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Prijava
Natural apocarotenoids and their synthetic glycopeptide conjugates inhibit SARS-CoV-2 replication
ID
Bereczki, Ilona
(
Avtor
),
ID
Kos, Janko
(
Avtor
),
ID
Herczegh, Pál
(
Avtor
),
ID
Borbás, Anikó
(
Avtor
), et al.
PDF - Predstavitvena datoteka,
prenos
(2,46 MB)
MD5: 608FB1C8455CF41F0BB58187C44CB5BA
URL - Izvorni URL, za dostop obiščite
https://www.mdpi.com/1424-8247/14/11/1111
Galerija slik
Izvleček
The protracted global COVID-19 pandemic urges the development of new drugs against the causative agent SARS-CoV-2. The clinically used glycopeptide antibiotic, teicoplanin, emerged as a potential antiviral, and its efficacy was improved with lipophilic modifications. This prompted us to prepare new lipophilic apocarotenoid conjugates of teicoplanin, its pseudoaglycone and the related ristocetin aglycone. Their antiviral effect was tested against SARS-CoV-2 in Vero E6 cells, using a cell viability assay and quantitative PCR of the viral RNA, confirming their micromolar inhibitory activity against viral replication. Interestingly, two of the parent apocarotenoids, bixin and β-apo-8′carotenoic acid, exerted remarkable anti-SARS-CoV-2 activity. Mechanistic studies involved cathepsin L and B, as well as the main protease 3CLPro, and the results were rationalized by computational studies. Glycopeptide conjugates show dual inhibitory action, while apocarotenoids have mostly cathepsin B and L affinity. Since teicoplanin is a marketed antibiotic and the natural bixin is an approved, cheap and widely used red colorant food additive, these readily available compounds and their conjugates as potential antivirals are worthy of further exploration.
Jezik:
Angleški jezik
Ključne besede:
teicoplanin
,
ristocetin
,
bixin
,
crocetin
,
β-apocarotenoic acid
,
SARS-CoV-2
,
antiviral activity
,
antibacterial activity
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:
2021
Št. strani:
25 str.
Številčenje:
Vol. 14, iss. 11, art. 1111
PID:
20.500.12556/RUL-136426
UDK:
577
ISSN pri članku:
1424-8247
DOI:
10.3390/ph14111111
COBISS.SI-ID:
83004931
Datum objave v RUL:
03.05.2022
Število ogledov:
1274
Število prenosov:
86
Metapodatki:
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Objavi na:
Gradivo je del revije
Naslov:
Pharmaceuticals
Skrajšan naslov:
Pharmaceuticals
Založnik:
MDPI
ISSN:
1424-8247
COBISS.SI-ID:
517582617
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.
Začetek licenciranja:
01.11.2021
Projekti
Financer:
EC - European Commission
Program financ.:
European Regional Development Fund
Številka projekta:
GINOP-2.3.2-15-2016-00044
Financer:
EC - European Commission
Program financ.:
European Regional Development Fund
Številka projekta:
GINOP-2.3.4-15-2020-00008
Financer:
Drugi - Drug financer ali več financerjev
Program financ.:
Hungary, National Research, Development and Innovation Office
Številka projekta:
K 131493
Financer:
Drugi - Drug financer ali več financerjev
Program financ.:
Hungary, National Research, Development and Innovation Office
Številka projekta:
KH129599
Financer:
EC - European Commission
Program financ.:
ERDF/ESF
Številka projekta:
CZ.02.1.01/0.0/0.0/16_019/0000729
Akronim:
ChemBioDrug
Financer:
ARRS - Agencija za raziskovalno dejavnost Republike Slovenije
Številka projekta:
P4-0127
Naslov:
Farmacevtska biotehnologija: znanost za zdravje
Financer:
Drugi - Drug financer ali več financerjev
Program financ.:
Hungarian Academy of Sciences, János Bolyai Research Scholarship
Financer:
Drugi - Drug financer ali več financerjev
Program financ.:
Ministry for Innovation and Technology, ÚNKP New National Excellence Program
Financer:
Drugi - Drug financer ali več financerjev
Program financ.:
United Kingdom, Foreign Commonwealth and Development Office
Financer:
EC - European Commission
Program financ.:
European Social Fund
Številka projekta:
EFOP-3.6.1.-16-2016-00004
Naslov:
Comprehensive Development for Implementing Smart Specialization Strategies at the University of Pécs
Financer:
Drugi - Drug financer ali več financerjev
Program financ.:
Hungary, Ministry for Innovation and Technology
Številka projekta:
TUDFO/47138/2019-ITM
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