Application of Five Grain Insect Oil in the Preparation of Preventive and / or Therapeutic Treatments of Neurodegenerative Diseases
By using supercritical CO2 extraction, various dosage forms of five-grain insect oil products were prepared, solving the problem of limited efficacy of existing drugs and achieving effective protection against neurodegenerative diseases and improvement of cognitive function.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- JINHUA HERUI LIFE HEALTH TECHNOLOGY CO LTD
- Filing Date
- 2026-05-29
- Publication Date
- 2026-06-30
AI Technical Summary
Existing drugs for treating neurodegenerative diseases have limited efficacy, significant adverse reactions, cannot reverse neuronal damage, and long-term use can burden the liver and kidneys with metabolic stress, thus failing to effectively block disease progression.
Using five-grain insect oil as the active ingredient, it is prepared by supercritical CO2 extraction and is rich in various neuroprotective active ingredients such as EPA and nervonic acid. It can be used to prepare drugs, foods and health products in various dosage forms to exert neuroprotective effects through multiple pathways.
Five-grain insect oil significantly protects neurons, inhibits β-amyloid protein deposition, reduces neuronal apoptosis, improves learning and memory abilities, and provides multiple neuroprotective effects. It is suitable for long-term use and has a high safety profile.
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Abstract
Description
Technical Field
[0001] This invention relates to the field of biomedicine, specifically to the application of five-grain insect oil in the preparation of prevention and / or treatment of neurodegenerative diseases. Background Technology
[0002] With the increasing aging of the global population, the incidence of neurodegenerative diseases continues to rise, becoming a serious public health problem. Alzheimer's disease (AD) and Parkinson's disease (PD) are the two most common neurodegenerative diseases in clinical practice. The core pathological manifestations are the progressive degeneration and loss of neurons in specific brain regions and functional decline, which ultimately leads to cognitive impairment or motor dysfunction, seriously affecting the quality of life of patients and increasing the social burden.
[0003] Currently, clinical treatments for this type of disease primarily focus on symptomatic relief, with representative drugs including cholinesterase inhibitors and NMDA receptor antagonists. However, existing drugs generally suffer from significant drawbacks such as limited efficacy, marked adverse reactions, and the inability to reverse neuronal damage or slow disease progression, making it difficult to meet long-term clinical needs.
[0004] The pathogenesis of neurodegenerative diseases is extremely complex, involving the interaction of multiple pathological pathways, including abnormal deposition of β-amyloid protein, hyperphosphorylation of Tau protein, damage to dopaminergic neurons, neuroinflammation, oxidative stress, and neuronal apoptosis. Current clinical treatments mostly target single points and cannot halt disease progression; furthermore, long-term use carries metabolic burdens on the liver and kidneys, as well as safety risks.
[0005] Insect-derived bioactive substances have shown great development potential in the fields of neuroprotection and pharmaceuticals in recent years due to their unique advantages, such as rich biodiversity, readily available raw materials, and high content of polyunsaturated fatty acids and various neuroactive components. As a traditional Chinese medicine, the oil of *Polygonum multiflorum* (a type of insect) is rich in unsaturated fatty acids, EPA, nervonic acid, and other neuroprotective active ingredients. However, to date, the medicinal value of *Polygonum multiflorum* oil in the fields of nervous system protection and prevention and treatment of neurodegenerative diseases has not been reported. Summary of the Invention
[0006] In view of this, the present invention provides the application of five-grain insect oil in the preparation of prevention and / or treatment of neurodegenerative diseases, revealing that five-grain insect oil has significant neuroprotective activity, can effectively combat neuronal damage, improve learning and memory ability, and provides a natural drug source for the prevention and treatment of neurodegenerative diseases.
[0007] The technical solution provided by this invention is as follows: In a first aspect, the present invention provides the use of five-grain insect oil in the preparation of products for the prevention and / or treatment of neurodegenerative diseases.
