Use of pyroglutamic acid in the preparation of muscle building products
By using pyroglutamic acid to prepare muscle-building products, the problem of muscle enhancement in the elderly and critically ill patients has been solved, achieving safe and effective muscle growth and functional improvement, and is suitable for the preparation of muscle-building products.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- SOUTH CHINA AGRICULTURAL UNIVERSITY
- Filing Date
- 2026-04-29
- Publication Date
- 2026-07-21
AI Technical Summary
There is a lack of safe and effective muscle-building products in the current technology, especially for solutions for the elderly and seriously ill patients who have difficulty strengthening their muscles through exercise training.
Using pyroglutamic acid as the sole active ingredient, muscle-building products are prepared, including oral liquids, powders, tablets, capsules, and other dosage forms, containing 0.1~0.3wt% pyroglutamic acid, which promotes skeletal muscle growth and development and improves function.
Pyroglutamic acid significantly increases muscle mass and motor function in mice, promotes muscle fiber cross-sectional area and protein deposition, and expresses related genes and proteins, thus achieving a muscle-building effect.
Smart Images
Figure CN122097351B_ABST
Abstract
Description
Technical Field
[0001] This invention relates to the field of biotechnology, and in particular to the application of pyroglutamic acid in the preparation of muscle-building products. Background Technology
[0002] Skeletal muscle accounts for 30% to 40% of body weight and is crucial for maintaining key physiological functions such as contractile ability, mobility, survival rate, morbidity, and quality of life. Skeletal muscle atrophy is a significant complication of skeletal muscle, characterized by an imbalance between protein synthesis and degradation mechanisms. Its causes involve a variety of clinical complications, including sarcopenia, prolonged bed rest, muscle disuse, denervation, and cachexia, all of which severely impact an individual's quality of life. The prevalence of sarcopenia is extremely high in people aged 60 and older, and this number is expected to increase further with the increasing aging of the global population. Sarcopenia significantly increases the risk of falls, weakness, disability, and subsequent hospitalization, and is significantly associated with prolonged hospital stays, increased risk of postoperative complications, and even premature death, placing a huge burden on patients, families, and society. Furthermore, with the increasing aging of the population, sarcopenia will become a major health problem for the elderly. Simultaneously, the demand for safe and effective muscle-building products among athletes and fitness enthusiasts continues to grow.
[0003] Exercise therapy has been proven to effectively increase muscle mass and function. However, older adults and seriously ill patients often find it difficult to engage in exercise training, thus necessitating the development of alternative exercise therapies to combat muscle failure. In recent years, technologies such as natural products, tissue engineering, cell therapy, nanocarrier delivery, and extracellular vesicles have been developed to regulate protein synthesis and degradation and promote muscle regeneration. Natural products and human dietary components, due to their diverse structures and functions and limited side effects on the human body, have been ideal sources for addressing various diseases and physical discomforts for centuries. Numerous natural compounds have been developed into standard drugs and drug design models for treating diseases. Natural products originate from a variety of sources, including plants, microorganisms, animals, insects, minerals, and marine organisms. Based on their source, natural products can be divided into unmodified natural products and natural product derivatives. Natural products possess complex structures and chemical properties, playing a crucial role in drug development. They have become important lead compounds and potential resources in current and future drug development. Studies have found that many natural products can improve skeletal muscle atrophy. For example, quercetin inhibits skeletal muscle atrophy by suppressing the activity of atrogin-1, a key ubiquitin ligase involved in muscle atrophy. Resveratrol regulates mitochondrial quality, reduces muscle atrophy, and improves muscle function in diabetic mice by decreasing MuRF1 expression and caspase-3 levels in skeletal muscle. Furthermore, various natural products have been found to combat skeletal muscle atrophy by regulating myocytokines. These natural products hold promise for development as dietary supplements, adjunctive therapies, or drugs, possessing broad market potential and significant social implications.
