CN102038190A - Application of ampelopsin to preparation of anti-mutagenic health-care foods and medicaments - Google Patents
Application of ampelopsin to preparation of anti-mutagenic health-care foods and medicaments Download PDFInfo
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Abstract
The invention discloses application of ampelopsin to preparation of anti-mutagenic health-care foods and medicaments. Pharmaceutically allowable oral formulations, injection formulations or externally applied formulations are prepared from purified ampelopsin or unpurified ampelopsin-containing extracts.
Description
Research field:
The present invention relates to the application of ampelopsin at health food and pharmaceutical field, the particularly ampelopsin application in preparation anti-sudden change health food and medicine.
Background technology:
Hepatitis B is a global health problem.The whole world has the chronic carrier of 300,000,000 5 thousand ten thousand HBV approximately, and the patient who dies from hepatitis B every year has 2,000,000, makes it to become the whole world the 9th and causes dead disease greatly.The chronic carrier of China HBV accounts for 1/3rd of the whole world, is that HBV virus is carried the highest country in the world.Estimation crowd HBsAg positive rate is 10.3%.Asymptomatic HBsAg carrier more than 100,000,000 is arranged, and existing clinical symptoms patient has surpassed 3,000 ten thousand people, and the incidence of disease is about 30.41%.Hepatitis B is serious threat China people's health not only, also brings serious financial burden for society.The mutation rate of HBV is higher, there are some researches show, the mutation rate of HBV reaches more than 30%.The different genes district of HBV all can undergo mutation, but the variation of main harm maximum occurs in S district and the variation of preceding S district.S gene " a " determinant G145 variation can produce the immunologic escape strain, and antigenicity changes, and the affinity reduction with anti-HBs causes the conventional vaccine immunity invalid.For clinical treatment, the easy mutability of HBV can directly cause viral persister to occur simultaneously, makes the effect of existing medicine reduce, even loses efficacy.It is reported that use the lamivudine therapy chronic hepatitis B, the incidence of YMDD variant is 14-32% after 1 year, 2 years be 38%, 3 year be 49%, 4 year be 66%.(Chinese hepatopathy magazine was rolled up the 425th page of the 7th phase in 2004 the 12nd)
The base unit of cancerous lesion is a cancer cell.Have neonatal cell after the aging death of human body cell and replace it, to keep body function.Human body overwhelming majority cells can hyperplasia, but this hyperplasia is limited, and the hyperplasia of cancer cell then is endless, and the nutriment in patient's body is consumed in a large number.Simultaneously, cancer cell also can be transferred to whole body growth and breeding everywhere, causes at last that human body is become thin, unable, anaemia, poor appetite, heating and organ function are impaired etc.Until wearing human body down.But tumour is not external invador unlike virus, and its composition is the same with normal structure, so body can't be discerned immunity to it.Clinical use resists the sudden change medicine, can slow down the process of canceration to a certain extent, suppresses the growth of cancer cell.Thereby make the nutriment in patient's body and do not consumed in a large number.Because suppressed the growth of cancer cell, make cancer cell can not let slip too much toxin, and can not each organ of human body be damaged, prolong patient's life cycle.
The applicant is surprisingly found out that ampelopsin has the effect that prevents the inhereditary material coding mutation significantly, prevent the generation of virus and/or cytometaplasia strain, strengthen the result of treatment of existing medicine, reduce clinical treatment of diseases difficulty such as hepatitis, AIDS, cancers.
Ampelopsin is a kind of compound known, be that Chinese south China one band is issued several ampelopsis of Vitaceae widely, as the main component of ampelopsis grossdentata [Ampelopsis grossedentata (Hand.-Mazz.) W.T.Wang] or Radix Ampelopsis Cantoniensis [Ampelopsis cantoniensis (HooK.etArm) Planch] etc.Ampelopsin has another name called dibydro myricetrin, belongs to flavone compound, and its structural formula is as follows.
