Abstract
Pharmacokinetic and metabolism studies of 12-riboside-pseudoginsengenin DQ (RPDQ), a novel ginsenoside with an anti-cancer effect, were carried out, aiming at discussing the characteristics of the ginsenoside with glycosylation site at C-12. In the pharmacokinetic analysis, we developed and validated a method by UPLC-MS to quantify RPDQ in rat plasma. In the range of 5–1000 ng/mL, the assay was linear (R2 > 0.9966), with the LLOQ (lower limit of quantification) being 5 ng/mL. The LOD (limit of detection) was 1.5 ng/mL. The deviations of intra-day and inter-day, expressed as relative standard deviation (RSD), were ≤ 3.51% and ≤ 5.41% respectively. The accuracy, expressed as relative error (RE), was in the range –8.82~3.47% and –5.61~2.87%, respectively. The recoveries were in the range 85.66~92.90%. The method was then applied to a pharmacokinetic study in rats intragastrically administrated with 6, 12, and 24 mg/kg RPDQ. The results showed that RPDQ exhibited slow oral absorption (Tmax = 7.0 h, 7.5 h, and 7.0 h, respectively), low elimination (t1/2 = 12.59 h, 12.83 h, and 13.74 h, respectively) and poor absolute bioavailability (5.55, 5.15, and 6.08%, respectively). Moreover, the investigation of metabolites were carried out by UPLC-QTOF-MS. Thirteen metabolites of RPDQ were characterized from plasma, bile, urine, and feces of rats. Some metabolic pathways, including oxidation, acetylation, hydration, reduction, hydroxylation, glycine conjugation, sulfation, phosphorylation, glucuronidation, glutathione conjugation, and deglycosylation, were profiled. In general, both the rapid quantitative method and a good understanding of the characteristics of RPDQ in vivo were provided in this study.
Highlights
Ginseng, a traditional Chinese medicine, has been widely used
To determine the fragmentation patterns, the reference compound of riboside-pseudoginsengenin DQ (RPDQ) was used for the major
In spite of lacking standards for the for the metabolites, the structures of them could be estimated based on retention time and mass metabolites, the structures of them could be estimated based on retention time and mass spectral patterns spectral patterns between RPDQ and its product ions
Summary
A traditional Chinese medicine, has been widely used. Ginsenosides are the main active ingredient [1,2]. According to the skeleton of sapogenin, ginsenosides can be divided into tetracyclic and pentacyclic triterpene types [3,4] The former type could be divided into dammarane-subtype and ocotillol-subtype saponins [5]. It is worth mentioning that ocotillol-type saponin (20, 24-epoxyside) has many high activities such as neuroprotective, antiinflammatory, antibacterial, and antitumor effect [6,7,8,9]. The discovery of this type showed that the natural ones were mainly existed in American ginseng, Vietnam ginseng, or Panax japonicas [10,11,12]. The semisynthesis has been receiving more and more attention aiming to increase the yields or obtain the novel ocotillol-type saponin [13,14,15,16]
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