[0004] Pyroglutamic acid, also known as 5-oxoproline, is a naturally occurring amino acid derivative widely found in animals and plants. Pyroglutamic acid has various physiological functions, such as hormone synthesis, neuroprotection, anti-tumor activity, anti-diabetic effects, improvement of gut health, and inflammation relief; however, its application in muscle building has not yet been reported.
[0005] Therefore, the technical problem to be solved in this case is: how to develop a new and safe muscle-building product, especially a muscle-building agent. Summary of the Invention
[0006] The purpose of this invention is to provide the application of pyroglutamic acid in the preparation of muscle-building products, and products containing pyroglutamic acid. This invention discloses a novel use of pyroglutamic acid in the preparation of muscle-building products, and it is a naturally occurring amino acid derivative widely found in animals and plants, exhibiting good biocompatibility.
[0007] To achieve the above objectives, the present invention provides the following technical solution:
[0008] Application of pyroglutamic acid as the sole active ingredient in muscle-building products.
[0009] Preferably, the product is used to promote skeletal muscle growth and / or improve skeletal muscle function, and / or promote the expression of genes and proteins related to protein deposition in skeletal muscle.
[0010] Preferably, the pyroglutamic acid further includes pharmaceutically acceptable excipients.
[0011] Preferably, the dosage form of the muscle-building product is an oral liquid, powder, tablet, or capsule.
[0012] Preferably, the product contains 0.1 to 0.3 wt% pyroglutamic acid.
[0013] Finally, this invention discloses a muscle-building product containing 0.1~0.3wt% pyroglutamic acid.
[0014] Compared with the prior art, the beneficial effects of the present invention are:
[0015] This invention discovers a novel use for pyroglutamic acid. Animal experiments show that supplementing drinking water with pyroglutamic acid at a 0.2% concentration for 15 weeks significantly increases the weight of the gastrocnemius, tibialis anterior, and soleus muscles in normally fed mice, increases the cross-sectional area of muscle fibers, and improves motor function, indicating that pyroglutamic acid can promote skeletal muscle growth and development and improve skeletal muscle function. Gene and protein level analysis reveals that pyroglutamic acid can promote the expression of genes and proteins related to protein deposition in the tibialis anterior muscle, thereby achieving muscle growth. Attached Figure Description
[0016] Figure 1 The effect of pyroglutamic acid on the weight-lifting ability of mice;
[0017] Figure 2 The effect of pyroglutamic acid on explosive power in mice;
[0018] Figure 3 The effect of pyroglutamic acid on running ability in mice;
[0019] Figure 4 The effect of pyroglutamic acid on mouse body weight;
[0020] Figure 5 The effect of pyroglutamic acid on the quality of mouse muscle tissue;
[0021] Figure 6 The effect of pyroglutamic acid on the cross-sectional area of muscle fibers in the tibialis anterior muscle tissue of mice;
[0022] Figure 7 The effect of pyroglutamate on the mRNA levels of Myhc, Murf1, and Mafbx in mice;
[0023] Figure 8 The effect of pyroglutamate on the protein level of MYHC in mice;
[0024] Figure 9 This is a schematic diagram of the γ-glutamyl cycle. Detailed Implementation
[0025] The technical solution of the present invention will be clearly and completely described below with reference to the embodiments of the present invention. Obviously, the described embodiments are only a part of the embodiments of the present invention, and not all of the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by those of ordinary skill in the art without creative effort are within the scope of protection of the present invention. It should be noted that, where specific conditions are not specified in the embodiments, conventional conditions or conditions recommended by the manufacturer shall be followed. Reagents or instruments whose manufacturers are not specified are all conventional products that can be purchased commercially. Unless otherwise specified, all parts used in the embodiments of the present invention are parts by weight, and % are weight percentages.
[0026] Example 1
[0027] Sixteen 3-week-old male C57BL / 6J mice were housed under specific conditions (ambient temperature 22±2℃, relative humidity 40~70%, 12h~12h light-dark cycle).