Ampelopsin can extract according to a conventional method from vitaceae ampelopsis grossdentata (having another name called vine tea) or Radix Ampelopsis Cantoniensis and obtain, and also can obtain by the chemical field conventional method.
From the seventies in 20th century, ampelopsin causes people's attention gradually, it is extracted purifying, separation evaluation etc. more comprehensively study.Chinese patent 00117225.5 has reported that it has antineoplastic action, and CN99119123.4 discloses the preparation method of dibydro myricetrin and treated hepatitis, liver protecting, anti-inflammation and enhancing immune system immunity purposes; CN03149572.9 discloses dibydro myricetrin in the medicine of preparation reducing blood lipid and the purposes in the health products; CN03149573.7 discloses dibydro myricetrin in preparation analgesia, the medicine that eliminates the phlegm and the purposes in the health products.CN200310110467.3 discloses the application of dibydro myricetrin in the preparation medicine, specifically is used to prepare the medicine of treatment canker sore, gastric ulcer, duodenal ulcer, acute or chronic pharyngitis, pelvic infecton and/or adnexitis, chronic gastritis and/or enteritis; CN200510087033.5 discloses the application of dibydro myricetrin as the feed addictive that improves the meat packing quality; CN 200710106278.7 discloses the purposes of dibydro myricetrin in the medicine of preparation treatment gastric ulcer and gastritis; CN 200710034610.3 discloses the purposes of dihydro myricotin element for treating cardiac blood diseases.But up to now, do not see the report that the application of ampelopsin in preparation anti-sudden change health food and medicine arranged.
Summary of the invention:
One of the object of the invention provides the new purposes of ampelopsin, and promptly it is in the application of preparation ampelopsin in preparation anti-sudden change health food and medicine.
Ampelopsin of the present invention can adopt any formulation that pharmaceutically allows all effective.Comprise peroral dosage form such as tablet, capsule, pill, granule, oral liquid etc.; Also can adopt injection type such as parenteral solution, transfusion, powder pin etc.Can also adopt exterior-applied formulation such as patch, paste, film, aerosol, liniment, gel, paint, suppository etc.
Ampelopsin among the present invention, can from the water extract of the plant (as ampelopsis grossdentata, Radix Ampelopsis Cantoniensis) that contains ampelopsin or alcohol extract through extracting purifying or obtain the higher ampelopsin of purity by the chemical field conventional method.Also can adopt the mode of the not purified mixed extract of the water extract of the plant (as ampelopsis grossdentata, Radix Ampelopsis Cantoniensis) that contains ampelopsin or alcohol extract, and needn't adopt the very high ampelopsin of purity.
The present invention can adopt the medicine of ampelopsin and other antimutanens to make compound preparation.
The result of treatment that anti-sudden change health food that contains ampelopsin among the present invention and medicine can strengthen antiviral drugs can be used as the antiviral adjuvant drug that comprises as various hepatitis, AIDS, influenza, rotavirus prevention and treatment.
The result of treatment that anti-sudden change health food that contains ampelopsin among the present invention and medicine can strengthen cancer drug can be used as the adjuvant drug that prevents and treat cancer.
Below in conjunction with specific embodiment, further set forth the present invention.Should be understood that these embodiment only to be used to the present invention is described and be not used in and limit the scope of the invention.
Specific embodiment:
Embodiment 1
Get ampelopsis grossdentata, adopt conventional extracting method extraction, purifying to prepare ampelopsin, be distributed into powder pin ampoule or parenteral solution that 0.4g/ props up.
Embodiment 2
Get vine tea and extract the ampelopsin extract through routine, not purified, behind assay, add auxiliary material according to a conventional method, granulate, sieve, add glidant magnesium sulfate, talcum powder, be processed into tablet by the tablet conventional production process, make the ampelopsin tablet, every contains ampelopsin 300mg.
