Browsing by Author "Kostadinova I."

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    Application of ABTS method for assessment of radical-binding effect of Creatine monohydrate
    (2023-01-01) Tsvetkova D.; Kostadinova I.; Landzhov B.; Vezenkov L.; Marinov L.; Ivanova I.
    Due to its antioxidant properties Creatine exhibits benefits on muscle, bone, and brain function, and can be of great importance for the prevention of the oxidative stress-related diseases. The aim of current study was the investigation of antiradical effect of Creatine monohydrate by the application of ABTS method. The radical-scavenging activity of Creatine monohydrate against methanol solution of ABTS radical was evaluated by measuring the decrease in the absorbance at λ = 744 nm. For the estimation of antiradical effect of the compound examined the following parameters were calculated: radical scavenging activity in [%], IC50 value; antioxidant power 1/IC50, Trolox equivalent activity. Linear relationship between the enhanced radical scavenging activity and decrease of absorbances and of not-bound ABTS-radical with the increase of concentration of Trolox (0.002 mM ÷ 0.75 mM) and Creatine monohydrate (20 mM ÷ 200 mM) has been established. Linearity was characterized by coefficients of linear regression, which were proven to be higher than 0.97. From the experimental results it was observed that Creatine monohydrate (IC50 = 100.98 mM) exerts antiradical effect, but is less active compared to Trolox (IC50 = 0.2 mM) due to higher IC50 value and lower antioxidant power (1/IC50, = 0.01) than Trolox (1/IC50 = 5).
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    Biological screening of novel structural analog of Celecoxib as potential anti-inflammatory and analgesic agent
    (2019-04-01) Zlatanova H.; Vladimirova S.; Kostadinov I.; Delev D.; Deneva T.; Kostadinova I.
    Background and objectives: The clinical use of non-steroidal anti-inflammatory drugs is limited due to high incidence of adverse drug reactions. The pyrrole heterocycle is included in the chemical structure of a number of drugs with various activities and shows relatively good tolerability and safety. The objectives of our study were to evaluate the analgesic and anti-inflammatory activity, as well as possible organ toxicity, of 2-[3-acetyl-5-(4-chloro-phenyl)-2-methyl-pyrrol-1-yl]-3-(1H-indol-3-yl)-propionic acid (compound 3g), a novel N-pyrrolylcarboxylic acid structurally similar to celecoxib. Materials and methods: All experiments were performed on 6-week-old male Wistar rats divided into parallel groups (n = 8). Antinociception was assessed using animal pain models with thermal and chemical stimuli (paw withdrawal, tail-flick, and formalin tests). Criteria for the analgesic effect were increased latency in the paw withdrawal and tail-flick tests and decreased paw licking time in the formalin test compared to animals treated with saline (control). Anti-inflammatory activity was measured using a carrageenan-induced paw edema model; the criterion for anti-inflammatory effect was decreased edema compared to control. Blood samples were obtained after animals were sacrificed to assess possible organ toxicity. Statistical analysis was performed with IBM SPSS 20.0. Results: 2-[3-Acetyl-5-(4-chloro-phenyl)-2-methyl-pyrrol-1-yl]-3-(1H-indol-3-yl)-propionic acid had analgesic action against chemical stimulus after single and multiple administration and against thermal stimulus after single administration. Compound 3g significantly suppressed carrageenan-induced paw edema after both single and continuous administration. After continuous administration, hematological tests showed that compound 3g decreased leukocyte and platelet levels and elevated serum creatinine levels. Conclusions: Antinociception with the tested compound is most likely mediated by spinal, peripheral, and anti-inflammatory mechanisms. Possible tolerance of the analgesic action at the spinal level develops after continuous administration. Anti-inflammatory activity is significant and probably the leading cause of antinociception. After multiple administration, compound 3g showed signs of potential nephrotoxicity and antiplatelet activity, as well as suppression of leukocyte levels.
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    Determination of radical scavenging activity of Creatine lysinate against methanol solutions of ABTS
    (2023-01-01) Tsvetkova D.; Kostadinova I.; Vezenkov L.; Marinov L.
    Dietrary Creatine supplements can exert benefits against muscular dystrophic diseases, such as Duchenne muscular dystrophy, myophosphorylase deficiency (McArdle's disease), and fibromyalgia and can provide protection towards neurodegenerative disorders as Huntington, Parkinson and Amyotrophic lateral sclerosis. Creatine supplementation improves cognition and memory and can promote muscle strength. Creatine plays an important role in maintaining heart function in congestive heart failure. The current investigation's goal was to learn more about the ability of creatine lysinate to scavenge ABTS-radicals. Radiation scavenging activity [%], idex of inhibition (IC50), antioxidant power (1/IC50), and Trolox equivalent activity were calculated using the reduction in the absorbance at = 744 nm of the methanol solution of the ABTS-radical. Creatine lysinate (IC50 = 62.8 mM) exhibits an antiradical action, as shown by the experimental findings. According to the available data, creatine lysinate is less active than trolox (IC50 = 0.2 mM), which is because it has a greater IC50 value and less antioxidant capacity (1/IC50, = 0.016) than trolox (1/IC50, = 5). In current investigation was confirmed that ABTS-radical scavenging effect of Creatine lysinate is higher in comparison with Creatine monohydrate (IC50 = 100.98 mM), which was proven by the obtained higher Trolox equivalent antioxidant capacity TEAC = 0.003 of Creatine lysinate, compared with that of Creatine monohydrate (TEAC = 0.002).