Background <p>Euphorbia species contain diverse secondary metabolites with reported biological activities, but <i>Euphorbia petrophila</i> remains pharmacologically underexplored. This study aimed to characterize the phytochemical profile of <i>E. petrophila</i> ethanol extract and evaluate its preliminary in vitro anticancer-related activity in lung and breast cancer cell models.</p> Methods <p>Aerial parts of <i>E. petrophila</i> were extracted with ethanol using ultrasonic-assisted extraction. The extract was profiled by LC–MS/MS. Cytotoxicity was assessed by MTT assay in A549 and MDA-MB-231 cancer cells and in BEAS-2B and MCF10A non-tumorigenic epithelial cells. Apoptosis and cell-cycle distribution were analyzed by flow cytometry. Migration and invasion were evaluated using Transwell assays, and selected gene-expression changes were measured by RT-qPCR. Data were analyzed using appropriate analysis of variance and post hoc comparisons.</p> Results <p>LC–MS/MS analysis identified phenolic acids and flavonoids, with gallic acid, quinic acid, ellagic acid, and isoquercitrin among the most abundant detected constituents. The extract reduced IC₅₀ value of in all tested cell lines, with the strongest cytotoxic effect observed in A549 cells. It increased apoptotic cell populations and promoted G0/G1 cell-cycle accumulation, particularly in A549 cells. The extract also markedly suppressed migration and invasion in A549 and MDA-MB-231 cells. These functional effects were accompanied by changes in TP53 and CDKN1A mRNA expression.</p> Conclusions <p><i>E. petrophila</i> ethanol extract shows preliminary antiproliferative, pro-apoptotic, anti-migratory, and anti-invasive activity in selected cancer cell models. However, because the findings are based on crude extract testing and transcript-level analyses, the results should be interpreted as preliminary and correlative. Further work should include extract standardization, LC–MS/MS method validation, broader normal-cell toxicity profiling, active-compound isolation, protein-level mechanistic assays, and in vivo safety and efficacy studies.</p>

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LC–MS/MS-based phytochemical profiling and preliminary in vitro anticancer-related bioactivity of Euphorbia petrophila ethanol extract

  • Mehmet Ali Güzel,
  • İrem Nur Menevşe,
  • Turgay Kolaç,
  • Şengül Yüksel,
  • Birol Mutlu

摘要

Background

Euphorbia species contain diverse secondary metabolites with reported biological activities, but Euphorbia petrophila remains pharmacologically underexplored. This study aimed to characterize the phytochemical profile of E. petrophila ethanol extract and evaluate its preliminary in vitro anticancer-related activity in lung and breast cancer cell models.

Methods

Aerial parts of E. petrophila were extracted with ethanol using ultrasonic-assisted extraction. The extract was profiled by LC–MS/MS. Cytotoxicity was assessed by MTT assay in A549 and MDA-MB-231 cancer cells and in BEAS-2B and MCF10A non-tumorigenic epithelial cells. Apoptosis and cell-cycle distribution were analyzed by flow cytometry. Migration and invasion were evaluated using Transwell assays, and selected gene-expression changes were measured by RT-qPCR. Data were analyzed using appropriate analysis of variance and post hoc comparisons.

Results

LC–MS/MS analysis identified phenolic acids and flavonoids, with gallic acid, quinic acid, ellagic acid, and isoquercitrin among the most abundant detected constituents. The extract reduced IC₅₀ value of in all tested cell lines, with the strongest cytotoxic effect observed in A549 cells. It increased apoptotic cell populations and promoted G0/G1 cell-cycle accumulation, particularly in A549 cells. The extract also markedly suppressed migration and invasion in A549 and MDA-MB-231 cells. These functional effects were accompanied by changes in TP53 and CDKN1A mRNA expression.

Conclusions

E. petrophila ethanol extract shows preliminary antiproliferative, pro-apoptotic, anti-migratory, and anti-invasive activity in selected cancer cell models. However, because the findings are based on crude extract testing and transcript-level analyses, the results should be interpreted as preliminary and correlative. Further work should include extract standardization, LC–MS/MS method validation, broader normal-cell toxicity profiling, active-compound isolation, protein-level mechanistic assays, and in vivo safety and efficacy studies.