CN119055667A - Application of psyllium glycosides in the preparation of drugs for the prevention and treatment of AIDS - Google Patents

Abstract

The invention discloses an application of plantain in preparing drugs for preventing and treating AIDS, which adopts three cell virus infection models of TZM-bl-HIV-1 _IIIB、MT-2-HIV-1_IIIB and peripheral blood mononuclear cells PBMCs-HIV-1 _BaL to verify the anti-HIV activity of the plantain, and researches the action mechanism of the plantain against HIV-1 by detecting the action target point of the drugs through experiments, and the research shows that the plantain can reduce the HIV-1 virus level in the safe concentration range without cytotoxicity in the TZM-bl-HIV-1 _IIIB、MT-2-HIV-1_IIIB and the PBMCs-HIV-1 _Bal models. Therefore, the invention discovers that the homoplantagin can be a potential multi-target inhibitor for resisting HIV-1, can be used for preventing or treating HIV infection, and becomes a potential anti-HIV drug.

Description

Application of homoplantagin in preparing medicine for preventing and treating AIDS

Technical Field

The invention belongs to the technical field of development of AIDS treatment medicines, and particularly relates to application of homoplantain in preparation of medicines for preventing and treating AIDS.

Background

According to the latest statistics published by the disease prevention and control bureau before date, 2021 AIDS (acquiredimmunedeficiencysyndrome, AIDS) reports 60154 cases of morbidity and 19623 cases of mortality, the morbidity is 4.2669/10 ten thousand, the mortality rate is as high as 1.3919/10 ten thousand, and the number of dead people is the first place of the first and second infectious diseases. At present, although more than 30 kinds of anti-HIV medicines exist in 6 kinds, the anti-HIV (humanimmunodeficiencyvirus, HIV) medicines used for clinical treatment still have a plurality of defects, such as that viruses in patients still remain, the drug resistance of the viruses is also enhanced, the dependence of the patients on the medicines is enhanced, the medicines need to be continuously taken, and various toxic and side effects caused by the medicines are born, so that the medicines for effectively and radically curing the diseases have not been developed so far worldwide, and therefore, the development of novel anti-HIV medicines is urgent.

HIV is an RNA virus belonging to the family retrovirus and genus lentivirus. During infection by HIV, the HIV-1 outer membrane glycoprotein gp120 specifically binds to the CD4 receptor on the surface of T4 lymphocytes and is adsorbed to the cells. With the aid of the accessory receptor CCR5 or CXCR4, the HIV-1 outer membrane glycoprotein gp41 fuses with the host cell membrane to allow entry of the virion into the cell, and subsequent removal of the capsid exposes the nucleic acid. The HIV-1 single-stranded RNA is reverse transcribed into single-stranded DNA under the catalysis of viral reverse transcriptase and ribonuclease H, and is in turn catalyzed into double-stranded DNA by cellular polymerase in the nucleus. The integrase of HIV-1 allows the double stranded DNA provirus to integrate into the chromosome of the host cell, resulting in a latent infection of HIV-1. The mRNA of the virus synthesized by using the integrated virus DNA as a template is translated into large fusion polyproteins, and then the polyproteins are spliced and processed under the action of virus protease to form mature virus structural proteins. Since HIV is prone to mutation during replication, the specific HIV inhibitors currently used are often of a narrow antiviral spectrum and therefore are prone to developing resistance. Therefore, there is a need to develop novel compounds with high efficacy, low toxicity and low drug resistance to cope with changes in HIV.