Embodiment 3
Get ampelopsis grossdentata 10kg, rhodiola root 10kg, adopt conventional alcohol extract method to extract 2 times, be concentrated into the clear cream that relative density is 1.35-1.38 after alcohol extract is merged, the adding cane sugar powder is an amount of, and mixing is made granule.
Embodiment 4
Get ampelopsis grossdentata, adopt conventional water extracting method, being concentrated into relative density after extract merges is 1.1～1.2 (85 ℃ ± 5 ℃), be cooled to 40 ℃, add alcohol and make and contain alcohol amount and reach 30%, stir evenly, left standstill 24 hours, and filtered, reclaim ethanol to there not being the alcohol flavor, add water and adjust total amount, stir evenly, leave standstill to 1000ml, filter, embedding, sterilization promptly gets oral liquid.
Embodiment 5
Get ampelopsis grossdentata 1000g, adopt conventional extracting method to extract, decolouring, being concentrated into relative density is 1.20, adds ethyl hydroxy benzoate, lanolin and vaseline, mixing is made the ampelopsin ointment.
Embodiment 6
Get ampelopsis grossdentata or ampelopsis cantoniensis Radix Ampelopsis Cantoniensis, adopt conventional extracting method to extract, be condensed into medicinal extract, standby.It is an amount of to get semi-synthetic fatty acid ester, heat fused in water-bath, and cold slightly back adds above-mentioned medicinal extract 7-10g, mixes, and injection molding promptly gets ampelopsin suppository.
Embodiment 7
The protective effect that the micronuclei in mice rate that ampelopsin parenteral solution (embodiment 1 is seen in preparation) causes endoxan (Cy) increases
With 40 18-22g kunming mice random packet, 10 every group.Negative control group intraperitoneal injection of saline, ampelopsin are established two dosage groups of height, and intraperitoneal injection is 10 days continuously, and in the 9th, 10 day and Cy positive controls while lumbar injection Cy.Press literature method and measure the mouse bone marrow cells micronuclear rates.
The antagonism that the micronuclei in mice rate that ampelopsin causes Cy increases
*：P＜0.001
The result shows that the ampelopsin test group all has tangible antagonism to the micronuclear rates increase that Cy causes, illustrates that the present invention has the mutation effect of anti-chemical induction.
Embodiment 8
The test of ampelopsin oral liquid (embodiment 4 is seen in preparation) radioresistance
60 kunming mices are divided into 3 groups at random, 20 every group, male and female half and half.Control group is irritated stomach with physiological saline every day, and prevention group and treatment group are irritated stomach, 150mg/kg, administration 5 days with the ampelopsin oral liquid every day.Carried out 7Gy on the 6th day
60Co-gamma-radiation, irradiation frequency be 157.7 human relations/minute.The irradiation back was administered once in half an hour.After the irradiation, control group and prevention group are irritated stomach with physiological saline every day, and the treatment group is irritated stomach 150mg/kg with the ampelopsin oral liquid, continue 4 days.From radiation, observe the death condition of mouse in 1 month.
The result shows, no matter is ampelopsin prevention group or treatment group, and mouse is accepted the Co60 irradiation back death rate and obviously reduces, and the treatment group is particularly evident, illustrates that the present invention has the radioresistance mutation effect.
Embodiment 9
The result of treatment of ampelopsin associating Lamivudine anti-DHB in the duck body
(1) medicine: ampelopsin sheet (embodiment 2 is seen in preparation), Lamivudine (Glaxo Wellcome drugmaker), above medicine is prepared with physiological saline.
(2) virus: DHB DHB DNA (DHBV-DNA) strong positive serum, pick up from the Shanghai sheldrake ,-70 ℃ of preservations.
(3) animal: 1 age in days Beijing duck, available from animal feeding field, progressive species duck field, Beijing.
