CN1107152A - Compound for inhibition of virus HIV of AIDS - Google Patents
Compound for inhibition of virus HIV of AIDS Download PDFInfo
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- CN1107152A CN1107152A CN 94101625 CN94101625A CN1107152A CN 1107152 A CN1107152 A CN 1107152A CN 94101625 CN94101625 CN 94101625 CN 94101625 A CN94101625 A CN 94101625A CN 1107152 A CN1107152 A CN 1107152A
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- compound
- aids
- morusin
- hiv
- glucose
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Abstract
The AIDS is a kind of HIV virus infection disease of immune system, the mortality is very high. The chemical compound provided by said invention can inhibitate the activity of HIV virus of AIDS disease. It cures AIDS diease by curing and preventing the infection caused by HIV virus of AIDS disease. The invented compound and its derivates are extracted from traditional Chinese medicinal plant root bark of white mulberry. The invention provides a new kind of inhibiter for HIV virus of AIDS.
Description
The invention relates to the compound that suppresses the viral HIV of people's AIDS (AIDS), the compound library watt promise H(Kuwanon H that particularly from Chinese medicinal plant White Mulberry Root-bark morus alba L., extracts), Mo Luxin (morusin) and derivative Morusin-4'-O-glucose thereof (morusin-4 '-O-glucose), but the activity of inhibition of virus HIV of AIDS.
In order to prevent or treat the infection that is caused by virus HIV of AIDS, the treatment AIDS was once used chemical compound pyrimidine, indoles, hormonal compounds adenosine deaminase, AZT, peptide class, plant milk extract tonka bean camphor, pelargonin class.The chemical ingredients of White Mulberry Root-bark morus alba L. was once studied by Japan, extracted, separates, identified Ku Wanuo H(Kuwanon H wherein) (HeterocyclesVOL14NO121980P
1943), Mo Luxin (morusin), (ChemPharmBull24(11) 1976P
2898-2900).But with Cortex Mori extract Ku Wanuo H(Kuwanon H), Mo Luxin (morusin), Morusin-4'-O-glucose (morusin-4 '-O-glucose) inhibition of virus HIV of AIDS, the infection that prevention or treatment are caused by HIV, treatment AIDS then is not reported.
The present invention is intended to the extract Ku Wanuo H(Kuwanon H with White Mulberry Root-bark), Mo Luxin (morusin) and derivative Morusin-4'-O-glucose (morusin-4-O-glucose) thereof are used to suppress the viral HIV of people's AIDS (AIDS), with the infection that prevention or treatment are caused by HIV, the treatment AIDS.
Compound library of the present invention watt promise H(Kuwanon H) extract from the Chinese medicinal plant White Mulberry Root-bark, its molecular formula is C
45H
44O
11, molecular weight is 760, structural formula is
This compound is yellow amorphous powder, and fusing point is 187-189 ℃.Dissolve in methyl alcohol, chloroform, ethyl acetate, water insoluble.
Compound, morus ignin of the present invention (morusin) extracts from the Chinese medicinal plant White Mulberry Root-bark, and its molecular formula is C
25H
24O
6, molecular weight is 420, structural formula is
This compound is a yellow crystals, and fusing point is 166-168 ℃.Be soluble in chloroform, methyl alcohol, ethyl acetate, water insoluble.
Compound, morus ignin glycoside of the present invention (morusin-4 '-O-glucose) be the derivative of Chinese medicinal plant Cortex Mori extract Mo Luxin (morusin), its molecular formula is C
31H
34O
11, molecular weight is 582, structural formula is
This compound is a yellow powder, and fusing point is 125-131 ℃.Water soluble, methyl alcohol are insoluble to chloroform.
Compound of the present invention is provided by following embodiment and laboratory report thereof the restraining effect of HIV (human immunodeficiency virus) HIV.
With compound library watt promise H(Kuwanon H) with dimethyl sulfoxide (DMSO) (DMSO) dissolving, be made into the solution A that concentration is 2mg/ml.A liquid water is diluted to many groups diluent that concentration is 1 μ g/ml-1mg/ml respectively, on Fig. 1, makes abscissa with the log value of its concentration.The diluent of getting 9 groups of different concns carries out toxicity test.Get human lymphoid T4 cell and be divided into 9 groups, the diluent that adds above-mentioned 9 groups of different concns was respectively cultivated 7 days, observe the surviving rate of these 9 groups of cells, on Fig. 1, make ordinate with 0-100%, obtain 9 experimental points, each point is linked to be curve, can sees the toxicity (among Fig. 1 shown in the thick line) of this compound pair cell by this curve.When cell survival rate was 50%, the compound concentration of this point was called IC50.
