent fraction of 40-80%, extracting at 25-50°C for 15-60 min, repeatedly extracting for 2-4 times, combining filtrates, concentrating under reduced pressure, and performing spray drying to obtain the green tea extract.

4. The composition according to claim 3, wherein the mass volume ratio of green tea to ethanol is 1: (10-25).

5. The composition according to claim 1, wherein the content of flavone is 10-30% in the citrus extract.

6. The composition according to claim 5, wherein a method for preparing the citrus extract comprises the following steps: respectively squeezing and crushing citrus fruits or peels, mixing with a solvent, extracting at 25-50°C for 10-120 min, filtering, placing the resulting filtrate at 2-8°C for 4-12 h, performing vacuum concentration on the supernatant, and drying, to obtain the citrus extract; the mass ratio of the citrus fruits or peels to the solvent is 1: (2-10).

7. The composition according to claim 7, wherein the solvent comprises water or ethanol with the volume percent fraction of 30-50%.

8. The composition according to claim 7, wherein the drying comprises vacuum drying or spray drying.

9 . A product with weight-losing and lipid-lowering activity that is prepared into tablets, granules or capsules from the composition of any one of claims 1 to 9 and auxiliary materials, or is prepared into foods by matching the composition of any one of claims 1 to 9 with other edible components.