CN1217185A - Anti-tumor noval use of cinnamamide - Google Patents
Anti-tumor noval use of cinnamamide Download PDFInfo
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- CN1217185A CN1217185A CN 98124419 CN98124419A CN1217185A CN 1217185 A CN1217185 A CN 1217185A CN 98124419 CN98124419 CN 98124419 CN 98124419 A CN98124419 A CN 98124419A CN 1217185 A CN1217185 A CN 1217185A
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- cinnamamide
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- antitumor action
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Abstract
The present invention relates to a new antineoplastic pharmacological action of known structure compound cinnamamide. Said compound possesses proliferation inhibiting action for malignant tumor cell, and can inhibit blood vessel formation. The animal test shows that it can inhibit the growth of mouse transplantation liver cancer, carcinoma of colon and lung cancer, it can reduce the malignant tumor metastatic incidence rate of the lung and number of metastatic foci. Said compound is low in toxicity, and can inhibit the growth and metastasis of tumor.
Description
The cinnamamide that the present invention relates to is a hypotoxic anti-malignant tumor active compound, is expected to be used for the transfer of clinical treatment tumour.
Malignant tumor serious threat human health and life.The chemotherapeutics toxicity of clinical practice at present is bigger, and is relatively poor to the solid tumor effect, accepts patient's overwhelming majority of chemotherapy and finally all die from transfer.Therefore, seek hypotoxicity and can suppress tumor growth, the medicine of transfer is the vital task of tumor chemotherapeutic drug research.The known structure chemical compound cinnamamide that the present invention relates to, its zoopery toxicity is very little, has the inhibition angiogenesis, suppresses growth of tumor and transferance.
The present invention seeks to cinnamamide is used for chemotherapy of tumors, obtain better curative effect.Content of the present invention and main points are: 1) utilize the blue tetrazolium method, detect cinnamamide to the human normal cell line of In vitro culture and the inhibited proliferation of tumor cell.With medicine and co-culture of cells 72 hours, add blue tetrazolium reagent, react 4 hours, remove culture fluid and add dimethyl sulfoxide with Rong Xie Jia Za granule, then at 540nm place measurement absorbance with the judgement pharmaceutically active.The result shows that it is to the half-inhibition concentration (IC of human embryo lung (HEL) 2BS cell
50) be 4.3mM, and to the IC of tumor cell (human hepatocellular carcinoma BEL-7402 cell, human oral cavity epithelial cancer KB cell, human fibrosarcoma HT-1080 cell)
50For 1-2mM (table 1), demonstrate certain selectivity.Utilization chick embryo allantois embrane method detects finds that cinnamamide can suppress the Embryo Gallus domesticus vessel growth when dosage is 60 μ g/.
The inhibited proliferation of table 1 cinnamamide and tumor cell normal to the people
| Cell strain | ????IC 50(mM) |
| Human embryo lung (HEL) 2BS cell human hepatocellular carcinoma BEL-7402 cell human oral cavity epithelial cancer KB cell human fibrosarcoma HT-1080 cell | ????4.33 ????1.94 ????1.62 ????1.29 |
2) find that this chemical compound can suppress the growth of mice transplanted tumor.In mouse hypodermic inoculation hepatocarcinoma 22, intestinal cancer 26 and Lewis lung cancer, abdominal cavity or oral administration are pressed tumor weight or volume calculation, and cinnamamide all can effectively suppress growth of tumor (table 2,3,4) on three kinds of transplanted tumor models.
Table 2 cinnamamide is to the inhibitory action of rat liver cancer 22 growths
* P＜0.05, compare notes with matched group: subcutaneous vaccination began administration after 24 hours, and 10 of every treated animals occur dead.
| Neat amount (mg/kg) | Body weight change (g) | Tumor heavy (g) | Tumour inhibiting rate (%) | |
| Matched group medicine group | ????75,ip ????150,ip ????75,po ????150,po | ????+10.85 ????+8.08 ????+3.38 ????+8.19 ????+6.69 | ?3.01±1.01 ?1.76±0.67 ?1.54±0.38 ?2.29±0.97 ?1.79±0.58 | ????41.5* ????48.8* ????23.9* ????40.5* |
Table 3 cinnamamide is to the inhibitory action of mice intestinal cancer 26 growths
* P＜0.01, compare notes with matched group: subcutaneous vaccination began administration after 24 hours, and 8 of every treated animals occur dead.
| Dosage (mg/kg) | Body weight change (g) | Tumor heavy (g) | Tumour inhibiting rate (%) | |
| Contrast mitomycin cinnamamide | ????1,ip ????50,ip ????100,ip | ????+2.64 ????+1.94 ????+0.94 ????+0.46 | ?2.41±0.4 ?1.31±0.67 ?1.67±0.53 ?1.47±0.26 | ????45.6* ????30.7* ????39.0* |
Table 4 cinnamamide is to the inhibitory action of Mice Bearing Lewis Lung Cancer growth
* P＜0.01, compare notes with matched group: subcutaneous vaccination began administration after 24 hours, and 8 of every treated animals occur dead.
