CN1052983C - Melim sulfate compound - Google Patents
Melim sulfate compound Download PDFInfo
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- CN1052983C CN1052983C CN98116970A CN98116970A CN1052983C CN 1052983 C CN1052983 C CN 1052983C CN 98116970 A CN98116970 A CN 98116970A CN 98116970 A CN98116970 A CN 98116970A CN 1052983 C CN1052983 C CN 1052983C
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- melim
- sulfate compound
- compound
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- aids
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Abstract
The present invention relates to a medicinal compound for resisting AIDS, particularly to a rutin sulfate compound. The rutin sulfate compound is obtained by that the water extract of the plant of a locust tree is treated by pyridine chlorosulfonic acid. The rutin sulfate has strong AIDS virus resistance.
Description
The present invention relates to the compound field, particularly, relate to the medical compounds of anti-AIDS.
As everyone knows, acquired immune deficiency syndrome (AIDS) is a kind of to the very serious transmissible disease of human health threat, also is the difficult medical problem of the world today.At present, screening anti AIDS virus and immunity function restructuring medicine from plant amedica, also is an important channel of development anti-AIDS drug.Also do not have so far from the water extract of plant Chinese scholartree, the sulfate compound of handling gained through pyridine-chlorsulfonic acid has the report of stronger anti-AIDS toxic action.
The object of the present invention is to provide a kind of Melim sulfate compound.
Structural formula of compound of the present invention is as follows:
Melim sulfate compound of the present invention can obtain through pyridine-chlorsulfonic acid processing from the water extract of plant Chinese scholartree.This compound has stronger anti-AIDS toxic action.
Pharmacological action with Melim sulfate compound of the present invention (replace number for M-36) illustrates beneficial effect of the present invention below:
Melim sulfate compound is soluble in water, and anti-HIV and anti-other virus experiments are carried out at U.S. NCI and Bayer A.G respectively, and with cell culture method or in vitro tests method (In-Vitro Anti-HIV testing), anti-HIV test repeats repeatedly favorable reproducibility.The activity of anti-HIV all reaches " level of signification " (Active), and each test all compares with anti-HIV active drug AZT, and antiviral activity intensity is with therapeutic index (TI)=IC
50/ EC
50Big or small last classification, TI is effective greater than 100.Test-results sees Table 1.
Table 1 Melim sulfate compound (using code name M-36 in the table)
The therapeutic index medicine numbering EC of anti AIDS virus
50(mg/ml) IC
50(mg/ml) therapeutic index TI=IC
50/ EC
50M-36 7.64 * 10
02.50 * 10
3327M-36 4.85 * 10
02.50 * 10
3514M-36 1.85 * 10
01.31 * 10
3162M-36 7.85 * 10
01.31 * 10
3167 contrast AZT 583
Can obtain conclusion from table, the therapeutic index of the anti AIDS virus of Melim sulfate compound of the present invention is 327.
Cell culture method that U.S. NCI is used or in vitro tests method (In-Vitro testing) are anti AIDS virus (Human Immunodeficiency Virus) drug screening methods general on present state-border.These method concrete steps are: place responsive susceptible host cell in culture dish, wherein half is infected with virus (HIV), and second half is a control group, adds that the medicine of different concns is sieved sample, places seven days in thermostatic chamber.It is most of or all damaged by virus not add the cell of medicine.Measure in above-mentioned two portions culture dish with fluorescent beam split photometry after seven days and remain in cell count.With the cell survival percentage is ordinate zou, is X-coordinate with experiment drug concentrations mcg/ml, and the result of each test is found out corresponding point on coordinate, connects these points and obtains two curves (solid black lines, another is represented by dotted lines).Dotted line represents to add without the host cell that HIV infects the result of medicine, and solid line represents to be subjected to the performance of cell under the experiment drug effect of HIV infection to scheme.Middle two horizontal lines are respectively 0% and 50% reference line.Because medicine has the inhibiting while restraining effect also to be arranged to normal cell to virus.Above the concentration of intersection point of dotted line and 50% reference line be called IC
50, the expression medicine makes normal cell growth produce 50% drug level when suppressing, below solid line and 50% reference line intersection point be called EC
50, the expression medicine makes the cell disease of virus reduce by 50% drug level.IC
50With EC
50Ratio get therapeutic index TI=IC
50/ EC
50The therapeutic index of AZT is 583.Exactness for the antivirus action that helps to be subjected to the reagent thing has the AZT experimental result of HIV (human immunodeficiency virus)-resistant activity to do reference with known.
