<p>AML is the second leading cause of mortality due to malignancies in humans, thus necessitating exploration of newer agents that may be specific, cheap, and less toxic. Various studies have shown that several monoterpenes exhibit anticancer properties. In present study, we assessed the anticancer activity of an acyclic monoterpene ester, geranyl acetate, against AML (Acute Myeloid Leukemia) cells in the present study. Antiproliferative activity and apoptosis were analysed using the MTT assay, crystal violet , and DAPI staining. Researchers measured <i>RelA</i> gene expression using quantitative PCR (qPCR). According to the results, geranyl acetate showed an effective anticancer activity, with an IC<sub>50</sub> value of 6.86 µM ascompared to the cytarabine (IC<sub>50</sub>: 12.5 µM) against AML cells. To investigate the possible disease-causing mechanism of monoterpenoid, DAPI staining was also performed. It is observed that the downregulation of the <i>RelA</i> gene expression, an important member of the NF–κBNpathway, triggers apoptosis in the AML cells. This phytocompound could be able to induce DNA damage and arrest AML cells in the G2/M phase. In conclusion, geranyl acetate may be a promising lead molecule for AML treatment. Various key cellular mechanisms, including apoptosis, DNA damage response, and cell cycle arrest, largely drive its anticancer activity.</p>

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Anticancer potential of geranyl acetate through RelA gene downregulation in acute myeloid leukemia cells

  • Athar Abdullah Baig,
  • Tahir Maqbool,
  • Awais Altaf,
  • Bishama Jamil,
  • Muhammad Sarwar,
  • Muqadas Shabbir,
  • Asia Kiran,
  • Qurban Ali,
  • Adnan Iqbal,
  • Ajaz Ahmad

摘要

AML is the second leading cause of mortality due to malignancies in humans, thus necessitating exploration of newer agents that may be specific, cheap, and less toxic. Various studies have shown that several monoterpenes exhibit anticancer properties. In present study, we assessed the anticancer activity of an acyclic monoterpene ester, geranyl acetate, against AML (Acute Myeloid Leukemia) cells in the present study. Antiproliferative activity and apoptosis were analysed using the MTT assay, crystal violet , and DAPI staining. Researchers measured RelA gene expression using quantitative PCR (qPCR). According to the results, geranyl acetate showed an effective anticancer activity, with an IC50 value of 6.86 µM ascompared to the cytarabine (IC50: 12.5 µM) against AML cells. To investigate the possible disease-causing mechanism of monoterpenoid, DAPI staining was also performed. It is observed that the downregulation of the RelA gene expression, an important member of the NF–κBNpathway, triggers apoptosis in the AML cells. This phytocompound could be able to induce DNA damage and arrest AML cells in the G2/M phase. In conclusion, geranyl acetate may be a promising lead molecule for AML treatment. Various key cellular mechanisms, including apoptosis, DNA damage response, and cell cycle arrest, largely drive its anticancer activity.