Herba plantaginis glycoside (Hom) is extracted from herba Salviae Plebeiae of Salvia of Labiatae, and belongs to flavonoid compounds. The common sage herb is also called as toad grass, snow common sage herb, wrinkled giant hyssop, frog grass and the like, is originally carried in the compendium of materia medica, has cool and bitter taste, has the efficacies of clearing heat, detoxification, cooling blood, stopping bleeding, promoting urination and the like, and has the pharmacological effects of resisting inflammation, oxidization, bacteria, virus and the like, is used for treating swelling and pain of throat, bronchitis, nephritis edema, carbuncle swelling and the like, externally treats diseases such as mastitis, hemorrhoids swelling and pain, hemorrhage and the like, and is produced in various places except Xinjiang, gansu, qinghai and Tibet. The homoplantain is one of main components of common sage herb, belongs to flavonoid compounds, has been the focus of drug research, has demonstrated its wide biological activity, and a plurality of documents report their antiviral ability. A methanol extract of Rhussuccedanea (Rhus verniciflua of Myricaceae) containing flavonoids robustaflavone and hinokitiol inhibits polymerase activity of HIV-1RT, wikstrolB is another biflavone isolated from extract of root of Wikstroemiaindica (Rabdosia of Rutaceae), and has anti-HIV-1 activity. Isoflavones and pterocarpan were found to have anti-HIV activity from the Erythrina genus of plants. Xanthohumol obtained from hops Humuluslupulus also inhibits HIV-1.

The anti-HIV activity of the homoplantagin has not been reported yet, and early pharmacological studies show that the homoplantagin has various pharmacological effects of relieving cough and asthma, treating liver injury, improving endothelial insulin resistance, inhibiting tumor growth, resisting osteoporosis, inducing cancer cell apoptosis, inhibiting a-glycosidase and the like. Experiments show that the homoplantagin has the functions of reducing blood sugar and regulating blood fat, can obviously improve the generation of NO, can improve vascular endothelial insulin resistance caused by free fatty acid, can protect vascular endothelial cells by inhibiting the generation of active oxygen, has the action mechanism related to antioxidant stress and has the function of resisting angiogenesis.

Disclosure of Invention

In order to solve the problems that most of HIV medicaments in the prior art are single-target inhibitors, the antiviral curative effect is clinically improved mainly through a plurality of medicament combinations (HAART), the defects of strong side effect, high medicament resistance and the like are overcome, the application provides a novel application of the homoplantaginide, and the application of a plurality of cell virus infection models to deeply research the anti-HIV-1 activity of the homoplantaginide extracted from common sage herb, provides a theoretical basis for developing novel anti-HIV-1 medicaments with originality and independent intellectual property rights, can be applied to further development and application of the anti-HIV medicaments, and provides application of the homoplantaginide in preparation of medicaments for preventing and treating AIDS, wherein the homoplantaginide is used for preparing homoplantaginide derivatives or compound medicaments containing the homoplantaginide, and has the following structural formula:

further, the AIDS is HIV-1 type.

Further, the homoplantagin and pharmaceutically acceptable auxiliary materials form a preparation.

Further, the preparation comprises injection, capsule, tablet, granule, sugar-coated pill and solution.

Further, the dosage form comprises a common excipient and a medicinal excipient;

the common excipients comprise fillers and solubilizers, binders, wetting agents, disintegrants, absorbents and lubricants;

The pharmaceutical excipients include solid, semi-solid, liquid forms.

Compared with the prior art, the application has the following advantages and effects:

1. The invention develops the anti-HIV-1 activity research of the homoplantagin for the first time, adopts three cell infection systems in HIV-1 strains with different tropisms and combines experiments to reveal the potential anti-HIV action mechanism of the two, and has original innovation.

2. The key point of the invention is to use various cell lines and different mesophilic viruses to develop an activity experiment of the plantain for resisting HIV-1, and reveal a potential action mechanism of the plantain, aiming at further researching the anti-HIV medicinal potential of the plantain so as to discover a high-efficiency low-toxicity low-cost multi-target anti-HIV medicament, solve the dilemma of the current clinical AIDS treatment, and lay a foundation for further mining the clinical value of the plantain.

3. The study of the invention finds that the homoplantagin plays an anti-HIV-1 role mainly by inhibiting reverse transcriptase and protease in the HIV-1 replication process. In addition, the invention adopts three cell infection models, and the high plantain glycoside has stronger anti-HIV-1 activity. In vitro pharmacological experiments are carried out by constructing three virus infection models through two virus strains of three cells, so that the inhibition effect of the homoplantagin on HIV-1 replication with different tropisms is further clarified.

