N-acetylneuraminic acid and lotus leaf composition with lipid-lowering and weight loss effects and application thereof in preparation of medicine for inhibiting weight gain
By combining lotus leaf alcohol extract with N-acetylneuraminic acid to create a variety of oral formulations, the problems of side effects and limited weight loss effects of existing obesity drugs have been solved, achieving effective weight management and improvement of blood lipids.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- JIANGNAN UNIV
- Filing Date
- 2024-06-25
- Publication Date
- 2026-07-21
AI Technical Summary
In the existing technology, drugs used to treat obesity usually have side effects and limited weight loss effects. Rapid weight loss methods can lead to insufficient energy intake and are difficult to effectively control weight gain in adults.
Lotus leaf alcohol extract is combined with N-acetylneuraminic acid in a weight ratio of 1:5 to 5:1 to make health food products such as powder, granules, capsules, tablets, pills or syrups, which can be administered orally to synergistically inhibit weight gain.
The composition significantly reduced body weight, adipose tissue weight and blood lipid levels in mice on a high-fat diet, exhibiting a synergistic lipid-lowering and weight-loss effect. In particular, the effect was best when the ratio of lotus leaf extract to N-acetylneuraminic acid was 1:1.
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Abstract
Description
Technical Field
[0001] This invention relates to the field of functional composition technology, and in particular to a composition of N-acetylneuraminic acid and lotus leaf and its application in inhibiting weight gain. Background Technology
[0002] According to the World Health Organization (WHO), overweight and obesity refer to abnormal or excessive fat accumulation and are a risk factor for death, significantly impacting human health and lifespan. Obesity has been linked to a variety of diseases, including hypertension, hyperlipidemia, diabetes, sleep apnea syndrome, and cognitive impairment. Influenced by physical condition and the aging process of various organs, overweight and obesity significantly increase the risk of disease and death in adults. Therefore, weight management is extremely important for adults.
[0003] Weight management is influenced by genetics, diet, exercise, and complex biology. Regarding diet, individuals with a high-fat diet are more prone to overweight and obesity. Currently, most medications for treating obesity work by reducing food intake or suppressing appetite, altering metabolism, or blocking fat absorption; however, these medications often cause side effects and have limited weight loss efficacy. Rapid weight loss and calorie restriction can lead to insufficient energy intake, thereby reducing muscle protein synthesis and muscle mass, and are not suitable for weight management in middle-aged and elderly individuals. Therefore, developing effective functional substances and methods for controlling obesity in adults is of great significance.
[0004] Lotus leaf (Nelumbo nucifera Gaertn. leaf) is an aquatic herbaceous plant belonging to the genus Nelumbo in the family Nelumbo. It is listed in the "List of Products That Are Both Food and Medicine" issued by the National Health Commission and the State Administration of Traditional Chinese Medicine, making it a multifunctional resource. In culinary terms, it is used to wrap food in special dishes such as zongzi (sticky rice dumplings) and lotus leaf rice, adding unique flavor while preserving the food's freshness. Medicinally, lotus leaf is believed to have effects such as clearing heat and detoxifying, promoting diuresis and aiding weight loss. It is commonly used to treat symptoms such as thirst, oral ulcers, and obesity.
[0005] N-acetylneuraminic acid, also known as sialic acid, is a monosaccharide belonging to the nonose group of sugars, naturally found in breast milk, dairy products, and other foods. The European Union, Japan, Malaysia, and Singapore, among other countries / regions, use N-acetylneuraminic acid as a food ingredient. my country included it as a new food ingredient in 2017. N-acetylneuraminic acid has numerous biological functions, serving as an important component of cell surface glycoproteins and glycolipids, playing a crucial role in human health and disease, including improving cognitive function, immune regulation, and weight management.
[0006] While existing technologies disclose that both lotus leaf and N-acetylneuraminic acid have lipid-lowering and weight-loss effects, there are no reports of their combined use in weight management. The inventors of this application unexpectedly discovered that the two have a synergistic effect in inhibiting weight gain, and combining lotus leaf and N-acetylneuraminic acid unexpectedly yielded even better results. Summary of the Invention
[0007] To address the shortcomings of existing technologies, this invention provides a composition of N-acetylneuraminic acid and lotus leaf and its application in inhibiting weight gain.
[0008] The technical solution adopted in this invention is as follows:
[0009] In one aspect, the present invention provides a composition of N-acetylneuraminic acid and lotus leaf, wherein the composition comprises lotus leaf alcohol extract and N-acetylneuraminic acid, and the weight ratio of lotus leaf alcohol extract to N-acetylneuraminic acid is in the range of 1:5 to 5:1.