[0008] Furthermore, the neurodegenerative diseases include Alzheimer's disease or Parkinson's disease.
[0009] Secondly, the present invention provides the use of five-grain insect oil in the preparation of products for neuroprotection, delaying neuroaging and / or improving cognitive function.
[0010] Furthermore, the improvement in cognitive function includes improved spatial learning and / or memory abilities.
[0011] Furthermore, the products include food, health products, or medicines.
[0012] Thirdly, this invention provides the application of five-grain insect oil in the preparation of Aβ aggregation inhibitors.
[0013] Furthermore, the five-grain insect oil contains 2.16g / 100g of EPA, 0.0104g / 100g of nervonic acid, and a total of 49.1g / 100g of unsaturated fatty acids.
[0014] Furthermore, the grain insect oil is an oily component obtained by extracting dried larvae of grain insects; in a specific embodiment of the present invention, the grain insect oil can be prepared by supercritical CO2 extraction, and it has a high total content of unsaturated fatty acids.
[0015] Fourthly, the present invention provides a pharmaceutical preparation for the prevention and / or treatment of neurodegenerative diseases, comprising the five grain insect oil described in any of the preceding claims and a pharmaceutically acceptable carrier.
[0016] Furthermore, the dosage forms include tablets, pills, granules, capsules, injections, oral liquids, suspensions, or emulsions.
[0017] The beneficial effects of this invention are as follows: This invention discloses the use of *Pseudolarix amabilis* oil in the preparation of drugs for the prevention and / or treatment of neurodegenerative diseases, providing a natural drug option for the prevention and treatment of neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease. *Pseudolarix amabilis* oil exerts neuroprotective effects through multiple pathways, including inhibiting β-amyloid protein deposition, reducing neuronal apoptosis, alleviating neuroinflammation, and protecting dopaminergic neurons, thus blocking the progression of neurodegenerative diseases from multiple pathways with significant and stable effects. Cell experiments have confirmed that *Pseudolarix amabilis* oil can significantly protect HT22 cells from glutamate-induced excitatory toxicity damage and effectively counteract oxidative stress-mediated neuronal apoptosis. Animal experiments further show that *Pseudolarix amabilis* oil can significantly improve spatial learning and memory abilities in Aβ-induced Alzheimer's disease model rats and alleviate cognitive decline. *Pseudolarix amabilis* oil is derived from the traditional Chinese medicinal herb *Pseudolarix amabilis* and is prepared using supercritical CO2 extraction, leaving no organic solvent residues. It is naturally safe and suitable for long-term use by patients. Furthermore, appropriate dosage forms can be selected according to different needs, providing good clinical application flexibility and patient compliance. The five-grain insect oil of the present invention has significant protective and repairing effects on nerve damage. It can be used for early prevention of diseases, as well as for disease intervention and rehabilitation assistance, and has multiple values of prevention, improvement and adjuvant treatment. Detailed Implementation
[0018] To make the objectives, technical solutions, and advantages of this invention clearer, the technical solutions of this invention will be clearly and completely described below in conjunction with the embodiments of this invention. Obviously, the described embodiments are only a part of the embodiments of this invention, not all of them. Based on the embodiments of this invention, all other embodiments obtained by those skilled in the art without creative effort are within the scope of protection of this invention. Experimental methods in the following embodiments that do not specify specific conditions are generally performed under conventional conditions or as recommended by the manufacturer. Unless otherwise stated, percentages and parts are weight percentages and parts by weight.
[0019] Unless otherwise specified, the technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this application pertains. It should be noted that the terms used herein are for the purpose of describing particular embodiments only and are not intended to limit the exemplary embodiments of this application.
