Effects of Leuzea carthamoides on Human Breast Adenocarcinoma MCF-7 Cells Determined by Gene Expression Profiling and Functional Assays
Abstract
Products derived from roots of Leuzea carthamoides (Maral root) are being promoted as dietary supplements with anti-aging, adaptogenic and anabolic activity, without much scientific evidence. We investigated the effects of a lipophilic Leuzea root extract and the major phytoecdysteroid, 20-hydroxyecdysone, in human breast adenocarcinoma MCF-7 cells. Cell proliferation was inhibited by the extract (IC50 = 30 microg/mL) but not by 20-hydroxyecdysone. Genome-wide expression profiling using Affymetrix HG U133 Plus 2.0 microarrays was carried out to analyse effects at the transcriptional level. 241 genes appeared to be differentially expressed after Leuzea treatment, more than after treatment with either 17beta-estradiol or tamoxifen. Transcripts linked to cell cycle regulation and DNA replication were highly over-represented and regulated in an anti-proliferative manner. Genes involved in apoptosis were regulated in a pro-apoptotic manner. Expression levels of several oxidoreductase transcripts were strongly induced, most prominent CYP1A1, known to be regulated via the aryl hydrocarbon receptor pathway. An XRE-dependent reporter gene assay confirmed the AhR-agonistic activity of the Leuzea root extract, whereas 20-hydroxyecdysone was not active. Leuzea extract also inhibited 5alpha-reductase, type II. While the extract significantly modulates cellular activities, the phytoecdysteroids, are most likely not the active principles of L. carthamoides.
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Extracts from Rhaponticum carthamoides show antibacterial, cytotoxic, anti-adipogenic, and antioxidant activities.
“Extracts from R. carthamoides show a variety of activities, including antibacterial, cytotoxic, anti-adipogenic, and antioxidant [69,121,122,123,124,125,126,127,128,129,130,131,132].”
From Ecdysterone and Turkesterone—Compounds with Prominent Potential in Sport and Healthy Nutrition (2024) · cites this paper as [126]
Investigations into Rhaponticum carthamoides revealed that its extracts are low in toxicity.
“The investigations into R. carthamoides revealed that its extracts are low in toxicity [69,121,122,123,124,125,126,127,128,129,130,131,132].”
From Ecdysterone and Turkesterone—Compounds with Prominent Potential in Sport and Healthy Nutrition (2024) · cites this paper as [126]
A lipophilic Leuzea root extract containing the major phytoecdysteroid 20-HE demonstrated potent cytotoxic effects on MCF-7 cells with IC50 30 μg/mL, yet 20-HE alone was not as effective.
“A lipophilic Leuzea root extract containing the major PE 20-HE demonstrated potent cytotoxic effects on MCF-7 cells. The extract exhibitied cell proliferation with IC50 30 μg/mL, yet 20-HE alone was not as effective171.”
From The Phytochemical, Biological, and Medicinal Attributes of Phytoecdysteroids: An Updated Review (2021) · cites this paper as [171]
The anticancer effects of a lipophilic Leuzea root extract containing 20-HE were mediated via gene regulation in an antiproliferative manner through downregulation of CCNE2, FOXM1, GTSE1, and PCNA and induced expression of CCNG2, GADD45α, and TP53INP1, pointing to cell cycle arrest at the G1/S transition checkpoint in MCF-7 cells.
“The anticancer effects of a lipophilic Leuzea root extract containing 20-HE was found to be medated via gene regulation in an antiproliferative manner through downregulation of cyclin E2 (CCNE2), forkhead box M1 (FOXM1), G-2 and S-phase expressed 1 (GTSE1), proliferating cell nuclear antigen (PCNA), induced expression of cyclin G2 (CCNG2), growth arrest and DNA-damage-inducible, alpha (GADD45α)”
From The Phytochemical, Biological, and Medicinal Attributes of Phytoecdysteroids: An Updated Review (2021) · cites this paper as [171]
Approximately thirty genes associated with DNA replication and synthesis appeared downregulated by Leuzea extract, indicating that reduced replication rate and cell cycle arrest at the G1/S transition checkpoint is more specific than the molecule mechanism in MCF-7 cells.
“In addition, approximately thirty genes associated with DNA replication and synthesis appeared to be downregulated by the extract, which indicated that reduced replication rate and cell cycle arrest at the G1/S-transition checkpoint is more specific than the molecule mechanism in MCF-7 cells171.”
From The Phytochemical, Biological, and Medicinal Attributes of Phytoecdysteroids: An Updated Review (2021) · cites this paper as [171]
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References 19 · Cited by 14
- Authors
- Gaube, F., Wölfl, S., Pusch, L., Werner, U., Kroll, T., Schrenk, D., Hartmann, R., & Hamburger, M.
- Affiliations
- Friedrich Schiller University Jena (DE)
- Heidelberg University (DE)
- University of Kaiserslautern (DE)
- Saarland University (DE)
- University of Basel (CH)
- Venue
- Planta Medica
- Publisher
- Georg Thieme Verlag KG
- Published
- 2008-10-29
- Volume
- 74
- Issue
- 14
- Pages
- 1701-1708
- ISSN
- 0032-0943 (ISSN-L)
- 1439-0221
- OpenAlex
- W1997876148
- Cited by
- 14
- References
- 19
- Citations by year
- 2025: 2 · 2024: 1 · 2023: 1 · 2020: 1 · 2019: 1 · 2018: 2 · 2017: 2 · 2013: 1
- FWCI
- 0.41
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Planta Medica (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Phytochemical Studies and Bioactivities
- Life Sciences › Agricultural and Biological Sciences › Plant Science › Medicinal Plant Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Medicinal Plants and Bioactive Compounds
- Keywords
- Leuzea carthamoides, 20-hydroxyecdysone, phytoecdysteroids, breast adenocarcinoma, MCF-7 cells, cell proliferation inhibition, apoptosis, cell cycle regulation, DNA replication, CYP1A1, aryl hydrocarbon receptor, gene expression profiling, dietary supplements, anti-aging products
- MeSH terms
- Adenocarcinoma, Breast Neoplasms, Female, Humans, Plant Extracts, Gene Expression Regulation, Neoplastic, Genome, Plant Roots, Gene Expression Profiling, Leuzea, Cell Line, Tumor, Cell Proliferation
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