Comparative analysis of neuroprotective activity of new chemical agent Vp and piracetam

The effect of new agent Vp (9-butylamine-3,3-dimethyl-3,4-dihydroacridine-1(2H) hydrochloride) on lifetime of isolated mechanoreceptive crayfish neurons was evaluated by the duration of its impulse activity. Vp significantly and dose-dependently prolonged the lifetime of both spontaneously degrading neurons and neurons degrading under conditions of inhibition of various stages of the energy metabolism: glycolysis and oxidative phosphorylation. The effect of Vp in a concentration of 10⁻⁷ M surpassed that of amiridine. Piracetam also prolonged the lifetime of spontaneously degrading neurons, but only in very high concentration (10⁻² M). It is concluded that Vp possesses a neuroprotective activity. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 129, No. 4, pp. 430–433, April, 2000     

Effect of the phenol antioxidant katavidan on autooxidation of microsomes exposed to visible light

A study is performed of the effect of the phenol antioxidant katavidan on autooxidation of microsomes from rat liver exposed to visible light. It is shown that katavidan in a concentration of 10⁻³ M inhibits but in concentrations of 10⁻⁵–10⁻⁷ M stimulates autooxidation of microsomes. No stimulation is observed under conditions of dark incubation. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 118, № 10, pp. 393–394, October, 1994 Presented by I. P. Ashmarin, Member of the Russian Academy of Medical Sciences     

Effect of ultralow doses of thyroliberin on microviscosity of lipid components of biological membranes

Effects of the regulatory peptide thyroliberin on microviscosity of lipid components of endoplasmic reticulum biological membranes in mouse hepatocytes were studied by electron paramagnetic resonance. Thyroliberin in a concentration of 10⁻³–10⁻¹⁸ M decreased microviscosity of surface layers of membrane lipids. This decrease was the most pronounced (30%) under effects of 10⁻¹⁰ and 10⁻¹⁶ M thyroliberin. Physiological effects of thyroliberin corresponded to its influence on the membrane structure. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 129, No. 1, pp. 38–40, January, 2000     

Effects of calcium antagonists on serotonin-dependent aggregation and serotonin transport in platelets of patients with migraine

Flunarizine and cinnarizine (IC₅₀ 6.8×10⁻⁶ and 2.8×10⁻⁵ M, respectively) inhibited³H-serotonin uptake by platelets. In higher doses, they blocked serotonin-induced platelet aggregation and stimulated³H-serotonin release from these cells. Imipramine did not affect serotonin-releasing effects of preparations. In all patients cinnarizine was more potent in inhibiting serotonin uptake, and in half of the patients cinnarizine displayed higher activity as an inductor of serotonin release. Translated fromByulleten's Eksperimental'noi Biologii i Meditsiny, Vol. 130, No. 7, pp. 24–27, July, 2000     

Assessment of nucleosomal DNA fragmentation in lung adenocarcinoma cells incubated with human platelets

No nucleosomal fragmentation of DNA from lung adenocarcinoma cells was observed after 18 h of their incubation with normal human platelets isolated from human peripheral blood. Platelet activation with 10⁻⁶, 10⁻⁷, and 10⁻⁸ M PAF did not lead to nucleosomal fragmentation of the target cell DNA. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 124, No. 11, pp. 547–549, November, 1997     

Effects of calcium antagonists on serotonin-dependent aggregation and serotonin transport in platelets of patients with migraine

Flunarizine and cinnarizine (IC₅₀ 6.8×10⁻⁶ and 2.8×10⁻⁵ M, respectively) inhibited³H-serotonin uptake by platelets. In higher doses, they blocked serotonin-induced platelet aggregation and stimulated³H-serotonin release from these cells. Imipramine did not affect serotonin-releasing effects of preparations. In all patients cinnarizine was more potent in inhibiting serotonin uptake, and in half of the patients cinnarizine displayed higher activity as an inductor of serotonin release. Translated fromByulleten's Eksperimental'noi Biologii i Meditsiny, Vol. 130, No. 7, pp. 24–27, July, 2000     

Interaction of bis-β-chlorethylamine estrogen derivatives with human ovarian adenocarcinoma cells

Antiproliferative effect of bis-β-chlorethylamine estrogen derivatives on human ovarian adenocarcinoma CaOV cells depends on the dose of the drug. In concentrations of 10⁻⁵ and 5×10⁻⁶ M they inhibit, while in a dose of 5×10⁻⁷ M stimulate cell proliferation. It is assumed that CaOV cells express estradiol receptors. The interaction of these cytostatics with estrogen-binding sites on CaOV cells is demonstrated. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 127, No. 3, pp. 302–304, March, 1999     

Effects of the nootropics piracetam and GVS-111 on voltage-dependent ion channels of neuronal membranes

