CN101011567A - Medicament for treating AIDS and its preparing method - Google Patents
Medicament for treating AIDS and its preparing method Download PDFInfo
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- CN101011567A CN101011567A CN 200710013485 CN200710013485A CN101011567A CN 101011567 A CN101011567 A CN 101011567A CN 200710013485 CN200710013485 CN 200710013485 CN 200710013485 A CN200710013485 A CN 200710013485A CN 101011567 A CN101011567 A CN 101011567A
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Abstract
Disclosed is a medicament for treating AIDS, wherein the active constituents include Fucoidan-Glycocalyx polymeric compound, which is a protein polysaccharide containing sulfate groups extracted from Chinese herbal sea apron. The preparing process consists of steps of choosing materials, soaking and cleaning, disintegrating, water extracting, low concentration alcohol depositing, high concentration depositing, purifying to obtain the end product.
Description
One, technical field
The present invention relates to a kind of treatment AIDS-treating medicine and preparation method thereof, belong to treatment AIDS-treating medicine technical field.
Two, background technology
The acquired immune deficiency syndrome (AIDS) (AIDS) that HIV (human immunodeficiency virus) (Human Immunodeficiency Virus) (HIV) causes is the strong and great infectious disease of hazardness of a kind of infectiousness.At present, there are 4,000 ten thousand the infecteds in the whole world according to statistics, and every day, there was the new patients infected hiv of 15000 examples in the whole world, had every day 8500 people dead because of acquired immune deficiency syndrome (AIDS) simultaneously, and the whole world prevents and treats acquired immune deficiency syndrome (AIDS), and the situation is tense.In China, HIV (human immunodeficiency virus) infection expands general crowd to from special population.According to statistics, China's patients infected hiv has reached 1,000,000 people.If it is improper to control, can reach 1,000 ten thousand people by 2010.The treatment of acquired immune deficiency syndrome (AIDS), still there is not at present the medicine that can cure in the world, the medicine that now is used for AIDS treatment mostly is chemicals greatly, though can relief of symptoms, prolong the course of disease, but still there are a lot of problems: can not thoroughly remove the body inner virus, the drug withdrawal bounce-back easily produces drug resistance, and side effect is big and medical expense is expensive, make the application of these medicines be very limited, thus low toxicity, effective and cheap conventional medicament particularly Chinese medicine enjoy attention both domestic and external.
Modern medicinal Sargassum reaches over one hundred kind, has that heat-clearing and toxic substances removing, inducing diuresis to remove edema, the kidney invigorating nourish heart, effects such as activating blood circulation to dissipate blood stasis and the anthelmintic that helps digestion.Contain plurality of active ingredients in the Sargassum, wherein, the sulphonic acid ester polysaccharide is to study comparatively deeply, simultaneously also is to possess the composition of practical value most.Sargassum polysaccharides is a kind of glycoconjugates with special construction, contains the proteoglycan of sulfate group.Drug research based on saccharide has great potential, and carbohydrate molecule plays an important role at aspects such as cell recognition, signal transmission, cell-cell interactions, and sugar moieties has determined the function of whole molecule.The saccharide medicine is at infection, and all there is exploitation and application in various degree aspect such as anticancer, antiviral and resisting rheumatoid disease arthritis.Conjugated protein component performance in the polysaccharide suppresses the effect of virus breeding and kill virus, is that multidigit is put antiviral molecular basis.
To the anti-HIV effect of Sargassum sulfonic acid polysaccharide, existing both at home and abroad (Zheng Yongtang, Ben Kunlong, Jin Shanwei, the HIV (human immunodeficiency virus)-resistant activity of protein extract in 17 kind of plant, Chinese virusology, 1998 reported; 13:312-24; Witvrouw M and De Clercq E.Sulfatedpolysaccharides extracted from sea algae as potentialantiviral drugs.Gen Pharmacol, 1997; 29:497-511; WitvrouwM, Este JA, Mateu MQ, et a1.Activity of a sulfatedpolysaccharides extracted from the red seaweedaghardhiella tenera against human immunodeficiency virusand enveloped viruses.Antiviral chemistry﹠amp; Chemotherapy, 1994; 5:297-303).But, to its antivirus action and pharmacology curative effect thereof, still there is not the deep research of complete sum, lack conclusive experimental data.
