Cytostatic, cytotoxic and protein tyrosine kinase inhibitory activity of ursolic acid in A431 human tumor cells

F. Hollósy, G. Mészáros, G. Bökönyi, M. Idei, A. Seprödi, B. Szende, G. Kéri

Research output: Contribution to journalArticle

41 Citations (Scopus)

Abstract

The effect of the tritepene, ursolic acid, on the proliferation of A431 human epidermoid carcinoma cells was studied. According to our investigations, ursolic acid is a potent inhibitor of A431 cell growth. Ursolic acid markedly reduced A431 cell growth in a time- and dose- dependent manner. We found a good correlation between the results of direct cell counting and the MTT test. During long periods of drug exposure, ursolic acid exhibited both cytotoxic and cytostatic activity. The effect was partially reversible on drug removal. The greatest cytotoxicity was observed both in the trypan blue test and in the MTT test at 50 mM. Investigations on tyrosine kinase inhibition were performed by biochemical and cellular assays on A431 cells. Ursolic acid inhibited tyrosine kinase activity of A431 cells in biochemical assay in a dose- dependent manner with an IC50 of 24 mM. In cellular assay, when A431 cells were pretreated with ursolic acid for 24, 48 and 168 hours at various concentrations (5, 10, 20, 30 and 50 mM), lower values of IC50 were measured: 6.8μM for 24 hours, 5.2 mM for 48 hours and 1.4 mM for 168 hours. The results suggest that ursolic acid exerts an antiproliferative effect through the inhibition of tyrosine kinase enzymes.

Original languageEnglish
Pages (from-to)4563-4570
Number of pages8
JournalAnticancer Research
Volume20
Issue number6 B
Publication statusPublished - 2000

Fingerprint

Cytostatic Agents
Protein-Tyrosine Kinases
Neoplasms
Inhibitory Concentration 50
Growth Inhibitors
Trypan Blue
ursolic acid
Pharmaceutical Preparations
Squamous Cell Carcinoma
Enzymes
Growth

Keywords

  • A431 human epidermoid carcinoma cell
  • Inhibition of protein tyrosine kinase
  • MTT-assay
  • Proliferation
  • Ursolic acid

ASJC Scopus subject areas

  • Cancer Research
  • Oncology

Cite this

Cytostatic, cytotoxic and protein tyrosine kinase inhibitory activity of ursolic acid in A431 human tumor cells. / Hollósy, F.; Mészáros, G.; Bökönyi, G.; Idei, M.; Seprödi, A.; Szende, B.; Kéri, G.

In: Anticancer Research, Vol. 20, No. 6 B, 2000, p. 4563-4570.

Research output: Contribution to journalArticle

@article{d0bb6acc5b4d4cb48db747f059e8cad3,
title = "Cytostatic, cytotoxic and protein tyrosine kinase inhibitory activity of ursolic acid in A431 human tumor cells",
abstract = "The effect of the tritepene, ursolic acid, on the proliferation of A431 human epidermoid carcinoma cells was studied. According to our investigations, ursolic acid is a potent inhibitor of A431 cell growth. Ursolic acid markedly reduced A431 cell growth in a time- and dose- dependent manner. We found a good correlation between the results of direct cell counting and the MTT test. During long periods of drug exposure, ursolic acid exhibited both cytotoxic and cytostatic activity. The effect was partially reversible on drug removal. The greatest cytotoxicity was observed both in the trypan blue test and in the MTT test at 50 mM. Investigations on tyrosine kinase inhibition were performed by biochemical and cellular assays on A431 cells. Ursolic acid inhibited tyrosine kinase activity of A431 cells in biochemical assay in a dose- dependent manner with an IC50 of 24 mM. In cellular assay, when A431 cells were pretreated with ursolic acid for 24, 48 and 168 hours at various concentrations (5, 10, 20, 30 and 50 mM), lower values of IC50 were measured: 6.8μM for 24 hours, 5.2 mM for 48 hours and 1.4 mM for 168 hours. The results suggest that ursolic acid exerts an antiproliferative effect through the inhibition of tyrosine kinase enzymes.",
keywords = "A431 human epidermoid carcinoma cell, Inhibition of protein tyrosine kinase, MTT-assay, Proliferation, Ursolic acid",
author = "F. Holl{\'o}sy and G. M{\'e}sz{\'a}ros and G. B{\"o}k{\"o}nyi and M. Idei and A. Sepr{\"o}di and B. Szende and G. K{\'e}ri",
year = "2000",
language = "English",
volume = "20",
pages = "4563--4570",
journal = "Anticancer Research",
issn = "0250-7005",
publisher = "International Institute of Anticancer Research",
number = "6 B",

