Apoptosis Induced by (+)-Betulin Through NF-κB Inhibition in MDA-MB-231 Breast Cancer Cells

Gerardo D Anaya-Eugenio1, Nicole A Eggers1, Yulin Ren1

  • 1Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH, U.S.A.

Anticancer Research
|December 8, 2020
PubMed
Abstract

Insights

(+)-Betulin effectively inhibits MDA-MB-231 cancer cell growth by targeting the NF-κB pathway. This natural compound shows promise as it does not induce toxicity in zebrafish models, offering a potential therapeutic avenue.

Area of Science:

  • Molecular Biology
  • Cancer Research
  • Pharmacology

Background:

  • The NF-κB pathway plays a crucial role in cell survival and inflammation.
  • MDA-MB-231 cells are a triple-negative breast cancer cell line.
  • (+)-Betulin is a natural compound with potential anti-cancer properties.

Purpose of the Study:

  • To investigate the effects of (+)-betulin on the NF-κB-apoptotic pathway in MDA-MB-231 cells.
  • To assess the in vivo toxicity and protein expression of (+)-betulin using a zebrafish model.

Main Methods:

  • Cytotoxicity was evaluated using the SRB assay.
  • In vivo toxicity was assessed in a zebrafish model.
  • Western blot, mitochondrial transmembrane potential (MTP) analysis, and computational modeling were employed.

Main Results:

  • (+)-Betulin inhibited MDA-MB-231 cell growth without causing zebrafish toxicity.
  • (+)-Betulin suppressed NF-κB p65 activity in silico and in vitro.
  • Down-regulation of NF-κB p50/p65, IKKα/β, ICAM-1, and bcl-2 was observed in cells; MTP loss was induced.

Conclusions:

  • (+)-Betulin induces apoptosis in MDA-MB-231 cells by inhibiting the NF-κB pathway.
  • The findings contribute to understanding the anti-cancer mechanism of (+)-betulin.
  • The study supports the potential of (+)-betulin as a therapeutic agent.

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