Two
sterols and seven
triterpenoids were isolated and identified from Ganoderma lucidum by
silica gel column chromatography, preparative high-performance liquid chromatography and spectra analysis. Then, the multidrug resistance reversal activities of these compounds were assessed using MTT assay. Among these compounds,
ganoderol B (3), ganoderone A (4), ganodermanondiol (6) and
ganoderiol F (8) were shown to reverse the resistance of human oral
epidermoid carcinoma cell line KBv200 to
doxorubicin, and the reversal folds were 6.59, 4.70, 4.01 and 7.09, respectively.
Ganoderiol F could increase the intracellular accumulation of
doxorubicin in KBv200 cells through inhibiting
P-glycoprotein transport function. Further mechanistic investigation found that
ganoderiol F did not alter
P-glycoprotein expression. In conclusion,
ganoderiol F has potent effect in reversing
P-glycoprotein mediated
tumor multidrug resistance. Potential reversal agents against multidrug resistance in
tumor may be found in
triterpenoids from Ganoderma lucidum.[Formula: see text].