Anti-aging compositions and uses thereof

Abstract

This invention belongs to the field of pharmaceutical technology, specifically relating to an anti-aging composition and its application. The active ingredients of this composition include quercetin and phospholipids, with a mass ratio of quercetin to phospholipids of 1:(0.1~5). A significant synergistic effect exists between the active ingredients quercetin and phospholipids, particularly in their combination for significant anti-aging efficacy. Furthermore, both quercetin and phospholipids are natural active ingredients with low toxicity and side effects. Therefore, this composition exhibits a very significant anti-aging effect, demonstrating higher anti-aging activity compared to NMN, and with fewer toxic side effects and high safety, showing broad application prospects.

Description

Technical Field

[0001] This invention belongs to the field of pharmaceutical technology, and in particular relates to an anti-aging composition and its application. Background Technology

[0002] With the progress of human society and the development of medical technology, people's average lifespan has been continuously increasing. However, this has also led to the intensification of the aging problem and the emergence of a variety of related issues, such as cognitive decline, motor function decline, and the increase in other chronic diseases, making social problems such as elderly care and medical care increasingly prominent. Aging is a complex process, influenced by a variety of internal and external factors. How to effectively combat aging and reduce the occurrence of related diseases is one of the major challenges facing human society.

[0003] There is currently a lot of research on anti-aging, such as NMN (β-nicotinamide mononucleotide), which has become quite popular in the international market in recent years. Studies have shown that NMN can delay aging and extend the lifespan of animals, but it also has many safety concerns, such as long-term use leading to tolerance, lack of relevant clinical data in humans, and short research time making it impossible to guarantee safety. Therefore, finding a safe and effective natural anti-aging composition is of great significance. Summary of the Invention

[0004] This invention aims to at least partially address one of the technical problems in the prior art. Therefore, one object of this invention is to provide an anti-aging composition and its application.

[0005] In a first aspect, the present invention provides an anti-aging composition, the active ingredients of which include quercetin and phospholipids, wherein the mass ratio of quercetin to phospholipids is 1:(0.1~5).

[0006] For example, the mass ratio of quercetin to the phospholipid is 1:0.1, 1:1, 1:2, 1:3, 1:4, 1:5, or any range between any two of the above values.

[0007] The anti-aging composition provided by this invention comprises quercetin and phospholipids as its active ingredients. As natural active ingredients, quercetin and phospholipids have very low toxicity and can be widely used in food, pharmaceuticals, cosmetics, and other fields. Although there are many reports on quercetin and phospholipids individually, there is currently no existing technology that combines them to achieve the desired effect. The inventors unexpectedly discovered a significant synergistic effect between quercetin and phospholipids, particularly demonstrating significant anti-aging efficacy when combined. Furthermore, controlling the mass ratio of quercetin to phospholipids within the range of 1:(0.1~5) is crucial for the composition to exhibit a significant anti-aging effect. If the amount of phospholipids added is too high or too low, not only will the anti-aging effect of the composition not be enhanced, but it may even be reduced compared to using quercetin alone. Therefore, controlling the mass ratio of quercetin to phospholipids plays a decisive role in the anti-aging efficacy of the composition. Therefore, this composition has a very significant anti-aging effect, with higher anti-aging activity compared to NMN. Moreover, this composition is a natural ingredient with fewer toxic side effects and has broad application prospects.

[0008] Preferably, the mass ratio of quercetin to phospholipid is 1:(0.5~2). For example, the mass ratio of quercetin to phospholipid is 1:0.5, 1:1.5, 1:2, etc., or any range between the two values ​​mentioned above.

[0009] According to the anti-aging composition provided by the present invention, the phospholipid includes at least one of plant phospholipids or animal phospholipids, preferably plant phospholipids, and more preferably soybean phospholipids.

[0010] According to the anti-aging composition provided by the present invention, the active ingredient of the composition also includes polysaccharides. The inventors have found that, compared with simply combining quercetin and phospholipids, the combination of polysaccharides with quercetin and phospholipids significantly enhances the anti-aging effects in terms of extending lifespan, improving motor function, and enhancing cognitive abilities.

[0011] In some embodiments of the present invention, the glucose content in the monosaccharide composition of the polysaccharide is not less than 80%, preferably not less than 95%.

[0012] In some embodiments of the present invention, the weight-average molecular weight of the polysaccharide is not less than 5000 Da, preferably 5000 Da-100000 Da.

[0013] In some embodiments of the present invention, the glycosidic bonds of the polysaccharide are 1,4 glycosidic bonds, preferably α-1,4 glycosidic bonds.

