Composition containing lipase inhibitor, and preparation method therefor and use thereof
The lipase inhibitor composition prepared by a specific proportion of cereal fermentation extracts and citrus extracts has solved the problems of side effects and changes in living habits of existing weight loss drugs, and achieved safe and efficient fat metabolism regulation and weight loss effects.
Patent Information
- Application Number
- PCT/CN2024/131931
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2024-02-21
- Filing Date
- 2024-11-14
- Publication Date
- 2025-08-28
AI Technical Summary
Existing weight loss drugs such as orlistat have side effects, and conventional weight loss methods require high self-discipline, making it difficult to effectively lose weight without changing your lifestyle.
Using a specific proportion of cereal fermented extracts and citrus extracts, the bioavailability of the composition is significantly improved by the preparation method, and a composition containing a lipase inhibitor is prepared to inhibit the digestion and absorption of fat by the intestine.
It has achieved significant inhibitory effect on lipase, safe and without side effects, effectively lost weight without changing diet and living habits, and regulated fat metabolism.
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Figure CN2024131931_28082025_PF_FP_ABST
Abstract
Description
Composition containing lipase inhibitor and preparation method and application thereof Technical Field
[0001] The present invention belongs to the technical field of food processing, and in particular relates to a composition containing a lipase inhibitor, and a preparation method and application thereof. Background Art
[0002] Obesity is a chronic metabolic disease caused by the conversion of excess energy into lipids, which then accumulate in the body. This excess lipid can negatively impact the endocrine, cardiovascular, digestive, and psychological and behavioral systems. There are two primary causes of obesity. The primary external cause is excessive eating and insufficient physical activity. When the body consumes more calories than it burns, the excess calories are stored as fat, exceeding normal physiological needs. When this amount reaches a certain level, obesity develops. The internal cause is obesity caused by abnormal fat metabolism.
[0003] According to the "Report on the Nutrition and Chronic Disease Status of Chinese Residents (2020)", the overweight rate of adults in China is 34.3% and the obesity rate is 16.4%. This is the first time that the prevalence of overweight and obesity among Chinese adults has exceeded 50%. It is estimated that by 2030, the prevalence of overweight and obesity among Chinese adults will reach 61%. Obesity not only affects appearance, but also affects overall health. Studies have shown that obesity is the basis for the onset of many metabolic diseases. For example, for diabetes, hypertension, and fatty liver, obesity is one of the main causes. Fatty liver, in particular, is the most common complication among obese patients. On the other hand, obesity also has a negative impact on personal mental health. These psychological problems may further aggravate the negative emotions and self-denial of obese patients, forming a vicious circle.
[0004] The treatment of this type of metabolic disease can be achieved by reducing calorie intake and increasing calorie expenditure. For example, it emphasizes comprehensive treatment based on behavior, diet, and exercise, supplemented by medication or surgery when necessary. Conventional exercise and diet require a high degree of self-discipline and willpower. With the fast-paced lifestyle of modern people, few people can stick to it. Therefore, many people turn to seek quick solutions with Western medicine, such as orlistat. Orlistat is a weight loss drug approved for use by the state. It can inhibit the digestion and absorption of fat in the body, thereby achieving the purpose of weight loss. It has a good effect, especially on abdominal fat, but it can cause side effects such as gastrointestinal reactions, allergic reactions, liver damage, endocrine disorders, and respiratory infections.
[0005] Therefore, there is an urgent need to develop a product that can assist in the treatment of obesity and metabolic syndrome without side effects and without requiring changes in diet or lifestyle. The inventors surprisingly discovered that a specific cereal fermentation extract and a citrus extract, when formulated in a specific ratio, can regulate fat metabolism in the body. Furthermore, the present invention's unique preparation method significantly improves the bioavailability of the composition in the body, effectively achieving the present invention's objectives. Summary of the Invention
[0006] The present invention aims to overcome the problems existing in the prior art by providing a composition containing a lipase inhibitor. This composition is derived from a natural, green, and healthy source and exhibits a significant inhibitory effect on lipase. It can effectively inhibit the digestion and absorption of fat in the intestine, thereby achieving the purpose of weight loss, while not causing side effects such as intestinal irritation.
[0007] The purpose of the present invention and the solution to its technical problems are achieved by adopting the following technical solutions.
[0008] A first aspect of the present invention provides a composition containing a lipase inhibitor, comprising composition I, composition II, and composition III, wherein the mass ratio of composition I, composition II, and composition III is (0.1-1):(0.1-20):(1-30).
[0009] In some preferred embodiments of the present invention, the composition I is selected from one or more extracts of the following groups, the group consisting of: berries, stone fruits, pome fruits, citrus fruits, multiple fruits, and aggregate fruits.
[0010] In some preferred embodiments of the present invention, the citrus fruits are selected from one or more of the following groups, which group consists of: kumquat, mandarin orange, sweet orange, grapefruit, grapefruit, kumquat, lemon, lime, mandarin orange, navel orange, sour orange, bergamot, and citron.
[0011] In some preferred embodiments of the present invention, the composition I is selected from one or more of the following groups: polysaccharides, fruit acids, pectin, flavonoids, volatile oils, alkaloids, minerals, proteins, and polypeptides.
[0012] In some preferred embodiments of the present invention, the composition I is one or more compositions or derivatives selected from the following group: naringin, naringin, wild sumac, hesperidin, naringenin, neohesperidin, hesperidin, naringin, dihydroquercetin, isoetolide, acacia, 8-hydroxyapigenin, luteolin, carkaol, pentahydroxyflavone, apigenin, geraniol, tangeretin, nobiletin, catechol, rutin, monocoumarin, furanocoumarin, α-limonene, β-myrcene, γ-terpinene, α-pinene, citrus flavonoids, citrus glycosides, quercetin, and tangeretin.
[0013] In some preferred embodiments of the present invention, the composition II is selected from one or more cereal extracts in the following group, which group consists of: oats, highland barley, naked oats, barley, buckwheat, wheat, sorghum, millet, foxtail millet, and millet.
[0014] In some preferred embodiments of the present invention, the composition II is selected from one or more of the following groups, which consists of: avenant alkaloids, polyphenols, p-hydroxybenzoic acid, 2,4-dihydroxybenzoic acid, salicylic acid, syringic acid, vanillic acid, gallic acid C, protocatechuic acid, syringaldehyde, vanillin, 4-hydroxyphenylacetic acid, p-coumaric acid, o-coumaric acid, cinnamic acid, ferulic acid, caffeic acid, sinapic acid, caffeic acid derivatives, ferulic acid derivatives, benzoic acid-O-sulfate, syringaldehyde-O-sulfuric acid, syringic acid-O-sulfuric acid, vanillin-O-sulfate, dihydroxybenzoic acid-O-sulfate, caffeic acid-O-sulfate, hydroxyphenylacetic acid-O-sulfate, homovanillic acid-O-glucuronic acid, sinapic acid-O-sulfate, feruloylglycine, benzoic acid-O-glucuronic acid, homovanillic acid-O-glucuronic acid, Vanillin-O-glucuronic acid, dihydrofuranyl-O-glucuronic acid, 3,4-dihydroxyoctanoyl-O-glucuronic acid, 4-hydroxyphenylacetic acid-O-glucuronic acid, ferulic acid-O-glucuronic acid, aldose-O-glucuronide, kaempferol, linalool, rutin, citrinin, myricetin, quercetin, tricin, avenanthin, β-glucan.
[0015] In some preferred embodiments of the present invention, the composition III is an oligosaccharide mixture enriched by starch through enzymatic hydrolysis or microbial fermentation, or a derivative obtained by modifying the oligosaccharide mixture as a substrate.
