Studies Of Triterpenoids Of Ganoderma Lucidum And Their Bioactivities

Objective: Ganoderma lucidum(Leyss.Ex Fr.)Karst widely distributed in China.It has the effect of invigorating qi for tranquilization and relieving cough and asthma.As a famous Traditional Chinese Medicine,it has been widely used for anti-diabetic,antitumor,hepatitis and hypertension.This research work mainly aimed to further inverstigate the chemical constituents and biological activities of ganoderma lucidum.Methods: The ethanolic extract of Ganoderma lucidum was extracted by chloroform.The CHCl3 extract was isolated and purified by various chromatographic techiques such as silica gel column,sephadex LH-20 column,MPLC and HPLC.The structures of isolated compounds were elucidated on the basis of UV,ESIMS,HRESIMS,1H NMR,13 C NMR,1H-1H COSY,HMBC,HMQC,and NOESY analysis.The P-glycoprotein(P-gp)inhibitory effects of isolated compounds were evaluated using an adriamycin-resistant human breast adenocarcinoma cell line(MCF-7/ADR).In addition,the ?-glucosidase enzyme inhibitior effects of isolated compounds were aslo determined.Results: Totally sixteen new highly oxygenated lanostane triterpenoids and thirteen known ganoderic acids were isolated from Ganoderma lucidum.The new compounds 1-16 were identified as Ganoderlactone A,Ganoderlactone B,Ganoderlactone C,Ganoderlactone D,Ganoderlactone E,Ganodernoid A,Ganodernoid B,Ganodernoid C,Ganodernoid D,Ganodernoid E,Ganodernoid F,Ganodernoid G,12-epi-ganoderlactone D,3?-hydroxyganodernoid D,3?-hydroxy-12?-acetoxy ganodernoid D,and 12?-hydroxyganoderenic F,respectively.Compounds 1,5,22,and 26 exhibited an approximate four-fold increase of adriamycin accumulation in MCF-7/ADR cells as well as verapamil with two times when compared with the control group.These data support the potential P-glycoprotein inhibitory activities of compounds 1,5,22,and 26.Furthermore,in an in vitro bioassay,compounds 2,5,10 and 11 showed moderate inhibitory effects against ?-glucosidase compared with those of the positive control acarbose.Conclusion: The chemical constituents of ganoderma lucidum were investigated systemically and sixteen new triterpenoids were obtained.The new bioactivities of isolated triterpenoids were also evaluated,all of which is a firm basement for further developing the ganoderma lucidum as a natural resource.