CN1377644A - Anti-leukemia medicine - Google Patents
Anti-leukemia medicine Download PDFInfo
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- CN1377644A CN1377644A CN 01106982 CN01106982A CN1377644A CN 1377644 A CN1377644 A CN 1377644A CN 01106982 CN01106982 CN 01106982 CN 01106982 A CN01106982 A CN 01106982A CN 1377644 A CN1377644 A CN 1377644A
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- leukemia
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Abstract
The present invention provides an anti-leukemia medicine prepared with gallo catechin and gallate as main raw material and through conventional process. It is preparation of a concentration range of 50-500 microgram/ml. The present invention is a kind of clinical medicine for treating acute promyelocyte leukemia, chronic granulocyte leukemia and promyelocyte leukemia with vitamin A acid resistance. As a kind of leukemia gene regulator, the medicine can inhibit the growth of acute leukemia promyecloyte HL-60 and induce its dealth without accumulation and no any toxic side effect. It has high efficiency and low toxicity.
Description
The present invention relates to a kind of anti-leukemia medicine, particularly adopt epigallocatechin gallate (EGCG) (EGCG) to be the anti-leukemia medicine of primary raw material.
Leukemic morbidity is except that inherited genetic factors, and is also closely related with environmental factors.The annual newly-increased leukemia people 4-5 ten thousand of China, the leukemia relapse patient is more than 150,000.Aspect the acute promyelocytic leukemic treatment, many employing all-trans-retinoic acids (ATRA) can make the Most patients state of an illness alleviate as differentiating inducer at present.But retinoic acid drug resistance and retinoic acid syndrome can cause the recurrence of patient's short-term, re-use the ATRA treatment and then do not reach therapeutic effect because of drug resistance produces.Bone marrow transplantation is one of treatment chronic myelocytic leukemia perfect method, but donor difficulty, allogene or autotransplantation all need could implant new ancestral cells after the clone of malignant proliferation is killed in pretreatment in addition, and its curative effect of the interferon therapy of more application is also not satisfied clinically.Since 1992, Chinese scholar is with arsenic trioxide (As
2O
3) be used for the treatment of acute and chronicly, the drug resistance leukemia is clinical, has obtained better curative effect, causes very big repercussion in the world.Further basic research shows As
2O
3Antileukemie mechanism is, significantly the apoptosis of inducing leukemia cell.Yet As
2O
3Be heavy metal compound, extremely strong cellulotoxic effect is arranged, easily accumulate in vivo and be difficult for metabolism, there is intensive toxic reaction in the patient who receives treatment.
The purpose of this invention is to provide a kind of antileukemie effect, mechanism unanimity, but nothing is accumulated, the anti-leukemia medicine of non-toxic reaction.
The present invention is a raw material with catechin monomers-epigallocatechin gallate (EGCG) in the Folium Camelliae sinensis (EGCG), and preparation process is prepared into the preparation that concentration range is 50-500 μ g/ml routinely, can be oral medicine, also can be injection.More preferably scope is 250-500 μ g/ml.
EGCG is the topmost monomer of catechin in the tea, has extremely strong hydrogen supply capacity, and its molecular structural formula is as follows:
The present invention is the clinical medicine dosage form, particularly injection that is suitable for treating the leukemia people, in order to treatment acute promyelocytic leukemic, chronic myelocytic leukemia, retinoic acid drug resistance promyelocytic leukemia.The present invention can be oral medicine, also can be injection.
The present invention is a kind of leukemia gene adjusting control agent, growth with remarkable inhibition acute promyelocytic leukemia cell HL-60, and can induce its effect of apoptosis, and there is not savings, without any side effects, having anti-acute, chronic, chemical sproof characteristics efficient, low toxicity, is a kind of ideal medicament for treatment of leukemia.
Embodiment:
1.EGCG experiment to leukaemia's growth effect:
With people's acute promyelocytic leukemic NK4 cell, people's acute promyelocytic leukemic HL-60 cell, chronic myelocytic leukemia K562 cell, retinoic acid drug resistance early children's grain leukemia MR-2 cell is inoculated in respectively in the RPMI-1640 culture fluid, contains 5%CO in 37 ℃
2Incubator in cultivate and to go down to posterity, be inoculated in 96 well culture plates, add variable concentrations EGCG during inoculation, parallel 4 holes of every concentration, the MTT reduction reaction is measured inhibition rate of tumor growth after 48 hours, the results are shown in Table 1.
