A triterpenoid friedelan-3\�-ol isolated from Euphorbia lactea exhibited cytotoxic activity against HN22 cells by inducing an S-phase cell cycle arrest

Abstract

The anticancer activity of Euphorbia lactea Haw. (E. lactea) has been observed by our lab and other research groups; however, the identity of the bioactive compounds harboring the anticancer effect remains unknown. Here, we report the first isolation of four triterpenoidal compounds, i.e., friedelin [1], friedelan-3β-ol [2], taraxerol [3], and friedelan-3α-ol [4], from the n-hexane fraction of the E. lactea extract. The cytotoxic activities of these compounds were investigated in several cancer cell lines, including HN22, HepG2, HCT116, and HeLa. These compounds exhibited a dose-dependent cytotoxic activity against HN22, HepG2, and HCT116, while the marginal cytotoxic effect was observed in HeLa cells. Among the four bioactive compounds, compound 2 exhibited the most prominent anticancer effect against HN22 cells. Flow cytometry analysis of HN22 cells treated with the compound revealed that compound 2 induced a cell cycle arrest at the S-phase, while apoptosis was not induced at the same concentration and exposure time. In summary, our results highlighted E. lactea as an attractive candidate for anticancer research and identified compound 2 as a chemical constituent of E. lactea harboring anticancer activity.

Anti-Inflammatory and Cytotoxic Compounds Isolated from Plants of Euphorbia Genus

“…Cynsaccatol (50) isolated from E. lathyris shows the greatest effect on the inhibition of the production of NO for macrophages stimulated with LPS. (4R,5S,8S,9R,10S,13R,16S)ent-16α,17-dihydroxy-19-tigloyloxykauran-3-one (248) and Euphorbia factors L1 and L3 have good cytotoxic activity.…”

Two spurge species, Euphorbia resinifera O. Berg and Euphorbia officinarum subsp. echinus (Hook.f. & Coss.) Vindt inhibit colon cancer

“…No previous data were found on the effects of E. resinifera and E. echinus extracts in human colon cancer cells, and the studies about the colon cancer effects of herbal extracts on colorectal cancers were limited. Previous reports by other researchers have documented the anti-migration of other Euphorbia species, including the hydroalcoholic extract of E. lacteal , which showed maximum inhibition (about 40%) at the concentration of 125 µg/ml against the migration of HN22 cells [ 64 ]. Another study on an ethanolic extract from seeds of E. lathyris showed a reduction in the migration capacity of 18.68% after 72 h of colon cancer cells (T84 cell line) [ 65 ].…”

Nature’s Green Potential: Anticancer Properties of Plants of the Euphorbiaceae Family

“…Additionally, in in vivo studies, it significantly inhibited TNBC tumor growth without causing side effects. Wongprayoon et al [ 149 ] noted that Euphorbia lactea triterpenoid friedelan-3β-ol was cytotoxic to several cancer cell lines, including HN22, HepG2, HCT116, and HeLa. Furthermore, the authors showed that the compound induced S-phase cell cycle arrest in HN22 cells without inducing apoptosis at the same concentration and exposure time.…”