CN112386642A - Large fan blade extract and preparation method and application thereof - Google Patents

Large fan blade extract and preparation method and application thereof Download PDF

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CN112386642A
CN112386642A CN202011443420.9A CN202011443420A CN112386642A CN 112386642 A CN112386642 A CN 112386642A CN 202011443420 A CN202011443420 A CN 202011443420A CN 112386642 A CN112386642 A CN 112386642A
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苏启表
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Guangdong Pharmaceutical University
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Abstract

The invention discloses a large fan blade extract, a preparation method and application thereof, wherein the large fan blade is callicarpa macrophylla of callicarpaceae plantCallicarpa macrophylla VahlThe large fan blade extract is an ethanol elution part of a large fan blade water extract, and the extraction method comprises the following steps: crushing a large fan blade into fine powder, adding a proper amount of water, heating and extracting for 2-4 times, collecting an extracting solution, and concentrating to 1.0-1.2 g/m; and performing column chromatography separation on the concentrated solution by using a silica gel chromatographic column, performing gradient elution by using ethanol with different concentrations as a mobile phase, collecting each eluate, and concentrating to obtain an extract. The large fan blade extract can be applied to the preparation of medicines for treating/preventing hyperuricemia and related diseases or having the function of regulating uric acid. The invention discovers for the first time that the large fan blade extract has obvious activity of regulating uric acid, has patent medicine potential for preparing a medicinal preparation for preventing or treating hyperuricemia and related diseases thereof, and has simple preparation method, low cost and good patent medicine economic benefit.

Description

Large fan blade extract and preparation method and application thereof
Technical Field
The invention belongs to the technical field of traditional Chinese medicines, and particularly relates to a large fan blade extract as well as a preparation method and application thereof.
Background
Uric acid is the terminal metabolite of human purine compounds, and disorders of purine metabolism lead to Hyperuricemia (HUA). Hyperuricemia refers to the condition that under the normal purine diet state, the level of uric acid in non-bidaily fasting blood is higher than 420 mu mol/L in male, and higher than 360 mu mol/L in female, namely hyperuricemia is called. Gout (gout) is a group of metabolic diseases caused by excessive uric acid production caused by purine metabolic disorder and/or reduction of uric acid excretion to increase uric acid level and form uric acid crystals deposited on joints, soft tissues, kidneys and the like. Hyperuricemia is generally considered a hallmark of gout, and it is statistically estimated that about 5% to 12% of patients with hyperuricemia may eventually develop gout. In addition, recent studies have found that hyperuricemia is not only the most important biochemical basis of gout, but also is closely related to the occurrence of hypertension, hyperlipidemia, atherosclerosis, obesity, insulin resistance, nephropathy, inflammation, the severity of infectious diseases, tumor lysis syndrome, climacteric syndrome, organ transplantation complications and certain problematic conditions (obstructive sleep apnea, primary sicca syndrome, etc.), so that control of hyperuricemia is of great significance for the treatment of severe metabolic diseases such as gout and the like and diseases related thereto.
