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Wyświetlanie 1-3 z 3
Tytuł:
Biokoniugaty antybiotykow jonoforowych : cele, strategie syntezy i właściwości
Bioconjugates of ionophore antibiotics : goals, synthesis strategies and properties
Autorzy:
Antoszczak, M.
Kordylas, M.
Huczyński, A.
Powiązania:
https://bibliotekanauki.pl/articles/172178.pdf
Data publikacji:
2018
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
antybiotyki jonoforowe
jonofory
biokoniugacja
hybrydy
aktywność przeciwbakteryjna
aktywność przeciwnowotworowa
ionophore antibiotics
ionophores
bioconjugation
hybrids
antibacterial
activity
anticancer activity
Opis:
Polyether ionophore antibiotics (ionophores) represent a large group of naturally- occurring lipophilic compounds which are able to form complexes with the metal cations and transport them across the lipid membranes. This process disturbs the intercellular Na+/K+ concentration gradient and intracellular pH, and leads to the mitochondrial damages, cell swelling, vacuolization and finally to apoptosis process. For this reason, ionophores are commonly used in veterinary medicine as the non-hormonal growth-promoting as well as coccidiostatic agents. In this group particularly interesting are monensin and salinomycin (Fig. 1) because of their proved anti-tumour activity, including efficiency against multidrug- -resistant cancer cells and cancer stem cells of different origin. Improved synthetic derivatives of both polyether ionophores are thus of considerable current interest. Selective derivatization of these structures whose display multiple reactive functional groups and, in the case of salinomycin, a sensitive tricyclic spiroketal ring system is however non-trivial. Even so, semi-synthetic analogs reported to date includes i.a. selective derivatization of the carboxyl group, the three hydroxyl groups, the ketone group, the alkene, and epimerization of the characteristic tricyclic salinomycin unit (for more details see: M. Antoszczak, A. Huczyński, B. Brzezinski, Wiad. Chem., 2017, 71, 629). On the other hand, as part of the original program to develop innovatory anti- -cancer pro-drugs and prompted by the idea that cancer cells may be individually effectively killed by monensin and salinomycin, a very interesting direction of research is bioconjugation of these ionophores. In this context, our review article is focused on the possible role of hybrids of both ionophore antibiotics with other biologically active substances (natural amino acids, Cinchona alkaloids, flavonoids, nucleosides) in anti-bacterial and anti-cancer treatment, and gives an overview of their properties.
Źródło:
Wiadomości Chemiczne; 2018, 72, 1-2; 1-28
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Synteza i aktywność biologiczna pochodnych salinomycyny
Synthesis and biological activity of salinomycin derivatives
Autorzy:
Antoszczak, M.
Huczyński, A.
Brzezinski, B.
Powiązania:
https://bibliotekanauki.pl/articles/171728.pdf
Data publikacji:
2017
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
antybiotyki jonoforowe
jonofory
struktura molekularna
aktywność przeciwbakteryjna
aktywność przeciwnowotworowa
ionophore antibiotics
ionophores
molecular structure
antibacterial activity
anticancer activity
Opis:
Polyether ionophore antibiotics (ionophores) represent a large group of naturally- occurring lipid-soluble compounds isolated from actinomycetes strains of Streptomyces genus. Ionophores are able to form complexes with the metal cations, especially sodium and potassium, and transport them across the lipid membranes according to electroneutral or electrogenic transport mechanism. This process disturbs the intercellular Na+/K+ concentration gradient and intracellular pH, leads to the mitochondrial injuries, cell swelling, vacuolization and finally to programmed cell death (apoptosis). For this reason, ionophore antibiotics found commercial use in veterinary medicine as coccidiostatic agents and non-hormonal growth promoters. In addition to the industrial use of ionophores, some of them effectively and selectively inhibit properties of different cancer cells as well as enhance the anti-cancer effects of radio- and/or chemotherapy. In this group, particularly interesting is salinomycin because of its potent anti-microbial and anti-cancer activity, including efficiency against multi-drug resistant cancer cells and cancer stem cells. A very interesting direction of research is the chemical modification of ionophore antibiotics, which can lead to obtaining various derivatives with better biological activity and lower toxicity than those of the starting substances. Because biological activity of ionophore antibiotics and their derivatives is strictly connected with the ability to form characteristic pseudocyclic structures around the complexed cations (host-guest complex), it is also important to establish the detailed information on these structures. In this context, our review article is focused on the possible role of salinomycin and its derivatives in anti-microbial as well as anti-cancer therapy, and gives an overview of the properties of this antibiotic.
Źródło:
Wiadomości Chemiczne; 2017, 71, 7-8; 629-661
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Zastosowanie chemii "klik" do syntezy biokoniugatów salinomycyny
Application of the click chemistry for the synthesis of salinomycin bioconjugates
Autorzy:
Sulik, Michał
Antoszczak, Michał
Huczyński, Adam
Powiązania:
https://bibliotekanauki.pl/articles/2200436.pdf
Data publikacji:
2022
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
salinomycyna
jonofory
biokoniugacja
chemia click
aktywność przeciwnowotworowa
chemia klik
salinomycin
ionophores
bioconjugation
click chemistry
anticancer activity
Opis:
Bioconjugation is a well-known method of designing new drug candidates for many different diseases, including cancer. The idea of the process is to join two or more bioactive molecules by means of a covalent bond. Thus, obtained hybrids often exhibit higher efficiency compared to that of the starting compounds. Recently, the use of click chemistry, especially Huisgen 1,3-dipolar cycloaddition, has attracted much attention for the synthesis of bioconjugates of natural compounds. The great advantage of this reaction is its high yield and enzymatic stability of the 1,2,3-triazole ring. Mild conditions of this reaction guarantee that it can be used to modify compounds with low stability, such as salinomycin – a representative of ionophore antibiotics. Salinomycin is a naturally occurring lipophilic compound isolated from Streptomyces albus. It is capable of forming complexes with metal cations and transport them across the lipid membranes. This process disturbs the intercellular Na+ /K+ concentration gradient and leads to apoptosis (programmed cell death). Salinomycin exhibits high anticancer activity, including efficiency against multidrug-resistant cancer cells and cancer stem cells of different origin. Chemical modification of the salinomycin skeleton to increase its biological activity is a very interesting research direction. Our review article is focused on the application of click chemistry for the synthesis of salinomycin bioconjugates with many different biologically active compounds (Cinchona alkaloids, nucleosides, triphenylphosphonium cation, betulinic acid and other ionophore antibiotics). Some of the obtained hybrids exhibit higher efficiency compared to that of the starting compounds, e.g., increased anticancer activity, the ability to overcome multi-drug resistance, or improved ionophoretic properties. These results are a good starting point for further research on the use of click chemistry in the synthesis of highly functional hybrids of natural compounds.
Źródło:
Wiadomości Chemiczne; 2022, 76, 11-12; 883--907
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
Dostawca treści:
Biblioteka Nauki
Artykuł
    Wyświetlanie 1-3 z 3

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