[0014] Preferably, the polysaccharide has a glucose content of not less than 80% in its monosaccharide composition, a weight-average molecular weight of not less than 5000 Da, and a glycosidic bond of 1,4.

[0015] More preferably, the polysaccharide has a glucose content of not less than 95% in its monosaccharide composition, the polysaccharide has a weight-average molecular weight of 5000 Da-100000 Da, and the polysaccharide has an α-1,4 glycosidic bond.

[0016] In some embodiments of the present invention, the polysaccharide is preferably a starch-based polysaccharide, and more preferably a dextrin-based polysaccharide.

[0017] In some embodiments of the present invention, the dextrin has a molecular weight distribution of 100,000 Da to 5,000 Da, and the glucose content in the monosaccharide composition is 95%.

[0018] It should be noted that the above molecular weight and monosaccharide composition detection methods refer to "Zhang Xu. Systematic Analysis and Immunological Activity Study of Ginseng Polysaccharides [D]. Northeast Normal University, 2009".

[0019] In some embodiments of the present invention, the polysaccharide accounts for 40% to 120% of the total mass of the quercetin and the phospholipids. By controlling the amount of polysaccharide added within the above range relative to the total mass of the quercetin and phospholipids, a better effect of prolonging life, improving motor skills, and enhancing cognitive abilities can be achieved.

[0020] In some embodiments of the present invention, the active ingredient is composed of quercetin, phospholipids, and polysaccharides in a mass ratio of 1:(0.1~5):(1~30), preferably 1:(0.5~2):(1~10). The active ingredient, composed of quercetin, phospholipids, and polysaccharides in the above-mentioned mass ratio, can fully leverage the synergistic effect of the three components and significantly enhance the anti-aging effect of the composition.

[0021] In a second aspect, the present invention proposes the application of the above-mentioned anti-aging composition in the preparation of food, pharmaceuticals, health products, cosmetics, and feed.

[0022] Its preferred applications are in the preparation of foods, pharmaceuticals, cosmetics, and animal feeds with anti-aging effects. Specifically, foods include both general foods and health foods.

[0023] In a third aspect, the present invention provides a pharmaceutical preparation containing the above-described anti-aging composition. Therefore, the pharmaceutical preparation exhibits excellent anti-aging efficacy, and has fewer toxic side effects and higher safety.

[0024] Preferably, the dosage form of the pharmaceutical preparation includes injections, tablets, granules, or capsules.

[0025] The beneficial effects of the present invention include at least the following: The anti-aging composition provided by this invention uses quercetin and phospholipids as natural active ingredients, with very few toxic side effects, and can be widely used in food, pharmaceuticals, cosmetics, and other fields. There is a significant synergistic effect between quercetin and phospholipids, especially when combined, which has a significant anti-aging effect. Adding polysaccharides to the composition, compared to combining quercetin and phospholipids alone, significantly enhances the anti-aging efficacy. Detailed Implementation

[0026] Based on the embodiments of this invention, all other embodiments obtained by those skilled in the art without inventive effort are within the scope of protection of this invention. The invention will now be described with reference to specific embodiments. It should be noted that these embodiments are merely descriptive and do not limit the invention in any way.

[0027] The phospholipids used in the embodiments and comparative examples of this invention are all soybean phospholipids, and dextrin (molecular weight distribution of 5500 Da-95000 Da, glucose content of 95%, glycosidic bond of α-1,4 glycosidic bond, manufacturer: Shandong Xiwang Sugar Industry Co., Ltd., batch number: 132310302) Example 1 The composition of the anti-aging composition in this embodiment is as follows: Quercetin and soybean lecithin were mixed at a mass ratio of 1:0.1 to obtain a composition.

[0028] Example 2 The composition of the anti-aging composition in this embodiment is as follows: Quercetin and soybean lecithin were mixed at a mass ratio of 1:0.5 to obtain a composition.

[0029] Example 3 The composition of the anti-aging composition in this embodiment is as follows: Quercetin and soybean lecithin were mixed at a mass ratio of 1:1.5 to obtain a composition.

[0030] Example 4 The composition of the anti-aging composition in this embodiment is as follows: Quercetin and soybean lecithin were mixed at a mass ratio of 1:2 to obtain a composition.

[0031] Example 5 The composition of the anti-aging composition in this embodiment is as follows: Quercetin and soybean lecithin were mixed at a mass ratio of 1:3 to obtain a composition.