Currently, drugs for clinical use against hyperuricemia are mainly concerned with both reducing uric acid production and increasing uric acid excretion. The medicine for reducing the uric acid generation comprises a Xanthine Oxidase (XOD) inhibitor, which mainly comprises allopurinol, but the allopurinol can cause adverse reactions such as allergy, liver and kidney damage, bone marrow suppression and the like, and limits the clinical application of the medicine to a certain extent. fexbuxostat is a xanthine oxidase/dehydrogenase selective inhibitor, has better safety than allopurinol for patients with moderate renal injury, and also has adverse reactions reported such as abnormal liver function, gastrointestinal reaction, arthralgia, eruption and the like. The uricosuric drugs comprise probenecid, metconazole, benzbromarone and the like, and act on a urate transporter of a renal proximal convoluted tubule so as to inhibit the reabsorption of uric acid. Recent studies have found that benzbromarone is at risk of causing fulminant hepatitis. Therefore, the research on the anti-hyperuricemia drugs with high efficiency and low toxicity is urgent. Researches in recent years find that the traditional Chinese medicine also has a good effect on treating hyperuricemia and shows little or no toxic and side effects. Such as: patent CN100464767C discloses a pharmaceutical composition which is composed of 1-8 parts of astragalus extract, 0.3-3 parts of ash bark extract and 0.1-2 parts of tea extract by weight and auxiliary components allowed in the medicine, and can control acute attack of gouty arthritis and treat hyperuricemia and chronic uric acid nephropathy for a long time, relieve arthralgia and promote uric acid excretion, and has small toxic and side effects. Patent CN106822331B discloses litchi rind extract mainly containing polymer polyphenol with locked state can effectively reduce uric acid level in blood serum, and can be used for preparing medicine for treating hyperuricemia and related diseases. Patent CN104983758B discloses that fructus terminaliae billericae extract and fructus terminaliae billericae polyphenol have the activity of inhibiting xanthine oxidase, can effectively reduce the uric acid concentration in the blood of a hyperuricemia model mouse, have the effect of treating hyperuricemia, and simultaneously have the effect of treating hyperuricemia related metabolic disorders: the gout can have better curative effect. And so on. Therefore, the extract of a large number of Chinese medicinal materials or the Chinese medicinal compound preparation has the patent medicine potential for preparing the medicament for treating the hyperuricemia, and the Chinese medicinal material has the advantages of small side effect, strong comprehensive treatment capacity and the like, so that the development of the new application of the Chinese medicinal material extract actively explores a potential medicament target of a new medicament for treating the hyperuricemia, and the search for a novel medicament for treating the hyperuricemia is an important problem which needs to be solved clinically at present.
The large fan blade is of Verbenaceae of CallicarpaPlant Callicarpa macrophyllaCallicarpa macrophylla VahlThe whole plant of (1) is mainly produced in Guangdong, Guangxi, etc. The beautyberry plant has more than 190 kinds, about 46 kinds of Chinese, 30 kinds of Chinese can be used as medicine, 24 kinds of Chinese have hemostatic effect, and at present, most of Chinese and foreign research is Dunhua (Rainbow flower)Callicarpa formosana Rolfe) Callicarpa nudiflora (A. nudiflora)Callicarpa nudiflora Hook. et Arn.) Zizhu (A. beautyberry)Callicarpa bodinieri Levl.) Root of common Callicarpa (Callicarpa arborea) Although most of callicarpa plants have the hemostatic effect, the medicinal components contained in the callicarpa plants are different due to different plants, so that the callicarpa plants are distinguished during use, and the influence on the medicinal effect or the health or even life endangering caused by wrong administration of the callicarpa plants is avoided. The product has mild nature, pungent and bitter taste, and contains condensed tannin, flavonoids, neutral resin, saccharides, hydroxyl compounds, magnesium, calcium, trace iron salt, etc.; has hemostatic, analgesic, blood stasis dispelling, and antiinflammatory effects; can be used for treating epistaxis, hemoptysis, gastrointestinal hemorrhage, tooth hemorrhage, metrorrhagia, traumatic injury, rheumatalgia, upper respiratory infection, and tonsillitis.
