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Bioactivities of Compounds from Elephantopus scaber, an Ethnomedicinal Plant from Southwest China.

ABSTRACT: Elephantopus scaber is an ethnomedicinal plant used by the Zhuang people in Southwest China to treat headaches, colds, diarrhea, hepatitis, and bronchitis. A new ? -truxinate derivative, ethyl, methyl 3,4,3',4'-tetrahydroxy- ? -truxinate (1), was isolated from the ethyl acetate extract of the entire plant, along with 4 known compounds. The antioxidant activity of these 5 compounds was determined by ABTS radical scavenging assay. Compound 1 was also tested for its cytotoxicity effect against HepG2 by MTT assay (IC50 = 60? ? M), and its potential anti-inflammatory, antibiotic, and antitumor bioactivities were predicted using target fishing method software.

SUBMITTER: Wang J

PROVIDER: S-EPMC4055671 | biostudies-literature | 2014

REPOSITORIES: biostudies-literature

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Bioactivities of Compounds from Elephantopus scaber, an Ethnomedicinal Plant from Southwest China.

Wang Jianjun J Li Ping P Li Baosai B Guo Zhiyong Z Kennelly Edward J EJ Long Chunlin C

Evidence-based complementary and alternative medicine : eCAM 20140519

Elephantopus scaber is an ethnomedicinal plant used by the Zhuang people in Southwest China to treat headaches, colds, diarrhea, hepatitis, and bronchitis. A new δ -truxinate derivative, ethyl, methyl 3,4,3',4'-tetrahydroxy- δ -truxinate (1), was isolated from the ethyl acetate extract of the entire plant, along with 4 known compounds. The antioxidant activity of these 5 compounds was determined by ABTS radical scavenging assay. Compound 1 was also tested for its cytotoxicity effect against HepG ...[more]

PMID: 24963325

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Project description:BackgroundElephantopus scaber and Phaleria macrocarpa have recently been interested as novel anticancer agents. However, there was no scientific evaluation of the anticancer effect of both plant combinations.ObjectiveThis study investigated the potential anticancer effects of combined E. scaber and P. macrocarpa leaves extract on human breast cancer cells lines.Materials and methodsT47D cells were treated with the combination of E. scaber and each part of P. macrocarpa (leaves/EL, mesocarp/EM, seed/ES and pericarp/EP). T47D cells were then exposed to three ratios (1:1, 2:1, and 1:2) of the best combination for 24, 48, and 72 h. The cell viability of T47D and TIG-1 cells was assessed using WST-1 assay. The apoptotic hallmarks were determined using FITC Annexin V-PI staining and DNA fragmentation assay. The cell proliferation and cell cycle profiles were analyzed using CFSE (carboxyfluorescein succinimidyl ester) and Propidium iodide-flowcytometry assays. The relative number of p-ERα, p-Nrf2, p-PI3K, p-AKT, and p-mTOR were assessed using flow cytometry. The molecular docking analysis was also performed to confirm the mechanism of the extract in silico.ResultsThe combination of E. scaber and P. macrocarpa leaves (EL) possessed strong cytotoxic activity (p < 0.05) than other combination groups and cisplatin. EL showed selective killing only to T47D cells. EL at a ratio of 2:1 potentially suppressed the cell viability and cell division, induced apoptosis, and arrested the cell cycle of T47D cells by triple inhibiting the p-Nrf2, p-ERα, and p-PI3K/AKT/mTOR signaling pathway. Molecular docking analysis confirmed that the possible mechanism of EL to reduce T47D cell growth was by inhibiting ERα and Nrf2-complex, resulting in the reduction in the crosstalk effect of Nrf2, ERα and PI3K/AKT/mTOR pathways.ConclusionThe combination of leaf extracts from E. scaber and P. macrocarpa caused cell death in breast cancer cells T47D and not in normal cells TIG-1; hence has the potential to show anticancer efficacy in preclinical and clinical trials.

Dataset Information

Bioactivities of Compounds from Elephantopus scaber, an Ethnomedicinal Plant from Southwest China.

Publications

Bioactivities of Compounds from Elephantopus scaber, an Ethnomedicinal Plant from Southwest China.

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