Potent antitrypanosomal triterpenoid saponins from Mussaenda luteola.

ABSTRACT: Five new triterpenoid saponins, heinsiagenin A 3-O-[?-l-rhamnopyranosyl-(1?2)-?-d-glucopyranosyl-(1?2)]-?-d-glucopyranoside (1), heinsiagenin A 3-O-[?-l-rhamnopyranosyl-(1?2)-?-d-glucopyranosyl-(1?2)]-[?-d-glucopyranosyl-(1?4)]-?-d-glucopyranoside (2), 2?-hydroxyheinsiagenin A 3-O-[?-l-rhamnopyranosyl-(1?2)-?-d-glucopyranosyl-(1?2)]-?-d-glucopyranoside (3), 2?-hydroxyheinsiagenin A 3-O-[?-d-glucopyranosyl-(1?2)]-[?-d-glucopyranosyl-(1?4)]-?-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-[?-l-rhamnopyranosyl-(1?2)-?-d-glucopyranosyl-(1?2)]-[?-d-glucopyranosyl-(1?4)]-?-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 8.80?M. Compounds 2-4 showed highly potent antitrypanosomal activity with IC50 values ranging between (2.57-2.84?M) and IC90 values ranging between (3.36-4.35?M), which are 5 fold greater than the positive control DFMO (IC50 and IC90 values of 13.06 and 28.99?M, respectively). Compounds 1 and 2 showed moderate affinity to ?-opioid receptors with Ki values of 9.936?M and 0.872?M, respectively compared to a Ki value of 1.958nM for the positive control, naloxone HCl.

SUBMITTER: Mohamed SM 

PROVIDER: S-EPMC4883117 | biostudies-literature | 2015 Dec

REPOSITORIES: biostudies-literature