Get human lymphoid T4 cell, be divided into 9 groups after the viral HIV of personnel selection AIDS (AIDS) infects, carry out of the inhibition experiment of this compound HIV.The diluent that adds above-mentioned 9 groups of different concns was respectively cultivated the surviving rate of observing these 9 groups of cells 7 days.On Fig. 1, make ordinate with 0-100%, obtain 9 test points.Each point is linked to be curve, can sees surviving rate under the experimental compound effect of different concns of the cell that infected by HIV (among Fig. 1 shown in the fine rule) by this curve.When surviving rate was 50%, the compound concentration of this point was called EC50.The surviving rate of human lymphoid T4 cell under the compound effects of this concentration that promptly infected by HIV of meaning is that the surviving rate of the HIV cells infected of the 50%(control group that do not add compound is 0%).
Data shown in the table 1 are the raw data of above-mentioned two groups of experiments, make graphic representation 1 with these data.Abscissa is the log value of experimental compound concentration μ g/ml among Fig. 1, and value 0 is 1 μ g/ml, and value 1 is 10 μ g/ml, and value 2 is 100 μ g/ml, and value 3 is 1000 μ g/ml.Ordinate is the surviving rate of human lymphoid T4 cell.Value 0 expression cell is all dead, and value 50 expression cell survival rates are 50%, and value 100 expression cell survival rates are 100%.Can find out the toxicity of this compound pair cell by thick line, by fine rule as can be seen this compound to the restraining effect of HIV (human immunodeficiency virus) HIV.IC/EC=TI represents the therapeutic index of this compound.
As seen from Figure 1, concentration compound library of the present invention watt promise H(Kuwanon H) just can suppress 50% virus HIV of AIDS about 1-2 μ g/ml.
Compound, morus ignin (morusin) is dissolved with dimethyl sulfoxide (DMSO) (DMSO), be made into the solution A that concentration is 2mg/ml, the A solution with water is diluted to many groups diluent that concentration is 1 μ g/ml-1mg/ml respectively, log value with its concentration is made abscissa on Fig. 2, the diluent of getting 9 groups of different concns carries out toxicity test.Get human lymphoid T4 cell and be divided into 9 groups, the diluent that adds above-mentioned 9 groups of different concns was respectively cultivated 7 days, observe the surviving rate of these 9 groups of cells, on Fig. 2, make ordinate with 0-100%, obtain 9 experimental points, each point is linked to be curve, can sees the toxicity (among Fig. 2 shown in the thick line) of this compound pair cell by this curve.When cell survival rate was 50%, the compound concentration of this point was called IC50.
Get human lymphoid T4 cell, after the viral HIV of personnel selection AIDS (AIDS) infects, be divided into 9 groups, carry out of the inhibition experiment of this compound HIV.The diluent that adds above-mentioned 9 groups of different concns was respectively cultivated 7 days, and the surviving rate of observing these 9 groups of cells is made ordinate with 0-100% on Fig. 2, obtain 9 experimental points, and each point is linked to be curve.Can be seen surviving rate under the compound effects of different concns of the cell that infected by HIV (among Fig. 2 shown in the fine rule) by this curve, when surviving rate was 50%, the compound concentration of this point was called EC50.The surviving rate of human lymphoid T4 cell under the compound effects of this concentration that promptly infected by HIV of meaning is that the surviving rate of the HIV cells infected of the 50%(control group that do not add compound is 0%).
Data shown in the table 2 are the raw data of above-mentioned two groups of experiments, make graphic representation 2 with these data.Abscissa is the log value of experimental compound concentration μ g/ml among Fig. 2.Value 0 is 1 μ g/ml, and value 1 is 10 μ g/ml, and value 2 is 100 μ g/ml, and value 3 is 1000 μ g/ml.Ordinate is the surviving rate of human lymphoid T4 cell.Value 0 expression cell is all dead, and value 50 expression cell survival rates are 50%, and value 100 expression cell survival rates are 100%.Can find out the toxicity of this compound pair cell by thick line, by fine rule as can be seen this compound to the restraining effect of HIV (human immunodeficiency virus) HIV.IC/EC=TI represents the therapeutic index of this compound.
As seen from Figure 2, the concentration of compound, morus ignin of the present invention (morusin) just can suppress 50% HIV (human immunodeficiency virus) HIV about 9 μ g/ml.
With the compound, morus ignin glycoside (morusin-4 '-O-glucose) with dimethyl sulfoxide (DMSO) (DMSO) dissolving, be made into the solution A that concentration is 2mg/ml, A liquid water is diluted to many groups diluent that concentration is 1 μ g/ml-1mg/ml respectively, on Fig. 3, makes abscissa with the log value of its concentration.The diluent of getting 9 groups of different concns carries out toxicity test.Get human lymphoid T4 cell and be divided into 9 groups, the diluent that adds above-mentioned 9 groups of different concns was respectively cultivated 7 days, and the surviving rate of observing these 9 groups of cells is made ordinate with 0-100% on Fig. 3, obtain 9 experimental points, and each point is linked to be curve.By this curve toxicity of this compound pair cell (among Fig. 3 shown in the thick line) as can be seen.When cell survival rate was 50%, the compound concentration of this point was called IC50.