The foregoing description is only an overview of the present application, and is intended to provide a better understanding of the technical means of the present application, so that the present application may be practiced according to the teachings of the present specification, and so that the above-mentioned and other objects, features and advantages of the present application may be better understood, and the following detailed description of the preferred embodiments of the present application will be presented in conjunction with the accompanying drawings.

The above and other objects, advantages and features of the present application will become more apparent to those skilled in the art from the following detailed description of the specific embodiments of the present application when taken in conjunction with the accompanying drawings.

Drawings

In order to more clearly illustrate the embodiments of the present application or the technical solutions in the prior art, the drawings that are required in the embodiments or the description of the prior art will be briefly described, and it is obvious that the drawings in the following description are some embodiments of the present application, and other drawings may be obtained according to these drawings without inventive effort for a person skilled in the art. Like elements or portions are generally identified by like reference numerals throughout the several figures. In the drawings, elements or portions thereof are not necessarily drawn to scale.

Wherein:

FIG. 1 is a schematic structural diagram of homoplantagin.

FIG. 2 is a flow chart of the mechanism of action of homoplantagin against HIV-1.

FIG. 3 is a schematic representation of the cytotoxicity and anti-HIV-1 activity of homoplantagin in a TZM-bl-HIV-1 _IIIB cell infection model:

3A TZM-bl cytotoxicity dose response curve of homoplantagin;

3B, an anti-HIV-1 active dose response curve of homoplantagin in a TZM-bl-HIV-1 _IIIB cell infection model;

TZM-bl cytotoxicity dose response curves for 3C: AZT;

3D AZT dose response curve against HIV-1 activity in TZM-bl-HIV-1 _IIIB cell infection model.

FIG. 4 is a schematic representation of the cytotoxicity and anti-HIV-1 activity of homoplantagin in MT-2-HIV-1 _IIIB cell infection model:

4A, MT-2 cytotoxic dose response curve of homoplantagin;

4B, anti-HIV-1 active dose response curve of homoplantagin in MT-2-HIV-1 _IIIB cell infection model;

MT-2 cytotoxic dose response curve for 4c: azt;

4D AZT dose response curve against HIV-1 activity in MT-2-HIV-1 _IIIB cell infection model.

FIG. 5 is a schematic representation of cytotoxicity of homoplantagin (A) and AZT (B) in PBMCs and HIV-1p24 levels.

FIG. 6 is a graph showing the results of the inhibition of HIV-1 induced CPE by homoplantagin.

FIG. 7 is a graph showing the results of the inhibition of HIV-1 virus key enzyme activity by homoplantaginide:

7A, influence of homoplantagin on HIV-1RT activity, and taking NVP as a positive drug control;

7B, influence of homoplantagin on HIV-1PR activity, wherein PEPSTATINA is used as a positive medicine control;

7C, influence of homoplantagin on HIV-1IN activity, and taking sodium azide as a positive drug control.

DETAILED DESCRIPTION OF EMBODIMENT (S) OF INVENTION

For the purpose of making the objects, technical solutions and advantages of the embodiments of the present application more apparent, the technical solutions of the embodiments of the present application will be clearly and completely described below with reference to the accompanying drawings in the embodiments of the present application, and it is apparent that the described embodiments are some embodiments of the present application, but not all embodiments of the present application. In the following description, specific details such as specific configurations and components are provided merely to facilitate a thorough understanding of embodiments of the application. It will therefore be apparent to those skilled in the art that various changes and modifications can be made to the embodiments described herein without departing from the scope and spirit of the application. In addition, descriptions of well-known functions and constructions are omitted in the embodiments for clarity and conciseness.

It should be appreciated that reference throughout this specification to "one embodiment" or "this embodiment" means that a particular feature, structure or characteristic described in connection with the embodiment is included in at least one embodiment of the present application. Thus, the appearances of the "one embodiment" or "this embodiment" in various places throughout this specification are not necessarily all referring to the same embodiment. Furthermore, the particular features, structures, or characteristics may be combined in any suitable manner in one or more embodiments.

