Untitled

Abstract

A sheep was dosed three times per day over six consecutive days with 70 g Narthecium ossifragum, and once on the seventh day with 70 g N. ossifragum. Additionally, it was dosed once on days 1-7 with 20 mg of [20,23,23-2H3]sarsasapogenin. After 7 days, the sheep was killed and GC-MS analysis of the free and conjugated sapogenin content in bile, urine, rumen, duodenum, jejunum, colon and rectum samples collected from the sheep, faecal samples collected on days 4-7, and dosed plant material was performed. The N. ossifragum contained mainly sarsasapogenin and smilagenin. Only neglible levels of deuterium-labelled sarsasapogenins were detected in the samples from the animal. Ingested saponins were quickly hydrolysed in the rumen to free sapogenins and, in part, epimerized at C-3 to afford episapogenins. The absorption of free sapogenins appeared to occur in the jejunum. The concentration of sapogenins in faeces reached a plateau 108 h after dosing started.

Ovine Metabolism of Lithogenic Sapogenins. Synthesis of [2,2,4,4-2H4]Sarsasapogenone, [2,2,4,4-2H4]Sarsasapogenin, and [2,2,4,4-2H4]Episarsasapogenin and Evaluation of Deuterium Retention in a Sheep-Dosing Trial

“…Because only a single sheep was dosed in the trials reported in this paper, care must be exercised when the results presented in Tables and 2 are interpreted. The results are, however, consistent with levels of free and conjugated sapogenins and episapogenins detected in previous dosing trials ( , ). Prior to the use of the methodology in a field trial, there is a need to validate the methodology in a multiple-sheep trial (e.g., n = 3) in which the deuterated subtrate is dosed over an extended time period.…”

“…Reduction of 1b using sodium borohydride afforded a 1:4 mixture of [2,2,4,4- 2 H 4 ]sarsasapogenin ( 2b ) and [2,2,4,4- 2 H 4 ]episarsasapogenin ( 3b ). The relative contributions of the deuterated genins 2b and 3b in the synthetic mixture are comparable to those of the natural genins 2a and 3a detected in fecal samples following the dosing, in previous trials, of N. ossifragum plant material ( , ). Complete 1 H and 13 C NMR assignments (see Supporting Information) of 1b , 2b , and 3b were derived from detailed analyses of one- and two-dimensional NMR spectral data, including COSY, TOCSY, ROESY, g-HSQC, and g-HMBC spectra.…”

“…During the present and previous dosing trials ( , ) we have observed (but not reported or discussed) that ruminal metabolism of β-sitosterol (a constituent of many plants grazed by animals) affords three isomeric dihydroanalogues of β-sitosterol, which, when acetylated, exhibit significant m / z 458 (M + ) and m / z 315 ions. The GC-MS retention times of two of the three dihydro-β-sitosterol acetate isomers detected in the extracts are similar to those of sarsasapogenin and episarsasapogenin acetates; however, provided care was taken to adjust GC-MS acquisition conditions to minimize peak overlap, interference was not significant.…”

“…Dosing Trial Results. Previous investigations have shown that in the rumen of a dosed sheep sapogenins are partly oxidized and reduced to afford episapogenins, which, along with sapogenins and low levels of oxidized sapogenins, are ultimately secreted in fecal material but not in urine ( , ). Fecal samples were collected daily before and during the trial period.…”

The bioavailability of red ginseng extract fermented by Phellinus linteus

“…Investigations of bacterial fermentation have shown that the intestinal degradation of PPD ginsenosides proceeds stepwise via the cleavage of sugar moieties, mainly liberating the monoglycosylated ginsenoside CK [10,41]. However, these intestinal microfloras are very changeable depending on host conditions (such as diet, health, and even stress) [42,43]. Therefore, it is hypothesized that individual differences in ginseng efficacy may be partially associated with the intestinal microflora of patients.…”