CN1475210A - New use of agmatine - Google Patents
New use of agmatine Download PDFInfo
- Publication number
- CN1475210A CN1475210A CNA021254958A CN02125495A CN1475210A CN 1475210 A CN1475210 A CN 1475210A CN A021254958 A CNA021254958 A CN A021254958A CN 02125495 A CN02125495 A CN 02125495A CN 1475210 A CN1475210 A CN 1475210A
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- China
- Prior art keywords
- agmatine
- tumor
- mice
- present
- cyclophosphamide
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Abstract
A novel application of guanidinobutylamine in preparing the medicines for preventing and treating tumor is disclosed.
Description
Invention field
The present invention relates to the new medical usage of agmatine.More specifically say, the present invention relates to agmatine and be used for prevention or medicine for treating tumor thing purposes in preparation.
Background technology
Agmatine is a known compound, and its chemical name is 4-guanidine radicals-butylamine and has following structure
Known agmatine has analgesic activity, has not yet to see the report of its antitumor action.
Goal of the invention
The objective of the invention is to seek and develop the new purposes of agmatine.
The invention summary
The inventor finds unexpectedly now after deliberation that agmatine has and well prevents and/or treats function of tumor.
Therefore, first aspect present invention relates to agmatine is used for preventing and/or treating tumor in preparation medicine purposes.
Further aspect of the present invention relates to the pharmaceutical composition that is used to prevent and/or treat tumor, and it comprises agmatine and pharmaceutical carrier or the excipient that prevents and/or treats the tumor effective dose.
Further aspect of the present invention relates to the method for prevention or treatment tumor disease or symptom, and it comprises to tumor or has the patient of potential tumor danger to prevent and/or treat the agmatine of effective dose.
Detailed Description Of The Invention
According to the present invention, term in this description " patient " is meant the mankind.
According to the present invention, used term " tumor " comprises optimum and malignant tumor among the present invention, as cancer.
According to the present invention, agmatine can separately or use with pharmaceutical compositions also can be by oral, and non-intestinal or local approach give.Say that for example the peroral dosage form of pharmaceutical composition of the present invention can be tablet, capsule, solution or suspension etc.; Its parenterai administration dosage form is subcutaneous, the injection of muscle, intraperitoneal administration or instillation etc.; But its topical dosage form patch, ointment etc.
According to the present invention, the dosage of agmatine depends on multiple factor such as sex, age, body weight, disease severity or route of administration and can be judged by the clinician.
Further, agmatine can or be buied by the means known in the art preparation from the market as a kind of known compound.
Below experimental example be to further describe but do not mean that to this any restriction to of the present invention.
The present invention adopts and irritates two kinds of route of administration of harmonization of the stomach subcutaneous injection on big two kinds of animals of mice, and (agmatine AGMT) has antidepressant effect to observe the confirmation agmatine in outstanding tail and two depression models of forced swimming.
This tests used AGMT available from U.S. Sigma company.
Experimental example 1AGMT is to the antitumor action of mice
The influence that after observing continuous subcutaneous injection various dose agmatine on the Kunming mouse body solid tumor models tumor is weighed is to estimate its anti-tumor activity.Get male mouse of kunming, body weight 18-22g.At first weigh,, inoculate back 24 hours beginning subcutaneous injection various dose agmatines (10 and 40mg/kg) thereafter at the right front armpit subcutaneous vaccination of mice S180 tumor cell to mice, one day three times, successive administration 10 days; With the positive contrast medicine of cyclophosphamide (15mg/kg).Weighed to mice once more in the 11st day, relatively body weight change before and after the separate groups of mice administration.Then mice is drawn neck to put to death, separated the Subcutaneous tumor tissue and weigh calculating tumour inhibiting rate [(control group mice tumor weight-medication group mouse tumor is heavy)/control group mice tumor heavy * 100%], the relatively difference of separate groups of mice tumor weight and tumour inhibiting rate.
The result shows, compares with matched group, and cyclophosphamide 15mg/kg (subcutaneous injection) can significantly suppress kunming mice body tumor growth (tumour inhibiting rate is 45.8%, P＜0.01); Also significantly suppressed the growth (tumour inhibiting rate is 48.6%, P＜0.01) of tumor tissues after 10 days with the processing of 40mg/kg agmatine.Compare with the saline group, agmatine and cyclophosphamide cause that all weight of mice obviously delays, and this may be relevant with cancerous tissue poor growth after its treatment.The results are shown in Table 1.The heavy tumour inhibiting rate mice of the influence grouping dosage number of animals mouse tumor body weight change that table 1. subcutaneous injection agmatine (3 times/day) was grown in the kunming mice body to the S180 tumor in continuous 10 days
(mg/kg) (gram) (%) (gram) saline--9 1.79 ± 0.88-8.69 ± 1.64 cyclophosphamide 15 10 0.97 ± 0.57
*45.8 6.38 ± 1.61
*Agmatine 10 7 1.74 ± 0.51 2.8 5.38 ± 1.14
*
40 9 0.92 ± 0.52
*48.6 5.30 ± 1.88
*X ± s,
*P＜0.01
*Compare with the saline control group P＜0.01.
