Photocatalytic degradation of some aqueous suspensions of propranolol

In this work, the photocatalytic degradation of Propranolol aqueous solutions of different concentrations was investigated in the presence of TiO2 and TiO2-MoO3 catalysts. Among the two photocatalysts used, the best performance can be attributed to the TiO2-MoO3 catalyst. Optimal reaction conditions were established: Ccat. = 2 g/L; CPropranolol. = 0,25 mM; V = 20 mL, lampe – sample distance = 10 cm, when the UV-A-induced photocatalytic oxidation over the Propranolol suspensions was able to degradate almost completely the studied drug. The speed of decomposition of Propranolol was accelerated when the process was carried out at a temperature of 50°C

The endothelial cell markers von Willebrand Factor (vWF), CD31 and CD34 are lost in glomerulonephritis and no longer correlate with the morphological indices of glomerular sclerosis, interstitial fibrosis, activity and chronicity.

Endothelial cells (ECs) are active participants of an inflammatory process in glomeruli. EC damage has been shown to play an important role in the progression of glomerulonephritis (GN). The degree of glomerular and peritubular capillary loss in models of progressive renal disease correlates with the severity of glomerulosclerosis and interstitial fibrosis. The aim of our study was to analyze the association of vWF, CD31 and CD34 immunoreactivity with the morphological indices of glomerular sclerosis, interstitial fibrosis, activity and chronicity in GN. A cross-sectional study of 22 patients with GN was conducted. Conventional stains (hematoxylin-eosin, periodic acid Schiff and Trichrome GĂśmĂśri stains) and immunohistochemistry (vWF, CD31 and CD34) were employed on kidney biopsies. Activity and chronicity of GN, as well as glomerular segmental sclerosis and interstitial fibrosis, were evaluated according to a scoring system initially used for lupus nephritis and antineutrophil-cytoplasmic-antibody-associated vasculitis. Immunohistochemistry was assessed using a semi-quantitative score. Statistical analysis was performed using EpiInfo 6.04. The mean patient age was 46.68+/-14.09; 14 patients were male, and eight were female. Performing Spearman's rank correlation test, no correlation was found between each marker and glomerular segmental sclerosis, interstitial fibrosis, activity and chronicity, which suggests a loss of these markers and microvasculature involvement

The Synergistic Biologic Activity of Oleanolic and Ursolic Acids in Complex with Hydroxypropyl-γ-Cyclodextrin

Oleanolic and ursolic acids are natural triterpenic compounds with pentacyclic cholesterol-like structures which gives them very low water solubility, a significant disadvantage in terms of bioavailability. We previously reported the synthesis of inclusion complexes between these acids and cyclodextrins, as well as their in vivo evaluation on chemically induced skin cancer experimental models. In this study the synergistic activity of the acid mixture included inside hydroxypropyl-gamma-cyclodextrin (HPGCD) was monitored using in vitro tests and in vivo skin cancer models. The coefficient of drug interaction (CDI) was used to characterize the interactions as synergism, additivity or antagonism. Our results revealed an increased antitumor activity for the mixture of the two triterpenic acids, both single and in complex with cyclodextrin, thus proving their complementary biologic activities

Albendazole-cyclodextrins binary systems : Thermal and spectral investigation on drug-excipient interaction

The aim of this study was to characterize the interaction between the binary systems of albendazole (ABZ)-cyclodextrins (CDs) with pharmaceutical excipients. Hydroxyl-propyl-beta-cyclodextrin (HPBCD) and random methyl-beta-cyclodextrin (RAMEB) were used as cyclodextrins and magnesium stearate, mannitol, polyvinylpyrrolidone K30 (PVP K30), colloidal silica, starch, and talc were used as excipients. The utilized investigation techniques were attenuated total reflection Fourier transform infrared spectroscopy (ATR-FTIR), powder X-ray diffractometry (PXRD) and thermoanalytical techniques: thermogravimetry (TG)/derivative thermogravimetry (DTG)/heat flow (HF) and differential scanning calorimetry (DSC). The ATR-FTIR analysis clearly suggested interactions under ambient conditions between ABZ-HPBCD with PVP K30 and SiO2 and between ABZ-RAMEB with SiO2 and talc. The PXRD patterns indicated the formation of less crystalline mixtures but with no clear indication of interactions, since no peaks appeared nor disappeared. The modifications on the DSC curves suggested an interaction between ABZ-HPBCD and PVP K30 and SiO2 respectively, and in case of ABZ-RAMEB was observed an interaction with talc. Thermal analysis (TG/DTG/HF) carried out in open crucibles in dynamic air atmosphere suggested that at temperatures over 40 degrees C dehydration of samples occurred, later followed by thermolysis and appearance of interactions in all studied cases. Our study concludes by recommending precautionary measures in elaborating new solid formulations containing ABZ, HPBCD and PVP K30/SiO2 and for the ones containing ABZ, RAMEB and Talc/SiO2, due to the present interactions under ambient conditions

