CN1127117A - Application of googerotin used as antineoplastic medicine - Google Patents
Application of googerotin used as antineoplastic medicine Download PDFInfo
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- CN1127117A CN1127117A CN 95115838 CN95115838A CN1127117A CN 1127117 A CN1127117 A CN 1127117A CN 95115838 CN95115838 CN 95115838 CN 95115838 A CN95115838 A CN 95115838A CN 1127117 A CN1127117 A CN 1127117A
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- yungumycin
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Abstract
For a kind of structure known googertin, the external test uses the cultured humanbody cancer cell (KB cell), the clone for mation determination method checks it possessing of killing and wounding actions to the KB cell, the concentration for inhibiting 50% clone formation is 3 mug/ml. The internal test uses colonic cancer 26 and sarcoma 180, the small piece of colonic cancer 26 tissue is inoculated to the axillary subdutaneous tissue of BALB/c mouse or the sarcoma 180 ascites of mouse is diluted with physiologic saline (1:3) and then inoculated to the axillary subcutaneous tissue of Kunming mouse. After 24 hr., the administration of intra-abdominal injection (ip) and gastric perfusion. (PO) are conducted, the inhibition rate for cancer is as follows: for colonic cancer (ip) 41-43%, (po) 72-86%, for sarcoma 180 (po) 80%. The results are close to that of 5-fluorouracil.
Description
Yungumycin (Yungumycin) is to economize the anti-tumor active substance that separates No. 2321 bacterial strains generations of streptomycete that obtain the soil of Guan Ping nature reserve area from Yunnan Province of China.Studies have shown that yungumycin shows lethal effect to the tumor cell of In vitro culture, the laboratory animal tumor is had significant curative effect, might be used for oncotherapy.(the generation bacterium of yungumycin is deposited in " China Committee for Culture Collection of Microorganisms's common micro-organisms " center ", BeiJing ZhongGuanCun.26 days July nineteen ninety-five of preservation date, numbering 0234).
Manager's voltinism matter and Study on Identification determine that yungumycin is identical with the preceding gougerotin of having reported (gougerotin)
According to early stage bibliographical information, gougerotin is the broad-spectrum antiseptic antibiotic, but weak antibacterial activity is only arranged; Report does not have anti-tumor activity (Journal of Antibiotics, Series A, 1962; 15:93).It is reported that asteromycin (asteromycin) is identical with gougerotin, asteromycin has inhibitory action in vitro tests to the HeLa cell, and valid density is 1-2 μ g/ml; It is said that the asteromycin intraperitoneal injection has activity to murine sarcoma 180 (ascitic type), but do not report concrete data (Journal of Antibiotics, 1972; 25:548).Qingfengmeisu it was reported it is a chemical constitution and the similar antibiotic of gougerotin, but report does not have anti-tumor activity (microorganism journal, 1975; 15:101).Ningnanmycin is stated to be the gougerotin isomers, and report does not have antitumor action (People's Republic of China's application for a patent for invention prospectus, application number 93104287.9).In sum, the gougerotin animal vivo test that do not appear in the newspapers both at home and abroad so far has definite curative effect to tumor, and the gougerotin that also do not appear in the newspapers is applied to clinical cancer therapy.Yungumycin is determined identical with gougerotin after deliberation.Studies have shown that of this invention, yungumycin has significant curative effect to animal tumor, may be used for the treatment of tumor.
The objective of the invention is to utilize yungumycin (gougerotin) as antitumor drug, the treatment tumor.
The content and the main points of this invention are:
1. yungumycin is to the lethal effect In vitro culture human cancer cell (oral squamous cell carcinomas KB cell) of tumor cell, forming algoscopy with the clone detects, medicine contacts 6 days with cancerous cell, studies have shown that yungumycin has lethal effect to the KB cell, the concentration (IC50) that suppresses 50% clone's formation is 3 μ g/ml (accompanying drawings 1).
