CN114306373B - Lipid-lowering composition containing acanthopanax trifoliatus neutral polysaccharide ATP1-1 and preparation method thereof - Google Patents
Lipid-lowering composition containing acanthopanax trifoliatus neutral polysaccharide ATP1-1 and preparation method thereof Download PDFInfo
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Abstract
The invention provides a lipid-lowering composition containing trifoliate acanthopanax neutral polysaccharide ATP1-1 and a preparation method thereof, and relates to the technical field of pharmacy. The composition prepared by compounding the raw materials has good lipid-lowering effect and alpha-glucosidase inhibiting effect.
Description
Technical Field
The invention relates to the technical field of pharmacy, in particular to a lipid-lowering composition containing trifoliate acanthopanax neutral polysaccharide ATP1-1 and a preparation method thereof.
Background
The acanthopanax trifoliatus is shrub of acanthopanax of araliaceae, has the main functions of cooling blood, detoxifying, expelling wind, expelling pus, promoting blood circulation, reducing swelling and the like, has high medicinal value, and modern pharmacological research shows that the acanthopanax trifoliatus contains various active ingredients and has pharmacological effects of increasing coronary artery blood flow, protecting heart and cerebral vessels, resisting tumors, reducing blood sugar and blood fat and resisting fatigue. All parts of the acanthopanax trifoliatus contain polysaccharides, wherein the stem bark has the highest polysaccharide content, and related researches show that the acanthopanax trifoliatus polysaccharide has good effects of reducing blood sugar, diminishing inflammation, relieving pain and resisting fatigue, but the researches on the neutral acanthopanax trifoliatus polysaccharide are still less so far, and the prior researches mostly focus on the extraction of the acanthopanax trifoliatus polysaccharide or the preparation process of related preparations thereof, such as documents: zhang Xugong, yang Huiwen, he Rongbin and the like, researches on preparation processes of the Acanthopanax trifoliatus polysaccharide tablet [ J ] academic press of high specialty schools such as Pingxiang, 2015,32 (6): 48-50, preparation of the tablet by taking the Acanthopanax trifoliatus polysaccharide as a raw material, and investigation on influence of auxiliary material composition and dosage on tablet quality, so that a forming process is optimized. And the literature: chen Jinlan, huang Pengna Acanthopanax trifoliatus polysaccharide extraction process and its dispersible tablet preparation [ J ]. Chinese medicine economics, 2018,13 (7): 3. The extraction process of Acanthopanax trifoliatus polysaccharide and its preparation process of Acanthopanax trifoliatus polysaccharide dispersible tablet are intensively researched. Some researches focus on the application of the trifoliate acanthopanax polysaccharide in preparing medicines for treating diabetes or related diseases such as tumor, for example, the literature: zheng Shijia, yang Huiwen, cheng Xuanxuan, et al, influence of Acanthopanax trifoliatus neutral polysaccharide ATP1-1 on sugar metabolism in type 1 diabetic mice [ J ] Chinese patent medicine, 2018,040 (012): 2618-2623. And references: zhou Lou, yang Huiwen, cheng Xuanxuan and the like, researches on sugar reducing action mechanism of acanthosporin-induced diabetic mice by using neutral homogeneous polysaccharide of Acanthopanax trifoliatus [ J ] food industry science and technology, 2017,038 (017): 288-291. In addition, related researches are also carried out on patents CN201310035607.9, CN201911286788.6 and CN201910707095.3, and the application of the acanthopanax trifoliatus in preparing medicines for treating diabetes is respectively and specifically researched; acanthopanax trifoliatus polysaccharide, a preparation method and application thereof in preparing antitumor drugs; and application of the trifoliate acanthopanax polysaccharide ATP1-1 in preparing a medicament for treating diabetes.
However, the development and application level of other effects of the trifoliate acanthopanax neutral polysaccharide ATP1-1, such as the preparation level of lipid-lowering drugs, is still blank in the field. Aiming at the problems, the composition containing the acanthopanax trifoliatus neutral polysaccharide ATP1-1 is needed to fully exert the efficacy of the acanthopanax trifoliatus polysaccharide in other aspects.
Disclosure of Invention
Aiming at the problems in the prior art, the invention provides a lipid-lowering composition containing trifoliate acanthopanax neutral polysaccharide ATP1-1 and a preparation method thereof, and the lipid-lowering composition containing trifoliate acanthopanax neutral polysaccharide ATP1-1 has good lipid-lowering effect and alpha-glucosidase inhibiting effect.
In order to achieve the purpose, the technical scheme adopted by the invention is as follows:
the invention provides application of trifoliate acanthopanax neutral polysaccharide ATP1-1 in preparation of a medicament with a lipid-lowering effect.
