Structural identification of neopanaxadiol metabolites in rats by ultraperformance liquid chromatography/quadrupole-time-of-flight mass spectrometry

Geng, C.; Yin, Jianyuan; Yu, Xiuhua; Yang, Yongqiang; Liu, Jingyan; Sun, Dandan; Chen, Fanbo; Wei, Zhonglin; Qin, Meng; Liu, Jihua

doi:10.1002/rcm.7107

Cited by 6 publications

(7 citation statements)

References 38 publications

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“…Low solubility of deglycosylated product, poor membrane permeability and extensive metabolism in the gastrointestinal tract limit the absorption of ginsenosides (Geng etal. , ; Qi, Wang, & Yuan, ; Tawab, Bahr, Karas, Wurglics, & Schubert‐zsilavecz, ). Changing the pharmaceutical formulation may improve bioavailability.…”

Section: Discussionmentioning

confidence: 99%

“…Our preliminary PK study of ocotillol type ginsenosides after oral intake also pointed out that they have low plasma exposure and poor absorption into blood. Low solubility of deglycosylated product, poor membrane permeability and extensive metabolism in the gastrointestinal tract limit the absorption of ginsenosides (Geng et al, 2015;Qi, Wang, & Yuan, 2011;Tawab, Bahr, Karas, Wurglics, & Schubert-zsilavecz, 2003 effect in vivo than intact PPD (Han, Chen, Chen, & Wang, 2010).…”

Section: Discussionmentioning

confidence: 99%

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Development and validation of an UPLC‐Q/TOF‐MS assay for the quantitation of neopanaxadiol in beagle dog plasma: Application to a pharmacokinetic study

Geng

Wang

et al. 2016

Biomedical Chromatography

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Neopanaxadiol (NPD), the main panaxadiol constituent of Panax ginseng C. A. Meyer (Araliaceae), has been regarded as the active component for the treatment of Alzheimer's disease. However, few references are available about pharmacokinetic evaluation for NPD. Accordingly, a rapid and sensitive method for quantitative analysis of NPD in beagle dog plasma based on ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry was developed and validated. Analytes were extracted from plasma by liquid-liquid extraction and chromatographic separation was achieved on an Agilent Zorbax Stable Bond C column. Detection was performed in the positive ion mode using multiple reaction monitoring of the transitions both at m/z 461.4 → 425.4 for NPD and internal standard of panaxadiol. All validation parameters, such as lower limit of quantitation, linearity, specificity, precision, accuracy, extraction recovery, matrix effect and stability, were within acceptable ranges and the method was appropriate for multitude sample determination. After oral intake, NPD was slowly absorbed and eliminated from circulatory blood system and corresponding plasma exposure was low. Application of this quantitative method will yield the first pharmacokinetic profile after oral administration of NPD to beagle dog. The information obtained here will be useful to understand the pharmacological effects of NPD.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Development and validation of an UPLC‐Q/TOF‐MS assay for the quantitation of neopanaxadiol in beagle dog plasma: Application to a pharmacokinetic study

Geng

Wang

et al. 2016

Biomedical Chromatography

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“…Rg 5 , the principal component in steamed American ginseng, was also transformed to Rh 3 by human intestinal microflora [23]. Additionally, systematic metabolic behaviors of aglycon were further investigated and epoxidation metabolite was identified as the main metabolic pathway of protopanaxadiol [24,25], NPD [26], and protopanaxatriol [27] in rats. Accordingly, to investigate the detailed reason for low oral bioavailability, the metabolic routes of ocotillol type ginsenosides need to be explored in the near future.…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetic Characterizations of Ginsenoside Ocotillol, RT<sub>5</sub> and F<sub>11</sub>, the Promising Agents for Alzheimer’s Disease from American Ginseng, in Rats and Beagle Dogs

