Anticancer agent

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the use of potassium osmate salt K2[OsO2(OH)4] with isotope 187Os as a anticancer agent.

EFFECT: salt shows high anticancer activity in system in vivo with no undesired side effects.

 

The invention relates to biologically active substances and can be used in medicine and biology as an independent anti-cancer drugs in a new class, as well as funds for a possible combined use with other anticancer drugs to enhance their therapeutic effect.

Currently, in clinical practice it is known more than 60 anticancer drugs (Anticancer chemotherapy. The Handbook. Ed. Nieremontowany. M.: 1996; Safit J.T., Bonavida Century, Cancer Res., 1992, V.52., P.630; Mikhailov IB workbook for the physician in clinical pharmacology - a guide for physicians. SPb. 2001. str; Knock A.N., Gershanovich M., Blank M.A., Form O.A., Mahnova E.V. Anticancer drugs. - SPb.: NIKA, 2011. - 656 C.). However, the effectiveness of most of them are inadequate and range of cancer that is sensitive to chemotherapy, limited. Among the most available and currently used drugs known drugs such as cisplatin and 5-fluorouracil, which are used separately or in complex therapy of gastric cancer, colon cancer, breast cancer, liver cancer (hepatoma), melanoma, etc. as most of the drugs used for the treatment of malignant diseases, cisplatin and 5-fluorouracil oblad who have high toxicity. In their application, as a rule, are nausea, vomiting, expressed violations of function of kidneys, disorders of the nervous system, bone marrow suppression, etc. (Mashkovsky PPM Medicines. M. 2001. str-428). Therefore, the development of new, more active against malignant neoplasm of medicines at the same time with little toxicity, is an important direction of research in the field of modern pharmacology and Oncology.

The task to be solved by the invention is the creation of new non-toxic anti-cancer drugs.

The problem is solved by use as antitumor agents potassium osmate K2[OsO2(OH)4] on the basis of isotope187Os (next connection).

The study of antitumor activity of the compounds was carried out in the research Institute of Oncology. You in the system in vivo in mice, which intraperitoneally transplanted cells solid Ehrlich tumor, which is usually used for preliminary screening of compounds with potential anticancer activity (Experimental evaluation of anticancer drugs in the USSR and the USA. Ed. Spoofing, Abberline (USSR). Agordina, Aklan (USA). M.: Medicine, 1979, 296 pages). The strain of transplantable op is Holi Ehrlich supported in Oncology research Institute in the form of ascites carcinoma, representing a suspension of tumor cells transplanted intraperitoneally. Intraperitoneal method of introducing the compound was selected for testing in connection with the fact that it is the most effective method of delivering compounds to tumor cells at least the required number of input connections. To obtain a solid tumor this suspension was injected into mice subcutaneously.

The studies used healthy adult animals - 74 mouse-male weight 30-33 g outbred lines SHR wiring research Institute of Oncology. You. Control and experimental animals were kept in a vivarium under the same conditions: in plastic cages type T-2 with small wood chips (no more than 10 animals in one cage with steel bars with a standard light mode and a temperature of 20-22°C, received water and complete briquetted feed PC-120 (produced by LLC "Laboratorium", Moscow) ad libirtum.

As a control drug to test the antitumor activity of the compounds were used cisplatin company Unterach, Austria in a solution of 50 mg/100 ml

All animals after inoculation of the tumor by the method of randomization were divided into groups:

1) control group - introduction of saline once through 48 h after inoculation of the tumor;

2) control group - introduction physiologist the ical solution three times a week, every other day, starting 48 h after inoculation of the tumor;

3) the band - the introduction of cisplatin - 125 μg/mouse once within 48 h after inoculation of the tumor:

4) group - introducing compound - 500 µg/mouse in saline once through 48 h after inoculation of the tumor;

5) group 12-fold introduction connections - 500 µg/mouse in saline three times per week, every other day, starting 48 h after inoculation of the tumor.

All studies were conducted at the same time in the morning.

All animals Ehrlich tumor transplanted subcutaneously into the right side in the amount of 0.2 ml of 10% suspension of cells ascites carcinoma (107cells/mouse).

Connection in saline, cisplatin and saline were injected at 0.25 ml intraperitoneally 48 h after inoculation of the tumor,

It is noted that the mouse was well tolerated by the introduction of the connection.

In the process of research, starting from 14 days after inoculation, 2 times per week measured the length and width of the tumor nodules and defined tumor volume, as the volume of the corresponding ellipsoid.

Efficacy of treatment was evaluated by the inhibition of tumor growth, which was determined in percentage as the ratio of the difference between the average tumor volume in the control group and the mean tumor volume in the experimental group to the average tumor volume in the control group.

Result is you obtained in the studies were subjected to statistical analysis to establish the reliability of the differences found. Differences were considered significant at p<0,05 using t-student test.

As a result of the studies statistically established since the 14th to the 31st day after inoculation:

1. Revealed no significant differences in the growth of the average value of tumor volume in mice from control groups 1 and 2, respectively, single and three times a week through the day the physiological solution.

2. A single intraperitoneal injection of cisplatin at a dose of 125 μg/mouse mice 3rd group significantly inhibited the growth of solid Ehrlich tumor. The maximum inhibition of tumor growth was 50%.

3. Single intraperitoneal administration of the compounds at a dose of 500 μg/mouse mice 4-th group significantly inhibited the growth of solid Ehrlich tumor. The maximum inhibition of tumor growth was 71%.

4. 12-Fold three times a week, every other day intraperitoneal administration of the compounds at a dose of 500 μg/mouse mice 5-th group significantly inhibited the growth of solid Ehrlich tumor. The maximum inhibition of tumor growth was 80%.

Studies have shown that the test connection shows yet in the system in vivo high antitumor properties. Not detected for undesirable side effects.

The results allow to reliably ascertain the presence of compounds - potassium osmate K2[OsO2(OH)4] on the basis of isotope187Os expressed high antitumor activity. This connection can be recommended for practical use as an independent antitumor agent of a new class, and as a means for possible combined use with other anticancer drugs to enhance therapeutic effect.

The use of potassium osmate K2[OsO2(OH)4] on the basis of isotope187Os as antitumor agents.



 

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9 ex, 4 tbl

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18 cl, 92 ex, 2 tbl

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1 tbl

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Material // 2437650

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7 tbl

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3 ex

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22 ex, 1 tbl

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