[0016] In some preferred embodiments of the present invention, the starch is selected from one or more of corn starch, tapioca starch, wheat starch, potato starch, and rice starch;
[0017] The enzyme is selected from one or more of α-amylase, β-amylase, CGT glucosyltransferase, and isoamylase;
[0018] The microorganism is selected from one or more of Bacillus, Thermobacterium, Bacillus circulans, Bacillus softening, alkali-resistant Bacillus megaterium, and Escherichia coli.
[0019] In some preferred embodiments of the present invention, the composition III is selected from one or more of the following groups, which consists of: xylooligosaccharides, fructooligosaccharides, maltotetraose, maltooligosaccharides, isomaltooligosaccharides, stachyose, raffinose, lactulose, chitosan oligosaccharides, galactooligosaccharides, α-cyclodextrin, β-cyclodextrin, γ-cyclodextrin, hydroxypropyl-β-cyclodextrin, permethylated β-cyclodextrin, cinnamaldehyde-β-cyclodextrin, limonene-β-cyclodextrin, linalool-β-cyclodextrin, myrcene-β-cyclodextrin, octanal-β-cyclodextrin, decanal-β-cyclodextrin, crotonic acid-β-cyclodextrin, poly-[6-deoxy-6-cysteine]-γ-cyclodextrin, thiolated β-cyclodextrin, methyl 4-hydroxy-2-thiazolinone ... Dextrin, α-cyclodextrin valeric acid, α-cyclodextrin polyrotaxane, permethylated α-cyclodextrin, permethylated γ-cyclodextrin, carboxymethyl β-cyclodextrin, ferulic acid-α-cyclodextrin, maltosyl-α-cyclodextrin, 2-phenylethanol-α-cyclodextrin, hydroxypropyl-γ-cyclodextrin, dialdehyde γ-cyclodextrin, ethyl butyrate-γ-cyclodextrin, hexanal-γ-cyclodextrin, hexanol-γ-cyclodextrin, high branched starch, amylose, resistant starch RS1, resistant starch RS2, starch stearate, starch octenylsuccinate, starch acetate, sodium carboxymethyl starch, acetylated starch, hydroxypropyl starch, starch acetate, starch phosphate, alkenyl starch esters, acetylated distarch, acetylated distarch phosphate.
[0020] The second aspect of the present invention provides a method for preparing the aforementioned composition containing a lipase inhibitor, comprising the following steps:
[0021] a) preparing composition I: drying citrus peel at 40-60°C, crushing and sieving to 40-200 mesh, adding 0.1%-5% pectinase for 0.5-5 h, extracting with 40%-90% ethanol solution at a solid-liquid ratio of 1:(1-30) at 20-80°C for 0.5-5 h, centrifuging the supernatant, removing ethanol by vacuum distillation, and drying in vacuo to obtain composition I;
[0022] b) Preparation of Composition II: After removing impurities from the cereal seeds, crush them and sieve them through 40-200 mesh. Prepare an aqueous solution with water at a ratio of 1:(1-10). After sterilization, inoculate 0.5%-10% of activated bacteria to the logarithmic stage (viable bacteria count greater than 1×10 9 CFU / mL) of Lactobacillus plantarum WSH048, stirring evenly, fermenting at 20-40°C for 12-48 hours, collecting the supernatant by centrifugation after the fermentation, and freeze-drying to obtain composition II;
[0023] c) Preparing Composition III: Prepare a 1-70% starch solution, adjust the pH of the solution to 4-9.0, add or not add amylase / inoculate or not inoculate with a microorganism, and react at 25-60°C for 0.5-5 hours. After the reaction is completed, increase the temperature to 50-90°C, adjust the pH to 2-8.0, and add or not add amylase, and react for 2-12 hours. After the reaction is completed, perform conventional enzyme inactivation and filtration to obtain a solution containing Composition III;
[0024] d) Composition preparation method: Composition I, composition II, and composition III are mixed in a mass ratio of (0.1-1):(0.1-20):(1-30), and composition I is slowly added to a solution of composition III. The mixture is stirred at 20-60°C for 0.5-10 hours, and freeze-dried to obtain a powder containing compositions I and III. The powder is then mixed with composition II to obtain the composition containing the lipase inhibitor.
[0025] The third aspect of the present invention provides a product for assisting in the treatment of obesity and metabolic syndrome, comprising the aforementioned composition, or a composition prepared according to the aforementioned preparation method.
[0026] In some preferred embodiments of the present invention, such products include solid beverages, liquid beverages, and dietary supplements.
[0027] A fourth aspect of the present invention provides a use of a composition containing a lipase inhibitor in the preparation of a drug for the auxiliary treatment of obesity and metabolic syndrome, wherein the composition is the aforementioned composition, or a composition prepared according to the aforementioned preparation method.
[0028] By means of the above technical solution, the present invention has at least the following advantages:
[0029] 1) The present invention innovatively combines cereal fermentation extracts with citrus seed peel or peel capsule extracts and starch enzymatic hydrolysis or fermentation products. At the same time, through a specific processing method, it can significantly increase the content and bioavailability of each functional ingredient in the composition, ensuring that the functional effect can be achieved with a relatively small addition amount, facilitating back-end applications, and having a greener and more natural source, safer and without side effects.
[0030] 2) Through specific combination, the composition of the present invention has a significant inhibitory effect on lipase, which can more effectively inhibit the digestion and absorption of fat in the intestine, thereby achieving the purpose of weight loss and regulating fat metabolism.
[0031] 3) The intake of the composition of the present invention does not change the diet and lifestyle habits of consumers, making it easier to achieve weight loss effects.
[0032] The above description is only an overview of the technical solution of the present invention. In order to more clearly understand the technical means of the present invention and implement it according to the contents of the specification, the following is a detailed description of the preferred embodiments of the present invention. BRIEF DESCRIPTION OF THE DRAWINGS
[0033] FIG1 shows the changing trend of the inhibition rate of pancreatic lipase by different compositions;
[0034] FIG2 shows the effects of different compositions on fat accumulation in rats fed a high-fat diet;
[0035] FIG3 shows the effects of different compositions on organ weights in rats fed a high-fat diet;
[0036] FIG4 shows the effects of different compositions on the body weight of obese patients. DETAILED DESCRIPTION
[0037] In order to make the technical means, creative features, objectives and effects achieved by the present invention easier to understand, the technical solutions in the embodiments of the present invention will be clearly and completely described below in conjunction with the embodiments of the present invention. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of them. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without making creative efforts shall fall within the scope of protection of the present invention.
[0038] The present invention provides a composition containing a lipase inhibitor, which is composed of a cereal fermentation extract, a citrus peel extract, and an enzymatic hydrolysis or fermentation product of starch, and is greener and more natural in source. The composition has a significant inhibitory effect on lipase, and can more efficiently inhibit the digestion and absorption of fat by the intestine, thereby achieving the purpose of losing weight and regulating fat metabolism. At the same time, through a specific processing method, the active ingredients in the composition have good bioavailability, are safe and have no side effects. Another object of the present invention is to provide the application of the composition in the auxiliary treatment of obesity and metabolic syndrome, which solves the problem that conventional weight loss and metabolic disease treatment products or programs require regular life and diet and have large side effects.
[0039] Citrus fruits are rich in pancreatic lipase inhibitors, characterized by low toxicity and diverse structures. Flavonoids are the primary active ingredients in these fruits. Studies have shown that various flavonoids extracted from fruits such as pomegranates, strawberries, and grapes exhibit potent lipase inhibition, demonstrating that fruit flavonoids are a source of lipase inhibitors. However, citrus seed peels are a byproduct of food processing and have yet to be effectively utilized.