Experimental example 2 agmatines are in the solid tumor models influence heavy to tumor
With mice influence heavy behind body solid tumor models observation continuous subcutaneous injection various dose agmatine, to estimate its anti-tumor activity to tumor.Get male Balb/C mouse, body weight 18-22g.At first weigh,, inoculate back 1 day beginning subcutaneous injection various dose agmatine at the right front armpit subcutaneous vaccination of mice S180 tumor cell to mice, one day three times, successive administration 10 days; With the positive contrast medicine of cyclophosphamide (15mg/kg).Administration was weighed to mice on the 11st day once more, relatively body weight change before and after the separate groups of mice administration.Then mice is drawn neck to put to death, separated the Subcutaneous tumor tissue and weigh calculating tumour inhibiting rate [(control group mice tumor weight-medication group mouse tumor is heavy)/control group mice tumor heavy * 100%], the relatively difference of separate groups of mice tumor weight and tumour inhibiting rate.
The result shows, compares with matched group, and cyclophosphamide 15mg/kg (subcutaneous injection) can significantly suppress the Balb/c mice body tumor growth (tumour inhibiting rate is 48.9%, P＜0.01); 5,10,20,40 and the effect of 80mg/kg agmatine also can significantly suppress the growth (P＜0.05 or P＜0.01) of tumor tissues after 10 days; Wherein 20 and the effect of 40mg/kg agmatine even the trend (tumour inhibiting rate is respectively 51.0% and 53.1%, and P＜0.01 and saline group are relatively) that has surpassed cyclophosphamide is arranged.Compare with matched group, cyclophosphamide treatment group mice body weight obviously alleviates (P＜0.01), and agmatine treatment group slightly alleviates (P＜0.05) except that 5mg/kg group mice body weight, all the other respectively organize the mice body weight all less than significantly changing, and this point has embodied less toxicity and the better therapeutic effect of agmatine.The results are shown in Table 2.The heavy tumour inhibiting rate body weight change of influence grouping dosage number of animals mouse tumor that table 2. subcutaneous injection agmatine (3 times/day) was grown in Balb/c mice body to the S180 tumor in continuous 10 days
(mg/kg) (gram) (%) (gram) saline--11 0.98 ± 0.25 0.91 ± 1.73 cyclophosphamide 15 11 0.50 ± 0.23
*48.9-3.41 ± 1.59
*Agmatine 5 11 0.75 ± 0.31
*23.5-0.37 ± 0.60
*
10 11 0.61±0.15
* 37.8 0.28±0.63
20 10 0.48±0.24
** 51.0 0.51±0.95
40 10 0.46±0.29
** 53.1 0.18±0.86
80 9 0.54 ± 0.19
*44.8 0.45 ± 0.82x ± s,
*P＜0.05,
*Compare with the saline control group P＜0.01.
Above-mentioned two example experiments confirm that all agmatine can suppress the S180 tumor in the intravital growth course of mice in dose dependent ground.
Claims (2)
1. the following formula agmatine is used for preventing and/or treating the medicine purposes of tumor disease or symptom in preparation.
2. be used to prevent and/or treat the pharmaceutical composition of tumor disease or symptom, it comprises agmatine and pharmaceutical carrier or the excipient that prevents and/or treats effective dose.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA021254958A CN1475210A (en) | 2002-08-13 | 2002-08-13 | New use of agmatine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA021254958A CN1475210A (en) | 2002-08-13 | 2002-08-13 | New use of agmatine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1475210A true CN1475210A (en) | 2004-02-18 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA021254958A Pending CN1475210A (en) | 2002-08-13 | 2002-08-13 | New use of agmatine |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1475210A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008107471A3 (en) * | 2007-03-07 | 2009-01-08 | Dextech Medical Ab | Modified hydroxypolymer conjugates with killing effect on tumor cells |
| CN103340844A (en) * | 2013-06-20 | 2013-10-09 | 杨家友 | Application of gamatine in preparing drug resisting high PTH |
-
2002
- 2002-08-13 CN CNA021254958A patent/CN1475210A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008107471A3 (en) * | 2007-03-07 | 2009-01-08 | Dextech Medical Ab | Modified hydroxypolymer conjugates with killing effect on tumor cells |
| CN103340844A (en) * | 2013-06-20 | 2013-10-09 | 杨家友 | Application of gamatine in preparing drug resisting high PTH |
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| PB01 | Publication | ||
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| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |