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Anticancer Activity and Molecular Targets of Piper cernuum Substances in Oral Squamous Cell Carcinoma Models

Thaíssa Queiróz Machado1, Maria Emanuelle Damazio Lima2, Rafael Carriello da Silva3

  • 1Postgraduate Program in Applied Science for Health Products, Faculty of Pharmacy, Fluminense Federal University, Niteroi 24241-000, RJ, Brazil.

Biomedicines
|July 29, 2023
PubMed

Insights

The dichloromethane partition of Piper cernuum (PCLd) is a nontoxic, promising anticancer agent for oral squamous cell carcinoma (OSCC). It reduces atypia and increases survival by inducing apoptosis via novel compounds and aporphine alkaloids.

Area of Science:

  • Pharmacology
  • Natural Products Chemistry
  • Oncology

Background:

  • Oral squamous cell carcinoma (OSCC) presents a significant global health challenge with high mortality rates.
  • Developing novel therapeutic agents for OSCC is crucial.
  • The Piper plant genus exhibits diverse biological activities, including potential anticancer properties.

Purpose of the Study:

  • To evaluate the efficacy and safety of Piper cernuum dichloromethane partition (PCLd) as a potential treatment for chemically induced oral squamous cell carcinoma (OSCC) in mice.
  • To identify and characterize the active compounds within PCLd responsible for anticancer effects.
  • To investigate the molecular mechanisms underlying the observed anticancer activity.

Main Methods:

  • Chronic toxicity assessment of PCLd in mice.
  • Chemical induction of OSCC in mice, followed by PCLd treatment.
  • Chromatographic purification of PCLd to isolate active fractions (09.07 and 14.05).
  • Apoptosis assays (phosphatidyl serine exposition, DNA fragmentation, caspase-3/7 activation) and hemolytic assays.
  • LC-DAD-MS/MS analysis for compound identification.
  • In silico molecular docking studies to predict potential drug targets.

Main Results:

  • PCLd demonstrated no toxicity during chronic treatment in mice.
  • PCLd significantly reduced oral atypia and increased survival rates in chemically induced OSCC models.
  • Purified fractions 09.07 and 14.05 exhibited potent and selective cytotoxic activity by inducing apoptosis.
  • Fraction 14.05 contained aporphine alkaloids, newly described in P. cernuum, which correlated with cytotoxic effects.
  • In silico analysis identified potential molecular targets including androgen receptor (AR), CHK1, CK2, DYRK1A, EHMT2, LXRβ, and VEGFR2.

Conclusions:

  • Piper cernuum fractions, particularly PCLd, show significant preclinical potential as anticancer agents for OSCC.
  • Novel compounds and aporphine alkaloids from P. cernuum induce cancer cell death via apoptosis.
  • These findings warrant further investigation of P. cernuum derivatives as candidates for novel OSCC therapies.
Keywords:
GNPSN-methylcoclaurinePiperaceaeantitumorapoptosisasimilobineboldinecoclaurineisocorydineoral cancer

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