This article focuses on linking structures of fractionated humic polyanions (PAs), which were molecularly defined using ultrahigh resolution Fourier transform mass spectrometry (FTMS), to their antiviral activities with respect to laboratory HIV-1 strains. Anti-HIV-1 activity was proven using a full HIV-1 replication system validated for antiviral testing. We demonstrated that all humic PAs tested in our study were capable of inhibiting HIV fusion. The most hydrophobic fractions of humic and hymatomelanic PAs also strongly inhibited HIV-1 reverse transcriptase. The structure-activity analysis revealed the direct relationship of antiviral activities with contribution of CHO molecules in humic PA composition and lipophilicity index, and the inverse relationship with their carboxylic and total acidity. This was explained by the supramolecular character of humic PAs, the properties of which are ruled rather by the contribution of most potent scaffolds than by the total charge density. It is concluded that all humic PAs tested in this study can be considered as promising precursors for developing cost-effective combinatorial microbicides with polymodal anti-HIV activity and low cytotoxicity capable of preventing HIV-1 transmission.
The antioxidant properties of humic substances of low-mineralization sulfidic muds (peloids) were investigated using initiated oxidation of 1,4-dioxane as a model reaction. Four groups of substances including humic, himatomelanic, fulvic, and humus acids were studied. Kinetic characteristics of the oxidation of humic substances were determined in terms of effective inhibition rate constants fk In . It is established that himatomelanic acids of peloids exhibit the maximum antioxidant activity among the studied substances.
The effect of individual components of humic substances of peloid on free radical oxidation processes has been investigated under conditions of oxidative stress induced in albino rats. Biological activity of peloids was determined using such parameters as the general antioxidant activity, activity superoxide dismutases, catalases and glutathione peroxidases on the third and tenth day of the experiment. Results indicate that the state of oxidative stress can be corrected on the third day of the experiment. Humic acids restore not only normal physiological redox systems, but also increase the activity of antioxidant enzymes on the 10th day.
This article is devoted to the development of technology and methods for assessing the quality of suppositories containing humic acids of low-mineralized silt sulfide mud. The quality standards of the studied medicinal product were established and its stability during storage was determined. The quantitative determination of humic acids in aqueous solutions was determined by the spectrophotometric method. When studying the technological indicators of the suppositories, the following indicators were taken into account: description, average weight, melting temperature and time of complete deformation. The results of visual control showed that the appearance of the suppositories did not change during one year of storage. However, some white plaque and color heterogeneity appeared with the increase of the shelf life up to 1.5 years. The amount of the active substance during the storage of suppositories changed slightly and did not exceed the permissible content standards. The melting point value did not exceed 36 C, and its decrease was not observed. The time of complete deformation of the suppositories did not exceed 15 minutes and was 5-6 minutes during storage. The average weight of suppositories during storage remained stable. The study allows to conclude that the proposed suppositories are stable for 12 months and the preliminary shelf life of suppositories is 1 year. The conducted chemical and pharmaceutical studies scientifically substantiate the expediency of using medicines with humic acids that demonstrate antioxidant and anti-inflammatory properties. This will expand the range of domestic medicines with the given spectrum of therapeutic action.
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