CN111973700A - Multifunctional garlic-allium mongolicum regel composition and preparation method thereof - Google Patents
Multifunctional garlic-allium mongolicum regel composition and preparation method thereof Download PDFInfo
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Abstract
The invention discloses a multifunctional garlic allium mongolicum regel composition and a preparation method thereof, wherein the raw material medicines comprise the following components in parts by weight: 1-30 parts of garlic and 1-2 parts of allium mongolicum regel, wherein after the raw materials are extracted by ethanol and water, the composition comprises 3-40 parts of garlic extract and 1.2-5.3 parts of allium mongolicum regel extract, and further comprises 2.5-20 parts of garlic alcohol extract, 0.5-20 parts of garlic water extract, 0.7-4.3 parts of allium mongolicum regel alcohol extract and 0.5-1 part of allium mongolicum regel water extract. The composition has high biological activity, and has the activities of reducing blood sugar, resisting viruses and resisting prostate cancer.
Description
Technical Field
The invention belongs to the field of medicines, and particularly relates to a multifunctional garlic allium mongolicum regel composition and a preparation method thereof.
Background
Garlic is an underground bulb of a Liliaceae (Liliaceae) Allium (Allium) plant, contains abundant proteins, oligosaccharides and polysaccharides, and also contains fat, mineral substances and the like, can be used as a seasoning, can be used as a medicine, is a famous plant for both food and medicine, can play a role in disease prevention and health care after being eaten for a long time, has various biological activities, and is expected to be used for developing products for preventing or treating various diseases.
Allium mongolicum regel, also known as mongolian leek, is a liliaceae allium plant, grows in desert, sandy land or arid hillside with the altitude of 800-2800 meters, and is mainly distributed in Sinkiang (northeast), Qinghai (north), Gansu, Ningxia (north), Shanxi (north), inner Mongolia and Liaoning (west) in China.
Disclosure of Invention
The invention aims to provide a multifunctional garlic allium mongolicum regel composition which is high in biological activity and has the activities of reducing blood sugar, resisting influenza viruses and resisting prostate cancer.
The invention provides a composition, which comprises the following raw material medicines in parts by weight: 1-30 parts of garlic and 1-2 parts of allium mongolicum regel.
Furthermore, the raw material medicines of the composition comprise 2-4 parts of garlic and 1 part of allium mongolicum regel, and preferably comprise 2-3.8 parts of garlic and 1 part of allium mongolicum regel.
The invention also provides a preparation method of the composition, which comprises the following steps:
(1) taking raw material medicines according to parts by weight;
(2) taking the water extract and the alcohol extract of the garlic and the water extract and the alcohol extract of the allium mongolicum regel to prepare a product;
further, the alcohol of the alcohol extract is selected from one or more of methanol, ethanol, butanol and pentanol.
The alcohol of the alcohol extract not only comprises alcohol compounds such as methanol, ethanol, butanol, pentanol and the like or mixed alcohol, but also comprises aqueous solution of alcohol.
In a particular embodiment of the invention, the alcohol is selected from ethanol; further, the aqueous solution of ethanol is 60 to 100% v/v, preferably 70 to 90% v/v.
Further, garlic alcohol extract: the mass ratio of the garlic water extract is 1-5: 1, preferably 5: 1; the allium mongolicum regel alcohol extract: the mass ratio of the allium mongolicum regel aqueous extract is 1.4-5.4: 1, and preferably 3.4-5.4: 1.
The invention also provides a composition which comprises the following components in parts by weight: 3-40 parts of garlic extract, 1.2-5.3 parts of allium mongolicum regel extract, preferably 6-12 parts of garlic extract and 2.2-3.2 parts of allium mongolicum regel extract.
In a specific embodiment of the invention, the garlic extract is an alcohol extract and/or an aqueous extract of garlic, and the allium mongolicum regel extract is an alcohol extract and/or an aqueous extract of allium mongolicum regel.
Further, the alcohol of the alcohol extract is selected from one or more of methanol, ethanol, butanol and pentanol.
