Interaction of spin-labeled bidquaternary ammonium ligands with acetylocholinesterase.
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Alpha Bungarotoxin binding protein belongs to the group of nicotinic receptors regarding their pharmacologic characteristics. Presence of alpha Bungarotoxin binding sites was confirmed on six cell lines of human microcellular lung carcinomas. The binding sites are saturable, specific and show high affinity for alpha Bungarotoxin. The presence of the binding sites was found on human microcellular lung carcinoma cultured in the mice of "Nude" clones. Using pharmacologically active substances like succinilcholine, decamethonium, atropine and propranolol, the nicotinic characteristics of alpha Bungarotoxin binding sites were confirmed. The presence of alpha 5 subunits in the alpha Bungarotoxin binding protein of human microcellular lung cells was established by Northern blot experiments classifying alpha Bungarotoxin binding protein on microcellular cells as a neuronal nicotinic receptor regarding its structure.
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Seventy-two patients with chronic bronchitis were examined and divided into 3 groups. Group I consisted of patients with chronic catarrhal bronchitis (CCB) group II of those with chronic purulent bronchitis (CPB), group III of subjects with bronchitis associated with purulent destructive pulmonary diseases. All the patients received combined treatment with decamethoxin as an antibacterial modality. It was found that decamethoxin promotes elimination of the infection of the bronchial secretion in 60% of chronic bronchitis suffers, the incidence of microorganisms resistent to several antibiotics reduced 2-fold. Local use of decamethoxin as an antibacterial and antiinflammatory drug in multimodality treatment of chronic purulent bronchitis proved highly effective.
The interaction of effective antibacterial drug decametoxyn with natural DNA was studied by UV-spectroscopy. Decametoxyn shows a specificity to nucleotides: it decreases the cooperativity of melting and the thermal stability of DNA parts enriched by AT pairs. The characteristics of the helix-coil transition on the DNA parts enriched by GC-pairs are invariable. Interaction with AT-pairs results in their partial or complete melting at room temperature, followed by intermolecule aggregation. Interacting with phosphates decametoxyn manifests itself not as a dication but as two single-charged ions.
Three cholinomimetics: acetylcholine, nicotine and muscarine were applied locally on soma of Helix lucorum RPa4 neuron to study ionic nature of its depolarization. Substances that inhibit Na-, K-, Ca- and Cl-conductances were used. Acetylcholine increased Na-, Ca- and Cl-conductances. As the chlorine response part was small due to the proximity of the resting membrane potential and chlorine equilibrium potential, it may be concluded that the dominating response to acetylcholine is connected with the chemocontrolled input of Na+ and Ca2+ ions into a cell. Nicotine induced mainly Na-conductance and muscarine induced Ca-conductance.
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Sensitivity of 50 Candida fungus strains isolated from patients with chronic intestine diseases was studied with respect to amphotericin B, levorin, enteroseptol, intestopan and decamethoxin. The rate of forming resistant variants of the strains with respect to decamethoxin and development of their cross resistance to levorin was estimated. It was shown that decamethoxin was the most active antifungal drug among the drugs tested. Estimation of sensitivity of the Candida strains to enteroseptol and intestopan revealed that the fungicidal concentration of enteroseptol for 78 per cent of the strains ranged within 3.9-7.8 micrograms/ml. It was demonstrated that development of resistance to decamethoxin in the strains of Candida albicans was slow and did not reach high levels. No cross resistance between decamethoxin and levorin was detected.
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The therapeutic and prophylactic effectiveness of gentamicin, decamethoxin and prodigiozan was determined on albino mice infected with two-fold lethal doses of the antibiotic-resistant strain of Ps. aeruginosa. Correlation between the effectiveness of the drug and the dose and time of its administration was found. Pronounced prophylactic and therapeutic effect of gentamicin in combination with decamethoxin was noted. Prodigiozan, a bacterial polysaccharide had no significant effect on the experimental pyocyanic infection of albino mice.
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