[0028] At the start of the experiment, mice were randomly divided into a control group and a pyroglutamic acid treatment group, with eight mice in each group. Both groups were fed a standard diet, while the pyroglutamic acid treatment group received 0.2 wt% pyroglutamic acid in their drinking water. The experiment lasted for 15 weeks, during which all mice had free access to food and water, and their weight was recorded weekly.
[0029] After 10 weeks of feeding, the mice underwent a weightlifting assessment. The mice were grasped by their tails, and their limbs were used to grip weights (from light to heavy) and slowly lifted until suspended in the air. Suspension for 3 seconds was considered a passing score; if successful, the next weight was used. If unsuccessful, the mice rested for 10 seconds and were tested again. The test continued for 3 attempts, and if successful within 3 attempts, the next weight was used; otherwise, the test ended. The weights used were 26, 33, 44, 63, 82, 100, and 120 g, representing scores of 1, 2, 3, 4, 5, 6, and 7, respectively. The final score was the cumulative score.
[0030] Weightlifting scoring test results as follows Figure 1 As shown, compared with the control group, the mice in the pyroglutamic acid treatment group had a higher cumulative lifting score, indicating that pyroglutamic acid can enhance the lifting ability of mice.
[0031] After 11 weeks of feeding, the mice underwent a claw strength test. The mice were placed on a metal grid of a claw strength testing instrument, with their limbs gripping the designated areas. The mice were then gently pulled by their tails until they were off the grid, with the pulling force and direction consistently consistent. The instrument readings were recorded. All mice were tested 10 times. The maximum and minimum values were discarded, and the average of the remaining 8 measurements was taken as the final claw strength result for each mouse.
[0032] Claw gripping force test results are as follows Figure 2 As shown, compared with the control group, the mice in the pyroglutamic acid treatment group had enhanced claw gripping ability, indicating that pyroglutamic acid can enhance the explosive power of mice.
[0033] After 14 weeks of feeding, the mice were subjected to a treadmill test. Three days before the formal running test, the mice were placed on the treadmill for 30 minutes of acclimatization training (10 m / min). Formal test conditions: initial speed of 11 m / min, increasing by 4 m / min every 5 minutes until the mice were exhausted; incline of 10°; and exhaustion was defined as the mouse remaining on the electric shock bar of the treadmill for 5 seconds.
[0034] Running test results as follows Figure 3 As shown in the figure, compared with the control group, the mice in the pyroglutamic acid treatment group had a longer running time and running distance, indicating that pyroglutamic acid can increase the running time and running distance of mice.
[0035] The mouse body weight change curve during the experimental period is as follows: Figure 4 As shown, pyroglutamic acid does not affect the normal growth of mice.
[0036] Example 2
[0037] Mice fed for 15 weeks were fasted for 12 hours and then euthanized by cervical dislocation. The gastrocnemius, tibialis anterior, extensor digitorum longus, and soleus muscles were harvested, weighed, and statistically analyzed.
[0038] result Figure 5 As shown, pyroglutamic acid can significantly improve the quality of the gastrocnemius, tibialis anterior, and soleus muscles in mice.
[0039] The obtained mouse tibialis anterior muscle was fixed with formalin, then removed and subjected to dehydration, embedding, sectioning, drying, dewaxing, and hematoxylin-eosin (H&E) staining to prepare pathological sections. The sections were observed under a 10x microscope and photographed. The cross-sectional area of the muscle fibers in the H&E-stained tibialis anterior muscle was analyzed using ImageJ software (National Institute of Health, Bethesda, MD, USA).
[0040] The results are as follows Figure 6 As shown, Figure 6 This indicates that pyroglutamic acid treatment can significantly increase the cross-sectional area of muscle fibers in the tibialis anterior muscle of mice.