[0032] Example 6 The composition of the anti-aging composition in this embodiment is as follows: Quercetin and soybean lecithin were mixed at a mass ratio of 1:5 to obtain a composition.

[0033] Example 7 The composition of the anti-aging composition in this embodiment is as follows: Quercetin, soybean lecithin, and dextrin were mixed in a mass ratio of 1:1.5:1 to obtain a composition.

[0034] Example 8 The composition of the anti-aging composition in this embodiment is as follows: Quercetin, soybean lecithin, and dextrin were mixed in a mass ratio of 1:1.5:5 to obtain a composition.

[0035] Example 9 The composition of the anti-aging composition in this embodiment is as follows: Quercetin, soybean lecithin, and dextrin were mixed in a mass ratio of 1:1.5:10 to obtain a composition.

[0036] Example 10 The composition of the anti-aging composition in this embodiment is as follows: Quercetin, soybean lecithin, and dextrin were mixed in a mass ratio of 1:1.5:30 to obtain a composition.

[0037] Comparative Example 1 The composition in this comparative example contains only quercetin.

[0038] Comparative Example 2 The composition in this comparative example contains only soybean lecithin.

[0039] Comparative Example 3 The composition in this comparative example contains only dextrin.

[0040] Comparative Example 4 The composition in this comparative example contains only quercetin.

[0041] Comparative Example 5 The composition in this comparative example contains only β-nicotinamide mononucleotide (NMN).

[0042] Comparative Example 6 The composition of the comparative example is as follows: Quercetin and soybean lecithin were mixed at a mass ratio of 1:0.05 to obtain a composition.

[0043] Comparative Example 7 The composition of the comparative example is as follows: Quercetin and soybean lecithin were mixed at a mass ratio of 1:6 to obtain a composition.

[0044] Comparative Example 8 The composition of the comparative example is as follows: Quercetin, soybean lecithin, and dextrin were mixed in a mass ratio of 1:1.5:0.5 to obtain a composition.

[0045] Comparative Example 9 The composition of the comparative example is as follows: Quercetin, soybean lecithin, and dextrin were mixed in a mass ratio of 1:1.5:31 to obtain a composition.

[0046] Comparative Example 10 The composition of the comparative example is as follows: Quercetin and soybean lecithin were mixed at a mass ratio of 1:1.5 to obtain a composition.

[0047] Comparative Example 11 The composition of the comparative example is as follows: Quercetin and soybean lecithin were mixed at a mass ratio of 1:3 to obtain a composition.

[0048] Comparative Example 12 The composition of the comparative example is as follows: Quercetin, soybean lecithin, and dextrin were mixed in a mass ratio of 1:1.5:5 to obtain a composition.

[0049] To verify the effectiveness of the anti-aging composition of the present invention, the following experiments were conducted.

[0050] I. Experimental Consumables (1) Materials Test samples: Compositions of the examples and comparative examples, stored at room temperature, protected from light and sealed. Nematode: N2 wild-type Caenorhabditis elegans; Mice: Male SAMP8 mice (rapid aging mice) (4 months old) and male SAMR1 mice (4 months old). Escherichia coli: Uracil-deficient Escherichia coli OP50; Feed and bedding.

[0051] (2) Reagents Cholesterol, peptone, tryptone, yeast extract, sodium hydroxide, sodium hypochlorite solution, anhydrous calcium chloride, anhydrous magnesium sulfate, dipotassium hydrogen phosphate, potassium dihydrogen phosphate, disodium hydrogen phosphate, sodium chloride, ammonium chloride, agar, glycerol, sodium carboxymethyl cellulose.

[0052] (3) Consumables Disposable culture dishes, glass slides, coverslips, scalpel blades, insect pickers, microporous filter membranes, 250, 500, and 1000 mL Erlenmeyer flasks, 1.5, 2, 10, and 50 mL centrifuge tubes, and 200, 1000, and 5000 μL pipette tips, etc.

[0053] (4) Instruments Fluorescence microscopes, stereomicroscopes, clean benches, autoclaves, analytical balances, biochemical incubators, water bath shakers, ultrasonic cleaners, vortex oscillators, centrifuges, open fields, Barnes mazes, mouse treadmills, mouse rotarods, new object recognition activity boxes, gripping devices, etc.

[0054] II. Experimental Methods (a) Nematode Experiment 1. Nematode Culture Methods 1.1 Nematode Culture Hermaphroditic nematodes were cultured on nematode growth medium (NGM) coated with Escherichia coli OP50 at 20°C. The growth of the nematodes was observed, and the nematodes were periodically transferred to new NGM medium coated with OP50.