[0040] Component I, one of the components of the composition of the present invention, is an extract of one or more of berries, stone fruits, pome fruits, citrus fruits, multiple fruits, and aggregate fruits, preferably a citrus fruit extract.
[0041] The citrus fruits described in the present invention can be, for example, kumquat, mandarin orange, sweet orange, grapefruit, grapefruit, kumquat, lemon, lime, mandarin orange, navel orange, sour orange, bergamot, citron and other Rutaceae fruits, and can also be fresh or pulped, dried, or processed parts of the seed coat, seeds, skin sac, pulp, leaves, roots, branches, flowers and other parts of the corresponding raw materials.
[0042] The extract can be obtained by water extraction, solvent extraction, enzyme extraction, or a combination of two or more methods, as long as the effective active substance can be extracted.
[0043] The extracts obtained by combining the selected raw materials with the corresponding extraction methods include but are not limited to polysaccharides, fruit acids, pectin, flavonoids, volatile oils, alkaloids, minerals, proteins, and polypeptides, such as naringin, naringin, wild sumac, hesperidin, naringenin, neohesperidin, hesperidin, naringin, dihydroquercetin, isoetolide, acacia, 8-hydroxyapigenin, luteolin, carkaol, pentahydroxyflavone, apigenin, geraniol, tangeretin, nobiletin, catechol, rutin, monocoumarin, furanocoumarin, α-limonene, β-myrcene, γ-terpinene, α-pinene, citrus flavonoids, citrus glycosides, quercetin, and tangeretin.
[0044] Component II, the second component of the composition of the present invention, is a cereal extract, including but not limited to oats, highland barley, naked oats, barley, buckwheat, wheat, sorghum, foxtail millet, foxtail millet, millet, and millet. Fermentation of cereals can significantly increase the content of active ingredients in the product, such as β-glucan, polyphenols, flavonoids, and protein. The inventors used the patented Lactobacillus plantarum WSH048 to ferment cereals and found that the extract, after fermentation, has anti-inflammatory, lipid-regulating, and blood sugar-lowering effects, and can be used as an adjunct treatment for obesity and metabolic syndrome.
[0045] The extract can be obtained by water extraction, solvent extraction, enzyme extraction, ultrasonic extraction, supercritical extraction, or a combination of two or more, as long as the effective active substance can be extracted.
[0046] The extracts obtained by combining the selected raw materials with the corresponding extraction methods include but are not limited to avenant alkaloids, polyphenols, p-hydroxybenzoic acid, 2,4-dihydroxybenzoic acid, salicylic acid, syringic acid, vanillic acid, gallic acid C, protocatechuic acid, syringaldehyde, vanillin, 4-hydroxyphenylacetic acid, p-coumaric acid, o-coumaric acid, cinnamic acid, ferulic acid, caffeic acid, sinapic acid, caffeic acid derivatives, ferulic acid derivatives, benzoic acid-O-sulfate, syringaldehyde-O-sulfate, syringic acid-O-sulfate, vanillin-O-sulfate, dihydroxybenzoic acid-O-sulfate, caffeic acid-O-sulfate, hydroxyphenylacetic acid-O-sulfate, homovanillic acid-O-glucuronic acid, sinapic acid-O-sulfate, feruloylglycine, benzoic acid-O-glucuronic acid, homovanillic acid-O-glucuronic acid, Vanillin-O-glucuronic acid, dihydrofuranyl-O-glucuronic acid, 3,4-dihydroxyoctanoic acid-O-glucuronic acid, 4-hydroxyphenylacetic acid-O-glucuronic acid, ferulic acid-O-glucuronic acid, aldose-O-glucuronic acid, kaempferol, linalool, rutin, citrinin, myricetin, quercetin, tricin, avenanthin, β-glucan, etc.
[0047] Component III, which is the third component of the composition of the present invention, is an oligosaccharide mixture enriched after starch is hydrolyzed by enzymes or fermented by microorganisms, or a derivative modified with the oligosaccharide mixture as a substrate. Starch is a high-molecular carbohydrate and a polysaccharide composed of a single type of sugar unit. The basic building block of starch is α-D-pyranose glucose. The covalent polymer formed by glucose after removing water molecules and connecting them together through glycosidic bonds is the starch molecule. After starch is hydrolyzed or fermented, the molecules are hydrolyzed to the range of dextrin and oligosaccharides, the number of substrate molecules increases, and the number of tail end groups increases. The special spatial structure forms a helical structure with a hydrophobic cavity and hydrophilicity, which enables it to form an inclusion complex. The encapsulated molecules are included in the cavity or between the helices, which can prevent the loss of guest molecules during processing and storage, or mask unpleasant flavors.
[0048] Typically, starch undergoes hydrolysis or microbial fermentation, followed by isolation and purification to obtain a single molecule of the target compound. This compound is then used in downstream products. The authors serendipitously discovered that the oligosaccharide mixture enriched by starch hydrolysis or microbial fermentation has the ability to encapsulate specific molecules. Based on this discovery, physically or chemically modified derivatives based on this oligosaccharide mixture enriched by starch hydrolysis or microbial fermentation also exhibit excellent encapsulation properties. This encapsulation can significantly improve the bioavailability of the encapsulated molecules.
[0049] The starch source used in the present invention can be any starch, including but not limited to corn starch, tapioca starch, wheat starch, potato starch, and rice starch. The enzymes used to hydrolyze starch include but are not limited to α-amylase, β-amylase, CGT glucosyltransferase, and isoamylase. Among them, CGT glucosyltransferase is CGTase N16, CGTase C100, or CGTase NC mentioned in the application document with application number 202311503221.6 submitted by the applicant Nanjing Shengde Chuangying Biotechnology Co., Ltd. on November 13, 2023. Preferably, it is CGT glucosyltransferase CGTase N16. The microorganisms used for fermentation include but are not limited to Bacillus, Thermobacterium, Bacillus circulans, Bacillus softening, alkali-resistant Bacillus megaterium, and Escherichia coli.
[0050] The oligosaccharide mixture enriched after starch is hydrolyzed by enzymes or fermented by microorganisms, or the derivatives obtained by modifying the oligosaccharide mixture as a substrate include but are not limited to xylooligosaccharides, fructooligosaccharides, maltotetraose, maltooligosaccharides, isomaltooligosaccharides, stachyose, raffinose, lactulose, chitosan oligosaccharides, galactooligosaccharides, α-cyclodextrin, β-cyclodextrin, γ-cyclodextrin, hydroxypropyl-β-cyclodextrin, permethylated β-cyclodextrin, cinnamaldehyde-β-cyclodextrin, limonene-β-cyclodextrin, linalool-β-cyclodextrin, myrcene-β-cyclodextrin, octanal-β-cyclodextrin, decanal-β-cyclodextrin, crotonic acid-β-cyclodextrin, poly-[6-deoxy-6-cysteine]-γ-cyclodextrin, thiophene methylated β-cyclodextrin, α-cyclodextrin valeric acid, α-cyclodextrin polyrotaxane, permethylated α-cyclodextrin, permethylated γ-cyclodextrin, carboxymethyl β-cyclodextrin, ferulic acid-α-cyclodextrin, maltosyl-α-cyclodextrin, 2-phenylethanol-α-cyclodextrin, hydroxypropyl-γ-cyclodextrin, dialdehyde γ-cyclodextrin, ethyl butyrate-γ-cyclodextrin, hexanal-γ-cyclodextrin, hexanol-γ-cyclodextrin, high branched starch, amylose, resistant starch RS1, resistant starch RS2, starch stearate, starch octenylsuccinate, starch acetate, sodium carboxymethyl starch, acetylated starch, hydroxypropyl starch, starch acetate, starch phosphate, alkenyl starch esters, acetylated distarch, acetylated distarch phosphate, etc.
