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Guaianolide is a type of naturally occurring sesquiterpene lactone compounds that have attracted attention due to their diverse biological properties. In this work, a guaiane-type sesquiterpene lactone identified as deoxycynaropicrin (compound  1 ) was isolated and reported for the first time from the leaves of  Centaurothamnus maximus  with two known flavonoid derivatives namely luteolin 6- O -methyl ether (compound  2 ) and quercetin 3-methyl ether 5- O -glucopyranoside (compound  3 ). The cytotoxic activity of all the three compounds was evaluated against the THP-1 human leukemia cell lines. Moreover, flow cytometry was employed to explore the cell cycle arrest and apoptosis induction for the active compound. We found that compound  1  (deoxycynaropicrin) exerted the highest cytotoxicity while compounds  2  and  3  showed no activity. Cell cycle analysis showed that compound  1  arrested the cells’ population at the G2/M phase. Furthermore, THP-1 cells treated with compound  1  exhibited a marked increase in the apoptotic cells compared to the control. Overall, this study showed that deoxycynaropicrin induces cytotoxicity against human leukemia cell lines and provided an important insight into its potential therapeutic effects against leukemia cells.

Cytotoxic activity of guaiane-type sesquiterpene lactone (deoxycynaropicrin) isolated from the leaves of Centaurothamnus maximus