[0020] Preparation Example A method for preparing five-grain insect oil includes the following steps: After the dried grain insects were crushed and passed through a 40-mesh sieve, the crushed insects were placed in a supercritical extraction vessel. The extraction pressure was set to 25 MPa, the extraction temperature to 43℃, and the CO2 flow rate to 20 L / h. The extraction was carried out for 3 hours, and the extract was collected to obtain crude oil from the grain insects. According to the test results from PONY Testing Group (report number: B1G205033B1F10I3053), the total amount of unsaturated fatty acids in Wugu Worm Oil is 49.1g / 100g, of which the content of EPA is 2.16g / 100g and the content of nervonic acid is 0.0104g / 100g.
[0021] Example 1: Preparation of tablets A grain insect oil tablet for the prevention and / or treatment of neurodegenerative diseases, composed of 40% grain insect oil, 30% microcrystalline cellulose, 20% sodium carboxymethyl starch, 5% silicon dioxide, and 5% magnesium stearate.
[0022] A method for preparing a grain insect oil tablet for the prevention and / or treatment of neurodegenerative diseases includes the following steps: (1) Place the five grain insect oil, microcrystalline cellulose, and sodium carboxymethyl starch in a mixer and stir for 15 minutes until uniform, so that the liquid oil is fully absorbed by the excipients to form a powdery mixture with good flowability; (2) Add an appropriate amount of starch paste to the powder mixture as a binder, stir to form a soft material, and granulate it through a 20-mesh sieve; (3) Dry the wet granules at 50℃ for 30 minutes, controlling the moisture content to 3%~5%, and then granulate them through a 20-mesh sieve after drying; (4) Add silica and magnesium stearate to the dry granules, mix for 10 minutes, and compress into tablets using a rotary tablet press.
[0023] Example 2: Preparation of Capsules A capsule formulation of five-grain insect oil for the prevention and / or treatment of neurodegenerative diseases, composed of 60% five-grain insect oil, 20% vitamin E, and 20% polyethylene glycol 400.
[0024] A method for preparing a grain insect oil capsule for the prevention and / or treatment of neurodegenerative diseases includes the following steps: (1) Mix the five grain insect oil, vitamin E and polyethylene glycol 400 evenly by high-speed shearing to obtain the contents; (2) Add the contents to a soft capsule press and press them into soft capsules; (3) After pressing, the soft capsules are shaped in a rotating drum for 30 minutes, and then placed in a drying tray to dry for 24-48 hours at 25-30℃ and 30%-40% relative humidity. (4) Clean the oil stains on the surface of the dried soft capsules with 95% ethanol, and pick out the defective products such as irregularly shaped capsules and oil-leaking capsules.
[0025] Example 3: Preparation of Emulsion An emulsion of barnyard grass oil for the prevention and / or treatment of neurodegenerative diseases, comprising 20% barnyard grass oil, 5% gum arabic, 3% glycerin, 2% steviol glycosides, 2% potassium sorbate and purified water (balance).
[0026] A method for preparing a grain insect oil emulsion for the prevention and / or treatment of neurodegenerative diseases, comprising the following steps: (1) Take the five grain insect oil, heat it in a water bath to 60-70℃, and set aside; take gum arabic, glycerin, steviol glycosides, potassium sorbate, add purified water, stir to dissolve, and heat to 60-70℃; (2) Under the stirring of a high-speed shear emulsifier, the oil phase is slowly added to the water phase and stirring is continued for 5-10 minutes to form a uniform primary emulsion; (3) Homogenize the colostrum 3-5 times with a high pressure homogenizer at 80-100MPa until the emulsion is fine and uniform; (4) The homogenized emulsion is diluted with purified water, mixed well, filled into a brown glass bottle, and sealed to obtain the final product.