[0051] Unless otherwise specified, the Lactobacillus plantarum WSH048 mentioned in the embodiments of the present invention has a deposit number of CGMCC No. 23159. The strain has been submitted for a patent application on May 2, 2023, with application number: 202111266897.9.
[0052] Example 1: This example provides a composition containing a lipase inhibitor and a preparation method. The specific preparation method is as follows:
[0053] a) Composition I: Citrus seed peel was dried at 40°C, crushed and sieved to 80 mesh, and enzymatically hydrolyzed with 0.1% pectinase for 2 hours. The extract was then extracted with 60% ethanol at a solid-liquid ratio of 1:20 at 60°C for 5 hours. The supernatant was centrifuged and the ethanol was removed by vacuum distillation. The extract was then dried in vacuo to obtain Composition I. According to the method in "NY / T 2014-2011 Determination of Hesperidin and Naringin Content in Citrus Fruits and Products", the main component of Composition I was naringin, with a content of 86.73%.
[0054] b) Composition II: After removing impurities from oat granules, crush and sieve through 60 mesh, mix with water at a ratio of 1:10 to prepare an aqueous solution, sterilize and inoculate 5% of activated bacteria to the logarithmic stage (viable bacteria count greater than 1×10 9 CFU / mL) of Lactobacillus plantarum WSH048 was stirred evenly, fermented at 40°C for 48 hours, the supernatant was collected by centrifugation, and freeze-dried to obtain Composition II; referring to the methods of "NY / T 2006-2011 Determination of β-glucan Content in Cereals and Cereals and Their Products", "T / AHFIA 005-2018 Determination of Total Polyphenols in Plant Extracts and Their Products - Spectrophotometric Method", and "GB 5009.5-2016 National Food Safety Standard - Determination of Protein in Foods", the main components of Composition II were measured to be 4.05% β-glucan and 16.3% total polyphenols.
[0055] c) Composition III: Prepare a 50% solution of cassava starch, adjust the pH of the solution to 7.0, add 0.15% α-amylase, and react at 55°C for 2 hours. After the reaction, raise the temperature to 90°C, adjust the pH to 6.0, and add 0.1% CGT glucosyltransferase CGTase N16. The reaction is carried out for 6 hours. After the reaction is completed, conventional enzyme inactivation, filtration, and other steps are performed to obtain a solution containing Composition III; with reference to the methods of "GB 1886.351-2021 National Food Safety Standard Food Additive α-cyclodextrin" and "GB 1886.353-2021 National Food Safety Standard Food Additive γ-cyclodextrin", the content of α-cyclodextrin in the Composition III solution was measured to be 50.7%, and the content of γ-cyclodextrin was 10.2%.
[0056] d) Preparation of the composition: Slowly add composition I to a solution of composition III at a ratio of 1:8, stir at 50°C for 5 hours, and freeze-dry to obtain a powder containing compositions I and III, which is then mixed with composition II at a ratio of 3:1 to obtain the composition containing the lipase inhibitor.
[0057] Example 2: This example provides a composition containing a lipase inhibitor and a preparation method. The specific preparation method is as follows:
[0058] a) Composition I: Grapefruit seed peel was dried at 40°C, crushed and sieved to 80 mesh, and enzymatically hydrolyzed with 0.15% pectinase for 2 h. The mixture was then extracted with 70% ethanol at a solid-liquid ratio of 1:25 at 60°C for 3 h. The supernatant was centrifuged and the ethanol was removed by vacuum distillation. The mixture was then dried in vacuo to obtain Composition I. According to the method in "NY / T 2014-2011 Determination of Hesperidin and Naringin Content in Citrus Fruits and Products", naringin was determined to be the main component of Composition I at a content of 96.18%.
[0059] b) Composition II: After removing impurities from oat granules, crush and sieve through 80 mesh, mix with water at a ratio of 1:10 to prepare an aqueous solution, sterilize and inoculate 5% of the oat granules to activate the oat granules to the logarithmic stage (viable cell count greater than 1×10 9 CFU / mL) of Lactobacillus plantarum WSH048 was stirred evenly, fermented at 35°C for 36 hours, the supernatant was collected by centrifugation, and freeze-dried to obtain Composition II; referring to the methods of "NY / T 2006-2011 Determination of β-glucan Content in Cereals and Cereals and Their Products", "T / AHFIA 005-2018 Determination of Total Polyphenols in Plant Extracts and Their Products - Spectrophotometric Method", and "GB 5009.5-2016 National Food Safety Standard - Determination of Protein in Foods", the main components of Composition II were measured to be 6.05% β-glucan and 18.6% total polyphenols.
[0060] c) Composition III: Prepare a 50% solution of cassava starch, adjust the pH of the solution to 7.0, add 0.3% CGT glucosyltransferase CGTase N16, and react for 6 hours. After the reaction is completed, conventional enzyme inactivation, filtration and other steps are performed to obtain a solution containing Composition III; with reference to the methods of "GB 1886.351-2021 National Food Safety Standard Food Additive α-cyclodextrin" and "GB 1886.353-2021 National Food Safety Standard Food Additive γ-cyclodextrin", the content of α-cyclodextrin in the Composition III solution was measured to be 68.3%, and the content of γ-cyclodextrin was 18.1%.
[0061] d) Preparation of the composition: Slowly add composition I to a solution of composition III at a ratio of 1:10, stir at 50°C for 6 hours, and freeze-dry to obtain a powder containing compositions I and III, which is then mixed with composition II at a ratio of 2:1 to obtain the composition containing the lipase inhibitor.
[0062] Example 3: This example provides a composition containing a lipase inhibitor and a preparation method. The specific preparation method is as follows:
[0063] a) Composition I: Lemon seed peel was dried at 50°C, crushed and sieved to 80 mesh, and enzymatically hydrolyzed with 0.2% pectinase for 1 hour. The mixture was then extracted with 65% ethanol at a solid-liquid ratio of 1:15 at 60°C for 5 hours. The supernatant was centrifuged and the ethanol was removed by vacuum distillation. The mixture was then dried in vacuo to obtain Composition I. According to the method in "NY / T 2014-2011 Determination of Hesperidin and Naringin Content in Citrus Fruits and Products", naringin was determined to be the main component of Composition I at a content of 78.58%.
[0064] b) Composition II: After removing impurities from highland barley granules, crush and sieve through 80 mesh, mix with water at a ratio of 1:10 to prepare an aqueous solution, sterilize and inoculate 4.5% of activated bacteria to the logarithmic stage (viable bacteria count greater than 1×10 9 CFU / mL) of Lactobacillus plantarum WSH048 was stirred evenly, fermented at 35°C for 24 hours, the supernatant was collected by centrifugation, and freeze-dried to obtain Composition II; referring to the methods of "NY / T 2006-2011 Determination of β-glucan Content in Cereals and Cereals and Their Products", "T / AHFIA 005-2018 Determination of Total Polyphenols in Plant Extracts and Their Products - Spectrophotometric Method", and "GB 5009.5-2016 National Food Safety Standard - Determination of Protein in Foods", the main components of Composition II were measured to be 4.45% β-glucan and 13.9% total polyphenols.
