Histone deacetylase inhibitory and cytotoxic activities of the constituents from the roots of three species of .

Objectives: Histone deacetylase inhibitory and cytotoxic activities of 18 naturally occuring terpenoids (ferutinin, stylosin, tschimgine and guaiol), coumarins (umbelliprenin, farnesiferone B, conferone, feselol, ligupersin A, conferdione, conferoside) and sulfur-containing derivatives (latisulfies A-E, persicasulphides A and C) from the roots of three species of ( and ) were evaluated.

Materials And Methods: The cytotoxic activity of compounds was evaluated against human cancer cell lines (HeLa, HCT116, A2780 and A549) by AlamarBlue® assay using vorinostat as the positive control. On the other hand, we aimed to evaluate their inhibitory activities against pan-HDAC.

Results: The methanolic extract of the roots of was subjected to silica gel column chromatography. Further purification by preparative thin-layer chromatography (PTLC) and semipreparative RP-HPLC yielded twelve known compounds (1-12). This is the first report on the isolation of guaiol (1), persicasulphide C (3) and conferoside (10) from the roots of . Six compounds including persicasulfide A, conferone, feselol, latisufide C, conferoside and ferutinin showed cytotoxic activity with IC values in the range of 11.61-49.40 μM against cancer cells and pan-HDAC inhibitory activity with IC values in the range of 1.06-35.27 μM.

Conclusion: Results indicated that persicasulfide A (2), conferone (6) and feselol (7) showed moderate cytotoxicity with IC50 values in the range of 11.76-39.24 μM against cancer cells and potent pan-HDAC inhibitory activity with IC values in the range of 1.06-10.73 μM. Conferone was more active than others with a higher potency for HDAC inhibition (1.06- 1.17 μM).