The invention provides a composition containing trifoliate acanthopanax neutral polysaccharide ATP1-1, comprising trifoliate acanthopanax neutral polysaccharide ATP1-1, tea polysaccharide, barley beta-glucan, bamboo leaf flavone and phytosterol.
Further, the weight ratio of the trifoliate acanthopanax neutral polysaccharide ATP1-1, the tea polysaccharide, the barley beta-glucan, the bamboo leaf flavone and the phytosterol is 10-15.
Preferably, the weight ratio of the trifoliate acanthopanax neutral polysaccharide ATP1-1, the tea polysaccharide, the barley beta-glucan, the bamboo leaf flavone and the phytosterol is 12-15.
Further preferably, the weight ratio of the trifoliate acanthopanax neutral polysaccharide ATP1-1, the tea polysaccharide, the barley beta-glucan, the bamboo leaf flavonoid and the phytosterol is 13.
Further, the phytosterols include one or more of beta-sitosterol, stigmasterol, campesterol, and brassicasterol.
Further, the composition is characterized in that: also comprises vitamins.
Preferably, the vitamins include one or more of vitamin B2, vitamin C and vitamin E.
The invention also provides a preparation method of the composition, which comprises the following steps: mixing radix Ilicis Pubescentis neutral polysaccharide ATP1-1, tea polysaccharide, barley beta-dextran, bamboo leaf flavone and phytosterol.
The invention also provides application of the composition in preparing a medicament with a lipid-lowering effect.
Further, the medicine comprises tablets, capsules, paste or granules.
The invention also provides a medicament with a lipid-lowering effect, which comprises the composition and medically acceptable auxiliary materials.
In some embodiments, the invention provides a tablet with lipid-lowering effect, which comprises the composition and pharmaceutically acceptable auxiliary materials.
In some specific embodiments, the invention provides a capsule with a lipid-lowering effect, which comprises the composition and pharmaceutically acceptable auxiliary materials.
The technical effects obtained by the invention are as follows:
the trifoliate acanthopanax neutral polysaccharide ATP1-1 and the lipid-lowering composition containing the trifoliate acanthopanax neutral polysaccharide ATP1-1 have good lipid-lowering effect and alpha-glucosidase inhibiting effect, the composition provided by the invention is mainly obtained by compounding trifoliate acanthopanax neutral polysaccharide ATP1-1, tea polysaccharide, barley beta-glucan, bamboo leaf flavone and phytosterol (vitamins can be additionally added), and the raw materials can fully cooperate and synergize to improve the lipid-lowering effect of the product.
Drawings
FIG. 1 shows the SOD levels of the livers of mice in each group (including normal group, model group, positive group, ATP1-1 high dose group and ATP1-1 low dose group) (SOD level of liver disease)
n＝6)；
FIG. 2 is an index of MDA content in liver of mice in each group (including normal group, model group, positive group, ATP1-1 high dose group and ATP1-1 low dose group) ((
n＝6)。
Detailed Description
The embodiments of the present invention are described below with reference to specific embodiments, and other advantages and effects of the present invention will be easily understood by those skilled in the art from the disclosure of the present specification. The invention is capable of other and different embodiments and of being practiced or of being carried out in various ways, and its several details are capable of modification in various respects, all without departing from the spirit and scope of the present invention.
Before the present embodiments are further described, it is to be understood that the scope of the invention is not limited to the particular embodiments described below; it is also to be understood that the terminology used in the examples is for the purpose of describing particular embodiments only, and is not intended to limit the scope of the present invention.
When numerical ranges are given in the examples, it is understood that both endpoints of each of the numerical ranges and any value therebetween can be selected unless the invention otherwise indicated. Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs.
It should be noted that the raw materials used in the present invention are all common commercial products, and thus the sources thereof are not particularly limited.
Example 1
The composition containing the trifoliate acanthopanax neutral polysaccharide ATP1-1 comprises trifoliate acanthopanax neutral polysaccharide ATP1-1, tea polysaccharide, barley beta-glucan, bamboo leaf flavone and beta-sitosterol in a weight ratio of 10.
Example 2
The composition containing the trifoliate acanthopanax neutral polysaccharide ATP1-1 comprises the trifoliate acanthopanax neutral polysaccharide ATP1-1, tea polysaccharide, barley beta-glucan, bamboo leaf flavone and stigmasterol, wherein the weight ratio of the trifoliate acanthopanax neutral polysaccharide ATP1-1 to the trifoliate acanthopanax neutral polysaccharide ATP 8.
