Inhibiting agent against the proliferation of tumor cells

Details Inhibiting agent against the proliferation of tumor cells Inhibiting agent against the proliferation of tumor cells

1991-05-14

1999-10-26

Davenport, Avis M.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

A61K 3800, A61K 3802

Patent

active

059728795

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

The present invention relates to an inhibiting agent against the proliferation of tumor cells of animals including human beings.


BACKGROUND ART

In spite of the fact that the study of development of carcinostatics are being carried out energetically on a worldwide scale, none of currently used effective carcinostatics are employed without anxiety because of the side effects. Also, in view of the current state that, among physicotherapies, there is no effective and noticeable one that gives less load, it is desired to develop satisfactory carcinostatics as soon as possible.
Taking this into consideration, the present applicant suggested inhibiting agents against the proliferation of malignant tumor cells of human beings in U.S. Pat. Nos. 4,810,495 and 4,963,358 and a process for the preparation of an inhibiting agent against the proliferation of malignant tumor cells of animals in U.S. Pat. No. 4,595,657.
However, in those patents, the substances that inhibit the proliferation of malignant tumor cells were unclear.
Further, the present applicant suggested an inhibiting agent against the proliferation of malignant tumor cells of human beings comprising 2-hydroxy-1-(P-hydroxyphenyl)-5-methylhexane-3-one in Japanese Patent Tokkai-hei 2-247121 (Laid-Open No. 247121/1995), an inhibiting agent against the proliferation of malignant tumor cells of human beings comprising a monoglyceride in Japanese Patent Tokkai-hei 2-247125 (Laid-Open No. 247125/1995), and an inhibiting agent against the proliferation of malignant tumor cells of human beings comprising 2-heptadecanol in Japanese Patent Tokkai-hei 2-247120 (Laid-Open No. 247120/1995).
The object of the present invention is. to provide an inhibiting agent against the proliferation of tumor cells which is not any of the substances that were suggested in the above inventions, does not affect at all, in a toxicity test using normal cells, their proliferation, further in a test of the inhibition of proliferation of tumor cells of human beings transplanted in nude mice, stops the proliferation several days after the start of the administration as well as permits the tumor to reduce significantly in spite of the absence of followed administration, shows stable effectiveness by hypodermic administration, and has a stable prolonged action in organisms.


DISCLOSURE OF INVENTION

The present inhibiting agent against the proliferation of tumor cells comprises a lower condensation polymer or oligomer of an .alpha.-hydroxy acid, an oligopeptide containing at least one pyroglutamic acid residue, and a stabilizer.
Said lower condensation polymer or oligomers of an .alpha.-hydroxy acid are mainly those comprising compounds formed by condensing and polymerizing 2 to 10 molecules of an .alpha.-hydroxy acid and their metal salts.
Further, said oligopeptide containing at least one pyroglutamic acid residue comprises a compound containing at least one pyroglutamic acid residue that is an oligopeptide made up of 2 to 8 amino acid residues and its metal salt.
The weight ratio of the components is such that the ratio of the lower condensation polymer or oligomer of an .alpha.-hydroxy acid is 10, the ratio of the oligopeptide containing at least one pyroglutamic acid residue is 1 to 4, and the ratio of the stabilizer (a saccharide or a sugaralcohol) is 1 to 3.


BRIEF DESCRIPTION OF THE DRAWING

FIG. 1 is a chart showing the relationship of the survival rates to the doses of the present inhibiting agent against the proliferation of tumor cells


BEST MODE FOR CARRYING-OUT THE INVENTION



EXAMPLE 1



Preparation of Lactic Acid Oligomer (Condensation Polymer of
.beta.-Hydroxypropionic Acid)
Lactic acid (.alpha.-hydroxypropionic acid) is chemically highly reactive and solidifies when heated for 100 min at 140.degree. C. When the solid is dissolved in water and is rendered alkaline, a precipitate is formed, which hardly dissolves even when it is rendered acid. When the precipitate is heated for 2 hours at 175.degree. C., it turns into a substance that does not dissolve i

REFERENCES:
patent: 4211769 (1980-07-01), Okada et al.
Patent Astracts of Japan, vol. 9, No. 130, (C-284) (1853) dated Jun. 5, 1985.

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