The influence of retinol concentration in liquid crystal formula on epidermal growth factor, interleukin-6 and transglutaminase-1 mRNA expression in the epidermis.

Topical retinol application effectively reduces the effects of photoaging and improves skin condition, e.g. influences the process of keratinization of the epidermis, which improves stratum corneum structure and reduces transepidermal water loss. However, cosmetics use lower concentrations of retinol, which has been associated with emerging hypersensitivity reactions as well as redness and irritation of the skin. The question arises whether the vehicle used in the cosmetic may be important in stimulating the inflammatory reaction in the skin and if the concentration of retinol used could significantly affects the growth of epidermal cells. The aim of this study was to evaluate the effects of different concentrations of liquid crystal retinol (0.15%, 0.3% and 0.5%) on the clinical and histological characteristics of a reconstructed epidermis skin model. It also compares the effectiveness of 0.3% retinol formula in liquid crystal to that in lipid. The study used reconstructed human epidermis tissue containing normal human keratinocytes. Four original formulas containing retinol were tested: 0.15%, 0.3% and 0.5% with a liquid crystal base, and 0.3% with a lipid base. Interleukin 6 (IL-6), transglutaminase-1 (TGM1), and epidermal growth factor (EGF) mRNA expression was measured expression of the skin-equivalent tissue for 10 days of exposure. Histopathological analysis and mRNA quantification were performed. Gene expression was analyzed by total mRNA extraction. All liquid crystal formulas induced higher EGF mRNA expression than lipid base formula. IL-6 expression did not differ significantly from the DPBS reference values. Interestingly, TGM1 expression was found to increase together with increasing retinol concentration (0.15%, 0.3%, 0.5%). Histological examination revealed changes in epidermal structure, mainly hyperkeratinization of the stratum corneum. Our results support the hypothesis liquid crystal formula might be regarded as more beneficial since it inducess less pro-inflammatory action manifested by lowered expression IL-6. In addition, EGF expression was found to correlate significantly with the retinol concentration of the liquid crystal formula: 0.5% > 0.3% > 0.15% (P < 0.05). Lower concentrations may increase TGM1 expression, thus enhancing the formation of a protective layer of cornified envelope.

Synthesis, structural characterization, antimicrobial and cytotoxic effects of aziridine, 2-aminoethylaziridine and azirine complexes of copper(II) and palladium(II).

The synthesis, spectroscopic and X-ray structural characterization of copper(II) and palladium(II) complexes with aziridine ligands as 2-dimethylaziridine HNCH(2)CMe(2) (a), the bidentate N-(2-aminoethyl)aziridines C(2)H(4)NC(2)H(4)NH(2) (b) or CH(2)CMe(2)NCH(2)CMe(2)NH(2) (c) as well as the unsaturated azirine NCH(2)CPh (d) are reported. Cleavage of the cyclometallated Pd(II) dimer [µ-Cl(C(6)H(4)CHMeNMe(2)-C,N)Pd](2) with ligand a yielded compound [Cl(NHCH(2)CMe(2))(C(6)H(4)CHMe(2)NMe(2)-C,N)Pd] (1a). The reaction of the aziridine complex trans-[Cl(2)Pd(HNC(2)H(4))(2)] with an excess of aziridine in the presence of AgOTf gave the ionic chelate complex trans-[(C(2)H(4)NC(2)H(4)NH(2)-N,N')(2)Pd](OTf)(2) (2b) which contains the new ligand b formed by an unexpected insertion and ring opening reaction of two aziridines ("aziridine dimerization"). CuCl(2) reacted in pure HNC(2)H(4) or HNCH(2)CMe(2) (b) again by "dimerization" to give the tris-chelated ionic complex [Cu(C(2)H(4)NC(2)H(4)NH(2)-N,N')(3)]Cl(2) (3b) or the bis-chelated complex [CuCl(C(2)H(2)Me(2)NC(2)H(2)Me(2)NH(2)-N,N')(2)]Cl (4c). By addition of 2H-3-phenylazirine (d) to PdCl(2), trans-[Cl(2)Pd(NCH(2)CPh)(2)] (5d) was formed. All new compounds were characterized by NMR, IR and mass spectra and also by X-ray structure analyses (except 3b). Additionally the cytotoxic effects of these complexes were examined on HL-60 and NALM-6 human leukemia cells and melanoma WM-115 cells. The antimicrobial activity was also determined. The growth of Gram-positive bacterial strains (S. aureus, S. epidermidis, E. faecalis) was inhibited by almost all tested complexes at the concentrations of 37.5-300.0 µg mL(-1). However, MIC values of complexes obtained for Gram-negative E. coli and P. aeruginosa, as well as for C. albicans yeast, mostly exceeded 300 µg mL(-1). The highest antibacterial activity was achieved by complexes 1a and 2b. Complex 2b also inhibited the growth of Gram-negative bacteria.

