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Diethoxyphosphoryloxy-oleanolic acid is a nanomolar-inhibitor of butyrylcholinesterase.
Petrova, Anastasiya V; Poptsov, Alexandr I; Heise, Niels V; Csuk, René; Kazakova, Oxana B.
Affiliation
  • Petrova AV; Ufa Institute of Chemistry, Ufa Federal Research Centre, Russian Academy of Science, Ufa, Russia.
  • Poptsov AI; Ufa Institute of Chemistry, Ufa Federal Research Centre, Russian Academy of Science, Ufa, Russia.
  • Heise NV; Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Halle (Saale), Germany.
  • Csuk R; Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Halle (Saale), Germany.
  • Kazakova OB; Ufa Institute of Chemistry, Ufa Federal Research Centre, Russian Academy of Science, Ufa, Russia.
Chem Biol Drug Des ; 103(3): e14506, 2024 03.
Article in En | MEDLINE | ID: mdl-38480508
ABSTRACT
A series of new betulin, lupeol, erythrodiol, and oleanolic acid phosphoryloxy- and furoyloxy-derivatives has been synthesized and their structure was confirmed by NMR spectroscopy. Synthesized compounds were subjected to Ellman's assays to determine their ability to inhibit the enzymes AChE and BChE. Among them, diethoxyphosphoryloxy-oleanolic acid inhibited BChE with a value of 99%, thereby acting as a mixed-type inhibitor holding very low Ki values of Ki = 6.59 nM and Ki ' = 1.97 nM, respectively.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Oleanolic Acid / Triterpenes Language: En Journal: Chem Biol Drug Des Journal subject: BIOQUIMICA / FARMACIA / FARMACOLOGIA Year: 2024 Document type: Article Affiliation country: Rusia

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Oleanolic Acid / Triterpenes Language: En Journal: Chem Biol Drug Des Journal subject: BIOQUIMICA / FARMACIA / FARMACOLOGIA Year: 2024 Document type: Article Affiliation country: Rusia