<abstract><title style='display:none'>Abstract</title> The skin barrier, which is essential for human survival on dry land, is located in the uppermost skin layer, the stratum corneum. The stratum corneum consists of corneocytes surrounded by multilamellar lipid membranes that prevent excessive water loss from the body and entrance of undesired substances from the environment. To ensure this protective function, the composition and organization of the lipid membranes is highly specialized. The major skin barrier lipids are ceramides, fatty acids and cholesterol in an approximately equimolar ratio. With hundreds of molecular species of ceramide, skin barrier lipids are a highly complex mixture that complicate the investigation of its behaviour. In this minireview, the structures of the major skin barrier lipids, formation of the stratum corneum lipid membranes and their molecular organization are described.</abstract>

Ceramides in the skin barrier

<abstract><title style='display:none'>Abstract</title>Syrian oregano (<italic>Origanum syriacum </italic>L., Lamiaceae) is a very popular culinary herb that has been used through the ages in traditional medicine mainly in Lebanon and the Arab world. The subject of this study was the microscopic analysis of the herbal drug Origani syriaci folium, as well as the chemical analysis of its essential oil components. Plant materials originated from Arabsalim - South Lebanon and were collected in 2010. The presence of very dense clusters of multicellular covering trichomes (510 μm × 18.47 μm) and peltate secretory glands (∅ 87.95 μm) with eight cells were observed. The essential oil of Origani syriaci folium was isolated and quantified using hydrodistillation according to SPhC 1997. The content of essential oil was 95 ml/1000 g, i.e. 9.5% (V/m). The volatile constituents of Origani syriaci folium were qualitatively and quantitatively evaluated using SPME GC/MS. The two dominant constituents identified in Syrian oregano leaves were carvacrol (78.4%) and thymol (17.9%).</abstract>

Comenius University in Bratislava, Faculty of Pharmacy, Department of Pharmacognosy and Botany

Semmelweis University, Faculty of Pharmacy, Department of Pharmacognosy Budapest

Analysis of the Essential Oil Compounds of Origanum Syriacum L.

<abstract><title style='display:none'>Abstract</title>Mentha × piperita (L.) Huds. of the family Lamiaceae is a very important species for commercial exploitation due to the high
content of essential oil. Besides the essential oils, there are also other significant secondary metabolites in peppermint, especially
flavonoids and hydroxycinnamic derivatives. In this study, we evaluate the variability of essential oil constituents and of phenolic
compounds in the leaves of M. × piperita during the development of inflorescence. Similar studies, dealing with the variation of the
essential oils and its composition, have been performed in the past, but no attention was paid to the variation of other secondary
metabolites. We examined M. × piperita cv. ‘Perpeta’, the domestic cultivar. The plants were cultivated in the climatic conditions
of south-west Slovakia. The contents of secondary metabolites were investigated in the week periods, from the beginning of
inflorescence formation to the end of flowering. The yield and the quality of essential oil have been carried out by distillation and
gas chromatography mass spectrometry (GC-MS). The phenolic substances were analysed using spectrophotometric methods
according to European Pharmacopoeia. The highest contents of phenolic substances have been found in leaves of plants during
the flowering phenophase, the same stage when essential oil of mint also achieves the highest quality.</abstract>

Comenius University in Bratislava, Faculty of Pharmacy, Departments of
Pharmacognosy and Botany, Slovakia

University of Veterinary and Pharmaceutical Sciences Brno, Faculty of
Pharmacy, Department of Natural Drugs, Czech Republic

The variability of secondary metabolites in mentha × piperita
cv . ‘perpeta’ during the development of inflorescence

<abstract><title style='display:none'>Abstract</title>Hypomethylating agent decitabine is being used in the treatment of certain types of leukaemia in combination with other anticancer drugs. Aberrant DNA methylation has been suggested to occur in pathological states including depression. Scarce data in male rats suggest antidepressant effects of decitabine. The main aim of our studies is to test the hypothesis that the inhibition of DNA methylation results in antidepressant effects in female rats. Before doing so, we decided to verify the effects of decitabine on DNA methylation in females. The findings demonstrate that the treatment with decitabine at the dose shown previously to inhibit DNA methylation in males, had no effect on total DNA methylation in two brain regions, namely the hippocampus and frontal cortex of female rats. In conclusion, the present study allows us to suggest that the effect of decitabine on DNA methylation in the brain is sex dependent.</abstract>