Three, summary of the invention
The objective of the invention is to solve the weak point that above-mentioned prior art exists, a kind of medicine that can contain effectively that HIV (human immunodeficiency virus) (Human Immunodeficiency Virus) (HIV) is duplicated is provided, improve body immunity, take for a long time and have no side effect, can not cause drug resistance, and cheap, acquired immune deficiency syndrome (AIDS) (AIDS) there is the medicine and preparation method thereof of the treatment acquired immune deficiency syndrome (AIDS) of obvious curative effects.
A kind of medicine for the treatment of acquired immune deficiency syndrome (AIDS) of the present invention, its effective ingredient that comprises are sulfonic acid fucoside polypeptide polymers;
Sulfonic acid fucoside polypeptide polymer is the effective site of single medicinal material Thallus Laminariae (Thallus Eckloniae), is the protein polysaccharide of a kind of sulfur acid ester group of extracting from the single medicinal material Thallus Laminariae (Thallus Eckloniae);
The main physicochemical characteristics of sulfonic acid fucoside polypeptide polymer is: soluble in water, and dissolubility 〉=30%, white or yellow polycrystal powder, the fragrance that tool is special; SO
4 2-Content is 20 ± 5%, and fucose content is 20 ± 5%, and protein content is 10-18%.
A kind of preparation method for the treatment of the medicine of acquired immune deficiency syndrome (AIDS) of the present invention, special character are that its sulfonic acid fucoside polypeptide polymer production extraction process may further comprise the steps:
1, selects materials: the high-quality limnetic dry kelp; The main place of production, Yantai, Shandong, marine site, Weihai;
2, immersion and cleaning: immersion and cleaning under the room temperature, immersion and cleaning time 30-50 minute controlled in strictness;
3, pulverize; 25-35mm width rectangular;
4, water is carried; Boiled for three times 1-1.5 hour, the 5-10 that each water yield is a Thallus Laminariae (Thallus Eckloniae) doubly;
5, low concentration precipitate with ethanol; The ethanol final concentration is 25-40%, centrifugal filtration;
6, high concentration precipitate with ethanol obtains thick product; The ethanol final concentration is 80-90%, centrifugal filtration;
7, purification obtains purified product, dry packing.
A kind of preparation method for the treatment of the medicine of acquired immune deficiency syndrome (AIDS) of the present invention, mild condition is not destroyed various natural nutrient components contained in the Thallus Laminariae (Thallus Eckloniae) frond, and is simple to operate, improves the Thallus Laminariae (Thallus Eckloniae) comprehensive utilization degree, productive rate higher (2%), cost is lower, is applicable to suitability for industrialized production.
A kind of medicine for the treatment of acquired immune deficiency syndrome (AIDS) of the present invention can be made into tablet, pill, injection and capsule (soft, hard).This medicine contains effective composition 500mg for every dose and follows the doctor's advice oral.
A kind of using method for the treatment of the medicine of acquired immune deficiency syndrome (AIDS) of the present invention, every day, consumption 3000mg-6000mg can divide to give for three times, each 1000mg-2000mg.
The present invention has realized independent application sulfonic acid fucoside polypeptide polymer in the treatment of acquired immune deficiency syndrome (AIDS), and composition is simple, belongs to Chinese medicine, natural drug, can improve body immunity, take for a long time and have no side effect, can not cause drug resistance, and cheap, (AIDS) has obvious curative effects to acquired immune deficiency syndrome (AIDS);
The medicine of treatment acquired immune deficiency syndrome (AIDS) of the present invention can effectively be contained the medicine that HIV (human immunodeficiency virus) (Human Immunodeficiency Virus) (HIV) is duplicated, and improves body immunity, takes for a long time to have no side effect, and can not cause drug resistance, and cheap, and (AIDS) has obvious curative effects to acquired immune deficiency syndrome (AIDS).
Four, the specific embodiment
Describe the present invention in detail with embodiment below, but these embodiment must not be interpreted as the limitation of the present invention that goes up in all senses.
