Studies » Biochemical Aspects of Action of EnergoIod Preparation
Biochemical Aspects of Action of EnergoIod Preparation
EnergoIod is a multicomponent medicinal agent with rather complex chemical composition containing iodine, potassium iodide, synthetic water soluble polymer, mono, oligo and polysaccharides.
As to physico-chemical properties EnergoIod is a colloid polymer water solution of iodine, its salts and low molecular organic compounds. The basis for development of this preparation was the idea of creating a medicinal agent with organic combination of universality, broad antimicrobial spectrum, low toxicity, “compatibility” with human organism, ability to “recognize aliens” by analogy with killer cells and eliminate products of destruction of those aliens from organism.
The idea of using antimicrobial properties of iodine contained in iodine polymer complexes is not new. Combinations of equilibrium systems of water solutions of iodine and its salts with starch, amylase, amylopectin and polyvinyl alcohol were studied thoroughly and the advantages of such high polymer iodine in comparison with sulfanilamides and antibiotics were established.
We included such a powerful oxidant as iodine in the composition of EnergoIod in order to obtain universal antimicrobial properties and eliminate or at least reduce probability of evolution of forms able to resist this preparation since no any cases of bacteria’s resistance to iodine were described in literature. Iodine acts topically and resorptively, it has antimicrobial and antiviral properties. Use of iodine is associated with a problem consisting in the fact that high concentrations of iodine irritate skin and mucosal membranes, a single 2-3 g. dose of iodine is very toxic for people. However in combination with polysaccharides and polymers iodine’s toxicity is reduced significantly, iodine acts more slowly (during 5 hours) while maintaining antiviral and antimicrobial properties.
Seven forms of iodine can be found in water solutions: elemental iodine (I2), hypoiodic acid (HOI), iodine cation (H2OI), triiodide ion (I-), hypoiodide ion (OI-) and iodate ion (IO-3). Spectrum of its antimicrobial activity covers both gram-negative and gram-positive microorganisms. 1% iodine solution destroys their vegetative forms in several minutes, pyococcus dies even with dilution rate of 1:5000. Iodine also possesses antifungal, protocidal, cellulicidal and virucidal effects, it is active against several spores.
In order to make the preparation maximally “compatible” we used blood plasma of mammals i.e. colloid polymer solution as a physico-chemical model. The main difference is the fact that the colloid component of EnergoIod consists not of proteins, but of polysaccharides, water soluble synthetic polymers and their complexes.
In combination with such substances as polyoxyethylene glycol and polyvinyl alcohol iodine not only maintains its valuable properties but also acquires a range of new ones. Antibacterial action of iodinated polysteren was described. Such polymers does not release active iodine and show antimicrobial effect only upon contact with an infectious matter. Effective inactivation of viral infections was observed after addition of iodine to polyurethane polymers. Release of iodine from polyurethane complex through desorption ensures prompt (within 15-30 minutes) inactivation of virions. Iodine high polymers (clcium iodine, iodinole, iodinate, iodovidone, polyvidone-iode, iodopirone, iodoform, chiniofonum) are sprayed on tonsils for treatment of chronic tonsillitis, otopyosis, sinusistis, keratitis, furunculosis, periodontitis, conjunctivitis, for management of wounds and operative site in surgery.
In long-term studies of the properties of water solutions of iodine with starch, polyvinyl alcohol and polyvinylpyrrolidone it was established that biological activity was shown by a part of polarized molecule 12 and oxyanion IO-, namely iodine in positively monovalent form with oxidation level +1. In human organism, apparently under the influence of iodidoxidase, active iodine is turned into physiologically active I+I. This is the form of iodine associated with blue coloration and antiseptic properties of iodine containing substances.
