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Semisynthetic teicoplanin derivatives with dual antimicrobial activity against SARS-CoV-2 and multiresistant bacteria
ID
Bereczki, Ilona
(
Avtor
),
ID
Vimberg, Vladimir
(
Avtor
),
ID
Lőrincz, Eszter
(
Avtor
),
ID
Papp, Henrietta
(
Avtor
),
ID
Nagy, Lajos
(
Avtor
),
ID
Kéki, Sándor
(
Avtor
),
ID
Batta, Gyula
(
Avtor
),
ID
Mitrović, Ana
(
Avtor
),
ID
Kos, Janko
(
Avtor
),
ID
Zsigmond, Áron
(
Avtor
)
PDF - Predstavitvena datoteka,
prenos
(1,83 MB)
MD5: D8518A7A5581B8E5AC8A9B7B7FBCF431
URL - Izvorni URL, za dostop obiščite
https://www.nature.com/articles/s41598-022-20182-y
Galerija slik
Izvleček
Patients infected with SARS-CoV-2 risk co-infection with Gram-positive bacteria, which severely affects their prognosis. Antimicrobial drugs with dual antiviral and antibacterial activity would be very useful in this setting. Although glycopeptide antibiotics are well-known as strong antibacterial drugs, some of them are also active against RNA viruses like SARS-CoV-2. It has been shown that the antiviral and antibacterial efficacy can be enhanced by synthetic modifications. We here report the synthesis and biological evaluation of seven derivatives of teicoplanin bearing hydrophobic or superbasic side chain. All but one teicoplanin derivatives were effective in inhibiting SARS-CoV-2 replication in VeroE6 cells. One lipophilic and three perfluoroalkyl conjugates showed activity against SARS-CoV-2 in human Calu-3 cells and against HCoV-229E, an endemic human coronavirus, in HEL cells. Pseudovirus entry and enzyme inhibition assays established that the teicoplanin derivatives efficiently prevent the cathepsin-mediated endosomal entry of SARS-CoV-2, with some compounds inhibiting also the TMPRSS2-mediated surface entry route. The teicoplanin derivatives showed good to excellent activity against Gram-positive bacteria resistant to all approved glycopeptide antibiotics, due to their ability to dually bind to the bacterial membrane and cell-wall. To conclude, we identified three perfluoralkyl and one monoguanidine analog of teicoplanin as dual inhibitors of Gram-positive bacteria and SARS-CoV-2.
Jezik:
Angleški jezik
Vrsta gradiva:
Članek v reviji
Tipologija:
1.01 - Izvirni znanstveni članek
Organizacija:
FFA - Fakulteta za farmacijo
Status publikacije:
Objavljeno
Različica publikacije:
Objavljena publikacija
Leto izida:
2022
Št. strani:
15 str.
Številčenje:
Vol. 12, art. 16001
PID:
20.500.12556/RUL-141440
UDK:
578.834:615.015.8
ISSN pri članku:
2045-2322
DOI:
10.1038/s41598-022-20182-y
COBISS.SI-ID:
123460611
Datum objave v RUL:
29.09.2022
Število ogledov:
616
Število prenosov:
77
Metapodatki:
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Objavi na:
Gradivo je del revije
Naslov:
Scientific reports
Skrajšan naslov:
Sci. rep.
Založnik:
Nature Publishing Group
ISSN:
2045-2322
COBISS.SI-ID:
18727432
Licence
Licenca:
CC BY 4.0, Creative Commons Priznanje avtorstva 4.0 Mednarodna
Povezava:
http://creativecommons.org/licenses/by/4.0/deed.sl
Opis:
To je standardna licenca Creative Commons, ki daje uporabnikom največ možnosti za nadaljnjo uporabo dela, pri čemer morajo navesti avtorja.
Sekundarni jezik
Jezik:
Slovenski jezik
Ključne besede:
protimikrobne snovi
,
večkratno odporne bakterije
,
SARS-CoV
Projekti
Financer:
ARRS - Agencija za raziskovalno dejavnost Republike Slovenije
Številka projekta:
P4-0127-2019
Naslov:
Farmacevtska biotehnologija: znanost za zdravje
Financer:
Drugi - Drug financer ali več financerjev
Program financ.:
National Research, Development and Innovation Office of Hungary
Številka projekta:
K 132870
Financer:
Drugi - Drug financer ali več financerjev
Program financ.:
Hungary, National Research, Development and Innovation Office
Številka projekta:
TKP2021-NVA-07 and TKP2021-EGA-13
Financer:
Drugi - Drug financer ali več financerjev
Program financ.:
European Regional Development Fund (European Union) and the Government of Spain
Financer:
Drugi - Drug financer ali več financerjev
Program financ.:
VimbergV Fund
Številka projekta:
CZ.02.1.01/0.0/0.0/16_ 019/0000729
Financer:
Drugi - Drug financer ali več financerjev
Program financ.:
United Kingdom, Foreign Commonwealth and Development Office
Številka projekta:
201832-30 and 202135-30
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