2. to be seeded in the BALB/c mouse armpit subcutaneous for yungumycin tumor tissue fritter (diameter 2mm) that the curative effect of mouse junction cancer is got colon cancer 26; Inoculate back 24 hours through intraperitoneal injection (ip) or the administration of filling stomach (po), control animals gives normal saline, puts to death animal after 10 days, gets tumor and weighs, and calculates tumour inhibiting rate.Result of study shows that yungumycin ip administration has certain curative effect to intestinal cancer 26, and tumour inhibiting rate is 41%-43%, p＜0.01 (table 1).Yungumycin po administration has significant curative effect, and tumour inhibiting rate can reach 72%-86% (table 2).
The intraperitoneal injection of table 1 yungumycin is to the inhibitory action of mouse junction cancer 26
Heavy (g) suppression ratio of dosage the weight of animals (g) tumor
(mg/kg) death toll begins/finishes X ± SD (%) contrast 0 19.8/21.5 1.73 ± 0.31 yungumycins 0.06 * 10 0 20.2/19.9 1.58 ± 0.71 4
0.12×10 0 19.4/17.9 1.34±0.28 22
0.25 * 10 0 20.5/16.8 0.97 ± 0.35 43* contrasts 0 18.6/17.8,2.44 ± 0.56 yungumycins 0.25 * 50 19.0/18.4,1.80 ± 0.34 26*
0.50×5 0 20.9/17.0 1.44±0.24 41**
1.00×3 0 18.7/18.5 1.39±0.19 43**
The subcutaneous vaccination tumor, ip gives yungumycin; N=6
* p＜0.05, * * p＜0.01, with matched group relatively.
Table 2 yungumycin gastric infusion is to the inhibitory action of mouse junction cancer 26
Heavy (g) suppression ratio of dosage the weight of animals (g) tumor
(mg/kg) death toll begins/finishes X ± SD (%) contrast 0 22.7/19.4 1.40 ± 0.19 yungumycins 12.5 * 30 22.5/15.2,0.39 ± 0.15 72**
25.0×3 1 22.4/16.9 0.20±0.08 86**
The subcutaneous vaccination tumor is irritated stomach and is given yungumycin; N=6
Compare with matched group * p＜0.01.
3. yungumycin is got murine sarcoma 180 ascites to the curative effect of murine sarcoma 180 and is added normal saline (1: 3) dilution, and it is subcutaneous to be inoculated in the Kunming mouse armpit, every Mus 0.2ml.Inoculate back 24 hours filling stomaches and give yungumycin, control animal gives normal saline, puts to death animal after 10 days, gets tumor and weighs, and calculates tumour inhibiting rate.Result of study shows that the yungumycin gastric infusion has significant curative effect to murine sarcoma 180 (solid type), uses tolerable dose (25mg/kg), and the tumour inhibiting rate of single-dose can reach 83%, p＜0.01; Use smaller dose (15mg/kg and 20mg/kg), the tumour inhibiting rate of 3 administrations is respectively 72% and 81%, p＜0.01 (table 3).
Table 3 yungumycin gastric infusion is to the inhibitory action of murine sarcoma 180
Heavy (g) suppression ratio of dosage the weight of animals (g) tumor
(mg/kg) death toll begins/finishes X ± SD (%)
I. contrast 0 19.1/28.8 2.86 ± 0.52
Yungumycin 15 * 10 19.8/27.3,1.59 ± 0.67 44**
20×1 0 19.0/25.4 0.84±0.29 71**
25×1 0 20.3/24.8 0.50±0.20 83**
II. contrast 19.5/29.4 2.74 ± 0.86
Yungumycin 15 * 30 19.0/28.6,0.76 ± 0.32 72**
20×3 1 20.1/24.7 0.52±0.20 81**
25×3 1 19.7/25.1 0.47±0.18 83**
The subcutaneous vaccination tumor, ip gives yungumycin; N=10
Compare with matched group * p＜0.01.
4. the antitumor action of yungumycin and 5-fluorouracil relatively adopts the test method of above-mentioned (3), mouse hypodermic inoculation sarcoma 180 cell is irritated stomach and is given yungumycin or 5-fluorouracil, and using dosage is equivalent to 1/3LD50 respectively, be yungumycin 15mg/kg, 5-fluorouracil 40mg/kg; Administration is 3 times altogether.Result of study proves that yungumycin and 5-fluorouracil are close to the curative effect of sarcoma 180 (solid type), and tumour inhibiting rate is respectively 72% and 70%, and both compare p＞0.05 (accompanying drawing 2).