The influence that table 1 variable concentrations EGCG grows to the leukaemia (x ± s)
| EGCG concentration μ g/ml | People's acute promyelocytic leukemic NK4 cell inhibitory rate (%) | People's acute promyelocytic leukemic HL-60 cell inhibitory rate (%) | Chronic myelocytic leukemia K562 cell inhibitory rate (%) | The retinoic acid drug resistance is children's grain leukemia MR-2 cell inhibitory rate (%) early |
| ????100 ????200 ????300 ????400 ????500 | ????34.12±5.21 ????45.67±8.99 ????51.78±9.72 ????68.25±15.22 ????78.53±13.24 | ????41.51±1.12 ????69.12±2.15 ????73.34±1.89 ????75.9?5±2.32 ????82.60±4.22 | ????39.65±11.57 ????43.54±12.35 ????55.67±11.22 ????61.62±15.13 ????78.22±13.74 | ????36.21±14.22 ????43.66±15.25 ????45.25±9.67 ????53.66±11.28 ????65.92±14.35 |
The result sees from table 1, and EGCG has stronger inhibitory action to various leukaemias' growth, and is tangible dose-effect relationship, and promptly with the raising of EGCG concentration, the inhibitory action that the leukaemia is grown also progressively strengthens.
Apoptosis is a focus of current oncology studies, is especially extensively used when the screening anti-tumor drug.Apoptosis has unique biochemistry and morphological feature, and by to being observed by the dead form of the various leukaemias after the EGCG effect, the result is as follows:
The peculiar morphological feature of apoptosis all occurred by the various leukaemias in EGCG effect back between 250-500 μ g/ml concentration: nuclear fold, chromatic agglutination forms the apoptotic body that is held by film after being cracked into fragment.
By the various leukaemias in EGCG effect back between 250-500 μ g/ml concentration, dna degradation is in the gel electrophoresis observation of sign between with nucleosome, and all visible typical DNA band confirms the cancer cell specific induction of apoptosis effect of EGCG.
Flow cytometry is the method for a kind of advanced person, accurate detection by quantitative apoptotic cell.Laboratory observation shows, EGCG is in 250-500 μ g/ml concentration range, induce people's acute promyelocytic leukemic NK4 cell, people's acute promyelocytic leukemic HL-60 cell, chronic myelocytic leukemia K562 cell, retinoic acid drug resistance early children's grain leukemia MR-2 apoptosis rate reach 71.85%, 75.63%, 81.22%, 69.12% respectively.The result shows that also it is early stage that EGCG mainly occurs in cell differentiation to cancerous cell differentiation blocking effect.
Claims (2)
1. anti-leukemia medicine, it is characterized in that: the present invention is a raw material with catechin monomers-epigallocatechin gallate (EGCG) in the Folium Camelliae sinensis (EGCG), and preparation process is prepared into the preparation that concentration range is 50-500 μ g/ml routinely, can be oral medicine, also can be injection.
2. medicine according to claim 1 is characterized in that: preferred concentration range is 250-500 μ g/ml.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 01106982 CN1377644A (en) | 2001-04-02 | 2001-04-02 | Anti-leukemia medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 01106982 CN1377644A (en) | 2001-04-02 | 2001-04-02 | Anti-leukemia medicine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1377644A true CN1377644A (en) | 2002-11-06 |
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ID=4655937
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 01106982 Pending CN1377644A (en) | 2001-04-02 | 2001-04-02 | Anti-leukemia medicine |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1377644A (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101507730B (en) * | 2009-03-26 | 2011-01-26 | 复旦大学 | Combination of epigallocatechin-3-gallate and cerubidin and use thereof |
| CN102232959A (en) * | 2010-04-23 | 2011-11-09 | 复旦大学 | Method for reducing daunorubicin cardiac toxicity |
| CN102600128A (en) * | 2012-02-16 | 2012-07-25 | 赵汉玺 | Epigallocatechin gallate medicament and application thereof |
| CN102908342A (en) * | 2012-11-20 | 2013-02-06 | 上海海洋大学 | Medicine for preventing hemorrhagic disease of grass carps |
-
2001
- 2001-04-02 CN CN 01106982 patent/CN1377644A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101507730B (en) * | 2009-03-26 | 2011-01-26 | 复旦大学 | Combination of epigallocatechin-3-gallate and cerubidin and use thereof |
| CN102232959A (en) * | 2010-04-23 | 2011-11-09 | 复旦大学 | Method for reducing daunorubicin cardiac toxicity |
| CN102600128A (en) * | 2012-02-16 | 2012-07-25 | 赵汉玺 | Epigallocatechin gallate medicament and application thereof |
| CN102908342A (en) * | 2012-11-20 | 2013-02-06 | 上海海洋大学 | Medicine for preventing hemorrhagic disease of grass carps |
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