[0027] Experimental Example 1: Protective effect of Five Grains Insect Oil on Glutamate-Induced HT22 Cells Hippocampal neurons from HT22 mice in the logarithmic growth phase were harvested at a concentration of 1 × 10⁻⁶ cells per well. 4 Cells were seeded at a density of [number] cells / well in 96-well plates and cultured for 24 hours to allow cell adhesion. The experiment included a blank control group (routine cell culture), a control group (HT22 cells without glutamate induction), a model group (treated with 5 mM sodium glutamate to induce damage), and a treatment group treated with *Polygonum multiflorum* oil (treated with 5 mM sodium glutamate and *Polygonum multiflorum* oil at concentrations of 12.5, 25, 50, and 100 μg / mL, respectively). Each group had six replicates. After culturing for another 24 hours, 10 μL of CCK-8 solution was added to each well, and the cells were incubated at 37°C in a 5% CO2 incubator for 2 hours. The absorbance (OD value) at 490 nm was measured using a microplate reader, and cell viability was calculated.
[0028] Cell viability (%) = (OD value of experimental group - OD value of blank group) / (OD value of control group - OD value of blank group) × 100%.
[0029] Table 1. HT22 cell survival rate
[0030] Table 1 shows that the cell survival rate in the model group was significantly lower than that in the control group, indicating that the glutamate-induced neuronal cell injury model was successfully established. Compared with the model group, the cell survival rate of different concentrations of *Polygonum multiflorum* oil treatment groups was improved, and the cell survival rate increased in a dose-dependent manner with increasing *Polygonum multiflorum* oil concentration. The cell survival rate of the high-concentration treatment group was close to that of the control group. These results indicate that *Polygonum multiflorum* oil has a significant protective effect against glutamate-induced HT22 cell injury, effectively combating oxidative stress-mediated neuronal apoptosis and exerting neuroprotective effects.
[0031] Experimental Example 2 Healthy adult SD rats were acclimatized for 7 days. Aβ... 25-35 The lyophilized powder was mixed with hexafluoroisopropanol at a ratio of 200 μL per mg of peptide, and the mixture was allowed to stand at room temperature for 2 hours under ice bath conditions to ensure complete dissolution. The solution was then transferred to ice and cooled for 10 minutes, followed by overnight evaporation in a fume hood. The next day, aeration was continued for 1 hour to completely remove residual solvent, resulting in a thin film precipitate at the bottom of the tube. An appropriate amount of DMSO was added to the precipitate, and the mixture was diluted with phenol red-free DMEM / F12 medium and incubated at 4°C for 24 hours to promote Aβ oligomer formation. Subsequently, the mixture was centrifuged at 10,000 rpm for 10 minutes at 4°C. The supernatant was collected, aliquoted, and stored at -10°C to obtain the oligomeric Aβ25-35 solution. Its aggregation state was assessed before use.
[0032] After anesthetizing rats via intraperitoneal injection, they were fixed on a stereotaxic instrument. The coordinates of the bilateral CA1 region of the hippocampus were determined using a rat stereotaxic atlas (3.0 mm posterior to the anterior fontanelle, 2.0 mm lateral to the midline suture, and 2.9 mm subdural depth). Following skull drilling, 5 μL of the prepared Aβ25-35 oligomer solution was slowly injected over 5 minutes using a microsyringe. The needle was retained for 30 minutes to ensure adequate diffusion. The needle was then slowly withdrawn, and the contralateral side was injected using the same method. The wound was sutured, and routine anti-infection treatment was administered, thus completing the establishment of the AD model in rats.
[0033] After successful establishment of the AD model, rats were randomly divided into four groups: a blank control group (healthy SD rats, given saline), a model group (given saline), a low-dose group of *Polygonum multiflorum* oil (250 mg / kg of *Polygonum multiflorum* oil daily by gavage), a medium-dose group of *Polygonum multiflorum* oil (500 mg / kg of *Polygonum multiflorum* oil daily by gavage), and a high-dose group of *Polygonum multiflorum* oil (1000 mg / kg of *Polygonum multiflorum* oil daily by gavage), with 10 rats in each group. All groups received the medication once daily by gavage for 28 consecutive days. After the treatment period, the spatial learning and memory abilities of the mice were assessed using the Morris water maze test.
