Vol 51, No 3 (2017)

This review summarizes published data on organic hydrogen sulfide donor compounds, including hybrid compounds, and their roles in cardioprotection.

This review addresses the main structural types of matrix metalloproteinase (MMP) inhibitors - hydroxamic acid derivatives, sulfonamides, bisphosphonates, compounds combining phosphoryl and hydroxamate groups, and functional derivatives of phosphonic and phosphinic acids. The selectivity of the inhibitory actions of these substances in relation to different types of MMP and the potential for the practical application of these substances in cancer treatment are discussed.

Heating of substituted benzimidazole-2-sulfonic acids in the presence of excess quantities of secondary amines was used to synthesize dialkylaminobenzimidazoles. Experimental studies of potential antiarrhythmic, antiaggregation, hemorheological, AT₁ angiotensin- and NHE-1-inhibiting, and antiserotonin activity identified active compounds. 1[-2-(5-Methyl)benzimidazole]pyrrolidine had greater NHE-inhibiting activity than zoniporide. 1-{[2-(5-Methoxy)benzimidazole]-4-N-methyl}piperazine dihydrochloride had greater antiaggregatory activity than acetylsalicylic acid, while 1-[2-(5-methyl)benzimidazole]piperidine was as active as cyproheptadine in terms of 5-HT_2A antagonistic activity. 1-(2-Benzimidazole)pyrrolidine and 1-[2-(5-chloro) benzimadazole pyrrolidine dihydrochlorides had 5-HT₃ antagonist activity equal to that of tropisetron..

The analgesic and antimicrobial activity of 1-substituted 4,4,4-trichlorobutane-1,3-diones were studied.

Abies pindrow Royle (Himalayan silver fir, family Pinaceae) has a long tradition of use as anxiolytic but not investigated scientifically. Previously, antianxiety activity of chloroform extract (CE) and ethyl acetate fraction (EAF) of methanol extract of the plant have been reported at the dose of 400 and 50 mg/kg, respectively. CE and EAF were subjected to bioactivity-guided-fractionation using column chromatography with a view to isolate anxiolytic constituents. The antianxiety activity of test samples was assessed by comparing with control as well as standard drug, diazepam (2 mg/kg, p.o.) using the elevated plus maze model. Among six fractions (F₁ – F₆) of CE obtained after column chromatography, F₂ and F₃ exhibited significant antianxiety activity at doses of 45 and 40 mg/kg, respectively. Further column chromatography of F₂ and F₃ led to the isolation of maltol and dipalmitin. Column chromatography of EAF yielded five fractions (F₁ – F₅). F₁ Exhibited antianxiety activity at the dose of 15 mg/kg. Column chromatography of F₁ led to the isolation of gallic acid, maltol, p-coumaric acid, 4-hydroxy benzoic acid, 3,4-dihydroxy benzoic acid, shikimic acid, pinitol, hesperitin, and apigenin. Among these compounds, maltol, gallic acid, p-coumaric acid, hesperitin, and apigenin exhibited antianxiety activity at doses of 100, 10, 30, 50 and 2 mg/kg, p.o., respectively.

Amethod for assaying sulfur hexafluoride in a new contrast agent by gas chromatography is described. Detection was with an electron capture detector (ECD). Sulfur hexafluoride was extracted from samples using heptane as the solvent. The method was validated in terms of the following parameters: specificity, linearity, correctness, stability, and inter- and intralaboratory precision.

An iodometric method for determining the antiradical activity (ARA) of dihydroxybenzenes in the reaction with 2,2′-azobis-(2-amidinopropane) (AAP) peroxyl radicals (rOO^• ) in conditions close to those obtaining in biological systems was developed. A means of calculating relative rate constants of reactions of phenols with rOO^• from the kinetics of consumption of an inhibitor added at low concentration was proposed. The greatest levels of ARA were seen with resorcinol, orcinol, and hydroquinone, which are able to dissociate to form highly reactive mono-and bianionic forms of phenolate ions. A method of calculating relative rate constants of these reactions was proposed, based on the AAP - AAP peroxyl radical - phenol kinetic model.

The stability and quality of pharmaceutical substances are assured by systematic evaluation using various analytical techniques. Biologically active compounds retain and exhibit maximum potency during their shelf life. Once the drug expiry period is crossed, deterioration, decrease of therapeutic activity, and increased toxicity can occur. The purpose of the present study was to develop a simple, rapid and reproducible analytical method for the determination of N-isonicotynoyl-N′-(2-fluorobenzal)hydrazone – a synthesized by us halogenated isoniazid derivative with high tuberculostatic activity – in aqueous phase, on the basis of RP-HPLC-PDA and UV/VIS spectrophotometry investigations. The proposed RP-HPLC-PDA procedure is characterized by short retention time (3.1 min), high precision (RSD < 3.52%), and good linearity (R² > 0.9941). HPLC patterns display well-resolved peaks without interference. Despite high linearity (R² = 0.9978) of the UV/VIS spectrophotometry, greater LOQ and LOD values indicated unsuitability of this method for the detection and quantification of N-isonicotynoyl-N′-(2-fluorobenzal)hydrazone at low concentrations (< 10 μg/mL).

The effects of using selenium dressings on A. schoenoprasum on the antioxidant activity of extracts were studied. Treatment of seeds with sodium selenate led to minor increases in polyphenol levels in extracts and the expression of the antioxidant gene katG, but had no effect on the radical-binding (RBA) or chelating (CA) activity of extracts, not increasing their antioxidant activity in a microbial test system. Selenate added artificially to extracts produced statistically significant reductions in indicators such as the concentrations of polyphenols, RBA, CA, and, to a small extent, antioxidant activity in the microbial test system, but had no effect on the ability of extracts to stimulate expression of the katG gene.

Studies using 224 blood samples as examples showed that the use of solid-phase extraction and gas chromatography with mass spectrometric detection for screening blood provides reliable identification of a wide range of narcotic and pharmaceutical substances of forensic medical interest, including “designer” synthetic narcotics – methylenedioxypyrovalerone (MDPV), pyrrolidinovalerophenone (PVP), and their metabolites; cannabimimetic metabolites N-(1-carbamoyl-2-methylpropyl)-1-pentyl-1H-indazole-3-carboxamide (ABPINACA) and/or N-[(1-pentyl-1H-indazol-3-yl)carbonyl]valine methyl ester (AMB). The distribution of substances in different elusion fractions is given and dissociation constants (pK_a) and coefficients of distribution in an octanol-water system (log P) are calculated.