[0065] c) Composition III: Rice starch was prepared into a 40% solution, the pH of the solution was adjusted to 7.0, 0.2% CGT glucosyltransferase CGTase N16 was added, and the reaction was carried out for 4 hours. After the reaction was completed, conventional enzyme inactivation, filtration and other steps were performed to obtain a solution containing Composition III; with reference to the methods of "GB 1886.351-2021 National Food Safety Standard Food Additive α-cyclodextrin" and "GB 1886.353-2021 National Food Safety Standard Food Additive γ-cyclodextrin", the content of α-cyclodextrin in the Composition III solution was measured to be 48.4%, and the content of γ-cyclodextrin was 10.6%.
[0066] d) Preparation of the composition: Slowly add composition I to a solution of composition III at a ratio of 1:5, stir at 60°C for 3 hours, and freeze-dry to obtain a powder containing compositions I and III, which is then mixed with composition II at a ratio of 4:1 to obtain the composition containing the lipase inhibitor.
[0067] Example 4: This example provides a composition containing a lipase inhibitor and a preparation method. The specific preparation method is as follows:
[0068] a) Composition I: Grapefruit seed peel was dried at 55°C, crushed and sieved to 60 mesh, and enzymatically hydrolyzed with 0.15% pectinase for 2 h. The mixture was then extracted with 65% ethanol at a solid-liquid ratio of 1:10 at 50°C for 6 h. The supernatant was centrifuged and the ethanol was removed by vacuum distillation. The mixture was then dried in vacuo to obtain Composition I. According to the method in "NY / T 2014-2011 Determination of Hesperidin and Naringin Content in Citrus Fruits and Products", naringin was determined to be the main component of Composition I at a content of 74.35%.
[0069] b) Composition II: After removing impurities from highland barley granules, crush and sieve through 80 mesh, mix with water at a ratio of 1:8 to prepare an aqueous solution, sterilize and inoculate 3.5% of activated bacteria to the logarithmic stage (viable bacteria count greater than 1×10 9 CFU / mL) of Lactobacillus plantarum WSH048 was stirred evenly, fermented at 40°C for 48 hours, the supernatant was collected by centrifugation, and freeze-dried to obtain Composition II; referring to the methods of "NY / T 2006-2011 Determination of β-glucan Content in Cereals and Cereals and Their Products", "T / AHFIA 005-2018 Determination of Total Polyphenols in Plant Extracts and Their Products - Spectrophotometric Method", and "GB 5009.5-2016 National Food Safety Standard - Determination of Protein in Foods", the main components of Composition II were measured to be 4.01% β-glucan and 16.1% total polyphenols.
[0070] c) Composition III: Rice starch was prepared into a 45% solution, the pH of the solution was adjusted to 7.0, 0.3% α-amylase was added, and the reaction was carried out at 60°C for 1 hour. After the reaction was completed, the temperature was raised to 90°C, the pH was adjusted to 6.0, and 0.15% CGT glucosyltransferase CGTase N16 was added, and the reaction was carried out for 5 hours. After the reaction was completed, conventional enzyme inactivation, filtration, and other steps were performed to obtain a solution containing Composition III; with reference to the methods of "GB 1886.351-2021 National Food Safety Standard Food Additive α-cyclodextrin" and "GB 1886.353-2021 National Food Safety Standard Food Additive γ-cyclodextrin", the content of α-cyclodextrin in the Composition III solution was measured to be 50.4%, and the content of γ-cyclodextrin was 11.3%.
[0071] d) Composition Preparation Method: Slowly add composition I to a solution of composition III at a ratio of 1:8, stir at 65°C for 2 hours, and freeze-dry to obtain a powder containing compositions I and III, which is then mixed with composition II at a ratio of 5:1 to obtain the composition containing the lipase inhibitor.
[0072] Example 5: This example provides a composition containing a lipase inhibitor and a preparation method. The specific preparation method is as follows:
[0073] a) Composition I: Penggan seed peel was dried at 50°C, crushed and sieved to 60 mesh, and enzymatically hydrolyzed with 0.3% pectinase for 0.5 h. The mixture was then extracted with 60% ethanol solution at a solid-liquid ratio of 1:10 at 55°C for 6 h. The supernatant was centrifuged and the ethanol was removed by vacuum distillation. The mixture was then dried under vacuum to obtain Composition I. According to the method in "NY / T 2014-2011 Determination of Hesperidin and Naringin Content in Citrus Fruits and Products", the main component of Composition I was naringin, with a content of 70.85%.
[0074] b) Composition II: After removing impurities, oat granules were crushed and sieved through 80 mesh, and then mixed with water at a ratio of 1:5 to prepare an aqueous solution. After sterilization, 4% of the solution was inoculated and activated to the logarithmic stage (viable cell count greater than 1×10 9 CFU / mL) of Lactobacillus plantarum WSH048 was stirred evenly, fermented at 40°C for 36 hours, the supernatant was collected by centrifugation, and freeze-dried to obtain Composition II; referring to the methods of "NY / T 2006-2011 Determination of β-glucan Content in Cereals and Cereals and Their Products", "T / AHFIA 005-2018 Determination of Total Polyphenols in Plant Extracts and Their Products - Spectrophotometric Method", and "GB 5009.5-2016 National Food Safety Standard - Determination of Protein in Foods", the main components of Composition II were measured to be 3.99% β-glucan and 12.1% total polyphenols.
[0075] c) Composition III: Corn starch was prepared into a 50% solution, the pH of the solution was adjusted to 7.0, 0.1% α-amylase was added, and the reaction was carried out at 60°C for 2 hours. After the reaction, the temperature was raised to 90°C, the pH was adjusted to 7.0, and 0.18% CGT glucosyltransferase CGTase N16 was added, and the reaction was carried out for 7 hours. After the reaction, conventional enzyme inactivation, filtration, and other steps were performed to obtain a solution containing Composition III; with reference to the methods in "GB 1886.351-2021 National Food Safety Standard Food Additive α-cyclodextrin" and "GB 1886.353-2021 National Food Safety Standard Food Additive γ-cyclodextrin", the content of α-cyclodextrin in the Composition III solution was measured to be 58.2%, and the content of γ-cyclodextrin was 14.3%.
[0076] d) Preparation of the composition: Slowly add composition I to a solution of composition III at a ratio of 1:10, stir at 65°C for 2 hours, and freeze-dry to obtain a powder containing compositions I and III, which is then mixed with composition II at a ratio of 3:1 to obtain the composition containing the lipase inhibitor.
[0077] Example 6: This example provides a composition containing a lipase inhibitor and a preparation method. The specific preparation method is as follows:
[0078] a) Composition I: Mandarin orange seed peel was dried at 55°C, crushed and sieved to 80 mesh, and enzymatically hydrolyzed with 0.25% pectinase for 2 hours. The mixture was then extracted with 65% ethanol at a solid-liquid ratio of 1:10 at 55°C for 4 hours. The supernatant was centrifuged and the ethanol was removed by vacuum distillation. The mixture was then dried in vacuo to obtain Composition I. According to the method in "NY / T 2014-2011 Determination of Hesperidin and Naringin Content in Citrus Fruits and Products", the main component of Composition I was naringin, with a content of 70.11%.
[0079] b) Composition II: After removing impurities from barley grains, crush and sieve through 80 mesh, mix with water at a ratio of 1:10 to prepare an aqueous solution, sterilize and inoculate 5% of activated bacteria to the logarithmic stage (viable count greater than 1×10 9 CFU / mL) of Lactobacillus plantarum WSH048 was stirred evenly, fermented at 40°C for 30 hours, the supernatant was collected by centrifugation, and freeze-dried to obtain Composition II; referring to the methods of "NY / T 2006-2011 Determination of β-glucan Content in Cereals and Cereals and Their Products", "T / AHFIA 005-2018 Determination of Total Polyphenols in Plant Extracts and Their Products - Spectrophotometric Method", and "GB 5009.5-2016 National Food Safety Standard - Determination of Protein in Foods", the main components of Composition II were measured to be 3.89% β-glucan and 11.4% total polyphenols.