The effect of two nootropics, piracetam and N-phenylacetyl-L-prolyglycine ethyl ester (GVS-111), is studied by measuring high-threshold K⁺ and Ca²⁺ currents in isolated snail neurons using a two-microelectrode patch-clamp technique. Piracetam and GVS-111 are shown to reduce the amplitude of both the K⁺ and the Ca²⁺ (to a lesser extent) current. The threshold concentrations for GVS-111 and piracetam are 10⁻⁹-10⁻⁸ M and 1–5×10⁻⁴ M, respectively. It is assumed that the antiamnestic effect of the nootropics is partially mediated by a blockade of ion channels of the neuronal membrane. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 121, N ^o 2, pp. 151–155, February, 1996 Presented by G. N. Kryzhanovskii, Member of the Russian Academy of Medical Sciences     

Antioxidant properties of thiamine

Thiamine (10⁻⁴–10⁻⁶ M) inhibits lipid peroxidation in rat liver microsome and free radical oxidation of oleic acidin vitro. Thiamine interacts with free radicals and hydroperoxides and is oxidized to thiochrome and thiamine disulfide. The antioxidant effect of thiamine is probably related to sucessive transfer of 2H⁺ from the NH₂ group of the pyrimidine ring and H⁺ from the thiazole ring (after its opening) to reactive substrates. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 130, No. 9, pp. 303–305, September, 2000     

Mechanism of heart-rate acceleration caused by stimulation of vagal centers in the frog

The mechanism by which heart rate is increased upon stimulation of vagal centers is studied using frog heart preparations perfused with Ringer—Locke solution containing atropine and/or benzohexonium. Atropine stimulates vagus-induced heart-rate acceleration in dilutions of 10⁻⁶ and 10⁻⁵ g/ml. In a dilution of 10⁻⁴ g/ml both atropine and benzohexonium abolish vagal tachycardia. Rausedyl (3–4 injections, 5 mg/kg, at 18–20-h interval) prevents tachycardia. Stimulation of both halves of the medulla oblongata increases heart rate to a greater extent than stimulation of one half. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 124, No. 7, pp. 16–20, July, 1997     

Antioxidant properties of thiamine

Thiamine (10⁻⁴–10⁻⁶ M) inhibits lipid peroxidation in rat liver microsome and free radical oxidation of oleic acidin vitro. Thiamine interacts with free radicals and hydroperoxides and is oxidized to thiochrome and thiamine disulfide. The antioxidant effect of thiamine is probably related to sucessive transfer of 2H⁺ from the NH₂ group of the pyrimidine ring and H⁺ from the thiazole ring (after its opening) to reactive substrates. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 130, No. 9, pp. 303–305, September, 2000     

Effects of synthetic bis-β-chloroethylamine estrogen derivatives on proliferation of skin sarcoma cells

The effects of four new synthetic bis-β-chloroethylamine-containing estrogens and known cytostatic agents chlorophenacyl and estradiol mustard were compared on monolayer cultures of transformed L-929 fibroblasts (from murine skin sarcoma). The drugs within the concentration range of 10⁻⁵-5×10⁻⁷M inhibited proliferation of cultured cells by 67%. Chlorophenacyl displayed the least antiproliferative activity (15% inhibition at 10⁻⁵M). Steroid nucleus introduced into the molecule enhanced antiproliferative activity of test drug in comparison with chlorophenacyl, probably due to accumulation of the hormone-cytostatic molecules in cells. Estradiol had no effect on proliferative activity of L-929 cells, and no specific estrogen-binding sites were found in cultured transformed fibroblasts. The antiproliferative effect of hormone-cytostatics on this culture is not mediated via specific interactions with estrogen receptors. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 129, No. 6, pp. 695–697, June, 2000     

Effects of sex hormones and antihormones on the activity of redox system enzymes of human erythrocyte glutathione

Effects of estradiol and testosterone and of the antiandrogens cyproterone acetate, niftolide, and antiestrogen tamoxifen on the activities of human erythrocyte glutathione peroxidase and glutathione reductase were studiedin vitro. In contrast to hormone preperations, antihormones in high concentrations (10⁻⁴−5×10⁻⁴ M) modified the enzyme activities. Cyproterone acetate and tamoxifen increased the activity of glutathione reductase, while tamoxifen stimulated glutathione reductase and inhibited glutathione peroxidase. Niftolide inhibited both enzymes. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 124, No. 8, pp. 185–187, August, 1997     

In vitro effects of folic acid on γ-glutamyltransferase and glutathione reductase activities in malignant lung and thymus tumors

