CN106668833B - Application of the Dalbavancin in the drug of preparation treatment AIDS - Google Patents
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Abstract
Application of the Dalbavancin in the drug of preparation treatment AIDS, the present invention provides the application of Dalbavancin and its pharmaceutically acceptable salt in preparation treatment AIDS-treating medicine.Dalbavancin (Dalbavancin) is to HIV-1NL4‑3The HIV-resistant activity experimental result of Strain shows the Dalbavancin of various concentration to HIV-1NL4‑3The inhibiting effect of Strain.Dalbavancin forms the EC of the inhibiting effect of plasomidum to HIV-1 induction C8166 cell50It is 8.694 μM, therapeutic index TI is greater than 23.0.Show that Dalbavancin inhibits the EC of p24 antigenic action in HIV-1p24 antigen quantitative result50It is 1.296 μM, therapeutic index TI is greater than 135.1.Above the experimental results showed that the cytotoxicity of Dalbavancin is smaller or nothing, there is significant HIV-resistant activity and higher therapeutic index, can be used as the application of preparation treatment AIDS-treating medicine.
Description
Technical field
The invention belongs to technical field of pharmaceuticals, and in particular to compound Dalbavancin (Dalbavancin) is treated in preparation
Application in the drug of AIDS.
Technical background
AIDS is a kind of by human immunodeficiency virus (Human Immunodeficiency Virus, HIV) infection
A kind of caused severe infection disease.The chronic infectious disease of human immune system can be directly destroyed as one kind, AIDS is
As one of the disease for seriously threatening human health in the world.The data of The Joint Programme on AIDS (UNAIDS) are shown, are cut
To 2011 end of the years, the whole world shares 34,200,000 people and has infected HIV.China's HIV/AIDS Epidemic is in the rapid growth phase at present, sense
Dye number exceedes 780,000 (UNAIDS, 2011).Therefore, the prevention and treatment of HIV/AIDS is had become and cannot be neglected social concern and great
Scientific research task.Research and develop the main path that novel inverase is treatment and prevention and control AIDS.Since the 1990s, with
The mankind to virus and its course of infection molecular biology research deepen continuously and the continuous wound of medicament research and development technology
Newly, antiviral drugs has the drug of the development advanced by leaps and bounds, especially AntiHIV1 RT activity.Many large-scale international drugmakers, such as brightness
Auspicious, Merck, GlaxoSmithKline PLC, Roche, Abbott Laboratories, Bristol Myers Squibb etc., investment vast resources are used for the medicament research and development of AntiHIV1 RT activity.
Wherein, part company has possessed a variety of inverases, and obtains abundant income and return whereby.From 1987 first
Treat HIV infection drug azidothymidine (zidovudine, AZT) be approved by the FDA in the United States listing since, end 2013 it is existing
The chemical entities drug of 33 kinds of anti HIV-1 virus is approved by the FDA in the United States listing, including 18 kinds of reverse transcriptase inhibitor, 11 kinds
Protease inhibitors, 2 kinds of integrase inhibitors, a kind of CCR5 cooperative expert systems antagonist and a kind of membrane fusion inhibitor (USFDA,
2013).These anti-HIV new medicaments for continuing to bring out out can effectively inhibit the duplication of inhibition of HIV in human body, slow down AIDS
Development process substantially increases the mean survival time of aids patient.But due to these drugs be predominantly targeting reverse transcriptase,
Limited several virus proteins such as protease, Gp41 and integrase, virus, which passes through frequently to make a variation easily adaptation and escape drug, to be applied
The selection pressure added.With being widely used for these drugs, it is easy to generate cross resistance and serious toxic side effect, make it
Clinical application is very limited.And AntiHIV1 RT activity infection medicine used at present, there is also other various disadvantages, such as price is high
It is expensive, inconvenient to use, toxicity is high, take medicine it is cumbersome, internal virus cannot be removed etc..For the above reasons, developing new drug gesture is must
Row, needs constantly to formulate out new, efficient, inexpensive inverase.
