Withania somnifera (L.) Dunal, shows several pharmacological properties which are attributed mainly to the
withanolides present in the root. The efficacy of medicinally active
withanolides constituents depends on the absorption and transportation through the intestinal epithelium. We examined these characteristics by employing the Sino-Veda Madin-Darby canine kidney cells culture system, which under in vitro condition shows the absorption characteristics similar to the human intestinal epithelium. Thus, the aim of the present investigation was to assess the bioavailability of individual
withanolides.
Withanolides were diluted in Hank's buffered saline at a concentration of 2 μg/ml were tested for permeability studies carried out for 1 h duration. Permeability was measured in terms of efflux pump (P eff) in cm/s. P eff values of
withanolide A (WN A),
withanone (WNN), 1,2-deoxywithastramonolide (1,2 DWM),
withanolide B (WN B),
withanoside IV-V (WS IV-V), and
withaferin A were 4.05 × 10(-5), 2.06 × 10(-5), 1.97 × 10(-5), 1.80 × 10(-5), 3.19 × 10(-6), 3.03 × 10(-6) and 3.30 × 10(-7) respectively. In conclusion, the nonpolar and low molecular weight compounds (WN A, WNN, 1,2 DWM, and WN B) were highly permeable. As against this, the glycosylated and polar WS IV and WS V showed low permeability. Surprisingly and paradoxically, the highly biologically active
withaferin A was completely impermeable, suggesting that further studies possibly using human epithelial colorectal
adenocarcinoma (Caco-2) cells may be needed to delineate the absorption characteristics of
withanolides, especially
withaferin A.