| In vitro |
Gypsogenin (1) was obtained by acidic hydrolysis from its saponin.?While the parent compound 1 acted as a selective inhibitor for butyrylcholinesterase (from equus) possessing a moderate mixed-type inhibition of the enzyme, Ki values as low as 2.67 0.59 μM were determined for (3β,4α) 3-O-acetyl-olean-12-ene-23,28-dinitrile (11) and acetylcholinesterase (AChE, from electric eel).?Thus, 11 possesses one-fifth of the inhibitory activity of the 'gold standard' galantamine hydrobromide;?this compound is one of the first pentacyclic triterpenoids described as a potent AChE-selective inhibitor |
| References |
1. Heller L , Schwarz S , Weber B A , et al. Gypsogenin Derivatives: An Unexpected Class of Inhibitors of Cholinesterases[J]. Archiv Der Pharmazie, 2015, 347(10):707-716. 2. Ciftci HI, Ozturk SE, Ali TFS, Radwan MO, Tateishi H, Koga R, Ocak Z, Can M, Otsuka M, Fujita M. The First Pentacyclic Triterpenoid Gypsogenin Derivative Exhibiting Anti-ABL1 Kinase and Anti-chronic Myelogenous Leukemia Activities. Biol Pharm Bull. 2018 Apr 1;41(4):570-574. doi: 10.1248/bpb.b17-00902. Epub 2018 Jan 30. PubMed PMID: 29386476. 3. Qu YF, Gao JY, Wang J, Geng YM, Zhou Y, Sun CX, Li F, Feng L, Yu MJ, Wang GS. New Triterpenoid Saponins from the Herb Hylomecon japonica. Molecules. 2017 Oct 23;22(10). pii: E1731. doi: 10.3390/molecules22101731. PubMed PMID: 29065554. 4. Smułek W, Zdarta A, Pacholak A, Zgoła-Grześkowiak A, Marczak Ł, Jarzębski M, Kaczorek E. Saponaria officinalis L. extract: Surface active properties and impact on environmental bacterial strains. Colloids Surf B Biointerfaces. 2017 Feb 1;150:209-215. doi: 10.1016/j.colsurfb.2016.11.035. Epub 2016 Nov 27. PubMed PMID: 27918965. |