Total DNA methylation in the brain in response to decitabine treatment in female rats

Presentations

<abstract xml:lang="en"><title style='display:none'>Contribution to the TLC separation of ursolic and oleanolic acid mixture</title>The aim of the study was to develop a rapid, simple, effective and reproducible TLC method for separation of a naturally occurring mixture of ursolic and oleanolic acids. Because of the similarity of chemical structures, <italic>in situ</italic> derivatisation by iodine was necessary to separate these triterpenic acids. Separation was achieved on silica gel plates. After derivatisation, a chromatographic plate was developed with the mobile phase consisting of light petrol, ethyl acetate and acetone (8.2:1.8:0.1, v/v/v) following visualisation by spraying with sulphuric acid in diethylether (25%, v/v) and heating to 120°C for 5 min. The method used enabled chromatographical differentiation of ursolic and oleanolic acid mixtures in all tested mutual ratios.</abstract>

Contribution to the TLC separation of ursolic and oleanolic acid mixture

<abstract>
<title style='display:none'>Abstract</title>
<sec><title style='display:none'>Aim</title>
The present study was aimed at preparing stable dry adsorbed nanoparticles (DANs) of olanzapine (OLZ) loaded solid lipid nanoparticles (SLNs) for sustained release.
</sec>
<sec><title style='display:none'>Materials/methods</title>
OLZ SLNs were prepared by hot melt emulsification and ultrasonication using Precirol ATO 5 (PRE) as a solid lipid, combination of Kolliphor ELP (KELP) and Tween 80 (T80) as surfactants, after optimising formulation and process variables. The SLN system was subjected to evaluation of particle size, zeta potential, entrapment efficiency (EE), <italic>in-vitro</italic> drug release and <italic>ex-vivo</italic> intestinal permeability studies using the chicken intestinal segments (jejunum). Further, these SLNs were converted into stable DANs by adsorbing onto a Neusilin US2 (NUS2) and Avicel CL 611 (ACL) carriers using the granulation-evaporative drying method. The DANs were characterised for redispersion properties, <italic>in-vitro</italic> drug release, thermal behaviour, crystallinity, and morphology.
</sec>
<sec><title style='display:none'>Results</title>
The SLN and DAN had a particle size of 238.0 nm [0.274 polydispersity index (PdI)] and 302.4 [0.494 PdI] respectively. The zeta potentials of SLN and DAN were found to be −29.3 mV and −26.3 mV, respectively. The SLN had 67% EE, and showed a sustained drug release in various media. The highest permeability of SLNs was observed in <italic>ex-vivo</italic> permeation model compared to the OLZ suspension, indicating that SLNs have the potential to bypass hepatic metabolism. The adsorption of SLNs onto carriers was confirmed by surface morphology. The DAN had good flow properties and sustained drug release similar to that of SLNs. The X-ray diffraction (XRD) patterns and endothermic peaks confirmed the complete encapsulation of actives in lipid matrices.
</sec>
<sec><title style='display:none'>Conclusion</title>
The encapsulating of OLZ in SLNs and converting it into DAN showed a sustained release and adsorption technique that can be used for improving the stability of NLC dispersion. The DANs can be offered in dosage forms such as filling into sachets, capsules and compressed into tablets.
</sec>
</abstract>

Formulation development, in-vitro and ex-vivo evaluation of dry adsorbed solid lipid nanoparticles: an approach of overcoming olanzapine drawbacks

<abstract>
<title style='display:none'>Abstract</title>
Metal complexes, which, under physiologic conditions, show redox properties and are able to bind to DNA, are great tools to cleave the DNA chain. This aspect is of great importance for their use as antineoplastic drugs. We synthesized ligands derived from short-chain amino acids and from salicylaldehyde. The prepared ligands of the type of reduced Schiff bases were subsequently used for the preparation of copper(II) complexes. The aim of the study was in vitro testing of copper(II) complexes, where it was confirmed that they are capable of cleaving DNA. Their cytotoxic activity was also confirmed by the resazurin redox method on Saccharomyces cerevisiae based on preserved healthy mitochondrial function.
</abstract>