Drug reorientation (Drug Repositioning) is the preference policy of quick discovery anticancer drug.Drug is reset
Position, also referred to as old medicine newly uses, refer to existing drug is screened again, combined or is transformed using relevant technical method from
And find the process of its unknown new application.Compared to zero-based new drug development, drug relocates the weight based on existing drug
It is newly developed to save a large amount of Innovation Inputs early period (such as discovery of medicine target, screening compound, security test).Therefore, system
The AntiHIV1 RT activity potentiality that all marketed drugs were excavated and evaluated on ground are used for AIDS for the discovery of novel inverase and drug reorientation
Disease treatment is of great significance and substantial worth.But it is a difficult, flower that all marketed drugs are screened by testing
Take expensive and time-consuming process.
Therefore the present invention has found and verifies Dalbavancin have using the method for predictive compound HIV-resistant activity newly developed
HIV-resistant activity can be applied in the drug of preparation treatment AIDS.Currently, there are no in the prior art rapidly and accurately
Prediction and the report for finding existing method of the drug with HIV-resistant activity, it is living with AntiHIV1 RT activity also to there are no compound Dalbavancin
The report of property.
Summary of the invention
It is an object of the invention to open up the new application of Dalbavancin (Dalbavancin) drug, Dalbavancin is provided
(Dalbavancin) application in the drug of preparation treatment AIDS.
In order to realize above-mentioned purpose of the invention, the present invention provides the following technical solutions:
The application of Dalbavancin and its pharmaceutically acceptable salt in preparation treatment AIDS-treating medicine.
The application of Dalbavancin and its pharmaceutically acceptable salt as mentioned in preparation treatment AIDS-treating medicine, wherein
Dalbavancin has significant HIV-resistant activity and cytotoxicity is lower.
The application of Dalbavancin and its pharmaceutically acceptable salt as mentioned in preparation treatment AIDS-treating medicine, wherein
Toxicity very little of the Dalbavancin to cell, CC50>200μM；It is equal to EC in concentration50When, Dalbavancin is complete to cell C8166
There is no toxicity entirely.
The application of Dalbavancin and its pharmaceutically acceptable salt as mentioned in preparation treatment AIDS-treating medicine, wherein
Dalbavancin forms the EC of the inhibiting effect of plasomidum to HIV-1 induction C8166 cell50It is 8.694 μM, therapeutic index TI is greater than
23.0；Show that Dalbavancin inhibits the EC of p24 antigenic action in HIV-1p24 antigen quantitative result50It is 1.296 μM, therapeutic index
TI is greater than 135.1.
The application of Dalbavancin and its pharmaceutically acceptable salt as mentioned in preparation treatment AIDS-treating medicine, it is special
Sign is in the drug that effective component Dalbavancin and its pharmaceutically acceptable salt account for 0.5-90%.
The application of Dalbavancin and its pharmaceutically acceptable salt as mentioned in preparation treatment AIDS-treating medicine, wherein
Detection Dalbavancin and its pharmaceutically acceptable salt HIV-resistant activity are to select human T lymphocyte system C8166 and HIV-1 experiment
Strain HIV-1NL4-3External cytotoxicity and HIV-resistant activity experiment are carried out to Dalbavancin, wherein cytotoxicity uses MTT colorimetric
Method detection, HIV-resistant activity inhibits to test using plasomidum and both HIV-1p24 antigen is quantitative method is detected.
The application of Dalbavancin and its pharmaceutically acceptable salt as mentioned in preparation treatment AIDS-treating medicine, wherein
The pharmaceutically acceptable salt of the Dalbavancin refers to that the salt formed with organic acid, the organic acid are tartaric acid, first
Acid, acetic acid, ethanedioic acid, butyric acid, maleic acid, succinic acid, adipic acid, alginic acid, citric acid, aspartic acid, benzene sulfonic acid, camphoric acid,
Camphorsulfonic acid, didextrose acid, pentamethylene propionic acid, dodecyl sulphate, ethanesulfonic acid, glucoheptonic acid, phosphoglycerol, enanthic acid, caproic acid,
Fumaric acid, lactic acid, methanesulfonic acid, niacin, 2- naphthalene sulfonic acids, flutters acid, pectinic acid, 3- phenylpropionic acid, new penta at 2- ethylenehydrinsulfonic acid
Acid, propionic acid, p- toluenesulfonic acid and hendecanoic acid.