5. the toxicity of yungumycin is 90mg/kg to the acute toxicity LD50 (po) of mice.Yungumycin gastric infusion treated animal (25mg/kg * 1 or 25mg/kg * 3 are 83% to the tumour inhibiting rate of sarcoma 180), through histopathologic examination, the heart, lung, liver,kidney,spleen, stomach, small intestinal etc. there is no the toxicity pathological changes.
Advantage of the present invention and good effect are: for yungumycin (gougerotin) has been opened up new purposes.The yungumycin oral administration has significant curative effect to the laboratory animal tumor.The antitumous effect of the 5-fluorouracil of yungumycin and present clinical use is close, but chemical constitution is different, and expection yungumycin (gougerotin) is used for clinical cancer therapy, can obtain good effect.
Description of drawings:
The lethal effect of Fig. 1 yungumycin oral cavity squamous cell carcinoma KB cell;
Fig. 2 yungumycin and 5-are to the inhibitory action of murine sarcoma 180.
(n＝10)
Claims (3)
1. yungumycin (Gu Shi mycin) is characterized in that as the application of antineoplastic agent the yungumycin in vitro tests has lethal effect to tumor cell, and in vivo test has remarkable therapeutic effect to tumor.
2. according to the application of the described antineoplastic agent of claim 1., it is characterized in that the In vitro culture human cancer cell, detect with clone forming method that yungumycin has lethal effect to human mouth scale cancer KB cell, IC50 is 3 μ g/ml.
3. according to the application of the described antineoplastic agent of claim 1., it is characterized in that animal vivo test, in BALB/c mouse subcutaneous vaccination colon cancer 26, or at Kunming mouse subcutaneous vaccination sarcoma 180, inoculate administration after 24 hours, put to death animal after 10 days, judge the tumour inhibiting rate of intraperitoneal injection administration and gastric infusion.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN95115838A CN1060933C (en) | 1995-09-01 | 1995-09-01 | Application of googerotin used as antineoplastic medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN95115838A CN1060933C (en) | 1995-09-01 | 1995-09-01 | Application of googerotin used as antineoplastic medicine |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1127117A true CN1127117A (en) | 1996-07-24 |
| CN1060933C CN1060933C (en) | 2001-01-24 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN95115838A Expired - Fee Related CN1060933C (en) | 1995-09-01 | 1995-09-01 | Application of googerotin used as antineoplastic medicine |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102250176A (en) * | 2011-05-16 | 2011-11-23 | 中国医学科学院医药生物技术研究所 | Antitumor antibiotic ancomycin and its derivative |
| CN109329207A (en) * | 2018-11-21 | 2019-02-15 | 胡学东 | A kind of experimental animal model for anticancer agents and its construction method |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS4625026B1 (en) * | 1968-09-11 | 1971-07-19 | ||
| CN1036307C (en) * | 1993-04-23 | 1997-11-05 | 中国科学院成都生物研究所 | A new antibiotic pesticides-Ningnan Meisu |
-
1995
- 1995-09-01 CN CN95115838A patent/CN1060933C/en not_active Expired - Fee Related
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102250176A (en) * | 2011-05-16 | 2011-11-23 | 中国医学科学院医药生物技术研究所 | Antitumor antibiotic ancomycin and its derivative |
| WO2012155824A1 (en) * | 2011-05-16 | 2012-11-22 | 中国医学科学院医药生物技术研究所 | Ancomycin and its derivatives, preparation methods and uses thereof |
| CN102250176B (en) * | 2011-05-16 | 2014-12-31 | 中国医学科学院医药生物技术研究所 | Antitumor antibiotic ancomycin and its derivative |
| CN109329207A (en) * | 2018-11-21 | 2019-02-15 | 胡学东 | A kind of experimental animal model for anticancer agents and its construction method |
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| Publication number | Publication date |
|---|---|
| CN1060933C (en) | 2001-01-24 |
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