[0034] The Morris water maze test setup consists of a circular pool, a platform, a tracking system, and analysis software. The pool has a diameter of 180 cm, a water depth maintained at 40-60 cm, and a water temperature controlled at 21±1℃ to ensure the rats are in a suitable physiological state. The platform is made of transparent material, approximately 20 cm in diameter, and its height is slightly below the water surface by 1-2 cm, preventing the rats from directly observing it but allowing them to reach it by swimming. Different colored and shaped geometric markers are affixed to the inner wall of the pool as spatial references, evenly dividing the pool into four quadrants. During the experiment, the platform's position remains fixed in the center of the target quadrant and does not change throughout the test.
[0035] The navigation training phase lasted for 5 consecutive days, with 4 training sessions per day. Each time, rats were randomly placed into the water from three different entry points in three different quadrants and allowed to swim freely to find the hidden platform. If a rat found the platform within 120 seconds, it was allowed to stay on the platform for 10 seconds, and the escape latency was recorded. If it did not find the platform within 120 seconds, it was guided to the platform and allowed to stay for 10 seconds, and the escape latency was recorded as 120 seconds.
[0036] On day 6, a spatial exploration test was conducted. The platform was removed, and the rats were placed in the water from the diagonal quadrant entry point. The time it took for the rats to find the original platform (i.e., the escape latency) and the number of times they crossed the original platform were recorded to evaluate their spatial memory ability. After each experiment, the inner wall of the pool and related components were wiped with clean water and 75% ethanol to eliminate any residual odor and avoid interfering with subsequent experiments.
[0037] Table 2 Results of the Morris Water Maze Test
[0038] Table 2 shows that, compared with the blank control group, the escape latency of the model group rats was significantly prolonged and the number of times they crossed the original platform position was significantly reduced, indicating that the learning and memory abilities of the Aβ-induced Alzheimer's disease model rats were severely impaired, and the model was successfully established. Compared with the model group, all doses of Wugu insect oil could shorten the escape latency and increase the number of times they crossed the original platform position to varying degrees, and the effect gradually increased with the increase of the dosage, indicating that Wugu insect oil can significantly improve the spatial learning and memory abilities of AD model rats, has a significant cognitive function improvement effect, and can effectively alleviate the cognitive decline associated with neurodegenerative diseases.
[0039] The above descriptions are merely embodiments of the present invention, and common knowledge such as specific technical solutions and / or characteristics are not described in detail here. It should be noted that those skilled in the art can make various modifications and improvements without departing from the technical solutions of the present invention, and these should also be considered within the scope of protection of the present invention. These modifications and improvements will not affect the effectiveness of the implementation of the present invention or the practicality of the patent. The scope of protection claimed in this application should be determined by the content of its claims, and the specific embodiments described in the specification can be used to interpret the content of the claims.
Claims
1. Application of Five Grain Insect Oil in the preparation of products for the prevention and / or treatment of neurodegenerative diseases.
2. The application according to claim 1, characterized in that, The neurodegenerative diseases mentioned include Alzheimer's disease or Parkinson's disease.
3. Application of Five Grain Insect Oil in the preparation of products for neuroprotection, delaying neuroaging and / or improving cognitive function.
4. The application according to claim 3, characterized in that, The improvement in cognitive function includes improved spatial learning and / or memory abilities.
5. The application according to any one of claims 1-4, characterized in that, The products include food, health products, or medicines.
6. Application of Five Grain Insect Oil in the Preparation of Aβ Aggregation Inhibitors.
7. The application according to any one of claims 1-6, characterized in that, The five-grain insect oil contains 2.16g / 100g of EPA, 0.0104g / 100g of nervonic acid, and 49.1g / 100g of total unsaturated fatty acids.
8. A pharmaceutical preparation for the prevention and / or treatment of neurodegenerative diseases, characterized in that, It comprises the five grain insect oil as described in any one of claims 1-7 and a pharmaceutically acceptable carrier.
9. The pharmaceutical preparation according to claim 8, characterized in that, Dosage forms include tablets, pills, granules, capsules, injections, oral liquids, suspensions, or emulsions.