In vitro and computational studies showed that perezone inhibits PARP-1 and induces changes in the redox state of K562 cells

In Vitro and Computational Studies of Perezone and Perezone Angelate as Potential Anti-Glioblastoma Multiforme Agents

“…As reported previously, perezone exerts pro-apoptotic effects by at least two mechanisms of action: the induction of oxidative stress and PARP-1 inhibition [ 13 ]. Figure 8 shows the proposed effects of perezone angelate to explain its pro-apoptotic effects in GBM cells.…”

“…The extraction of perezone and perezone angelate from roots of Acourtia cordata was performed as previously described [ 13 ]. Physical and spectroscopic data were correlated with the literature [ 14 ].…”

“…Cytotoxic evaluation of perezone and perezone angelate was performed in U373 cells, considering its pro-apoptotic effect, as previously reported [ 13 ], employing suberoylanilide hydroxamic acid as a positive control. Figure 2 a shows the cytotoxic activity of suberoylanilide hydroxamic acid, with an 85.8% viability at 10 μM, similar to data previously reported [ 15 ].…”

“…As it can be seen in Figure 5 , the potent inhibition of PARP-1 by olaparib was confirmed with an IC 50 of 5.5 nM (± 0.3 μM), which is in accordance with the literature [ 18 ]. Importantly, PARP-1 inhibitory activity by perezone angelate was confirmed, with an IC 50 of 5.25 μM (± 1.2 μM), in this way, showing a higher potency than perezone [ 13 ].…”

“…This fact emphasizes the importance of PARP-1 inhibitors as a potential drug for the treatment of GBM. In this sense, perezone, a phyto-compound extracted from roots of the plant of the genus Acourtia , has exhibited anti-neoplastic activity by PARP-1 inhibition and reactive oxygen species release [ 13 ]. For this reason, the present research work aimed to perform in vitro and computational evaluation of perezone and its chemically related compound, perezone angelate ( Figure 1 ), as anti-GBM agents.…”