Influence of the Abiotic Elicitors Ag Salts of Aspartic Acid Derivatives, Self-Organized in Nanofibers with Monomeric and Dimeric Molecular Structures, on the Antioxidant Activity and Stevioside Content in Micropropagated Bert.

The use of nanomaterials in biotechnology for the in vitro propagation of medical plants and the accumulation of certain biologically active metabolites is becoming an efficient strategy. This study aimed to evaluate the influence of the concentration (0, 1, 10, 50, and 100 mg L) of two types of nanofibers on the growth characteristics, the antioxidant status, and the production of steviol glycosides in micropropagated Bert. plantlets.

Synthesis and Biological Study of 4-Aminopyridine-Peptide Derivatives Designed for the Treatment of Neurodegenerative Disorders.

Background: Alzheimer's disease (AD) and Multiple sclerosis (MS) lead to neurodegenerative processes negatively affecting millions of people worldwide. Their treatment is still difficult and practically incomplete. One of the most commonly used drugs against these neurodegenerative diseases is 4-aminopyridine.

Improvement of Bertoni Propagation and Steviol Glycoside Content Using Aminoacid Silver Nanofibers.

The food industry is interested in replacing artificial sweeteners with natural sugars that possess zero calories and carbohydrates and do not cause spikes in blood sugar levels. The steviosides leaves, synthesized at Bertoni, are 300 times sweeter than common table sugar. propagation is limited due to the poor viability of the seeds, the long time and low germination rate, and the poor rooting ability of vegetative cuttings.

Kinetic and structural studies on the inhibition of acetylcholinesterase and butyrylcholinesterase by a series of multitarget-directed galantamine-peptide derivatives.

Complex neurological disorders, including Alzheimer's disease, are one of the major therapeutic areas to which multitarget drug discovery strategies have been applied in the last twenty years. Due to the complex multifactorial etiopathogenesis of Alzheimer's disease, it has been proposed that to be successful the pharmaceutical agents should act on multiple targets in order to restore the complex disease network and to provide disease modifying effects. Here we report on the synthesis and the anticholinergic activity profiles of seven multitarget anti-Alzheimer compounds designed by combining galantamine, a well-known acetylcholinesterase inhibitor, with different peptide fragments endowed with inhibitory activity against BACE-1.

Effects of New Galantamine Derivatives in a Scopolamine Model of Dementia in Mice.

Alzheimer's disease (AD), a progressive neurodegenerative disorder characterized by memory loss and cognitive functions decline, is a leading cause for dementia and currently ranked as the sixth foremost cause of death. As of present, treatment of AD is symptomatic without convincing therapeutic benefits and new, effective, therapeutic agents are pursued. Due to massive loss of cholinergic neurons and decreased acetylcholine levels, cholinesterase inhibitors like galantamine, remain the backbone of pharmacological treatment of the disease.

New Galantamine Derivatives with Inhibitory Effect on Acetylcholinesterase Activity.

Background: Inhibitors of acetylcholinesterase (AChE) are used to treat many disorders, among which are neurodegenerative upsets, like Alzheimer's disease (AD). One of the limited licensed AChE inhibitors (AChEIs) used as drugs is the natural compound galantamine (Gal).

Objective: As Gal is a toxic compound, here we expose data about its four derivatives in hybrid peptide-norgalantamine molecules, which have shown 100 times lower toxicity.

Effect of Original Peptide Derivatives of Galantamine on Passive Avoidance in Mice.

The effect of original peptide derivatives of galantamine on scopolamine-induced memory impairment in mice was assessed using the passive avoidance test over 12 days. It was found that some galantamine derivatives administered in a dose of /LD improved the memory in experimental mice, especially on days 5-12 of the experiment.

Monolayer formed by l-Asp-based gemini surfactants self-assembled in 1D nanostructures.

Herein, studies on the surface activities of newly synthesized l-Asp-based gemini surfactants, both nonionic and anionic, are presented. Conductometry, tensiometry, and the Langmuir-Blodgett (LB) film technique were applied for this purpose. - isotherms were obtained with a Langmuir trough and Wilhelmy balance.