| Dosage (mg/kg) | Body weight change (g) | Tumor volume (mm 3) | Tumour inhibiting rate (%) | |
| Contrast cyclophosphamide cinnamamide | ?100,ip×3 ?50,ip×10 ?50,ip×14 ?100,ip×10 | ????+8.55 ????-3.16 ????+1.75 ????-0.93 ????+0.42 | ?7975±1816 ?3663±816 ?4578±1021 ?2504±1011 ?3745±711 | ????54.1* ????42.6* ????68.6* ????53.9* |
3) find that this chemical compound can suppress the transfer of tumor.Lumbar injection gives cinnamamide on the spontaneous metastasis model of Mice Bearing Lewis Lung Cancer, and the result has reduced the number of mice (rate of transform) that the lung transfer occurs, and the number of lung transfer simultaneously also obviously reduces (table 5).
The inhibitory action that table 5 cinnamamide shifts the Mice Bearing Lewis Lung Cancer lung
* P＜0.05, compare notes with matched group: subcutaneous vaccination began administration after 24 hours, and 8 of every treated animals occur dead.
| Dosage (mg/kg) | The rate of transform | Mean transferred kitchen range number | Suppression ratio (%) | |
| Contrast cyclophosphamide cinnamamide | ?100,ip×3 ?50,ip×10 ?50,ip×19 ?100,ip×10 | ?8/8 ?7/8 ?7/8 ?5/8 ?7/8 | ?11.0±5.7 ?8.8±5.6 ?10.3±5.7 ?4.8±1.9 ?4.5±2.6 | ?20.5 ?56.8* ?59.1* |
4) by intraperitoneal injection, observe the interior animal dead situation of kunming mice fortnight to weigh its toxicity, experiment shows that this toxicity of compound is very low in the body, the median lethal dose(LD 50) of its acute toxicity is 503mg/kg.
Advantage of the present invention and good effect are the new purposes of having opened up the cinnamamide antitumor action, and this toxicity of compound is low, and it can suppress the growth and the transfer of tumor primary tumor, show that this chemical compound has development prospect.
Claims (5)
- The new purposes of 1 cinnamamide antitumor action is characterized in that experiment in vitro is inhibited to the propagation of tumor cell, and experiment toxicity is low in the body, can suppress tumor growth and transfer.
- 2 new purposes by the described cinnamamide antitumor action of claim 1, it is characterized in that experiment in vitro adopts the blue tetrazolium method, with medicine and tumor cell co-cultivation, adding blue tetrazolium reagent reacts, remove culture fluid, add dimethyl sulfoxide,, survey absorbance at the 540nm place to judge pharmaceutically active with Rong Xie Jia Za granule.
- The 3 new purposes of antitumor action by the described cinnamamide of claim 1 is characterized in that by the intraperitoneal injection fortnight, observe the normal mouse death condition, to judge the hypotoxicity of cinnamamide.
- 4 new purposes by the described cinnamamide antitumor action of claim 1, it is characterized in that experiment in the animal body, in mouse hypodermic inoculation pulmonary carcinoma 22, intestinal cancer 26 and Lewis lung cancer, abdominal cavity or oral administration, press tumor weight or volume calculation, cinnamamide all can effectively suppress tumor growth to three kinds of transplanted tumor models.
- 5 according to the new purposes of the described cinnamamide antitumor action of claim 1, it is characterized in that the mouse hypodermic inoculation Lewis lung cancer after, through intraperitoneal injection, can suppress the formation of pulmonary metastases.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN98124419A CN1086577C (en) | 1998-10-30 | 1998-10-30 | Anti-tumor noval use of cinnamamide |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN98124419A CN1086577C (en) | 1998-10-30 | 1998-10-30 | Anti-tumor noval use of cinnamamide |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1217185A true CN1217185A (en) | 1999-05-26 |
| CN1086577C CN1086577C (en) | 2002-06-26 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN98124419A Expired - Fee Related CN1086577C (en) | 1998-10-30 | 1998-10-30 | Anti-tumor noval use of cinnamamide |
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| CN (1) | CN1086577C (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8599999B2 (en) | 2009-06-30 | 2013-12-03 | Nuctech Company Limited | Detection system, DR imaging apparatus and CT imaging apparatus |
| WO2014044028A1 (en) * | 2012-09-18 | 2014-03-27 | 中国人民解放军第四军医大学 | Anti lung cancer drug made of oleum cassiae and major constituent cinnamaldehyde thereof and use thereof |
-
1998
- 1998-10-30 CN CN98124419A patent/CN1086577C/en not_active Expired - Fee Related
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8599999B2 (en) | 2009-06-30 | 2013-12-03 | Nuctech Company Limited | Detection system, DR imaging apparatus and CT imaging apparatus |
| WO2014044028A1 (en) * | 2012-09-18 | 2014-03-27 | 中国人民解放军第四军医大学 | Anti lung cancer drug made of oleum cassiae and major constituent cinnamaldehyde thereof and use thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1086577C (en) | 2002-06-26 |
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Granted publication date: 20020626 Termination date: 20131030 |