N-acetyl-D-glucosamine composition with anti-tumor effect and application of N-acetyl-D-glucosamine composition

Abstract

The invention relates to an N-acetyl-D-glucosamine composition with an anti-tumor effect and application of the N-acetyl-D-glucosamine composition, and relates to the technical field of medicines and health care products, the N-acetyl-D-glucosamine composition with the anti-tumor effect comprises the following raw materials by weight: 17-29 parts of N-acetyl-D-glucosamine and 5-10 parts of an extract of Tongshan. According to the invention, the N-acetyl-D-glucosamine and the extract in a proper proportion are matched for use for the first time, so that the synergistic interaction of the N-acetyl-D-glucosamine and the extract is realized. In-vitro animal anti-tumor experiments show that the N-acetyl-D-glucosamine composition provided by the invention can significantly reduce the tumor volume in a rat model, provides a new way for clinical treatment of tumor patients, and has a wide application prospect.

Description

Technical Field

[0001] The present invention relates to the technical field of medicine and health products, and particularly relates to an N-acetyl-D-glucosamine composition with anti-tumor efficacy and its application. Background Art

[0002] In the technical field of medicine and health products, the research and development of anti-tumor drugs and health products have always been hot topics. As a disease that seriously threatens human health, the incidence and mortality of tumors are both high globally. Therefore, finding safe and effective anti-tumor drugs or health products is of great significance for improving the quality of life and prolonging the survival period of tumor patients.

[0003] N-acetyl-D-glucosamine (N-Acetyl-D-glucosamine, abbreviated as GlcNAc) is a naturally occurring amino sugar and an important component of biological macromolecules such as glycoproteins and glycolipids. In recent years, studies have shown that N-acetyl-D-glucosamine has a variety of biological activities, including anti-inflammatory, antioxidant, immunomodulatory, etc., and also shows certain potential in anti-tumor. However, the anti-tumor effect of using N-acetyl-D-glucosamine alone often has limitations and cannot meet the requirements of clinical treatment effects.

[0004] Dafabiao is a plant of the genus Campylotropis in the legume family, Campylotropis trigonoclada (Franch.) A.K.Schindl., and its roots and whole plants are used as medicine. Dafabiao tastes pungent, slightly sweet, astringent, non-toxic, neutral in nature, and belongs to the liver, large intestine, and heart meridians. Its extract contains a variety of bioactive components and has the effects of clearing heat and detoxifying, dissipating swelling and nodules. In folk medicine and modern medical research, it can be used to treat diseases such as cold and fever, rheumatoid arthritis, etc.

[0005] In order to overcome the disadvantage of the limited anti-tumor effect of the single component of N-acetyl-D-glucosamine, scientific research personnel have begun to explore the compounding of different anti-tumor active components in order to achieve a synergistic effect. However, there are still few studies on the compounding of GlcNAc and Dafabiao for anti-tumor at present, and there is a lack of a clear and appropriate ratio to achieve the best synergistic effect between the two. Summary of the Invention

[0006] To solve the above problems, the present invention provides an N-acetyl-D-glucosamine composition with anti-tumor efficacy and its application.

[0007] In the first aspect, the present invention provides an N-acetyl-D-glucosamine composition with anti-tumor efficacy. Calculated by weight parts, the N-acetyl-D-glucosamine composition with anti-tumor efficacy comprises the following raw materials:

[0008] 17 to 29 parts of N-acetyl-D-glucosamine and 5 to 10 parts of the extract of Clinopodium gracile (Benth.) Kuntze.

[0009] Furthermore, by weight parts, the N-acetyl-D-glucosamine composition with anti-tumor efficacy comprises the following raw materials:

[0010] 23 parts of N-acetyl-D-glucosamine and 7 parts of the extract of Clinopodium gracile (Benth.) Kuntze.

[0011] Furthermore, by weight parts, the N-acetyl-D-glucosamine composition with anti-tumor efficacy comprises the following raw materials:

[0012] 17 parts of N-acetyl-D-glucosamine and 5 parts of the extract of Clinopodium gracile (Benth.) Kuntze.

