2024-03-28T19:39:18Zhttp://digital.csic.es/dspace-oai/requestoai:digital.csic.es:10261/1213412021-12-27T16:26:19Zcom_10261_86com_10261_1col_10261_339
urn:hdl:10261/121341
Cytotoxic activity and chemical composition of the root extract from the mexican species Linum scabrellum: mechanism of action of the active compound 6-Methoxypodophyllotoxin
Alejandre-García, Ivonne
Álvarez, Laura
Cardoso-Taketa, Alexandre
González-Maya, Leticia
Antúnez-Mojica, Mayra
Salas-Vidal, Enrique
Díaz, José Fernando
Marquina-Bahena, Silvia
Villarreal, María Luisa
12 p.-6 fig.-1 tab.
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.
2015
artículo
Evid Based Complement Alternat Med.: :298463 (2015)
1741-427X
http://hdl.handle.net/10261/121341
10.1155/2015/298463
1741-4288
26246833
eng
Publisher's version
http://dx.doi.org/10.1155/2015/298463
Sí
http://creativecommons.org/licenses/by-nc-sa/3.0)
openAccess
Hindawi Publishing Corporation