The existing research on the large fan blade mainly focuses on the aspects of crude drug identification, chemical component analysis, active component extraction, hemostasis and blood coagulation and the like. Callicarpa macrophylla can treat hemorrhage of different parts, the hemostasis mechanism is different, and the mechanism of treating nephritis hematuria is to further inhibit the immunoinflammatory reaction by reducing the level of serum IL-1, so as to relieve the hematuria symptom of a nephritis model rat (Lishulan, Liwenhui, Liubaosheng, Callicarpa macrophylla has influence on urine red blood cells and serum IL-1 of the nephritis hematuria model rat [ J ], (Western medicine) No. 9 year 2010). The Callicarpa macrophylla Total Flavonoids (Total Flavonoids from Callicarpa macrophylla, TFCM) has a certain in vitro antioxidant activity, can be used for inhibiting the injury of SH-SY5Y cells induced by rotenone, and the mechanism of the Total Flavonoids (Lily glume. the antioxidant activity of the Callicarpa macrophylla Total Flavonoids and the research on the mechanism of resisting SH-SY5Y cell injury induced by rotenone [ D ], 2015-Wuhan university: biology) is probably related to oxidative stress, up-regulation of apoptosis related gene Mcl-1 and down-regulation of clear caspase-3 expression. The callicarpa maxima water decoction can play a role in hemostasis by activating endogenous and exogenous coagulation systems and regulating the levels of TXB2 and 6-keto-PGF1a (Lu He., influence of callicarpa maxima on the coagulation function of rats and the expression of TXB2 and 6-keto-PGF1a [ D ], (report of Chinese medicine science) 6 years 2017). Patent CN 107383149B discloses a method for rapidly extracting ursolic acid and pulegone from beautyberry, which comprises the steps of crushing beautyberry, extracting with alcohol, extracting with petroleum ether, adsorbing with macroporous resin column, crystallizing and recrystallizing to obtain pure products of ursolic acid and pulegone. Patent application CN 104887865 a discloses a traditional Chinese medicine composition for treating gout, which is prepared from the following raw material medicines in parts by weight: 12-16 parts of honeysuckle stem; 9-17 parts of Acer truncatum; 6-12 parts of polyporus umbellatus; 14-18 parts of clematis; 7-11 parts of daphne leaf; 5-10 parts of fox meat; 12-15 parts of nux vomica; 8-17 parts of murraya paniculata root; 7-15 parts of photinia root; adenophora trachelioides 9-13; 11-16 parts of Chinese starjasmine stem; 8-13 parts of Damnacanthus; 7-12 of a sweetgum fruit; 12-15 of callicarpa; 6-10 parts of Curculigo latifolia. Patent application CN 104887866 a discloses a traditional Chinese medicine prescription for treating gout, which is prepared from the following raw material medicines in parts by weight: 12-16 parts of cape jasmine; 8-17 parts of clematis; 9-19 parts of daphne leaf; 8-13 parts of fox meat; 7-12 of a sweetgum fruit; 11-15 parts of murraya paniculata root; 6-12 parts of polyporus umbellatus; 11-16 parts of juniper; 9-13 parts of callicarpa; 9-17 parts of Chinese starjasmine stem; 12-15 parts of Damnacanthus indicus; 7-15 parts of photinia serrulata; 6-10 parts of nux vomica; 7-11 parts of ligusticum; 10-16 parts of curculigo majorana. In the above two patent application documents, it is mentioned that the Zizania latifolia can be used in the Chinese herbal preparation for treating gout, but in the two formula preparations, the Zizania latifolia only plays a role of adjuvant therapy, and in the documents, it is mentioned that the Zizania latifolia has hemostatic and antibacterial effects, and the disease mechanism analysis of the obtained Chinese herbal preparation is not performed. Therefore, at present, there is no research on whether the large fan blade has activities of regulating uric acid and treating hyperuricemia/gout, and at present, there are few researches on drug effect and application of the large fan blade, so how to enlarge and use the large fan blade to generate the maximum efficacy and exert the corresponding efficacy is still the main direction of medical research.
Disclosure of Invention
The invention aims to provide a large fan blade extract, a preparation method and application thereof, the invention discovers for the first time that the large fan blade extract has obvious activity of regulating uric acid, has patent medicine potential of preparing a medicinal preparation for preventing or treating hyperuricemia and related diseases thereof, and the medicinal preparation has simple preparation method, low cost and good patent medicine economic benefit.
In order to achieve the purpose, the invention adopts the following technical scheme:
the application of the large fan blade extract in preparing medicines for treating/preventing hyperuricemia and related diseases or medicines with function of regulating uric acid.