It when Dalbavancin is as drug, can be used directly, or used in the form of pharmaceutical composition.The pharmaceutical composition
In the Dalbavancin compound containing 0.1-99%, the effective component Dalbavancin of preferably 0.5-90%, remaining is materia medica
With acceptable in pharmacy, the pharmaceutic adjuvant nontoxic to humans and animals or carrier.
The pharmaceutical carrier is one or more solids, semisolid and/or liquid diluent, filler and pharmaceutical preparation
Auxiliary material.Pharmaceutical composition of the invention is used in the form of per weight dose.Drug of the invention can be injected (intramuscular injection and
Intravenous) and oral two kinds of forms administration.
Compared with prior art, excellent benefit of the present invention is:
In order to predict and find out the medical compounds with HIV-resistant activity, the present invention for the first time using following technology come into
Row operation.There is presently no only utilize compound structure can direct predictive compound HIV-resistant activity method.The present invention
By using a large amount of HIV-resistant activity data and integrating the molecular fingerprint method and machine learning method of relative frequency weight
(vector machine and random forest) realizes the prediction to the HIV-resistant activity of compound.The technology only needs to input the knot of compound
Structure can quickly and accurately predict whether the compound has HIV-resistant activity.Using the technology we have found that Da Bawan
Star has significant HIV-resistant activity and cytotoxicity is lower, can apply in the drug of preparation treatment AIDS.Dalbavancin
It is currently the drug for being used to prepare treatment acute bacterial skin and skin structure infection as caused by gram-positive bacteria.Cause
This, does not there is the record of any following mechanism and method also in the prior art:
The present invention is predicted and is sent out using the anti-HIV-1 compounds that one is known as " Anti-HIV-Predictor " have been initially set up
It digs platform (http://bsb.kiz.ac.cn/Anti-HIV-Predictor).The establishment process of the platform is shown in Fig. 1.The platform
3 kinds of methods (molecular fingerprint method, support vector machine method and the random forest method of relative frequency weight) are integrated come prediction
Close the HIV-resistant activity of object.Area is greater than 0.95 under the ROC curve line of the platform and accuracy rate is more than 93% (Fig. 2).Therefore should
Platform can rapidly and accurately predict whether appointed compound has HIV-resistant activity.The present invention is flat to having listed using this
1835 drugs are predicted and are screened, and are used for anti-hiv therapy to carry out drug reorientation to these drugs.Present invention prediction
Up to the present several new anti-HIV-1 compounds out, these compounds did not all do any HIV-resistant activity experiment.Therefore,
The present invention has carried out a series of external HIV-resistant activity to these compounds and has tested.Experimental result finds compound Dalbavancin
(Dalbavancin) there is significant HIV-resistant activity and cytotoxicity is lower.Therefore Dalbavancin has AIDS very high
Therapeutic index.Dalbavancin is a kind of novel semi-synthetic glycopeptides antibiotic, and mechanism of action is identical as vancomycin, is to inhibit G+
The biosynthesis of bacterium cell wall.Dalbavancin is approved for treatment by gram-positive bacteria (including methicillin-resistant staphylococcus
Staphylococcus) caused by acute bacterial skin and skin structure infection.Therefore, the present invention opens the new use of Dalbavancin
Application of the way i.e. as preparation treatment AIDS-treating medicine.
Dalbavancin (Dalbavancin) is to HIV-1NL4-3The HIV-resistant activity experimental result of Strain shows different dense
The Dalbavancin of degree is to HIV-1NL4-3The inhibiting effect of Strain.Dalbavancin forms plasomidum to HIV-1 induction C8166 cell
Inhibiting effect EC50It is 8.694 μM, therapeutic index TI is greater than 23.0.Da Bawan is shown in HIV-1p24 antigen quantitative result
The EC of star inhibition p24 antigenic action50It is 1.296 μM, therapeutic index TI is greater than 135.1.Above the experimental results showed that Dalbavancin
Cytotoxicity is smaller or nothing, there is significant HIV-resistant activity and higher therapeutic index, can be used as preparation treatment AIDS medicine
The application of object.