Embodiment 1:
A kind of medicine for the treatment of acquired immune deficiency syndrome (AIDS), its effective ingredient that comprises is a sulfonic acid fucoside polypeptide polymer, sulfonic acid fucoside polypeptide polymer is the effective site of single medicinal material Thallus Laminariae (Thallus Eckloniae), it is the protein polysaccharide of a kind of sulfur acid ester group of from the single medicinal material Thallus Laminariae (Thallus Eckloniae), extracting, its main physicochemical characteristics is: soluble in water, dissolubility 〉=30%, white or yellow polycrystal powder, the fragrance that tool is special; SO
4 2-Content is 20 ± 5%, and fucose content is 20 ± 5%, and protein content is 10-18%.
The preparation method of medicine, its sulfonic acid fucoside polypeptide polymer production extraction process may further comprise the steps: the 100kg Sargassum, through soaking, clean, pulverizing, add water 800kg, 90-100 ℃ extracts 3.5h 3 times.Get the supernatant concentrating under reduced pressure to 25L, precipitate under 30% ethanol condition, get supernatant again, reduction vaporization is to 10L, adds in the ethanol of 85L95%, filter thick product.60 ℃ of dryings, purification, 100 orders are pulverized.
Embodiment 2:
A kind of medicine for the treatment of acquired immune deficiency syndrome (AIDS), the mechanism of the anti-HIV effect of its sulfonic acid fucoside polypeptide polymer is as follows:
The one, deactivation HIV-1 virion; The 2nd, the free HIV-1 virus absorption onto cell of blocking-up; The 3rd, suppress the HIV-1 reverse transcriptase activity; The 4th, HIV-1's duplicates in the inhibition infection cell.Its effect characteristics are one to be that lymphocyte is had growth-promoting functions; The 2nd, acute and chronic infection all has inhibitory action to H1V-1: the 3rd, but suppressing HIV-1, duplicates multidigit point;
Sulfonic acid fucoside polypeptide polymer medicine is to the toxicity test of MT-4 cell: medicine is mixed with 20mg/ml solution with culture fluid, adds 96 porocyte culture plates behind the doubling dilution, and same concentration liquid was changed in per 3 days in every concentration 3 holes, established no drug cell matched group.Cell and medicine are cultivated a week at 37 ℃, measure cell survival rate with mtt assay.
Sulfonic acid fucoside polypeptide polymer medicine is to the inhibitory action of virus absorption; In virus infected cell, add sulfonic acid fucoside polypeptide polymer, if feminine gender and positive control, placed 1 hour for 4 ℃, clean, remove the virus and the medicine of not absorption, with the cell resuspending in culture medium, cultivate a week for 37 ℃, the observation of cell pathological changes is measured cytoactive, collects supernatant and measures P24 antigen.
Sulfonic acid fucoside polypeptide polymer medicine is to the active inhibitory action of hiv reverse transcriptase, separate the HIV-1 virion, get 20ul, add 10ul employing virus cracking liquid (0.5%TritonX-100,0.8M Nacl, 05.M phenylmethylsulfonyl fluoride, 20% (v/v) glycerol, 50Mtris-HCLpH7.8) with virion in the cracking supernatant, discharge reverse transcriptase (RT) wherein.Under 4 ℃ of condition of ice bath, add 20L medicine (20,4,0.8,0.16,0.032,0.0064mg/ml), the reactant mixture that adds 80L then, reactant mixture to join method as follows: 0.05M Tris-HCL (pH8.4), 2mMdtt, 100Mmkcl, 10mMMgcl2,0.1%TritonX-100,1.5gpoly " dA "-" dT " 12-18,1.5Ci3H-Dttp.With 37 ℃ of reactions of above-mentioned reaction system 2 hours, then the activity of RT can be mixed how much representing of Polya-oligodT12-18 templa-primer by 3H-dTTP.After reaction finishes, add 10% ice-cold trichloroacetic acid of 3ml and 70% ethanol and wash film,, add 8ml scintillation solution (containing 0.5%PPO, the xylene solution of 0.015%POPOP) liquid scintillation counter and measure cpm, calculate suppression ratio the film oven dry.
