T. M. Lachowicz

Properties of Binuclear Rhodium(II) Complexes and Their Antibacterial Activity.

Binuclear rhodium(II) complexes [Rh2Cl2(μ-OOCR)2(N-N)2], [Rh2(μ-OOCR)2(N-N)2(H2O)2](RCOO)2 and [Rh2Cl2(μ-OOCCH3)(terpy)2](H3O)Cl2.9H2O (R = H, Me, Bun, ph, PhCHOH; N-N = 2,2′-bipyridine (bpy), 1,10-phenanthroline (phen), 2,9-dimethyl-1,10-phenanthroline (dmp) and 6,7-dimethyl-2,3- di(2-pyridyl)quinoxaline (dmpq); terpy 2,2′:6′,2′′-terpyridine) have been synthesized and their structure and properties have been studied by electronic, IR and 1H NMR spectroscopy. Antibacterial activity of these complexes against Staphylococcus aureus and Escherichia coli has been investigated. The most active antibacterial agents against S. aureus were [Rh2(OOCPh)2(phen)2(H2O)2]2+, [Rh2(OOCPh)2(dmpq)2(H2O)2]2+, [Rh2(OOCBu)2(phen)2(H2O)2]2+ and [Rh2-(OOCBu)2(bpy)2(H2O)2]2+ which were considerably more active than the appropriate nitrogen ligands. The complexes show rather low activity against E. coli.

DL-leucine transport in aSaccharomyces cerevisiae mutant resistant to quaternary ammonium salts

Conclusions1.Quaternary ammonium salts seem to be potent inhibitors of amino acid uptake inS. cerevisiae.2.Inhibition is the strongest in yeast with derepressed transport (growth in Yeast Carbon Base medium with proline as the sole nitrogen source).3.The single-gene resistance to quaternary ammonium salts leads to lowering of transport inhibition.

Aminoethyl esters of fatty acids as model lysosomotropic substances.

Conclusions1.The activity of the DM-n compounds is chain length and pH dependent; the highest activity being observed for 11–13 carbon atoms chain.2.The highest biological activity was observed at pH above 7, which is characteristic for lysosomotropic agents.3.Hemolytic experiments conformed the lysosomotropic character of DM-n. The free amine (DMF-11) can pass through membranes and at lower pH can interact with the vacuolar membrane.4.In yeast, DM-n mobilized respiration of endogenous substrates.5.In yeast protoplasts treated with DM-n, temporary increase in Ca2+ uptake (characteristic for apoptosis) takes place. This indicates that the compounds have a killing effect.

N-substituted aminoethylesters of fatty acid as lysosomotropic substances

[1] SUBIK J., KOLAROV J., KOVA(~ L.: BiochemBiophys.Res.Commun. 49, 192-198 (1972). [2] HAPALA 1.: Biochem.Biophys.Res.Commun. 159, 612-617 (1989). [3] HAPALA I., HUNAKOVA A., GERZANIt~OVA G., BUTKO P.: Biochim.Biophys.Acta 1190, 40-42 (1994). [4] DRGO~q T., ~ABOVA L., NELSON N., KOLAROV J.: FEBS Lett. 289, 159-162 (1991). [5l HAPALA 1,, HUNAKOVA A.: Folia Microbiol. 41, 95-96 (1996). [6] ZINSER E., PALTAUF F., DAUM G.: J.Bacteriol. 175, 2853-2858 (1993).

Plasma membrane H+-ATPase activity in wild type and mutants ofSaccharomyces cerevisiae treated by some lysosomotropic drugs

Conclusions(1)The aminoesters inhibit glucose-stimulated proton extrusion by yeast cells.(2)The inhibitory activity depends on aliphatic carbon chain length.(3)The inhibition of proton extrusion is concentration-dependent.(4)The aminoesters stimulate quinacrine accumulation in vacuoles of yeast cells so they should possess affinities for lysosomes.

Functionalized Permeatoxins: Derivatives of Dihydrocinnamic Acid with Antioxidant Function

[1] OBLAtK E., LACHOWlCZ T.M., WITEK S.: Folia Microbiol. 41, 116-118 (1996). [2] LACHOW1CZ T.M., WITEK S., LUCZY?;/SKI J., WITKOWSKA R., KLESZCZYlqSKA H., PRZESTALSK1 S.: Folia Microbiol. 42, 231-232 (1997). [3] GOFFEAU A., AMORY A., DUFOUR J.P.: Methods in Enzymology 157, 513-528 (1988). [4] GOFFEAU A., SLAYMAN C.W.: Biochem.Biophys.Acta 639, 197-223 (1981). [5] GALZY P., SLONIMSKI P.P.: C.R.Acad.Sci. 245, 2556-2559 (1957).