Furthermore, the present application may repeat reference numerals and/or letters in the various examples. This repetition is for the purpose of simplicity and clarity and does not in itself dictate a relationship between the various embodiments and/or configurations discussed.

The term "and/or" herein is merely one kind of association relation describing the association object, and indicates that three kinds of relations may exist, for example, a and/or B may indicate that a alone exists, B alone exists, and a and B exist simultaneously, and the term "/and" herein is another kind of association object relation describing that two kinds of relations may exist, for example, a/and B may indicate that a alone exists, and a and B exist separately, and in addition, a character "/" herein generally indicates that the association object is an "or" relation.

The term "at least one" is used herein to describe only one association relationship of associated objects, and means that three relationships may exist, for example, at least one of A and B may mean that A exists alone, while A and B exist together, and B exists alone.

It is further noted that relational terms such as first and second, and the like are used solely to distinguish one entity or action from another entity or action without necessarily requiring or implying any actual such relationship or order between such entities or actions. Moreover, the terms "comprise," "include," or any other variation thereof, are intended to cover a non-exclusive inclusion.

Example 1

The application of homoplantagin in preparing medicine for preventing and treating AIDS is described in the embodiment, please refer to FIG. 1, the homoplantagin is used for preparing homoplantagin derivatives or compound medicine containing homoplantagin, and the structural formula of the homoplantagin is as follows:

further, the AIDS is HIV-1 type.

Furthermore, the homoplantagin can be mixed with conventional auxiliary materials to prepare various dosage forms for prevention or treatment. Injection, capsule, tablet, granule, sugar-coated pill, solution, etc. are all available in the form of alternative medicine. The dosage forms of capsules, tablets, granules, dragees, solutions and the like can be prepared by known conventional methods.

Further, the dosage forms of capsules, tablets, granules, dragees and the like may contain one or more commonly used excipients-fillers and solubilizing agents, such as starches, microcrystalline cellulose and the like, binders, such as carboxymethyl cellulose, polyvinylpyrrolidone and the like, wetting agents, such as glycerin, disintegrating agents, such as calcium carbonate and the like, absorbents, such as kaolin and the like, lubricants, such as talc and the like.

Further, the pharmaceutically acceptable excipients may be in various forms such as solid, semisolid, liquid, etc., and the formulation auxiliary may be of various types.

Further, the solution may contain general solvents, solubilizers, emulsifiers, preservatives, etc., such as water, ethanol, glycerol, polyethylene glycol, benzyl benzoate, etc.

Example 2

The present example describes the mechanism of action of homoplantagin in anti-AIDS drugs, and further described based on the above example, as shown in FIG. 2, the present example adopts the following technical scheme that three cell virus infection models, namely TZM-bl-HIV-1 _IIIB、MT-2-HIV-1_IIIB and peripheral blood mononuclear cells PBMCs-HIV-1 _BaL, are adopted to verify the anti-HIV activity of homoplantagin, and the action targets of drugs are detected through experiments to explore the anti-HIV-1 mechanism of action of homoplantagin.

Experiment one, cytotoxicity of homoplantagin in TZM-bl cells and anti-HIV-1 Activity

(1) Cytotoxicity test

TZM-bl cells after pancreatin digestion were collected, adjusted to a concentration of 1X 105 cells/ml with DMEM complete medium, and inoculated into 96-well cell culture plates at a volume of 100. Mu.l/well. Placed in a 37℃incubator with 5% CO2 for cultivation. The next day, serial dilutions of compound (40 μl/well) were added and 3 replicate wells were set at the same concentration. Cells treated without compound were also used as negative controls, culture medium was used as background control, and culture medium was supplemented per well to a total volume of 200 μl. After placing the cell culture plate into an incubator for further culturing for 48 hours, 20. Mu.l/well of the culture plate was addedThe cell viability detection reagent is vibrated for 3min, placed in a 37 ℃ and 5% CO2 incubator for incubation for 10min, finally, the luminescence signal is detected on a multifunctional enzyme label instrument, and the relative cell activity is calculated according to the following formula that the cell activity (%) = (experimental hole luminescence value-background hole luminescence value)/(negative control hole luminescence value-background hole luminescence value) ×100%.

