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Hispolon

In vitro / Animal

Mechanism of Action

Inhibits NF-kB signaling by blocking phosphorylation of IKK-alpha and I-kappa-B-alpha in LPS-stimulated macrophages, suppressing downstream iNOS, COX-2, and pro-inflammatory cytokine (TNF-alpha, IL-1-beta, IL-6) expression. Additionally induces apoptosis in tumor cells through caspase-3 activation, PARP1 cleavage, and p53 pathway engagement. Network pharmacology analysis identified binding to core targets CASP3, PARP1, and TP53 in colon cancer models.
Induces apoptosis in cancer cells through multiple mechanisms: activation of the intrinsic (mitochondrial) apoptotic pathway via caspase-9 and caspase-3 cleavage, downregulation of anti-apoptotic proteins Bcl-2 and Bcl-xL, upregulation of pro-apoptotic Bax and Bad, and inhibition of the NF-κB signaling pathway (which tumors exploit for survival). Also inhibits the PI3K/Akt/mTOR cell survival pathway and suppresses matrix metalloproteinases (MMP-2, MMP-9) involved in tumor invasion and metastasis. Demonstrates anti-angiogenic activity via VEGF suppression.

Research Notes

In vitro studies in LPS-stimulated RAW264.7 macrophages demonstrated dose-dependent suppression of iNOS, COX-2, and pro-inflammatory cytokines by P. baumii hispolon-enriched extracts. Network pharmacology studies published in 2023 (PMC) elucidated binding of hispolon and osmundacetone to CASP3, PARP1, and TP53 as core anti-colon-cancer targets. MTT assays confirmed dose-dependent suppression of HepG2 liver cancer cell proliferation with cell-cycle arrest at S phase. All evidence is preclinical.

Chen et al. (2013) demonstrated that hispolon induced apoptosis in human gastric cancer cells (AGS line) via ROS-mediated mitochondrial pathway activation with IC50 values of 15–25 μM. Huang et al. (2011) showed hispolon inhibited breast cancer cell (MDA-MB-231) proliferation and migration by suppressing NF-κB-mediated MMP-9 expression. Jang et al. (2016) found hispolon sensitized multidrug-resistant breast cancer cells to doxorubicin by inhibiting P-glycoprotein efflux pump expression. All studies are in vitro or animal; no human clinical trials with isolated hispolon have been published.

Found In 2 Herbs

3D Molecular Structure

Polyphenol (styrylpyrone derivative)
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Hispolon

Polyphenol (styrylpyrone derivative)Simple aromatic compounds with antimicrobial properties

Representative pattern: C₇H₆O₃

Atoms
Carbon
Oxygen
Hydrogen

Live Research

Open on PubMed

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