[0013] Furthermore, by weight parts, the N-acetyl-D-glucosamine composition with anti-tumor efficacy comprises the following raw materials:

[0014] 29 parts of N-acetyl-D-glucosamine and 10 parts of the extract of Clinopodium gracile (Benth.) Kuntze.

[0015] Furthermore, the extract of Clinopodium gracile (Benth.) Kuntze is the water extract of Clinopodium gracile (Benth.) Kuntze.

[0016] Furthermore, the preparation method of the water extract of Clinopodium gracile (Benth.) Kuntze comprises the following process:

[0017] Crush the whole plant of Clinopodium gracile (Benth.) Kuntze, and then add it to water to obtain a mixture liquid;

[0018] Perform vacuum reflux extraction on the mixture liquid, and then concentrate and dry the obtained water extract to obtain the water extract of Clinopodium gracile (Benth.) Kuntze.

[0019] Furthermore, the working condition parameters of the vacuum reflux extraction include: the pressure is 4 to 9 kPa, the temperature is 33 to 47 °C, the time is 1 to 2 hours, and the number of times is 1 to 3 times.

[0020] Furthermore, the working condition parameters of the vacuum reflux extraction include: the pressure is 7 kPa, the temperature is 43 °C, the time is 1 to 2 hours, and the number of times is 1 to 3 times.

[0021] Furthermore, the weight ratio of the whole plant of Clinopodium gracile (Benth.) Kuntze to the water is (1 to 2):(8 to 12).

[0022] In the second aspect, the present invention provides the application of the N-acetyl-D-glucosamine composition with anti-tumor efficacy according to any one of the first aspect in the preparation of anti-tumor drugs and health products with anti-tumor efficacy.

[0023] The above technical solution provided by the embodiment of the present invention has at least the following advantages compared with the prior art:

[0024] The embodiment of the present invention provides an N-acetyl-D-glucosamine composition with anti-tumor efficacy and its application. The present invention uses N-acetyl-D-glucosamine and Dafa extract in a suitable ratio for the first time, achieving a synergistic effect of the two. In vitro animal anti-tumor experiments show that the N-acetyl-D-glucosamine composition provided by the present invention can significantly reduce the tumor volume in the rat model, providing a new way for the clinical treatment of tumor patients, and has broad application prospects. DETAILED DESCRIPTION

[0025] In order to make the purpose, technical solution and advantages of the embodiments of the present invention clearer, the technical solution of the present invention will be clearly and completely described in combination with the embodiments of the present invention. Obviously, the described embodiments are part of the embodiments of the present invention, not all of the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without creative work are within the scope of protection of the present invention.

[0026] Unless otherwise specified, various raw materials, reagents, instruments and equipment used in the present invention can be purchased from the market or prepared by existing methods.

[0027] In a first aspect, the present invention provides an N-acetyl-D-glucosamine composition having anti-tumor efficacy, wherein the N-acetyl-D-glucosamine composition having anti-tumor efficacy comprises the following raw materials in parts by weight:

[0028] 17-29 parts of N-acetyl-D-glucosamine and 5-10 parts of Dahurian taro extract.

[0029] The embodiment of the present invention provides an N-acetyl-D-glucosamine composition with anti-tumor efficacy. The present invention uses N-acetyl-D-glucosamine and Dafa extract in a suitable ratio for the first time, achieving a synergistic effect of the two. In vitro animal anti-tumor experiments have shown that the N-acetyl-D-glucosamine composition provided by the present invention can significantly reduce the tumor volume in the rat model, providing a new way for the clinical treatment of tumor patients and having broad application prospects.

[0030] In some specific embodiments, the N-acetyl-D-glucosamine composition with anti-tumor efficacy comprises the following raw materials in parts by weight:

[0031] N-acetyl-D-glucosamine 23 parts and Dahurian basil extract 7 parts.

[0032] In some specific embodiments, based on parts by weight, the N-acetyl-D-glucosamine composition with anti-tumor efficacy comprises the following raw materials:

[0033] 17 parts of N-acetyl-D-glucosamine and 5 parts of the extract of Clinopodium polycephalum (Vant.) C. Y. Wu et Hsuan.

