4 articles
Thiosemicarbazones represent a class of organic compounds with well-documented pharmacological properties, including antitumor, antimicrobial, and antiviral activities. Contemporary research highlights their role in modulating cellular redox equilibrium through antioxidant pathway regulation. The growing interest in copper-based coordination complexes with thiosemicarbazones is driven by the unique redox flexibility and high biocompatibility of copper ions, properties that underlie their potential in therapeutic and diagnostic applications. This investigation assessed the capacity of specific local bioactive thiosemicarbazones to impact the antioxidant system using in vitro methodologies.
Peripheral blood samples from ten healthy volunteers were used to evaluate in vitro the influence of 10 copper-based coordination complexes with thiosemicarbazones at concentrations of 10.0 μM/L and 1.0 μM/L on antioxidant markers ‒ total antioxidant activity (via ABTS assay), total antioxidant capacity, antioxidant substance mass, and antioxidants total activity.
Data indicated that targeted copper-based coordination complexes with thiosemicarbazones affect general antioxidant markers. The study demonstrates that thiosemicarbazones exhibit concentration- and structure-dependent redox modulation, disclosing distinct mechanisms of action across three structural classes – benzothiazole, phenyl, and allyl thiosemicarbazone derivatives. Structural optimization (e.g., benzothiazole with methoxy groups) yields compounds like MG-22 that maintain redox equilibrium, while pro-oxidant variants (CMA-18) offer therapeutic potential through selective oxidative cytotoxicity.
Copper-based coordination complexes with thiosemicarbazones represent a promising class of redox modulators with tunable biological effects. Their bidirectional activity, manifested by stimulation or inhibition of antioxidant mechanisms, confirms the potential of these derivatives as selective therapeutic agents. When these results are integrated in the context of personalized medicine, thiosemicarbazones become valuable candidates in the development of therapeutic strategies aimed at maintaining cellular homeostasis, especially in pathologies characterized by increased oxidative stress, such as cancer and neurodegenerative diseases.
Cholestatic jaundice installed in gallstones is considered a multifactorial pathogenetic process. The correlation of endogenous hepatic intoxication with the reaction of the pro- and antioxidant system, characteristic of various complications of gallstones associated with cholestatic jaundice, remains an undefined subject.
The study included the investigation of 105 patients with complicated gallstones and associated cholestatic jaundice, and the control group – 35 patients with uncomplicated gallstones. The age of the patients varied between 51 and 72 years, with an F/M ratio of 3/1.
The degree of endotoxemia, assessed at hospitalization by peptides with average mass values, was consistent with the inflammation present in groups 2 and 3, reporting a statistically significant difference compared to the control group [p c/2 < 0.001 (t = 11.1); p c/3 < 0.001 (t = 11.07)]. DAM, as the final product of lipid peroxidation, evaluated at hospitalization, shows double marked values in all groups compared to the control group [p < 0.001 (t = 10.7); (t = 10.9); (t = 16.5)]. The antioxidant activity, assessed at hospitalization, shows a statistically significant decrease in superoxide dismutase values [p < 0.001 (t = 6.4); (t = 4.1); (t = 5.7)], as well as catalase [p < 0.001 (t = 6.7); (t = 5.6); (t = 7.2)] in all groups, by 30-40% compared to the control group.
In established cholestatic jaundice, there is an obvious activation of lipoperoxidation processes, contributing to the increase of endogenous intoxication and early suppression of antioxidant activity. There is a direct relationship between the increase in prooxidant activity and the level of endogenous intoxication in all complications of gallstones associated with cholestatic jaundice, but it is more elevated in infectious complications, indicating a need for an early approach.
Insects, throughout evolution, have developed a huge arsenal of active compounds, which they use to defend themselves against enemies and diseases, at the same time in recent years insects have shown great interest as a source of food rich in biologically active substances. Research in recent decades has shown that insects produce a variety of proteins and peptides with antibacterial, antifungal, antiviral, immunomodulatory, anti-inflammatory, antioxidant, antitumor, hepatoprotective, antithrombotic, antihypertensive and detoxifying activity during or after contact with the microbial agent or unfavourable factor.
The anti-inflammatory effect of imuheptin and imupurin was investigated in a rat model of subacute inflammation induced by subcutaneous implantation of felt discs. The intensity of the exudative and proliferative phase of inflammation, cytokine profile (TNFalpha, IL-6, IL-10), ceruloplasmin and antioxidant enzymes (superoxide dismutase, catalase, glutathione reductase, glutathione peroxidase and glutathione-S-transferase) in the serum of rats were evaluated.
Imuheptin and imupurin reduced the level of pro-inflammatory cytokines (TNF-alpha, IL-6) and increased that of the anti-inflammatory cytokine (IL-10), as well as ceruloplasmin, glutathione reductase and glutathione peroxidase in subacute inflammation. Additionally, imupurin significantly increased the level of catalase and imuheptin that of glutathione-S-transferase.
Imuheptin and imupurin determined a moderate effect of inhibiting the exudative and proliferative processes, compared to the reference preparation - dexamethasone, but with a favourable effect on the cytokine profile, decreasing the level of pro-inflammatory cytokines (TNF-alpha, IL-6) and increasing the level the anti-inflammatory one (IL-10), as well as the modulation of antioxidant enzyme activity.
Identification, study and testing of new remedies for treatment approaches of diseases, resulting from imbalance between oxidants and antioxidants in favor of oxidants, with potentially destructive potential and pathogenesis in liver disorders is of particular interest due to the increase in incidence and severity of these pathologies.
The action of novel local copper coordination compounds, thiosemicarbazide derivatives - CMD-4, CMJ-33 and CMT-67, was evaluated in experiments on white rats after subcutaneous administration in two different doses (0.1 and 1.0 µM / kg) 3 times a week for 30 days. The main indices of oxidative stress were evaluated: the level of malonic dialdehyde (MDA), nitric oxide derivatives (NO), S-nitrosothiols, advanced glycation end products (AGEs), advanced oxidation protein products (AOPP) and ischemia-modified proteins (IMP), and antioxidant system: - superoxidismutase (SOD) and catalase activity (CAT), the level of histidine (His) and total antioxidant activity (TAA) in liver tissue of white rats.
The administration of CC resulted in the reduction of oxidative stress indices - MDA, AGEs and S-nitrosothiols, which denotes the antioxidant effect of the studied compounds. The level of NO and AOPP derivatives does not change substantially. When administering CMD-4 (1 µM / kg), SOD activity and catalase function decreased markedly. Changes in the content of His and TAA have been shown to be inconclusive, maintaining within the limits of the values recorded in the control group.
The elucidation of the modifications of the free radicals processes in liver tissues, which are the basis of the CC action, broadens the theoretical knowledge about the biological properties of a number of chemical compounds; as well provide new possibilities to explore perspective objects in order to obtain new efficient drug preparations.