(2) Antiviral Activity experiment

TZM-bl cells after pancreatin digestion were collected, adjusted to a concentration of 1X 105 cells/ml with DMEM complete medium, and inoculated into 96-well cell culture plates at a volume of 100. Mu.l/well. Placed in a 37℃incubator with 5% CO2 for cultivation. The next day, 100TCID50 HIV-1 _IIIB virus dilutions (60. Mu.l/well) and serial dilutions of compound (40. Mu.l/well) were added simultaneously, and 3 duplicate wells were set at the same concentration. The positive control wells were only virus-added, the negative control was simultaneously without compound and virus, and then the culture broth was supplemented to a total volume of 200 μl/well. After the cell culture plate was placed in an incubator for further culturing for 48 hours, 20. Mu.l/well of Bright-Glo ^TM Luciferase detection reagent was added, shake was performed for 3 minutes, and a luminescence signal was detected by a multifunctional microplate reader, and a relative virus level was calculated as the following formula: relative virus level (%) = (experimental well luminescence value-negative control well luminescence value)/(positive control well luminescence value-negative control well luminescence value) ×100%.

(3) Experimental results

Cell viability was measured by the ATP method to reflect cytotoxicity of the compound, which was considered to be present when cell viability was < 80%. As shown in FIG. 3, the relative activity of the TZM-bl cells treated with the homoplantagin is more than 80%, no obvious toxic effect on the TZM-bl cells is observed, and the homoplantagin can inhibit the replication of HIV-1 _IIIB in TZM-b1 in a dose-dependent manner at a concentration which does not affect the activity of the cells, and the relative viral load is reduced, namely the inhibition rate is increased, with the increase of the drug concentration. Under the treatment of the standard control drug AZT, the relative virus level of HIV-1 is reduced, and the dose dependence is better.

Example 3

The present embodiment describes the mechanism of action of homoplantagin in anti-AIDS drug, please refer to FIG. 4, based on the above embodiment for further description:

experiment two, cytotoxicity of homoplantagin in MT-2 cells and anti-HIV-1 activity.

(1) Cytotoxicity test

MT-2 cells in the logarithmic growth phase were prepared and the concentration was adjusted to 2X 10 ⁵ cells/ml with RPMI1640 complete medium, and inoculated into 96-well cell culture plates at a volume of 160. Mu.l/well. At the same time, serial dilutions of compound (40 μl/well) were added and 3 replicate wells were set at the same concentration. Cells treated without compound were used as negative control, culture medium was used as background control, and culture medium was supplemented to a total volume of 200. Mu.l. After placing the cell culture plate in an incubator for further culturing for 72 hours, 20. Mu.l/well of the culture plate was addedThe cell viability detection reagent is vibrated for 3min, placed in a 37 ℃ and 5% CO2 incubator for incubation for 10min, finally, the luminescence signal is detected on a multifunctional enzyme label instrument, and the relative cell activity is calculated according to the following formula that the cell activity (%) = (experimental hole luminescence value-background hole luminescence value)/(negative control hole luminescence value-background hole luminescence value) ×100%.

(2) Antiviral Activity experiment

MT-2 cells in the logarithmic growth phase were inoculated into 96-well cell culture plates at a density of 3.2X10 ⁴ cells/well. Serial dilutions of compound (40 μl/well) and 320TCID50 HIV-1 _IIIB virus dilutions were added simultaneously to make the total volume per well 200 μl, and 3 duplicate wells were set at the same concentration. The positive control wells were only virus-added, the negative control was simultaneously without compound and virus, and then the culture broth was supplemented to a total volume of 200 μl/well. After placing the cell culture plate into an incubator for further culture for 72 hours, 60 μl/well of supernatant is transferred to a TZM-bl cell plate inoculated 1 day in advance (3×10 ⁵ cells/ml, 100 μl/well), after further culture for 24 hours, 20 μl/well of Bright-Glo ^TM Luciferase detection reagent is added, shake is performed for 3 minutes, a luminescence signal is detected by a multifunctional enzyme-labeled instrument, and a relative virus level (%) is calculated according to the following formula: relative virus level (%) = (experimental well luminescence value-negative control well luminescence value)/(positive control well luminescence value-negative control well luminescence value) ×100%.