[0034] In some specific embodiments, based on parts by weight, the N-acetyl-D-glucosamine composition with anti-tumor efficacy comprises the following raw materials:

[0035] 29 parts of N-acetyl-D-glucosamine and 10 parts of the extract of Clinopodium polycephalum (Vant.) C. Y. Wu et Hsuan.

[0036] In some specific embodiments, the extract of Clinopodium polycephalum (Vant.) C. Y. Wu et Hsuan is the water extract of Clinopodium polycephalum (Vant.) C. Y. Wu et Hsuan.

[0037] In some specific embodiments, the preparation method of the water extract of Clinopodium polycephalum (Vant.) C. Y. Wu et Hsuan comprises the following process:

[0038] Crush the whole plant of Clinopodium polycephalum (Vant.) C. Y. Wu et Hsuan, and then add it to water to obtain a mixed material liquid;

[0039] Perform reduced-pressure reflux extraction on the mixed material liquid, and then concentrate and dry the obtained water extract to obtain the water extract of Clinopodium polycephalum (Vant.) C. Y. Wu et Hsuan.

[0040] In some specific embodiments, the working condition parameters of the reduced-pressure reflux extraction include: the pressure is 4 - 9 kPa, the temperature is 33 - 47 °C, the time is 1 - 2 hours, and the number of times is 1 - 3 times.

[0041] In some specific embodiments, the working condition parameters of the reduced-pressure reflux extraction include: the pressure is 7 kPa, the temperature is 43 °C, the time is 1 - 2 hours, and the number of times is 1 - 3 times.

[0042] In some specific embodiments, the weight ratio of the whole plant of Clinopodium polycephalum (Vant.) C. Y. Wu et Hsuan to the water is (1 - 2):(8 - 12).

[0043] In some specific embodiments, the preparation method of the N-acetyl-D-glucosamine composition with anti-tumor efficacy comprises the following steps: stir and mix N-acetyl-D-glucosamine and the extract of Clinopodium polycephalum (Vant.) C. Y. Wu et Hsuan according to the weight ratio, and then crush and pass through a 100-mesh sieve.

[0044] In a second aspect, the present invention provides the application of the N-acetyl-D-glucosamine composition with anti-tumor efficacy according to any one of the first aspect in the preparation of anti-tumor drugs and health products with anti-tumor efficacy.

[0045] It should be noted that, the components and raw materials involved in the N-acetyl-D-glucosamine composition with anti-tumor efficacy and its application provided by the embodiment of the present invention, unless otherwise specified or described, can be directly commercially available products or homemade according to existing preparation processes. At the same time, the operation steps involved in the N-acetyl-D-glucosamine composition with anti-tumor efficacy and its application provided by the embodiment of the present invention, unless otherwise specified or described, can be performed in a conventional manner in the art or using existing equipment, and will not be described one by one here.

[0046] The present invention will be further described below in conjunction with specific examples. It should be understood that these examples are intended only to illustrate the present invention and are not intended to limit the scope of the present invention. The experimental methods in the following examples that do not specify specific conditions are usually measured according to national standards. If there is no corresponding national standard, then the conditions recommended by the manufacturer are followed.

[0047] Example 1

[0048] This example provides an N-acetyl-D-glucosamine composition with anti-tumor efficacy. The N-acetyl-D-glucosamine composition with anti-tumor efficacy comprises the following raw materials in parts by weight:

[0049] 23 parts of N-acetyl-D-glucosamine and 7 parts of Dafa extract;

[0050] The preparation method of the Dachufa extract includes the following processes: crushing the whole plant of Dachufa, and then adding it into water, wherein the weight ratio of the whole plant of Dachufa to the water is 1.5:10, to obtain a mixed liquid; performing reduced pressure reflux extraction on the mixed liquid, the pressure is 7 kPa, the temperature is 43°C, the time is 1.5 hours, the number of times is 2, and then the obtained water extract is concentrated and dried to obtain the Dachufa extract.

[0051] The preparation method of the above-mentioned N-acetyl-D-glucosamine composition having anti-tumor efficacy comprises the following steps:

[0052] N-acetyl-D-glucosamine and Dafa extract are stirred and mixed according to the weight ratio, and then crushed and passed through a 100-mesh sieve.