[0055] 1.2 Nematode Synchronization Select plates with a good growth status and a large number of nematodes in the oviposition stage. Wash the nematodes off the culture medium with M9 buffer and collect them in centrifuge tubes. Centrifuge at 10,000 r / min for 90 s and discard the supernatant. Add 1 mL of prepared nematode lysis buffer, vortex, and stop vortexing when the nematodes are fully lysed and a large number of eggs are observed in the centrifuge tube. Centrifuge at 10,000 r / min for 90 s and discard the supernatant. Repeat this process 3 times to wash away the lysis buffer in the centrifuge tube. Finally, place the eggs on blank NGM plates and incubate them in a constant temperature incubator at 20℃ for 16 h. Transfer them to NGM plates coated with OP50 and wait for them to grow to the L4 stage for subsequent experiments.

[0056] 2. Methods for detecting nematode lifespan The synchronized L4 stage nematodes were transferred to NGM plates containing 0.02 mg / mL of each sample (the compositions of the examples and comparative examples) and 5-FU (to prevent nematode oviposition) and cultured for 5 days, changing the plates 1-2 times during the period. On the 6th day, nematodes were picked and transferred to plates without 5-FU. 50 nematodes were picked from each plate. The nematodes were transferred to a new plate every 2-3 days. The number of nematode deaths and losses was recorded daily. After the experiment, the average lifespan and average lifespan extension rate of the nematodes were calculated.

[0057] The results of the nematode lifespan test are shown in Table 1.

[0058] Table 1

[0059] As can be seen from Table 1, the composition of the present invention can significantly prolong the lifespan of nematodes compared to using marigoldin, soybean lecithin, quercetin, etc. alone. In particular, compared to the composition formed by marigoldin and phospholipids, the composition formed by marigoldin, phospholipids, and polysaccharides has a significant life-prolonging effect on nematodes.

[0060] (ii) Mouse experiment Animal grouping: Experimental animals were observed for 5 days under a maintenance diet within the barrier system. Mice were randomly divided into 24 groups according to body weight: blank control group (SAMR1 control group), model control group (SAMP8 control group), Example 1-10 groups, and Comparative Example 1-12 groups, with 15 mice in each group. The Example and Comparative Example groups were given 50 mg / kg bw of each composition, while the blank control group and model control group were given the same amount of the corresponding solvent. The administration was carried out continuously for 3 months, and behavioral indicators were detected.

[0061] 1. Effects on the motor function of mice (1) Treadmill Experiment To assess treadmill performance, mice were acclimatized to a 5° inclined electric treadmill over three days, with 5 minutes of training each day. On the test day, mice ran on the treadmill at an initial speed of 5 m / min for 2 minutes, then increased the speed by 2 m every 2 minutes until exhaustion. The time it took for the mice to fall was recorded, and the average of the three test results was taken.

[0062] (2) Tensile test Place the mouse's two forelimbs on the lever of the force meter, keep the mouse's body horizontal with the table, and slowly and evenly pull the mouse backward until the two forelimbs leave the lever of the force meter. Repeat the recording three times and take the maximum value for statistical calculation.

[0063] (3) Rotating bar experiment Two days prior to the test, mice were trained at a rotation speed of 4-20 rpm, maintaining the maximum speed for 60 seconds. Each mouse was trained three times daily, and baseline values ​​were recorded on day 7. During the test, each mouse was tested three times, and the longest dwell time was recorded. The test was terminated when the mouse's dwell time exceeded 60 seconds, and 60 seconds was taken as the final score. The dwell time of the mice on the horizontal rotating bar was statistically analyzed.

[0064] (4) Pole climbing experiment Gently place the mouse head-down on the top of the bar, which is placed vertically on the table. Record the time it takes for the mouse to descend from the top of the bar to the bottom of the platform. Train the animals twice daily for three consecutive days, stopping the test if the mouse remained in the position for more than 15 seconds. Repeat the experiment three times, recording the average time for each mouse to descend to the bottom of the platform.

[0065] The results of the effects on the motor function of rapidly aging mice are shown in Table 2.

[0066] Table 2

[0067] Note: Different letters indicate significant differences between groups (P < 0.05).

[0068] As shown in Table 2, the composition of the present invention has a significant effect on delaying or restoring the motor function of rapidly aging mice. In particular, compared with NMN used in Comparative Example 5, the composition of the present invention has a more significant anti-aging effect. By adding polysaccharides to the composition, the anti-aging effect of the composition is further enhanced. Specifically, the compositions used in Examples 7-10, which consist of quercetin, phospholipids, and polysaccharides, showed significant differences in time spent on treadmills, tumbling bars, and pole climbing compared to other examples and comparative examples.

