Vol 50, No 10 (2017)

The influence of pectin and laminarid NP complex on biological oxidation processes in lead-intoxicated rats was estimated using parameters such as oxidative phosphorylation, ATP synthesis, activities of biological oxidation enzymes, lipid peroxidation, and erythrocyte resistance to osmotic shock and oxidation by oxygen in air, liver antitoxic function, and blood hematological indices. It was established that the polyuronides exhibited antihypoxic, antioxidant, and membrane-stabilizing action.

Water-soluble pentasubstituted anionic and cationic C₆₀-fullerene derivatives were synthesized in highly selective reactions of chlorofullerene C₆₀Cl₆ with captopril and an aliphatic amine. Hybrid supramolecular complexes of the functionalized C₆₀-fullerene derivatives and tetracycline antibiotics (in a stoichiometric 1:1 mole ratio) with polymodal hydrodynamic-radius distributions were synthesized in aqueous solution as nano-sized micelles and vesicles. Hybrid complexes of the antibiotics and cationic amino-C₆₀-fullerene derivatives exhibited synergic antibacterial effects that were more pronounced against a tetracycline-resistant Escherichia coli strain (carrier of the Tc^R gene).

3-Aryloxy- and 3-phenylsulfanylthietane-1,1-dioxides were synthesized by reacting 3,5-dibromo-1-(1,1-dioxothietan-3-yl)-1,2,4-triazole with sodium phenolates and thiophenolate. The 5-aryloxy- and 5-arenesulfonyl-3-bromo-1-(1,1-dioxothietan-3-yl)-1,2,4-triazoles were synthesized via oxidation by H₂O₂ of 5-aryloxy- and 5-phenylsulfanyl-3-bromo-1,2,4-triazoles containing thietane or thietane oxide rings. The 3-substituted thietane-1,1-dioxide IId (2 and 20 mg/kg) displayed antidepressant properties in tail-suspension (TST) and forced-swim tests (FST) that were comparable with those of imipramine. Low toxicity risks (mutagenicity, tumorigenicity, irritation, reproductive toxicity) and satisfactory pharmacokinetic characteristics (correspondence to Lipinski’s rule of five) were predicted (Osiris Property Explorer, Molinspiration) for it.

The chemical compositions of homeopathic mother tinctures (HMT) from the two snowdrop species Galanthus woronowii Losinsk. and Galanthus nivalis L. were compared using gas chromatography with mass-selective detection (GC-MS). A total of 13 compounds were identified in G. woronowii HMT; 42, in G. nivalis HMT. The common constituents of the two tinctures were ethyl-α-D-glucopyranoside, ethyl-α-D-riboside, ethyl linoleate, and 2,3-dihydro-3,5-dihydroxy-6-methyl-4H-pyran-4-one. The main marker compounds (galantamine and licorine) were determined. Their contents were used to standardize the homeopathic drugs.

A method for rapid determination of sodium thiosulfate in solution for injection that is based on titration of the active ingredient by photogenerated iodine is proposed. The titrant was produced by 1-2-min irradiation of an absorbing solution containing KI, acetate buffer, and eosin. The limits of detection (with errors of <3.0%) for sodium thiosulfate were 0.20 μg using current and 0.32 μg using the iodine-generation time in the absorbing solution. The time for a single determination of sodium thiosulfate could be reduced by using this method.

Decoctions of two herbal mixtures including Filipendula ulmaria (L.) Maxim. (meadowsweet), Vaccinium myrtillus L. (bilberry), and shoot and green leaves of Bergenia crassifolia (L.) Fritsch. (badan) were found to improve cognitive-mnestic functions and normalize conditioned reflex activity and explorative behavior of animals after hypoxic exposure. The decoction of mixture II containing mainly meadowsweet was most active at a dose of 5 mL/kg. The quantitative contents of flavonoids calculated as rutin in decoctions of mixtures I and II were (0.22 ± 0.007) and (0.36 ± 0.011) mg/mL, respectively. A total of 22 elements were detected in ash of mixture II and its potent decoction, including 15 essential or conditionally essential ones. Mixture II contained primarily K, Ca, Na, Mg, Si, P, Fe, and Mn; its decoction; Ca, Mg, K, Na, P, Si, Mn, and Zn. The accumulation in the decoction of high concentrations of B, P, Mg, and Mo was noteworthy.

A series of pyimidino derivatives including 4,5-dihydro-5-(1H-indol-1-yl)-6-(phenyl)-4-(4-substituted phenyl) pyrimidine-2-(1H)-one/thione and 4,5-dihydro-4-(3,4,5-trimethoxyphenyl)-6-phenyl-5-[3-(substitute-1-yl))-1H-indol-1-yl]pyrimidin-2(1H)-one/thione have been synthesis and their antimicrobial activity has been assessed in order to study the antimicrobial synergism of indole and benzene nuclei in single molecule. The structures of synthesized compounds were confirmed by IR, NMR and mass spectroscopy data. Antimicrobial activity assessment gives comparable to excellent results against all test microbes. It is concluded that nuclei separately possessing antimicrobial activity exhibit synergism when combined in a single molecule.

The present research was aimed at finding informative criteria for regulating the procedure to determine the interchangeability of systemic levofloxacin-based medicinal products (MP) registered in the RF. The chemical and pharmaceutical characteristics of excipients in 26 commercial levofloxacin products (film-coated tablets for internal use) were compared. Their product lines and instructions for medicinal use were also analyzed. It was shown that the compositions of levofloxacin tablets offered on the RF market differed significantly. It was established that the elaboration and implementation of informative criteria for regulating the procedure to determine the interchangeability of levofloxacin-based drugs should benefit the evaluation of drug quality during the determination of the interchangeability for medicinal use.

A quantitative determination method for total anthraquinone glycosides in Cassia Syrup was developed using direct spectrophotometry at analytical wavelength 530 nm. A processing scheme for producing Cassia Syrup based on a decoction of Cassia acutifolia Del. leaves was proposed.

Development and implementation of pilot and industrial absorption-chromatographic and membrane technologies for the isolation and purification of plant- and animal-based APIs are extremely important issues for the domestic pharmaceutical industry in the RF. The potential of using available Russian scientific and human resources for development and rapid implementation of competitive industrial production technologies with the lowest operating costs and greatest economic efficiencies is demonstrated.