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Cytotoxic Activity and Chemical Composition of the Root Extract from the Mexican Species Linum scabrellum: Mechanism of Action of the Active Compound 6-Methoxypodophyllotoxin
Joint Authors
Alejandre-García, Ivonne
Álvarez, Laura
Cardoso-Taketa, Alexandre
González-Maya, Leticia
Antúnez, Mayra
Salas-Vidal, Enrique
Marquina-Bahena, Silvia
Villarreal, María Luisa
Diaz, J. Fernando
Source
Evidence-Based Complementary and Alternative Medicine
Issue
Vol. 2015, Issue 2015 (31 Dec. 2015), pp.1-11, 11 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2015-07-12
Country of Publication
Egypt
No. of Pages
11
Main Subjects
Abstract EN
The cytotoxic activity and the chemical composition of the dichloromethane/methanol root extract of Linum scabrellum Planchon (Linaceae) were analyzed.
Using NMR spectra and mass spectrometry analyses of the extract we identified eight main constituents: oleic acid (1), octadecenoic acid (2), stigmasterol (3), α-amyrin (4), pinoresinol (5), 6 methoxypodophyllotoxin (6), coniferin (7), and 6-methoxypodophyllotoxin-7-O-β-D-glucopyranoside (8).
By using the sulforhodamine B assay, an important cytotoxic activity against four human cancer cell lines, HF6 colon (IC50 = 0.57 μg/mL), MCF7 breast (IC50 = 0.56 μg/mL), PC3 prostate (IC50 = 1.60 μg/mL), and SiHa cervical (IC50 = 1.54 μg/mL), as well as toward the normal fibroblasts line HFS-30 IC50 = 1.02 μg/mL was demonstrated.
Compound 6 (6-methoxypodophyllotoxin) was responsible for the cytotoxic activity exhibiting an IC50 value range of 0.0632 to 2.7433 µg/mL against the tested cell lines.
Cell cycle studies with compound 6 exhibited a cell arrest in G2/M of the prostate PC3 cancer cell line.
Microtubule disruption studies demonstrated that compound 6 inhibited the polymerization of tubulin through its binding to the colchicine site (binding constant K b = 7.6 × 10 6 M - 1 ).
A dose-response apoptotic effect was also observed.
This work constitutes the first investigation reporting the chemical composition of L.
scabrellum and the first study determining the mechanism of action of compound 6.
American Psychological Association (APA)
Alejandre-García, Ivonne& Álvarez, Laura& Cardoso-Taketa, Alexandre& González-Maya, Leticia& Antúnez, Mayra& Salas-Vidal, Enrique…[et al.]. 2015. Cytotoxic Activity and Chemical Composition of the Root Extract from the Mexican Species Linum scabrellum: Mechanism of Action of the Active Compound 6-Methoxypodophyllotoxin. Evidence-Based Complementary and Alternative Medicine،Vol. 2015, no. 2015, pp.1-11.
https://search.emarefa.net/detail/BIM-1061329
Modern Language Association (MLA)
Alejandre-García, Ivonne…[et al.]. Cytotoxic Activity and Chemical Composition of the Root Extract from the Mexican Species Linum scabrellum: Mechanism of Action of the Active Compound 6-Methoxypodophyllotoxin. Evidence-Based Complementary and Alternative Medicine No. 2015 (2015), pp.1-11.
https://search.emarefa.net/detail/BIM-1061329
American Medical Association (AMA)
Alejandre-García, Ivonne& Álvarez, Laura& Cardoso-Taketa, Alexandre& González-Maya, Leticia& Antúnez, Mayra& Salas-Vidal, Enrique…[et al.]. Cytotoxic Activity and Chemical Composition of the Root Extract from the Mexican Species Linum scabrellum: Mechanism of Action of the Active Compound 6-Methoxypodophyllotoxin. Evidence-Based Complementary and Alternative Medicine. 2015. Vol. 2015, no. 2015, pp.1-11.
https://search.emarefa.net/detail/BIM-1061329
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1061329