[0080] c) Composition III: Corn starch was prepared into a 50% solution, the pH of the solution was adjusted to 7.0, 0.15% α-amylase was added, and the reaction was carried out at 55°C for 3 hours. After the reaction was completed, the temperature was raised to 90°C, the pH was adjusted to 6.0, and 0.2% CGT glucosyltransferase CGTase N16 was added, and the reaction was carried out for 5 hours. After the reaction was completed, conventional enzyme inactivation, filtration, and other steps were performed to obtain a solution containing Composition III; with reference to the methods of "GB 1886.351-2021 National Food Safety Standard Food Additive α-cyclodextrin" and "GB 1886.353-2021 National Food Safety Standard Food Additive γ-cyclodextrin", the content of α-cyclodextrin in the Composition III solution was measured to be 48.1%, and the content of γ-cyclodextrin was 9.3%.
[0081] d) Composition preparation method: Slowly add composition I to a solution of composition III at a ratio of 1:10, stir at 60°C for 4 hours, and freeze-dry to obtain a powder containing compositions I and III, which is then mixed with composition II at a ratio of 2:1 to obtain the composition containing the lipase inhibitor.
[0082] Comparative Example 1: This example provides a composition and a preparation method that does not contain composition I. The specific preparation method is as follows:
[0083] a) Composition II: After removing impurities from oat granules, crush and sieve through 80 mesh, mix with water at a ratio of 1:10 to prepare an aqueous solution, sterilize and inoculate 5% of activated bacteria to the logarithmic stage (viable bacteria count greater than 1×10 9 CFU / mL) of Lactobacillus plantarum WSH048 was stirred evenly, fermented at 35°C for 36 hours, the supernatant was collected by centrifugation, and freeze-dried to obtain Composition II; referring to the methods of "NY / T 2006-2011 Determination of β-glucan Content in Cereals and Cereals and Their Products", "T / AHFIA 005-2018 Determination of Total Polyphenols in Plant Extracts and Their Products - Spectrophotometric Method", and "GB 5009.5-2016 National Food Safety Standard - Determination of Protein in Foods", the main components of Composition II were measured to be 6.05% β-glucan and 18.6% total polyphenols.
[0084] b) Composition III: Prepare a 50% solution of cassava starch, adjust the pH of the solution to 7.0, add 0.3% CGT glucosyltransferase CGTase N16, and react for 6 hours. After the reaction, obtain a solution containing Composition III through conventional enzyme inactivation, filtration, etc.; with reference to the methods in "GB 1886.351-2021 National Food Safety Standard Food Additive α-cyclodextrin" and "GB 1886.353-2021 National Food Safety Standard Food Additive γ-cyclodextrin", the content of α-cyclodextrin in the Composition III solution was measured to be 68.3%, and the content of γ-cyclodextrin was 18.1%.
[0085] c) Preparation method of the composition: freeze-dry the solution of composition III to obtain a powder containing composition III, and then mix it with composition II in a ratio of 2:1 to obtain the composition required in comparative example 1.
[0086] Comparative Example 2: This example provides a composition and a preparation method that does not contain composition II. The specific preparation method is as follows:
[0087] a) Composition I: Grapefruit seed peel was dried at 40°C, crushed and sieved to 80 mesh, and enzymatically hydrolyzed with 0.15% pectinase for 2 h. The mixture was then extracted with 70% ethanol at a solid-liquid ratio of 1:25 at 60°C for 3 h. The supernatant was centrifuged and the ethanol was removed by vacuum distillation. The mixture was then dried in vacuo to obtain Composition I. According to the method in "NY / T 2014-2011 Determination of Hesperidin and Naringin Content in Citrus Fruits and Products", naringin was determined to be the main component of Composition I at a content of 96.18%.
[0088] b) Composition III: Prepare a 50% solution of cassava starch, adjust the pH of the solution to 7.0, add 0.3% CGT glucosyltransferase CGTase N16, and react for 6 hours. After the reaction, obtain a solution containing Composition III through conventional enzyme inactivation, filtration, etc.; with reference to the methods in "GB 1886.351-2021 National Food Safety Standard Food Additive α-cyclodextrin" and "GB 1886.353-2021 National Food Safety Standard Food Additive γ-cyclodextrin", the content of α-cyclodextrin in the Composition III solution was measured to be 68.3%, and the content of γ-cyclodextrin was 18.1%.
[0089] c) Preparation method of the composition: slowly add composition I to the solution of composition III at a ratio of 1:10, stir at 50°C for 6 hours, and freeze-dry to obtain a powder containing compositions I and III to obtain the composition required for Comparative Example 2.
[0090] Comparative Example 3: This example provides a composition and a preparation method that does not contain composition III. The specific preparation method is as follows:
[0091] a) Composition I: Grapefruit seed peel was dried at 40°C, crushed and sieved to 80 mesh, and enzymatically hydrolyzed with 0.15% pectinase for 2 h. The mixture was then extracted with 70% ethanol at a solid-liquid ratio of 1:25 at 60°C for 3 h. The supernatant was centrifuged and the ethanol was removed by vacuum distillation. The mixture was then dried in vacuo to obtain Composition I. According to the method in "NY / T 2014-2011 Determination of Hesperidin and Naringin Content in Citrus Fruits and Products", naringin was determined to be the main component of Composition I at a content of 96.18%.
[0092] b) Composition II: After removing impurities from oat granules, crush and sieve through 80 mesh, prepare a solution at a ratio of 1:10, sterilize and inoculate 5% of the solution to activate it to the logarithmic stage (viable cell count greater than 1×10 9 CFU / mL) of Lactobacillus plantarum WSH048 was stirred evenly, fermented at 35°C for 36 hours, the supernatant was collected by centrifugation, and freeze-dried to obtain Composition II; referring to the methods of "NY / T 2006-2011 Determination of β-glucan Content in Cereals and Cereals and Their Products", "T / AHFIA 005-2018 Determination of Total Polyphenols in Plant Extracts and Their Products - Spectrophotometric Method", and "GB 5009.5-2016 National Food Safety Standard - Determination of Protein in Foods", the main components of Composition II were measured to be 6.05% β-glucan and 18.6% total polyphenols.
[0093] d) Preparation method of the composition: Composition I and composition II were mixed in a ratio of 2:1 to obtain the composition of Comparative Example 3.
[0094] Comparative Example 4: Comparative Example 4 contains only the ingredients of component I in the composition of the present invention, and the preparation method is as follows.
[0095] Grapefruit seed peels were dried at 40°C, crushed and sieved through an 80-mesh screen, and enzymatically digested with 0.15% pectinase for 2 hours. Extraction was then carried out at 60°C for 3 hours using a 70% ethanol solution at a material-to-liquid ratio of 1:25. The supernatant was centrifuged and the ethanol was removed by vacuum distillation. The product was then dried under vacuum to obtain the material of Comparative Example 4. According to the method specified in "NY / T 2014-2011 Determination of Hesperidin and Naringin Content in Citrus Fruits and Products," the main component of Comparative Example 4 was determined to be naringin, with a content of 96.18%.
[0096] Comparative Example 5: Comparative Example 5 contains only the ingredients of component II in the composition of the present invention, and the preparation method is as follows.