Detailed description of the invention
Fig. 1 is shown: anti-HIV-1 compounds are predicted and are excavated the establishment process of platform " Anti-HIV-Predictor " and in medicine
Application in object reorientation；
Fig. 2 is shown: anti-HIV-1 compounds prediction and the estimated performance for excavating platform " Anti-HIV-Predictor "；
Fig. 3 is shown: Dalbavancin is to the toxic effect (shown in square curve) of C8166 and to the inhibiting effect of HIV-1p24
(shown in circle point curve).
Specific embodiment
With reference to the accompanying drawing, essentiality content of the invention is further illustrated with the embodiment of the present invention, but not with
This limits the present invention.
Embodiment 1
Test the AntiHIV1 RT activity effect of Dalbavancin (Dalbavancin):
1, experiment purpose: the AntiHIV1 RT activity effect of test Dalbavancin (Dalbavancin)
2, experimental material
2.1. drug and compound are measured
Sample to be tested Dalbavancin is purchased from Beijing Le Bo Biotechnology Co., Ltd.Positive reference compound retrovir
(3 '-Azido-3 '-deoxythymidine, AZT) is purchased from Sigma company.Sample to be tested is dissolved in RPMI- according to dissolubility
In 1640 complete mediums or DMSO, the sample stock concentrations being dissolved in DMSO are 50mM, are dissolved in RPMI-1640 and train completely
The sample stock concentrations for supporting base are 10mM, 5mM or 2mM (being determined according to solubility), condition of storage are as follows: -20 DEG C；AZT is dissolved in
In RPMI-1640 complete medium, 0.22 μm of membrane filtration degerming, storage liquid concentration is 6mg/ml, -20 DEG C of preservations after packing.
2.2. reagent and solution
2.2.1. reagent
HEPES(N-2(2-Hydroxyothyl)piperazine-N'-(2-ethanesufonic acid)、MTT(3,
(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide)、DMF(N,N’-
Dimethyl formamine), penicillin (Penicillin), streptomycin sulphate (Streptomycin sulfate), paddy ammonia
Amide (Glutamine) is purchased from Sigma company；2 mercapto ethanol (2-ME, 2-Mercaptoethanol) is Bio-Rad
Products.RPMI-1640 and fetal calf serum are Invitrogen Products.
2.2.2. culture medium
RPMI-1640 complete medium contains 10% fetal calf serum, 2mM glutamine, 10mM HEPES, 50 μM of 2- mercaptos
Base ethyl alcohol, 100,000IU penicillin, 100 μ g/ml streptomysins.
2.3. cell and virus
Human T lymphocyte system C8166, HIV-1 test strain HIV-1ⅢBBy Britain Medical Research Council,
AIDS Reagent Project give.HIV-1 tests strain HIV-1NL4-3It is given by NIH.All cells and virus are to contain
The RPMI-1640 complete medium of 10% fetal calf serum is cultivated.HIV-1 is prepared according to a conventional methodⅢBAnd HIV-1NL4-3, drop
Determine and calculate the TCID of virus50.After virus storage liquid packing, -70 DEG C of preservations are set.Cell and virus freeze according to a conventional method and
Recovery.
3, HIV-1 infectious titration
HIV-1NL4-3It is titrated, is summarized as follows: by HIV-1 by the improvement of Johnson&Byington (1990) the method
Storage liquid makees 4 times of dilutions, 10 gradients, 6 repeating holes of every gradient on 96 orifice plates, while 6 hole of control wells is arranged.Every hole is added
50 μ l of C8166 cell, every hole final volume are 200 μ l.37 DEG C, 5%CO2Culture.Fresh RPMI-1640 is added within 3rd day to train completely
100 μ l of base is supported, the cytopathic effect (Cytopathic that HIV-1 is induced in every hole is observed within the 7th day under inverted microscope
Effect, CPE), whether there is the formation of plasomidum (Syncytium) to determine with every hole；Virus is calculated by Reed&Muench method
TCID50(50%Tissue Culture Infection Dose).
