Withanolide sulfoxide from Aswagandha roots inhibits nuclear transcription factor‐kappa‐B, cyclooxygenase and tumor cell proliferation

• DOI: 10.1002/ptr.2736
• Publication Date: 2009-01-16T12:17:42Z
• Authors: Vanisree Mulabagal; Gottumukkala V. S...; Chirravuri V. Rao; Chillara Sivarama...; David L. DeWitt; Daniel Holmes; Bokyung Sung; Bharat B. Aggarwal; Hsin‐Sheng Tsay; Muraleedharan G. ...
• Keywords: Withanolide; Sulfoxide

Investigation of the methanol extract Aswagandha (Withania somnifera) roots for bioactive constituents yielded a novel withanolide sulfoxide compound (1) along with known dimer ashwagandhanolide (2) an S-linkage. The structure 1 was established by extensive NMR and MS experiments. Compound highly selective in inhibiting cyclooxygenase-2 (COX-2) enzyme 60% at 100 microm no activity against COX-1 enzyme. IC(50) values human gastric (AGS), breast (MCF-7), central nervous system (SF-268) colon (HCT-116) cancer cell lines were range 0.74-3.63 microm. Both S-containing dimeric withanolides, 2, completely suppressed TNF-induced NF-kappaB activation when tested isolation from W. somnifera its ability to inhibit COX-2 suppress tumor proliferation are reported here first time. In addition, this is report on abrogation compounds 2.