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Comparative pharmacokinetics of bergenin, a main active constituent of Saxifraga stolonifera Curt., in normal and hepatic injury rats after oral administration.

Abstract Bergenin, isolated from the herb of Saxifrage stolonifera Curt. (Hu-Er-Cao) has hepatoprotective, anti-inflammatory, antitussive, and neuroprotective activities. The aim of the present study was to establish a simple, rapid, and sensitive RP-HPLC method for determination of bergenin in rat plasma and compare its oral pharmacokinetic behaviors in normal and CCl4-induced hepatic injury rats. With norisoboldine as an internal standard, chromatographic separation was performed on a C18 analytical column with acetonitrile and water (11 : 89, V/V) containing 0.1% formic acid as the mobile phase. A good linearity was obtained over the range of 100-10 000 ng·mL(-1). The lower limit of quantification was 50 ng·mL(-1). The developed method was successfully applied to a study of the pharmacokinetic difference of bergenin (100 mg·kg(-1)) between normal and hepatic injury rats after oral administration. Marked alterations of pharmacokinetic parameters in hepatic injury rats were observed. Compared to normal rats, the AUC(0-∞) of bergenin in hepatic injury rats was elevated to 2.11-fold and Cmax was increased by 130%, whereas CL value was only 55% of the normal rats, suggesting that the systemic exposure of bergenin was significantly increased under hepatic injury status.
PMID
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Authors

Mayor MeshTerms
Keywords

Bergenin

HPLC

Hepatic injury

Pharmacokinetic

Saxifrage stolonifera Curt

Journal Title chinese journal of natural medicines
Publication Year Start




PMID- 28236407
OWN - NLM
STAT- MEDLINE
DA  - 20170225
DCOM- 20170303
LR  - 20170303
IS  - 1875-5364 (Electronic)
IS  - 1875-5364 (Linking)
VI  - 14
IP  - 10
DP  - 2016 Oct
TI  - Comparative pharmacokinetics of bergenin, a main active constituent of Saxifraga 
      stolonifera Curt., in normal and hepatic injury rats after oral administration.
PG  - 776-782
LID - S1875-5364(16)30092-9 [pii]
LID - 10.1016/S1875-5364(16)30092-9 [doi]
AB  - Bergenin, isolated from the herb of Saxifrage stolonifera Curt. (Hu-Er-Cao) has
      hepatoprotective, anti-inflammatory, antitussive, and neuroprotective activities.
      The aim of the present study was to establish a simple, rapid, and sensitive
      RP-HPLC method for determination of bergenin in rat plasma and compare its oral
      pharmacokinetic behaviors in normal and CCl4-induced hepatic injury rats. With
      norisoboldine as an internal standard, chromatographic separation was performed
      on a C18 analytical column with acetonitrile and water (11 : 89, V/V) containing 
      0.1% formic acid as the mobile phase. A good linearity was obtained over the
      range of 100-10 000 ng.mL-1. The lower limit of quantification was 50 ng.mL-1.
      The developed method was successfully applied to a study of the pharmacokinetic
      difference of bergenin (100 mg.kg-1) between normal and hepatic injury rats after
      oral administration. Marked alterations of pharmacokinetic parameters in hepatic 
      injury rats were observed. Compared to normal rats, the AUC(0-infinity) of
      bergenin in hepatic injury rats was elevated to 2.11-fold and Cmax was increased 
      by 130%, whereas CL value was only 55% of the normal rats, suggesting that the
      systemic exposure of bergenin was significantly increased under hepatic injury
      status.
CI  - Copyright (c) 2016 China Pharmaceutical University. Published by Elsevier B.V.
      All rights reserved.
FAU - Pan, Rong-Hua
AU  - Pan RH
AD  - The Chinese Traditional Medical Hospital of Liyang City, Liyang 213300, China.
FAU - He, Hong-Mei
AU  - He HM
AD  - Department of Chinese Materia Medica Analysis, China Pharmaceutical University,
      Nanjing 210009, China.
FAU - Dai, Yue
AU  - Dai Y
AD  - Department of Pharmacology of Chinese Materia Medica, China Pharmaceutical
      University, Nanjing 210009, China.
FAU - Xia, Yu-Feng
AU  - Xia YF
AD  - Department of Chinese Materia Medica Analysis, China Pharmaceutical University,
      Nanjing 210009, China. Electronic address: [email protected]
LA  - eng
PT  - Comparative Study
PT  - Journal Article
DEP - 20161031
PL  - China
TA  - Chin J Nat Med
JT  - Chinese journal of natural medicines
JID - 101504416
RN  - 0 (Benzopyrans)
RN  - 0 (Drugs, Chinese Herbal)
RN  - CL2T97X0V0 (Carbon Tetrachloride)
RN  - L84RBE4IDC (bergenin)
SB  - IM
MH  - Animals
MH  - Benzopyrans/administration & dosage/*pharmacokinetics
MH  - Carbon Tetrachloride
MH  - Chemical and Drug Induced Liver Injury/*drug therapy
MH  - Chromatography, High Pressure Liquid
MH  - Chromatography, Liquid
MH  - Drugs, Chinese Herbal/administration & dosage/*pharmacokinetics
MH  - Humans
MH  - Male
MH  - Rats
MH  - Rats, Sprague-Dawley
MH  - Saxifragaceae/*chemistry
MH  - Tandem Mass Spectrometry/methods
OTO - NOTNLM
OT  - *Bergenin
OT  - *HPLC
OT  - *Hepatic injury
OT  - *Pharmacokinetic
OT  - *Saxifrage stolonifera Curt
EDAT- 2017/02/27 06:00
MHDA- 2017/03/04 06:00
CRDT- 2017/02/26 06:00
PHST- 2015/10/17 [received]
AID - S1875-5364(16)30092-9 [pii]
AID - 10.1016/S1875-5364(16)30092-9 [doi]
PST - ppublish
SO  - Chin J Nat Med. 2016 Oct;14(10):776-782. doi: 10.1016/S1875-5364(16)30092-9. Epub
      2016 Oct 31.

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