(3) Experimental results

As shown in FIG. 4, in the MT-2-HIV-1 _IIIB cell infection model, homoplantain has less than 50% of cell activity at the highest experimental concentration, has certain cytotoxicity to MT-2 cells, has the maximum non-toxic concentration of 200 mu mol/L (see FIG. 4A), and AZT has no influence on MT-2 cell activity at the maximum experimental concentration (10 mu mol/L) (see FIG. 4C, table 1). In the concentration range which does not affect the activity of the cells, homoplantagin can reduce the relative virus level of MT-2 cells HIV-1, and the relative virus amount is reduced, namely the inhibition rate is increased along with the increase of the concentration of the compound.

Example 4

The present embodiment describes the mechanism of action of homoplantagin in anti-AIDS drug, please refer to FIG. 5, based on the above embodiment for further description:

experiment three, high plantagin cytotoxicity in Peripheral Blood Mononuclear Cells (PBMCs) and anti-HIV-1 Activity.

(1) Cytotoxicity test

PBMCs after 3d stimulation with PHA were plated with 100U/ml of IL-2 in RPMI1640 complete medium to adjust the cells to 2X 10 ⁶ cells/ml, seeded in 96-well cell culture plates at a volume of 100. Mu.l/well, and serial dilutions of compound (40. Mu.l/well) were added at the same time, and 3 replicate wells were set at the same concentration. Cells treated without compound were used as negative control, culture medium was used as background control, and culture medium was supplemented per well to a total volume of 200 μl. Culturing in incubator for 12 hr, taking out, washing with PBS for three times, adding fresh culture solution, and culturing in incubator for 120 hr. Added to 20. Mu.l/wellThe cell activity detection reagent is oscillated for 3min, placed in an incubator for incubation for 10min, finally, the luminescence signal is detected on a multifunctional enzyme label instrument, and the relative cell activity is calculated according to the following formula, wherein the cell activity (%) = (experimental hole luminescence value-background hole luminescence value)/(negative control hole luminescence value-background hole luminescence value) ×100%.

(2) Antiviral Activity experiment

PBMCs after 3d stimulation with PHA were plated with 100U/ml of IL-2 in RPMI1640 complete medium to adjust the cells to 2X 10 ⁶ cells/ml, seeded in 96-well cell culture plates at a volume of 100. Mu.l/well, and 3 replicate wells were placed at the same concentration, with serial dilutions of compound (40. Mu.l/well) and appropriately diluted HIV-1 _Bal virus stock (p 24:44 ng/ml). Positive control wells were not added with compound while the culture broth was replenished to a total volume of 200 μl/well. After the cell plates were placed in an incubator for 12 hours, the cell plates were taken out and washed three times with PBS, the original volume of fresh culture solution was added, and the culture was returned to the incubator, after further culturing for 120 hours, the supernatant was collected, the HIV-1p24 content was detected by ELISA, and the relative virus level was calculated as relative virus level (%) = experimental well p24 content/positive control well p24 content x 100%.

(3) Experimental results

As shown in FIG. 5A, homoplantagin was non-cytotoxic to PBMCs over the experimental concentration range, and HIV-1p24 levels were reduced compared to the virus-infected group over the non-toxic concentration range. As shown in FIG. 5B, there was no significant decrease in PBMCs activity at the maximum experimental concentration of AZT (2. Mu. Mol/L), and the relative levels of HIV-1p24 were decreased compared to the virus-infected group. Homoplantaginide exhibits dose-dependent anti-HIV-1 activity similar to AZT over a non-toxic concentration range.