The preparation method of the large fan blade extract comprises the following steps:
(1) crushing a large fan blade into fine powder, adding a proper amount of water, heating and extracting for 2-4 times, collecting an extracting solution, and concentrating to 1.0-1.2 g/mL;
(2) performing column chromatography separation on the concentrated solution by using a silica gel chromatographic column, performing gradient elution by using ethanol with different concentrations as a mobile phase, collecting each eluate, and concentrating to obtain an extract, namely the large fan blade extract.
The specific extraction method in the step (1) comprises the following steps:
(1) crushing a large fan blade into fine powder, adding distilled water with the mass of 6-8 times of that of the large fan blade, soaking for 40-80 min, heating to 80-100 ℃, extracting for 40-80 min, filtering, and collecting filtrate;
(2) adding 6-8 times of distilled water into the filter residue, heating to 80-100 ℃, extracting for 40-80 min, filtering, and collecting the filtrate;
(3) and repeatedly extracting the filter residue for 1-3 times, combining the filtrates obtained by multiple extraction, and concentrating to 1.0-1.2 g/mL to obtain the water extract of the large fan blade.
The ethanol with different concentrations is ethanol with volume concentration of 0-95%. Selecting a plurality of gradient eluents with the concentration of 0-95% by volume.
Preferably, the different concentrations of ethanol are 0%, 30%, 60%, 75%, 95% ethanol by volume.
Preferably, the large fan blade extract obtained by eluting with 30-75% ethanol by volume concentration is selected to prepare the medicine for treating/preventing hyperuricemia and related diseases thereof or the medicine with function of regulating uric acid.
The hyperuricemia and related diseases are one or more of hypertension, hyperlipidemia, atherosclerosis, obesity, insulin resistance, nephropathy, inflammation, infectious diseases, tumor lysis syndrome, climacteric syndrome, organ transplantation complications, obstructive sleep apnea and primary sicca syndrome caused by uric acid metabolic disorder.
The large fan blade extract is selectively added with conventional auxiliary materials and prepared into a clinically acceptable pharmaceutical preparation for treating/preventing hyperuricemia and related diseases or having the function of regulating uric acid according to a conventional process.
The preparation comprises tablets, capsules, dripping pills, granules and the like.
The conventional adjuvants include more than one of starch, lactose, microcrystalline cellulose, dextrin, calcium phosphate, polyethylene glycol-4000, polyethylene glycol-6000, sodium carboxymethylcellulose, hydroxypropyl cellulose or crospovidone, etc.
The invention has the beneficial effects that:
1. the invention discovers for the first time that the large fan blade extract has obvious activity of regulating uric acid, has the patent medicine potential of preparing a medicinal preparation for preventing or treating hyperuricemia and related diseases thereof, provides a new material basis for developing an anti-hyperuricemia innovative medicine, and has potential and huge social and economic benefits.
2. The large fan blade has rich resources, is convenient and easy to obtain, and can be used for preparing a large amount of large fan blade extracts. Although the water extract or the alcohol extract of the large fan blade also has certain activity for resisting hyperuricemia when the dosage is high, the dosage is large and the activity is low, therefore, in the preparation method of the large fan blade, the large fan blade is subjected to water extraction and combination of extracting solutions for many times to obtain the water extract of the large fan blade, then the water extract of the large fan blade is eluted by ethanol with different concentrations to obtain different eluting parts, and finally the parts with obvious curative effects on hyperuricemia and related diseases are collected, so that the activity of regulating uric acid of the finally obtained large fan blade extract and the pharmaceutical preparation thereof is greatly improved; and the whole extraction and preparation method is simple and easy to implement, low in cost, small in pollution, beneficial to large-scale production under the conditions of energy conservation and emission reduction, and good in industrialization prospect.
3. The influence of the large fan blade extract on the level of uric acid in serum of a mouse with hyperuricemia caused by hypoxanthine and the influence of the large fan blade extract on the toe swelling of a rat induced by sodium urate are researched respectively, so that the large fan blade extract disclosed by the invention has obvious activity of regulating uric acid on the hyperuricemia.