[0053] Example 2

[0054] This example provides an N-acetyl-D-glucosamine composition with anti-tumor efficacy. The N-acetyl-D-glucosamine composition with anti-tumor efficacy comprises the following raw materials in parts by weight:

[0055] 17 parts of N-acetyl-D-glucosamine and 5 parts of Dafa extract;

[0056] The preparation method of the Dachufa extract includes the following processes: crushing the whole plant of Dachufa, and then adding it into water, wherein the weight ratio of the whole plant of Dachufa to the water is 1:8, to obtain a mixed liquid; performing reduced pressure reflux extraction on the mixed liquid, at a pressure of 4 kPa, a temperature of 33°C, a time of 1.5 hours, and a number of times, and then concentrating and drying the obtained water extract to obtain the Dachufa extract.

[0057] The preparation method of the above-mentioned N-acetyl-D-glucosamine composition having anti-tumor efficacy comprises the following steps:

[0058] N-acetyl-D-glucosamine and Dafa extract are stirred and mixed according to the weight ratio, and then crushed and passed through a 100-mesh sieve.

[0059] Example 3

[0060] This example provides an N-acetyl-D-glucosamine composition with anti-tumor efficacy. The N-acetyl-D-glucosamine composition with anti-tumor efficacy comprises the following raw materials in parts by weight:

[0061] N-acetyl-D-glucosamine 29 parts and Dafa extract 10 parts;

[0062] The preparation method of the Dachufa extract includes the following processes: crushing the whole plant of Dachufa, and then adding it into water, wherein the weight ratio of the whole plant of Dachufa to the water is 1.5:12, to obtain a mixed liquid; performing reduced pressure reflux extraction on the mixed liquid, the pressure is 9 kPa, the temperature is 47°C, the time is 1.5 hours, the number of times is 2 times, and then concentrating and drying the obtained water extract to obtain the Dachufa extract.

[0063] The preparation method of the above-mentioned N-acetyl-D-glucosamine composition having anti-tumor efficacy comprises the following steps:

[0064] N-acetyl-D-glucosamine and Dafa extract are stirred and mixed according to the weight ratio, and then crushed and passed through a 100-mesh sieve.

[0065] Comparative Example 1

[0066] This example provides an anti-tumor substance, which is N-acetyl-D-glucosamine.

[0067] Comparative Example 2

[0068] This example provides an anti-tumor substance, which is a Dashuba extract. The preparation method of the Dashuba extract includes the following processes: crushing the whole plant of Dashuba, and then adding it into water, wherein the weight ratio of the whole plant of Dashuba to the water is 1.5:10, to obtain a mixed liquid; subjecting the mixed liquid to reduced pressure reflux extraction, the pressure is 7 kPa, the temperature is 43°C, the time is 1.5 hours, the number of times is 2, and then the obtained water extract is concentrated and dried to obtain the Dashuba extract.

[0069] Comparative Example 3

[0070] This example provides an N-acetyl-D-glucosamine composition, which is different from Example 1 only in that the weight portion of the Dafa extract is adjusted to 17 parts; the remaining steps and parameters are the same.

[0071] The above-mentioned N-acetyl-D-glucosamine composition, in parts by weight, comprises the following raw materials:

[0072] 23 parts of N-acetyl-D-glucosamine and 17 parts of Dafa extract;

[0073] The preparation method of the Dachufa extract includes the following processes: crushing the whole plant of Dachufa, and then adding it into water, wherein the weight ratio of the whole plant of Dachufa to the water is 1.5:10, to obtain a mixed liquid; performing reduced pressure reflux extraction on the mixed liquid, the pressure is 7 kPa, the temperature is 43°C, the time is 1.5 hours, the number of times is 2, and then the obtained water extract is concentrated and dried to obtain the Dachufa extract.

[0074] The preparation method of the above-mentioned N-acetyl-D-glucosamine composition having anti-tumor efficacy comprises the following steps:

[0075] N-acetyl-D-glucosamine and Dafa extract are stirred and mixed according to the weight ratio, and then crushed and passed through a 100-mesh sieve.

