In the course of our research on the oligoglycosidic constituents of Turkis
h Astragalus species, we have isolated a number of cycloartane-type triterp
ene glycosides. The current study examines the immunostimulatory effects of
nineteen of these cycloartane-type compounds using a transcription-based b
ioassay for Nuclear Factor kappa B (NF-kappa B) activation in a human macro
phage/monocyte cell line, THP-1. All compounds were inactive at 100 mu g/ml
except astragaloside I which increased NF-kappa B directed luciferase expr
ession to levels about 65% as compared with maximal stimulation by E, coli
lipopolysaccharide (LPS) at 10 mu g/ml. None of the compounds were active a
t Low dosage levels (0.1 mu g/ml) in combination with 50 ng/ml LPS. Astraga
loside I also Increased mRNA expression of the inflammatory cytokines inter
leukin-1 beta (IL-1 beta) and tumor necrosis factor-alpha (TNF-alpha) as me
asured using reverse transcriptase-polymerase chain reaction (RT)-PCR, Base
d on these results it is clear that certain structural features are require
d for immunostimulation of cycloartane-type triterpene glycosides.