Medicine is to the inhibitory action of virus replication: infect MT-4 cell (6*105/ml) with 200ECID50HIV-1 (SF33), cell and viral ratio of solvent are 1: 1,37 ℃, hatched 2 hours, clean, abandon supernatant, with the infection cell resuspending in culture medium, in the presence of medicine, cultivated for 1 week or 4 weeks, carry out the detection of every index.
The experiment proved that, can suppress HIV infection cell and Normocellular fusion, have short coming into force to answer, show to have antivirus action normal cell.Can directly suppress a certain step of duplicating after virus enters cell or enters cell.HIV-1 invades body, and the target cell of effect is the CD4+T lymphocyte.HIV-1 shell glycoprotein gpl20 is and the position of T lymphocytic cell surface HIV acceptor molecule CD4 specific bond that gpl20 V3 zone is positively charged, can combine with the V3 district, thereby suppress HIV-1 absorption CD4+T cell and plasmodial formation.In addition, reverse transcriptase there is certain inhibitory action.By Profilin kinase activity and nuclear factor, suppress duplicating and transcribing of HIV-1.To the synthetic later stage of HIV-1, also there is certain inhibition to do friend as albumen packing etc.Another effect is to activate body immune system, and specificity and non-specific immunity that can the human body immunity improving system promote lymphopoiesis, promote cytokine (IL-2, IL-6, IFN etc.) to discharge.
With reference to State Standard of the People's Republic of China GB15193.3-94, GB15193.5-94, GB15193.8-94, GB15193.7-94, GB15193.4-94, GB15193.14-94, GB15193.13-94, carry out the test of rat acute poison, the test of chmice acute poison, mouse bone marrow cells micronucleus test (male), mouse bone marrow cells micronucleus test (female), mouse sperm deformity test, mouse testis chromosomal aberration test, Salmonella reversion test, the tertogenicity test of rat system and 30 days feeding trials of rat, the result shows large and small Mus LD
50＞21.50g/kg; Capsule test group and group of solvents compare, and the mouse Bone marrow cells micronucleus rate does not have significant difference; Capsule test group and group of solvents compare, and it is different that the mouse sperm deformity rate does not have significance difference; Capsule test group and group of solvents compare, mice primary spermatocyte chromosome aberrations rate, no significant difference; Salmonella reversion test, experimental group return and become clump count and be less than or equal to nature and return and become 2 times of clump counts; In the rat tertogenicity test, experimental group and group of solvents compare, and index differences such as pregnant Mus pregnancy period weight gain and reproduction embryo inspection, tire Mus growth promoter and skeleton deformity inspection are not remarkable; Rat was fed in 30 days, compared clinical examination with the normal feedstuff matched group: internal organs weighing, blood biochemical are learned and are checked, histopathologic examination, difference that there are no significant.It is nontoxic that this result shows that medicine of the present invention belongs to, hereditary-less toxicity and no teratogenesis material.
The oral medicament capsule of the present invention of rat (4000mg/kg), one day 2 times, serve on 10 days, under the state of waking up, observe its spiritual nervous system, the cardiovascular system respiratory system of unifying, all no abnormal performance of result.
Clinical trial is indicated, is applicable to HIV (human immunodeficiency virus) (Human Immunodeficiency Virus) (HIV) the infected or acquired immune deficiency syndrome (AIDS) (AIDS) patient, and no obvious toxic-side effects can be taken for a long time.Both can directly suppress virus, but enhancing human body immunity is again regulated the oxidative stress attitude.And be single medicinal material effective site, produce stable, quality controllable.Drug price is with low cost, is easy to the patient and accepts, and is easy to utilize, and life, the spreading of acquired immune deficiency syndrome (AIDS) of retardance of saving HIV sufferers is significant.
Claims (9)
1, a kind of medicine for the treatment of acquired immune deficiency syndrome (AIDS) is characterized in that its effective ingredient that comprises is a sulfonic acid fucoside polypeptide polymer.