DNA Cleavage and Cytotoxic Activity of Copper(II) Complexes Based on Reduced Schiff Bases Derived From Salicylaldehyde and Amino Acids

<abstract>
<title style='display:none'>Abstract</title>
Mushrooms from the genus <italic>Cordyceps</italic> are characterized by a wide range of biological effects due to the diverse amount of substances contained in them and are an important source of bioactive compounds. In China, mushrooms of the genus <italic>Cordyceps</italic> have been used as a medicinal preparation of traditional Chinese medicine for centuries. So far, a considerable number of studies have been conducted that focused on analyzing the effects of <italic>Cordyceps</italic>, which include their antioxidant, antibacterial, immunomodulatory, antidiabetic, antitumor, and many other effects. The ability of fungi to form complexes with various metals is also interesting. It is believed that polysaccharides are the main component of the extracts involved in the complexation with metals, after which their biological effects are improved and deepened. The work deals with the comparison of the antioxidant and antibacterial effects of <italic>Cordyceps</italic> extracts with extracts of this mushroom enriched with silver ions. Based on scientific studies, it is assumed that there is a complexation between the chemical compounds of the extracts and silver.
</abstract>

Medicinal Mushrooms Cordyceps as a New Source of Bioactive Compounds and Their Complexation With Silver Ions

<abstract>
<title style='display:none'>Abstract</title>
Aminopeptidase N (APN) is a broad specificity zinc metallopeptidase with many functions that do not always depend on its enzymatic activity. Among others, it is involved in tumor angiogenesis and metastasizing and also serves as a cellular receptor of some coronaviruses. Some APN inhibitors, such as bestatin or tosedostat, were used or tested as anticancer drugs in the past. Within the past two decades, we have prepared several series of potential APN inhibitors. Some of them reached interesting values of inhibitory activity and were also successfully tested for antiproliferation activity in cancer cell lines. We also performed some QSAR studies with APN inhibitors prepared by us and other authors.
</abstract>

Aminopeptidase N as a potential drug target

Book of Abstracts 51st Conference Synthesis and Analysis of Drugs (SAD 2023) Oral Presentations

Book of Abstracts 51st Conference Synthesis and Analysis of Drugs (SAD 2023) Poster Session

<abstract>
<title style='display:none'>Abstract</title>
Primaquine (PQ) has long been recognized as the only effective drug in the treatment of hepatic stage malaria. However, severe toxicity limits its therapeutical application. Combining PQ with chloroquine (CQ) has been reported as enhancing the former’s efficacy, while simultaneously reducing its toxicity. In this study, the optimal conditions for encapsulating PQ-CQ in liposome, including incubation time, temperature and drug to lipid ratio, were identified. Furthermore, the effect of the loading combination of these two drugs on liposomal characteristics and the drug released from liposome was evaluated. Liposome is composed of HSPC, cholesterol and DSPE-mPEG2000 at a molar ratio of 55:40:5 and the drugs were loaded by means of the transmembrane pH gradient method. The particle size, ζ-potential and drug encapsulation efficiency were subsequently evaluated. The results showed that all liposome was produced with a similar particle size and ζ -potential. PQ and CQ could be optimally loaded into liposome by incubating the mixtures at 60°C for 20 minutes at a respective drug to lipid ratio of 1:3 for PQ and CQ. However, compared to single drug loading, dual-loading of PQ+CQ into liposome resulted in lower drug encapsulation and slower drug release. In conclusion, PQ and CQ can be jointly loaded into liposome with differing profiles of encapsulation and drug release.
</abstract>

