Synthesis, Hemolytic Activity, and In Silico Studies of New Bile Acid Dimers Connected with a 1,2,3-Triazole Ring.

The synthesis of bile acid conjugates plays a significant role in pharmacology and organic chemistry. These complex compounds are widely studied due to their potential therapeutic applications (e.g.

Next step in (Montagu, 1803) phylogeography: northern French and Dutch populations (Eupulmonata, Stylommatophora, Hygromiidae).

Features of shell and genitalia as well as nucleotide sequences of selected mitochondrial and nuclear genes of specimens of from ten northern French and two Dutch populations were compared with the same features of British and Italian populations. They were found to be very similar to populations previously identified as belonging to the CAN-1 lineage of . This confirms previous suggestions that was introduced to western Europe (England, France and the Netherlands) in historical times.

Click chemistry as a method for the synthesis of steroid bioconjugates of bile acids derivatives and sterols.

Six steroid conjugates of bile acids and sterol derivatives have been synthesized using the click chemistry method. The azide-alkyne Huisgen cycloaddition of the propionyl ester of lithocholic, deoxycholic and cholic acid with azide derivatives of cholesterol and cholestanol gave new bile acid-sterol conjugates linked with a 1,2,3-triazole ring. Previously, sterols were converted to bromoacetate substituted derivatives by reaction with bromoacetic acid bromide in anhydrous dichloromethane.

The Spray-Dried Alginate/Gelatin Microparticles with Luliconazole as Mucoadhesive Drug Delivery System.

species are opportunistic fungi, which are primary causative agents of vulvovaginal candidiasis. The cure of candidiasis is difficult, lengthy, and associated with the fungi resistivity. Therefore, the research for novel active substances and unconventional drug delivery systems providing effective and safe treatment is still an active subject.

Does the Freeze-Thaw Technique Affect the Properties of the Alginate/Chitosan Glutamate Gels with Posaconazole as a Model Antifungal Drug?

Hydrogels are semi-solid systems with high flexibility, which, due to holding large amounts of water, are similar to natural tissues and are very useful in the field of biomedical applications. Despite the wide range of polymers available to form hydrogels, novel techniques utilized to obtain hydrogels with adequate properties are still being developed. The aim of this study was to evaluate the impact of the freeze-thaw technique on the properties of cryogels based on sodium alginate and chitosan glutamate with posaconazole as a model antifungal substance.

Bromodomain-containing subunits BRD1, BRD2, and BRD13 are required for proper functioning of SWI/SNF complexes in .

SWI/SNF chromatin remodelers are evolutionarily conserved multiprotein complexes that use the energy of ATP hydrolysis to change chromatin structure. A characteristic feature of SWI/SNF remodelers is the occurrence in both the catalytic ATPase subunit and some auxiliary subunits, of bromodomains, the protein motifs capable of binding acetylated histones. Here, we report that the bromodomain-containing proteins BRD1, BRD2, and BRD13 are likely true SWI/SNF subunits that interact with the core SWI/SNF components SWI3C and SWP73B.

Freeze-Drying Technique for Microencapsulation of Ethanolic Extract Using Different Coating Materials.

The present study reports on the encapsulation of ethanolic extract by freeze-drying method using skim milk, sodium caseinate, gum Arabic, maltodextrin, beta-maltodextrin, and resistant-maltodextrin alone or in mixtures of two or four encapsulants. The encapsulation ability of the final mixtures was evaluated based on their microencapsulating efficiency (EE) of total phenolic compounds (TPC) and the physicochemical properties of freeze-dried powders. Results showed that the freeze-dried powders produced using two encapsulants have a lower moisture content, but higher solubility, Carr index, and Hausner ratio than freeze-dried powders produced using only one encapsulant in the formulation.

Chromosome instabilities in resynthesized Brassica napus revealed by FISH.

Brassica napus is an allopolyploid plant, derived from spontaneous hybridization between Brassica rapa and Brassica oleracea. Intensive breeding has led to a significant reduction in genetic and phenotypic diversity within this species. Newly resynthesized hybrids from progenitor species may restore some diversity in B.

In vivo anti-inflammatory and anti-allergic activities of cynaroside evaluated by using hydrogel formulations.

Objectives: Cynaroside (CYN) is the predominant derivative of luteolin in aerial parts of Bidens tripartita which has been used in folk medicine as a diaphoretic, diuretic, antiseptic and anti-inflammatory agent. In our study, alginate (ALG), which is an anionic polymer with bioadhesive properties, was used as a CYN carrier, and multiple hydrogel formulations were created. Additionally, the present study evaluated the in vivo anti-inflammatory and anti-allergic activities of all preparations.

Estimation of seed yield in oilseed rape to identify the potential of semi-resynthesized parents for the development of new hybrid cultivars.

Resynthesized (RS) Brassica napus can be used to increase the genetic diversity of this important crop plant and to develop the heterotic gene pool required for successful hybrid breeding programmes. The level of heterosis in F1 hybrids depends on the individual performance of the parents and on the degree of genetic difference between them. However, RS forms obtained from crosses of B.

Oxythiamine improves antifungal activity of ketoconazole evaluated in canine Malassezia pachydermatis strains.

Background: Malassezia pachydermatis is an opportunistic yeast involved in skin and ear canal infections of dogs and cats. Reports suggest that strains of M. pachydermatis resistant to commonly used antifungal agents may be emerging.

Calcium Chloride Modified Alginate Microparticles Formulated by the Spray Drying Process: A Strategy to Prolong the Release of Freely Soluble Drugs.

