Back to Search
Start Over
Potent antitrypanosomal triterpenoid saponins from Mussaenda luteola.
- Source :
-
Fitoterapia [Fitoterapia] 2015 Dec; Vol. 107, pp. 114-121. Date of Electronic Publication: 2015 Oct 30. - Publication Year :
- 2015
-
Abstract
- Five new triterpenoid saponins, heinsiagenin A 3-O-[α-l-rhamnopyranosyl-(1→2)-β-d-glucopyranosyl-(1→2)]-β-d-glucopyranoside (1), heinsiagenin A 3-O-[α-l-rhamnopyranosyl-(1→2)-β-d-glucopyranosyl-(1→2)]-[β-d-glucopyranosyl-(1→4)]-β-d-glucopyranoside (2), 2α-hydroxyheinsiagenin A 3-O-[α-l-rhamnopyranosyl-(1→2)-β-d-glucopyranosyl-(1→2)]-β-d-glucopyranoside (3), 2α-hydroxyheinsiagenin A 3-O-[β-d-glucopyranosyl-(1→2)]-[β-d-glucopyranosyl-(1→4)]-β-d-glucopyranoside (4) and N-(2S, 3R, 4R-3-methyl-4-pentanolid-2-yl)-18-hydroxylanosta-8 (9), 22E, 24E-trien-27-amide-3-O-[α-l-rhamnopyranosyl-(1→2)-β-d-glucopyranosyl-(1→2)]-[β-d-glucopyranosyl-(1→4)]-β-d-glucopyranoside (5) were isolated from the aerial parts of Mussaenda luteola Delile (Rubiaceae). Structural elucidation was based on the analysis of spectroscopic data (1D and 2D NMR) and HR-ESI-MS. Compound 1 showed potent antitrypanosomal activity with an IC50 value of 8.80μM. Compounds 2-4 showed highly potent antitrypanosomal activity with IC50 values ranging between (2.57-2.84μM) and IC90 values ranging between (3.36-4.35μM), which are 5 fold greater than the positive control DFMO (IC50 and IC90 values of 13.06 and 28.99μM, respectively). Compounds 1 and 2 showed moderate affinity to μ-opioid receptors with Ki values of 9.936μM and 0.872μM, respectively compared to a Ki value of 1.958nM for the positive control, naloxone HCl.<br /> (Copyright © 2015 Elsevier B.V. All rights reserved.)
- Subjects :
- Antiprotozoal Agents isolation & purification
Leishmania donovani drug effects
Molecular Structure
Plant Extracts chemistry
Saponins isolation & purification
Triterpenes isolation & purification
Trypanosoma brucei brucei drug effects
Antiprotozoal Agents chemistry
Rubiaceae chemistry
Saponins chemistry
Triterpenes chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1873-6971
- Volume :
- 107
- Database :
- MEDLINE
- Journal :
- Fitoterapia
- Publication Type :
- Academic Journal
- Accession number :
- 26524249
- Full Text :
- https://doi.org/10.1016/j.fitote.2015.10.011