Example 3
The composition containing the trifoliate acanthopanax neutral polysaccharide ATP1-1 comprises trifoliate acanthopanax neutral polysaccharide ATP1-1, tea polysaccharide, barley beta-glucan, bamboo leaf flavone and phytosterol (beta-sitosterol and stigmasterol in a weight ratio of 1:1) in a weight ratio of 13.
Example 4
The composition containing the trifoliate acanthopanax neutral polysaccharide ATP1-1 comprises the following raw materials in parts by weight of 12.
Example 5
The composition containing the trifoliate acanthopanax neutral polysaccharide ATP1-1 comprises the following raw materials in parts by weight of 15.
Application example 1
A tablet with lipid-lowering effect contains the composition in example 1, and is prepared by the following steps:
1) Uniformly mixing the composition, the starch, the microcrystalline cellulose and the internally added crosslinked PVP in the embodiment 1 according to the proportion of the raw material components to obtain mixed powder;
2) Adding an adhesive into the mixed powder for wet granulation, and drying to obtain dry granules;
3) Adding the cross-linked PVP and the magnesium stearate into the dry granules according to the raw material component ratio, fully and uniformly mixing, tabletting to obtain plain tablets, and carrying out a film coating process on the plain tablets to obtain finished products;
comparative example 1
The only difference from example 1 is that barley beta-glucan and bamboo leaf polysaccharide were replaced by an equal amount of trifoliate acanthopanax neutral polysaccharide ATP1-1.
Comparative example 2
The difference from example 1 is only that the weight ratio of the trifoliate acanthopanax neutral polysaccharide ATP1-1, the tea polysaccharide, the barley beta-glucan, the bamboo leaf flavone and the beta-sitosterol is 7.
Lipid lowering action of the composition of the invention
1. Animal modeling, grouping and administration
The mice were fed with the normal feed adaptively for 7d, and were randomly divided into a normal group (n = 6) and a model group (n = 66), and the normal group was fed with the normal feed, and after the model group was fed with the high-fat high-sugar feed for one month, the mice were fasted for 12h without water deprivation, and were subjected to intraperitoneal injection of STZ130mg/kg. After one week of STZ injection, fasting is not forbidden for 6h, blood is taken from the tail part to measure the fasting blood glucose value of the mouse, and the blood glucose value is more than 11.1mmol/L, which is regarded as successful molding. After the model is stabilized, the 66 mice successfully molded are randomly divided into 11 groups (n = 6) according to the blood sugar value, wherein the 11 groups are respectively a model group, a positive group, a high dose group, a low dose group and a test group, the positive group is perfused with 185mg/kg of metformin solution, the low and high dose groups are separately perfused with 40mg/kg of ATP1-1 solution and 80mg/kg of ATP1-1 solution, the test group is perfused with 80mg/kg of the composition (prepared into suspension) of each example in the invention, and the model group and the normal group are separately perfused with double distilled water with equal volume, and the administration is carried out for 1 time per day and is carried out for 8 weeks continuously. During the normal period, basal diet is continuously given to the normal group, and high-fat and high-sugar diet is given to the rest, and free food intake and drinking water are carried out during the administration period.
2. Sample collection
At 8 weeks after administration, fasting is not forbidden for 12h, blood is taken from orbit, centrifugation is carried out at 4000r for 15min, and serum is collected and stored at-20 ℃. Then taking out the liver rapidly, washing with normal saline, wiping, weighing, wrapping with tinfoil, and storing with liquid nitrogen for subsequent index determination.
Test 1: the effect of the composition of the invention on the serum TG, TC, HDL-C, LDL-C of diabetic mice
TABLE 1
| Examples of the invention | TC | TG | LDL-C | HDL-C |
| Normal group | 2.75±0.93 ** | 1.44±0.13 ** | 2.92±0.33 ** | 1.57±0.15 ** |
| Model set | 7.18±0.39 | 2.50±0.23 | 5.13±0.44 | 0.45±0.14 |
| Positive group | 5.69±0.77 ** | 1.99±0.14 ** | 3.88±0.48 ** | 0.74±0.09 ** |
| ATP1-1 high dose group | 4.28±0.40 ** | 1.70±0.07 ** | 3.87±0.28 ** | 1.11±0.10 ** |
| ATP1-1 Low dose group | 5.07±0.57 ** | 2.04±0.27 * | 4.40±0.13 ** | 0.64±0.03 * |
| Example 1 | 4.21±0.22 ** | 1.72±0.36 ** | 3.90±0.12 ** | 1.15±0.06 ** |
| Example 2 | 4.14±0.21 ** | 1.65±0.24 ** | 3.87±0.15 ** | 1.18±0.10 ** |
| Example 3 | 3.84±0.36 ** | 1.60±0.10 ** | 3.70±0.23 ** | 1.22±0.11 ** |
| Example 4 | 3.69±0.55 ** | 1.54±0.06 ** | 3.64±0.11 ** | 1.25±0.19 ** |
| Example 5 | 3.63±0.40 ** | 1.58±0.05 ** | 3.66±0.36 ** | 1.28±0.09 ** |
| Comparative example 1 | 4.43±0.32 ** | 1.97±0.39 * | 3.98±0.44 ** | 1.09±0.17 ** |
| Comparative example 2 | 4.79±0.98 ** | 2.06±0.28 * | 4.22±0.37 ** | 0.95±0.15 ** |
(Note: P <0.05, P <0.01. Compared to model group.)