2, according to the described a kind of medicine for the treatment of acquired immune deficiency syndrome (AIDS) of claim 1, it is characterized in that sulfonic acid fucoside polypeptide polymer is the effective site of single medicinal material Thallus Laminariae (Thallus Eckloniae), is the protein polysaccharide of a kind of sulfur acid ester group of extracting from the single medicinal material Thallus Laminariae (Thallus Eckloniae).
3,, it is characterized in that the main physicochemical characteristics of sulfonic acid fucoside polypeptide polymer is according to claim 1 or 2 described a kind of medicines for the treatment of acquired immune deficiency syndrome (AIDS): soluble in water, dissolubility 〉=30%, white or yellow polycrystal powder, the fragrance that tool is special; SO
4 2-Content is 20 ± 5%, and fucose content is 20 ± 5%, and protein content is 10-18%.
4, the described a kind of preparation method for the treatment of the medicine of acquired immune deficiency syndrome (AIDS) of arbitrary claim among the claim 1-3 is characterized in that its sulfonic acid fucoside polypeptide polymer production extraction process may further comprise the steps:
(1), selects materials: the high-quality limnetic dry kelp;
(2), soak and clean: room temperature soaks down and cleans, and soaks and time 30-50 minute of cleaning;
(3), be ground into the rectangular of 25-35mm width;
(4), water is carried;
(5), low concentration precipitate with ethanol;
(6), the high concentration precipitate with ethanol, obtain thick product;
(7), purification, obtain purified product, dry packing.
5,, it is characterized in that sulfonic acid fucoside polypeptide polymer medicine can be made into a kind of in tablet, pill, injection and the capsule according to the described a kind of preparation method for the treatment of the medicine of acquired immune deficiency syndrome (AIDS) of claim 4.
6, according to the described a kind of preparation method for the treatment of the medicine of acquired immune deficiency syndrome (AIDS) of claim 4, it is characterized in that: in (4), it is to boil 1-1.5 hour for three times that water is carried, and the 5-10 that each water yield is a Thallus Laminariae (Thallus Eckloniae) doubly.
7, according to the described a kind of preparation method for the treatment of the medicine of acquired immune deficiency syndrome (AIDS) of claim 4, it is characterized in that: in (5), the low concentration precipitate with ethanol is 25-40% for the ethanol final concentration, centrifugal filtration.
8, according to the described a kind of preparation method for the treatment of the medicine of acquired immune deficiency syndrome (AIDS) of claim 4, it is characterized in that: in (6), the high concentration precipitate with ethanol is 80-90% for the ethanol final concentration, centrifugal filtration.
9, the described a kind of using method for the treatment of the medicine of acquired immune deficiency syndrome (AIDS) of arbitrary claim among the claim 1-3, it is characterized in that sulfonic acid fucoside polypeptide polymer medicine contains effective composition 500mg for every dose, every day, consumption 3000mg-6000mg divided to give for three times, each 1000mg-2000mg.
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| CN 200710013485 CN101011567A (en) | 2007-02-02 | 2007-02-02 | Medicament for treating AIDS and its preparing method |
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| CN 200710013485 CN101011567A (en) | 2007-02-02 | 2007-02-02 | Medicament for treating AIDS and its preparing method |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102247590A (en) * | 2010-05-18 | 2011-11-23 | 天津市扶素生物技术有限公司 | Drug composition for preventing or treating HIV (human immunodeficiency virus) infection and application thereof |
| CN102971432A (en) * | 2009-12-15 | 2013-03-13 | 73100-七十三千零一百有限公司 | Fucose-containing bacterial biopolymer |
-
2007
- 2007-02-02 CN CN 200710013485 patent/CN101011567A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102971432A (en) * | 2009-12-15 | 2013-03-13 | 73100-七十三千零一百有限公司 | Fucose-containing bacterial biopolymer |
| CN102971432B (en) * | 2009-12-15 | 2017-06-23 | 73100-七十三千零一百有限公司 | Bacterium living beings condensate containing fucose |
| CN102247590A (en) * | 2010-05-18 | 2011-11-23 | 天津市扶素生物技术有限公司 | Drug composition for preventing or treating HIV (human immunodeficiency virus) infection and application thereof |
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