Bratisl Med J
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In silico and in vitro studies of Tyr-Lys-Thr tripeptide against human lung cancer cell line (A549).
The main purpose of this study is to predict the effect of Tyr-Lys-Thr (YKT) tripeptide, recognized for its anticancer properties, on lung cancer through theoretical and experimental analyzes. ⋯ In silico docking studies were conducted with PI3K, Akt1, and mTOR, known to be active in human cancer, as well as caspase-3 and caspase-8, key enzymes in apoptosis. It was determined that YKT exhibited a robust binding tendency with each receptor. YKT tripeptide was also found to have a cytotoxic effect on human lung carcinoma cell line A549 (Tab. 5, Fig. 11, Ref. 28).
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To create a new mucoadhesive dosage form based on PluronicF127 followed by transformation into a gel form upon intranasal administration for targeted delivery to brain tissueMETHODS: Citicoline, cytidine diphosphocholine, designated as CDP-choline, was purchased as a white powder with the molecular weight of 510.31 g/mol. The triblock copolymers of polyethylene glycol-block-polypropylene glycol-block-polyethylene glycol (PEG-PPG-PEG), branded as Pluronic F127, was used. ⋯ The polymer's gelling and adhesive properties performed well, which is crucial for further research at the preclinical stage (Tab. 1, Fig. 5, Ref. 28).
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The study aims to investigate how changes in the conductance of axonal (Na+) and calcium (Ca2+) ion channels affect the generation, course, excitability and firing rate of action potentials in a model of Purkinje cell neurons. ⋯ Our findings demonstrate that alterations in ion channel conductance influence the timing and generation of action potentials, suggesting that magnetic fields can modulate neuronal behaviour (Tab. 4, Fig. 12, Ref. 34). Text in PDF www.elis.sk Keywords: axon, ion channels, conductance, action potential, magnetic field, Purkinje cell.
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We aimed to investigate the possible cardioprotective effects of paricalcitol (PR), its vitamin D receptor agonist, and vitamin D3 (VIT-D3) on an experimental model of doxorubicin (DX) cardiotoxicity by 99mTc-PYP scintigraphy, electrocardiographic (ECG) and biochemical methods. ⋯ Results show that vitamin D receptor agonist paricalcitol and vitamin D protect against DX-induced cardiotoxicity through anti-inflammatory and antioxidant effects (Fig. 4, Ref. 59). Text in PDF www.elis.sk Keywords: paricalcitol, doxorubicin, vitamin D, ECG, 99mTc-PYP scintigraphy, cardiotoxicity, inflammation.
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In the present study, two structurally similar alkaloids from trees of Cinchona genus, chloroquine and cinchonine, were examined for their vasorelaxant effects in a model of phenylephrine-induced smooth muscle contractions. ⋯ Molecular docking studies predicted that chloroquine possesses a significant activity toward a suitable model of LTCCs, while cinchonine does not. The results of the present study point to the fact that great caution should be paid while administering chloroquine to vulnerable patients, especially those with cardiovascular disorders (Tab. 3, Fig. 3, Ref. 28).