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<p>Deoxyelephantopin (DET), a sesquiterpene lactone predominantly isolated from <i>Elephantopus scaber</i>, has garnered attention for its emerging multifaceted potential bioactivity in both oncology and neurobiology. This review synthesizes current preclinical evidence on the pharmacological actions of DET and elucidates the pharmacological spectrum of DET, highlighting its potent anticancer, anti-inflammatory, hepatoprotective, and neuroprotective activities. DET demonstrates broad-spectrum cytotoxicity across various cancer cell lines, including breast, colon, pancreatic, and osteosarcoma, inducing apoptosis via mitochondrial pathways, generating reactive oxygen species (ROS), and modulating cell cycle regulators. Mechanistically, inhibits key oncogenic and inflammatory signalling cascades such as the NF-κB, PI3K/AKT/mTOR, MAPK, and STAT3 cascades, consequently inhibiting tumour proliferation, metastasis, and resistance to apoptosis. In preclinical models of neurodegeneration, DET exhibits pronounced neuroprotective effects against LPS-induced degeneration and associated cognitive decline. DET attenuates neuroinflammatory responses by diminishing pro-inflammatory mediators such as (iNOS, COX-2, TNF-α, IL-6) and increases anti-inflammatory cytokines (IL-4, IL-10) as well as maintains synaptic integrity with the upregulation of synaptic markers (PSD-95, SYP). Furthermore, DET mitigates neuronal apoptosis by inhibiting key apoptotic proteins (PARP-1, caspase 3), underscoring its preclinical potential for conditions like Alzheimer’s (AD) and Parkinson’s (PD) diseases. The review also discusses the translational potential of DET, emphasizing the need for dose optimization, clinical evaluation, and the exploration of synergistic therapies and analogue developments to overcome pharmacokinetic limitations. Collectively, the evidence positions DET as a versatile bioactive molecule with significant prospects for the development of novel therapeutics targeting various neurodegenerative diseases, warranting further investigation in clinical interventions. Nevertheless, no clinical data are available, and all existing evidence is based on in vitro and animal research. Rigorous pharmacokinetic, toxicological, and preclinical studies are needed before classifying deoxyelephantopin as a viable therapeutic agent.</p> Graphical abstract <p></p>

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Pharmacological insights into deoxyelephantopin: a multifunctional sesquiterpene with therapeutic promise in cancer and neurodegenerative disorders

  • 期刊论文

  • 发表日期：

    2026年4月10日

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  • Ananya Priyadarshni,
  • Ritika Sharma,
  • kundan Singh Bora,
  • Hitesh Kumar Dewangan

摘要

Deoxyelephantopin (DET), a sesquiterpene lactone predominantly isolated from Elephantopus scaber, has garnered attention for its emerging multifaceted potential bioactivity in both oncology and neurobiology. This review synthesizes current preclinical evidence on the pharmacological actions of DET and elucidates the pharmacological spectrum of DET, highlighting its potent anticancer, anti-inflammatory, hepatoprotective, and neuroprotective activities. DET demonstrates broad-spectrum cytotoxicity across various cancer cell lines, including breast, colon, pancreatic, and osteosarcoma, inducing apoptosis via mitochondrial pathways, generating reactive oxygen species (ROS), and modulating cell cycle regulators. Mechanistically, inhibits key oncogenic and inflammatory signalling cascades such as the NF-κB, PI3K/AKT/mTOR, MAPK, and STAT3 cascades, consequently inhibiting tumour proliferation, metastasis, and resistance to apoptosis. In preclinical models of neurodegeneration, DET exhibits pronounced neuroprotective effects against LPS-induced degeneration and associated cognitive decline. DET attenuates neuroinflammatory responses by diminishing pro-inflammatory mediators such as (iNOS, COX-2, TNF-α, IL-6) and increases anti-inflammatory cytokines (IL-4, IL-10) as well as maintains synaptic integrity with the upregulation of synaptic markers (PSD-95, SYP). Furthermore, DET mitigates neuronal apoptosis by inhibiting key apoptotic proteins (PARP-1, caspase 3), underscoring its preclinical potential for conditions like Alzheimer’s (AD) and Parkinson’s (PD) diseases. The review also discusses the translational potential of DET, emphasizing the need for dose optimization, clinical evaluation, and the exploration of synergistic therapies and analogue developments to overcome pharmacokinetic limitations. Collectively, the evidence positions DET as a versatile bioactive molecule with significant prospects for the development of novel therapeutics targeting various neurodegenerative diseases, warranting further investigation in clinical interventions. Nevertheless, no clinical data are available, and all existing evidence is based on in vitro and animal research. Rigorous pharmacokinetic, toxicological, and preclinical studies are needed before classifying deoxyelephantopin as a viable therapeutic agent.

Graphical abstract