Dual Loading Of Primaquine And Chloroquine Into Liposome

<abstract><title style='display:none'>Abstract</title> Aim: Patient-oriented pharmaceutical care in pharmacies could improve patient satisfaction and influence patient’s choice of a community pharmacy. The aim of the work was to assess patient satisfaction and attendance in community pharmacies in Slovakia. Methods: A self-administered, anonymous questionnaire was distributed to patients visiting 33 community pharmacies in a total of 23 Slovak cities during October-December 2013. The questionnaire contained 29 items and three dimensions were supposed (managing therapy, interpersonal relationship, general satisfaction). A 5-point Likert-type scale (1 = very satisfied, 2 = satisfied, 3 = neither satisfied nor dissatisfied, 4 = dissatisfied, 5 = very dissatisfied) was used for assessing patient satisfaction. The results are presented in percentages and by the level of satisfaction within the range: high satisfaction (score 1.00-2.50), moderate satisfaction (score 2.51-3.50) and low satisfaction (score 3.51-5.00). Reasons for attendance in the community pharmacy and factors influencing pharmacy choice were evaluated either. Results: A total 2 844 respondents were included into the survey. Patient satisfaction with pharmaceutical care achieved high satisfaction level: interpersonal relationship (1.85 ± 0.598; 86.7% highly satisfied respondents) and general satisfaction (2.02 ± 0.643; 71.3% highly satisfied respondents). Managing therapy scored lower (2.24 ± 0.704; 65.4% highly satisfied respondents). The most frequently reported reasons for attending community pharmacy were to obtain prescription (70.4%) and over-the-counter medications (70.4%). The patient choice of a particular pharmacy was influenced by its location (74.1%). Conclusion: This study presents the first nationwide patientreported outcomes about patient satisfaction and attendance in community pharmacies in Slovakia. Future development and advancement of pharmacy practice leading to higher patient satisfaction requires modification of community pharmacists’ professional behaviour in Slovakia namely in managing therapy of patients.</abstract>

The Assessment of Patient Satisfaction and Attendance of Community Pharmacies in Slovakia

<abstract><title style='display:none'>Abstract</title> The neuroprotective or neurotoxic effects of the products of the kynurenine pathway of tryptophan metabolism highly depend on the action of kynurenine-3-monooxygenase (KMO). The present results show increased concentrations of the KMO in the plasma of rats repeatedly exposed to an immune challenge. Increased concentrations of this key enzyme are likely to cause a shift of kynurenine pathway towards enhanced production of neurotoxic metabolites. </abstract>

Slovak Academy of Sciences, Institute of Experimental Pharmacology and Toxicology, Bratislava

Comenius University Bratislava, Jessenius Faculty of Medicine in Martin, Department of Pharmacology, BioMed, Martin,

Slovak Academy of Sciences, Institute of Experimental Pharmacology and Toxicology, Bratislava,

Comenius University in Bratislava, Faculty of Pharmacy, Department of Galenic Pharmacy, Bratislava,

Evaluation of the effect of carnosine, its novel derivative trolox-carnosine and trolox in a pre-clinical study focussing on the regulation of immunity

<abstract><title style='display:none'>Abstract</title>Present research is oriented on the synthesis of some novel 12-(<italic>N</italic>-arylmethaniminyl)indolo[1,2-<italic>c</italic>]quinazoline analogs (4b1–4b11) and their characterization by 1H NMR, 13C NMR, FTIR and mass spectrophotometry. Their free radical scavenging activity and antibacterial potential were also evaluated. Many derivatives have shown a marked free radical scavenging capacity in all the concentrations but specifically compounds 4b7, 4b8 and 4b11 have shown good antioxidant potential with an IC50 value of 25.18 μmol/L, 28.09 μmol/L &amp; 44.22 μmol/L, respectively (DPPH method) and 39.46 μmol/L, 44.47 μmol/L &amp; 35.61 μmol/L, respectively (H2O2 method). The antibacterial evaluation was carried out against <italic>B. subtilis</italic> and <italic>E. coli</italic> by agar well diffusion method and it revealed that all the compounds in the series were having marked antibacterial activity but compounds 4b9 and 4b11 have shown best antibacterial potential. Then, it was concluded that the derivatives which were containing substituted anilines (4-Nitro, 4-Fluoro, 4-Bromo &amp; 4-Chloro-2-nitro) on the carbon attached on the 12th position of indoloquinazoline moiety were having marked potential as an antibacterial and free radical scavenger.</abstract>

Synthesis, antibacterial and free radical scavenging activity of some newer <italic>N</italic>-((10-nitro-1<italic>H</italic>-indolo [1, 2-c]quinazolin-12-yl)methylene)benzenamines

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Acta Facultatis Pharmaceuticae Universitatis Comenianae (formerly)

  Formerly Acta Facultatis Pharmaceuticae Universitatis Comenianae.  All areas of pharmaceutical and related sciences.  Original research articles....

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  Formerly Acta Facultatis Pharmaceuticae Universitatis Comenianae.  All areas of pharmaceutical and related sciences. ...

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