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The potential of Fluorine 19F in in Targeted Therapy

100%
Bartusik-Aebisher D., Aebisher D., Podgórski R., Leksa N.
Acta Poloniae Pharmaceutica - Drug Research
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2019
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vol. 76
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issue 6
939-943
EN
Fluorine-19 (19F) can provides critical information about the mobility of the drug and drug uptake in cancer tissue when used together with 19F Magnetic Resonance Imaging (19F MRI) in vitro or in vivo. This review is aimed at the current limitations of drugs such as quantitative visualization during treatments of tumor cells. The main rationale about the utility of 19F MRI is visualization of fluorinated drug and fluorine conjugates on the cellular in vitro and in vivo levels.
2
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Congenital adrenal hyperplasia: clinical symptoms and diagnostic methods

88%
Podgórski R., Aebisher D., Stompor M., Podgórska D., Mazur A.
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2018
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vol. 65
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issue 1
25-33
EN
The aim of this paper is a straightforward presentation of the steroidogenesis process and the most common type of congenital adrenal hyperplasia (CAH) - 21-hydroxylase deficiency - as well as the analytical diagnostic methods that are used to recognize this disease. CAH is a family of common autosomal recessive disorders characterized by impaired adrenal cortisol biosynthesis with associated androgen excess due to a deficiency of one or more enzymes in the steroidogenesis process within the adrenal cortex. The most common and prototypical example of the CAH disorders group (90-95%) is caused by 21-hydroxylase deficiency. Less frequent types of CAH are 11β-hydroxylase deficiency (up to 8% of cases), 17α-hydroxylase deficiency, 3β-hydroxysteroid dehydrogenase deficiency, P450 oxidoreductase deficiency and StAR deficiencies. In the 21-hydroxylase and 11β-hydroxylase deficiency, only adrenal steroidogenesis is affected, whereas a defect in 3β-hydroxysteroid dehydrogenase or 17α-hydroxylase also involves gonadal steroid biosynthesis. Many countries have introduced newborn screening programs based on immunoassays measuring 17-hydroxyprogesterone from blood spots used for other neonatal screening tests which enable faster diagnosis and treatment of CAH. Currently, chromatographic techniques coupled with mass spectrometry are gaining popularity due to an increase in the reliability of the test results.
3
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Synthesis and biological evaluation of 4'-O-acetyl-isoxanthohumol and its analogues as antioxidant and antiproliferative agents

76%
Stompor M., Świtalska M., Podgórski R., Uram Ł., Aebisher D., Wietrzyk J.
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2017
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vol. 64
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issue 3
577-583
EN
Isoxanthohumol (2) and its 4'-O-monoacylated (3) and 7,4'-O-diacetylated (4) derivatives were synthesized and evaluated in vitro for their cytotoxic activity against several cancer cell lines of various origins: MCF-7 (breast), A549 (lung), MESSA (uterine sarcoma), LoVo (colon), drug-resistant human cancer cells (MESSA/DX and LoVo/DX), glioblastoma (U-118 MG), and also towards the non-cancerous cell line MCF-10A (normal breast cells). An antiproliferative assay indicates that 7,4'-di-O-acylisoxanthohumol (4) has similar cytotoxicity to its precursor, isoxanthohumol (2), against selected cell lines (A549, MES-SA, MES-SA/5DX, and U-118 MG). Compound 4 was only slightly more cytotoxic to lung, colon, breast (cancerous and normal) and uterine sarcoma (drug sensitive and drug resistant) cell lines compared to its monoacylated derivative (3). Both acylated isoxanthohumols showed preferential activity against tumor cells (MCF-7) and low cytotoxicity to normal cells (MCF-10A), which suggests selectivity of the acylated isoxanthohumols towards cancer cells. Additionally, the activity of the acylated isoxanthohumols was higher than for 2. To the best of our knowledge this is the first report on bioactivity of monoacylated isoxanthohumol (3) and its ester derivatives as antiproliferative compounds in drug resistant cell cultures. Acylation of 2 decreased the antioxidant activity determined by the DPPH method in the order isoxanthohumol (2) >4'-O-acetylisoxanthohumol (3) >7,4'-di-O-acetylisoxanthohumol (4).
4
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Applications of cytisine extraction and detection in biological materials for clinical medicine

64%
Bartusik-Aebisher D., Aebisher D., Courtney R., Sobczak A., Bober Z., Podgórski R., Kołodziejczyk P., Tutka P.
Acta Poloniae Pharmaceutica - Drug Research
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2019
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vol. 76
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issue 5
797-804
EN
Tobacco use is a leading cause of preventable mortality worldwide. New cost-effective smoking cessation treatments are needed especially in some low-to-middle income countries where smoking rates are rising, and current pharmacotherapy treatments remain cost-prohibitive. Since the 1960’s, cytisine has been used as an effective nicotine substitution agent to aid in smoking cessation albeit limited to a selected few Eastern/Central Europe and Central Asian countries. Cytisine is a biologically active alkaloid of plant origin and is known to be a ligand of nicotinic acetylcholinergic receptors (nAChRs). For several decades, the properties of cytisine have been investigated and reported in the biomedical and pharmaceutical literature. Due to the beneficial impact of cytisine on smoking cessation and its costly multistep synthesis, there is a growing interest in extraction from natural sources as well as in analytical identification and quantification for clinical medicine and forensic toxicology. In this paper, we present several current analytical approaches to cytisine extraction and identification from biological samples of plant and human origin. The development of extraction techniques will allow for the widespread use of the drug in experimental and clinical pharmacology, toxicology and forensic medicine.
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