Albanian
Arabic
Armenian
Azerbaijani
Belarusian
Bengali
Bosnian
Catalan
Czech
Danish
Deutsch
Dutch
English
Estonian
Finnish
Français
Greek
Haitian Creole
Hebrew
Hindi
Hungarian
Icelandic
Indonesian
Irish
Italian
Japanese
Korean
Latvian
Lithuanian
Macedonian
Mongolian
Norwegian
Persian
Polish
Portuguese
Romanian
Russian
Serbian
Slovak
Slovenian
Spanish
Swahili
Swedish
Turkish
Ukrainian
Vietnamese
Български
中文(简体)
中文(繁體)
Bioorganic and Medicinal Chemistry 2010-Feb

11beta-Hydroxysteroid dehydrogenase 1 inhibiting constituents from Eriobotrya japonica revealed by bioactivity-guided isolation and computational approaches.

Samo registrirani korisnici mogu prevoditi članke
Prijava Registriraj se
Veza se sprema u međuspremnik
Judith M Rollinger
Denise V Kratschmar
Daniela Schuster
Petra H Pfisterer
Christel Gumy
Evelyne M Aubry
Sarah Brandstötter
Hermann Stuppner
Gerhard Wolber
Alex Odermatt

Ključne riječi

Sažetak

The inhibition of 11beta-hydroxysteroid dehydrogenase 1 (11beta-HSD1), which catalyzes the conversion of inactive 11-ketoglucocorticoids to active 11beta-hydroxyglucocorticoids, emerged as promising strategy to treat symptoms of the metabolic syndrome, including obesity and type 2 diabetes. In this study the leaves of the anti-diabetic medicinal plant loquat (Eriobotrya japonica) were phytochemically investigated following hints from a pharmacophore-based virtual screening and a bioactivity-guided approach. Determination of the 11beta-HSD1 and 11beta-HSD2 inhibitory activities in cell lysates revealed triterpenes from the ursane type as selective, low micro-molar inhibitors of 11beta-HSD1, that is, corosolic acid (1), 3-epicorosolic acid methyl ester (4), 2-alpha hydroxy-3-oxo urs-12-en-28-oic acid (6), tormentic acid methyl ester (8), and ursolic acid (9). Importantly, a mixture of loquat constituents with moderate activities displayed a pronounced additive effect. By means of molecular modeling studies and the identification of the 11beta-HSD1-inhibiting 11-keto-ursolic acid (17) and 3-acetyl-11-keto-ursolic acid (18) a structure-activity relationship was deduced for this group of pentacyclic triterpenes. The mechanism of action elucidated in the present work together with the previously determined pharmacological activities provides these natural products with an astonishing multi-targeted anti-diabetic profile.

Pridružite se našoj
facebook stranici

Najkompletnija baza ljekovitog bilja potpomognuta znanošću

  • Radi na 55 jezika
  • Biljni lijekovi potpomognuti znanošću
  • Prepoznavanje bilja slikom
  • Interaktivna GPS karta - označite bilje na mjestu (uskoro)
  • Pročitajte znanstvene publikacije povezane s vašom pretragom
  • Pretražite ljekovito bilje po učincima
  • Organizirajte svoje interese i budite u toku s istraživanjem vijesti, kliničkim ispitivanjima i patentima

Upišite simptom ili bolest i pročitajte o biljkama koje bi mogle pomoći, unesite travu i pogledajte bolesti i simptome protiv kojih se koristi.
* Svi podaci temelje se na objavljenim znanstvenim istraživanjima

Google Play badgeApp Store badge