Based on the method developed in this study for obtaining water-soluble PGKCo and PGNaCo, which we had previously synthesized, a pharmacological composition (PC) containing simultaneously the macroelements K and Na, as well as the trace element Co, was obtained for the first time. The effect of polygalacturonates and PC on the viability of cells of tumor lines of various origins was studied in vitro. It was shown that the target products have water solubility, low toxicity (LD50 above 5000 mg kg–1) and selective cytotoxic activity against the tumor cell line of human lung carcinoma A549, breast adenocarcinoma MCF-7 and cervical carcinoma M-HeLa. The results obtained confirm the prospects for further research into water-soluble metal complexes and PC based on pectin biopolymers for the treatment of cancer.
New pharmacological compositions based on water-soluble pectin metal complexes PG-NaCaFe and PG-NaFeCoCu (PG is polygalacturonate) in weight ratios of 6: 1, 9: 1, and 12: 1 promising for pharmacology and medicine as drugs for the treatment of both iron deficiency and pernicious anemia are developed. According to the testing results on males of the Sprague Dawley rat line in vivo , the most pronounced increase in the number of erythrocytes and hematocrit is observed upon the introduction of the composition with the 9: 1 PG-NaCaFe to PG-NaFeCoCu weight ratio indicating the highest efficiency of this complex drug.
Formation of stable complexes of pectin polysaccharides with Nifedipine hypotensive drug has been shown by IR and UV spectroscopy, stereochemistry of the complexes has been determined, their preparation conditions have been optimized. Features of thermal decomposition of pectin and the prepared complexes with Nifedipine have been studied by TGA/DSC. Obtained results provide scientific foundation to design new water-soluble non-toxic formulation of Nifedipine to expand the use of the drug in medicine.
The formation of complexes of sodium polygalacturonate with the antimicrobial drug tetracycline was confirmed by UV spectroscopy, powder X-ray diffraction, and dynamic light scattering. The stoichiometry of the complexes with the maximum tetracycline content (6.68 wt.%) was determined. The morphological characteristics of the synthesized complexes were studied by scanning electron microscopy in comparison with the initial compounds.
Magnesium complexes based on sodium polygalacturonate and pectinate were prepared and characterized. The conditions of complex formation were optimized and the immunomodulatory activity of the complexes was studied in vivo for the first time. The pectin complexes with magnesium ions decrease the immunosuppressive effect of the cyclophosphamide cytostatic, associated with a decrease in the number of immune cells in the blood (leukopenia) after administration of cyclophosphamide, and promote restoration of the white blood cell count in blood and the ratio of their subpopulations, i.e., the complexes exhibit immunomodulatory properties.
New water-soluble pectin complexes with nonsteroidal anti-inflammatory drug Ibuprofen have been synthesized. The formation of stable water-soluble pectin complexes with Ibuprofen has been established and the stoichiometry of the complexes has been determined using IR and UV spectroscopy, powder X-ray diffraction, and dynamic light scattering.
The aim of this work is a comparison of anti-inflammatory properties of the molecular pectin complex with 10% acetylsalicylic acid (P-ASA) and acetylsalicylic acid (ASA) in equimolar doses on the model of carrageenan-induced paw edema of rats. The study was carried out on a total of 28 adult male Sprague Dawley rats at 7 months of age. 30 min after injection of 1% aqueous solution of carrageenan to the plantar aponeurosis, studied drugs were orally administered once at the doses of 10, 20, 40 mg/kg ASA and 100, 200, 400 mg/kg P-ASA. The severity of edema, pain sensitivity, leukocyte count, its subpopulation ratio and IL-1 beta, IL-6, IL-8, TNF alpha level were determined. Normality, t-test and Mann-Whitney tests were used for statistical analyses. The ulcerogenic effect of P-ASA (dose 400 mg/kg) is significantly less than that of ACA (dose 40 mg/kg). The analgesic effect of P-ASA is comparable to ASA at equimolar doses. The anti-edema effect of ASA at the doses of 10 and 20 mg/kg is more pronounced than that of P-ASA at equimolar doses. P-ASA contributes to normalization of blood leukocyte profile. P-ASA may be recommended to using as anti-inflammatory agent with low ulcerogenic properties.