In vitro effects of folic acid (10⁻⁵, 10⁻⁴, and 10⁻³ M) on activities of γ-glutamyltransferase and glutathione reductase, the enzymes involved in glutathione metabolism, were studied in tissue samples obtained after surgical treatment of the lungs and thymus. Folic acid did not change γ-glutamyltransferase activity in lung cancer tissue, but in thymoma tissue this substance in a concentration of 10⁻³ M inhibited it by 16%. Folic acid had no effects on glutathione reductase activity in benign tumors and normal lung and thymus tissues, but increased this activity in thymoma and lung cancer tissues. Activation of glutathione reductase was probably related to binding of folic acid in the allosteric center of the enzyme, which probably induced conformational changes in the catalytic center, acceleration of electron transport from NADPH₂ to oxidized glutathione via flavin adenine nucleotide, and intense production of reduced glutathione. Translated fromByulleten', Eksperimental'noi Biologii i Meditsiny, Vol. 130, No. 10, pp. 422–425, October, 2000     

Suppression of increased alcohol consumption caused by adoptive transfer of splenocytes from animals with abstinent syndrome by antibodies to serotonin

Experiments on C57B1/6 mice prone to experimental alcoholism demonstrated that adoptive transfer of splenocytes from animals with the abstinent syndrome stimulates alcohol consumption. Incubation of splenocytes with antibodies to serotonin in a dose of 10⁻⁷ M for 1 or 24 h completely suppressed this effect. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 126, No. 9, pp. 328–330, September, 1998     

Synthesis and properties of the immunotoxin CD5-ricin

Synthesis and properties of an immunotoxin produced by conjugating ricin with a novel monoclonal antibody (IgG3 of the ICO-104 class) are described. Cytolytic activity of the synthesized immunotoxin, determined by two independent methods and expressed in LD₅₀, is 0.3–0.6×10⁻⁷ M. Its specificity for target cells containing the CD5 antigen is shown. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 119, N ^o 1, pp. 76–79, January, 1995 (Presented by Yu. A. Romanov, Member of the Russian Academy of Medical Sciences)     

Modulation of the oxidative burst in mouse macrophages and human neutrophils by superlow concentrations of GM1 ganglioside

It is shown that ganglioside GM1 in picomolar concentrations stimulates the phorbol-12-myristate-13-acetate (PMA)-induced generation of active forms of oxygen by neutrophils and peritoneal macrophages. GM1 (10⁻¹¹ M) is found to enhance the luminol-dependent chemiluminescence induced by 10⁻⁸ M PMA in mouse macrophages in comparison with the effect of PMA alone. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 117, N ^o 1, pp. 44–46, January, 1994 Presented by A. N. Klimov, Member of the Russian Academy of Medical Sciences     

Effect of elementary proline-containing peptides on functional activity of anticoagulation system and primary homeostasis

Elementary proline-containing peptides being added to rat platelet-rich plasma or platelet suspension in concentrations of 10⁻¹–10⁻⁷ mg/ml elicit a considerable antiplatelet effect. Efficiency of inhibition of platelet aggregation increases in the following order: Pro-Gly>Pro-Gly-Pro>Gly-Pro-Gly-Gly. Intravenous injection of these peptides activates blood anticoagulation system in experimental animals. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 125, No. 4, pp. 496–499, May, 1998     

Xymedon restores T-cell immune response inhibited by γ-irradiationin vivo: Interrelations with Ca2+-ATPase and DNA-relaxing activities

High radioprotective activity of xymedon was shown in mice. Radioprotective effects of this preparation were accompanied by restoration of the delayed-type hypersensitivity response and Ca²⁺-ATPase activity in splenocytes which were inhibited by γ-irradiation (3 Gy). At concentrations of 10⁻³ and 10⁻⁶ M xymedon stimulated the activity of DNA topoisomerase-I of splenocyte nuclei. Here we discuss a mechanism of radioprotective effects of pyrimidine derivatives associated with the inhibition of apoptosis of lymphoid cells and the stimulation of proliferation and differentiation of lymphoid precursor cells. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 127, No. 1, pp. 66–70, January, 1999     

Effect of exogenous acetylcholine on neuromuscular transmission in the stimulated rat diaphragm

Nerve stimulation is performed in rat phrenicodiaphragmal preparations with armine-inhibited acetylcholinesterase. Acetylcholine (1×10⁻⁷ M) is added to the saline for 15 min, and as it is washed off (during 1–2 h), the amplitude of isometric contractions and of the total action potential increases in the continuously stimulated muscle. Contractions in response to direct muscle stimulation remain unchanged. The membrane resting potential of muscle fibers exposed to acetylcholine shifts by 2–3 mV toward hyperpolarization and remains at this level for 2 h after the removal of acetylcholine from the saline. Presented by S. N. Golikov, Member of the Russian Academy of Medical Sciences Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 118, N ^o 11, pp. 457–459, November, 1994