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Bioactivity of Cyperus amuricus extracts against hepatocellular carcinoma and molecular docking analysis targeting
Thanh Luan Nguyen1, Thanh Khoi Tu2,3, Thien-Vy Phan4
1HUTECH Institute of Applied Science, HUTECH University, Ho Chi Minh City, Vietnam.
Abstract:
Cyperus amuricus (Cyperaceae) has exhibited potential anticancer activity against hepatocellular carcinoma (HCC), yet its molecular mechanisms and phytoconstituent interactions with oncogenic pathways remain underexplored. This study integrates in vitro cytotoxicity assays and molecular docking to evaluate the effects of C. amuricus fractionated extracts on HCC, focusing on PI3K/AKT/mTOR signaling axis. The ethyl acetate (EA) fraction selectively inhibited HepG2 cell proliferation (IC50 = 159.76 µg/mL) with minimal toxicity to normal fibroblasts. Apoptotic features-cell shrinkage, membrane blebbing, nuclear condensation, and DNA fragmentation-were confirmed through DAPI staining and gel electrophoresis. Western blot analysis revealed dose-dependent suppression of phosphorylated Akt and p70S6K, indicating pathway inhibition. Molecular docking identified strong binding affinities between Cyperaceae-derived compounds and PI3K/AKT/mTOR targets, with luteolin 7-O-β-D-glucuronopyranoside-6″-methyl ester blocked PI3K activation, vitexin bound AKT's allosteric site, and digitoxin targeted mTOR's ATP-binding pocket, showing comparable binding energies to reference ligands. These findings suggest C. amuricus as a promising candidate for natural product-based HCC therapy.
Insights
Cyperus amuricus shows promise for treating liver cancer (HCC). Its compounds effectively inhibit cancer cell growth and key signaling pathways, suggesting potential as a natural therapeutic agent.
Area of Science:
- Pharmacology
- Molecular Biology
- Natural Products Chemistry
Background:
- Hepatocellular carcinoma (HCC) remains a significant health challenge.
- The anticancer potential of Cyperus amuricus against HCC is recognized but poorly understood.
- Investigating the molecular mechanisms and specific phytoconstituents is crucial for therapeutic development.
Purpose of the Study:
- To evaluate the in vitro anticancer effects of Cyperus amuricus extracts on HCC.
- To elucidate the molecular mechanisms, particularly the PI3K/AKT/mTOR pathway.
- To identify specific phytoconstituents responsible for the observed activity through molecular docking.
Main Methods:
- In vitro cytotoxicity assays using HepG2 cells and normal fibroblasts.
- Analysis of apoptotic features via DAPI staining and DNA fragmentation assays.
- Western blot analysis to assess PI3K/AKT/mTOR pathway modulation.
- Molecular docking simulations to predict binding interactions of phytoconstituents with target proteins.
Main Results:
- The ethyl acetate fraction of C. amuricus demonstrated selective cytotoxicity against HepG2 cells (IC50 = 159.76 µg/mL).
- Evidence of apoptosis induction and dose-dependent inhibition of phosphorylated Akt and p70S6K.
- Molecular docking revealed strong binding affinities of specific compounds (luteolin derivative, vitexin, digitoxin) to PI3K, AKT, and mTOR targets.
Conclusions:
- Cyperus amuricus exhibits significant anticancer activity against HCC through apoptosis induction and PI3K/AKT/mTOR pathway inhibition.
- Specific phytoconstituents display favorable interactions with key oncogenic targets.
- C. amuricus represents a promising source for developing novel, natural product-based therapies for HCC.
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