Effects of Ginseng Polysaccharides on the Metabolism of Ginsenoside Re in vivo and Transformation of Ginsenoside Re in vitro†

doi:10.7503/cjcu20180080

Abstract

Abstract:

To study the effect of ginseng polysaccharides on the absorption of ginsenoside Re metabolite into the blood and the transformation of ginsenoside Re by intestinal microflora in vitro, rapid resolution liquid chromatography coupled with quadruple-time-of-flight mass spectrometry(RRLC/Q-TOF-MS) was performed to investigate the biotransformation process of ginsenoside Re by intestinal microflora in media with and without ginseng polysaccharides, and the pharmacokinetics of the ginsenoside Re metabolite, ginsenoside Rg1, in rats with or without pretreatment with ginseng polysaccharides. For transformation of Re by rat intestinal microflora, five transformed products including ginsenoside Rg1, Rh1, Rg2, F1 and PPT, as well as three transformation pathways were identified. When the intestinal microbiota of rat feces was cultured in vitro, their ginsenoside Re biotransformation activities were significantly induced by ginseng polysaccharides. When ginsenoside Re was orally administered to rats, the peak time(t_max), the maximum plasma concentration(c_max) and area under the plasma drug concentration-time curve(AUC) for the main metabolite, ginsenoside Rg1, were (11.6±6.1) h, (80.1±44.0) ng/mL and (549.3±209.4) ng·h/mL, respectively. When ginsenoside Re was orally administered to rats fed ginseng polysaccharides, t_max, c_max and AUC for ginsenoside Rg1 were (8.2±5.4) h, (98.2±50.6) ng/mL and (691.9±231.2) ng·h/mL, respectively. The results show that ginseng polysaccharides may promote the metabolic conversion of ginsenoside Re to Rg1 and the subsequent absorption of Rg1 in the gastrointestinal tract and may potentiate the pharmacological effects of ginseng.

Key words: Ginsenoside Re, Ginsenoside Rg1, Biotransformation, Intestinal microflora, Pharmacokinetics

CLC Number:

O657

TrendMD:

LI Ruigang,ZHU Na,ZHAO Huanxi,WANG Nan,SUN Hongmei,YUE Hao,LI Jing. Effects of Ginseng Polysaccharides on the Metabolism of Ginsenoside Re in vivo and Transformation of Ginsenoside Re in vitro^†[J]. Chem. J. Chinese Universities, 2018, 39(10): 2192.

Figures/Tables 6

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No.	Compound	t_R/min	Molecula formula	M_w	[M+HCOO]^- measured value(mass accuracy<10^-6)	MS/MS fragment ions of [M+HCOO]^-(mass accuracy<10^-6)
1	Rg1	24.428	C₄₂H₇₂O₁₄	800.4922	845.4885	475.3781[M-H-Glc-Glc]^-, 637.4301[M-H-Glc]^-, 799.4799[M-H]^-, 845.4885[M+HCOO]^-
2	Rh1	41.425	C₃₆H₆₂O₉	638.4394	683.4354	475.3780[M-H-Glc]^-, 637.4382[M-H]^-, 683.4354 [M+HCOO]^-
3	Rg2	41.715	C₄₂H₇₂O₁₃	784.4973	829.4966	475.3779[M-H-Rha-Glc]^-, 637.4314[M-H-Rha]^-, 783.4918[M-H]^-, 829.4966[M+HCOO]^-,
4	F1	48.946	C₃₆H₆₂O₉	638.4394	683.4361	475.3783[M-H-Glc]^-, 637.4315[M-H]^-, 683.4361 [M+HCOO]^-
5	PPT	56.338	C₃₀H₅₂O₄	476.3866	521.3827	475.3798[M-H]^-, 521.3827[M+HCOO]^-

No.	Compound	t_R/min	Molecula formula	M_w	[M+HCOO]^- measured value(mass accuracy<10^-6)	MS/MS fragment ions of [M+HCOO]^-(mass accuracy<10^-6)
1	Rg1	24.428	C₄₂H₇₂O₁₄	800.4922	845.4885	475.3781[M-H-Glc-Glc]^-, 637.4301[M-H-Glc]^-, 799.4799[M-H]^-, 845.4885[M+HCOO]^-
2	Rh1	41.425	C₃₆H₆₂O₉	638.4394	683.4354	475.3780[M-H-Glc]^-, 637.4382[M-H]^-, 683.4354 [M+HCOO]^-
3	Rg2	41.715	C₄₂H₇₂O₁₃	784.4973	829.4966	475.3779[M-H-Rha-Glc]^-, 637.4314[M-H-Rha]^-, 783.4918[M-H]^-, 829.4966[M+HCOO]^-,
4	F1	48.946	C₃₆H₆₂O₉	638.4394	683.4361	475.3783[M-H-Glc]^-, 637.4315[M-H]^-, 683.4361 [M+HCOO]^-
5	PPT	56.338	C₃₀H₅₂O₄	476.3866	521.3827	475.3798[M-H]^-, 521.3827[M+HCOO]^-