As shown in Table 1, the serum TG, TC and LDL-C of the model group mice are obviously increased (P < 0.01) and the HDL-C is obviously reduced (P < 0.01) compared with the normal group, which indicates that the type 2 diabetes mice have obvious lipid metabolism disorder symptoms. After 8 weeks of treatment, the levels of TC, TG and LDL-C were significantly reduced and the level of HDL-C was significantly increased (P < 0.05) in each administration group compared to the model group, wherein the effect of the ATP1-1 high dose was superior to that in the low dose group and the effect of the composition in each example was superior to that in the comparative example group.
Test 2: the influence of the composition on the activity of SOD enzyme and MDA content of liver of diabetic mice
TABLE 2
(note: P <0.05, P <0.01. Compared to model group.)
As can be seen from the combination of Table 2 and FIGS. 1-2, the liver SOD enzyme activity of the model mice is significantly lower than that of the normal group (P < 0.01), and the MDA content is higher than that of the normal group (P < 0.05), which indicates that the liver antioxidant capacity of the type 2 diabetic mice is reduced. After 8 weeks of treatment with different ATP1-1 doses, SOD enzyme activity of diabetic mice is remarkably increased (P < 0.01), MDA content is remarkably reduced (P < 0.05), wherein the effect of the high ATP1-1 dose is better than that of a low dose group, the SOD enzyme activity is better improved, MDA effect is better, and even the SOD enzyme activity and MDA effect can be improved/reduced to be better than that of ordinary normal mice, and similarly, the effect of the composition in each embodiment is also better, and is especially better than that of a comparative example group.
In addition, through further research, the IC50 of ATP1-1 for inhibiting maltase is far less than that of sucrase, but when a certain concentration is reached, the inhibition rate of the sucrase (46.91%) is far higher than that of maltase (15.86%), and the composition containing ATP1-1 also has better inhibition effect on alpha-glucosidase.
Finally, it should be noted that the above-mentioned contents are only used for illustrating the technical solutions of the present invention, and not for limiting the protection scope of the present invention, and that the simple modifications or equivalent substitutions of the technical solutions of the present invention by those of ordinary skill in the art can be made without departing from the spirit and scope of the technical solutions of the present invention.
Claims (7)
1. A composition containing trifoliate acanthopanax neutral polysaccharide ATP1-1 for reducing blood fat is characterized in that: comprises 1-1 parts of trifoliate acanthopanax neutral polysaccharide ATP, tea polysaccharide, barley beta-glucan, bamboo leaf flavone, phytosterol and vitamins;
the weight ratio of the trifoliate acanthopanax neutral polysaccharide ATP1-1, the tea polysaccharide, the barley beta-glucan, the bamboo leaf flavone and the phytosterol is (4-15).
2. The composition of claim 1, wherein: the weight ratio of the trifoliate acanthopanax neutral polysaccharide ATP1-1, the tea polysaccharide, the barley beta-glucan, the bamboo leaf flavone and the phytosterol is (12-15).
3. The composition of claim 1, wherein: the phytosterol comprises one or more of beta-sitosterol, stigmasterol, campesterol and brassicasterol.
4. A process for preparing a composition according to any one of claims 1 to 3, characterized in that: the method comprises the following steps: mixing radix Ilicis Pubescentis neutral polysaccharide ATP1-1, tea polysaccharide, barley beta-dextran, bamboo leaf flavone, phytosterol and vitamins.
5. Use of a composition according to any one of claims 1 to 3 for the preparation of a medicament having lipid lowering effect.
6. Use according to claim 5, characterized in that: the medicine comprises tablets, capsules, paste or granules.
7. A medicament with lipid-lowering effect is characterized in that: the medicament comprises the composition of any one of claims 1 to 3 and medically acceptable auxiliary materials.
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