Example 5

The present embodiment describes the mechanism of action of homoplantagin in anti-AIDS drug, please refer to FIG. 6, based on the above embodiment for further description:

Experiment IV, inhibition of HIV-1 induced cytopathic Effect (CPE) by homoplantagin

MT-2 cells are induced to produce cytopathic effects (Cytopathiceffect, CPE) after infection with HIV-1 virus, forming syncytia. By means of a fully automatic cell imager, cytopathic effects produced by different concentrations of homoplantagin and AZT can be observed and compared with pure HIV-1 infected groups (positive control group) and pure cell groups (negative control group) to evaluate the inhibition of syncytia formation by the compounds. As shown in FIG. 6 (the formation of syncytia is observed under a microscope, as indicated by the red arrow in the figure) and Table 2, the compound-free HIV-1 infected group had a large amount of syncytia formed, the negative control group had no syncytia formed, and the amount of syncytia formed was correspondingly decreased in the different concentrations of the homoplantaginide group as the concentration of the compound was increased, and the homoplantaginide group had fewer syncytia formed at 200. Mu. Mol/L and 40. Mu. Mol/L compared to the HIV-1 infected group, thereby demonstrating that homoplantaginide could decrease HIV-1 induced syncytia certain concentration range.

TABLE 1 summary of in vitro cytotoxicity and anti-HIV-1 Activity data of plantaginside

(IC ₅₀: drug concentration effective to inhibit 50% of the virus)

TABLE 2 high plantagin inhibition of HIV-1 induced CPE conditions

Gaocapin can reduce HIV-1 virus levels in a safe concentration range without cytotoxicity in both TZM-b-HIV-1 _IIIB、MT-2-HIV-1_IIIB and PBMCs-HIV-1 _Bal models, and SI values are shown in Table 1. SI values of homoplantagin are greater than 20 in all three models, and based on the study, the mechanism of action of homoplantagin against HIV-1 will be continuously discussed.

Example 6

The present embodiment describes the mechanism of action of homoplantagin in anti-AIDS drug, please refer to FIG. 7, based on the above embodiment for further description:

experiment five, high plantain in vitro inhibiting HIV-1 key enzyme activity

The cell experiments show that the homoplantagin has a certain anti-HIV-1 activity, so that the enzyme ELISA kit is further used for detecting the influence of the homoplantagin on the activity of HIV-1 integrase (integrase, IN), reverse Transcriptase (RT) and Protease (PR). As shown in FIG. 7A, homoplantagin can reduce the activity of HIV-1 reverse transcriptase, the reverse transcriptase activity is lower than 40% at the maximum experimental concentration, and the enzyme activity gradually increases with the reduction of the compound concentration. As shown in FIG. 7B, homoplantagin can inhibit HIV-1 protease activity within a certain concentration range, the protease activity is lower than 20% at the highest experimental concentration, and the inhibition effect gradually decreases with the decrease of the concentration. As shown in FIG. 7C, homoplantagin had no significant inhibitory effect on HIV-1 integrase activity.

The above description is only of the preferred embodiments of the present invention and it is not intended to limit the scope of the present invention, but various modifications and variations can be made by those skilled in the art. Variations, modifications, substitutions, integration and parameter changes may be made to these embodiments by conventional means or may be made to achieve the same functionality within the spirit and principles of the present invention without departing from such principles and spirit of the invention.

Claims (5)

1. The application of the homoplantagin in preparing the medicine for preventing and treating the AIDS is characterized in that the homoplantagin is used for preparing homoplantagin derivatives or compound medicines containing the homoplantagin, and the structural formula of the homoplantagin is as follows:

2. the use of homoplantagin according to claim 1 for preparing medicine for preventing and treating AIDS, wherein the AIDS is HIV-1 type.

3. The use of homoplantagin according to claim 2 for preparing a medicament for preventing and treating aids, wherein said homoplantagin forms a formulation with pharmaceutically acceptable excipients.

4. Use of homoplantagin according to claim 3 for preparing medicine for preventing and curing AIDS, wherein the dosage forms of said preparation include injection, capsule, tablet, granule, sugar-coated pill and solution.

5. The use of homoplantagin in preparing medicine for preventing and treating AIDS according to claim 4, wherein the dosage form comprises common excipient and medicinal excipient;

the common excipients comprise fillers and solubilizers, binders, wetting agents, disintegrants, absorbents and lubricants;

The pharmaceutical excipients include solid, semi-solid, liquid forms.