[0069] 2. Effects on cognitive abilities in mice (1) Open field experiment The open field measured 50×50×60 cm. It was divided into two areas: a central area measuring 25×25 cm and an outer edge area. During the experiment, mice were placed along the boundaries into corners of the open field, and video recording began simultaneously. Mice were allowed to explore freely for 6 minutes. The collected videos were analyzed using EthoVision XT 8.0, recording the number of times mice entered the central area and the duration of their stay there.

[0070] (2) Identification of new things The experiment consisted of three phases. In the first phase (adaptation period), mice were placed in an empty box for 6 minutes to acclimatize. In the second phase (training period), two identical objects (denoted as A and A') were placed parallel to each other, and the mice were placed in the box to explore for 5 minutes. One hour later, in the third phase (testing period), one of the objects (A') was replaced with a new object B, in the same position, and the mice were placed in the box to explore for another 5 minutes. The mice's movement speed, distance traveled, and contact time with each object were recorded. The experimental results were expressed as the discrimination index (DI). .

[0071] (3) Barnes Maze Animals were trained continuously for 4 days, 4 times a day. During the testing period (Day 5), the target box was removed, and the mice were placed in the activation box in the center of the maze. After 15 seconds of noise stimulation, the activation box was removed, and the mice were allowed to explore freely for 90 seconds. The time the mice spent in the quadrant containing the target hole was measured.

[0072] The results of the effects on cognitive abilities in rapidly aging mice are shown in Table 3.

[0073] Table 3

[0074] Note: Different letters indicate significant differences between groups (P < 0.05).

[0075] As shown in Table 3, the mice administered the compositions in the examples exhibited significantly improved cognitive abilities compared to mice administered other components. In particular, the compositions in Examples 7-10, consisting of quercetin, phospholipids, and polysaccharides, showed significant differences in open field test, novelty discrimination index, and target quadrant dwell time compared to other examples and comparative examples.

[0076] In summary, the composition of the present invention can effectively prolong the lifespan of nematodes, significantly delay or restore the motor function of rapidly aging mice, and significantly improve the cognitive ability of rapidly aging mice, indicating that the composition of the present invention has significant anti-aging effects.

[0077] Finally, it should be noted that the above embodiments are only used to illustrate the technical solutions of the present invention, and not to limit them; although the present invention has been described in detail with reference to the foregoing embodiments, those skilled in the art should understand that modifications can still be made to the technical solutions described in the foregoing embodiments, or equivalent substitutions can be made to some of the technical features; and these modifications or substitutions do not cause the essence of the corresponding technical solutions to deviate from the spirit and scope of the technical solutions of the embodiments of the present invention.

Claims

1. An anti-aging composition characterized in that, Its active ingredients include quercetin and phospholipids, wherein the mass ratio of quercetin to phospholipids is 1:(0.1~5).

2. The composition of claim 1, wherein, The mass ratio of the quercetin to the phospholipid is 1:(0.5~2).

3. The composition according to claim 1, characterized in that, The phospholipids include at least one of plant phospholipids or animal phospholipids, preferably plant phospholipids, and more preferably soybean phospholipids.

4. The composition of any one of claim 1, wherein, Its active ingredients also include polysaccharides.

5. The composition of claim 4, wherein, The monosaccharide composition of the polysaccharide contains a glucose content of not less than 80%, preferably not less than 95%. And / or, the weight-average molecular weight of the polysaccharide is not less than 5000 Da, preferably 5000 Da-100000 Da.

6. The composition according to claim 4 or 5, wherein The polysaccharide has a 1,4 glycosidic bond, preferably an α-1,4 glycosidic bond.

7. The composition of claim 4, wherein The active ingredient is composed of the quercetin, the phospholipid, and the polysaccharide in a mass ratio of 1:(0.1~5):(1~30).

8. The composition of claim 7, wherein, The mass ratio of the quercetin, the phospholipid, and the polysaccharide is 1:(0.5~2):(1~10).

9. The use of the anti-aging composition according to any one of claims 1-8 in the preparation of food, pharmaceuticals, cosmetics, and feed; preferably in the preparation of food, pharmaceuticals, health products, cosmetics, and feed with anti-aging effects.

10. A pharmaceutical preparation, characterized in that, Contains the anti-aging composition according to any one of claims 1-8; Preferably, the dosage form of the pharmaceutical preparation includes injections, tablets, granules, or capsules.

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