[0097] After the oat granules were cleaned, they were crushed and sieved through 80 mesh, and then mixed with water at a ratio of 1:10 to prepare an aqueous solution. After sterilization, 5% of the oat granules were inoculated to activate the oat granules until the logarithmic phase (the number of viable bacteria was greater than 1×10 9 CFU / mL) of Lactobacillus plantarum WSH048 was stirred evenly, fermented at 35°C for 36 hours, centrifuged, and freeze-dried to obtain the material of Comparative Example 5. Referring to the methods of "NY / T 2006-2011 Determination of β-glucan Content in Cereals and Cereals and Their Products", "T / AHFIA 005-2018 Determination of Total Polyphenols in Plant Extracts and Their Products - Spectrophotometric Method", and "GB 5009.5-2016 National Food Safety Standard - Determination of Protein in Foods", the main components of Comparative Example 5 were measured to be 6.05% β-glucan and 18.6% total polyphenols.
[0098] Comparative Example 6: Comparative Example 6 contains only the ingredients of component III in the composition of the present invention, and the preparation method is as follows.
[0099] Cassava starch was prepared into a 50% solution, the pH value of the solution was adjusted to 7.0, 0.3% CGT glucosyltransferase CGTase N16 was added, and the reaction was carried out for 6 hours. After the reaction, the material of Comparative Example 6 was obtained after conventional enzyme inactivation, filtration, and vacuum drying. Referring to the methods of "GB 1886.351-2021 National Food Safety Standard Food Additive α-cyclodextrin" and "GB 1886.353-2021 National Food Safety Standard Food Additive γ-cyclodextrin", the content of α-cyclodextrin and γ-cyclodextrin in Comparative Example 6 was measured to be 75.2%, and the content of γ-cyclodextrin was 24.8%.
[0100] Experimental Example 1: Inhibitory effects of different compositions on pancreatic lipase
[0101] 0.2 mL of pancreatic lipase solution, 0.2 mL of the composition solutions of Examples 1-6 and Comparative Examples 1-6 (mixed with water to a 20% concentration), and 0.5 mL of Tris-HCl buffer were mixed and preheated in a 37°C dry block for 10 minutes. The reaction was initiated by adding 0.6 mL of pNPL substrate solution. After 20 minutes of reaction, the sample was removed and then placed in a boiling water bath to terminate the reaction for 10 minutes. The sample was centrifuged at 3000 g for 5 minutes, and the supernatant was retained. The absorbance was measured at 405 nm using a UV spectrophotometer. A blank control group did not contain pancreatic lipase solution, and a control group did not contain inhibitor solution. A blank control group did not contain both inhibitor and pancreatic lipase solution. Orlistat was used as a positive control.
[0102] The experiment was repeated three times, and the inhibition rate was calculated according to the equation: inhibition rate (%) = 1-(A experimental group-A experimental blank group) / (A control group-A control blank group)*100%.
[0103] In vitro activity is expressed as inhibitor concentration, which can inhibit pancreatic lipase activity by 50%. The results are shown in Figure 1. The inhibitor concentration is positively correlated with enzyme inhibition and is dose-dependent. As the concentration of Examples 1-6, Comparative Examples 1-3, and orlistat increases, the activity of pancreatic lipase gradually decreases. Examples 1-6 and Comparative Examples 1-3 all have a certain inhibitory effect on pancreatic lipase, and their inhibitory effect on pancreatic lipase is better than that of orlistat. However, Examples 1-6 have a better inhibitory effect on pancreatic lipase than Comparative Examples 1-6.
[0104] Experimental Example 2: Effects of different compositions on fat accumulation and organ weight in rats fed a high-fat diet
[0105] To evaluate the effects of different compositions on fat accumulation in rats, a long-term (12-week) animal experiment was conducted. SD rats (purchased from Nanjing Jicui Yaokang Biotechnology Co., Ltd.) were randomly divided into 12 groups, with 10 rats in each group: a normal diet group, a high-fat diet group, experimental groups 1-6 (administered with the compositions of Examples 1-6 at a ratio of 200 mg / kg), control groups 1-3 (administered with the compositions of Comparative Examples 1-3 at a ratio of 200 mg / kg), and a positive control group (administered with orlistat at a ratio of 10 mg / kg). To prevent auto-oxidation of dietary fat, the diet was freshly prepared weekly and stored at -20°C. The rats were weighed weekly. After 12 weeks of feeding, the rats were anesthetized with chloral hydrate, and white epididymal fat and liver tissue were removed and weighed. Changes in rat body weight, liver tissue, and epididymal fat weight are shown in Figures 2-3.
[0106] As shown in Figure 2, at the beginning of the first week, the weights of all 12 groups of rats were similar. As the number of feeding days increased, the weights of the rats in each group increased to varying degrees. However, the rats fed a high-fat diet gained weight much faster than those fed a normal diet. After 12 weeks of feeding, the weights of the rats in experimental groups 1-6 and control groups 1-6 decreased to varying degrees compared to the high-fat diet group, demonstrating that the Example composition can reduce the weight gain caused by a high-fat diet in rats after 12 weeks of treatment. Furthermore, compared to the positive control group, the weight reduction effect in experimental groups 1-6 was significantly greater than that in control groups 1-6.
[0107] Increased organ weight can also be used as an indicator of obesity, as excessive energy intake leads to fat accumulation in various organs. As shown in Figure 3, compared to the normal control group, the liver and white epididymal fat weights of rats in the high-fat diet group were significantly increased, indicating excessive fat deposition around the organs in the high-fat diet group. Compared to the high-fat diet group, supplementation with the experimental group composition and orlistat reduced white epididymal fat deposition and liver weight to a certain extent. Control groups 1-6 also had some effect on white epididymal fat deposition and liver weight, but the reduction was not as great as in experimental groups 1-6.
[0108] Experimental Example 3: Effects of different compositions on the body weight of obese patients
[0109] Experimental Method: 200 obese subjects (aged 35-45 years) were selected as subjects and randomly divided into six experimental groups and four control groups based on body weight and body fat mass, with 20 subjects in each group. The experimental groups took the test samples of Examples 1-6 (corresponding to Experimental Groups 1-6, respectively) according to the recommended method for human use; Control Groups 1-6 took Control Examples 1-6 and orlistat for 60 consecutive days, maintaining a normal diet and daily routine during the experimental period. Body weight was measured every two weeks. The subjects' health was not affected before and after the experiment, and their trace element levels met the standard. Figure 4 shows the weight change curve. The results in Figure 4 show that the product of the present invention can effectively help obese patients lose weight. In addition, the efficacy of the three-component combination of the present invention (Examples 1-6) was significantly better than that of the single component combination (Comparative Examples 1-6).
[0110] The above description is merely a preferred embodiment of the present invention and does not constitute any form of limitation to the present invention. Although the present invention has been disclosed as a preferred embodiment as above, it is not intended to limit the present invention. Any technician familiar with this profession can make slight changes or modifications to equivalent embodiments of the methods and technical contents disclosed above without departing from the scope of the technical solution of the present invention. However, any simple modifications, equivalent changes and modifications made to the above embodiments based on the technical essence of the present invention without departing from the content of the technical solution of the present invention are still within the scope of the technical solution of the present invention.
Claims
1. A composition containing a lipase inhibitor, characterized in that The composition includes composition I, composition II, and composition III, wherein the mass ratio of composition I, composition II, and composition III is (0.1-1):(0.1-20):(1-30).
2. The composition according to claim 1, characterized in that The composition I is selected from one or more extracts of the following group, the group consisting of: berries, stone fruits, pome fruits, citrus fruits, multiple fruits, and aggregate fruits.