4. The large fan blade extract also has the effects of stopping bleeding, relieving pain, removing blood stasis and diminishing inflammation, can be used for treating symptoms such as epistaxis, hemoptysis, gastrointestinal hemorrhage, tooth extraction hemorrhage, metrorrhagia, traumatic swelling and pain, rheumatic osteodynia, upper respiratory infection, tonsillitis and the like, and can play a role in treating other complications while preventing or treating hyperuricemia or gout.
5. The large fan blade extract and auxiliary materials are mixed to prepare tablets, capsules, dripping pills, granules and the like, the preparations are convenient to take, can be taken alone or matched with other medicaments, and can be taken orally to quickly convey the medicine property to the disease part through blood for effective treatment.
Detailed Description
In order to describe the present invention in more detail, the present invention will be further described with reference to the following examples.
Example 1 preparation of aqueous extract of Blume
Pulverizing large fan blade into fine powder, collecting 1kg of the large fan blade fine powder, soaking in 6L distilled water for 60min, heating to 80 deg.C, extracting for 60min, filtering, and collecting filtrate; adding 6L distilled water into the residue, heating to 80 deg.C, extracting for 60min, filtering, and collecting filtrate; adding 6L distilled water into the residue, heating to 80 deg.C, extracting for 60min, filtering, and collecting filtrate; and combining the extracting solutions for 3 times, and concentrating to 1.0-1.2 g/mL to obtain the compound.
Example 2 preparation of aqueous extract of Large Fan blades
Pulverizing large fan blade into fine powder, collecting 1kg of the large fan blade fine powder, soaking in 7L of distilled water for 60min, heating to 90 deg.C, extracting for 60min, filtering, and collecting filtrate; adding 7L distilled water into the residue, heating to 90 deg.C, extracting for 60min, filtering, and collecting filtrate; adding 7L distilled water into the residue, heating to 90 deg.C, extracting for 60min, filtering, and collecting filtrate; and combining the extracting solutions for 3 times, and concentrating to 1.0-1.2 g/mL to obtain the compound.
Example 3 preparation of aqueous extract of Large Fan blades
Pulverizing large fan blade into fine powder, collecting 1kg of the large fan blade fine powder, soaking in 8L of distilled water for 60min, heating to 98 deg.C, extracting for 60min, filtering, and collecting filtrate; adding 8L distilled water into the residue, heating to 98 deg.C, extracting for 60min, filtering, and collecting filtrate; adding 8L distilled water into the residue, heating to 98 deg.C, extracting for 60min, filtering, and collecting filtrate; and combining the extracting solutions for 3 times, and concentrating to 1.0-1.2 g/mL to obtain the compound.
Example 4 preparation of aqueous extract of Large Fan blades
Pulverizing large fan blade into fine powder, collecting 1kg of the large fan blade fine powder, soaking in 8L of distilled water for 80min, heating to 80 deg.C, extracting for 80min, filtering, and collecting filtrate; adding 7L distilled water into the residue, heating to 90 deg.C, extracting for 60min, filtering, and collecting filtrate; adding 6L distilled water into the residue, heating to 98 deg.C, extracting for 40min, filtering, and collecting filtrate; and combining the extracting solutions for 3 times, and concentrating to 1.0-1.2 g/mL to obtain the compound.
Example 5 preparation of ethanol elution part of Large Fan blade Water extract
Taking the concentrated solution of the aqueous extract of the large fan blade prepared by the preparation method of the embodiment 2, performing column chromatography separation by using a silica gel chromatographic column, sequentially performing gradient elution by using ethanol with volume concentration of 0%, 5%, 10%, 15%, 20%, 25%, 30%, 35%, 40%, 45%, 50%, 55%, 60%, 65%, 70%, 75%, 80%, 85%, 90% and 95% as a mobile phase, and respectively collecting each eluate and concentrating the eluate to obtain an extract, thereby obtaining the large fan blade extract.