(4) experimental technique
1. duck hepatitis B virus infection:
1 age in days Beijing duck, through the positive duck serum of leg shin intravenous injection Shanghai sheldrake DHBV-DNA, every 0.2ml got blood in back 7 days in infection, separation of serum ,-70 ℃ of preservations are to be checked.
2. drug therapy test:
DHBV infect duckling after 7 days random packet carry out drug therapy test, 6 every group.
Positive controls: Lamivudine, oral administration 50mg/kg, 1 day 2 times, 10 days.
Negative (DHBV) control group:, with the physiologic saline for substitute medicine.
3 dosage groups of combination medicine: be respectively 1.0,2.0,3.0g/kg porcelain ampelopsis sheet group+50mg/kg Lamivudine, oral administration, 1 day 2 times, 10 days.
The 7th day is (T0) before the medication after infection, and medication the 5th day (T5) after medication the 10th day (T10) and the drug withdrawal the 3rd day (P3), is got blood from duck leg shin vein, separation of serum, and-70 ℃ of preservations are to be checked.
3. detection method:
Get above-mentioned duck serum to be checked, every batch with the time point film, the DHBV-DNA level is dynamic in the mensuration duck serum, press nick translation kit specification method,, and make duck serum dot hybridization with 32P mark DHBV-DNA probe, autoradiograph diaphragm spot, measure OD value (optical filter is 490nm) at enzyme mark detector, calculating serum DHBV-DNA density, with hybridization spot OD value as sample DHBV-DNA level value.
(5) drug effect is calculated
1. calculate the mean value (X ± SD) of every group of duck different time serum DNA OD value, and with (T0) OD value comparison before the 3rd day (P3) serum DHBV-DNA level after different time (T5, T10) and the drug withdrawal after every group of duck medication and the administration on the same group, adopt paired t-test, calculate t1, P1 value.Analyze the conspicuousness of difference, judge the inhibition effect of medicine virus infections.
2. calculate the inhibition % of different time (T5, T10) and the 3rd day (P3) serum of drug withdrawal DHBV-DNA after every group of duck medication, and mapping, respectively organize duck serum DHBV-DNA inhibiting rate dynamically.
3. with identical with the virus control group respectively time D HBV-DNA inhibiting rate of drug treatment group different time DHBV-DNA inhibiting rate relatively, adopt t check in groups, take statistics to learn and handle, calculate t2, P2 value, analyze the conspicuousness of difference, judge drug effect.
The comparison of treatment group and the horizontal inhibiting rate of virus infections control group duck serum DHBV-DNA
Statistical disposition: t2, P2: (T5, T10, P3) duck serum DHBV-DNA level suppresses % relatively (t checks in groups) with infection preceding (T0) inhibition % and virus control group relatively to administration group different time.*p2＜0.05，**p2＜0.01，
The result shows that ampelopsin can significantly improve the effect of Lamivudine anti-hepatitis B virus.Simultaneously, ampelopsin can obviously suppress the bounce-back of hepatitis B after the Lamivudine drug withdrawal.
Embodiment 10
Ampelopsin granule (embodiment 3 is seen in preparation) commissural arch phosphamide is to the result of treatment of mice-transplanted tumor Heps
Experimental technique: get 60 of ICR mouse, (get the knurl piece under the aseptic condition by transplanted tumor research method inoculation Heps solid type knurl, weigh, grind with the glass Potter-Elvehjem Tissue Grinders, put into sterile chamber after mill is even, add the cell suspension that physiological saline is diluted to 1: 3, container is put on the ice cube, with the empty needle suction, each suction is preceding with the cell mixing, every mouse right fore armpit subcutaneous vaccination 0.2ml), inoculate back 24 hours and claim mouse heavy, and being divided into 6 groups at random, blank group (0.5%CMC-Na) is respectively cloudy with endoxan (20mg/kg) group, positive controls, porcelain ampelopsis are established high, normal, basic 3 dosage groups (3.0,2.0,1.0g/kg).Inoculate administration after 24 hours, the ig administration, once a day, administration is 7 times altogether, and the 2nd day execution mouse weighed after drug withdrawal, and separates the knurl piece and weigh, and the gained data are carried out statistical procedures.