4, to the toxicity test of C8166 cell
4×105100 μ l of/ml C8166 cell suspension is mixed from different drug solutions to be measured, if 3 repeating holes.Simultaneously
The control wells of not drug containing are set, 37 DEG C, 5%CO2Culture 3 days, using MTT colorimetric determination cytotoxicity.ELx800 enzyme mark
Instrument measures OD value, and measurement wavelength is 570nm, reference wavelength 630nm.CC is calculated50It is worth (50%Cytotoxic
Concentration), i.e., to 50% normal T-lymphocytes system C8166 generate toxicity when drug concentration.
5, to HIV-1NL4-3The Inhibition test of cytopathogenic effect (CPE)
By 8 × 10550 hole μ l/ of/ml C8166 cell is inoculated into 96 holes containing 100 μ l/ gradient pores doubling dilution drugs
On tissue culture plate, the HIV-1 of 50 μ l is then addedNL4-3Dilute supernatant, the hole 1300TCID50/.If 3 repeating holes.It sets simultaneously
Set the normal cell controls hole of not drug containing.AZT is positive drug control.37 DEG C, 5%CO2Culture 3 days, under inverted microscope
(100 ×) formation of plasomidum is counted.EC50(50%Effective Concentration) is to inhibit Syncytium formation 50%
When drug concentration.
6, to HIV-1NL4-3The Inhibition test of virus replication in acute infection C8166 cell
By 4 × 105The C8166 cell and HIV-1 of a/mLNL4-3(MOI=0.04) it is infected 2 hours at 37 DEG C, uses PBS
Centrifuge washing 2 times, free viral ion is removed, takes 100 μ L cell inoculations to containing 100 μ L difference dilution untested compounds
96 orifice plates on, 37 DEG C, 5%CO2 cultivate 3 days.Culture supernatant is collected after centrifugation, and is split with final concentration 0.5%Triton X-100
Solution inactivation.Detection drug uses the inhibiting effect that HIV-1 is replicated and captures p24 antigen ELISA method.
7, ELISA detects p24 antigen
The anti-4 DEG C of plate overnights of mouse IgG-Fc antibody of 1 μ L/ plate；5% 4 DEG C of skimmed milk power sealing plate is stayed overnight；100 hole μ l/ mouse are added
Anti- p24 monoclonal antibody (is prepared, Liu G J, Wang J P, Xiao J C, et using the method that Liu G J et al. is established
al.Preparation and characterization of three monoclonal antibodies against
HIV-1p24capsid protein [J] .Cell MolImmunol, 2007,4 (3): 203-208.) 37 DEG C, 1 hour；It is added
100 holes μ l/ cracking infection cell culture supernatant, 37 DEG C, 2 hours；Mostly anti-(the benefit of the diluted rabbit-anti p24 in 100 hole μ l/ 1: 100 is added
The method preparation established with Liu G J et al., Liu G J, Wang J P, Xiao J C, et al.Preparation and
characterization of three monoclonal antibodies against HIV-1p24capsid
Protein [J] .Cell MolImmunol, 2007,4 (3): 203-208.), 37 DEG C, 1 hour；100 holes μ l/ 1: 20000 are added
Diluted goat anti-rabbit igg-HRP (Sigma), 37 DEG C, 1 hour；OPD substrate reactions liquid is added.After ten minutes, 2M sulfuric acid terminates anti-
It answers.Elx800ELISA instrument measures OD value, measures wavelength 490nm, reference wavelength 630nm.Drug is calculated to HIV-1 duplication table
Up to the inhibiting rate and EC50 of p24 antigen, that is, inhibit the drug concentration of 50%HIV-1p24 antigen presentation.
