Summary

Oridonin, a naturally occurring ent-kaurane diterpenoid derived from the traditional Chinese herb Isodon rubescens, has emerged as a potent inducer of programmed cell death across a broad spectrum of malignancies. Its pro-apoptotic activity is mediated primarily through the intrinsic mitochondrial pathway, characterised by disruption of mitochondrial membrane potential, upregulation of pro-apoptotic proteins (for example Bax), downregulation of anti-apoptotic factors (for example Bcl-2), and activation of initiator and effector caspases. Concomitant generation of reactive oxygen species and depletion of intracellular glutathione amplify oxidative stress, while modulation of key signalling axes—including TP53, NF-κB, Nrf2 and endoplasmic reticulum stress sensors—further commits tumour cells to apoptosis. Preclinical studies spanning leukaemia, colorectal, gallbladder, osteosarcoma and hepatic carcinoma models demonstrate both in vitro cytotoxicity and in vivo tumour suppression, highlighting oridonin’s potential as a versatile anticancer scaffold.

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Oridonin-Induced Apoptosis in Cancer Cells publication trend

The graph below shows the total number of articles in oridonin-induced apoptosis in cancer cells across all publications each year (not limited to Nature Index journals).

Technical terms

Apoptosis: Programmed cell death involving characteristic cellular shrinkage, DNA fragmentation and membrane blebbing.

Reactive Oxygen Species (ROS): Highly reactive oxygen-containing molecules that can damage cellular components or mediate signal transduction.

Glutathione (GSH): A tripeptide antioxidant that neutralises ROS and maintains redox homeostasis in cells.

Endoplasmic Reticulum (ER) Stress: A condition arising from the accumulation of misfolded proteins in the ER lumen, triggering adaptive or apoptotic pathways.

Caspases: A family of cysteine proteases that orchestrate the dismantling of cellular structures during apoptosis.

Mitochondrial Membrane Potential (MMP): The electrochemical gradient across the inner mitochondrial membrane essential for ATP production and apoptotic regulation.

References

  1. Glutathione-depleting Liposome Adjuvant for Augmenting the Efficacy of a Glutathione Covalent Inhibitor Oridonin for Acute Myeloid Leukemia Therapy. Journal of Nanobiotechnology (2024).
  2. Oridonin promotes endoplasmic reticulum stress via TP53-repressed TCF4 transactivation in colorectal cancer. Journal of Experimental & Clinical Cancer Research (2023).
  3. Oridonin, a Promising ent-Kaurane Diterpenoid Lead Compound. International Journal of Molecular Sciences (2016).
  4. Oridonin induces apoptosis and cell cycle arrest of gallbladder cancer cells via the mitochondrial pathway. BMC Cancer (2014).
  5. Oridonin exerts anticancer effect on osteosarcoma by activating PPAR-γ and inhibiting Nrf2 pathway. Cell Death & Disease (2018).
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