Synthesis of New Galanthamine-Peptide Derivatives Designed for Prevention and Treatment of Alzheimer's Disease.

Background: Although no effective treatment for the Alzheimer's disease currently exist, some drugs acting as Acetylcholinesterase inhibitors, like galanthamine have positively affected such patients. β- and/or γ-secretase inhibitors are another type of potential drugs. Here we report synthesis of new peptide-galanthamine derivatives, with expected inhibitory activity against both Acetylcholinesterase and β-secretase.

Cellular Pharmacology of Palladinum(III) Hematoporphyrin IX Complexes: Solution Stability, Antineoplastic and Apoptogenic Activity, DNA Binding, and Processing of DNA-Adducts.

Two paramagnetic Pd complexes of hematoporphyrin IX ((7,12-bis(1-hydroxyethyl)-3,8,13,17-tetramethyl-21H-23H-porphyn-2,18-dipropionic acid), Hp), namely a dinuclear one [Pd₂(Hp)Cl₃(H₂O)₅]·2PdCl₂, and a mononuclear metalloporphyrin type [Pd(Hp)Cl(H₂O)]·H₂O, have been synthesized reproducibly and isolated as neutral compounds at different reaction conditions. Their structure and solution stability have been assayed by UV/Vis and EPR spectroscopy. The compounds researched have shown in vitro cell growth inhibitory effects at micromolar concentration against a panel of human tumor cell lines.

Synthesis, structure and in vitro cytotoxic studies of novel paramagnetic palladium(III) complexes with hematoporphyrin IX.

Two coordination compounds of Pd(III) with hematoporphyrin IX ((7,12-bis(1-hydroxyethyl)-3,8,13,17-tetramethyl-21H-23H-porphyn-2,18-dipropionic acid), Hp), dinuclear [Pd(III)2(Hp-3H)Cl3(H2O)5]·2PdCl2, 1 and mononuclear [Pd(III)(Hp-2H)Cl(H2O)]·H2O, 2 were obtained and structurally characterized in solid state and solution using spectroscopic, thermal and magnetic methods. In the dinuclear complex, 1 one of the Pd(III) ions is coordinated to the deprotanated COO(-) groups from the side chains of the porphyrin ligand and the second Pd(III) ion - to two adjacent pyrrole N-atoms on the top of the porphyrin ring and a Pd(III)-Hp-Pd(III) system was formed. The Pd(III) ion in the mononuclear complex, 2 is incorporated in the porphyrin core.

In vitro pharmacological study of monomeric platinum(III) hematoporphyrin IX complexes.

Three stable mononuclear hematoporphyrin IX ((7,12-bis(1-hydroxyethyl)-3,8,13,17-tetramethyl-21H-23H-porphyn-2,18-dipropionic acid), Hp) complexes of Pt(III), namely cis-[ Pt(III)(NH(3))(2)(Hp(-3H))(H(2)O)(2)].H(2)O 1, [Pt(III)(Hp(-3H))(H(2)O)(2)].H(2)O 2 and [Pt(III)((O,O)Hp(-2H))Cl(H(2)O)(3)] 3 with distorted octahedral structure and (d(z)2)(1) ground state have been tested in vitro for antineoplastic activity in a panel of tumor cell lines.

In vitro evaluation of a stable monomeric gold(II) complex with hematoporphyrin IX: cytotoxicity against tumor and kidney cells, cellular accumulation, and induction of apoptosis.

The antineoplastic potential of a stable monomeric Au(II) complex with hematoporphyrin IX (Hp), namely [Au(II)Hp(-2H).(H(2)O)(2)], was investigated in a panel of tumor cell lines. The complex exhibits strong cytotoxicity, whereby the leukaemia- and lymphoma-derived cell lines are more sensitive, with IC(50) values comparable to those of the reference anticancer drug cisplatin.

Synthesis, Structural Characterization, and Cytotoxic Activity of Novel Paramagnetic Platinum Hematoporphyrin IX Complexes: Potent Antitumor Agents.

