Lupeol-Related Anticancer and Anti-Inflammatory Mechanisms
Summary
Lupeol is a naturally occurring pentacyclic triterpene found in numerous fruits, vegetables and medicinal plants. It exerts anticancer effects through multiple pathways, notably by inhibiting pro-survival signalling cascades such as NF-κB, STAT3 and PI3K/Akt, inducing intrinsic apoptosis via mitochondrial depolarisation and caspase activation, and arresting the cell cycle at G1 or G2/M phases. In parallel, lupeol modulates inflammatory responses by downregulating cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS) and pro-inflammatory cytokines (TNF-α, IL-1β), while enhancing antioxidant defences against reactive oxygen species. Structural analogues and esterified derivatives of lupeol exhibit varied potency and pharmacokinetic profiles, shedding light on structure–activity relationships. Preclinical investigations highlight additive or synergistic interactions with other anti-inflammatory agents or kinase inhibitors, underscoring the translational potential of lupeol for both oncology and chronic inflammatory disorders.
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Lupeol-Related Anticancer and Anti-Inflammatory Mechanisms publication trend
The graph below shows the total number of articles in lupeol-related anticancer and anti-inflammatory mechanisms across all publications each year (not limited to Nature Index journals).
Technical terms
Pentacyclic triterpene: A class of naturally occurring compounds built from five cyclohexane rings, known for diverse bioactivities.
STAT3: A transcription factor activated by phosphorylation that drives tumour cell survival, proliferation and angiogenesis.
SHP-2: A protein tyrosine phosphatase that negatively regulates receptor and non-receptor tyrosine kinase signalling.
NF-κB: A transcription factor complex that controls expression of genes involved in inflammation, immune responses and cell survival.
Apoptosis: Programmed cell death characterised by caspase activation, DNA fragmentation and membrane blebbing.
COX-2: An inducible enzyme that converts arachidonic acid into pro-inflammatory prostaglandins.
iNOS: An enzyme that produces high levels of nitric oxide during inflammation, contributing to cellular damage and signalling.
References
- Anti-inflammatory effects and possible mechanism of action of lupeol acetate isolated from Himatanthus drasticus (Mart.) Plumel. Journal of Inflammation (2010).
- Negative regulation of signal transducer and activator of transcription-3 signalling cascade by lupeol inhibits growth and induces apoptosis in hepatocellular carcinoma cells. British Journal of Cancer (2014).
- Lupeol and its esters: NMR, powder XRD data and in vitro evaluation of cancer cell growth. Brazilian Journal of Pharmaceutical Sciences (2018).
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