SrasV1, Main, Exploration, bibRecord, 002458

SARS-CoV 3CLpro inhibitory effects of quinone-methide triterpenes from Tripterygium regelii.

Identifieur interne : 002458 ( Main/Exploration ); précédent : 002457; suivant : 002459

SARS-CoV 3CLpro inhibitory effects of quinone-methide triterpenes from Tripterygium regelii.

Auteurs : Young Bae Ryu [Corée du Sud] ; Su-Jin Park ; Young Min Kim ; Ju-Yeon Lee ; Woo Duck Seo ; Jong Sun Chang ; Ki Hun Park ; Mun-Chual Rho ; Woo Song Lee

Source :

Bioorganic & medicinal chemistry letters [ 1464-3405 ] ; 2010.

RBID : pubmed:20167482

Descripteurs français

KwdFr :
- Antiviraux (pharmacologie), Benzoquinones (), Extraits de plantes (pharmacologie), Modèles moléculaires, Tripterygium (), Triterpènes (), Triterpènes (pharmacologie), Virus du SRAS ().
MESH :
- pharmacologie : Antiviraux, Extraits de plantes, Triterpènes.
- Benzoquinones, Modèles moléculaires, Tripterygium, Triterpènes, Virus du SRAS.

English descriptors

KwdEn :
- Antiviral Agents (pharmacology), Benzoquinones (chemistry), Models, Molecular, Plant Extracts (pharmacology), SARS Virus (drug effects), Tripterygium (chemistry), Triterpenes (chemistry), Triterpenes (pharmacology).
MESH :
- chemical , chemistry : Benzoquinones, Triterpenes.
- chemical , pharmacology : Antiviral Agents, Plant Extracts, Triterpenes.
- chemistry : Tripterygium.
- drug effects : SARS Virus.
- Models, Molecular.

Abstract

Quinone-methide triterpenes, celastrol (1), pristimerin (2), tingenone (3), and iguesterin (4) were isolated from Triterygium regelii and dihydrocelastrol (5) was synthesized by hydrogenation under palladium catalyst. Isolated quinone-methide triterpenes (1-4) and 5 were evaluated for SARS-CoV 3CL(pro) inhibitory activities and showed potent inhibitory activities with IC(50) values of 10.3, 5.5, 9.9, and 2.6 microM, respectively, whereas the corresponding 5 having phenol moiety was observed in low activity (IC(50)=21.7 microM). As a result, quinone-methide moiety in A-ring and more hydrophobic E-ring assist to exhibit potent activity. Also, all quinone-methide triterpenes 1-4 have proven to be competitive by the kinetic analysis.

DOI: 10.1016/j.bmcl.2010.01.152
PubMed: 20167482

Affiliations:

Corée du Sud

Le document en format XML

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<front><div type="abstract" xml:lang="en">Quinone-methide triterpenes, celastrol (1), pristimerin (2), tingenone (3), and iguesterin (4) were isolated from Triterygium regelii and dihydrocelastrol (5) was synthesized by hydrogenation under palladium catalyst. Isolated quinone-methide triterpenes (1-4) and 5 were evaluated for SARS-CoV 3CL(pro) inhibitory activities and showed potent inhibitory activities with IC(50) values of 10.3, 5.5, 9.9, and 2.6 microM, respectively, whereas the corresponding 5 having phenol moiety was observed in low activity (IC(50)=21.7 microM). As a result, quinone-methide moiety in A-ring and more hydrophobic E-ring assist to exhibit potent activity. Also, all quinone-methide triterpenes 1-4 have proven to be competitive by the kinetic analysis.</div>
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<name sortKey="Lee, Ju Yeon" sort="Lee, Ju Yeon" uniqKey="Lee J" first="Ju-Yeon" last="Lee">Ju-Yeon Lee</name>
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Serveur d'exploration SRAS

SARS-CoV 3CLpro inhibitory effects of quinone-methide triterpenes from Tripterygium regelii.

SARS-CoV 3CLpro inhibitory effects of quinone-methide triterpenes from Tripterygium regelii.

Source :

Descripteurs français

English descriptors

Abstract

Links toward previous steps (curation, corpus...)

Le document en format XML

Pour manipuler ce document sous Unix (Dilib)

Pour mettre un lien sur cette page dans le réseau Wicri

Pour générer des pages wiki

	Serveur d'exploration SRAS
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