Anti-tumor target prediction and activity verification of Ganoderma lucidum triterpenoids / 中国中药杂志

It has reported that Ganoderma lucidum triterpenoids had anti-tumor activity. However, the anti-tumor target is still unclear. The present study was designed to investigate the anti-tumor activity of G. lucidum triterpenoids on different tumor cells, and predict their potential targets by virtual screening. In this experiment, molecular docking was used to simulate the interactions of 26 triterpenoids isolated from G. lucidum and 11 target proteins by LibDock module of Discovery Studio2016 software, then the anti-tumor targets of triterpenoids were predicted. In addition, the in vitro anti-tumor effects of triterpenoids were evaluated by MTT assay by determining the inhibition of proliferation in 5 tumor cell lines. The docking results showed that the poses were greater than five, and Libdock Scores higher than 100, which can be used to determine whether compounds were activity. Eight triterpenoids might have anti-tumor activity as a result of good docking, five of which had multiple targets. MTT experiments demonstrated that the ganoderic acid Y had a certain inhibitory activity on lung cancer cell H460, with IC₅₀ of 22.4 μmol•L ⁻¹, followed by 7-oxo-ganoderic acid Z2, with IC₅₀ of 43.1 μmol•L ⁻¹. However, the other triterpenoids had no anti-tumor activity in the detected tumor cell lines. Taking together, molecular docking approach established here can be used for preliminary screening of anti-tumor activity of G.lucidum ingredients. Through this screening method, combined with the MTT assay, we can conclude that ganoderic acid Y had antitumor activity, especially anti-lung cancer, and 7-oxo-ganoderic acid Z2 as well as ganoderon B, to a certain extent, had anti-tumor activity. These findings can provide basis for the development of anti-tumor drugs. However, the anti-tumor mechanisms need to be further studied.

Study on in vitro anti-tumor activity of triterpenoids from Ganoderma lucidum / 国际检验医学杂志

Objective To investigate the anti-tumor activity of triterpenoids from Ganoderma lucidum on different tumor cells . Methods The MTT assay was adopted to detect the in vitro inhibition effect on 5 kinds of tumor cells .The inhibiting curve was drawn ,IC50 was calculated for reflecting the compound′s cytotoxic activity .Results The in vitro experiments demonstrated that three kinds of triterpenoids compound monomer showed different degrees of inhibition effect ,in which the inhibitory effect of gano-derenic acid Y was stronger ,its IC50 on H460 lung cancer cells was 22 .4 μmol/L ,followed by 7-oxo-ganoderic acid Z2 ,its IC50 was 43 .1 μmol/L .Conclusion Ganoderenic acid Y shows a strong inhibitory activity on H 460 lung cancer cells ,7-oxo-ganoderic acid Z2 shows a certain inhibitory activity on H 460 lung cancer cells ,moreover the inhibitory activity is dose dependent .The three com-pounds of ganoderenic acid Y ,7-oxo-ganoderic acid Z2 and ganoderon B have no activity or very weak activity to the other detected cell lines .The anti-lung cancer activity of ganoderenic acid Y and 7-oxo-ganoderic acid Z2 needs to be further deeply studied .