Example 6 preparation of ethanol elution part of Large Fan blade Water extract
Taking the concentrated solution of the large fan blade water extract prepared by the preparation method of the embodiment 2, performing column chromatography separation by using a silica gel chromatographic column, sequentially performing gradient elution by using ethanol with volume concentrations of 0%, 15%, 30%, 45%, 60%, 75% and 90% as a mobile phase, and respectively collecting each eluate and concentrating the eluate to an extract to obtain the large fan blade extract.
Example 7 preparation of ethanol elution fraction of aqueous extract of Blume flabellum
Taking the concentrated solution of the large fan blade water extract prepared by the preparation method of the embodiment 2, performing column chromatography separation by using a silica gel chromatographic column, sequentially performing gradient elution by using ethanol with volume concentrations of 0%, 30%, 60%, 75% and 95% as a mobile phase, and respectively collecting eluates and concentrating the eluates into extractum to obtain the large fan blade extract.
Example 8 preparation of ethanol elution fraction of aqueous extract of Blume flabellum
Taking the concentrated solution of the large fan blade water extract prepared by the preparation method of the embodiment 2, performing column chromatography separation by using a silica gel chromatographic column, sequentially performing gradient elution by using ethanol with volume concentrations of 15%, 35%, 55%, 75% and 95% as a mobile phase, and respectively collecting eluates and concentrating the eluates into extractum to obtain the large fan blade extract.
EXAMPLE 9 preparation of Large leaf alcohol extract
Pulverizing large fan blade into fine powder, collecting 1kg of the large fan blade fine powder, soaking in 6L of 60% ethanol for 60min, heating under reflux for extracting for 60min, filtering, and collecting filtrate; adding 6L of 60% ethanol into the residue, heating, reflux extracting for 60min, filtering, and collecting filtrate; adding 6L of 60% ethanol into the residue, heating, reflux extracting for 60min, filtering, and collecting filtrate; mixing the extractive solutions for 3 times, concentrating, and recovering ethanol to obtain paste.
EXAMPLE 10 preparation of Large leaf extract tablet
[ prescription ] the 60% ethanol elution part (corresponding to 3.5kg of the medical herb of the large fan blade) of the large fan blade water extract prepared by the method of example 7 and 600g of dry starch are taken;
[ PREPARATION METHOD ] mixing the 60% ethanol elution part of the large fan blade water extract and dry starch uniformly, adding a proper amount of sodium carboxymethylcellulose and talcum powder, granulating, drying, pressing into 1000 tablets, and obtaining large fan blade extract tablets, wherein each tablet contains 3.5g of large fan blades.
The above-mentioned dry starch, sodium carboxymethylcellulose and talc powder are all commercially available.
EXAMPLE 11 preparation of Large leaf extract Capsule
[ prescription ] the 60% ethanol elution part (corresponding to 3.5kg of the medical herb of the large fan blade) of the large fan blade water extract prepared by the method of example 7 and 600g of dry starch are taken;
[ PREPARATION METHOD ] mixing the 60% ethanol elution part of the water extract of the large fan blade with dry starch, adding a proper amount of sodium carboxymethylcellulose and talcum powder, granulating, drying, and encapsulating into 1000 capsules, wherein each capsule contains 3.5g of large fan blade.
The above-mentioned dry starch, sodium carboxymethylcellulose and talc powder are all commercially available.
Example 12 preparation of Large leaf extract granules
The 60% ethanol elution part (corresponding to 10kg of the medical herb of the large fan blade) of the water extract of the large fan blade prepared by the method of the embodiment 7 and 1kg of dry starch are taken;
mixing the 60% ethanol elution part of the water extract of the large fan blade with dry starch, adding appropriate amount of sodium carboxymethylcellulose and pulvis Talci, granulating, drying, and packaging into 1000 bags containing 10g of large fan blade.
The above-mentioned dry starch, sodium carboxymethylcellulose and talc powder are all commercially available.