Ampelopsin is to the inhibitory action of mice-transplanted tumor Heps
Experimental result is compared with the Cy group, and ampelopsin associating Cy group can significantly suppress the tumor growth effect of Heps.Illustrate that ampelopsin can improve the antitumor action of endoxan.
Claims (9)
1. the application of ampelopsin in preparation anti-sudden change health food and medicine.
2. the application of ampelopsin according to claim 1 in preparation anti-sudden change health food and medicine is characterized in that adopting any peroral dosage form that allows on the pharmacy.
3. the application of ampelopsin according to claim 1 in preparation anti-sudden change health food and medicine is characterized in that adopting any injection type that allows on the pharmacy.
4. the application of ampelopsin according to claim 1 in preparation anti-sudden change health food and medicine is characterized in that adopting any exterior-applied formulation that allows on the pharmacy.
5. according to the application of the described ampelopsin of claim 1-4 in preparation anti-sudden change health food and medicine, it is characterized in that the medicine of ampelopsin and other antimutanens is made compound preparation.
6. according to the application of the described ampelopsin of claim 1-5 in preparation anti-sudden change health food and medicine, it is characterized in that the not purified extract of ampelopsin employing ampelopsis grossdentata in the formulation.
7. according to the application of the described ampelopsin of claim 1-5 in preparation anti-sudden change health food and medicine, it is characterized in that the not purified extract of ampelopsin employing Radix Ampelopsis Cantoniensis in the formulation.
8. according to the application of the described ampelopsin of claim 1-7 in preparation anti-sudden change health food and medicine, it is characterized in that to strengthen the result of treatment of antiviral drugs, can be used as the antiviral adjuvant drug that comprises as various hepatitis, AIDS, influenza, rotavirus prevention and treatment.
9. according to the application of the described ampelopsin of claim 1-7 in preparation anti-sudden change health food and medicine, it is characterized in that to strengthen the result of treatment of cancer drug, can be used as the adjuvant drug of prevention and treatment cancer.
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| CN2009101809722A CN102038190A (en) | 2009-10-23 | 2009-10-23 | Application of ampelopsin to preparation of anti-mutagenic health-care foods and medicaments |
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| CN2009101809722A CN102038190A (en) | 2009-10-23 | 2009-10-23 | Application of ampelopsin to preparation of anti-mutagenic health-care foods and medicaments |
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| CN 201310062135 Division CN103251581A (en) | 2009-10-23 | 2009-10-23 | Application of ampelopsin in mutation resistance composition preparation |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102771594A (en) * | 2011-05-13 | 2012-11-14 | 贵州省生物研究所 | Antibacterial, inflammation-diminishing, and analgesic Ampelopsis grossedentata preparation and preparation method thereof |
| CN102772398A (en) * | 2011-05-13 | 2012-11-14 | 贵州省生物研究所 | Application of dihydromyricetin in preparation of drug preventing and treating influenza |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1304934A (en) * | 2000-07-05 | 2001-07-25 | 中山医科大学科技开发部 | Antineoplastic medicine and its preparing process |
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- 2009-10-23 CN CN2009101809722A patent/CN102038190A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1304934A (en) * | 2000-07-05 | 2001-07-25 | 中山医科大学科技开发部 | Antineoplastic medicine and its preparing process |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102771594A (en) * | 2011-05-13 | 2012-11-14 | 贵州省生物研究所 | Antibacterial, inflammation-diminishing, and analgesic Ampelopsis grossedentata preparation and preparation method thereof |
| CN102772398A (en) * | 2011-05-13 | 2012-11-14 | 贵州省生物研究所 | Application of dihydromyricetin in preparation of drug preventing and treating influenza |
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