Get human lymphoid T4 cell, after the viral HIV of personnel selection AIDS (AIDS) infects, be divided into 9 groups, carry out of the inhibition experiment of this compound HIV.The diluent that adds above-mentioned 9 groups of different concns was respectively cultivated the surviving rate of observing these 9 groups of cells 7 days.On Fig. 3, make ordinate with 0-100%, obtain 9 experimental points, each point is linked to be curve.Can see the surviving rate of infected cells under the compound effects of different concns (among Fig. 3 shown in the fine rule) by this curve.When surviving rate was 50%, the compound concentration of this point was called EC50, and the surviving rate of human lymphoid T4 cell under the compound effects of this concentration that promptly infected by HIV of meaning is that the surviving rate of the HIV cells infected of the 50%(control group that do not add compound is 0%).
Data shown in the table 3 are the raw data of above-mentioned two groups of experiments, make graphic representation 3 with these data.Abscissa is the log value of compound concentration μ g/ml among Fig. 3.Value 0 is 1 μ g/ml, and value 1 is 10 μ g/ml, and value 2 is 100 μ g/ml, and value 3 is 1000 μ g/ml.Ordinate is the surviving rate of human lymphoid T4 cell.Value 0 expression cell is all dead, and value 50 expression cell survival rates are 50%, and value 100 expression cell survival rates are 100%.By the thick line toxicity of this compound pair cell as can be seen, by fine rule as can be seen this compound to the restraining effect of HIV (human immunodeficiency virus) HIV.IC/EC=TI represents the therapeutic index of this compound.
As seen from Figure 3, compound, morus ignin glycoside of the present invention (morusin-4 '-O-glucose) concentration just can suppress 50% HIV (human immunodeficiency virus) HIV about 5g/ml.
Claims (4)
1, the compound of the viral HIV of a kind of inhibition people's AIDS (AIDS), the activity that is used for inhibition of virus HIV of AIDS, it is characterized in that the compound and the derivates library watt promise H (Kuwanon H) thereof that from Chinese medicinal plant White Mulberry Root-bark morus alba L., extract, Mo Luxin (morusin), Morusin-4'-O-glucose (morusin-4 '-O-glucose).
2, compound according to claim 1 is characterized in that Ku Wanuo H(KuwanonH) molecular formula be C
45H
44O
11, molecular weight is 760, structural formula is
Be yellow amorphous powder, fusing point is 187-189 ℃, dissolves in methyl alcohol, chloroform, ethyl acetate, and is water insoluble.
3, compound according to claim 1, the molecular formula that it is characterized in that Mo Luxin (morusin) is C
25H
24O
6, molecular weight is 420, structural formula is
Be yellow crystals, fusing point is 166-168 ℃, is soluble in chloroform, methyl alcohol, ethyl acetate, and is water insoluble.
4, compound according to claim 1, it is characterized in that Morusin-4'-O-glucose (morusin-4 '-O-glucose) molecular formula is C
31H
34O
11, molecular weight is 582, structural formula is
Be yellow powder, fusing point is 125-131 ℃, dissolves in methyl alcohol, water, is insoluble to chloroform.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 94101625 CN1058609C (en) | 1994-02-15 | 1994-02-15 | Compound for inhibition of virus HIV of AIDS |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 94101625 CN1058609C (en) | 1994-02-15 | 1994-02-15 | Compound for inhibition of virus HIV of AIDS |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1107152A true CN1107152A (en) | 1995-08-23 |
| CN1058609C CN1058609C (en) | 2000-11-22 |
Family
ID=5030273
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 94101625 Expired - Fee Related CN1058609C (en) | 1994-02-15 | 1994-02-15 | Compound for inhibition of virus HIV of AIDS |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1058609C (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101787030A (en) * | 2010-03-09 | 2010-07-28 | 周英 | Preparation and application methods of anti-HIV compound, morus ignin L |
| CN105566340A (en) * | 2016-01-20 | 2016-05-11 | 贵州大学 | White mulberry root-bark active ingredient Morusin derivative and application and preparation method thereof |
-
1994
- 1994-02-15 CN CN 94101625 patent/CN1058609C/en not_active Expired - Fee Related
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101787030A (en) * | 2010-03-09 | 2010-07-28 | 周英 | Preparation and application methods of anti-HIV compound, morus ignin L |
| CN105566340A (en) * | 2016-01-20 | 2016-05-11 | 贵州大学 | White mulberry root-bark active ingredient Morusin derivative and application and preparation method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1058609C (en) | 2000-11-22 |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C56 | Change in the name or address of the patentee |
Owner name: WANG LIHONG Free format text: FORMER NAME OR ADDRESS: LUO SHIDE; NING BINGMEI |
|
| CP03 | Change of name, title or address |
Address after: Baiyun road 650024 Yunnan city of Kunming province (No. 525 Beijing Road, Huayuan 6-3-202) Patentee after: Wang Lihong Address before: 650031 Yunnan city of Kunming province Tianjun Dian Xiang Lin Street five building 1 unit 303 Co-patentee before: Ning Bingmei Patentee before: Luo Shide |
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Granted publication date: 20001122 Termination date: 20120215 |