Alginate (ALG) cross-linking by CaCl₂ is a promising strategy to obtain modified-release drug delivery systems with mucoadhesive properties. However, current technologies to produce CaCl₂ cross-linked alginate microparticles possess major disadvantages, such as a poor encapsulation efficiency of water-soluble drugs and a difficulty in controlling the process. Hence, this study presents a novel method that streamlines microparticle production by spray drying; a rapid, continuous, reproducible, and scalable technique enabling obtainment of a product with low moisture content, high drug loading, and a high production yield.

NANOEMULSION WITH CLOTRIMAZOLE - DESIGN AND OPTIMALIZATION OF MEAN DROPLET SIZE USING MICROFLUIDIZATION TECHNIQUE.

Poor water solubility of clotrimazole (CLO) hinders development of the effective pharmaceutical dosage forms. Many different concepts and approaches, including lipid based formulations, have been undertaken to improve delivery of CLO. The purpose of this study was to design the composition of nanoemulsion with CLO for topical use, which could be processed by microfluidization method.

Hydrogel Containing an Extract of Tormentillae rhizoma for the Treatment of Bioflim-Related Oral Diseases.

In the present study, hydrogels containing the dried extract of tormentil (Potentilla erecta (L.) Raeusch., Rosaceae) were designed and qualitatively evaluated regarding their viscosity, thixotropy, and texture properties.

The Influence of Chitosan Cross-linking on the Properties of Alginate Microparticles with Metformin Hydrochloride-In Vitro and In Vivo Evaluation.

Sodium alginate is a polymer with unique ability to gel with different cross-linking agents in result of ionic and electrostatic interactions. Chitosan cross-linked alginate provides improvement of swelling and mucoadhesive properties and might be used to design sustained release dosage forms. Therefore, the aim of this research was to develop and evaluate possibility of preparing chitosan cross-linked alginate microparticles containing metformin hydrochloride by the spray-drying method.

Development of new restorer lines for CMS system with the use of resynthesized oilseed rape ( L.).

Resynthesized (RS) oilseed rape ( L.) is potentially of great interest for hybrid breeding. However, a major problem with the direct use of RS is the quality of seed oil (high level of erucic acid) and seed meal (high glucosinolate content), which does not comply with double-low quality oilseed rape.

HD2C histone deacetylase and a SWI/SNF chromatin remodelling complex interact and both are involved in mediating the heat stress response in Arabidopsis.

Studies in yeast and animals have revealed that histone deacetylases (HDACs) often act as components of multiprotein complexes, including chromatin remodelling complexes (CRCs). However, interactions between HDACs and CRCs in plants have yet to be demonstrated. Here, we present evidence for the interaction between Arabidopsis HD2C deacetylase and a BRM-containing SWI/SNF CRC.

EVALUATION OF ALGINATE MICROSPHERES WITH METRONIDAZOLE OBTAINED BY THE SPRAY DRYING TECHNIQUE.

In the present study, nine formulations (F1-F9) of alginate microspheres with metronidazole were prepared by the spray drying technique with using different drug:polymer ratio (1:2, 1:1, 2:1) and different sodium alginate concentration (1, 2, 3%). The obtained microspheres were characterized for size, morphology, drug loading, (potential and swelling degree. Mucoadhesive properties were examined using texture analyzer and three different models of adhesive layers--gelatin discs, mucin gel and porcine vaginal mucosa.

Evaluation of cationic polyamidoamine dendrimers' dermal toxicity in the rat skin model.

Polyamidoamine (PAMAM) dendrimers are multi-branched, three-dimensional polymers with unique architecture, which makes these molecules attractive for medical and pharmaceutical applications. Using PAMAM as drug carriers for topical delivery might be beneficial as they only produce a transient effect without skin irritation. To evaluate the dermal toxicity of cationic PAMAM dendrimers generation 2 and generation 3, skin irritation studies were performed in vivo in the rat skin model.

Application of pollination of opened ovaries to obtain L. × L. hybrids.

This study presents the results of experiments concerning: (1) interspecific hybridization of × via application of placental pollination and (2) embryological analysis of the process of resynthesis of . In order to overcome certain stigma/style barriers, pollen was placed on an opened ovary (with style removed). Pollinated ovaries were cultured on Murashige and Skoog (MS) medium.

Poly(amidoamine) dendrimers increase antifungal activity of clotrimazole.

Clotrimazole (CLO) is a local imidazolic antifungal agent. A major problem associated with the successful formulation of effective dosage forms containing CLO is its poor aqueous solubility, which presents a hindrance for the local availability of CLO and limits the effective antifungal therapy. In the present study, the effects of various concentrations of poly(amidoamine) (PAMAM) dendrimers generation 2 (G2) and generation 3 (G3) with amine (PAMAM-NH(2)) or hydroxyl surface groups (PAMAM-OH) on aqueous solubility and antifungal activity of CLO were studied.

Stability of extemporaneous enalapril maleate suspensions for pediatric use prepared from commercially available tablets.

In this paper, the stability of enalapril maleate in oral formulations prepared from commercially available tablets was investigated. Extemporaneously compounded, 0.1 mg/mL and 1.

Novel amidine analogue of melphalan as a specific multifunctional inhibitor of growth and metabolism of human breast cancer cells.

A novel amidine analogue of melphalan (AB4) was compared to its parent drug, melphalan in respect to cytotoxicity, DNA and collagen biosynthesis in MDA-MB-231 and MCF-7 human breast cancer cells. It was found that AB4 was more active inhibitor of DNA and collagen synthesis as well more cytotoxic agent than melphalan. The topoisomerase I/II inhibition assay indicated that AB4 is a potent catalytic inhibitor of topoisomerase II.