Investigations on benz[1,2]oxaphosphinane derivatives.

The structures of two compounds, 3-[1-(2-hydroxyethylamino)ethylidene]-2-methoxy-3,4-dihydro-1,2lambda(5)-benzoxaphosphinane-2,4-dione, C(13)H(16)NO(5)P, and 3-[1-(2-hydroxy-ethylamino)ethylidene]-2-methoxy-6-methyl-3,4-dihydro-1,2lambda(5)-benzoxaphosphinane-2,4-dione, C(14)H(18)NO(5)P, have been studied and compared. The oxophosphinane rings have a half-chair conformation and extra six- and five-membered rings are formed by intramolecular N-H...O hydrogen bonds. An intermolecular O-H...O hydrogen bond is also observed.

Synthesis, antimicrobial, and alkylating properties of 3-phosphonic derivatives of chromone.

Dimethyl 2,6-dimethyl-4-oxo-4H-chromen-3-yl-phosphonate (1a) and dimethyl 6-methyl-2-phenyl-4-oxo-4H-chromen-3-yl-phosphonate (1b) were synthesized and reacted with primary aliphatic amines to yield title compounds 4-6. Their antibacterial properties against Gram-positive and Gram-negative bacteria strains were tested by the MIC method. Four of seventeen tested compounds (1d, 3, 4a, and 4b) exhibit detectable activity against S. aureus. Some representative examples of newly synthesized compounds were tested for their alkylating properties in vitro in the Preussmann test. Compounds 1a, 1c, 1d, 3, 5d, and 6a possess highly alkylating activity toward standard derivative 4-(4'-nitrobenzyl)pyridine (NBP).

Synthesis and action on the central nervous system of 9,10-dihydropyrrolo [3,4-b][1,4]benzoxazepine derivatives.

The synthesis of tricyclic system ring, 9,10-dihydropyrrolo[3,4-b] [1,4]benzoxazepine, and its derivatives is described. Some of the chemical and pharmacological properties of these compounds are also reported.

[Synthesis and pharmacologic examination of derivatives of benzoxazaphosphoryl-4-one and 2-phenyl-10-methyl-3a-triethoxyphosphone-1H,2,3,9,10-tetrahydropyrrolo [3,4-b][1,4]benzoxazepine-1,3,9-trione]. / Synteza i badania farmakologiczne pochodnych benzoksazafosforyno-4-on i 2-fenylo-10-metylo-3a-trietoksyfosfonio-1H,2,3,9,10-tetrahydropirolo [3,4-b][1,4] benzoksazepino-1,3,9-trionu.

A series of N-derivatives of 2-phenyl-2,3-dihydro-1,3,2(lambda 5)- benzoxazaphosphoryl-4-one and 2-phenyl-10-methyl-3a-triethoxyphosphonio- 1H,2,3,9,10-tetrahydropyrrolo[3,4-b]([1,4]benzoxazepine-1,3,9-trio ne have been prepared. The pharmacological investigation of the above mentioned compounds shows antitumor action against leukaemia in the case of three N-derivatives.