Three novel stable Pt(III) complexes with distorted octahedral structure and (dz2)1 ground state have been obtained in the course of Pt(II)-hematoporphyrin IX ((7,12-bis(1-hydroxyethyl)-3,8,13,17-tetramethyl-21H-23H-porphyn-2,18-dipropionic acid), Hp) interaction in alkaline aqueous medium and aerobic conditions. A redox interaction also takes place together with the complexation process leading to the formation of Pt(III) species and organic radicals. The processes in the reaction system and the structure of the complexes formed cis-[Pt(III)(NH3)2(Hp-3H)(H2O)2]H2O1, [Pt(III)(Hp-3H)(H2O)2]H2O2, and [Pt((O,O)Hp-2H)Cl(H2O)3] 3, were studied by UV-Vis, IR, EPR and XPS spectra, thermal (TGS, DSC), potentiometric and magnetic methods.

Energy barrier for protein adhesion and crystal nucleation on flat alien substrates.

From the experimentally defined rate of heterogeneous formation of protein crystals and number of collisions between protein molecules with substrate, the energy barrier for adhesion of protein molecule to alien materials is estimated. According to the Boltzmann equation for energy distribution this barrier is of the order of 10(-12) erg per molecule.

Nucleation rate determination by a concentration pulse technique: application on ferritin crystals to show the effect of surface treatment of a substrate.

The nucleation of horse spleen ferritin (HSF) crystals on substrates was investigated using a new modification of the double pulse technique. The influence of three different structureless substrates (glass, glass covered by methyl groups and poly-L-lysin template) on the nucleation was studied. The boundaries in the phase-diagram, which separate zones of crystal nucleation and growth were obtained by keeping pH = 5.

[The serum concentration of trace elements in chronic kidney failure].

The serum copper, zinc, selenium and magnesium levels were studied in 37 patients with chronic renal failure of various degree. The examination of the oligoelements and magnesium was performed on flame and electrothermal atomic absorption spectrophotometry. Reference values from 345 clinically healthy persons were used in the interpretation of the results.

[Long-term (beyond 5 years) prognosis of successfully resuscitated patients with ventricular fibrillation].

An investigation was carried out of 58 patients who had survived ventricular fibrillation during the period 1975-1982 and had been successfully resuscitated in the Cardiologic Clinic of the High Medical Institute in Varna. 12 of the patients were women and 46 were men, mean age 60.8 years (from 43 up to 85 years).

[The diagnostic significance of antibodies to lipid A in patients with chronic kidney infections].

The interest in antilipid A antibodies increases in recent years. By means of an immunoenzyme test developed by the authors the frequency, quantity and characteristic of these antibodies were studied in 46 patients with chronic renal infections and in 36 healthy controls. The frequency of antilipid A antibodies class IgM is 5.

[Cell subpopulations of pyelonephritis patients studied using monoclonal antibodies].

The paper is devoted to a very important problem of immune mechanisms participation in the origination and maintenance of the inflammatory processes in kidneys and urinary ducts. The results from the study of lymphocyte subpopulations, making use of monoclonal antibodies in patients with clinical-laboratory data about chronic pyelonephritis without chronic renal insufficiency, as compared with healthy controls, are reported. Significantly reduced total T-lymphocyte (OKT1+) were established as well as T-helpers lymphocytes (OKT4+) and increased number of monocytes (OKM5+).

[Plasma protein loss via the gastrointestinal tract in nephrotic syndrome patients].

Plasma protein loss via gastrointestinal tract was determined in 24 patients with clinical and laboratory data for manifested nephrosis syndrome, 21 of them being with various histological forms of chronic glomerulonephritis, 2--with disseminated lupus erythematosus and 1--with renal amyloidosis. Isotope labelled chromium trichloride was intravenously applied, marking the albumin pool in a dose of 0.5 micro curie (20 KBq/kg body weight).

[Possibilities of combined treatment of diffuse collagenous glomerulonephritis].

Combined corticosteroid, immunosuppressive and anticoagulant treatment was performed to 17 patients with various histological forms of collagenous glomerulonephritis, 14--with disseminated lupus erythematodes, 1--with periartheritis nodosa and 2--with Schönlein-Henoch disease. The immunosuppressive treatment was carried out for an average of 14.62 months, the corticosteroid treatment--an average of 17 months and the anticoagulant--18.