Preparation and Antibacterial Properties of Substituted 1,2,4-Triazoles

Background. Both 1,2,3- and 1,2,4-triazoles are nowadays incorporated in numerous antibacterial pharmaceutical formulations. Aim. Our study aimed to prepare three substituted 1,2,4-triazoles and to evaluate their antibacterial properties. Materials and Methods. One disubstituted and two trisubstituted 1,2,4-triazoles were prepared and characterised by physical and spectroscopic properties (melting point, FTIR, NMR, and GC-MS). The antibacterial properties were studied against three bacterial strains: Staphylococcus aureus (ATCC 25923), Escherichia coli (ATCC 25922), and Pseudomonas aeruginosa (ATCC 27853), by the agar disk diffusion method and the dilution method with MIC (minimal inhibitory concentration) determination. Results. The spectroscopic characterization of compounds and the working protocol for the synthesis of the triazolic derivatives are described. The compounds were obtained with 15–43% yields and with high purities, confirmed by the NMR analysis. The evaluation of biological activities showed that the compounds act as antibacterial agents against Staphylococcus aureus (ATCC 25923), while being inactive against Escherichia coli (ATCC 25922) and Pseudomonas aeruginosa (ATCC 27853). Conclusions. Our results indicate that compounds containing 1,2,4-triazolic moiety have great potential in developing a wide variety of new antibacterial formulations

Evaluation of phenolic profile, antioxidant and anticancer potential of two main representants of Zingiberaceae family against B164A5 murine melanoma cells

BACKGROUND: Curcuma longa Linnaeus and Zingiber officinale Roscoe are two main representatives ofZingiberaceae family studied for a wide range of therapeutic properties, including: antioxidant, anti-inflammatory, anti-angiogenic, antibacterial, analgesic, immunomodulatory, proapoptotic, anti-human immunodeficiency virus properties and anticancer effects. This study was aimed to analyse the ethanolic extracts of Curcuma rhizome (Curcuma longa Linnaeus) and Zingiber rhizome (Zingiber officinale Roscoe) in terms of polyphenols, antioxidant activity and anti-melanoma potential employing the B164A5 murine melanoma cell line. RESULTS: In order to evaluate the total content of polyphenols we used Folin-Ciocâlteu method. The antioxidant activity of the two ethanolic extracts was determined by DPPH assay, and for the control of antiproliferative effect it was used MTT proliferation assay, DAPI staining and Annexin-FITC-7AAD double staining test. Results showed increased polyphenols amount and antioxidant activity forCurcuma rhizome ethanolic extract. Moreover, 100 μg/ml of ethanolic plant extract from both vegetal products presented in a different manner an antiproliferative, respectively a proapoptotic effect on the selected cell line. CONCLUSIONS: The study concludes that Curcuma rhizome may be a promising natural source for active compounds against malignant melanoma

The Anti-Melanoma Effect of Betulinic Acid Functionalized Gold Nanoparticles: A Mechanistic In Vitro Approach

Implementing metallic nanoparticles as research instruments for the transport of therapeutically active compounds remains a fundamentally vital work direction that can still potentially generate novelties in the field of drug formulation development. Gold nanoparticles (GNP) are easily tunable carriers for active phytocompounds like pentacyclic triterpenes. These formulations can boost the bioavailability of a lipophilic structure and, in some instances, can also enhance its therapeutic efficacy. In our work, we proposed a biological in vitro assessment of betulinic acid (BA)-functionalized GNP. BA-GNP were obtained by grafting BA onto previously synthesized citrate-capped GNP through the use of cysteamine as a linker. The nanoformulation was tested in HaCaT human keratinocytes and RPMI-7951 human melanoma cells, revealing selective cytotoxic properties and stronger antiproliferative effects compared to free BA. Further examinations revealed a pro-apoptotic effect, as evidenced by morphological changes in melanoma cells and supported by western blot data showing the downregulation of anti-apoptotic Bcl-2 expression coupled with the upregulation of pro-apoptotic Bax. GNP also significantly inhibited mitochondrial respiration, confirming its mitochondrial-targeted activity

The Hydractinia echinata Test-System. III: Structure-Toxicity Relationship Study of Some Azo-, Azo-Anilide, and Diazonium Salt Derivatives

Structure-toxicity relationships for a series of 75 azo and azo-anilide dyes and five diazonium salts were developed using Hydractinia echinata (H. echinata) as model species. In addition, based on these relationships, predictions for 58 other azo-dyes were made. The experimental results showed that the measured effectiveness Mlog(1/MRC50) does not depend on the number of azo groups or the ones corresponding to metobolites, but it is influenced by the number of anilide groups, as well as by the substituents’ positions within molecules. The conformational analysis pointed out the intramolecular hydrogen bonds, especially the simple tautomerization of quinoidic (STOH) or aminoidic (STNH2) type. The effectiveness is strongly influenced by the “push-pull” electronic effect, specific to two hydroxy or amino groups separated by an azo moiety (double alternate tautomery, (DAT), to the –COOH or –SO3H groups which are located in ortho or para position with respect to the azo group. The levels of the lipophylic/hydrophilic, electronic and steric equilibriums, pointed out by the Mlog(1/MRC50) values, enabled the calculation of their average values Clog(1/MRC50) (“Köln model”), characteristic to one derivative class (class isotoxicity). The azo group reduction and the hydrolysis of the amido/peptidic group are two concurrent enzymatic reactions, which occur with different reaction rates and mechanisms. The products of the partial biodegradation are aromatic amines. No additive or synergic effects are noticed among them