Exp Mol Med.  2005 Apr;37(2):111-120.

Antitumor activity of spinasterol isolated from Pueraria roots

• Jeon GC
• Park MS
• Yoon DY
• Shin CH
• Sin HS
• Um SJ

Abstract

We purified phytoestrogens from Pueraria root (Pueraria mirifica from Thailand and Pueraria lobata from Korea), which is used as a rejuvenating folk medicine in Thailand and China. Dried, powdered plant material was extracted with 100% ethanol and further separated by concentration, filtration, and thin layer silica gel chromatography. Using the fractions obtained during separation, we first investigated their cytotoxicity in several cancer cell lines from various tissues. The ethanol-extracted components (PE1, PE4) had significant antiproliferative effects on breast cancer cell lines, including MCF-7, ZR-75-1, MDA-MB-231, SK-BR-3, and Hs578T. Second, we compared these results with the cytotoxic effects of known flavonoids, sterols, and coumarins from Pueraria root. The known compounds were not as effective, and occurred in a different polarity region on HPLC. Third, further separation resulted in the isolation of eight different components (Sub PE-A to -H). One of these, PE-D, affected the growth of some breast cancer cell lines (MCF-7, MDA-MB-231) in a dose- and time-dependent manner, as well as the growth of ovarian (2774) and cervical cancer cells (HeLa). Finally, a transfection assay showed that this component had an estrogenic effect similar to 17beta-estradiol, which activates both estrogen receptor a (ER alpha) and ER beta. The NMR analysis determined that spinasterol (stigmasta-7, 22-dien-3beta-ol) is an active cytotoxic component of Pueraria root.

Keyword

breast neoplasms; estrogen replacement; phytoestrogens; pueraria; receptors; estrogen; spinasterol; therapy

MeSH Terms

Antineoplastic Agents/isolation & purification/*pharmacology
Chromatography, High Pressure Liquid
Estrogen Receptor alpha/agonists
Estrogen Receptor beta/agonists
Female
Humans
Plant Preparations/therapeutic use
Plant Roots/*chemistry
Pueraria/*chemistry
Research Support, Non-U.S. Gov't
Stigmasterol/*analogs & derivatives/isolation & purification/pharmacology
Transfection
Tumor Cells, Cultured