Isolation and Characterization of Compounds with Anti-prostate Cancer Activity from Arctium lappa L. Using Bioactivity-guided Fractionation

Abstract

The methanolic extract of the seeds of Arctium lappa was found to show inhibitory activity against prostate cancer cell lines. Bioactivity-guided fractionation of a 95% ethanol extract from the seeds of A. lappa led to the isolation of seven compounds: β-sitosterol (1), daucosterol (2), lappaol C (3), lappaol A (4), and arctignan E (5), lappaol F (6), and arctiin (7). Their structures were elucidated by UV, IR, MS, and NMR data, as well as by comparison with those of the literature. Compounds 3–7 were studied for their cytotoxicity using a prostate cancer cell line. Compounds 3, 4, and 6 showed activity against the LNCaP prostate cancer cell line with IC₅₀ values of 8, 16, and 40 µg/mL, respectively.

Keywords::

• Arctium lappa
• β-sitosterol
• daucosterol
• lappaol C
• lappaol A
• and arctignan E. Lappaol F
• and arctiin
• anti-prostate cancer cell line