Volumen 66 (2019): Edición 2 (November 2019)

Valproic acid, beside its anticonvulsant action, is widely used as a mood stabilizer in the therapy of bipolar disorder. The potential antidepressant action of valproic acid has not been sufficiently characterized so far. The aim of the present study was to evaluate the antidepressant effect of valproic acid in an aldosterone model of depression. Subchronic treatment with valproic acid resulted in a reduction of the time spent in immobility in the forced swim test. In conclusion, the present study provides evidence on antidepressant effects of valproic acid using a classical behavioral approach for testing the efficacy of antidepressant drug in animal models.

The goal of the present study is to prepare a stable, multiple-unit, extended-release dosage form containing oxycodone pellets coated with aqueous ethylcellulose (EC) dispersion, Surelease E-7-19050. The application of 18% w/w of EC leads to the similar drug release with the hydrophobic, non-swelling, matrix reference product containing 20 mg of oxycodone. Increasing the compression force to 9 kN and including more than 50% w/w of oxycodone pellets into the formulation resulted in faster drug release, indicating the damaging to the EC film coating. The physical appearance of the final formulation, assay of oxycodone, moisture content, and dissolution data over the stability period showed that the multiple-unit pellet system (MUPS) is efficient for the production of highly stable product.

Resveratrol and caffeic acid belong to plant polyphenols and are known for their antioxidant effects. The aim of our research was to study their impact on Maillard reaction. This one occurs when the reducing saccharides react with amino groups of biomolecules including proteins, alter their protein conformation and transform to the variety of advanced glycation end products (AGEs). AGEs exhibit browning and generate fluorescence. There exist expectations that this oxidative protein glycosylation could be prevented by antioxidants. In this study, we incubated bovine serum albumin (BSA) with glucose for 7 days at 37°C and measured characteristic fluorescence and UV absorbance of the formed AGEs. Surprisingly, resveratrol and caffeic acid enhanced transformation of BSA to glycation products, which was confirmed either when cupric Cu(II) or ferric Fe(III) ions in nanomolar concentration were added to the system as pro-oxidant agent.

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.

Trees and shrubs of the genus Cordia are widely distributed in the warmer regions, including Indonesia. The aim of this study was to evaluate the analgesic and anti-inflammatory properties of the ethanolic extract of plant leaves in Wistar albino rats. The analgesic activity was evaluated using the hot plate method and acetic acid-induced writhing, and the anti-inflammatory activity was determined using carrageenan-induced paw oedema. The results showed that the Cordia sebestena ethanol extract (100, 200 and 400 mg/kg) exhibited significant analgesic effects in a dose-dependent manner in the two pain models tested. The extract also exhibited significant anti-inflammatory effects in the carrageenan-induced inflammation test. The data obtained support the traditional folklore therapeutic claim about its analgesic and anti-inflammatory properties. Nonetheless, further scientific investigation is required to establish its analgesic and anti-inflammatory properties in other experimental models and clinical settings.

Physiological functions of cardiovascular system (CVS) are exhibiting circadian patterns regulated by complex system of endogenous factors. Preserving this rhythmicity is important for its normal function, whereas disturbing the synchronization with natural day–night cycle can increase the risk of cardiovascular damage. Cardiovascular pathophysiology also follows cyclic variation; time susceptibility and period with maximum risk associated with elevated blood pressure (BP) can be predicted. Given this rhythmic nature, significant changes in efficacy between morning and evening administration of the drug may occur; appropriate timing of pharmacological intervention in therapy of hypertension may affect the efficacy of the treatment.

The volume-sensitive outwardly rectifying anion channel (VSOR) is a key component of volume regulation system critical for cell survival in non-isosmotic conditions. The aim of the present study was to test the effects of four tannin extracts with defined compositions on cell volume regulation and VSOR. Preparation I (98% of hydrolysable tannins isolated from leaves of sumac Rhus typhina L.) and Preparation II (100% of hydrolysable tannins isolated from leaves of broadleaf plantain Plantago major L) completely and irreversibly abolished swelling-activated VSOR currents in HCT116 cells. Both preparations profoundly suppressed the volume regulation in thymocytes with half-maximal effects of 40.9 μg/ml and 12.3 μg/ml, respectively. The inhibition was more efficient at lower concentrations but reverted at higher doses due to possible non-specific membrane-permeabilizing activity. Preparations III and IV (54,7% and 54.3% of hydrolysable tannins isolated, respectively, from roots and aboveground parts of Fergana spurge Euphorbia ferganensis B.Fedtch) inhibited VSOR activity in a partially reversible manner and suppressed the volume regulation with substantially higher half-maximal doses of 270 and 278 μg/ml, respectively, with no secondary reversion at higher doses. Hydrolysable tannins represent a novel class of VSOR channel inhibitors with the capacity to suppress the cell volume regulation machinery.

It was known that hawthorn - Crataegus L. is a polymorphic genus. Two hawthorn species and their hybrids are included in the European Pharmacopoeia, twelve – in Ukrainian pharmacopoeia. Determination of chromatographic profiles of hawthorn fruits species native to Ukraine and other countries that are non-pharmacopoeial, but have sufficient plant raw material base, is essential for quality control of drugs.

Aim. To analyze and compare the chromatographic profiles of fruits of 23 Crataegus L. species on phenolic compounds, evaluated by means of high-performance thin-layer chromatography procedure (HPTLC), and determine the specific features of chromatographic fingerprints.

Materials and Methods. A total of 39 samples of fruits of 23 hawthorn species that are native to Europe, Asia and North America, such as Crataegus monogyna, C. laevigata/C. oxyacantha, C. leiomonogyna, C. curvisepala, C. pseudokyrtostyla, C. fallacina, C. subrotunda, C. ambigua, C. pentagyna, C. sanguinea, C. chlorosarca, C. almaatensis, C.pseudoheterophylla subsp. turkestanica, C. pinnatifida, C. pentagyna subsp. pseudomelanocarpa, C. punctata, C. pringlei, C. festiva, C. douglasii, C. holmesiana, C. submollis, C. flabellata, C. canadensis were investigated. The analysis has been done following the TLC method from European Pharmacopeia modified into HPTLC, using automated HPTLC herbal system (CAMAG, Switzerland).

The results have shown that chromatographic profiles of phenolic constituents of nine Crataegus L. species of Europe, both pharmacopoeial and non-pharmacopoeial, were quite similar, despite the significant morphological distinctions. The chromatographical profiles of three species of Asia were similar to the pharmacopoeial species; three other species looked different and had specific marker zones. In addition, eight Crataegus L. species of North America had specific markers helping for discriminative analysis from pharmacopoeial species.

Conclusion. The findings could help to identify the possible adulterations and prevent the falsification of finished products. The results will be taken into consideration during revision of the Ukrainian national pharmacopoeial monograph for hawthorn fruits.