[0076] Comparative Example 4

[0077] This example provides an N-acetyl-D-glucosamine composition, which is different from Example 1 only in that the pressure is adjusted to 25 kPa and the temperature is adjusted to 68° C. during the preparation of the Dafa extract; the remaining steps and parameters are the same.

[0078] The above-mentioned N-acetyl-D-glucosamine composition, in parts by weight, comprises the following raw materials:

[0079] 23 parts of N-acetyl-D-glucosamine and 7 parts of Dafa extract;

[0080] The preparation method of the Daphniphyllum yunnanense extract comprises the following process: pulverize the whole plant of Daphniphyllum yunnanense, then add water, and the weight ratio of the whole plant of Daphniphyllum yunnanense to the water is 1.5:10 to obtain a mixed material liquid; subject the mixed material liquid to reduced pressure reflux extraction, with a pressure of 25 kPa, a temperature of 68 °C, a time of 1.5 hours, and the number of times being 2 times, and then concentrate and dry the obtained water extract to obtain the Daphniphyllum yunnanense extract.

[0081] The preparation method of the above N-acetyl-D-glucosamine composition with anti-tumor efficacy comprises the following steps:

[0082] Stir and mix N-acetyl-D-glucosamine and the Daphniphyllum yunnanense extract according to the weight ratio, and then pulverize and pass through a 100-mesh sieve.

[0083] Test example

[0084] In this example, the anti-tumor effects of the substances obtained in the above examples and comparative examples were tested according to the test methods disclosed in the prior art.

[0085] Test method:

[0086] 1. Experimental animals: Wistar rats were selected, with a body weight range of 150 g to 180 g, and both males and females were included to ensure the general applicability of the experimental results.

[0087] 2. Grouping design:

[0088] One blank control group was established, with 10 rats, as the benchmark reference for the experiment.

[0089] One to seven drug administration experimental groups were established, and the substances obtained in Example 1 (i.e., drug administration experimental group 1), Example 2 (i.e., drug administration experimental group 2), Example 3 (i.e., drug administration experimental group 3), Comparative Example 1 (i.e., drug administration experimental group 4), Comparative Example 2 (i.e., drug administration experimental group 5), Comparative Example 3 (i.e., drug administration experimental group 6), and Comparative Example 4 (i.e., drug administration experimental group 7) were sequentially administered for intervention treatment. Each group included 10 rats to ensure the reliability of statistics.

[0090] 3. Tumor inoculation and model establishment: All rats were subjected to W256 intrahepatic inoculation to construct a tumor model. Seven days after inoculation, subsequent experimental operations were carried out.

[0091] 4. Anesthesia and surgical operation:

[0092] Sodium pentobarbital was used for intraperitoneal injection anesthesia at a dose of 35 mg / kg.

[0093] After the anesthesia took effect, the rats were fixed and the abdomen was opened to expose the liver.

[0094] Measure the maximum diameter (a) and minimum diameter (b) of the surface of the liver tumor, and calculate the tumor volume according to Formula 1: (a * b^2) / 2 = V (tumor volume, mm 3 ).

[0095] 5. Drug administration and treatment course:

[0096] After the surgery, wait for the rats to fully wake up and resume normal diet.

[0097] Each drug administration test group was given the test drug by gavage, and the dosage was 50 mg / kg / day.

[0098] The blank control group was given an equal amount of normal saline as a control.

[0099] Administer the drug continuously for 3 weeks, once a day, to ensure the full exertion of the drug effect.

[0100] 6. Evaluation of tumor volume change:

[0101] 24 hours after the last drug administration, measure and calculate the tumor volume again according to Formula 1 to obtain the tumor volume V2 after treatment.

[0102] Combined with the tumor volume V1 before treatment, according to Formula 2: △ tumor volume reduction value = V2 - V1, calculate the reduction amount of the tumor volume. The test results are shown in Table 1. In Table 1, when the △ tumor volume reduction value is "+", it indicates that the tumor volume V2 after treatment is larger than the tumor volume V1 before treatment. When the △ tumor volume reduction value in Table 1 is "-", it indicates that the tumor volume V2 after treatment is smaller than the tumor volume V1 before treatment.