}

TY - JOUR

T1 - Cytostatic, cytotoxic and protein tyrosine kinase inhibitory activity of ursolic acid in A431 human tumor cells

AU - Hollósy, F.

AU - Mészáros, G.

AU - Bökönyi, G.

AU - Idei, M.

AU - Seprödi, A.

AU - Szende, B.

AU - Kéri, G.

PY - 2000

Y1 - 2000

N2 - The effect of the tritepene, ursolic acid, on the proliferation of A431 human epidermoid carcinoma cells was studied. According to our investigations, ursolic acid is a potent inhibitor of A431 cell growth. Ursolic acid markedly reduced A431 cell growth in a time- and dose- dependent manner. We found a good correlation between the results of direct cell counting and the MTT test. During long periods of drug exposure, ursolic acid exhibited both cytotoxic and cytostatic activity. The effect was partially reversible on drug removal. The greatest cytotoxicity was observed both in the trypan blue test and in the MTT test at 50 mM. Investigations on tyrosine kinase inhibition were performed by biochemical and cellular assays on A431 cells. Ursolic acid inhibited tyrosine kinase activity of A431 cells in biochemical assay in a dose- dependent manner with an IC50 of 24 mM. In cellular assay, when A431 cells were pretreated with ursolic acid for 24, 48 and 168 hours at various concentrations (5, 10, 20, 30 and 50 mM), lower values of IC50 were measured: 6.8μM for 24 hours, 5.2 mM for 48 hours and 1.4 mM for 168 hours. The results suggest that ursolic acid exerts an antiproliferative effect through the inhibition of tyrosine kinase enzymes.

AB - The effect of the tritepene, ursolic acid, on the proliferation of A431 human epidermoid carcinoma cells was studied. According to our investigations, ursolic acid is a potent inhibitor of A431 cell growth. Ursolic acid markedly reduced A431 cell growth in a time- and dose- dependent manner. We found a good correlation between the results of direct cell counting and the MTT test. During long periods of drug exposure, ursolic acid exhibited both cytotoxic and cytostatic activity. The effect was partially reversible on drug removal. The greatest cytotoxicity was observed both in the trypan blue test and in the MTT test at 50 mM. Investigations on tyrosine kinase inhibition were performed by biochemical and cellular assays on A431 cells. Ursolic acid inhibited tyrosine kinase activity of A431 cells in biochemical assay in a dose- dependent manner with an IC50 of 24 mM. In cellular assay, when A431 cells were pretreated with ursolic acid for 24, 48 and 168 hours at various concentrations (5, 10, 20, 30 and 50 mM), lower values of IC50 were measured: 6.8μM for 24 hours, 5.2 mM for 48 hours and 1.4 mM for 168 hours. The results suggest that ursolic acid exerts an antiproliferative effect through the inhibition of tyrosine kinase enzymes.

KW - A431 human epidermoid carcinoma cell

KW - Inhibition of protein tyrosine kinase

KW - MTT-assay

KW - Proliferation

KW - Ursolic acid

UR - http://www.scopus.com/inward/record.url?scp=0034477152&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0034477152&partnerID=8YFLogxK

M3 - Article

VL - 20

SP - 4563

EP - 4570

JO - Anticancer Research

JF - Anticancer Research

SN - 0250-7005

IS - 6 B

ER -