[0010] The further technical solution is as follows:
[0011] The weight ratio of the lotus leaf alcohol extract to N-acetylneuraminic acid is 1:1.
[0012] A second aspect of the present invention provides the use of the composition in synergistically inhibiting weight gain.
[0013] A third aspect of the present invention provides the application of the composition in the preparation of health food with lipid-lowering and weight-loss effects.
[0014] The further technical solution is as follows:
[0015] The health food product in question is an oral preparation.
[0016] The oral preparations include powders, granules, capsules, tablets, pills, or syrups.
[0017] The beneficial effects of this invention are as follows:
[0018] Animal experiments have demonstrated that the lotus leaf alcohol extract and N-acetylneuraminic acid in the composition of this invention have a synergistic effect in inhibiting weight gain, and can effectively reduce lipids and promote weight loss.
[0019] Other features and advantages of the invention will be set forth in the description which follows, and will be apparent in part from the description, or may be learned by practicing the invention. Detailed Implementation
[0020] The present invention discloses an N-acetylneuraminic acid and lotus leaf composition, wherein the composition comprises lotus leaf alcohol extract and N-acetylneuraminic acid, and the weight ratio of the lotus leaf alcohol extract and N-acetylneuraminic acid is in the range of 1:5 to 5:1.
[0021] As a preferred embodiment, the weight ratio of the lotus leaf alcohol extract to N-acetylneuraminic acid is 1:1.
[0022] The acquisition of the lotus leaf alcohol extract includes:
[0023] Using dried lotus leaves as raw material, the leaves are pulverized into powder, and then 10 times the amount of 80% ethanol is added. Extraction is carried out at 45℃, with an ultrasonic frequency of 40kHz, an ultrasonic power of 50W, and an ultrasonic time of 30 minutes. Extraction is performed twice, each time for 1.5 hours. The filtrates from each extraction are combined, and the ethanol is recovered until the filtrate has no alcohol odor. The solution is then concentrated and freeze-dried to obtain the final product. The product specification is 10:1. The applicable standard is the enterprise filing standard Q / 610000-G1705260.
[0024] The N-acetylneuraminic acid used in this invention is a commercially available product with a purity of over 98%, which can be obtained through legitimate commercial channels.
[0025] The experimental methods used in this invention are conventional techniques in the field, and the experimental reagents used are commercially available or prepared according to conventional methods in the field.
[0026] The following describes specific embodiments of the present invention based on the above-mentioned raw materials and proportions.
[0027] Example 1
[0028] A composition of N-acetylneuraminic acid and lotus leaf, wherein the composition comprises, by weight, the following components: N-acetylneuraminic acid: lotus leaf alcohol extract = 3:1.
[0029] Example 2
[0030] A composition of N-acetylneuraminic acid and lotus leaf, wherein the composition comprises, by weight, the following components: N-acetylneuraminic acid: lotus leaf alcohol extract = 1:3.
[0031] Example 3
[0032] A composition of N-acetylneuraminic acid and lotus leaf, wherein the composition comprises, by weight, the following components: N-acetylneuraminic acid: lotus leaf alcohol extract = 1:1.
[0033] Example 4
[0034] A granule formulation comprising the composition of Example 1, exhibiting lipid-lowering and weight-loss effects. The granule formulation is manufactured by adding pharmaceutically acceptable excipients to the lipid-lowering and weight-loss composition of Example 1, followed by conventional processes such as mixing, granulation, drying, sizing, and packaging. This granule formulation can be used as a solid beverage for convenient consumption.
[0035] In the same manner, the compositions of Examples 2 and 3 were prepared into granules with corresponding lipid-lowering and weight-loss effects.
[0036] Example 5
[0037] A capsule formulation comprising the composition of Example 1, having a lipid-lowering and weight-loss effect. The capsule formulation is prepared by adding pharmaceutically acceptable excipients to the composition of Example 1 having a lipid-lowering and weight-loss effect, forming granules using conventional methods, and then encapsulating the granules.
[0038] In the same manner, the compositions of Examples 2 and 3 were prepared into capsules with corresponding lipid-lowering and weight-loss effects.
[0039] Example 6
[0040] A tablet comprising the composition of Example 1, having a lipid-lowering and weight-loss effect. The tablet is prepared by adding pharmaceutically acceptable excipients to the composition of Example 1 having a lipid-lowering and weight-loss effect, granulating it using conventional methods, and then compressing the granules into a tablet.
[0041] In the same manner, the compositions of Examples 2 and 3 were made into tablets with corresponding lipid-lowering and weight-loss effects.
