Bioactivity of Cyperus amuricus extracts against hepatocellular carcinoma and molecular docking analysis targeting the PI3K/AKT/mTOR pathway

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.

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Publication Details

Journal
PLoS ONE
Published
2026-01-09
DOI
https://doi.org/10.1371/journal.pone.0340868
Primary Topic
Botany, Ecology, and Taxonomy Studies
Type
article
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article

Bioactivity of Cyperus amuricus extracts against hepatocellular carcinoma and molecular docking analysis targeting the PI3K/AKT/mTOR pathway

Thien-Vy Phan, Thanh Khoi Tu, Hai Ha Pham Thi, Minh Quan Pham et al.
PLoS ONE
Botany, Ecology, and Taxonomy Studies
article

Bioactivity of Cyperus amuricus extracts against hepatocellular carcinoma and molecular docking analysis targeting the PI3K/AKT/mTOR pathway

Thien-Vy Phan, Thanh Khoi Tu, Hai Ha Pham Thi, Minh Quan Pham, Chanh M. Nguyen, Thành Phát Nguyễn, Khoa D. Nguyen
article en

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.

PLoS ONEVol. 21(1)
Trường ĐH Nguyễn Tất Thành (VN), Van Lang University (VN), Ho Chi Minh City University of Technology (VN), Vietnam Academy of Science and Technology (VN)
Openalex Percentile: Top 92%
Botany, Ecology, and Taxonomy Studies
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