The toxicity test result of Melim sulfate compound: when being 500mg/kg for mouse mainline (IV) or oral (P.O) dosage, the overt toxicity reaction do not occur, the LD of this compound is described
50＞500mg/kg.
Further specify flesh and blood of the present invention below in conjunction with accompanying drawing with embodiment, but content of the present invention is not limited thereto.
Fig. 1 is the anti-HIV pharmacological evaluation graphic representation of Melim sulfate compound;
Fig. 2 is the anti-HIV pharmacological evaluation graphic representation of contrast AZT.
Embodiment one:
Get bud 100 grams of Chinese scholartree plant flowers, with methyl alcohol extracting 2 times, each 2000 milliliters, be condensed into 500 milliliters under the methanol extract liquid decompression, filter the rear filtrate extracted with diethyl ether, discard ether layer, the water liquid layer is decompressed to 200 milliliters, cooling, solid crystal filters and to be divided into mother liquor and crystallization, crystallization wash with water the back with ether wash rutin, recrystallization from methyl alcohol gets pure rutin 10 grams.
The structural formula of Melim sulfate compound of the present invention is:
Claims (1)
1, the Melim sulfate compound shown in (I) formula:
In the formula:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN98116970A CN1052983C (en) | 1998-07-28 | 1998-07-28 | Melim sulfate compound |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN98116970A CN1052983C (en) | 1998-07-28 | 1998-07-28 | Melim sulfate compound |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1209434A CN1209434A (en) | 1999-03-03 |
| CN1052983C true CN1052983C (en) | 2000-05-31 |
Family
ID=5225289
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN98116970A Expired - Fee Related CN1052983C (en) | 1998-07-28 | 1998-07-28 | Melim sulfate compound |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1052983C (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2006233256B2 (en) * | 2006-10-30 | 2012-01-19 | Armaron Bio Pty Ltd | Improved flavonols |
| CN102250171B (en) * | 2010-05-21 | 2014-06-11 | 广东东阳光药业有限公司 | Rutin ester compound and application thereof in medicaments |
| CN103145781B (en) * | 2013-01-14 | 2016-03-16 | 李玉山 | A kind of synthesis technique of anti-AIDS compound rutin sodium sulfonate |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1030764A (en) * | 1987-05-25 | 1989-02-01 | 北京工业大学 | Process for producing rutin |
| CN1160048A (en) * | 1996-10-16 | 1997-09-24 | 翟广玉 | Process for production of rutin by continuous extraction |
-
1998
- 1998-07-28 CN CN98116970A patent/CN1052983C/en not_active Expired - Fee Related
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1030764A (en) * | 1987-05-25 | 1989-02-01 | 北京工业大学 | Process for producing rutin |
| CN1160048A (en) * | 1996-10-16 | 1997-09-24 | 翟广玉 | Process for production of rutin by continuous extraction |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1209434A (en) | 1999-03-03 |
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Legal Events
| Date | Code | Title | Description |
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| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C06 | Publication | ||
| PB01 | Publication | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| ASS | Succession or assignment of patent right |
Owner name: CONBA GROUP CO.,LTD. Free format text: FORMER OWNER: KUNMING INST. OF BOTANY, CHINESE ACADEMY OF SCIENCES Effective date: 20010911 |
|
| C41 | Transfer of patent application or patent right or utility model | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20010911 Address after: Twelve building, No. 60, Sima cross lane, Hangzhou, Zhejiang, 310003 Patentee after: Conba Group Co. Ltd. Address before: 650204 Black dragon Pool, Yunnan, Kunming Patentee before: Kunming Institute of Botany, Chinese Academy of Sciences |
|
| EE01 | Entry into force of recordation of patent licensing contract |
Assignee: Zhejiang Modern Chinese Medicine and Natural Medicine Academy Co., Ltd. Assignor: Conba Group Co. Ltd. Contract fulfillment period: 2008.8.20 to 2014.8.20 contract change Contract record no.: 2008330000663 Denomination of invention: Melim sulfate compound Granted publication date: 20000531 License type: Exclusive license Record date: 2008.9.26 |
|
| LIC | Patent licence contract for exploitation submitted for record |
Free format text: EXCLUSIVE LICENCE; TIME LIMIT OF IMPLEMENTING CONTACT: 2008.8.20 TO 2014.8.20 Name of requester: ZHEJIANG MODERN CHINESE MEDICINE AND NATURAL MEDI Effective date: 20080926 |
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| C17 | Cessation of patent right | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20000531 Termination date: 20120728 |