In a particular embodiment of the invention, the alcohol is selected from ethanol; further, the aqueous solution of ethanol is 60 to 100% v/v, preferably 70 to 90% v/v, for example, 70%, 80% or 90% ethanol.
In addition, in the extraction process, if the extraction is carried out for more than 2 times, the ethanol concentration in each extraction can be the same or different, for example, garlic is extracted for 3 times, and each extraction is carried out by using 80% ethanol water solution; or extracting Bulbus Allii for 3 times, sequentially extracting with 90% v/v, 80% v/v, and 70% v/v ethanol water solution; or sequentially extracting garlic by 70% v/v, 80% v/v and 90% v/v ethanol water solution; alternatively, garlic is sequentially extracted with 90% v/v, 70% v/v ethanol aqueous solution, and so on.
Extracting Allium mongolicum regel with 80% ethanol water solution for 3 times; or extracting Allium mongolicum regel for 3 times, sequentially extracting with 90% v/v, 80% v/v and 70% v/v ethanol water solution; or, sequentially extracting allium mongolicum regel by 70% v/v, 80% v/v and 90% v/v ethanol water solution; alternatively, allium mongolicum regel is sequentially extracted with 90% v/v, 70% v/v ethanol aqueous solution, and so on.
The extraction method of the invention can adopt the conventional extraction method of natural plant medicines, such as ultrasonic, reflux, decoction, microwave assistance, impregnation and the like.
Further, the composition comprises 2.5-20 parts of garlic alcohol extract, 0.5-20 parts of garlic water extract, 0.7-4.3 parts of allium mongolicum regel alcohol extract and 0.5-1 part of allium mongolicum regel water extract; preferably, the garlic oil comprises 5-10 parts of garlic alcohol extract, 1-2 parts of garlic water extract, 1.7-2.7 parts of allium mongolicum regel alcohol extract and 0.5 part of allium mongolicum regel water extract.
Further, the alcohol extract of garlic in the composition: the mass ratio of the garlic water extract is 1-5: 1, preferably 5: 1; the allium mongolicum regel alcohol extract: the mass ratio of the allium mongolicum regel aqueous extract is 1.4-5.4: 1, and preferably 3.4-5.4: 1.
Further, the composition comprises 5 parts of garlic alcohol extract, 1 part of garlic water extract, 1.7 parts of allium mongolicum regel alcohol extract and 0.5 part of allium mongolicum regel water extract;
or comprises 10 parts of garlic alcohol extract, 2 parts of garlic water extract, 2.7 parts of allium mongolicum regel alcohol extract and 0.5 part of allium mongolicum regel water extract.
The invention also provides a product comprising any of the compositions described above.
Further, the product may also comprise pharmaceutically acceptable excipients.
As used herein, "pharmaceutically acceptable" is meant to include any material that does not interfere with the effectiveness of the biological activity of the active ingredient and is not toxic to the host to which it is administered.
The pharmaceutically acceptable auxiliary materials are general names of all the additional materials except the main medicine in the medicine, and the auxiliary materials have the following properties: (1) no toxic effect on human body and few side effects; (2) the chemical property is stable and is not easily influenced by temperature, pH, storage time and the like; (3) has no incompatibility with the main drug, and does not influence the curative effect and quality inspection of the main drug; (4) does not interact with the packaging material. The auxiliary materials in the invention include, but are not limited to, a filler (diluent), a lubricant (glidant or anti-adhesion agent), a dispersing agent, a wetting agent, an adhesive, a regulator, a solubilizer, an antioxidant, a bacteriostatic agent, an emulsifier, a disintegrating agent and the like. The binder comprises syrup, acacia, gelatin, sorbitol, tragacanth, cellulose and its derivatives (such as microcrystalline cellulose, sodium carboxymethylcellulose, ethyl cellulose or hydroxypropyl methylcellulose), gelatin slurry, syrup, starch slurry or polyvinylpyrrolidone; the filler comprises lactose, sugar powder, dextrin, starch and its derivatives, cellulose and its derivatives, inorganic calcium salt (such as calcium sulfate, calcium phosphate, calcium hydrogen phosphate, precipitated calcium carbonate, etc.), sorbitol or glycine, etc.; the lubricant comprises superfine silica gel powder, magnesium stearate, talcum powder, aluminum hydroxide, boric acid, hydrogenated vegetable oil, polyethylene glycol and the like; the disintegrating agent comprises starch and its derivatives (such as sodium carboxymethyl starch, sodium starch glycolate, pregelatinized starch, modified starch, hydroxypropyl starch, corn starch, etc.), polyvinylpyrrolidone or microcrystalline cellulose, etc.; the wetting agent comprises sodium lauryl sulfate, water or alcohol, etc.; the antioxidant comprises sodium sulfite, sodium bisulfite, sodium pyrosulfite, dibutylbenzoic acid, etc.; the bacteriostatic agent comprises 0.5% of phenol, 0.3% of cresol, 0.5% of chlorobutanol and the like; the regulator comprises hydrochloric acid, citric acid, potassium (sodium) hydroxide, sodium citrate, and buffer (including sodium dihydrogen phosphate and disodium hydrogen phosphate); the emulsifier comprises polysorbate-80, sorbitan fatty acid, pluronic F-68, lecithin, soybean lecithin, etc.; the solubilizer comprises Tween-80, bile, glycerol, etc.