[0041] Example 3
[0042] The tibialis anterior muscle of mice was harvested, and the expression of genes and proteins related to protein synthesis and degradation in the tibialis anterior muscle was measured.
[0043] Total RNA was extracted from the tibialis anterior muscle using the Trizol method. Extraction was performed with chloroform, and the supernatant was precipitated with an equal volume of isopropanol. The precipitate was then washed with 75% ethanol, and the RNA precipitate was dissolved in DEPC water for subsequent experiments. Reverse transcription was performed using a cDNA kit. A qPCR premix kit was used to prepare the reaction system, and GAPDH was used as an internal control to quantify mRNA levels. Results are as follows: Figure 7 As shown, the results revealed that the Myhc mRNA level in the pyroglutamate group was significantly higher than that in the control group, while the Murf1 and Mafbx mRNA levels did not change significantly, indicating that pyroglutamate can promote muscle protein deposition, thereby achieving muscle growth.
[0044] Total protein was extracted from the tibialis anterior muscle using RIPA lysis buffer containing PMSF, and the protein concentration was adjusted to 1 μg / μL. The protein was denatured by heating at 95℃ for 5 min. SDS-PAGE 10% separating gel and 5% stacking gel were prepared, and protein samples and markers were added. Electrophoresis was performed at 90V for 90 min. A PVDF membrane was activated with methanol, and electrotransfer was performed at 180 MA for 75 min using the "wet transfer method." The PVDF membrane was then removed, blocked with rapid blocking buffer for 15 min, incubated overnight at 4℃ with primary antibody (1:1000), washed with TBST, and incubated at room temperature with secondary antibody (1:50000) for 1 h, followed by TBST washing. ECL chemiluminescence solution was added, and imaging was performed under a developing instrument. Results are as follows: Figure 8 As shown, the results indicate that the MYHC protein level in the pyroglutamic acid group was significantly higher than that in the control group.
[0045] Safety of pyroglutamic acid
[0046] L-pyroglutamic acid is a naturally occurring amino acid derivative found in animals and plants. The human body can process this substance through normal metabolism. L-pyroglutamic acid participates in various physiological processes, including neurotransmitter synthesis, protein metabolism, and energy metabolism (its involvement in metabolic processes can be found in [reference needed]). Figure 9 (The diagram shows a schematic of the γ-glutamyl cycle). It is widely used in the food, pharmaceutical, and cosmetic industries. Existing research and animal experiments of this invention have demonstrated that this amino acid has good safety.
[0047] In summary, the analysis shows that pyroglutamic acid can effectively enhance the motor ability of mice; pyroglutamic acid can significantly increase the mass of the gastrocnemius, tibialis anterior, and soleus muscles of mice; pyroglutamic acid can significantly increase the cross-sectional area of muscle fibers in the tibialis anterior muscle of mice; and pyroglutamic acid can promote the expression of genes and proteins related to protein deposition in the tibialis anterior muscle.
[0048] It will be apparent to those skilled in the art that the present invention is not limited to the details of the exemplary embodiments described above, and that the invention can be implemented in other specific forms without departing from the spirit or essential characteristics of the invention. Therefore, the embodiments should be considered in all respects as exemplary and non-limiting, and the scope of the invention is defined by the appended claims rather than the foregoing description. Thus, it is intended that all variations falling within the meaning and scope of equivalents of the claims be included within the present invention.
Claims
1. An application of using pyroglutamic acid as the sole active ingredient in muscle-building products, characterized in that, The product is used to promote skeletal muscle growth and / or improve skeletal muscle function, and / or promote the expression of skeletal muscle-related growth genes and proteins.
2. The application according to claim 1, characterized in that, The pyroglutamic acid also includes pharmaceutically acceptable excipients.
3. The application according to claim 1, characterized in that, The dosage forms of the muscle-building products are oral liquids, powders, tablets, and capsules.
4. The application according to claim 1, characterized in that, The product contains 0.1-0.3 wt% pyroglutamic acid.