8, calculation formula
Dose-effect curve is drawn according to experimental result, compound is calculated by Reed&Muench method and inhibits virus
50% effective concentration (EC50), 50% inhibits cell growth concentration (CC50) and Anti-HIV-1 Active therapeutic index TI value
(Therapeutic index) are as follows: TI=CC50/EC50。
1), cell grows survival rate (%)=experimental port OD value/value × 100 control wells OD
2), the inhibiting rate (%) of HIV-1 cytopathogenic effect=(1- experimental port plasomidum number/control wells plasomidum number) ×
100
3), the inhibiting rate (%) of HIV-1p24 antigen presentation=(1- experimental port OD value/control wells OD value) × 100
9, experimental result and evaluation
9.1. toxicity test result of the Dalbavancin (Dalbavancin) to C8166 cell
Table 1 lists the CC of Dalbavancin50, Fig. 3 (shown in square curve) of the invention shows the Da Ba of various concentration
Toxic effect of ten thousand stars to cell C8166.The experimental results showed that toxicity very little of the Dalbavancin to cell, CC50>200μM(CC50
Bigger expression toxicity is smaller).It is equal to EC in concentration50When (1.296 μM), Dalbavancin is to cell C8166 absolutely not toxicity (figure
3)。
9.2. Dalbavancin (Dalbavancin) is to HIV-1NL4-3The HIV-resistant activity experimental result of Strain
Table 1 lists the EC of Dalbavancin50, Fig. 3 (shown in circle point curve) of the invention shows the Da Ba of various concentration
Ten thousand stars are to HIV-1NL4-3The inhibiting effect of Strain.The inhibition that Dalbavancin forms plasomidum to HIV-1 induction C8166 cell is made
EC50It is 8.694 μM, therapeutic index TI is greater than 23.0.Show that Dalbavancin inhibits p24 in HIV-1p24 antigen quantitative result
The EC of antigenic action50It is 1.296 μM, therapeutic index TI is greater than 135.1.
Above the experimental results showed that the cytotoxicity of Dalbavancin is smaller or nothing, there is significant HIV-resistant activity and higher
Therapeutic index, can be used as preparation treatment AIDS-treating medicine application.
1. Dalbavancin of table (Dalbavancin) is to HIV-1NL4-3The inhibiting effect of Strain and poison to C8166 cell
Property effect
Embodiment 2:
Excipient, granulation pressure is added in the ratio of Dalbavancin (Dalbavancin) and excipient weight ratio 1:1 or 1:2
Piece.
Embodiment 3:
Dalbavancin (Dalbavancin) is effective component, and routinely capsule is made in capsule preparations method.
Embodiment 4:
Tablet: Dalbavancin (Dalbavancin) 10mg
Appropriate starch
Appropriate corn pulp
Magnesium Stearate proper quantity
Preparation method: will be mixed by Dalbavancin (Dalbavancin) with auxiliary agent, sieving, in suitable container uniformly
Mixing, obtained granulating mixture tabletting.
Embodiment 5:
Capsule: Dalbavancin (Dalbavancin) 10mg
Appropriate starch
Magnesium Stearate proper quantity
Preparation method: Dalbavancin (Dalbavancin) is mixed with auxiliary agent, and sieving uniformly mixes in suitable container
It closes, obtained mixture is packed into hard gelatin capsule.
Embodiment 6:
Tablet: Dalbavancin (Dalbavancin) 10mg, lactose 180mg, starch 55mg, magnesium stearate 5mg.
Preparation method: Dalbavancin (Dalbavancin), newborn sugar and starch are mixed, uniformly moistened with water, after wet
Mixture be sieved and dry, magnesium stearate is added in re-sieving, and then by mixture tabletting, every slice weight 250mg, compound contains
Amount is 10mg.
Embodiment 7:
Ampulla: Dalbavancin (Dalbavancin) 2mg, sodium chloride 10mg；
Preparation method: Dalbavancin (Dalbavancin) and sodium chloride are dissolved in suitable water for injection, filter institute
Solution is obtained, is aseptically fitted into ampoule bottle.
Embodiment 8:
Capsule: Dalbavancin (Dalbavancin) 10mg, lactose 187mg, magnesium stearate 3mg；
Preparation method: Dalbavancin (Dalbavancin) is mixed with auxiliary agent, and sieving uniformly mixes, obtained mixing
Object is packed into hard gelatin capsule, each capsule weight 200mg, active component content 10mg.
Claims (1)
1. the application of Dalbavancin and its pharmaceutically acceptable salt in preparation treatment AIDS-treating medicine.
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| CN1634922A (en) * | 2004-09-24 | 2005-07-06 | 中国科学院昆明植物研究所 | Anti-AIDS compound, its preparing method and pharmaceutical composition with anti-AIDS compound as active component and use thereof |
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