In a specific embodiment of the present invention, the pharmaceutically acceptable excipient is microcrystalline cellulose.
Optionally, the product is in a dosage form selected from the group consisting of a tablet, powder, granule, capsule, pill, emulsion, solution, suspension, syrup, and tincture.
In one embodiment of the invention, the product is a capsule.
The invention has the beneficial effects that:
(1) the invention provides a series of compositions consisting of garlic alcohol extract, garlic water extract, allium mongolicum regel alcohol extract and allium mongolicum regel water extract, and tests prove that the compositions can effectively inhibit the activity of alpha-glucosaccharase, inhibit virus replication or reproduction and keep the proliferation of prostate cancer cells, and can be used for preparing products for preventing and/or treating related diseases.
(2) The garlic and the allium mongolicum regel are both daily usable raw materials, and the garlic and the allium mongolicum regel are natural food extracts and have high safety.
Detailed Description
The technical solutions of the present invention are described clearly and completely below, and it is obvious that the described embodiments are some, not all embodiments of the present invention. All other embodiments, which can be derived by a person skilled in the art from the embodiments given herein without making any creative effort, shall fall within the protection scope of the present invention.
Example 1 preparation of extracts of Allium Sativum and Allium mongolicum
(1) Preparing the garlic alcohol extract: extracting dried Bulbus Allii powder with 90% v/v, 80% v/v, and 70% v/v ethanol under reflux for 3 times, filtering, collecting residue, mixing extractive solutions, recovering ethanol, and drying to obtain Bulbus Allii ethanol extract with an extract rate of 75.13 + -5%.
(2) Preparing garlic aqueous extract: and (2) taking the medicine residues in the step (1), adding water, decocting for 3 times, filtering, combining the filtrates, concentrating and drying to obtain the garlic water extract, wherein the paste yield is about 15.18 +/-2% by determination.
(3) Preparing the allium mongolicum regel alcohol extract: and (3) adding 90% v/v, 80% v/v and 70% v/v ethanol into the dry allium mongolicum regel powder dried to constant weight respectively, performing reflux extraction for 3 times, filtering, reserving dregs, merging extracting solutions, recovering ethanol, and drying to obtain the allium mongolicum regel ethanol extract, wherein the determined extraction rate is about 68.92 +/-5%.
(4) Preparing an allium mongolicum regel aqueous extract: and (2) taking the medicine residues in the step (1), adding water, decocting for 3 times, filtering, combining the filtrates, concentrating and drying to obtain the allium mongolicum regel water extract, wherein the paste yield is about 16.21 +/-2% by determination.
Example 2 Allium mongolicum compositions
And (3) uniformly mixing 5g of the garlic alcohol extract prepared in the example 1, 1g of the garlic water extract, 1.7g of the allium mongolicum regel alcohol extract and 0.5g of the allium mongolicum regel water extract to obtain the composition.