Test of drug Property
In order to verify the activity of the large fan blade extract of the invention in regulating uric acid, the applicant carried out the following tests:
1. influence of large leaf extract on serum uric acid level of mice with hyperuricemia caused by hypoxanthine
And (3) testing the sample: the large fan blade water extracts are the large fan blade water extracts prepared by the method in the embodiment 2, the large fan blade alcohol extracts are the large fan blade alcohol extracts prepared by the method in the embodiment 9, and the large fan blade extracts are 60% ethanol elution parts of the large fan blade water extracts prepared by the method in the embodiment 7.
The treatment method comprises the following steps: 120 mice, randomly divided into 12 groups of 10 mice each, namely a normal group, a model group, a positive control group (allopurinol 20 mg.kg)-1) High, medium and low dose groups of large fan blade extract (respectively equivalent to 10g.kg of large fan blade medicinal material)-1、5g.kg-1And 2.5g.kg-1) Big fan bladeHigh, medium and low dosage groups of water extract (respectively equivalent to 20g.kg of large fan blade medicinal material)-1、10g.kg-1And 5g.kg-1) High, medium and low dose groups of large fan blade alcohol extract (respectively equivalent to 20g.kg of large fan blade medicinal material)-1、10g.kg-1And 5g.kg-1) Gavage was performed 1 time per day, and equal volume of distilled water was gavage for 12 consecutive days in the normal group and the model group. After the last administration for 1h, except the normal group, the other groups were administered with hypoxanthine 0.4g.kg by gavage-12.5h later, blood was collected from the eyeballs of mice in each group at 3000r.min-1Centrifuging for 10min, collecting serum, and determining serum uric acid content by phosphotungstic acid colorimetric method.
As a result: as shown in table 1, compared with the model group, the serum uric acid levels of mice in the large leaf extract high and medium dose groups and the large leaf water extract high and large leaf alcohol extract high dose groups were significantly reduced, and the comparison was statistically significant (P < 0.05).
Figure 994590DEST_PATH_IMAGE001
2. Influence of the extract of the Blumeae folium on the toe swelling of rats induced by sodium urate
And (3) testing the sample: the large fan blade water extracts are the large fan blade water extracts prepared by the method in the embodiment 2, the large fan blade alcohol extracts are the large fan blade alcohol extracts prepared by the method in the embodiment 9, and the large fan blade extracts are 60% ethanol elution parts of the large fan blade water extracts prepared by the method in the embodiment 7.
The treatment method comprises the following steps: 90 rats were randomly divided into 9 groups of 10 rats, i.e., normal group, model group, and positive control group (colchicine 0.5 mg.kg)-1) The high and low dose groups of the large fan blade extract (respectively equal to 10g.kg of the large fan blade medicinal material)-1And 2.5g.kg-1) The high and low dosage groups of the large fan blade water extract (respectively equal to 10g.kg of the large fan blade medicinal material)-1And 2.5g.kg-1) The high and low dose groups of the large fan blade alcohol extract (respectively equal to 10g.kg of the large fan blade medicinal material)-1And 2.5g.kg-1) Administration by intragastric administrationEqual volume of distilled water was gavaged 1 time per day for 12 consecutive days in the normal and model groups. After 1 hour of the last administration, 0.15mL of physiological saline was subcutaneously injected to the right hind sole of the rat in the normal group, and 0.15mL of sodium urate (100 g.L) was subcutaneously injected to the right hind sole of the rat in each of the other groups-1) For inflammation, the circumference of the right hind paw of the rat was measured before and after injection. The swelling condition and the circumference of the right hind foot sole of the rat at 3, 4, 5 and 6h after the injection are observed and measured, and the swelling rate is calculated.
Footpad swelling rate =100 (-t time circumference-t)0Time circumference)/t0The time circumference.
