Biomedical subjects

M Mikulásová

Publications and source records attributed to M Mikulásová.

8 recordsLinked to original sources

PubMed2006

[A study of qualitative properties of the essential oil of Tanacetum vulgare L].

The study examined the qualitative properties of the essential oil obtained from the flower heads of the species Tanacetum vulgare L. The composition of the essential oil was evaluated in plants from various localities, which differed in the altitude, temperature gradient, as well as soil-climate conditions. With the use of gas chromatography (GC/MS), 49 constituents of the essential oil were separated, out of which 35 was identified. The shares of the constituents in the essential oil differed in dependence on the locality. In the lowest-lying locality with a relatively large sunshine, the content of beta-tujons in the essential oil was the highest, whereas in the regions lying towards the north the content of the essential oil was decreased and the content of camphor was increased. In the northern most region an increased number of chemovars of the camphor-cineole type was observed. In conclusion, it must be said that different climatic and agrotechnical conditions, geographical origin and adaptation of the genotypes of Tanacetum vulgare to the growth conditions can be the causes of the found chemotypes in the localities under examination.

Flowers↗

PubMed2004

Cytotoxic and genotoxic effects of some substituted tetrazolo[1,5-c]quinazolines.

Nine substituted tetrazolo[1,5-c]quinazolines have been tested for cytotoxic effects and structure activity relationship on the murine cancer cell line B16 and four bacterial strains. The most cytotoxic activity had non-substituted in the aromatic ring or substituted by bromo- or chloro-group, and in the pyrimidine ring of quinazoline skeleton by phenyl or morpholine group, respectively. In the bacterium all tested quinazolines had a lower antibacterial effect than ampicillin. 9-bromo-5-morpholino-tetrazolo[1,5-c]quinazoline (BMTQ) at the highest concentration tested (30.0 micromol/l) had an acute cytostatic effect manifested by the total inhibition of the cell proliferation. Other concentrations caused a cytotoxicity proportional to the concentration used. The IC50 values were found to be less than 4 microg/ml, a limit put forward by the National Cancer Institute (NCI) for classification of the compound as a potential anticancer drug. BMTQ induced mutations in a dose-related manner, starting from 10 microg/plate in strains TA100 and TA102. Lesser but significant increases in revertant colonies were also obtained in strain TA98. The mutagenity was slightly enhanced by metabolic activation.

Animals↗

PubMed2001

Copper complexes with bioactive ligands Part I--Antimicrobial activity.

Biological properties of new copper(II) complexes of 2-methylthionicotinate (2-MeSNic) of composition Cu(2-MeSNic)2(MeNia)(2).4H2O (where MeNia is N-methyl-nicotinamide), Cu(2-MeSNic)2(Nia)(2).2H2O (where Nia is nicotinamide) and Cu(2-MeSNic)2L2 (where L is isonicotinamide (iNia) or ethyl nicotinate (EtNic)) are reported. Gram(-)-bacteria (Escherichia coli) are more resistant against Cu(II) complexes than Gram(+)-bacteria (Staphylococcus aureus)--significant antistaphylococcal activity was found with Cu(2-MeSNic)2(MeNia)(2).4H2O (IC50 1.3 mmol/L). Candida parapsilosis was most inhibited by Cu(2-MeSNic)2.H2O and Cu(2-MeSNic)2(MeNia)(2).4H2O (IC50 1.4 mmol/L and 1.5 mmol/L, respectively). Biosynthesis of nucleic acids influenced by Cu(2-MeSNic)2(Nia)(2).2H2O indicated by incorporation of 14C-adenine (IC50(Ade) 0.31 mmol/L) is more sensitive than biosynthesis of proteins indicated by incorporation of 14C-leucine (IC50(Leu) 9.94 mmol/L). Cu(II) complexes with expressed antimicrobial activity showed no mutagenic activity.

Anti-Bacterial Agents↗

PubMed2001

Novel oxindole derivatives and their biological activity.

The antifungal activity of fourteen novel derivatives of oxindole with side chain was studied using representatives of toxinogenic, phytopathogenic and dermatophytic filamentous fungi. Derivatives with exocyclic C=C bond in position C-3 exhibited a higher antifungal activity compared with derivatives with an exocyclic C-C bond in the same position. The strongest antifungal effects were shown by 3-(-2-thienoylmethylidene)-indol-2(3H)-ones.

Antifungal Agents↗

PubMed2001

Antibacterial and mutagenic activities of new isothiocyanate derivatives.

Nine newly synthesized isothiocyanate derivatives were demonstrated to posses antibacterial and genotoxic activities in vitro. 4-Hydroxybutyl isothiocyanate exhibited a broad antibacterial effect, with MIC values of 762 mumol/L for Staphylococcus aureus and Escherichia coli. Ethyl 4-methylsulfoxidobutanoate had the highest antibacterial activity in Gram-positive bacteria, the MIC value being 425 mumol/L for S. aureus. The highest tested concentrations of ethyl 4-isothiocyanatobutanoate and 4-hydroxybutyl isothiocyanate produced a bacteriocidal effect in Gram-positive bacteria. The compounds showed no mutagenic effects on Salmonella typhimurium tester strains TA 98 and TA 100, either in the absence or in the presence of a metabolically active microsomal S9 fraction from rat liver using standard Ames test.