et al. 2019

Pharmacology

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Background: Ocotillol, RT₅ and F₁₁, the main active components of ocotillol type ginsenosides, have attracted a lot of attention due to their beneficial effects on neurodegenerative disease models of Alzheimer’s disease. Pharmacokinetic (PK) is a bridge linking the herbal medicines and their pharmacological responses. However, few data are available regarding PK behaviors of ocotillol type ginsenosides. Methods: The liquid chromatography-tandem mass spectrometry methods were developed and validated to calculate the concentrations of 3 ginsenosides in different biological matrices. Rat and beagle dog plasma samples were deproteinized with methanol and separated on Shim-pack GIST C₁₈ column. All of the analytes were detected in positive ion mode using multiple reaction monitoring. Results: The methods showed good linearity (r > 0.996) in the established concentration range. All validated data, such as specificity, intra- and inter-day precision, accuracy, extraction recovery, matrix effect, and stability were within required limits. The values of C_max and AUC_(0–t) indicated ocotillol type ginsenosides had low systemic exposure and poor absorption into blood. T_1/2 and MRT_(0–t) demonstrated the elimination process of ocotillol type ginsenosides might be slow. Double peaks were observed in the mean plasma concentration versus time profiles of ocotillol, RT₅, and F₁₁ after oral intake. Conclusions: This was the first PK investigation of the ocotillol type ginsenosides in rats and beagle dogs. The results we found here were helpful to our understanding of the absorption mechanism of ocotillol type ginsenosides and provided the scientific basis for further pre-clinical research.

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“…For screening ginsenosides in GD, a customized library was set up and imported to UNIFI 1.8 software (Waters, Milford, MA, USA) containing 118 ginsenosides based on references 27–42 . The library contains most of the isolated and semisynthesized ginsenosides reported in recent years.…”

Section: Methodsmentioning

confidence: 99%

Different absorption and metabolism of ginsenosides after the administration of total ginsenosides and decoction of Panax ginseng

Liu

Wang

et al. 2020

Rapid Comm Mass Spectrometry

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Rationale: Panax ginseng C.A. Meyer (PG), which contains polysaccharides and ginsenosides as the major bioactive components, has been used to promote health and treat diseases for thousands of years in China. Total ginsenosides were extracted from a decoction of Panax ginseng (GD), which included both ginsenosides and polysaccharides, and dissolved in water to obtain a total ginsenosides aqueous solution (TGAS). To study their absorption and metabolism, the pharmacokinetics (PK) and metabolites of ginsenosides in vivo were investigated after the administration of GD and TGAS.Methods: Rat and mice plasma samples were collected after the administration of GD and TGAS. Ultra-performance liquid chromatography coupled with time-of-flight mass spectrometry was used with the UNIFI platform to identify metabolites in the plasma sample. The pharmacokinetic parameters were calculated using a noncompartmental method in the Drug and Statistics software package.Results: Thirty ginsenoside metabolites were identified in mice plasma, of which only seven were found in the rat plasma after the administration of GD. The PK of ginsenosides Rb 1 , Rc, and Rd were also determined after the oral administration of GD and TGAS and showed significant differences in the pharmacokinetic parameters.Conclusions: There was no difference in the biotransformation pathways after the oral administration of GD and TGAS, indicating that there was no influence of polysaccharides on the biotransformation of ginsenosides in vivo. However, the pharmacokinetic parameters were different after the administration of GD and TGAS, possibly because of the polysaccharides in GD. This study should be of significance in exploring the basis of PG bioactivities and lays the foundation for the further development of new drugs using PG.

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Structural identification of neopanaxadiol metabolites in rats by ultraperformance liquid chromatography/quadrupole-time-of-flight mass spectrometry

Cited by 6 publications

References 38 publications

Development and validation of an UPLC‐Q/TOF‐MS assay for the quantitation of neopanaxadiol in beagle dog plasma: Application to a pharmacokinetic study

Development and validation of an UPLC‐Q/TOF‐MS assay for the quantitation of neopanaxadiol in beagle dog plasma: Application to a pharmacokinetic study

Pharmacokinetic Characterizations of Ginsenoside Ocotillol, RT<sub>5</sub> and F<sub>11</sub>, the Promising Agents for Alzheimer’s Disease from American Ginseng, in Rats and Beagle Dogs

Different absorption and metabolism of ginsenosides after the administration of total ginsenosides and decoction of Panax ginseng

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