As a result: as shown in Table 2, the toe swelling rate of the model rats was significantly increased compared to the control group; compared with the model group, the swelling rate of rats in the large fan blade extract high-dose group (the dose is 10g of medicinal materials) after model building is obviously reduced in 3 and 4 hours, and the swelling rate of rats in the large fan blade extract low-dose group (the dose is 2.5g of medicinal materials) after model building is obviously reduced in 4 hours; the swelling rate of the rats in the large leaf alcohol extract high-dose group (10 g of medicinal material) after molding for 4 hours is remarkably reduced, and the difference has statistical significance (P is less than 0.05). The large fan blade water extract low-dose group (the dose is 2.5g of medicinal materials) and the large fan blade alcohol extract low-dose group (the dose is 2.5g of medicinal materials) have no obvious influence.
Figure 915273DEST_PATH_IMAGE002
The above description is only a preferred embodiment of the present invention and is not intended to limit the present invention, and various modifications and changes may be made by those skilled in the art. Any modification, equivalent replacement, or improvement made within the spirit and principle of the present invention should be included in the protection scope of the present invention.

Claims (9)

1. The application of the large fan blade extract in preparing medicines for treating/preventing hyperuricemia and related diseases or medicines with function of regulating uric acid.
2. The use of claim 1, wherein the Blumeae folium is a whole plant of Callicarpa macrophylla of Verbenaceae of Callicarpa, and the Blumeae folium extract is prepared by the following steps:
(1) crushing a large fan blade into fine powder, adding a proper amount of water, heating and extracting for 2-4 times, collecting an extracting solution, and concentrating to 1.0-1.2 g/mL;
(2) performing column chromatography separation on the concentrated solution by using a silica gel chromatographic column, performing gradient elution by using ethanol with different concentrations as a mobile phase, collecting each eluate, and concentrating to obtain an extract, namely the large fan blade extract.
3. The use of claim 2, wherein the specific extraction method in step (1) is as follows:
(1) crushing the large fan blades into fine powder, adding distilled water with the mass of 6-8 times of that of the large fan blades, soaking for 40-80 min, heating to 80-100 ℃, extracting for 40-80 min, filtering, and collecting filtrate;
(2) adding 6-8 times of distilled water into the filter residue, heating to 80-100 ℃, extracting for 40-80 min, filtering, and collecting the filtrate;
(3) and repeatedly extracting the filter residue for 1-3 times, combining the filtrates obtained by multiple extraction, and concentrating to 1.0-1.2 g/mL to obtain the water extract of the large fan blade.
4. The use according to claim 2, wherein the ethanol concentration in step (2) is in the range of 0 to 95% by volume.
5. Use according to claim 4, characterized in that the ethanol has a concentration by volume of 0%, 30%, 60%, 75%, 95%.
6. The use of the extract as claimed in claim 4 or 5, wherein the extract is obtained by eluting with 30-75% ethanol.
7. The use according to claim 1, wherein the hyperuricemia and related disorders are one or more of hypertension, hyperlipidemia, atherosclerosis, obesity, insulin resistance, nephropathy, inflammation, infectious diseases, tumor lysis syndrome, climacteric syndrome, organ transplantation complications, obstructive sleep apnea and primary sicca syndrome caused by dysregulation of uric acid metabolism.
8. The use as claimed in claim 6, wherein the extract of Blumeae folium is optionally added with conventional adjuvants, and made into clinically acceptable pharmaceutical preparations for treating/preventing hyperuricemia and related diseases or regulating uric acid function according to conventional process.
9. The use according to claim 8, wherein the formulation comprises a tablet, capsule, drop pill or granule.
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Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104887866A (en) * 2015-07-03 2015-09-09 李军 Traditional Chinese medicine for treating gout

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Publication number Priority date Publication date Assignee Title
CN104887866A (en) * 2015-07-03 2015-09-09 李军 Traditional Chinese medicine for treating gout

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刘小颖: "大叶紫珠总黄酮抗氧化活性及抗鱼藤酮诱导的SH-SY5Y细胞损伤机制的研究", 《中国优秀硕士学位论文全文数据库 医药卫生科技辑（2015年）》 *
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