Example 3 Allium mongolicum compositions
Taking 10g of the garlic alcohol extract prepared in the example 1, 2g of the garlic water extract, 1.7g of the allium mongolicum regel alcohol extract and 0.5g of the allium mongolicum regel water extract, and uniformly mixing to obtain the composition.
Example 4 Allium mongolicum compositions
Taking 10g of the garlic alcohol extract prepared in the example 1, 2g of the garlic water extract, 2.7g of the allium mongolicum regel alcohol extract and 0.5g of the allium mongolicum regel water extract, and uniformly mixing to obtain the composition.
EXAMPLE 5 Allium mongolicum and allium mongolicum composition capsules
Taking 5g of the garlic alcohol extract, 1g of the garlic water extract, 1.7g of the allium mongolicum regel alcohol extract and 0.5g of the allium mongolicum regel water extract prepared in the example 1, adding a proper amount of microcrystalline cellulose, uniformly mixing, drying and encapsulating to obtain the capsule of the composition.
Example 6 alpha-glucosidase inhibitory Activity
The extracts in this example were prepared as described in example 1.
Measurement of α -glucosidase inhibitory activity:
the influence of the garlic extract and the allium mongolicum regel extract on the activity of the alpha-glucosidase is determined by adopting a 4-nitrophenol-alpha-D-glucopyranoside (PNPG) colorimetric method. Sequentially adding 50uL of extracts (20mg/mL) with different ratios and 100uL of alpha-glucosaccharase solution (5mg/mL) into a 96-well plate, uniformly mixing, and reacting at 25 ℃ for 10 min; adding 50uLPNPG solution (5mmol/L), and reacting at 37 deg.C for 10 min; finally 50uLNa is added2CO3And (3) mixing the solution (0.67mol/L), measuring the absorbance at the wavelength of 405nm, and calculating the inhibition rate. Acarbose was used as a positive control in this assay to add 100uL of alpha-glucosidase solution (5mg/mL), 50uLPNPG solution (5mmol/L) and 50uLNa to 50uL of phosphate buffer (pH 6.8)2CO3The solution (0.67mol/L) served as a control group; to 50uL of phosphate buffer (pH 6.8) were added 100uL of an alpha-glucosidase solution (5mg/mL), 50uL of phosphate buffer, and 50uLNa2CO3Solution (0.67mol/L) was used as control blank; to 50uL of garlic extract and allium mongolicum extract (20mg/mL), 100uL of alpha-glucosidase solution (5mg/mL), 50uL of phosphate buffer solution and 50uLNa were added2CO3The solution (0.67mol/L) served as a sample blank. The garlic extract and the allium mongolicum regel extract in different proportions can inhibit alpha-glucosidaseThe rate was measured and the hypoglycemic activity was evaluated, and the results are shown in Table 1.
TABLE 1 inhibition of alpha-glucosidase by different extracts
As can be seen from the data in Table 1, the garlic alcohol extract, the garlic water extract, the allium mongolicum regel alcohol extract and the allium mongolicum regel water extract all have the inhibition effect on alpha-glucosaccharase, but the inhibition effect is weaker; after the four components are combined, the inhibition effect on alpha-glucosaccharase is stronger than that of any single extract under the same dosage, which shows that the garlic alcohol extract, the garlic water extract, the allium mongolicum regel alcohol extract and the allium mongolicum regel water extract are combined to realize synergistic interaction, so that the inhibition activity of the extracts is improved, wherein the garlic alcohol extract: garlic water extract: the allium mongolicum regel alcohol extract: the allium mongolicum regel aqueous extract has the highest inhibitory activity when the allium mongolicum regel aqueous extract is 5.0:1.0:1.7:0.5, and can be used for preparing products for preventing and/or treating diseases taking alpha-glucosaccharase as a target.
Example 7 antiviral Activity
The extracts in this example were prepared as described in example 1.
