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Oridonin inhibits aberrant AKT activation in breast cancer

Bowen Sun1,2, Geng Wang2,3, Huidong Liu2,3

  • 1The first Affiliate Hospital, Biomedical Translational Research Institute, Guangdong Province Key Laboratory of Molecular Immunology and Antibody Engineering, Jinan University, Guangzhou 510632, China.

Oncotarget
|May 31, 2018
PubMed

Insights

Oridonin, a traditional Chinese medicine extract, effectively inhibits breast cancer cell growth by targeting the PI3K/AKT pathway. This natural compound shows promise as a therapeutic agent for specific breast cancer types.

Area of Science:

  • Oncology
  • Pharmacology
  • Natural Products Chemistry

Background:

  • Aberrant activation of phosphatidylinositol-4,5-bisphosphate 3-kinase/protein kinase B (PI3K/AKT) signaling is common in cancer.
  • Existing PI3K and AKT inhibitors have shown limited efficacy and significant adverse effects.

Purpose of the Study:

  • To screen traditional Chinese medicine (TCM) plant extracts for novel inhibitors of the PI3K/AKT pathway.
  • To evaluate the therapeutic potential of Oridonin, a TCM extract, in preclinical models of breast cancer.

Main Methods:

  • Screening of 441 authenticated TCM plant extracts against HMEC-PIK3CAH1047R cells.
  • Assessing Oridonin's effect on cell viability and tumor growth in vitro and in vivo.
  • Investigating Oridonin's mechanism of action as an AKT inhibitor.

Main Results:

  • Oridonin, from Rabdosia rubescens, demonstrated the most significant reduction in cell viability.
  • Oridonin selectively inhibited tumor growth in human breast cancer cells with hyperactivated PI3K/AKT signaling.
  • Oridonin prevented mammary tumor initiation in a mouse model driven by PIK3CAH1047R mutation.

Conclusions:

  • Oridonin acts as a potent ATP-competitive AKT inhibitor.
  • Oridonin exhibits selective efficacy against breast cancers with PI3K/AKT pathway hyperactivation.
  • Oridonin represents a promising therapeutic candidate for breast cancer treatment.
Keywords:
PI3K/AKT signalingTCM plant extractsmammary tumor preventionoridonintumorigenesis

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