Abstract
The aim. To study the cell immunity status under influence of 3-[5-(1H-indol-3-ylmethylene)-4-oxo-2-thioxo-thiazolidin-3-yl]-propionic acid, as a prominent 4-thiazolidinone derivative and a class of biologically active compounds with polypharmacological properties. Materials and methods. Experimental method on the model of laboratory animals (guinea pigs); intradermal allergy tests; relative and absolute content in the peripheral blood of T- and B-lymphocytes subpopulations; hematological indexies: index of the ratio of lymphocytes and monocytes, index of the ratio of neutrophils and monocytes, index of the ratio of neutrophils and eosinophils, phagocytic index, phagocytic number; ELISA; organic synthesis; pharmacological screening. Results. The effect of 3-[5-(1H-indol-3-ylmethylene)-4-oxo-2-thioxo-thiazolidin-3-yl]-propionic acid has antifungal properties and affect cellular component of immunity in vivo in the guinea pigs model. There are no changes in the skin of guinea pigs during and after chemical applications of the skin and after intradermal tests. The compound stimulate the immune cells, in particular the lymphocyte (increase in the absolute number of CD3 T-lymphocytes by 21.46 % and the absolute number of CD8 T-suppressors by 27.15 %), but with a selective inhibitory effect on certain units (decrease the relative number of NK cells CD16 by 11.57 % and B-lymphocytes CD22 by 23.08 %). There was an increase in the activity of the macrophage phagocytic system (increase in PN by 439.87 % and PI by 62.73 % at 120 minutes), which indicates the reliability of the absorbing function of phagocytes, but with a decrease in their ability to endocytosis (PCI decreased significantly by 78,72 %). Conclusions. Synthesized 3-[5-(1H-indol-3-ylmethylene)-4-oxo-2-thioxo-thiazolidin-3-yl]-propionic acid has a selective activating effect on certain parts of cellular immunity and on phagocytic activity. Derivate influence on the phagocytic activity of neutrophils is ambiguous, and the effect of the compound directed to the cellular part of the immune system does not cause cellular immunodeficiency. The studied derivative is promising for further study of the drug-like molecule with antifungal and antitumor effects
Highlights
Cancer is the cause of every sixth death on the planet and ranks second among the leading causes of death [1]
There were observed no changes in the skin of the guinea pig during the chemical application of skin applications and after intradermal tests in doses of 1:10 and 1:100
The total number of leukocytes increased by 21.76 %, an increase in the absolute number of eosinophils
Summary
Cancer is the cause of every sixth death on the planet and ranks second among the leading causes of death [1]. It is important to search for new molecules with polypharmacological properties capable of polytarget activity, in particular with respect to antibiotic-resistant microorganisms and chemotherapeutic-resistant cancer cells [2]. 4-thiazolidinone derivatives are an important class of “drug-like” molecules with anticancer [3, 4], antiprypanosomal [5], antiviral [6], antimicrobial [7], antifungal [8], anti-inflammatory [9], antioxidant [10] activity. The thiazole heterocycle is present in drugs with antimicrobial activity, such as penicillin, monobactam, sulfathiazole, thiabendazole, nizatidine, as well as drugs for the treatment of cancer, such as sunitinib, which makes thiazole/thiazolidinone derivatives a potential source of new agents with polytargetative action. The prospects for the use in medicine of the isolated compound-leader (Fig. 1) became the basis for the study of its effect on the cellular immune system and allergenic action in vivo
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