Animals↗

PubMed2001

Biological activity of some 4-anilinoquinazolines: cytotoxic, genotoxic and antiprotease effects, induction of necrosis and changes of actin cytoskeleton.

Fourteen substituted 4-anilinoquinazolines have been tested for cytotoxic effect and structure activity relationships. The most active derivatives were substituted by chlorine or bromine group in the aromatic ring, in the pyrimidine ring by morpholine group and in the aniline skeleton by nitro group in position 4 or 2. Derivatives 6-bromo-2-(morpholin-1-yl)-4-(4'-nitroanilino)quinazoline, 6-bromo-2-morpholin-1-yl)-4-anilinoquinazoline, 2-(morpholin-1-yl)-4-(4'-bromoanilino)-quinazoline and 6-chloro-2-(morpholin-1-yl)-4-(4'-nitroanilino)quinazoline inhibited growth of tumor cell lines HeLa, B16 and L1210. Mutagenic data provided by Ames test showed, that the compounds 6-bromo-2-morpholin-1-yl)-4-anilinoquinazoline and 2-(morpholin-1-yl)- 4-(4'-bromoanilino)quinazoline did not exhibit the mutagenic effect, whereas the compounds 6-bromo-2-(morpholin-1-yl)-4-(4'-nitroanilino)quinazoline and 6-chloro-2-(morpholin-1-yl)-4-(4'-nitroanilino) quinazoline increased slightly the number of revertants of the strain TA 98 without metabolic activation. Concentration 26 micromol/L of 6-bromo-2-(morpholin-1-yl)-4-anilinoquinazoline induced necrosis of tumor cells B16. Concentration 5.2 micromol/l induced a significant increase of filamentous actin in the transformed HepG2 cells. Derivatives 6-bromo-2-(morpholin-1-yl)-4-(4'-nitroanilino)quinazoline, 6-bromo-2-morpholin-1-yl)-4-anilinoquinazoline, 2-(morpholin-1-yl)-4-(4'-bromoanilino)quinazoline and 6-chloro-2-(morpholin-1-yl)-4-(4'-nitroanilino)quinazoline exhibited antiprotease effect on plasmine. This results could be relevant for the anticancer properties of these compounds.

Animals↗

PubMed2001

[Cytotoxic and genotoxic activity of certain preservative agents in cosmetics].

Cytotoxic effects of the preservative compounds for cosmetics JMAC TD, Bronopol, CA 24, and Euxyl K100 were studied. Bronopol demonstrated the highest cytotoxic effect on the proliferation of V79 and VH10 fibroblast cell lines--the IC100 values being 10 mg/l during the whole experiment. The preservatives CA 24 and Euxyl K100 showed 4-times and 5-times smaller cytotoxic activity than Bronopol IC100 = 42 or 50.3 mg/l). The preservative compounds on silver chloride ions JMAC TD manifested the lowest cytotoxicity of the preservatives tested (IC100 = 150 mg/l); 15-times smaller than Bronopol, 3.5-times smaller than CA 24 and 3-times smaller than Euxyl K100. The biocide JMAC TD did not exhibit mutagenic effects on the bacteria Salmonella typhimurium TA 98 and TA 100.

Animals↗

PubMed1999

Cytotoxic and genotoxic effect of inhibitor of vulcanisation N-cyclohexylthiophthalimide in a battery of in vitro assays.

Mutagenicity of N-cyclohexylthiophthalimide (Duslin P) was tested first by the Ames test in the bacteria, Salmonella typhimurium. The negative results of the Ames test suggested that this compound does not induce mutations in the genome of S. typhimurium under the conditions used. To estimate the cytotoxicity of Duslin P to human cells, we measured cellular DNA and protein as well as cell proliferation, i.e., the mitotic index of treated and control cells. The genotoxic effects were assayed by two biochemical methods developed for detection of single-strand breaks of DNA in mammalian cells, i.e., by the alkaline single cell gel electrophoresis (comet assay) and by the DNA unwinding method, respectively. The DNA unwinding method showed that this compound did not induce DNA damage at concentrations < 7 micrograms/ml. Alkaline single cell gel electrophoresis revealed approximately double the level of DNA damage (in comparison to untreated control DNA) at a concentration of 2 micrograms/ml, which reduced proliferation to approximately 30%, and triple the level of DNA damage at higher concentrations (6 and 7 micrograms/ml), which inhibited completely both DNA synthesis and proteosynthesis. Cells with moderately damaged DNA were more common than cells with heavily damaged DNA. Parallel experiments with the strong mutagen and carcinogen MNNG showed that MNNG induced in cells a high level of DNA damage at concentrations which did not reduce the mitotic index or proteosynthesis, while DNA synthesis inhibited only partially. After treatment with MNNG, cells with heavily damaged DNA were more common than cells with moderately damaged DNA. Duslin P-treated VH10 cells were also tested cytogenetically, confirming that Duslin P induced neither chromosomal aberrations nor aneuploidy. We conclude that Duslin P has no mutagenic effect on bacteria, does not induce chromosomal aberrations and CREST positive or CREST negative micronuclei in human cells and induces only a small increase of DNA damage in human cells which is consistent with DNA fragmentation due to cell death.

Animals↗