[0042] Example 7
[0043] A pill comprising the composition of Example 1, having a lipid-lowering and weight-loss effect. The pill is prepared by adding pharmaceutically acceptable excipients to the lipid-lowering and weight-loss composition of Example 1, using conventional methods.
[0044] In the same manner, the compositions of Examples 2 and 3 were prepared into pills with corresponding lipid-lowering and weight-loss effects.
[0045] Example 8
[0046] A syrup containing the composition of Example 1, having lipid-lowering and weight-loss effects. The syrup is prepared by adding pharmaceutically acceptable excipients to the composition of Example 1 with lipid-lowering and weight-loss effects, using conventional methods.
[0047] In the same manner, the compositions of Examples 2 and 3 were prepared into syrups with corresponding lipid-lowering and weight-loss effects.
[0048] Pharmacodynamic experiments:
[0049] Mice on a high-fat diet were fed the composition of the present invention dissolved in a 0.5% sodium carboxymethyl cellulose solution via oral gavage for 12, 24, and 40 weeks, and the effects on mouse body weight and blood glucose and lipid levels were monitored.
[0050] 1. Materials and Methods
[0051] 1.1 Test materials
[0052] N-acetylneuraminic acid (Shanghai Yuanye Biotechnology Co., Ltd., purity ≥98%), lotus leaf (Beijing Tongrentang).
[0053] C57BL / 6J mice were purchased from Beijing Vital River Laboratory Animal Technology Co., Ltd.
[0054] High-fat diet (60% high-fat diet TP23300, protein calories 19%, carbohydrates 21%, fat 60.0%; formula: casein 189g / kg; dextrin 108g / kg; sucrose 67g / kg; corn starch 497g / kg; soybean oil 21g / kg; lard 21g / kg; cellulose 48g / kg; minerals 36g / kg; vitamins 9g / kg; L-cysteine 2g / kg; choline tartrate 2g / kg; 5TBHQ 0.067g / kg) and control diet (TP 23302, protein calories 19%, carbohydrates 71%, fat 10.0%; formula: casein 267g / kg; dextrin 157g / kg; sucrose 89g / kg; soybean oil 33g / kg; lard 301g / kg; cellulose 67g / kg; minerals 66g / kg; vitamins 13g / kg; L-cysteine 4g / kg; choline tartrate 3g / kg; 5TBHQ 0.067g / kg), purchased from Nantong Trofi Feed Technology Co., Ltd.
[0055] 1.2 Test Methods
[0056] 1.2.1 Animal experiments and grouping
[0057] 168 five-week-old male C57BL / 6J mice were selected for the experiment and housed in the Experimental Animal Center of Jiangnan University (SPF grade). The experiment was conducted in strict accordance with the approval of the Animal Experiment Ethics Committee of Jiangnan University (ethics number: JN.No20230415c1300730
[142] ). The ambient temperature was 20℃~26℃, the humidity was 60%, and the light time was 8:00am-20:00pm, with a 12h day-night cycle. During the period of housing, the mice had free access to food and water. After one week of acclimatization, the mice were randomly divided into 7 groups, with 24 mice in each group (divided into 3 batches, with 8 mice in each batch for different cycles). The details of each group are as follows:
[0058] ND group: given control feed;
[0059] HFD group: fed a high-fat diet;
[0060] NANA group: fed a high-fat diet and administered N-acetylneuraminic acid (200 mg / (kg.bw) / day) orally by gavage;
[0061] LLE group: fed a high-fat diet and administered lotus leaf extract (200 mg / (kg.bw) / day) orally by gavage;
[0062] Example 1 group: fed a high-fat diet and administered N-acetylneuraminic acid (150 mg / (kg.bw) / day) and lotus leaf alcohol extract (50 mg / (kg.bw) / day) by oral gavage;
[0063] Example 2 group: fed a high-fat diet and administered N-acetylneuraminic acid (50 mg / (kg.bw) / day) + lotus leaf alcohol extract (150 mg / (kg.bw) / day) by oral gavage;
[0064] Example 3 group: fed a high-fat diet and administered N-acetylneuraminic acid (100 mg / (kg.bw) / day) + lotus leaf alcohol extract (100 mg / (kg.bw) / day) by oral gavage.
[0065] Throughout the experiment, the mice were allowed free access to food and water. Their weight was recorded weekly, and their food intake was recorded every 3 days. The total experimental period was 40 weeks, divided into three batches, with dissections performed at the end of weeks 12, 24, and 40, respectively.
[0066] 1.2.2 Fasting blood glucose measurement
[0067] Mice in each group were fasted for 12 hours at weeks 12, 24 and 40, and blood was collected from the tail vein. The initial blood glucose level (mM) of the mice was measured using a glucometer.