Half of the cell infection was measured: influenza A virus A/PR/8/34(H1N1) was diluted to 10 gradient with cell maintenance medium-1~10-8Add to wash dog kidney cell line (MDCK) monolayers 3 times, add 100. mu.L virus to each well of MDCK cells in 5% CO2Adsorbing for 1h at 37 ℃ in an incubator, removing supernatant after infecting cells, washing for 5 times by PBS, adding 100 mu L of cell maintenance liquid into each hole, observing cytopathic effect after 72h, and recording the number and degree of cytopathic holes. Calculating by using Reed-Muench methodThe infection amount of the half cell is 10-4.1/0.1mL。
Inhibition of the extract: setting a normal cell control group, a virus control group, a positive control group and different compatible drug groups, adding 100 mu L/hole virus-free cell maintenance liquid into the normal cell control group, taking the cell maintenance liquid, diluting the extract to 0.5mg/mL, adding the diluted extract into the different compatible drug groups, respectively neutralizing the extract with influenza virus liquid in equal volume, incubating for 1h at 37 ℃, inoculating 100 mu L/hole into MDCK cells, and preparing 5 compatible holes. 5% CO2After culturing in an incubator at 37 ℃ for 48h, adding 20 μ L of 5g/LMTT into each well, measuring the OD value at 490nm, calculating the inhibition rate of different compatible extracts on viruses, and the results are shown in Table 2:
the virus inhibition rate%
Table 2 inhibition of different extracts on influenza infection of MDCK cells (n ═ 3)
As can be seen from the data in Table 2, the garlic alcohol extract, the garlic water extract, the allium mongolicum regel alcohol extract and the allium mongolicum regel water extract all have the inhibition effect on influenza viruses, but the inhibition effect is weaker; after the four extracts are combined, the effect of inhibiting the influenza virus is stronger than that of any single extract under the same dosage, which shows that the garlic alcohol extract, the garlic water extract, the allium mongolicum regel alcohol extract and the allium mongolicum regel water extract are combined to realize synergistic interaction, so that the inhibiting activity of the extracts is improved, wherein the garlic alcohol extract comprises the following components in percentage by weight: garlic water extract: the allium mongolicum regel alcohol extract: the allium mongolicum regel aqueous extract has the highest inhibitory activity when the allium mongolicum regel aqueous extract is 5.0:1.0:1.7:0.5, and can be used for preparing products for treating and/or preventing influenza.
Example 8 anti-prostate cancer Activity
The extracts in this example were prepared as described in example 1.
Detection of prostate cancer cell LNCaP proliferation: and detecting the proliferation of the prostate cancer cells LNCaP by adopting an Alamar-Blue method. Add 180. mu.L of prostate cancer cells LNCaP (5X 10) to 96-well plates4one/mL) suspensionLiquid, after 48h, 20 μ L of garlic extract and allium mongolicum regel extract (200ug/mL) with different proportions are added. And taking finasteride as a positive control and sterile water as a negative control, and arranging 3 multiple wells in each ratio. 5% CO at 37 ℃2Culturing for 48h, removing old culture medium by suction, adding 20 μ L Alamar Blue reagent (75ug/mL) and 180 μ L1640 culture medium, measuring absorbance at 570nm and 600nm after color change, and calculating the influence of different compatible extracts on LNCaP proliferation by formula, the result is shown in Table 3.
TABLE 3 inhibition of prostate cancer cells LNCaP by different extracts (n ═ 3)
As can be seen from the data in Table 3, the garlic alcohol extract, the garlic water extract, the allium mongolicum regel alcohol extract and the allium mongolicum regel water extract can inhibit the proliferation of prostate cancer cells to a certain extent, but the inhibition effect is weak; after the four components are combined, the inhibition effect on the proliferation of the prostate cancer cells is stronger than that of any single extract under the same dosage, which shows that the garlic alcohol extract, the garlic water extract, the allium mongolicum regel alcohol extract and the allium mongolicum regel water extract are combined to realize synergistic interaction, so that the inhibition activity of the extracts is improved, wherein the garlic alcohol extract: garlic water extract: the allium mongolicum regel alcohol extract: the allium mongolicum regel aqueous extract has the highest inhibitory activity when the allium mongolicum regel aqueous extract is 10.0:2.0:2.7:0.5, and can be used for preparing products for treating and/or preventing prostate cancer.