[0103] Table 1

[0104]

[0105]

[0106] As can be seen from Table 1, the N-acetyl-D-glucosamine composition provided by the embodiments of the present invention can significantly reduce the tumor volume in the rat model, and the reduction effect is significantly better than that of the comparative example.

[0107] In summary, the embodiments of the present invention provide an N-acetyl-D-glucosamine composition with anti-tumor efficacy and its application. The present invention first combines N-acetyl-D-glucosamine and the extract of Polygonum bistorta L. in a suitable ratio to achieve the synergistic effect of the two. The in vitro animal anti-tumor experiment shows that the N-acetyl-D-glucosamine composition provided by the present invention can significantly reduce the tumor volume in the rat model, providing a new way for the clinical treatment of tumor patients and having broad application prospects.

[0108] The above are only specific embodiments of the present invention, enabling those skilled in the art to understand or implement the present invention. Various modifications to these embodiments will be obvious to those skilled in the art, and the general principles defined herein can be implemented in other embodiments without departing from the spirit or scope of the present invention. Therefore, the present invention will not be limited to these embodiments shown herein, but rather to the broadest scope consistent with the principles and novel features claimed herein.

Claims

1. An N-acetyl-D-glucosamine composition having anti-tumor efficacy, characterized in that: The N-acetyl-D-glucosamine composition having anti-tumor efficacy comprises the following raw materials in parts by weight: 17-29 parts of N-acetyl-D-glucosamine and 5-10 parts of Dahurian taro extract.

2. The N-acetyl-D-glucosamine composition with anti-tumor efficacy according to claim 1, characterized in that: The N-acetyl-D-glucosamine composition having anti-tumor efficacy comprises the following raw materials in parts by weight: N-acetyl-D-glucosamine 23 parts and Dahurian basil extract 7 parts.

3. The N-acetyl-D-glucosamine composition with anti-tumor efficacy according to claim 1, characterized in that: The N-acetyl-D-glucosamine composition having anti-tumor efficacy comprises the following raw materials in parts by weight: N-acetyl-D-glucosamine 17 parts and Dahurian basil extract 5 parts.

4. The N-acetyl-D-glucosamine composition with anti-tumor efficacy according to claim 1, characterized in that: The N-acetyl-D-glucosamine composition having anti-tumor efficacy comprises the following raw materials in parts by weight: N-acetyl-D-glucosamine 29 parts and Dahurian basil extract 10 parts.

5. The N-acetyl-D-glucosamine composition with anti-tumor efficacy according to any one of claims 1 to 4, characterized in that: The radix daphne extract is a radix daphne water extract.

6. The N-acetyl-D-glucosamine composition with anti-tumor efficacy according to claim 5, characterized in that: Preparation method of the radix sutchuenensis aqueous extract The process includes: The whole plant of Dahurian dahurian is crushed and then added into water to obtain a mixed liquid; The mixed liquid is subjected to reduced pressure reflux extraction, and then the obtained water extract is concentrated and dried to obtain the large-scale aqueous extract.

7. The N-acetyl-D-glucosamine composition with anti-tumor efficacy according to claim 6, characterized in that: The working condition parameters of the reduced pressure reflux extraction include: pressure of 4 to 9 kPa, temperature of 33 to 47° C., time of 1 to 2 hours, and number of times of 1 to 3 times.

8. The N-acetyl-D-glucosamine composition with anti-tumor efficacy according to claim 6, characterized in that: The working condition parameters of the reduced pressure reflux extraction include: pressure of 7 kPa, temperature of 43° C., time of 1 to 2 hours, and number of times of 1 to 3 times.

9. The N-acetyl-D-glucosamine composition with anti-tumor efficacy according to claim 6, characterized in that: The weight ratio of the whole plant of Dalbergia paniculata to the water is (1-2):(8-12).

10. Use of the N-acetyl-D-glucosamine composition with anti-tumor efficacy according to any one of claims 1 to 9 in the preparation of anti-tumor drugs and health products with anti-tumor efficacy.

Images