[0068] 1.2.3 Determination of Blood Biochemical Indicators in Mice
[0069] Mice raised for 12, 24, and 40 weeks were anesthetized, and blood was collected from their eyeballs. The blood was centrifuged at 3000 rpm for 15 min, and the serum was separated. The serum levels of total cholesterol (TC, mmol / L), triglycerides (TG, mmol / L), high-density lipoprotein cholesterol (HDL-C, mmol / L), and low-density lipoprotein cholesterol (LDL-C, mmol / L) were measured according to the kit instructions.
[0070] 1.2.4 Weighing of mouse epididymal adipose tissue
[0071] After blood was drawn from the eyeballs of mice, the epididymal adipose tissue was dissected, rinsed with physiological saline, and excess water was absorbed with absorbent paper before being weighed.
[0072] 2. Experimental Results
[0073] Table 1: Effects of different compositions on body weight and epididymal adipose tissue weight in high-fat diet-induced obese mice
[0074]
[0075]
[0076] Note: Different lowercase letters in the same column represent significant differences (p<0.05).
[0077] As shown in Table 1, the weight gain of mice fed a high-fat diet was significantly higher than that of mice fed a control diet at different time periods. The combination of the three example groups showed better inhibitory effects on weight gain than any single group, especially when the ratio of N-acetylneuraminic acid to lotus leaf extract was 1:1 (Example 3 group), the inhibitory effect was the best. Furthermore, there was no significant difference in food intake among the different groups, indicating that food intake was not a factor affecting weight change. In addition, the results on the effect on epididymal adipose tissue weight showed that the different combinations in the NANA and LLE groups significantly inhibited white adipose tissue formation, with better effects than any single group, especially when the ratio of NANA to LLE was 1:1.
[0078] Table 2: Effects of different compositions on serum lipid and blood glucose levels in high-fat diet-induced obese mice
[0079]
[0080] Note: Different lowercase letters in the same column represent significant differences (p<0.05).
[0081] Table 2 shows that long-term high-fat diet feeding caused abnormal blood glucose and lipid levels in mice. The compositions of the three example groups showed better inhibitory effects on triglycerides, total cholesterol, and low-density lipoprotein cholesterol than any single group, especially when the ratio of N-acetylneuraminic acid to lotus leaf extract was 1:1 (Example 3 group), the inhibitory effect was the best. In addition, the results of high-density lipoprotein levels and fasting blood glucose measurements showed no significant difference between the different experimental groups and the normal group.
[0082] 3. Conclusion
[0083] Examples 1, 2, and 3 of the present invention significantly reduced body weight, adipose tissue weight, blood lipids, and blood glucose in mice fed a high-fat diet, showing significant differences compared to the model group. Furthermore, compared to single components, the compositions of the present invention have a synergistic effect in improving obesity and abnormal blood glucose and lipid levels induced by a high-fat diet, with the inhibitory effect being best when the ratio of N-acetylneuraminic acid to lotus leaf extract is 1:1.
[0084] In summary, the inventors unexpectedly achieved a better weight-loss inhibition effect by combining lotus leaf and N-acetylneuraminic acid. It is speculated that when N-acetylneuraminic acid is used in combination with lotus leaf extract, it can promote the binding of lotus leaf extract to the target site of β3-adrenergic receptor (β3-AR), thus making the effect of inhibiting blood lipids and body weight more significant. Therefore, the combined use of N-acetylneuraminic acid and lotus leaf extract has important application prospects in weight management.
[0085] It will be understood by those skilled in the art that the above description is merely a preferred embodiment of the present invention and is not intended to limit the present invention. Although the present invention has been described in detail with reference to the foregoing embodiments, those skilled in the art can still modify the technical solutions described in the foregoing embodiments or make equivalent substitutions for some of the technical features. Any modifications, equivalent substitutions, improvements, etc., made within the spirit and principles of the present invention should be included within the protection scope of the present invention.
Claims
1. A composition of N-acetylneuraminic acid and lotus leaf with lipid-lowering and weight-loss effects, characterized in that, The composition comprises lotus leaf ethanol extract and N-acetylneuraminic acid, wherein the weight ratio of lotus leaf ethanol extract to N-acetylneuraminic acid is 1:1; the lotus leaf ethanol extract is obtained by extraction with 80% ethanol.
2. Use of the composition of claim 1 in the preparation of a medicament for inhibiting weight gain.
3. The use of the composition of claim 1 in the preparation of a health food product with lipid-lowering and weight-loss effects.
4. The application according to claim 3, characterized in that, The health food product in question is an oral preparation.
5. The application according to claim 4, characterized in that, The oral preparations are powders, granules, capsules, tablets, pills, or syrups.