Constituents of talisia nervosa with potential utility against metabolic syndrome
- Format
- Article
- Status
- publishedVersion
- Description
This study is focused on the isolation and characterization of bioactive secondary metabolites from the ethanolic extract of stems of the Panamanian plant Talisia nervosa Radlk, through a series of target-based cellular assays related to the metabolic syndrome (MetS): a combination of type 2 Diabetes Mellitus (T2DM), hypercholesterolemia, inflammation, and obesity. Bioassay guided fractionation allowed the isolation of four known compounds: (–)-catechin (1), methyl gallate (2), ethyl gallate (3), and ß-D-glucopyranose,1,4,6-tris(3,4,5-trihydroxybenzoate) (4). This is the first report of (–)-catechin (1) and ß-Dglucopyranose,1,4,6-tris (3,4,5-trihydroxybenzoate) (4) from T. nervosa. Among the isolates, 1 activated PPAR, but had no effect on PPAR. Compounds 2 - 4 activated PPAR, PPAR and LXR. Interestingly, 2 was stronger than 3 towards all three targets. Methyl gallate (2) showed the most potent effect toward both PPAR and PPAR with an increase of 3.0 and 13-fold, respectively, while 4 was most potent in activating LXR with a fold induction of 5.3 at concentrations of 100 µg/mL. The nitric oxide (NO) production was reduced by compounds 2 and 3 with IC50 values of 7.0 and 7.5 μg/mL, respectively. ß-Dglucopyranose,1,4,6-tris (3,4,5-trihydroxybenzoate) (4) did not cause a significant increase in adipogenesis despite its strong PPARγ agonistic action (8.6-fold increase) and may represent a good candidate for the treatment of MetS without the undesirable side effect of weight gain.
- Publication Year
- 2019
- Language
- Topic
- QK Botany
R Medicine (General)
RM Therapeutics. Pharmacology
- Repository
- RI Digital de la Universidad de Panamá
- Get full text
- http://up-rid.up.ac.pa/6891/1/yelkaira_vasquez.pdf
- Rights
- openAccess
- License
- cc_by_nc_sa_4