It was established that elemental iodine penetrates cells membranes of microorganisms and gets into cells quite easily. Iodine contained in EnergoIod preparation exists in molecular form and in the form of salts existing in several active forms on account of complex formation reactions. The role of matrix is plaid by combination of complex iodine compounds with high molecular ligands forming associates. Their water solution possesses some properties of gel allowing iodine to interact actively with all classes of substances contained in human organism and organism of mammals, as well as in membranes and cells. This process is accompanied by reactions of complex formation and halogenation. A sequence of biochemical reactions in a live organism entails interaction of one of active forms of iodine resulting in evolution of its new active form (iodine enzyme, iodine hormone, iodine biological membrane, iodine protein etc.).
Iodine participates actively in metabolic processes in organism, it enhances lecitin-cholesterol ratio, lipoproteinase and fibrinolytic activity of blood, inhibits coagulation of blood, reduces level of cholesterol and beta lipoprotein.
Each of these newly formed active complexes is “friendly” to human organism. Due to the mechanism of recognition and specific chemical interaction iodine contained in EnergoIod preparation, as well as its complexes, halogenate (iodinate) DNA and RNA containing viruses both inside and outside of cells. This process is carried out through replacement of hydrogen atom in the groups of purine and pyrimidine bases contained in the molecules of DNA and RNA containing viruses. As a result of halogenation new substances without viral properties are produced. This is the basis of the preparation’s virucidal effect.
Broad spectrum antimicrobial activity of EnergoIod and effectiveness of short-term treatment prevent adaptation of pathogenic microorganisms and evolution of their resistant forms. At the same time this preparation is nontoxic and non-cumulative and it has high chemotherapeutic index.
Inclusion of iodine as one of the main active antimicrobial components in EnergoIod preparation is well reasoned taking into account its ability to penetrate easily through cells membranes, which makes it especially valuable in treatment of infections (viral hepatitis) with the main pathologic process taking place in intracellular structures.
Upon creation and adjustment of pharmacokinetics of EnergoIod we used polysaccharides as the main colloid component because their carbohydrate chains, in contrast to other polymers, are more rigid and capability of changing their conformation in biological environment is rather high due to ramified structure of carbohydrate chains and presence of various types of connections in branching points. Furthermore in the last years large amount of experimental data was collected confirming immunogenic and antiviral activity of sulfated polysaccharides. Especially important is activity of sulfated dextrins against viral infections. Such activity is shown by dextrin2sulfate, dextrin3sulfate and dextrin6sulfate. All of them are bound with virions meanwhile non-sulfated dextrins do not show such activity. Upon intralymphatic administration of dextrin2sulfate reduction of intensity of symptoms of Kaposi’s sarcoma is observed. Authors believe that this effect occurs irrespective of activity of D2S because dextrin sulfate does not affect virions directly, but interacts with target cells and blocks ways of penetration of viruses into cells, i.e. this interaction is of ionic nature.
Sulfated polysaccharides prevent viral contamination.
The main physicochemical and curative properties of EnergoIod were ensured by us through purposeful creation of this preparation in the form of water solution of complex iodine compounds with low and high molecular synthetic and natural substances stereochemistry of which is ensured by dynamically balanced conformations of ordered polymer chains. Polysaccharide matrix of EnergoIod carries coordinately linked positively and negatively charged active ions of iodine and cations of microelements and ensures attraction of its whole molecule to lymphocyte and penetration into intracellular structures.
Low toxicity, deferred hydrolytic decomposition of iodine, prolonged action and other properties of thixotropic gel are predetermined by three-dimensional network with iodine molecules and triiodidanions arranged through donor-acceptor interaction of zwitterion type and complex iodine compounds with mono and oligosaccharides - of “shake-cage” type. After use the preparation penetrates into organism’s internal environment contaminated with viruses and is transported to the infected sites in organs and cells, which is the basis of “compatibility” of blood and EnergoIod.
Selection of ingredients contained in EnergoIod by their qualitative and quantitative characteristics was based upon numerous experimental data. Meanwhile qualitative composition of the ingredients was obvious initially, each of them demonstrated unobvious properties after inclusion in the preparation.