The above description is only an embodiment of the present invention, and not intended to limit the scope of the present invention, and all modifications of equivalent structures and equivalent processes, which are made by the present specification, or directly or indirectly applied to other related technical fields, are included in the scope of the present invention.
Claims (10)
1. The composition is characterized in that the raw material medicines comprise the following components in parts by weight: 1-30 parts of garlic and 1-2 parts of allium mongolicum regel.
2. The composition according to claim 1, comprising 2-4 parts of garlic and 1 part of allium mongolicum regel, preferably comprising 2-3.8 parts of garlic and 1 part of allium mongolicum regel.
3. A process for the preparation of a composition according to claim 1 or 2, characterized in that it comprises the following steps:
(1) taking raw material medicines according to parts by weight;
(2) taking the water extract and the alcohol extract of the garlic and the water extract and the alcohol extract of the allium mongolicum regel to prepare a product;
further, the alcohol of the alcohol extract is selected from one or more of methanol, ethanol, butanol and pentanol, preferably ethanol; further, the aqueous solution of ethanol is 60 to 100% v/v, preferably 70 to 90% v/v.
4. The preparation method according to claim 3, wherein the alcohol extract of garlic: the mass ratio of the garlic water extract is 1-5: 1, preferably 5: 1; the allium mongolicum regel alcohol extract: the mass ratio of the allium mongolicum regel aqueous extract is 1.4-5.4: 1, and preferably 3.4-5.4: 1.
5. The composition is characterized by comprising the following components in parts by weight: 3-40 parts of garlic extract, 1.2-5.3 parts of allium mongolicum regel extract, preferably 6-12 parts of garlic extract and 2.2-3.2 parts of allium mongolicum regel extract;
further, the garlic extract is a garlic alcohol extract and/or a garlic water extract, and the allium mongolicum regel extract is an allium mongolicum regel alcohol extract and/or an allium mongolicum regel water extract;
further, the alcohol of the alcohol extract is selected from one or more of methanol, ethanol, butanol and pentanol, preferably ethanol; further, the aqueous solution of ethanol is 60 to 100% v/v, preferably 70 to 90% v/v.
6. The composition of claim 5, which comprises 2.5-20 parts of alcohol extract of garlic, 0.5-20 parts of water extract of garlic, 0.7-4.3 parts of alcohol extract of allium mongolicum regel and 0.5-1 part of water extract of allium mongolicum regel; preferably, the garlic oil comprises 5-10 parts of garlic alcohol extract, 1-2 parts of garlic water extract, 1.7-2.7 parts of allium mongolicum regel alcohol extract and 0.5 part of allium mongolicum regel water extract.
7. The composition of claim 6, wherein the alcohol extract of garlic: the mass ratio of the garlic water extract is 1-5: 1, preferably 5: 1; the allium mongolicum regel alcohol extract: the mass ratio of the allium mongolicum regel aqueous extract is 1.4-5.4: 1, and preferably 3.4-5.4: 1.
8. The composition of claim 6, comprising 5 parts of alcohol extract of garlic, 1 part of water extract of garlic, 1.7 parts of alcohol extract of allium mongolicum regel and 0.5 part of water extract of allium mongolicum regel;
or comprises 10 parts of garlic alcohol extract, 2 parts of garlic water extract, 2.7 parts of allium mongolicum regel alcohol extract and 0.5 part of allium mongolicum regel water extract.
9. A product comprising the composition of any one of claims 1, 2, 5 to 8; further, pharmaceutically acceptable auxiliary materials are also included; further, the pharmaceutically acceptable auxiliary material is microcrystalline cellulose.
10. The composition according to claim 9, wherein the product is in a dosage form selected from the group consisting of a tablet, a powder, a granule, a capsule, a pill, an emulsion, a solution, a suspension, a syrup, and a tincture, and further a capsule.
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Publication number | Priority date | Publication date | Assignee | Title |
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CN113995136A (en) * | 2021-12-06 | 2022-02-01 | 南京晓庄学院 | Efficient extraction method of allium mongolicum regel extract and allium mongolicum regel extract preparation |
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