3. The composition according to claim 2, characterized in that The citrus fruits are selected from one or more of the following groups, which group consists of: kumquat, mandarin orange, sweet orange, grapefruit, kumquat, lemon, lime, mandarin orange, navel orange, sour orange, bergamot, and citron.
4. The composition according to claim 2, characterized in that The composition I is selected from one or more of the following groups: polysaccharides, fruit acids, pectin, flavonoids, volatile oils, alkaloids, minerals, proteins, and polypeptides.
5. The composition according to claim 4, characterized in that The composition I is one or more compositions or derivatives selected from the following group: naringin, naringin, wild sumac, hesperidin, naringenin, neohesperidin, hesperidin, naringin, dihydroquercetin, isoetolide, acacia, 8-hydroxyapigenin, luteolin, carkaol, pentahydroxyflavone, apigenin, geraniol, tangeretin, nobiletin, catechol, rutin, monocoumarin, furanocoumarin, α-limonene, β-myrcene, γ-terpinene, α-pinene, citrus flavonoids, citrus glycosides, quercetin, and tangeretin.
6. The composition according to claim 1, characterized in that The composition II is selected from one or more cereal extracts in the following group, which consists of oats, highland barley, naked oats, barley, buckwheat, wheat, sorghum, millet, foxtail millet, and millet.
7. The composition according to claim 6, characterized in that The composition II is selected from one or more of the following groups, which consists of: oat alkaloids, polyphenols, p-hydroxybenzoic acid, 2,4-dihydroxybenzoic acid, salicylic acid, syringic acid, vanillic acid, gallic acid C, protocatechuic acid, syringaldehyde, vanillin, 4-hydroxyphenylacetic acid, p-coumaric acid, o-coumaric acid, cinnamic acid, ferulic acid, caffeic acid, sinapic acid, caffeic acid derivatives, ferulic acid derivatives, benzoic acid-O-sulfate, syringaldehyde-O-sulfuric acid, syringic acid-O-sulfuric acid, vanillin-O-sulfate, dihydroxybenzoic acid-O-sulfate, caffeic acid-O-sulfate, hydroxyphenylacetic acid-O-sulfate, homovanillic acid-O-glucuronic acid, sinapic acid-O-sulfate, feruloylglycine, benzoic acid-O-glucuronic acid, homovanillic acid-O-glucuronic acid, Vanillin-O-glucuronic acid, dihydrofuranyl-O-glucuronic acid, 3,4-dihydroxyoctanoyl-O-glucuronic acid, 4-hydroxyphenylacetic acid-O-glucuronic acid, ferulic acid-O-glucuronic acid, aldose-O-glucuronide, kaempferol, linalool, rutin, citrinin, myricetin, quercetin, tricin, avenanthin, β-glucan.
8. The composition according to claim 1, characterized in that The composition III is an oligosaccharide mixture enriched after starch is hydrolyzed by enzymes or fermented by microorganisms, or a derivative obtained by modifying the oligosaccharide mixture as a substrate.
9. The composition according to claim 8, characterized in that The starch is selected from one or more of corn starch, tapioca starch, wheat starch, potato starch, and rice starch; The enzyme is selected from one or more of α-amylase, β-amylase, CGT glucosyltransferase, and isoamylase; The microorganism is selected from one or more of Bacillus, Thermobacterium, Bacillus circulans, Bacillus softening, alkali-resistant Bacillus megaterium, and Escherichia coli.
10. The composition according to claim 8, characterized in that The composition III is selected from one or more of the following groups, which consists of: xylooligosaccharides, fructooligosaccharides, maltotetraose, maltooligosaccharides, isomaltooligosaccharides, stachyose, raffinose, lactulose, chitosan oligosaccharides, galactooligosaccharides, α-cyclodextrin, β-cyclodextrin, γ-cyclodextrin, hydroxypropyl-β-cyclodextrin, permethylated β-cyclodextrin, cinnamaldehyde-β-cyclodextrin, limonene-β-cyclodextrin, linalool-β-cyclodextrin, myrcene-β-cyclodextrin, octanal-β-cyclodextrin, decanal-β-cyclodextrin, crotonic acid-β-cyclodextrin, poly-[6-deoxy-6-cysteine]-γ-cyclodextrin, thiolated β-cyclodextrin, α-cyclodextrin Arginine valeric acid, α-cyclodextrin polyrotaxane, permethylated α-cyclodextrin, permethylated γ-cyclodextrin, carboxymethyl β-cyclodextrin, ferulic acid-α-cyclodextrin, maltosyl-α-cyclodextrin, 2-phenylethanol-α-cyclodextrin, hydroxypropyl-γ-cyclodextrin, dialdehyde γ-cyclodextrin, ethyl butyrate-γ-cyclodextrin, hexanal-γ-cyclodextrin, hexanol-γ-cyclodextrin, high branched starch, amylose, resistant starch RS1, resistant starch RS2, starch stearate, starch octenylsuccinate, starch acetate, sodium carboxymethyl starch, acetylated starch, hydroxypropyl starch, starch acetate, starch phosphate, alkenyl starch esters, acetylated distarch, acetylated distarch phosphate.
11. A method for preparing the composition containing a lipase inhibitor according to any one of claims 1 to 10, characterized in that: The following steps are involved: a) preparing composition I: drying citrus peel at 40-60°C, crushing and sieving to 40-200 mesh, adding 0.1%-5% pectinase for 0.5-5 h, extracting with 40%-90% ethanol solution at a solid-liquid ratio of 1:(1-30) at 20-80°C for 0.5-5 h, centrifuging the supernatant, removing ethanol by vacuum distillation, and drying in vacuo to obtain composition I; b) Preparation of Composition II: After removing impurities from the cereal seeds, crush them and sieve them through 40-200 mesh. Prepare an aqueous solution with water at a ratio of 1:(1-10). After sterilization, inoculate 0.5%-10% of activated bacteria to the logarithmic stage (viable bacteria count greater than 1×10 9 CFU / mL) of Lactobacillus plantarum WSH048, stirring evenly, fermenting at 20-40°C for 12-48 hours, collecting the supernatant by centrifugation after the fermentation, and freeze-drying to obtain composition II; c) Preparing Composition III: Prepare a 1-70% starch solution, adjust the pH of the solution to 4-9.0, add or not add amylase / inoculate or not inoculate with a microorganism, and react at 25-60°C for 0.5-5 hours. After the reaction is completed, increase the temperature to 50-90°C, adjust the pH to 2-8.0, and add or not add amylase, and react for 2-12 hours. After the reaction is completed, perform conventional enzyme inactivation and filtration to obtain a solution containing Composition III; d) Composition preparation method: Composition I, composition II, and composition III are mixed in a mass ratio of (0.1-1):(0.1-20):(1-30), and composition I is slowly added to a solution of composition III. The mixture is stirred at 20-60°C for 0.5-10 hours, and freeze-dried to obtain a powder containing compositions I and III. The powder is then mixed with composition II to obtain the composition containing the lipase inhibitor.
12. A product for assisting the treatment of obesity and metabolic syndrome, characterized in that: A composition comprising the composition according to any one of claims 1 to 10, or a composition prepared according to the preparation method according to claim 11.
13. The product according to claim 12, characterized in that Including solid beverages, liquid beverages, and dietary supplements.
14. Use of a composition containing a lipase inhibitor in the preparation of a drug for auxiliary treatment of obesity and metabolic syndrome, characterized in that: The composition is the composition according to any one of claims 1 to 10, or the composition prepared by the preparation method according to claim 11.
Citation Information
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